58 results on '"Mohammed Samim"'
Search Results
2. Synthesis, biological evaluation and theoretical studies of (E)-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibitors
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Farhat Ramzan, Syed Ayaz Nabi, Mehak Saba Lone, Alessandro Bonardi, Aabid Hamid, Sameena Bano, Kalicharan Sharma, Syed Shafi, Mohammed Samim, Kalim Javed, and Claudiu T. Supuran
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Human carbonic anhydrase ,benzenesulphonamide ,pyrrolone ,anticancer drugs ,enzyme inhibitors ,Therapeutics. Pharmacology ,RM1-950 - Abstract
A series of 20 newly designed (E)-1-(4-sulphamoylphenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones was synthesised and assessed as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors towards four human isoforms of pharmaceutical interest, that is, hCA I, II, IX and XII. The compounds displayed low to high nanomolar potency against all the isoforms. Introducing strong electron withdrawing groups at the para position of the arylidene ring increased the binding affinity to the enzyme. All compounds showed acceptable pharmacokinetic range and physicochemical characteristics as determined by computational ADMET analysis. Density Functional Theory (DFT) calculations of 3n were carried to gain understanding on the stability of the E and Z isomers. The energy values clearly indicate the stability of E isomer over Z isomer by −8.2 kJ mol−1. Our findings indicate that these molecules are useful as leads for discovering new CA inhibitors.
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- 2023
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3. Synthesis, Molecular Docking, and Biological Evaluation of a New Series of Benzothiazinones and Their Benzothiazinyl Acetate Derivatives as Anticancer Agents against MCF‑7 Human Breast Cancer Cells and as Anti-Inflammatory Agents
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Farhat Ramzan, Syed Ayaz Nabi, Mehak Saba Lone, Khalid Imtiyaz, Laraib Urooj, Vishakha Vishakha, Kalicharan Sharma, M. Moshahid A. Rizvi, Syed Shafi, Mohammed Samim, Sameena Bano, and Kalim Javed
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Chemistry ,QD1-999 - Published
- 2023
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4. Nanonization of Magnoflorine-Encapsulated Novel Chitosan–Collagen Nanocapsules for Neurodegenerative Diseases: In Vitro Evaluation
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Dar Junaid Bashir, Saliha Manzoor, Imran A. Khan, Masarat Bashir, Nidhi Bharal Agarwal, Shweta Rastogi, Indu Arora, and Mohammed Samim
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Chemistry ,QD1-999 - Published
- 2022
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5. Synthesis and Characterization of Zero-Valent Iron Nanoparticles, and the Study of Their Effect against the Degradation of DDT in Soil and Assessment of Their Toxicity against Collembola and Ostracods
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Bhanja Kishore Khuntia, Mohammad Faiyaz Anwar, Tanveer Alam, Mohammed Samim, Mithlesh Kumari, and Indu Arora
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Chemistry ,QD1-999 - Published
- 2019
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6. Neuroprotective Effect of Fisetin Through Suppression of IL-1R/TLR Axis and Apoptosis in Pentylenetetrazole-Induced Kindling in Mice
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Saima Khatoon, Nidhi Bharal Agarwal, Mohammed Samim, and Ozair Alam
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pentylenetetrazole ,fisetin ,interleukin ,toll like receptor-4 ,caspase-3 ,epilepsy ,Neurology. Diseases of the nervous system ,RC346-429 - Abstract
Epilepsy is a complex neurological disorder, characterized by frequent electrical activity in brain regions. Inflammation and apoptosis cascade activation are serious neurological sequelae during seizures. Fisetin (3, 3′,4′,7-tetrahydroxyflavone), a flavonoid molecule, is considered for its effective anti-inflammatory and anti-apoptotic properties. This study investigated the neuroprotective effect of fisetin on experimental epilepsy. For acute studies, increasing current electroshock (ICES) and pentylenetetrazole (PTZ)-induced seizure tests were performed to evaluate the antiseizure activity of fisetin. For the chronic study, the kindling model was established by the administration of PTZ in subconvulsive dose (25 mg/kg, i.p.). Mice were treated with fisetin (5, 10, and 20 mg/kg, p.o.) to study its probable antiseizure mechanism. The kindled mice were evaluated for seizure scores. Their hippocampus and cortex were assessed for neuronal damage, inflammation, and apoptosis. Histological alterations were observed in the hippocampus of the experimental mice. Levels of high mobility group box 1 (HMGB1), Toll-like receptor-4 (TLR-4), interleukin-1 receptor 1 (IL-1R1), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) were assessed in the hippocampus and cortex by ELISA. The immunoreactivity and mRNA expressions of nuclear factor-κB (NF-κB), cyclooxygenase-2 (COX-2), cytochrome C, and caspase-3 were quantified by immunohistochemical analysis and real-time PCR. Phosphorylation ELISA was performed to evaluate AkT/mTOR (mammalian target of rapamycin) activation in the hippocampus and cortex of the kindled mice. The results showed that fisetin administration increased the seizure threshold current (STC) in the ICES test. In PTZ-induced seizures, fisetin administration increased the latency for myoclonic jerks (MJs) and generalized seizures (GSs). In the PTZ-induced kindling model, fisetin administration dose-dependently suppressed the development of kindling and the associated neuronal damage in the experimental mice. Further, fisetin administration ameliorated kindling-induced neuroinflammation as evident from decreased levels of HMGB1, TLR-4, IL-1R1, IL-1β, IL-6, and TNF-α in the hippocampus and cortex of the kindled mice. Also, the immunoreactivity and mRNA expressions of inflammatory molecules, NF-κB, and COX-2 were decreased with fisetin administration in the kindled animals. Decreased phosphorylation of the AkT/mTOR pathway was reported with fisetin administration in the hippocampus and cortex of the kindled mice. The immunoreactivity and mRNA expressions of apoptotic molecules, cytochrome C, and caspase-3 were attenuated upon fisetin administration. The findings suggest that fisetin shows a neuroprotective effect by suppressing the release of inflammatory and apoptosis molecules and attenuating histological alterations during experimental epilepsy.
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- 2021
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7. Collagen Nanoparticle-Mediated Brain Silymarin Delivery: An Approach for Treating Cerebral Ischemia and Reperfusion-Induced Brain Injury
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Pankaj Rathore, Indu Arora, Shweta Rastogi, Mohd Akhtar, Shruti Singh, and Mohammed Samim
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ischemia ,reperfusion ,apoptosis ,stroke ,neuroprotection ,Neurosciences. Biological psychiatry. Neuropsychiatry ,RC321-571 - Abstract
Silymarin is a bioactive constituent isolated from milk thistle (Silybum marinum). Since its discovery, silymarin has been considered a gold standard drug in treating ailments related to the liver, resulting from alcohol consumption and viral hepatitis. This hepatoprotective nature of silymarin arises out of antioxidative and tissue-regenerating properties of silymarin. However, several recent studies have established the neuroprotective link of silymarin, too. Thus, the current investigation was aimed at exploring the neuroprotective effect of nanosilymarin (silymarin encapsulated inside collagen-based polymeric nanoparticulate drug delivery system). The study aimed at bringing out the role of nanoparticles in enhancing the therapeutic effect of silymarin against neuronal injury, originating out of oxidative-stress-related brain damages in focal cerebral ischemia. Collagen-based micellar nanoparticles were prepared and stabilized using 3-ethyl carbodiimide-hydrochloride (EDC-Hcl) and malondialdehyde (MDA) as crosslinkers. Nanoparticles were characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), and Fourier transform infrared (FT-IR) spectroscopy techniques, and the size of nanoparticles was found to be around 48 nm. Male albino Wistar rats were pretreated with three different doses of nanosilymarin of 10, 100, and 1,000 μg/kg b.wt and a dose of free silymarin of 100 mg/kg b.wt intraperitoneally (i.p.) for 7 days. Focal cerebral ischemia was induced using the middle cerebral artery occlusion (MCAO) model on the eighth day for 1 h followed by 24 h reperfusion. The animals were then evaluated for neurobehavioral, infarct analysis, biochemical, histopathological, and immunohistochemical studies. All the above parameters showed remarkable improvement in nanosilymarin-treated groups in comparison to the silymarin-treated group. Nanoparticle encapsulation of drug enhanced neuroprotection by increasing drug bioavailability and targeting. Thus, the present study concluded with satisfactory results, showing the critical role played by nanoparticles in improving the neuroprotection at very low drug doses.
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- 2020
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8. Hierarchically Grown NiO-Decorated Polyaniline-Reduced Graphene Oxide Composite for Ultrafast Sunlight-Driven Photocatalysis
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Preety Ahuja, Sanjeev Kumar Ujjain, Indu Arora, and Mohammed Samim
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Chemistry ,QD1-999 - Published
- 2018
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9. Isonicotinoyl-butanoic acid hydrazone derivatives as anti-tubercular agents: In-silico studies, synthesis, spectral characterization and biological evaluation
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Mehak Saba Lone, Mohamad Mosa Mubarak, Syed Ayaz Nabi, Farhat Ramzan Wani, Shaista Amin, Sayima Nabi, Hadiya Amin Kantroo, Mohammed Samim, Syed Shafi, Shamim Ahmad, Zahoor Ahmad, Syed Ovais Rizvi, and Kalim Javed
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Organic Chemistry ,General Pharmacology, Toxicology and Pharmaceutics - Published
- 2023
10. Design, synthesis and evaluation of 5-chloro-6-methylaurone derivatives as potential anti-cancer agents
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Mehak Saba Lone, Syed Ayaz Nabi, Farhat Ramzan Wani, Manika Garg, Shaista Amin, Mohammed Samim, Syed Shafi, Farah Khan, and Kalim Javed
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Structural Biology ,General Medicine ,Molecular Biology - Published
- 2023
11. Magnoflorine-Loaded Chitosan Collagen Nanocapsules Ameliorate Cognitive Deficit in Scopolamine-Induced Alzheimer’s Disease-like Conditions in a Rat Model by Downregulating IL-1β, IL-6, TNF-α, and Oxidative Stress and Upregulating Brain-Derived Neurotrophic Factor and DCX Expressions
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Dar Junaid Bashir, Saliha Manzoor, Mohd Sarfaraj, Shekh Mohammad Afzal, Masarat Bashir, null Nidhi, Shweta Rastogi, Indu Arora, and Mohammed Samim
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General Chemical Engineering ,General Chemistry - Published
- 2023
12. Fisetin provides neuroprotection in pentylenetetrazole-induced cognition impairment by upregulating CREB/BDNF
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Saima Khatoon, Mohammed Samim, Mansi Dahalia, and null Nidhi
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Pharmacology - Published
- 2023
13. Resveratrol-Loaded Glutathione-Coated Collagen Nanoparticles Attenuate Acute Seizures by Inhibiting HMGB1 and TLR-4 in the Hippocampus of Mice
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Mobin A. Siddiqui, Mohammad Asad, Juheb Akhter, Ubedul Hoda, Shweta Rastogi, Indu Arora, Nidhi B. Aggarwal, and Mohammed Samim
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Epilepsy ,Physiology ,Cognitive Neuroscience ,Cell Biology ,General Medicine ,Biochemistry ,Glutathione ,Hippocampus ,Toll-Like Receptor 4 ,Mice ,Resveratrol ,Seizures ,Animals ,Nanoparticles ,Pentylenetetrazole ,Anticonvulsants ,Collagen ,HMGB1 Protein - Abstract
Epilepsy is a relatively complicated neurological disorder that results in seizures. The use of resveratrol in treating seizures has been reported in recent studies. However, the low bioavailability of resveratrol and the difficulty of reaching the targeted location in the brain reduce its efficacy considerably. The side effects due to the higher concentration of drugs are another matter of concern. The purpose of the present study is to enhance the antiepileptic potential of resveratrol by delivering it to the brain's targeted location by encapsulating it in glutathione-coated collagen nanoparticles. The collagen nanoparticles increase the bioavailability of resveratrol, while the transport of resveratrol to its target location in the brain is facilitated by glutathione. By encapsulating resveratrol in glutathione-coated collagen nanoparticles, the concentration also substantially decreases. Resveratrol encapsulated in synthesized nanoparticles is referred to as nanoresveratrol. In the present study, nanoresveratrol effectiveness was studied through PTZ-induced seizures (PTZ-IS) and the increasing current electroshock (ICES) test. The efficacy of nanoresveratrol was further established using biochemical analysis, histopathological examinations, ELISA and real-time-PCR tests, and immunohistochemistry examination of the hippocampus of mice. Hence, this study is unique in the sense that it synthesized nanoresveratrol by using glutathione-coated collagen nanoparticles, followed by its application to treating seizures. On the basis of the study results, nanoresveratrol was found to be effective in preventing cognitive impairment in the mice and controlling epilepsy seizures to a greater extent than resveratrol. The proposed nanoformulation also reduces the concentration of resveratrol considerably. The present study results show that even 0.4 mg/kg of nanoresveratrol outperforms 40 mg/kg of resveratrol.
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- 2022
14. Impact of cardiovascular diseases on severity of COVID-19 patients: A systematic review
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Ram Bajpai, Pinki Mishra, Nidhi Bharal Agarwal, Rizwana Parveen, and Mohammed Samim
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medicine.medical_specialty ,business.industry ,COVID-19 ,General Medicine ,Disease ,Odds ratio ,030204 cardiovascular system & hematology ,RC666 ,medicine.disease ,Chronic liver disease ,03 medical and health sciences ,0302 clinical medicine ,Cardiovascular Diseases ,Internal medicine ,Meta-analysis ,Diabetes mellitus ,medicine ,Risk of mortality ,Humans ,Middle East respiratory syndrome ,030212 general & internal medicine ,business ,Kidney disease - Abstract
Introduction: Coronavirus disease 2019 (COVID-19) cases are increasing rapidly worldwide. Similar to Middle East respiratory syndrome where cardiovascular diseases were present in nearly 30% of cases, the increased presence of cardiovascular comorbidities remains true for COVID-19 as well. The mechanism of this association remains unclear at this time. Therefore, we reviewed the available literature and tried to find the probable association between cardiovascular disease with disease severity and mortality in COVID-19 patients. Methods: We searched Medline (via PubMed) and Cochrane Central Register of Controlled Trials for articles published until Sept 5, 2020. Nineteen articles were included involving 6,872 COVID-19 patients. Results: The random-effect meta-analysis showed that cardiovascular disease was significantly associated with severity and mortality for COVID-19: odds ratio (OR) 2.89, 95% confidence interval (CI) 1.98–4.21 for severity and OR 3.00, 95% CI 1.67–5.39 for mortality, respectively. Risk of COVID-19 severity was higher in patients having diabetes, hypertension, chronic obstructive pulmonary disease, malignancy, cerebrovascular disease and chronic kidney disease. Similarly, patients with diabetes, hypertension, chronic liver disease, cerebrovascular disease and chronic kidney disease were at higher risk of mortality. Conclusion: Our findings showed that cardiovascular disease has a negative effect on health status of COVID-19 patients. However, large prevalence studies demonstrating the consequences of comorbid cardiovascular disease are urgently needed to understand the extent of these concerning comorbidities. Keywords: Cardiovascular disease, COVID-19, SARS-CoV-2
- Published
- 2021
15. Bio-engineered palladium nanoparticles: model for risk assessment study of automotive particulate pollution on macrophage cell lines
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Mohammed Samim, Nidhi Bharal Agarwal, Manoj Pratap Singh, Saba Naqvi, and Aarzoo
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Chemistry ,General Chemical Engineering ,02 engineering and technology ,General Chemistry ,010501 environmental sciences ,021001 nanoscience & nanotechnology ,medicine.disease ,01 natural sciences ,Cell membrane ,medicine.anatomical_structure ,Cell culture ,Apoptosis ,In vivo ,Toxicity ,medicine ,Viability assay ,0210 nano-technology ,Cytotoxicity ,Cell damage ,0105 earth and related environmental sciences ,Nuclear chemistry - Abstract
The surge in vehicular activity in densely populated areas has led to an increased concentration of airborne palladium nanoparticles (PdNPs) in the environment. Recent toxicity data have indicated that PdNPs exhibit adverse effects in in vitro and in vivo models, however, their effect on the immune system is not fully understood. Therefore, in the present study, we aimed to evaluate possible toxic effects of bio-engineered palladium nanoparticles on the murine macrophage cell line (J774). Here we prepared palladium nanoparticles using aqueous leaf extract of Parthenium hysterophorus and characterized them by UV-Vis spectroscopy, XRD, FT-IR spectroscopy, HR-TEM, EDX, SEM and zeta potential. Toxicity parameters such as cell viability, cell membrane integrity, induction of apoptosis and ROS production were assessed on J774 cell lines. Spherical palladium nanoparticles of mean size ∼4 nm, when subjected to time and dose-dependent cytotoxicity assay, showed cell viability was >95% at lower doses (25, 200 μg mL−1) and
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- 2021
16. Targeted delivery of thermoresponsive polymeric nanoparticle-encapsulated lycopene:in vitroanticancer activity and chemopreventive effect on murine skin inflammation and tumorigenesis
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Sameena Bano, Faheem Ahmed, Mohammed Samim, Farha Khan, and Sandeep C. Chaudhary
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Antioxidant ,Chemistry ,General Chemical Engineering ,medicine.medical_treatment ,04 agricultural and veterinary sciences ,General Chemistry ,Pharmacology ,medicine.disease_cause ,040401 food science ,In vitro ,Lycopene ,Bioavailability ,03 medical and health sciences ,chemistry.chemical_compound ,0404 agricultural biotechnology ,0302 clinical medicine ,Apoptosis ,030220 oncology & carcinogenesis ,Lipophilicity ,medicine ,Tumor promotion ,Oxidative stress - Abstract
Naturally occurring lycopene has been reported for its chemopreventive and chemotherapeutic efficiency in various cancers, but its exceptional lipophilicity, poor aqueous solubility, instability, and consequently poor bioavailability limit its usage as a chemopreventive and chemotherapeutic agent. The present study aimed to synthesize co-polymeric nanoparticle-encapsulated formulations of commercial lycopene (NLY) and extracted lycopene (NLX) and evaluate their in vitro anticancer activity and inhibitory effect on 12-O-tetradecanoylphorbol-13-acetate (TPA)-promoted skin inflammation and tumorigenesis in Swiss albino mice. To prepare the nanoparticle-encapsulated formulations of lycopene, thermosensitive PNIPAAM–PEG-based co-polymeric nanoparticles were synthesized and characterized by FTIR spectroscopy, NMR spectroscopy, DLS, and TEM. Nanolycopene, unlike free lycopene, could be readily dispersed in aqueous media. Nanolycopene demonstrated stronger antioxidant activity and comparable in vitro anticancer efficacy to free lycopene against the melanoma cell line B16. Furthermore, nanolycopene showed comparable reduction of TPA-induced skin edema, expression of COX-2, and oxidative stress response. Additionally, it showed significant inhibition of tumor promotion. It also altered Bax and Bcl2 expressions, which led to the induction of apoptosis. The results also supported that the extracted lycopene-encapsulated nanoparticles may be a good alternative to the expensive commercial lycopene for cancer treatment.
- Published
- 2020
17. Nanonization of Magnoflorine-Encapsulated Novel Chitosan-Collagen Nanocapsules for Neurodegenerative Diseases
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Dar Junaid, Bashir, Saliha, Manzoor, Imran A, Khan, Masarat, Bashir, Nidhi Bharal, Agarwal, Shweta, Rastogi, Indu, Arora, and Mohammed, Samim
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Neurodegeneration is one of the most common diseases in the aged population, characterized by the loss in the function of neuronal cells and their ultimate death. One of the common features in the progression of this type of diseases is the oxidative stress. Drugs which are currently being used have been found to show lateral side effects, which is partly due to their inefficiency to cross blood-brain barrier. Nanoencapsulation of bioactive compounds is a profound approach in this direction and has become a method of choice nowadays. This study involved the evaluation of the anti-oxidative properties of magnoflorine (MF), which is an aporphine quaternary alkaloid, and synthesis of MF-loaded chitosan-collagen nanocapsules (MF-CCNc) for its better efficacy as a potent anti-oxidant. Physiochemical characterization of the synthesized nanocapsules was done by using dynamic light scattering and transmission electron microscopy. It revealed that the synthesized nanocapsules are of small size range, as small as 12 ± 2 nm, and are more or less of spherical shape. Sustained release was shown by MF in the
- Published
- 2021
18. Neuroprotective Effect of Fisetin Through Suppression of IL-1R/TLR Axis and Apoptosis in Pentylenetetrazole-Induced Kindling in Mice
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Ozair Alam, Mohammed Samim, Saima Khatoon, and Nidhi Bharal Agarwal
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0301 basic medicine ,caspase-3 ,fisetin ,Hippocampus ,Pharmacology ,Neuroprotection ,03 medical and health sciences ,chemistry.chemical_compound ,Epilepsy ,0302 clinical medicine ,medicine ,RC346-429 ,PI3K/AKT/mTOR pathway ,Original Research ,Seizure threshold ,pentylenetetrazole ,interleukin ,Kindling ,medicine.disease ,030104 developmental biology ,Neurology ,chemistry ,epilepsy ,Neurology. Diseases of the nervous system ,Neurology (clinical) ,Kindling model ,toll like receptor-4 ,030217 neurology & neurosurgery ,Fisetin - Abstract
Epilepsy is a complex neurological disorder, characterized by frequent electrical activity in brain regions. Inflammation and apoptosis cascade activation are serious neurological sequelae during seizures. Fisetin (3, 3′,4′,7-tetrahydroxyflavone), a flavonoid molecule, is considered for its effective anti-inflammatory and anti-apoptotic properties. This study investigated the neuroprotective effect of fisetin on experimental epilepsy. For acute studies, increasing current electroshock (ICES) and pentylenetetrazole (PTZ)-induced seizure tests were performed to evaluate the antiseizure activity of fisetin. For the chronic study, the kindling model was established by the administration of PTZ in subconvulsive dose (25 mg/kg, i.p.). Mice were treated with fisetin (5, 10, and 20 mg/kg, p.o.) to study its probable antiseizure mechanism. The kindled mice were evaluated for seizure scores. Their hippocampus and cortex were assessed for neuronal damage, inflammation, and apoptosis. Histological alterations were observed in the hippocampus of the experimental mice. Levels of high mobility group box 1 (HMGB1), Toll-like receptor-4 (TLR-4), interleukin-1 receptor 1 (IL-1R1), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) were assessed in the hippocampus and cortex by ELISA. The immunoreactivity and mRNA expressions of nuclear factor-κB (NF-κB), cyclooxygenase-2 (COX-2), cytochrome C, and caspase-3 were quantified by immunohistochemical analysis and real-time PCR. Phosphorylation ELISA was performed to evaluate AkT/mTOR (mammalian target of rapamycin) activation in the hippocampus and cortex of the kindled mice. The results showed that fisetin administration increased the seizure threshold current (STC) in the ICES test. In PTZ-induced seizures, fisetin administration increased the latency for myoclonic jerks (MJs) and generalized seizures (GSs). In the PTZ-induced kindling model, fisetin administration dose-dependently suppressed the development of kindling and the associated neuronal damage in the experimental mice. Further, fisetin administration ameliorated kindling-induced neuroinflammation as evident from decreased levels of HMGB1, TLR-4, IL-1R1, IL-1β, IL-6, and TNF-α in the hippocampus and cortex of the kindled mice. Also, the immunoreactivity and mRNA expressions of inflammatory molecules, NF-κB, and COX-2 were decreased with fisetin administration in the kindled animals. Decreased phosphorylation of the AkT/mTOR pathway was reported with fisetin administration in the hippocampus and cortex of the kindled mice. The immunoreactivity and mRNA expressions of apoptotic molecules, cytochrome C, and caspase-3 were attenuated upon fisetin administration. The findings suggest that fisetin shows a neuroprotective effect by suppressing the release of inflammatory and apoptosis molecules and attenuating histological alterations during experimental epilepsy.
- Published
- 2021
19. Biofabricated platinum nanoparticles: therapeutic evaluation as a potential nanodrug against breast cancer cells and drug-resistant bacteria
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Meher Rizvi, Tasneem Fatma, Nidhi Bharal Agarwal, Indu Arora, Khalid Imtiyaz, Irshad Ahamad, Saliha Manzoor, Mohammed Samim, and Dar Junaid Bashir
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Chemistry ,General Chemical Engineering ,Nanoparticle ,chemistry.chemical_element ,02 engineering and technology ,General Chemistry ,010402 general chemistry ,021001 nanoscience & nanotechnology ,Platinum nanoparticles ,01 natural sciences ,0104 chemical sciences ,Dynamic light scattering ,Zeta potential ,Nanomedicine ,Fourier transform infrared spectroscopy ,0210 nano-technology ,High-resolution transmission electron microscopy ,Platinum ,Nuclear chemistry - Abstract
Use of plant extracts for the synthesis of various metal nanoparticles has gained much importance recently because it is a simple, less hazardous, conservative and cost-effective method. In this research work, platinum nanoparticles were synthesized by treating platinum ions with the leaf extract of Psidium guajava and their structural properties were studied using various characterization techniques. The formation of platinum nanoparticles was confirmed by the disappearance of the absorbance peak at 261 nm in UV-visible spectra. The results of gas chromatography-mass spectrometry (GC-MS) and Fourier transform infrared spectroscopy (FT-IR) analysis showed functional moieties responsible for bio-reduction of metal ions and stabilization of platinum nanoparticles. The use of dynamic light scattering (DLS) imaging techniques confirmed the formation of stable monodispersed platinum nanoparticles showing a zeta potential of −23.4 mV. The morphological examination using high resolution transmission electron microscopy (HR-TEM) and Scanning electron microscopy (SEM) confirmed the formation of spherical platinum nanoparticles with an average diameter of 113.2 nm. X-ray powder diffraction (XRD) techniques showed the crystalline nature of biosynthesized platinum nanoparticles with a face-centered cubic structure. The results of energy-dispersive X-ray spectroscopy (EDAX) showed 100% platinum content by weight confirming the purity of the sample. The cytotoxic effect of biosynthesized platinum nanoparticles assessed in a breast cancer (MCF-7) cell-line by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, revealed an IC50 of 167.2 μg ml−1. The results of a wound healing assay showed that treatment with platinum nanoparticles induced an anti-migratory effect on MCF-7 cells. In the cell cycle phase distribution, treatment with platinum nanoparticles inhibited cell proliferation as determined by flow cytometry with PI staining. Significant cell cycle arrest was detected at the G0/G1 phase with a notable decrease in the distribution of cells in the S and G2/M phases. The anti-bacterial activity of bio-synthesized platinum nanoparticles was evaluated against four pathogenic bacteria i.e. B. cereus (Gram positive), P. aeruginosa (Gram negative), K. pneumonia (Gram negative) and E. coli (Gram negative). The biosynthesized platinum nanoparticles were found to show dose-dependent inhibition against pathogenic bacteria with a significant effect on Gram-negative bacteria compared to Gram-positive bacteria. This synergistic blend of green and simplistic synthesis coupled with anti-proliferative and anti-bacterial properties makes these biogenic nanoparticles suitable in nanomedicine.
- Published
- 2021
20. Application of chemometric approach for development and validation of high performance liquid chromatography method for estimation of ropinirole hydrochloride
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Farhan Jalees Ahmad, Mohammed Samim, Sarwar Beg, and Saman Fatima
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Detection limit ,Active ingredient ,Indoles ,Chromatography ,Central composite design ,Chemistry ,Drug Compounding ,010401 analytical chemistry ,Fractional factorial design ,Filtration and Separation ,01 natural sciences ,High-performance liquid chromatography ,0104 chemical sciences ,Analytical Chemistry ,Solvent ,03 medical and health sciences ,0302 clinical medicine ,Forced degradation ,Ropinirole Hydrochloride ,Chromatography, High Pressure Liquid ,030217 neurology & neurosurgery - Abstract
A systematic Quality by Design approach was employed for developing an isocratic reversed-phase liquid chromatographic technique for the estimation of ropinirole hydrochloride in bulk drug and pharmaceutical formulations. LiChrospher RP 18-5 Endcapped column (25 cm × 4.6 mm id) at ambient temperature (25 ± 2°C) was used for the chromatographic separation of the drug. The screening of factors influencing chromatographic separation of the active pharmaceutical ingredient was performed employing fractional factorial design to identify the influential factors. Optimization of the selected factors was carried out using central composite design for selecting the optimum chomatographic conditions. The mobile phase employed was constituted of Solvent A/Solvent B (65:35 v/v) (Solvent A [methanol/0.05 M ammonium acetate buffer, pH 7, 80:20 v/v] and Solvent B [high performance liquid chromatography grade water]) and used at 0.6 mL/min flow rate, while UV detection was performed at 250 nm. Linearity was achieved in the drug concentration range 5-100 µg/mL (R2 = 0.9998) with limits of detection and quantification of 1.02 and 3.09 µg/mL, respectively. Method validation was performed as per ICH guidelines followed by forced degradation studies, which indicated good specificity of the developed method for detecting ropinirole hydrochloride and its possible degradation products in the bulk drug and pharmaceutical formulations.
- Published
- 2019
21. Identification and evaluation of glutathione conjugate gamma-<scp>l</scp>-glutamyl-<scp>l</scp>-cysteine for improved drug delivery to the brain
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Mohammed Samim, Afzal Hussain, Tabish Rehman, Taj Mohammad, Md. Imtaiyaz Hassan, Saman Fatima, Deeba Shamim Jairajpuri, Mohammed F. Alajmi, and Farhan Jalees Ahmad
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gamma-L-Glutamyl-L-cysteine ,Antioxidant ,medicine.medical_treatment ,Drug delivery to the brain ,Brain ,General Medicine ,Glutathione ,Human brain ,Tripeptide ,Pharmacology ,Molecular Docking Simulation ,chemistry.chemical_compound ,Drug Delivery Systems ,medicine.anatomical_structure ,Pharmaceutical Preparations ,chemistry ,Structural Biology ,medicine ,Humans ,Cysteine ,Receptor ,Molecular Biology ,Conjugate - Abstract
Glutathione (GU), an endogenous antioxidant tripeptide, is frequently transferred in the human brain through N-methyl-d-aspartate receptor (NMDAR), profusely expressed at the blood–brain barrier (B...
- Published
- 2019
22. Synthesis, crystallographic study, molecular docking, ADMET, DFT and biological evaluation of new series of aurone derivatives as anti-leishmanial agents
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Syed Ayaz Nabi, Farhat Ramzan, Mehak Saba Lone, Mirza Adil Beg, Aabid Hamid, Lalit Mohan Nainwal, Mohammed Samim, Syed Shafi, Sameena Bano, and Kalim Javed
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Inorganic Chemistry ,Organic Chemistry ,Spectroscopy ,Analytical Chemistry - Published
- 2022
23. Controlled phase synthesis of VmOn in differing oxidation states using a simplified formic acid process, quantified with a new generalized index designed for use with public domain materials process information
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Devi, Henam Sylvia, primary, Mishra, Akshita, additional, Reza, Mohammed Samim, additional, Akhtar, Parvez, additional, Henam, Premananda Singh, additional, Singh, Thiyam David, additional, and Singh, Madhusudan, additional
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- 2021
- Full Text
- View/download PDF
24. Decreased Hip Labral Width Measured via Preoperative MRI is Associated with Inferior Outcomes for Arthroscopic Labral Repair
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Mohammed Samim, Robert J. Meislin, Samuel L. Baron, Christopher J. Burke, and Daniel Kaplan Thomas Youm
- Subjects
medicine.medical_specialty ,business.industry ,Medicine ,Orthopedics and Sports Medicine ,business ,Article ,Surgery - Abstract
Objectives: There are few pre-operative prognostic factors for hip labral repair outcomes. The objective of this study was to determine if hip labrum width measured on MRI was predictive of outcomes Methods: A retrospective review of prospectively gathered hip arthroscopy patients from 2010 to 2017 was performed. Inclusion criteria was defined as: patients >18 years old with radiographic evidence of femoroacetabular impingement who underwent a primary labral repair with >2 years of follow-up. Exclusion criteria was defined as: inadequate imaging, prior hip surgery, Tonnis grade ≥2 or lateral central edge angle 4mm. Statistical analysis was performed using: linear and polynomial regression, Mann-Whitney U, Fischer exact, and interclass-correlation coefficients (ICC) testing Results: One hundred and three patients (107 hips) met criteria (mean age 39.4years+/-17, BMI 25.0+/-4, 51%right-sided, 68%female). Mean labrum measurements and number of patients with ≤4mm labrums at the 12:00 (indirect rectus), 3:00 (Psoas U), and 1:30 (point ½ between) positions were 7.1mm+/-2.2; 15 labrums≤4mm, 7.0 mm+/-2.0;13 labrums≤4mm, and 5.5+/-1.9; 27 labrums≤4mm, respectively. ICC agreements were good to excellent between readers at all positions (0.83-0.91,p0.05). Sex, laterality, and BMI had no significant effect on outcomes (p>0.05).HHS, mHHS, and NAHS scores were found to be significantly lower in the ≤4mm group at each location tested (p0.05). Polynomial regression was significant at the 12:00 (R2=0.23,pConclusion: A non-linear relationship may exist between labral width and patient outcomes following labral repair. Labrum width of ≤4mm measured via MRI may negatively impact labral repair outcomes. Future research may determine if torn labrums ≤4mm should be reconstructed instead of repaired.
- Published
- 2020
25. Enhancement of the cancer inhibitory effect of the bioactive food component resveratrol by nanoparticle based delivery
- Author
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Sandeep C. Chaudhary, Farha Khan, Mohammed Samim, Sameena Bano, and Faheem Ahmed
- Subjects
Antioxidant ,Carcinogenesis ,medicine.medical_treatment ,Phytochemicals ,Biological Availability ,Apoptosis ,02 engineering and technology ,Resveratrol ,Pharmacology ,010402 general chemistry ,medicine.disease_cause ,01 natural sciences ,Antioxidants ,chemistry.chemical_compound ,Mice ,medicine ,Animals ,Anticarcinogenic Agents ,Skin ,Inflammation ,General Medicine ,021001 nanoscience & nanotechnology ,Bioactive Food Component ,In vitro ,0104 chemical sciences ,Bioavailability ,Oxidative Stress ,chemistry ,Nanoparticles ,Tetradecanoylphorbol Acetate ,0210 nano-technology ,Oxidative stress ,Food Science - Abstract
Naturally occurring bioactive food components such as dietary polyphenols have shown many beneficial biological activities due to their good antioxidant properties. Among them significant attention has been given to resveratrol (RV) in recent years as it plays a promising role in cancer prevention. It has demonstrated anti-proliferative effects, as well as the ability to inhibit the initiation and progression of induced cancer in a wide variety of tumor models. However, the benefits of its therapeutic effects were found to be limited due to its poor pharmacokinetic properties such as poor aqueous solubility, instability and extensive first pass metabolism. To overcome these limitations, the present study aimed to synthesize thermosensitive copolymeric nanoparticle encapsulated formulations of resveratrol-nanoresveratrol (NRV) and evaluate their in vitro anticancer activity and inhibitory effect on 12-O-tetradecanoylphorbol-13-acetate (TPA)-promoted skin inflammation and tumorigenesis in Swiss albino mice. For this purpose PNIPAAM-PEG based thermosensitive copolymeric nanoparticles were synthesized followed by the encapsulation of RV in their hydrophobic core. This enhanced the therapeutic bioavailability of resveratrol. Nanoresveratrol demonstrated stronger antioxidant activity and comparable anticancer efficacy to free resveratrol. Nanoparticles were characterized by IR, NMR, DLS and TEM. The best results were obtained with NRV at significantly lower doses. NRV demonstrated better in vitro anticancer activity against melanoma cell line B16. It showed comparable reduction of TPA induced skin edema, hyperplasia and oxidative stress response. In the promotion phase, a significant reduction was found in tumor incidence and tumor burden in mice pre-treated with NRV. Moreover, at all doses NRV altered Bax and Bcl2 expressions which lead to the induction of apoptosis.
- Published
- 2020
26. Collagen Nanoparticle-Mediated Brain Silymarin Delivery: An Approach for Treating Cerebral Ischemia and Reperfusion-Induced Brain Injury
- Author
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Mohd Akhtar, Indu Arora, Shweta Rastogi, Mohammed Samim, Shruti Singh, and Pankaj Rathore
- Subjects
0301 basic medicine ,food.ingredient ,Ischemia ,ischemia ,Pharmacology ,Neuroprotection ,lcsh:RC321-571 ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,food ,medicine ,lcsh:Neurosciences. Biological psychiatry. Neuropsychiatry ,Original Research ,Milk Thistle ,Silybum ,General Neuroscience ,apoptosis ,Malondialdehyde ,medicine.disease ,stroke ,Bioavailability ,reperfusion ,030104 developmental biology ,chemistry ,Apoptosis ,Drug delivery ,neuroprotection ,030217 neurology & neurosurgery ,Neuroscience - Abstract
Silymarin is a bioactive constituent isolated from milk thistle (Silybum marinum). Since its discovery, silymarin has been considered a gold standard drug in treating ailments related to the liver, resulting from alcohol consumption and viral hepatitis. This hepatoprotective nature of silymarin arises out of antioxidative and tissue-regenerating properties of silymarin. However, several recent studies have established the neuroprotective link of silymarin, too. Thus, the current investigation was aimed at exploring the neuroprotective effect of nanosilymarin (silymarin encapsulated inside collagen-based polymeric nanoparticulate drug delivery system). The study aimed at bringing out the role of nanoparticles in enhancing the therapeutic effect of silymarin against neuronal injury, originating out of oxidative-stress-related brain damages in focal cerebral ischemia. Collagen-based micellar nanoparticles were prepared and stabilized using 3-ethyl carbodiimide-hydrochloride (EDC-Hcl) and malondialdehyde (MDA) as crosslinkers. Nanoparticles were characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), and Fourier transform infrared (FT-IR) spectroscopy techniques, and the size of nanoparticles was found to be around 48 nm. Male albino Wistar rats were pretreated with three different doses of nanosilymarin of 10, 100, and 1,000 μg/kg b.wt and a dose of free silymarin of 100 mg/kg b.wt intraperitoneally (i.p.) for 7 days. Focal cerebral ischemia was induced using the middle cerebral artery occlusion (MCAO) model on the eighth day for 1 h followed by 24 h reperfusion. The animals were then evaluated for neurobehavioral, infarct analysis, biochemical, histopathological, and immunohistochemical studies. All the above parameters showed remarkable improvement in nanosilymarin-treated groups in comparison to the silymarin-treated group. Nanoparticle encapsulation of drug enhanced neuroprotection by increasing drug bioavailability and targeting. Thus, the present study concluded with satisfactory results, showing the critical role played by nanoparticles in improving the neuroprotection at very low drug doses.
- Published
- 2020
27. Polymeric nanoparticles as a platform for permeability enhancement of class III drug amikacin
- Author
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Mohammed Samim, Sushama Talegaonkar, Zeenat Iqbal, Amulya K. Panda, Farhan Jalees Ahmad, and Saman Fatima
- Subjects
Drug ,Polymers ,Surface Properties ,media_common.quotation_subject ,Microbial Sensitivity Tests ,02 engineering and technology ,Pharmacology ,010402 general chemistry ,01 natural sciences ,chemistry.chemical_compound ,Colloid and Surface Chemistry ,Escherichia coli ,Tumor Cells, Cultured ,medicine ,Humans ,Particle Size ,Physical and Theoretical Chemistry ,Amikacin ,media_common ,Aminoglycoside ,Surfaces and Interfaces ,General Medicine ,Permeation ,021001 nanoscience & nanotechnology ,Intestinal epithelium ,Anti-Bacterial Agents ,0104 chemical sciences ,Klebsiella pneumoniae ,PLGA ,chemistry ,Permeability (electromagnetism) ,Pseudomonas aeruginosa ,Drug delivery ,Nanoparticles ,0210 nano-technology ,HT29 Cells ,Biotechnology ,medicine.drug - Abstract
Amikacin (A), a water soluble aminoglycoside antibiotic is commercially available for intravenous administration only. Present investigation is aimed at the development of poly-lactic-co-glycolic acid (PLGA) nanoparticles (A-NPs). 1 for oral permeability enhancement of amikacin. The pharmaceutical attributes of the A-NPs revealed particle size, 260.3 ± 2.05 nm, zeta potential, −12.9 ± 1.12 mV and drug content, 40.10 ± 1.87 μg/mg with spherical shape and smooth surface. In vitro antibacterial studies showed that the A-NPs were active against P. aeruginosa, K. pneumoniae and E. coli. The permeation study across rat ileum showed 2.6-fold improvement in Papp for A-NPs than A-S 2 This increase in permeability is due to the uptake of nanoparticles by Peyer’s patches of intestinal epithelium and endocytic uptake via enterocytes. Flow cytometric analysis demonstrated 2.2-fold higher uptake of Rh B-NPs 3 than Rh B-S 4 and elucidated the dominance of enterocytes mediated endocytosis of nanoparticles. Furthermore, stability data collected as per ICH guidelines for three months under accelerated conditions had shown that the A-NPs were stable. The purported drug delivery system hence, seems a promising tool to replace successfully the current intravenous therapy and is used to support relevant patient compliance thereby, adding value to the “patient care at home”.
- Published
- 2018
28. Hierarchically Grown NiO-Decorated Polyaniline-Reduced Graphene Oxide Composite for Ultrafast Sunlight-Driven Photocatalysis
- Author
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Mohammed Samim, Preety Ahuja, Indu Arora, and Sanjeev Kumar Ujjain
- Subjects
Nanocomposite ,Materials science ,Graphene ,General Chemical Engineering ,Nickel oxide ,Non-blocking I/O ,Oxide ,Nanoparticle ,02 engineering and technology ,General Chemistry ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,Article ,0104 chemical sciences ,law.invention ,lcsh:Chemistry ,chemistry.chemical_compound ,lcsh:QD1-999 ,chemistry ,Chemical engineering ,law ,Polyaniline ,Photocatalysis ,0210 nano-technology - Abstract
Polymers and transition-metal oxides have gained great interest as a photocatalyst in environmental remediation. They could be modified with each other in order to improve their activity. Here, a sunlight-responsive hierarchically structured ternary composite of nickel oxide, polyaniline, and reduced graphene oxide (NiO@PANI/RGO) has been synthesized and employed as a catalyst for dye [methylene blue (MB)] degradation. PANI/GO synthesized by interfacial polymerization acts as a matrix for the growth of NiO using a microemulsion solvothermal method, ensuing an in situ reduction of graphene oxide during the formation of a hierarchical NiO@PANI/RGO composite. Morphological studies of the as-synthesized NiO@PANI/RGO composite reveal fine NiO (10 nm) nanoparticles intercalated between the uniformly grown PANI spines (50-60 nm) over the RGO surface. The optical band gap of ∼1.9 eV calculated from the UV-vis spectrum illustrates the extended light absorption range for the NiO@PANI/RGO photocatalyst. The efficiency of 98% MB degradation within 11 min with the degradation rate constant 0.086 min-1 for NiO@PANI/RGO has surpassed any other report on metal oxide/graphene-based ternary composites. Overall, this work could pave the way for the fabrication of futuristic hierarchical structured ternary nanocomposites as an efficient photocatalyst and facilitate their application in the environmental protection issues.
- Published
- 2018
29. Collagen-curcumin nanocomposites showing an enhanced neuroprotective effect against short term focal cerebral ischemia
- Author
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Mohd Akhtar, Shweta Rastogi, Mohammed Samim, Shruti Singh, Indu Arora, and Pankaj Rathore
- Subjects
0303 health sciences ,business.industry ,General Chemical Engineering ,030302 biochemistry & molecular biology ,Ischemia ,Ischemic injury ,General Chemistry ,Pharmacology ,medicine.disease ,medicine.disease_cause ,Neuroprotection ,Pathogenesis ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,chemistry ,medicine ,Curcumin ,business ,Mode of action ,Reperfusion injury ,030217 neurology & neurosurgery ,Oxidative stress - Abstract
The effectiveness of curcumin in treating cerebral ischemia has been reported in recent studies. However, its mode of action is still not defined. The objective of the present study is to formulate collagen–curcumin nanocomposites which will work effectively against cerebral ischemia/reperfusion injury. Ischemic injury is followed by inflammatory damage and oxidative stress, which together contribute a lot in the pathogenesis of cerebral ischemia and may be considered a good target for treatment. The present study focused on examining the effectiveness of collagen–curcumin nanocomposites stabilized by increasing the degree of crosslinking in reducing oxidative stress associated with brain injury resulting from cerebral ischemia. The collagen nanoparticles were prepared by conjugating collagen on the surface of Tween©80 micelles, and further stabilizing them using crosslinkers. The effectiveness of the prepared nanocomposite was validated by performing infarct analysis followed by biochemical, behavioral, histopathological and immunohistochemical studies. The outcomes of this study are promising for the use of collagen–curcumin nanocomposites in showing neuroprotective potential in treating ischemic injury.
- Published
- 2019
30. Resveratrol loaded nanoparticles attenuate cognitive impairment and inflammatory markers in PTZ-induced kindled mice
- Author
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Aarzoo, Shweta Rastogi, Mohammed Samim, Mobin A. Siddiqui, Nidhi Aggarwal, Saliha Manzoor, Dar Junaid Bashir, Juheb Akhter, and Indu Arora
- Subjects
Male ,Immunology ,Resveratrol ,Pharmacology ,Hippocampus ,Antioxidants ,Mice ,chemistry.chemical_compound ,Epilepsy ,medicine ,Animals ,Humans ,Immunology and Allergy ,Hippocampus (mythology) ,Cognitive Dysfunction ,Cognitive impairment ,Glutathione ,medicine.disease ,Bioavailability ,Disease Models, Animal ,Oxidative Stress ,chemistry ,Pentylenetetrazole ,Collagen ,Nanoparticle Drug Delivery System - Abstract
Resveratrol has been found to exert protective effects in neurological disorders, including epilepsy. However, its poor bioavailability and difficulty in reaching the brain’s targeted location reduce resveratrol’s efficacy substantially. The side effects due to the higher concentration of drugs are another matter of concern. The objective of the present study is to propose solutions to these issues by encapsulating resveratrol in glutathione-coated collagen nanoparticles’ core. The collagen nanoparticles increase the resveratrol’s bioavailability, and glutathione helps in the passage of the encapsulated resveratrol to the target location in the brain. The concentration also substantially reduces due to resveratrol’s encapsulation in glutathione-coated collagen nanoparticles. The encapsulated resveratrol is termed nanoresveratrol. The effectiveness of nanoresveratrol on epilepsy seizures was evaluated through histopathological examinations, ELISA tests, and qRT-PCR tests on the hippocampus of the kindled mice. The novelty of the present study thus lies in (i) the synthesis of nanoresveratrol using glutathione-coated collagen nanoparticles and (ii) the application of synthesized nanoresveratrol in the treatment of epilepsy. The study’s outcome shows that nanoresveratrol has a favorable impact in reducing cognitive impairment in kindled mice, and it is more effective in controlling epilepsy seizures than resveratrol. The p-values of all the nanoresveratrol-given groups of mice (compared with the diseased group) were substantially smaller (∼ 10 - 4 to 10 - 2 ) than the significance level (0.05), indicating that the nanoresveratrol-given groups are significantly different from the diseased group, i.e., the nanoresveratrol has a significant effect on the mice. The concentration of resveratrol also decreases substantially in the proposed nanoformulation. It was observed that even 0.4 mg/kg of nanoformulation of resveratrol is performing better than 40 mg/kg of resveratrol.
- Published
- 2021
31. Embelin ameliorates cognitive dysfunction and progression of kindling in pentylenetetrazol-induced kindling in mice by attenuating brain inflammation
- Author
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Seema Jain, Mohammed Samim, Gaurav Kumar Jain, Nidhi Bharal Agarwal, and Ubedul Hoda
- Subjects
Male ,Hippocampus ,Pharmacology ,Epileptogenesis ,Mice ,03 medical and health sciences ,Behavioral Neuroscience ,0302 clinical medicine ,Dopamine ,Benzoquinones ,Kindling, Neurologic ,medicine ,Animals ,Cognitive Dysfunction ,030212 general & internal medicine ,Pentylenetetrazol ,Seizure threshold ,Kindling ,Chemistry ,Glutamate receptor ,Neurology ,Encephalitis ,Pentylenetetrazole ,Neurology (clinical) ,030217 neurology & neurosurgery ,medicine.drug ,Behavioural despair test - Abstract
Objective This study was conducted to evaluate the effect of embelin (EMB) on various epileptic models and related brain inflammation. Methods Male Swiss albino mice were administered EMB (5, 10, and 20 mg/kg/p.o.) in acute and chronic study for 7 days and 35 days, respectively. Acute study included increasing current electroshock (ICES) and pentylenetetrazol (PTZ)-induced seizure test. Step-down latency (SDL) and forced swim test (FST) were performed to evaluate cognitive functions and depression-like behavior, respectively. Chronic study included PTZ-induced kindling. Levels of inflammatory biomarkers, namely interleukin-1 beta (IL-1β), interleukin-1 receptor antagonist (IL-1Ra), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α), were estimated in the hippocampus and cortex of the kindled brains by ELISA technique. Further, neurotransmitters (NTs), namely gamma aminobutyric acid (GABA), glutamate, and dopamine, were estimated by using validated liquid chromatography–mass spectrometry (LC–MS) method followed by ultra-high-performance liquid chromatography (UHPLC). Results Embelin (EMB) treatment increased the seizure threshold to hind limb extension (HLE) in the ICES test and decreased the seizure scores in the kindling experiment. Significantly low levels of IL-1β, IL-1Ra, IL-6, and TNF-α were observed in the hippocampus of PTZ + EMB (10 and 20 mg/kg)-treated groups compared with PTZ+ vehicle-treated group. Significantly lower levels of IL-1Ra, IL-6, and TNF-α compared with PTZ+ vehicle-treated group were observed in the cortex of PTZ + EMB (10 and 20 mg/kg)-treated groups, while IL-1β levels were found to be significantly lower only in the cortex of PTZ + EMB (20 mg/kg)-treated group. Increased levels of dopamine and GABA and decreased levels of glutamate in both hippocampus and cortex were observed in EMB + PTZ-treated groups compared with vehicle + PTZ-treated group. Latency of step down was found to be increased and immobility time in FST was decreased in EMB + PTZ groups compared with vehicle + PTZ group. Conclusion Embelin suppressed epileptogenesis in the kindled mice via neurochemical modulation of neurotransmitters and inhibiting the inflammatory pathway. Further, EMB was also observed to be protecting the kindled animals from cognition and depression-like behavior.
- Published
- 2021
32. Design and synthesis of pyridazinone-substituted benzenesulphonylurea derivatives as anti-hyperglycaemic agents and inhibitors of aldose reductase – an enzyme embroiled in diabetic complications
- Author
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Ameer Ismael, Syed Ovais, Alhamza Dheyaa, G. Bhanuprakash Reddy, Surender Singh, Syed Shafi, Mohammed Samim, Kalicharan Sharma, Ayad Ahmed, Kalim Javed, Pooja Rathore, H. Pushpalatha, Raed Yaseen, and Mymoona Akthar
- Subjects
Male ,0301 basic medicine ,medicine.drug_class ,Pharmacology ,Diabetes Complications ,03 medical and health sciences ,chemistry.chemical_compound ,Aldehyde Reductase ,Lens, Crystalline ,Drug Discovery ,medicine ,Animals ,Hypoglycemic Agents ,Gliclazide ,Rats, Wistar ,IC50 ,Aldose reductase ,Spectrum Analysis ,Area under the curve ,General Medicine ,Sulfonylurea ,Rats ,Pyridazines ,Sulfonylurea Compounds ,030104 developmental biology ,chemistry ,Biochemistry ,Docking (molecular) ,Area Under Curve ,Drug Design ,Female ,Quercetin ,medicine.drug - Abstract
Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I-XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III-XI, XIV-XVII, XIX-XXIV, XXVI and XXVIII-XXX) showed more or comparable area under the curve (AUC) reduction percentage (ranging from 21.9% to 35.5%) as compared to the standard drug gliclazide (22.0%). On the basis of docking results, 18 compounds were screened for their in vitro ability to inhibit rat lens aldose reductase. Ten compounds (III-VI, XII, XVI-XVIII, XXI and XXVII) showed ARI activity with IC50 ranging from 34 to 242 μM. Out of these, two compounds IV and V showed best ARI activity which is comparable with that of quercetin. As a result, two compounds (IV and V) possessing significant dual action (anti-hyperglycaemic and aldose reductase inhibition) were identified and may be used as lead compounds for developing new drugs.
- Published
- 2016
33. Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti-Inflammatory and Anti-Proliferative Agents
- Author
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Alhamzah Dh. Hameed, Mohammed Samim, Mymona Akhtar, Surender Singh, Kalicharan Sharma, Kalim Javed, Raed Yaseen, Pooja Rathore, and Syed Ovais
- Subjects
0301 basic medicine ,Drug ,medicine.drug_class ,Chemistry ,media_common.quotation_subject ,Pharmaceutical Science ,Nanotechnology ,Carbon-13 NMR ,Pharmacology ,Anti-inflammatory ,In vitro ,03 medical and health sciences ,chemistry.chemical_compound ,030104 developmental biology ,0302 clinical medicine ,In vivo ,030220 oncology & carcinogenesis ,Drug Discovery ,medicine ,Proton NMR ,Phthalazine ,Etoricoxib ,medicine.drug ,media_common - Abstract
The chemistry of phthalazine derivatives has been of increasing interest since many of these compounds have found many chemotherapeutic applications. So this study aims to synthesize a library of phthalazine derivatives and to investigate their anti-inflammatory and anti-proliferative activities. Sixteen new phthalazinone derivatives (2a-p) were synthesized and tested for their in vitro antiproliferative and in vivo anti-inflammatory activities. All the synthesized compounds were identified and characterized by IR, (1) H NMR, (13) C NMR spectroscopy, and MS. Two compounds, 2b and 2i, showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib in the carrageenan-induced rat paw edema model at 3 and 5 h, respectively. Three compounds (2h, 2j, and 2g) showed moderate sensitivity toward the renal cancer cell line UO-31.
- Published
- 2016
34. Combinatorial drug delivery strategy employing nano-curcumin and nano-MiADMSA for the treatment of arsenic intoxication in mouse
- Author
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Abhishek Yadav, Swaran J.S. Flora, Pramod Kushwaha, and Mohammed Samim
- Subjects
0301 basic medicine ,Male ,Sodium arsenite ,Curcumin ,chemistry.chemical_element ,Arsenic poisoning ,Pharmacology ,Toxicology ,Arsenic ,03 medical and health sciences ,chemistry.chemical_compound ,Mice ,Metal poisoning ,Arsenic Poisoning ,medicine ,Animals ,Chelation therapy ,Drug Carriers ,Arsenic toxicity ,Deoxyguanosine ,Drug Synergism ,General Medicine ,medicine.disease ,Glutathione ,Enzymes ,Oxidative Stress ,030104 developmental biology ,chemistry ,Liver ,8-Hydroxy-2'-Deoxyguanosine ,Nanoparticles ,Reactive Oxygen Species ,Succimer ,Combination drug - Abstract
Chelation therapy is the mainstream treatment for heavy metal poisoning. Apart from this, therapy using antioxidant/herbal extracts are the other strategies now commonly being tried for the treatment. We have previously reported individual beneficial efficacy of nanoparticle mediated administration of an antioxidant like 'curcumin' and an arsenic chelator 'monoisoamyl 2,3-dimercaptosuccinic acid (MiADMSA)' for the treatment of arsenic toxicity compared to bulk drugs. The present paper investigates our hypothesis that a combination drug delivery therapy employing two nanosystems, a chelator and a strong antioxidant, may produce more pronounced therapeutic effects compared to individual effects in the treatment of arsenic toxicity. An in-vivo study was conducted wherein arsenic as sodium arsenite (100 ppm) was administered in drinking water for 5 months to Swiss albino mice. This was followed by a treatment protocol comprising of curcumin encapsulated chitosan nanoparticles (nano-curcumin, 15 mg/kg, orally for 1 month) either alone or in combination with MiADMSA encapsulated polymeric nanoparticles (nano-MiADMSA, 50 mg/kg for last 5 days) to evaluate the therapeutic potential of the combination treatment. Our results demonstrated that co-treatment with nano-curcumin and nano-MiADMSA provided beneficial effects in a synergistic way on the adverse changes in oxidative stress parameters and metal status induced by arsenic.
- Published
- 2018
35. Synthesis and biological evaluation of some new pyrazoline substituted benzenesulfonylurea/thiourea derivatives as anti-hyperglycaemic agents and aldose reductase inhibitors
- Author
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Syed Ovais, Kalim Javed, H. Pushpalatha, Mymoona Akthar, Rafia Bashir, Pooja Rathore, Omprakash Tanwar, G. Bhanuprakash Reddy, Alhamza Dheyaa, Shafiya Yaseen, Mohammed Samim, and Raed Yaseen
- Subjects
Blood Glucose ,Protein Conformation ,Stereochemistry ,Pyrazoline ,Chemistry Techniques, Synthetic ,Inhibitory Concentration 50 ,chemistry.chemical_compound ,Aldehyde Reductase ,Drug Discovery ,Animals ,Hypoglycemic Agents ,Enzyme Inhibitors ,Pharmacology ,Aldose reductase ,Chemistry ,Organic Chemistry ,Thiourea ,General Medicine ,Carbon-13 NMR ,Rats ,Anti hyperglycaemic ,Molecular Docking Simulation ,Docking (molecular) ,Proton NMR ,Pyrazoles ,Sorbinil - Abstract
Seventeen new pyrazoline substituted benzenesulfonylurea/thiourea derivatives (2a–q) were synthesized and characterized by elemental analysis and various spectroscopic techniques viz; IR, 1H NMR, 13C NMR, and MS data. Thirteen compounds showed moderate to good anti-hyperglycaemic activity in glucose fed hyperglycaemic normal rats at the dose of 0.05 mM/kg b.w. On the basis of docking results nine compounds (2a, 2c, 2e, 2h, 2k, 2l, 2n, 2o and 2q) were evaluated for their ability to inhibit rat lens aldose reductase. Out of these six compounds (2h, 2k, 2l, 2n, 2o and 2q) were found more effective than the known ARI sorbinil. Five compounds (2h, 2k, 2l, 2n and 2o) showed significant dual action (anti-hyperglycaemic and aldose reductase inhibition).
- Published
- 2014
36. A Prospective Evaluation of 3D-MRI Versus 3D-CT in the Evaluation of Osseous Anatomy in Femoracetabular Impingement
- Author
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Soterios Gyftopoulos, Mohammed Samim, Nima Eftekhary, Roy I. Davidovitch, Ameer Elbuluk, Ahmad Badri, and Jonathan M. Vigdorchik
- Subjects
medicine.medical_specialty ,business.industry ,medicine ,Orthopedics and Sports Medicine ,Radiology ,business ,Femoracetabular Impingement ,Prospective evaluation - Published
- 2018
37. Synthesis and blood glucose lowering activity of some novel benzenesulfonylthiourea derivatives substituted with 4-aryl-1-oxophthalazin-2(1H)yl-ones
- Author
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Mohammed Samim, Rafia Bashir, Kalim Javed, Shafiya Yaseen, Pooja Rathore, and Syed Ovais
- Subjects
Blood Glucose ,Male ,Stereochemistry ,Rat model ,Medicinal chemistry ,Structure-Activity Relationship ,chemistry.chemical_compound ,Isothiocyanates ,Drug Discovery ,Acetone ,Animals ,Hypoglycemic Agents ,Rats, Wistar ,Pharmacology ,Glucose lowering ,Aryl ,Benzenesulfonates ,Thiourea ,General Medicine ,Rats ,Glucose ,chemistry ,Elemental analysis ,Drug Design ,Hyperglycemia ,Isothiocyanate ,Anhydrous ,Proton NMR ,Phthalazines ,Female - Abstract
Some new benzenesulfonylthiourea derivatives substituted with phthalazones (2a–q) were synthesized by refluxing the appropriate 4-aryl-1-oxophthalazin-2(1H)yl benzenesulfonamides with isothiocyanate in dry acetone over anhydrous K2CO3. All the synthesized compounds were characterized on the basis of IR, 1H NMR, MS data and elemental analysis. These synthesized compounds (2a–q) at the dose of 20 mg/kg were tested for antihyperglycemic activity in the glucose-fed hyperglycemic normal rat model and among these compounds 2f and 2m showed modest antihyperglycemic activity.
- Published
- 2013
38. Size- and shape-dependent clinical and mycological efficacy of silver nanoparticles on dandruff
- Author
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Sumeet Kapoor, Indu Arora, Swati Jain, Mohammad Anwar, Deepak Yadav, Shweta Rastogi, and Mohammed Samim
- Subjects
0301 basic medicine ,Pathology ,medicine.medical_specialty ,030106 microbiology ,Dispersity ,Biophysics ,Pharmaceutical Science ,Nanoparticle ,Bioengineering ,02 engineering and technology ,Silver nanoparticle ,Biomaterials ,03 medical and health sciences ,Minimum inhibitory concentration ,In vivo ,International Journal of Nanomedicine ,Drug Discovery ,medicine ,Potency ,Original Research ,Chemistry ,Organic Chemistry ,Malassezia furfur ,General Medicine ,Dandruff ,021001 nanoscience & nanotechnology ,Wistar rat model ,in vivo analysis ,Nanorod ,medicine.symptom ,0210 nano-technology ,nanorods ,Nuclear chemistry - Abstract
Mohammad F Anwar,1 Deepak Yadav,2 Swati Jain,3 Sumeet Kapoor,4 Shweta Rastogi,5 Indu Arora,6 Mohammed Samim1 1Department of Chemistry, Faculty of Science, 2Faculty of Medicine, Jamia Hamdard University, New Delhi, 3Amity Institute of Nanotechnology, Amity University, Noida, Uttar Pradesh, 4Centre for Biomedical Engineering, Indian Institute of Technology, Delhi, 5Department of Chemistry, Hans Raj College, 6Department of Biomedical Sciences, Rajguru College of Applied Sciences for Women, University of Delhi, Delhi, India Abstract: Dandruff is a prominent scalp problem caused by the growth of fungus Malassezia furfur, potentially cascading into dermal inflammation, itching, and tissue damage. The present work outlines a detailed analysis of the treatment of scalp infection using silver nanomaterials (Ag NMs), and focuses on biocidal activity owing to manipulation of size, shape, and structure. Monodisperse silver spherical nanoparticles (NPs) and nanorods (NRs) were synthesized by chemical routes that were characterized using analytical and spectroscopic techniques. Ag NMs demonstrated enhanced biocidal tendencies compared to market available drugs, itracanozole and ketoconazole, showing greater zones of inhibition. The obtained 20nm and 50nm spherical-shaped NPs and 50nm NRs showed concentration-, size-, and shape-dependent antifungal activity, with 20nm spherical-shaped NPs exhibiting excellent potency. Minimum inhibitory concentration for 20nm was lowest at 0.2mg/mL in comparison to 0.3mg/mL for NRs. Primary irritation index was 0.33 and 0.16 for 20nm and 50nm spherical-shaped NPs, respectively, while 50nm rod-shaped NMs exhibited negligible redness. An in vivo model for M. furfur infection was generated by passing fungi subcutaneously in rats’ skin. Again, 20nm particles showed best normalization of skin after 10days on regular dosing, in comparison with bigger and rod-shaped particles. The statistical clinical score was highest for Ag nanorods, followed by 50nm Ag NPs-treated animals. It was observed that 20nm spherical particles exhibited the lowest score (0) compared with others as well as with antifungal drugs. Biochemical analysis performed by checking antioxidant enzymatic activities indicated tissue repair and normalization of enzymes and protein concentration by Ag NPs. Keywords: Malassezia furfur, nanorods, in vivo analysis, Wistar rat model
- Published
- 2016
39. Synthesis and anti-inflammatory activity of celecoxib like compounds
- Author
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Syed Ovais, Vinod Nair, Rafia Bashir, Mohammed Samim, Surender Singh, Kalim Javed, Pooja Rathore, and Shafiya Yaseen
- Subjects
medicine.drug_class ,Analgesic ,Antineoplastic Agents ,Pyrazoline ,Pharmacology ,Carrageenan ,Nitric Oxide ,Anti-inflammatory ,Structure-Activity Relationship ,chemistry.chemical_compound ,Drug Discovery ,medicine ,Animals ,Edema ,Humans ,Cell Proliferation ,Sulfonamides ,Dose-Response Relationship, Drug ,Molecular Structure ,Tumor Necrosis Factor-alpha ,Melanoma ,Anti-Inflammatory Agents, Non-Steroidal ,General Medicine ,Reference drug ,medicine.disease ,Rats ,chemistry ,Celecoxib ,Cell culture ,Prostaglandins ,Pyrazoles ,Drug Screening Assays, Antitumor ,medicine.drug - Abstract
Nine novel 4-[3-(4-Dimethylamino-phenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]-benzenesulfonamides (2a-i) were synthesized and evaluated for their anti-inflammatory and antiproliferative activities. These compounds (2a-i) showed moderate to strong anti-inflammatory activity in carrageenan rat paw oedema test. Compounds 2b, 2d and 2g showing comparable anti-inflammatory activity to that of reference drug celecoxib were evaluated for their ulcerogenic and analgesic activities. The effect of 2b, 2d and 2g on the content of NO, TNF-α and PGE2 in exudates from rat paw stimulated by carrageenan was also evaluated. The compound 2c showed considerable antitumor activities against all 60 human tumor cell lines with effective GI50 (MG-MID) value of 3.63 µM. It exhibited maximum activity against melanoma (LOX IMVI and SK-MEL-5) cancer cell lines with GI50 value less than 2 μM.
- Published
- 2012
40. Curcumin encapsulated in chitosan nanoparticles: A novel strategy for the treatment of arsenic toxicity
- Author
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Abhishek Yadav, Swaran J.S. Flora, Vinay Lomash, and Mohammed Samim
- Subjects
Male ,Biogenic Amines ,Curcumin ,Antioxidant ,Sodium arsenite ,medicine.medical_treatment ,Arsenic poisoning ,chemistry.chemical_element ,Pharmacology ,Toxicology ,medicine.disease_cause ,Thiobarbituric Acid Reactive Substances ,Arsenic ,chemistry.chemical_compound ,Arsenic Poisoning ,medicine ,Animals ,Tissue Distribution ,Rats, Wistar ,Arsenic toxicity ,Brain ,General Medicine ,Glutathione ,medicine.disease ,Rats ,Oxidative Stress ,Liver ,chemistry ,Nanoparticles ,Lipid Peroxidation ,Reactive Oxygen Species ,Oxidative stress - Abstract
Water-soluble nanoparticles of curcumin were synthesized, characterized and applied as a stable detoxifying agent for arsenic poisoning. Chitosan nanoparticles of less than 50 nm in diameter containing curcumin were prepared. The particles were characterized by TEM, DLS and FT-IR. The therapeutic efficacy of the encapsulated curcumin nanoparticles (ECNPs) against arsenic-induced toxicity in rats was investigated. Sodium arsenite (2mg/kg) and ECNPs (1.5 or 15 mg/kg) were orally administered to male Wistar rats for 4 weeks to evaluate the therapeutic potential of ECNPs in blood and soft tissues. Arsenic significantly decreased blood δ-aminolevulinic acid dehydratase (δ-ALAD) activity, reduced glutathione (GSH) and increased blood reactive oxygen species (ROS). These changes were accompanied by increases in hepatic total ROS, oxidized glutathione, and thiobarbituric acid-reactive substance levels. By contrast, hepatic GSH, superoxide dismutase and catalase activities significantly decreased on arsenic exposure, indicative of oxidative stress. Brain biogenic amines (dopamine, norepinephrine and 5-hydroxytryptamine) levels also showed significant changes on arsenic exposure. Co-administration of ECNPs provided pronounced beneficial effects on the adverse changes in oxidative stress parameters induced by arsenic. The results indicate that ECNPs have better antioxidant and chelating potential (even at the lower dose of 1.5 mg/kg) compared to free curcumin at 15 mg/kg. The significant neurochemical and immunohistochemical protection afforded by ECNPs indicates their neuroprotective efficacy. The formulation provides a novel therapeutic regime for preventing arsenic toxicity.
- Published
- 2012
41. Synthesis and pharmacological evaluation of some novel 2-pyrazolines bearing benzenesulfonamide as anti-inflammatory and blood glucose lowering agents
- Author
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Syed Ovais, Rafia Bashir, Shafiya Yaseen, Pooja Rathore, Mohammed Samim, and Kalim Javed
- Subjects
Chalcone ,medicine.drug_class ,Hydrochloride ,Organic Chemistry ,Sulfonamide (medicine) ,Pyrazoline ,Pharmacology ,Anti-inflammatory ,chemistry.chemical_compound ,chemistry ,In vivo ,Edema ,medicine ,Moiety ,General Pharmacology, Toxicology and Pharmaceutics ,medicine.symptom ,medicine.drug - Abstract
A series of novel pyrazolines (2a–l) bearing benzenesulfonamide moiety were synthesized by condensing appropriate chalcone (1a–l) with 4-hydrazinobenzenesulfonamide hydrochloride. Structure of all novel synthesized compounds was characterized on basis of elemental analysis data and spectral data (IR, 1HNMR, MS). Compounds (2a–l) were screened for in vivo anti-inflammatory action in carrageenan-induced rat paw edema model and blood glucose lowering action in glucose fed hyperglycemic normal rats. Compounds 2a, 2e, and 2l showed significant anti-inflammatory action (more than 75 %) at 5 h and also showed superior gastrointestinal safety profiles as compared to celecoxib. One compound (2i) was found to exhibit significant blood glucose lowering activity.
- Published
- 2012
42. Application of Novel Nanotechnology Strategies in Plant Biotransformation: A Contemporary Overview
- Author
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M. Amin Hejazi, Mehrnaz S. Ohadi Rafsanjani, Amene Alvari, Malik Zainul Abdin, and Mohammed Samim
- Subjects
business.industry ,Computer science ,Gene Transfer Techniques ,Bioengineering ,Gene transfer ,Nanotechnology ,Genetically modified crops ,Plants, Genetically Modified ,Applied Microbiology and Biotechnology ,Biotechnology ,Plant development ,Biotransformation ,Liposomes ,Agrobacterium species ,Nanoparticles ,business - Abstract
During the past epoch we have gone through the remarkable progress in plant gene transformation technology. The production of transgenic plants is considered as a valuable tool in plant research and the technology is extensively applied in phytomedicines and agricultural research. Gene transformation in plants is normally carried out by Agrobacterium species, application of some chemicals and physical techniques (electroporation, microprojectile, etc.). Now a days with better efficacy and reproducibility, novel technologies for the direct gene transfer like liposome, positively charged liposome (lipofectin) and nanoparticle based delivery systems are used for genetic transformation of plants. In this review, we have enlightened the novel nanotechnologies like liposome, Carbon nano-tube and nanoparticles with their current status and future prospects in transgenic plant development. Moreover, we have also highlighted the limitations of conventional techniques of gene transfer. Furthermore, we have tried to postulate innovative ideas on the footprints of established nanotechnology and chemical based strategy with improved efficacy, reproducibility and accuracy along with less time consumption.
- Published
- 2012
43. Synthesis and evaluation of anticancer activity of some novel 6-aryl-2-(p-sulfamylphenyl)-pyridazin-3(2H)-ones
- Author
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Mohammad Sarwar Alam, K. K. Pillai, Syed Ovais, Shamim Ahmad, Sameena Bano, I. G. Rathish, Mohammed Samim, Mymoona Akhter, and Kalim Javed
- Subjects
Hydrochloride ,Cell ,Mice, Nude ,Antineoplastic Agents ,Pharmacology ,Mice ,chemistry.chemical_compound ,Cell Line, Tumor ,Neoplasms ,Drug Discovery ,medicine ,Animals ,Humans ,Moiety ,Cell Proliferation ,Sulfonamides ,Chemistry ,Melanoma ,Organic Chemistry ,Cancer ,General Medicine ,medicine.disease ,Acute toxicity ,Pyridazines ,Leukemia ,medicine.anatomical_structure ,Cell culture ,Drug Screening Assays, Antitumor - Abstract
Absract A series of novel pyridazinone derivatives bearing benzenesulfonamide moiety ( 2a – h ) has been synthesized by the condensation of appropriate aroylacrylic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Five derivatives ( 2a , 2b , 2d , 2g and 2h ) were evaluated for their anticancer activity toward human cancer cell lines by the National Cancer Institute. The 2h showed remarkable activity against SR (leukemia) and NCI-H522 (non-small cell lung) with a GI 50 value of less than 0.1 μM. It also displayed good activity against leukemia (CCRF-CEM, HL-60 (TB), K-562, MOLT-4, RPMI-8226), non-small cell lung cancer (NCI-H460), colon (HCT-116, HCT-15, HT29, KMI2, SW-620), CNS (SF-295), melanoma (MALME-3M, M14, MDA-MB-435 SK-MEL-5), ovarian (OVCAR-3, NCI/ADR-RES) and breast (MCF7) cancer cell lines with a GI 50 less than 1.0 μM. The acute toxicity study of 2h indicated that it is well tolerated intra-peritoneally (400 mg/kg) by athymic nude mice. The 2h may possibly be used as lead compound for developing new anticancer agents.
- Published
- 2012
44. Synthesis and blood glucose lowering activity of some novel benzenesulfonylurea derivatives substituted with 6-aryl-4,5-dihyropyridazin-3(2H)-ones
- Author
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Syed Ovais, Hinna Hamid, Kalim Javed, Mohammad Sarwar Alam, Rafia Bashir, Shafiya Yaseen, and Mohammed Samim
- Subjects
medicine.drug_class ,Aryl ,Organic Chemistry ,Pharmacology ,Carbon-13 NMR ,medicine.disease ,Sulfonylurea ,chemistry.chemical_compound ,chemistry ,Diabetes mellitus ,medicine ,Proton NMR ,Acetone ,Anhydrous ,Gliclazide ,General Pharmacology, Toxicology and Pharmaceutics ,medicine.drug ,Nuclear chemistry - Abstract
Five (2a–e) benzenesulfonylurea derivatives bearing pyridazinone were synthesized by refluxing the appropriate 6-aryl-2-(p-sulfamylphenyl)-4,5-dihydropyridazine-3(2H)-one with benzylisocyanate in dry acetone over anhydrous K2CO3. These compounds were characterized by elemental analysis and various spectroscopic techniques viz; IR, 1H NMR, 13C NMR, and MS data. These compounds (2a–e) at the dose of 20 mg/kg were tested for blood glucose lowering activity in glucose-fed hyperglycemic normal rats. Compound 2b showed more potent anti-hyperglycemic activity than the standard drug gliclazide. The compound 2b was also tested for its hypoglycemic effect in fasted normal rats. It also showed significant hypoglycemic effect (but less than that of gliclazide).
- Published
- 2012
45. Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti-Inflammatory and Anti-Proliferative Agents
- Author
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Alhamzah Dh, Hameed, Syed, Ovais, Raed, Yaseen, Pooja, Rathore, Mohammed, Samim, Surender, Singh, Kalicharan, Sharma, Mymona, Akhtar, and Kalim, Javed
- Subjects
Male ,Cyclooxygenase 2 Inhibitors ,Anti-Inflammatory Agents, Non-Steroidal ,Antineoplastic Agents ,Carrageenan ,Structure-Activity Relationship ,Cell Line, Tumor ,Animals ,Edema ,Humans ,Phthalazines ,Female ,Sulfones ,Drug Screening Assays, Antitumor ,Rats, Wistar - Abstract
The chemistry of phthalazine derivatives has been of increasing interest since many of these compounds have found many chemotherapeutic applications. So this study aims to synthesize a library of phthalazine derivatives and to investigate their anti-inflammatory and anti-proliferative activities. Sixteen new phthalazinone derivatives (2a-p) were synthesized and tested for their in vitro antiproliferative and in vivo anti-inflammatory activities. All the synthesized compounds were identified and characterized by IR, (1) H NMR, (13) C NMR spectroscopy, and MS. Two compounds, 2b and 2i, showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib in the carrageenan-induced rat paw edema model at 3 and 5 h, respectively. Three compounds (2h, 2j, and 2g) showed moderate sensitivity toward the renal cancer cell line UO-31.
- Published
- 2015
46. Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors
- Author
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Mohammed Samim, Pooja Rathore, Deniz Ekinci, Murat Şentürk, Syed Ovais, Alhamzah Dh. Hameed, Kalim Javed, Claudiu T. Supuran, Raed Yaseen, Ondokuz Mayıs Üniversitesi, and Belirlenecek
- Subjects
Gene isoform ,Carbonic Anhydrase I ,Stereochemistry ,Carbonic anhydrase II ,Clinical Biochemistry ,Pharmaceutical Science ,01 natural sciences ,Biochemistry ,Isozyme ,Carbonic Anhydrase II ,Structure-Activity Relationship ,Carbonic anhydrase ,Drug Discovery ,medicine ,Structure–activity relationship ,Humans ,Carbonic Anhydrase Inhibitors ,Molecular Biology ,chemistry.chemical_classification ,Sulfonamides ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Enzyme inhibitors ,0104 chemical sciences ,Sulfonamide ,Pyridazines ,010404 medicinal & biomolecular chemistry ,Drug Design ,biology.protein ,Molecular Medicine ,Human carbonic anhydrase ,Acetazolamide ,medicine.drug - Abstract
A series of sulfonamide derivatives (2a-l) incorporating substituted pyridazinone moieties were investigated for the inhibition of two human cytosolic carbonic anhydrase isoforms, hCA I and hCA II. All these compounds, together with the clinically used sulfonamide acetazolamide were investigated as inhibitors of the physiologically relevant isozymes I and II. These sulfonamides showed very strong inhibition against all these isoforms with K-I's in the range of 0.98-8.5 nM which makes such molecules possible to be used as leads for discovery of novel effective CA inhibitors targeting other isoforms with medicinal chemistry applications. (C) 2016 Elsevier Ltd. All rights reserved., TUBITAK (The Scientific and Technological Research Council of Turkey) [114Z731], This study was financed by TUBITAK (The Scientific and Technological Research Council of Turkey) (Project no: 114Z731) for (MS).
- Published
- 2015
47. Nanoencapsulation of DMSA monoester for better therapeutic efficacy of the chelating agent against arsenic toxicity
- Author
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Vinay Lomash, Abhishek Yadav, A.K. Babbar, Mohammed Samim, Rashi Mathur, Swaran J.S. Flora, Anil K. Mishra, Mahabir Parshad Kaushik, Pramod Kushwaha, and Uma Pathak
- Subjects
Male ,Sodium arsenite ,Materials science ,Stereochemistry ,Biomedical Engineering ,Medicine (miscellaneous) ,chemistry.chemical_element ,Arsenic poisoning ,Bioengineering ,Development ,Pharmacology ,Kidney ,Arsenic ,chemistry.chemical_compound ,Mice ,Metal poisoning ,Arsenic Poisoning ,medicine ,Animals ,General Materials Science ,Chelation ,Chelation therapy ,Rats, Wistar ,Chelating Agents ,Drug Carriers ,Arsenic toxicity ,Kidney metabolism ,Brain ,medicine.disease ,Rats ,chemistry ,Liver ,Nanoparticles ,Rabbits ,Succimer - Abstract
Aims: Exposure to toxic metals remains a widespread occupational and environmental problem in world. Chelation therapy is a mainstream treatment used to treat heavy metal poisoning. This paper describes the synthesis, characterization and therapeutic evaluation of monoisoamyl 2,3-dimercaptosuccinic acid (MiADMSA)-encapsulated polymeric nanoparticles as a detoxifying agent for arsenic poisoning. Materials & Methods: Polymeric nanoparticles entrapping the DMSA monoester, which can evade the reticulo-endothelial system and have a long circulation time in the blood, were prepared. Particle characterization was carried out by transmission electron microscopy and dynamic light scattering. An in vivo study was conducted to investigate the therapeutic efficacy of MiADMSA-encapsulated polymeric nanoparticles (nano-MiADMSA; 50 mg/kg orally for 5 days) and comparison drawn with bulk MiADMSA. Swiss albino mice exposed to sodium arsenite for 4 weeks were treated for 5 days to evaluate alterations in blood, brain, kidney and liver oxidative stress variables. The study also evaluated the histopathological changes in tissues and the chelating potential of the nanoformulation. Results: Our results show that nano-MiADMSA have a narrow size distribution in the 50-nm range. We observed an enhanced chelating potential of nano-MiADMSA compared with bulk MiADMSA as evident in the reversal of biochemical changes indicative of oxidative stress and efficient removal of arsenic from the blood and tissues. Histopathological changes and urinary 8-OHdG levels also prove better therapeutic efficacy of the novel formulation for arsenic toxicity. Conclusion: The results from our study show better therapeutic efficacy of nano-MiADMSA in removing arsenic burden from the brain and liver.
- Published
- 2014
48. Fabrication of nanoadjuvant with poly-ε-caprolactone (PCL) for developing a single-shot vaccine providing prolonged immunity
- Author
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Mohammed Samim, Madhusudan Bhat, C.K. Prashant, Amar Singh, Amit K. Dinda, Manoj Kumar, Ankit Saxena, Sandeep Kumar Srivastava, and Farhan Jalees Ahmad
- Subjects
Materials science ,medicine.medical_treatment ,Antigen presentation ,Biophysics ,Macrophage polarization ,Pharmaceutical Science ,Bioengineering ,Spleen ,Booster dose ,poly-ε-caprolactone nanoparticles ,Cell Line ,Biomaterials ,Lactones ,Mice ,Immune system ,Antigen ,Adjuvants, Immunologic ,adjuvant ,International Journal of Nanomedicine ,T-Lymphocyte Subsets ,vaccine ,Drug Discovery ,medicine ,Tetanus Toxoid ,Animals ,Humans ,Nanotechnology ,Particle Size ,Caproates ,Original Research ,Antigen Presentation ,Vaccines ,Macrophages ,Organic Chemistry ,Toxoid ,technology, industry, and agriculture ,General Medicine ,Molecular biology ,medicine.anatomical_structure ,Nanomedicine ,Immunology ,Nanoparticles ,antigen cross-presentation ,Female ,Adjuvant - Abstract
Purpose The aim of the study was to load a model antigen, tetanus toxoid (TT), in poly-ε-caprolactone nanoparticles (PCL NPs) of two size ranges, ie, mean 61.2 nm (small) and 467.6 nm (large), and study its effect on macrophage polarization as well as antigen presentation in human monocyte-derived macrophages in vitro, along with humoral and cell-mediated immune (CMI) response generated in Swiss albino mice following immunization with the TT-loaded NPs. Materials and methods PCL NPs were synthesized by solvent evaporation. The antigen-loaded PCL NPs were characterized for size, zeta potential, and protein-release kinetics. Swiss albino mice were immunized with the antigen-loaded PCL NPs. Flow cytometry was used to quantify interferon-γ- and interleukin-4-secreting cluster of differentiation (CD)4+ and CD8+ T cells in the spleen, and enzyme-linked immunosorbent assay was used to quantify anti-TT antibody levels in the serum of immunized mice. Results Small PCL NPs generated an M1/M2 type polarization of human blood monocyte-derived macrophages and T helper (Th)1/Th2 polarization of autologous CD4+ T cells. Efficient CD8+ T-cell responses were also elicited. Large PCL NPs failed to cause any type of macrophage polarization. They did not elicit efficient CD8+ T-cell responses. Conclusion TT-loaded small PCL NPs were able to generate persistent and strong CMI and humoral responses against TT 2 months after single injection in mice without booster dose. This biodegradable nanoadjuvant system may help to develop single-shot immunization for prolonged immunity without booster doses. The capability of enhanced CMI response may have high translational potential for immunization against intracellular infection., Video abstract
- Published
- 2014
49. Synthesis and evaluation of some new pyrazoline substituted benzenesulfonylureas as potential antiproliferative agents
- Author
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Kalim Javed, Alhamzah Dh. Hameed, Mohammed Samim, Pooja Rathore, Rakesh Gupta, Shafiya Yaseen, Syed Ovais, Rafia Bashir, Raed Yaseen, and Firasat Hussain
- Subjects
Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Pyrazoline ,Antineoplastic Agents ,Biochemistry ,chemistry.chemical_compound ,Structure-Activity Relationship ,Cell Line, Tumor ,Drug Discovery ,medicine ,Humans ,Molecular Biology ,Cell Proliferation ,Dose-Response Relationship, Drug ,Molecular Structure ,Organic Chemistry ,Cancer ,medicine.disease ,In vitro ,Sulfonylurea Compounds ,chemistry ,Cell culture ,Antiproliferative Agents ,Molecular Medicine ,Pyrazoles ,Growth inhibition ,Drug Screening Assays, Antitumor ,Human cancer - Abstract
Twenty six new pyrazoline substituted benzenesulfonylureas (2a–z) were synthesized and tested for in vitro anticancer activity. Fourteen derivatives (2i, 2k–2p, 2r, 2s–2x) were screened for their antiproliferative activity towards 60 human cancer cell lines by the National Cancer Institute (USA). Among them four compounds (2i, 2n, 2v and 2x) exhibited significant growth inhibition and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compounds 2i, 2n, 2v and 2x showed effective growth inhibition (GI50 MID) values of 2.62, 3.93, 3.33, 3.74 μM respectively beside cytostatic activity TGI (MG-MID) values of 8.42, 65.80, 24.00 and 36.06 μM respectively. The compound 2i displayed remarkable antiproliferative activity in 8 different cell lines with GI50 less than 2 μM. Compounds 2n, 2v and 2x also displayed good antiproliferative activity against 11, 18 and 14 different cell lines respectively with GI50 less than 3 μM.
- Published
- 2013
50. ChemInform Abstract: Synthesis and Biological Evaluation of 4-Arylphthalazones Bearing Benzenesulfonamide and Anti-Inflammatory and Anticancer Agents
- Author
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Surender Singh, Syed Ovais, Vinod Nair, Shafiya Yaseen, Pooja Rathore, Mohammed Samim, Kalim Javed, and Rafia Bashir
- Subjects
Bearing (mechanical) ,medicine.drug_class ,law ,Chemistry ,medicine ,General Medicine ,Condensation reaction ,Combinatorial chemistry ,Anti-inflammatory ,Biological evaluation ,law.invention - Abstract
The synthesized compounds are tested for their anti-inflammatory and anticancer activities.
- Published
- 2013
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