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Abstract: This article reports the microwave-assisted synthesis, characterization, and evaluation of some -4-one derivatives (2a-2h) for their in-vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv strain by microplate Alamar blue assay (MABA) method. All these final compounds (2a-2h) were synthesized from Schiff’s bases, 1-arylidene-2-(4-methylphenyl)hydrazines (1a-1h), and thioglycolic acid by using zinc chloride as a catalyst. Compounds (1a-1h) were synthesized from the reaction of 4-methylhydrazine and appropriate aromatic aldehydes by Schiff’s reaction. Among the target compounds, 2-(4-ethoxyphenyl)-3-(4-methylarylamino)thiazolidin-4-one (2f) and 2-(4-ethylphenyl)-3-(4-methylarylamino)thiazolidin-4-one (2g) were promising with a minimum inhibitory concentration (MIC) of 12.5 μg/mL against M. tuberculosisH37Rv. Based on the preliminary results, compounds 2f and 2g were considered as lead compounds for the advanced design and development of antimycobacterial agents.

Aim: The current study observed the antidiabetic effect of Vasant Kusumakar Ras, an Ayurvedic polyherbal formulation, in alloxan-induced and dexamethasone-induced diabetic rats. Materials and Methods: Alloxan (120 mg/kg, i.p.) and dexamethasone sodium phosphate (5 mg/kg, i.p.) were used to induce diabetes in rats. The oral antidiabetic activity of Vasant Kusumakar Ras was evaluated by single doses of Vasant Kusumakar Ras (400 and 600 mg/kg, p.o.) in albino rats during a 10-day treatment period, with the effect of the Vasant Kusumakar Ras on blood glucose levels and serum lipid parameters measured on 0, 7th, and 11th day. Glibenclamide (5 mg/kg, p.o.) was used as the reference drug. Results: In alloxan-induced diabetic rats, the elevated levels of blood glucose significantly (p < 0.05) decreased after oral administration of Vasant Kusumakar Ras (400 mg/kg and 600 mg/kg), and Glibenclamide (5 mg/kg). When compared to the diabetic control group, treatment with Vasant Kusumakar Ras and Glibenclamide for 10 days reduced total cholesterol (TC) significantly (p < 0.001). Treatment with Vasant Kusumakar Ras and Glibenclamide for 10 days, significantly (p < 0.001) decreased low-density lipoprotein (LDL) level when compared to the diabetic control group. In dexamethasone-induced diabetic rats, all rats given with dexamethasone and Vasant Kusumakar Ras (400 mg/kg and 600 mg/kg) showed a significant (p

A new liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) method has been developed and validated for alfuzosin quantification in human plasma using amlodipine as an internal standard (IS). The analyte and IS were extracted using a mixture of diethyl ether-dichloroethane (70 : 30, v/v). The samples were separated on a Waters XBridge HILIC column, where a tandem mass spectrometer with a turbo ion spray interface was used for analytes detection. The chromatographic run time of the method was 4.0 min. The method was linear over the concentration range of 0.20–30 ng/mL for alfuzosin. On evaluating the selectivity of the method, no interference was observed for the two MRM transitions of alfuzosin and MRM transition for amlodipine at their respective retention times. The mean matrix effect for alfuzosin was excellent at 99.9%. The method was carefully tested for linearity, system suitability, precision and accuracy. Intra- and inter-day accuracy and precision were evaluated at three quality control levels (LQC, MQC and HQC). Stability of alfuzosin was evaluated under diverse storage conditions. The percentage accuracy for 1 : 2 diluted samples was 93.2% of their nominal concentration with the coefficient of variation of 5.6%. Hence, a highly precise, accurate, rapid, selective and sensitive LC-ESI-MS/MS method has been developed and validated for the quantification of alfuzosin in human plasma using amlodipine as the internal standard.

Wound healing is the repair process of injury on the skin and other soft tissues. After injury, an inflammatory response occurs and tissue cells below the dermis begin to increase collagen formation. Later, the epithelial tissue is regenerated. There are three stages of wound healing process: inflammation, proliferation and remodeling. Traditionally, Ficus benghalensis plant has been used for wound healing but no clear scientific data are available related to this activity. The present work was designed to explore the wound-healing efficacy of petroleum, ethanolic and aqueous extracts of F. benghalensis leaves as evaluated on excision wound models. These leaves extracts were studied for their phytochemicals by means of different chemical tests. Parameters studied include the rate of wound contraction and period of complete epithelialization of incision wound. Student’s t-test was used to analyze the results obtained from this study and confidence level P < 0.05 was considered significant. All the petroleum, ethanolic and aqueous extracts of F. benghalensis leaves were found to possess significant wound-healing activity, which was evidenced by decrease in the period of epithelialization and increase in the rate of wound contraction. The obtained results showed that all extracts of F. benghalensis leaves were capable of accelerated wound-healing activity comparable with a control drug.

Fluoroquinolones, a class of compound, actviainhibiting DNA gyrase and topoisomerase IV enzymes.

Risedronate is a nitrogen-containing bisphosphonate for the treatment and prevention of postmenopausal osteoporosis. The current work aims to develop a novel green HPLC-UV method for the rapid analysis of risedronate sodium in bulk and tablet formulation. The analyzed samples were separated on Waters Atlantis dC18 (150 mm × 3.9 mm; 5 μm) column using a green mobile phase consisting of potassium phosphate buffer pH 2.9 and potassium edetate buffer pH 9.5 in a ratio of 1:2, the final pH was adjusted to 6.8 with phosphoric acid, the mobile phase was pumped at a rate of 1.0 mL/min, with column temperature set at 30°C, eluted samples were detected at 263 nm and the chromatographic run time was 3.0 minutes. The method was found to be linear over the concentration range of 14-140 μg/mL with a correlation coefficient (r2) of 0.9994. Accuracy and precision were evaluated from three QC samples (LQC, MQC and HQC) together with the five calibrators where the percentage accuracy was found to be 101.84%. Processed quality control samples of risedronate sodium were tested for stability at different conditions, short term, long term and freeze- thaw stability. The current method was further extended to study the content uniformity of Actonel® tablets following United States Pharmacopoeia (USP) guidelines. The proposed method was fully validated as per ICH guidelines.

Background and Objective: Bambusa arundinaceae leaves are widely used for treating numerous diseases in Indian traditional medicine. The current study explored the neuroprotective effect of Bambusa arundinaceae leaves ethanolic extract (EEBA) on memory impairment induced by streptozotocin (STZ) in mice. Materials and Methods: The neuroprotective effect of EEBA (100 and 200 mg kgG1 b.wt., p.o.) was assessed in the Morris Water Maze (MWM) test, Pole Climbing Test (PCT) and in the Elevated Plus Maze (EPM) test in comparison with standard piracetam (100 mg kgG1 b.wt., i.p.). The activity of acetylcholinesterase (AChE), malondialdehyde (MDA) and reduced glutathione (GSH) were also measured in various mice brain regions. Gene expression was also performed by RT-PCR and western blot test. Results: Treatment with EEBA 200 mg kgG1 showed a significant effect in all behavioral tests that demonstrated neuroprotective activity. EEBA treatment significantly reduced the AChE and MDA levels in mice brain regions, along with a rise in GSH level. RT-PCR results showed Bax and Bak mRNA were down-regulated, while Bcl-2 mRNA and protein were up-regulated in EEBA (200 mg kgG1) group. NR1, NR2B and GAP-43 proteins lead to the reduction of brain cell damage. EEBA 200 mg kgG1 showed a significant effect by shielding against STZ induced brain damage by interacting with these proteins. Conclusion: The effect of EEBA (200 mg kgG1 b.wt.) on behavioral and biochemical parameters was comparable with that observed in piracetam treated rats. These findings indicated that EEBA may exert a neuroprotective effect that may be accredited to inhibiting AChE and regulating the protein expression in the brain as well as its antioxidant mechanisms.

The current study proposed the in vivo antidepressant and anxiolytic activities of the aqueous extract from Solanum melongena fruits (AESM) in mice. The mice were administered with AESM 100 and 200 mg/kg, p.o. for anxiolytic (elevated plus maze test (EPMT) and locomotor action), and antidepressant (forced swimming test (FST) and tail suspension test (TST) activities. The possible mechanism of action of Solanum melongena fruits was also analyzed by measuring the level of serotonin (5HT), monoamine oxidase enzyme (MAO-A) and GABA activity in the blood of experimental animals. When mice were treated for seven days with 100 (*** P < 0.01) and 200 mg / kg, AESM p.o. and 2 mg / kg, diazepam p.o. (*** P < 0.001) showed significant increases in the average time expended and the number of entries into the open arms of the EPMT, as compared to control group in dose dependent fashion. However, when mice were treated with standard Imipramine (10 mg/kg) (***P < 0.001), AESM 100 mg/kg (**P < 0.01) and 200 mg/kg (*P < 0.05) after day 7, there was significant reduction in locomotor activity in both TST and FST in dose dependent fashion. Monoamine oxidase - A level in the entire brain of mice were significantly reduced when pretreated with AESM 100 and 200 mg/kg, p.o. for 7 days as compared to control group in dose dependent fashion. The mechanisms of action of antidepressant effect of Solanum melongena fruits extract act by increasing serotonin and also GABA. Moreover, the extract also decreased the MAO-A enzyme in the experimental animals. These results demonstrated that both of these doses. Of aqueous extract from Solanum melongena fruits possess potential antidepressant activities in dose dependent fashion.

Graphical abstract, Traditional pertinence Argyreia speciosa Sweet (Linn.), belongs to the family convolvulaceae, a traditional Indian medicinal herb, has been used to treat acute/chronic ulcers, gonorrhea, rheumatoid arthritis and several nervous disorders having a long history. Aim of the study A broad spectrum approach of this work was to find out the antioxidant activity of Argyreia speciosa seeds, in vitro and in vivo antioxidant assay were performed. Material and methods Total phenolic content (TPC), reducing power (RP), antioxidant activity (AOA), O2·- (superoxide anion), DPPḢ (1,1-diphenyl-2-picrylhydrazyl) and ˙OH (hydroxyl) radicals scavenging activities, GSH (glutathione), CAT (catalase), SOD (superoxide dismutase) and LPO (lipid peroxidase) are the major parameters which were studied for determining in vitro and in vivo antioxidant property of seed extract & their six fractions obtained from A. speciosa. Carbon tetrachloride (CCl4) induced rat model was used to determine in vivo antioxidant assay of extract and its fractions. Results Butanol fraction (AS-BF) showed strong antioxidant property and protected oxidative DNA damage. AS-BF was found best as compared to all other fraction for determining antioxidant property of seeds with the reduction in lipid peroxide formation and increment in GSH, CAT and SOD. AS-BF showed the presence of phenolic compounds viz. gallic acid, chlorogenic acid, and ellagic acid. Conclusion From these results, it was proved that A. speciosa seeds prevent tissue damage due to oxidative stress with strong antioxidant activity.

Free radicals are the byproducts of physiological aerobic cellular metabolism. Intrinsic antioxidant system plays its pivotal function in prevention of any loss due to free radicals. Though, incorporation or excess production of free radicals from environment to living system or imbalanced defense mechanism of antioxidant system leads to severe consequences like neuro-degeneration. Sensory or functional loss occurs in neural cells in neurodegenerative diseases. Besides numerous other genetic or environmental factors, oxidative stress is the major cause which leads to damage of neurons and production of neurodegenative diseases. However, oxygen is vital for existence, excessive reactive oxygen species production and imbalanced metabolism leads to a variety of diseases such as aging, Parkinson’s disease, Alzheimer’s disease, and many other neurodegenative diseases. Free radicals toxicity contributes to DNA and proteins damage, tissue damage, inflammation and consequent cellular apoptosis. Neuroprotection is a broad term commonly used to refer therapeutic strategies that can prevent, delay or even reverse neuronal damage. Since thousands of years, lots of medicinal plants have been used in a group of herbal preparations of Ayurveda (Indian traditional health care system) named Rasayana because of the antioxidant principles present in it, responsible for their medicinal use in neurodegenerative diseases. This work constitutes a literature review on natural products contain antioxidant principles used in the treatment of neurodegenerative disease.

Background: Overexpression of Histone deacetylase 1 (HDAC1) is responsible for carcinogenesis by promoting epigenetic silence of tumour suppressor genes. Thus, HDAC1 inhibitors have emerged as the potential therapeutic leads against multiple human cancers, as they can block the activity of particular HDACs, renovate the expression of several tumour suppressor genes and bring about cell differentiation, cell cycle arrest and apoptosis. Methods: The present research work comprises atom-based 3D-QSAR, docking, molecular dynamic simulations and DFT (density functional theory) studies on a diverse series of hydroxamic acid derivatives as selective HDAC1 inhibitors. Two pharmacophoric models were generated and validated by calculating the enrichment factors with the help of the decoy set. The Four different 3D-QSAR models i.e., PLS (partial least square) model, MLR (multiple linear regression) model, Field-based model and GFA (Genetic function approximation) model were developed using ‘PHASE’ v3.4 (Schrödinger) and Discovery Studio (DS) 4.1 software and validated using different statistical parameters like internal and external validation. Results and Discussion: The results showed that the best PLS model has R2=0.991 and Q2=0.787, the best MLR model has R2= 0.993 and Q2= 0.893, the best Field-based model has R2= 0.974 and Q2= 0.782 and the best GFA model has R2= 0.868 and Q2= 0.782. Cross-validated coefficients, (rcv 2) of 0.967, 0.926, 0.966 and 0.829 was found for PLS model, MLR, Field based and GFA model, respectively, indicated the satisfactory correlativity and prediction. The docking studies were accomplished to find out the conformations of the molecules and their essential binding interactions with the target protein. The trustworthiness of the docking results was further confirmed by molecular dynamics (MD) simulations studies. Density Functional Theory (DFT) study was performed which promptly optimizes the geometry, stability and reactivity of the molecule during receptor-ligand interaction. Conclusion: Thus, the present research work provides spatial fingerprints which would be beneficial for the development of potent HDAC1 inhibitors.

The aim of the current study was to evaluate and compare the toxicities of different types of mosquito repellents i.e. coils, mats and liquid vapors in animal models. Different types of mosquito repellents including liquid vaporizers, coils and mats have been extensively used by the people to get protection from the mosquitoes and diseases associated with them. The active constituents of these repellents include; allethrins, pyrethrins, paraffin and various other derivatives, are well known for their toxicities. Exposure of albino mice to these repellents for 3 h per day over a period of 20 days produced significant toxicological effects on vital body organs including; liver, lungs, kidneys, brain and heart. The order of toxicity of different repellents on nervous and hepatic tissues was found to be: Coil > Liquid > Mat while in renal and cardiac tissues, the coil was again found to be the most toxic one, mat with medium toxicity whereas liquid as least toxic (Coil > Mat > liquid). Lungs tissues are almost equally affected by all the repellants. On the basis of current findings, it has been concluded that exposure to various types of mosquito repellents can be deleterious to health and can cause various health related issues by producing pathological changes in the vital organs. Keywords: Allethrin, Mosquito repellents, Subchronic toxicity, Vital organs, Mice

Ethyl 2-(1H-pyrazol-1-yl)acetate (1) was synthesized by the reaction of ethylchloroacetate with 1H-pyrazole, Then compound (1) refluxed with hydrazine hydrate to get 2-(1H-pyrazol-1-yl) acetohydrazide (2). Compound (2) was reaction with appropriate aryl aldehyde to get schiff bases N'-arylidine-2-(1H-pyrazol-1-yl)acetohydrazide derivatives (3a-3f). schiff’s base (3a-3e) were cyclized by reflux with acetic anhydride to get new 1-(5-((1H-pyrazol-1-yl)methyl)-2-aryl-1,3,4-oxadiazol-3(2H)-yl)ethanone derivatives (4a-4e). The structures of the synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, mass spectra, and elemental analysis data. Synthesized compounds (4a-4e) were evaluated as antibacterial agents against some common pathogenic bacteria Gram-positive (Staphylococcus aureus, Streptococcus pyogenes) and Gram-negative bacteria (Escherichia coli, Psuedomonas aeruginosa). The result of antibacterial activity was compared with standard drugs (Ciprofloxacin and Tetracycline).

The pyrethroid toxicants, fatal at high doses, are found as remnants of crop pesticides and ingredients of commercially available insecticides. The toxic effects of high-content insecticidal pyrethroid formulations are available in 0.05 g, 1.17 g, and 0.04 g pyrethroid-instilled products, namely burning coils, pyrethroid-soaked mats, and liquid formulations of pyrethroids that release pyrethroid vapor/smoke upon heating. They provided 5.46 g/kg, 21.15 g/kg, and 4.24 g/kg of toxicants to the experimental animals over a total of 3 weeks/5 h per os (p.o.) administration, producing necrosis, hyperemia, and fatty changes in the liver, fiber separation in cardiac muscles, atrophy, lymphatic infiltration, blood vessel congestion, and hyperemia in the heart tissues of the experimental animals. The glomerular tuft necrosis, cytoplasmic degeneration of renal tubular cells, necrotic tubules, congestion, and dilatation of blood vessels were observed in the kidney tissue of intoxicated animals. Air-space enlargement, interstitial inflammation, lymphocyte infiltration aggregates, connective tissue infiltration by inflammatory cells, and hyperemia were found in the lung tissues. The pyrethroid toxicants also produced nervous tissue degeneration and decreased neurons in the brain, which were observed through histopathological examinations of the brain, lungs, heart, kidneys, and liver. The protective effects of ascorbic acid (AA/vitamin C) and &alpha, tocopherol (E307/vitamin E) at 100 mg/kg oral doses administered daily for the entire period of the toxicant exposure of three weeks to the experimental mice, aged between 3&ndash, 4 months and weighing &asymp, 30 g, ameliorated the tissue damage, as observed through the histopathological examinations. The ascorbic acid caused recovery of the liver, kidney, brain, and heart tissue damage, while &alpha, tocopherol was effective at ameliorating the damage in the kidneys and lung tissue compared with the control groups. The high levels of tissue damage recovery suggested a prophylactic effect of the concurrent use of ascorbic acid and &alpha, tocopherol for the subjects under the exposure of pyrethroids.

Histone deacetylase inhibitors (HDACi) have been demonstrated as an emerging class of anticancer drugs involved in regulation of gene expression and chromatin remodeling thus indicating valid targets for different types of cancer therapeutics. The pan-deacetylase inhibitor panobinostat (Farydac®, LBH589) is developed by Novartis Pharmaceuticals and a newly US FDA approved drug for the multiple myeloma. It is under clinical investigation for a range of hematological and solid tumors worldwide in both oral and intravenous formulations. Panobinostat inhibits tumor cell growth by interacting with acetylation of histones and nonhistone proteins as well as various apoptotic, autophagy-mediated targets and various tumorigenesis pathways involved in the development of cancer. The current article summarizes the status of panobinostat in gastrointestinal cancers. Preclinical and clinical data suggest that panobinostat has potential inhibitory activity in hepatocellular, pancreatic, colorectal, gastric and gastrointestinal stromal tumors. Clinical evaluations of panobinostat are currently underway. Herein, we have also reviewed the rationale behind the combination therapy under the trials and possible future prospective for the treatment of GI tumors.

The aim of this study was to investigate the anticonvulsant and neuroprotective effects of methanolic extract of Cinnamomum camphora leaves (MECC) in albino wistar rats against maximal electroshock seizure (MES) and seizures induced by pentylenetetrazol (PTZ) models. Acetylcholinesterase (AChE) activity and oxidative stress parameters like malondialdehyde (MDA) and reduced glutathione (GSH) were estimated in the brains after completion of the anticonvulsant studies. MECC (50 and 100 mg/kg b.w., p.o.) exhibited anticonvulsant activity as indicated by significant (P

Total extracts of Drechslera rostrata and Eurotium tonophilum in addition of two isolated compounds from their cultures [di-2-ethylhexyl phthalate (H1) and 1,8-Dihydroxy-3-methoxy-6-methyl-anthraquinone (H2)] were tested for their antitumor activity using four human carcinoma cell lines. Antitumor activity was assessed by performing MTT assay to check the % cell viability. The % viability of HCT-116 (colon carcinoma), HeLa (cervical carcinoma), HEp-2 (larynx carcinoma) and HepG-2 (hepatocellular carcinoma) cells decreased after treatment with Drechslera rostrata and Eurotium tonophilum extracts, these effects were ranged from 059.0 ± 0.1 to 217.0 ± 0.3 µg/ml on all types of cancer cells. The best activity was recorded for Eurotium tonpholium extract (054.5 ± 0.3, 059.0 ± 0.5 and 059.0 ± 0.1 for HEp-2, Hela, and HepG-2 respectively). The isolated compounds (H1&H2) were found to be responsible about the activities because they recorded the lowest IC50 on tested cell lines with range of 9.5–20.3 μg/ml. Vinblastine sulphate was used as a reference standard and showed in vitro anticancer activity. This study demonstrated that all extracts and isolated compounds have antitumor activity against HCT-116, HeLa, HEp-2 and HepG-2 cells.

Ultrasound-assisted extraction (UAE) or ultrasonic extraction technology has been used for the isolation of bioactive compounds from Argyreia speciosa (Linn. f.) Sweet plant (family: Convolvulaceae). Argyreia speciosa is an Indian traditional medicinal plant having strong evidence of various properties widely used in Ayurveda. Dried flowers were used for extraction and the response surface methodology (RSM) was used to optimize the conditions of extraction for the yield of total phenolics and antioxidants from A. speciosa flowers (ASF) in respect of three variables: temperature, power, and time. Damage and structural changes of the bioactive compounds were studied by scanning electron microscopy (SEM) and Fourier-transform infrared (FTIR) spectroscopy techniques. The optimum UAE conditions obtained by RSM for the yield of total phenolic content from ASF were 42.41°C temperature, 43.62 % power, and 26.51 min process time and conditions for the maximum antioxidant activity by DPPH radical scavenging were 41.36°C temperature, 57.02 % power, and 26.63 min. These findings showed that the UAE under optimum conditions increased the percentage yield of bioactive compounds. SEM results showed that there was no relevant damage to the cells, and FTIR spectroscopy verified that there were no changes in chemical structure. It has been concluded that UAE method is an effective technique for enhancing the yields of major phenolic compounds from A. speciosa flowers.

Non-nucleosidase reverse transcriptase inhibitors (NNRTIs) are highly promising agents for use in highly effective antiretroviral therapy. We implemented a rational approach for the identification of promising NNRTIs based on the validated ligand- and structure-based approaches. In view of our state-of-the-art techniques in drug design and discovery utilizing multiple modeling approaches, we report here, for the first time, quantitative pharmacophore modeling (HypoGen), docking, and in-house database screening approaches in the identification of potential NNRTIs. The validated pharmacophore model with three hydrophobic groups, one aromatic ring group, and a hydrogen-bond acceptor explains the interactions at the active site by the inhibitors. The model was implemented in pharmacophore-based virtual screening (in-house and commercially available databases) and molecular docking for prioritizing the potential compounds as NNRTI. The identified leads are in good corroboration with binding affinities and interactions as compared to standard ligands. The model can be utilized for designing and identifying the potential leads in the area of NNRTIs.

Wound healing is a complex process in which injured skin and tissues repaired by interaction of a complex cascade of cellular events that generates resurfacing, reconstitution and restoration of the tensile strength of injured skin. It follows β-catenin, extracellular signal regulated kinase (ERK) and Akt signaling pathways. Aegle marmelos L., generally known as bael is found to act as anti-inflammatory, antioxidant and anti-ulcer agent. Furthermore, studies have demonstrated that this Indian traditional medicinal plant, A. marmelos flower extract (AMF) was used for wound injury. Henceforth, the current study was investigated to ascertain the effect of its active constituents in vitro wound healing with mechanism involve in migration of cells and activation of β-catenin in keratinocytes, inhibition of PGE2 in macrophages and production of collagen in fibroblasts. We have taken full thickness wound of rats and applied AMF for 2 weeks. Cutaneous wound healing activity was performed using HaCaT keratinocytes, Hs68 dermal fibroblasts and RAW264.7 macrophages to determine cell viability, nitric oxide production, collagen expression, cell migration and β-catenin activation. Results shows that AMF treated rats demonstrated reduced wound size and epithelisation was improved, involved in keratinocytes migration by regulation of Akt signaling, beta-catenin and extracellular signal-regulated kinase (ERK) pathways. AMF and its active constituent’s increased mRNA expression, inhibited nitric oxide, PGE2 release, mRNA expression of mediators in RAW 264.7 macrophages and enhances the motility of HaCaT keratinocytes in vitro wound healing of rats. Keywords: Aegle marmelos, Akt signaling pathways, Cutaneous wound, Dermal fibroblasts HaCaT keratinocytes

To the article “Standardization and Wound-Healing Activity of Petroleum, Ethanolic and Aqueous Extracts of Ficus Benghalensis Leaves,” by Mohd Imran, Jyoti Nanda Sharma, Mehnaz Kamal, and Mohammad Asif, Vol. 54, No. 10, pp. 1057 – 1062, January, 2021

A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran- 3-yl)-2-(substituted)-acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg-1 body mass during 0.5-4 h, indicating their ability to prevent seizure spread at low doses. Relative to phenytoin, [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(cyclohexyl( methyl) amino)-acetamide] (5i) and [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4-methylpiperidin-1- yl)-acetamide] (5c) demonstrated comparable relative anticonvulsant potency of 0.74 and 0.72, respectively, whereas [(N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4-(furan-2-carbonyl)-piperazin-1-yl)-acetamide] (5f) exhibited the lowest relative potency of 0.16. The ALD50 of tested compounds ranged from 1.604 to 1.675 mmol kg-1 body mass. The ED50 of synthesized compounds ranged from 0.055 to 0.259 mmol kg-1 (~23.4 to 127.6 mg kg-1) body mass. The pharmacophore mapping of the examined compounds on standard drugs (phenobarbital, phenytoin, ralitolin and carbamazepine) strongly suggests that these compounds may exert their anticonvulsant activity via the same established mechanism as that of known drugs.

The comparative study of neuroprotective effect of angiotensin converting enzyme inhibitors against scopolamine-induced neuroinflammation in albino Wistar rats was studied. Male albino rats were administered with scopolamine to induce memory impairment. The standard nootropic agent, piracetam (200 mg/kg b.w., [i.p.]), perindopril (0.1 mg/kg b.w., [i.p.]), enalapril (0.1 mg/kg b.w., [i.p.]), and ramipril (0.1 mg/kg b.w., [i.p.]) were administered in different group of animals for 5 days. On 5(th) day, scopolamine (1 mg/kg b.w., i.p.) was administered after 60 min of the last dose of test drug. Memory function was evaluated in Morris water maze (MWM) test and pole climbing test (PCT). Biochemical estimations like glutathione (GSH), malondialdehyde (MDA), and acetylcholinesterase activity in the brain were estimated after completion of behavior study. All three test groups shows improvement in learning and memory in comparison to control group. Perindopril treated group showed a more effective significant decrease in escape latency time and transfer latency time compared to enalapril and ramipril treated group on day 4 in MWM test and PCT, respectively. Perindopril shows a significant reduction in MDA level and acetylcholinesterase activity and a significant rise in GSH level compared to enalapril and ramipril. The finding of this study indicates that Perindopril is more effective in memory retention compared to enalapril and ramipril.

To study the estrogenic activity of the hydro-alcoholic extract of Bambusa arundinaceae leaves (HEBA) in female Wistar rats. The dried powdered leaves were extracted with hydroalcoholic mixture (60%), and the resultant extract was subjected for phytochemical analyses to identify different phytoconstituents. HEBA were administered to ovariectomized rats for 7 days at three different doses (viz., 200, 300, 400 mg/kg body weight, p.o.) and their estrogenic activity were compared with each of daily treatment with 0.2 mg/kg body weight, i.p. conjugated equine estrogen as a positive control or olive oil as a negative control. Estrogenic activity was evaluated by doing uterotropic assay, vaginal cytology and measurement of vaginal opening in female Wistar rats. Oral administration of HEBA in ovariectomized immature and mature female Wistar rats in a dose of 400 mg/kg b.w. resulted in significant increase in the uterine wet weight (in mg) (224.82 ± 7.01) and (912.25 ± 27.22) when compared with ovariectomized control rats (111.52 ± 3.17) and (506.67 ± 21.39). HEBA (400 mg/kg b.w., p.o.) treated rats, showing only cornified epithelial cells which was an indication of the presence of the estrogen and also showed 100% vaginal opening. It was observed that HEBA possess significant estrogenic activity at 400 mg/kg b.w., p.o. which was evident by uterotropic assay, measurement of vaginal opening, and histopathological changes.

A series of 12, N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide analogs was designed and synthesized to meet the pharmacophore requirement essential for anticonvulsant activity. All the compounds were characterized by IR, 1 H NMR and mass spectral data followed by their anticonvulsant evaluation according to the Antiepileptic Drug Development Program (ADD) protocol. The present study has proved the hypothesis concerning the pharmacophore model with essential binding sites. N-(2-benzoylbenzofuran-3-yl)-3-(4-(2-fluorophenyl)piperazin-1-yl) propanamide, 6h was found to be the most active compound in both maximal electroshock seizure (MES) and subcutaneous metrazol (scMET) seizure test at 30 and100 mg/kg respectively at 0.5 and 4.0 h.

Lawsonia inermis L. is a much branched glabrous shrub or small tree (2-6 m in height), cultivated for its leaves although stem bark, roots, flowers and seeds have also been used in traditional medicine. The plant is reported to contain Lawsone, Esculetin, Fraxetin, Isoplumbagin, Scopoletin, Betulin, Betulinic acid, Hennadiol, Lupeol, Lacoumarin, Laxanthone, Flavone glycosides, Two pentacytic triterpenes. The plant has been reported to have analgesic, hypoglycemic, antimalarial, hepatoprotective, nootropic, immunostimulant, anti-inflammatory, antibacterial, antimicrobial, antifungal, antiviral, antiparasitic, antitrypanosomal, antidermatophytic, antioxidant, anthelmintic, antifertility, tuberculostatic and anticancer properties. It is now considered as a valuable source of unique natural products for development of medicines against various diseases and also for the development of industrial products. This review gives a view mainly on the traditional uses, phytochemistry and pharmacological actions of the plant.

Histone deacetylase (HDAC) inhibitors have been established as a novel class of anticancer agents. The HDAC enzyme plays a vital role in gene transcription for regulation of cell proliferation, migration and apoptosis, immune pathways and angiogenesis. In this work, a series of 49 hydroxamate derivatives with available IC50 data were analyzed by computational method for the identification of leads. 3D-QSAR and pharmacophore modeling investigation were accomplished to identify the crucial pharmacophoric features and correlate 3D-chemical structure with HDAC inhibitory activity. The e-pharmacophore script and phase module were used for development of pharmacophore hypotheses, which characterized the 3D arrangement of molecular features necessary for the presence of biological activity. The 3D-QSAR analyses were carried out for five partial least square (PLS) factor model with excellent information and predictive ability, acquired R2 =0.9824, Q2 =0.8473 and with low standard deviation SD=0.2161. Molecular docking studies showed intermolecular interactions between small molecules and some amino acids, such as GLY140, Zn501, HIS132 and PHE 141 with good GlideScore as compared with that of vorinostat (SAHA).