Search

Abstract: Indole is an important heterocyclic molecule having a number of pharmacologically useful properties. Adolf von Baeyer synthesized indole by reducing oxindole in the presence of a catalytic amount of zinc dust in 1866. A number of studies have been conducted and many more are in the pipeline to investigate the medicinal potential of indole and its derivatives. Indomethacin, Indolmycin, Oxypertine, Yohimbine, Pindolol, and Delavirdine are indole containing drugs that are in high demand in the market. The present study aims to highlight the indole nucleus containing drugs developed by researchers over the last 25 years, with a focus on antibacterial and antifungal properties present in these drugs. The mode of action and Structure–Activity Relationship (SAR) of indole derivatives, which are responsible for antibacterial and other relevant actions, are also highlighted in the present review. To aid scientists in exploring future potential in this domain, the present study includes the key qualities and highlights of each research activity done by researchers especially related to synthetic derivatives of Indoles. All the available information on Indole derivatives was collected via electronic search (using Pubmed, SciFinder, Scirus, Google Scholar, and Web of Science) and the resources available in Central Library, IFTM University, Moradabad were also referred. The present review is based on literature collected and studied over the previous 23 years. This article will aid researchers in the development of new molecules with indole derivatives undoubtedly which must have improved antibacterial and other properties.

In the present review article, different advanced liquid chromatographic techniques and the advanced techniques other than liquid chromatography that are used to estimate the pesticide residues from different plant-based samples are presented. In the beginning of the article, details of pesticides, their health effects and various cell lines used for the related study has been outlined. Afterward, detailed descriptions regarding pesticides classification are inscribed. In the end, recent advancements in the area of analysis of pesticides for herbal drugs are explained. Solid phase micro extraction (SPME) and solid-phase extraction (SPE) are considered as most common method of sample preparation for pesticides and its residual analysis. The most commonly used analytical separation technique for pesticide analysis is liquid chromatography (LC) integrated with mass spectrometry (MS) and MS/MS as Triple Quadrupole Mass Spectrometer (QqQ) for the samples analysis where high level of sensitivity and accuracy is required in quantification.

Bryophyllum pinnatum Lam. (Oken) (Crassulaceae) are commonly known as miracle plant. Traditionally, this plant is used to heal wounds and to treat diarrhoea. For this reason, the main aim of the present study is to evaluate the antidiarrheal activity using castor oil-induced diarrhea model. Loperamide drug (3 mg dose, p.o.) was used as standard drug. The EAE and EE at 200mg dose and 400 mg dose, p.o. respectively produced dose-dependent protection of mice with significant P value (P < 0.001). Both extracts of plant produced dose-dependent and significant P-value (P < 0.001) towards antimotility effect compared with negative control (castor oil) group in model. EE (400 mg dose p.o.) possess better antidiarrheal potential in mice groups due to presence of flavone. 5-methyl-4,5,7- trihydroxy flavone was isolated from the ethanol extract. Finally, it can be concluded that, Bryophyllum pinnatum Lam. (Oken) leaves can be used ethnomedicinally to treat, counterbalance, bulwark, and control diarrhea.

Cancer is a catchall term that refers to a collection of more than one chronic disease that can adversely affect the body, including the organs of the body. These diseases can be grouped together under the umbrella term "cancer." Cancer is a catch-all term that is used to refer to a number of different diseases. During the process of looking for new chemical entities, it was found that certain compounds with a basic nucleus of benzoic acid (BA) exhibit a remarkable anticancer potential. This was discovered while the researchers were looking for new chemical entities. In the sixteenth century, the aromatic chemical known as BA, which is also known as an aromatic carboxylic acid, was discovered. BA is also referred to as an aromatic carboxylic acid. When it comes to the chemical synthesis of a wide range of different active molecules, the utilization of a sizeable quantity of BA as a raw material is absolutely necessary. In addition to being present in a variety of other naturally occurring compounds, the BA moiety is the component that is responsible for the activity of the naturally occurring compounds vanillin, gallic acid, and syringic acid. In the synthesis of a wide variety of synthetic bioactive molecules, the BA scaffold is utilized as a building block. The drugs furosemide, bumetanide, benzocaine, tetracaine, and bexarotene are all examples of molecules that fall into this category. The scope of this review article allows for the discussion of a number of noteworthy and recent achievements of BA derivatives in terms of their effectiveness against cancer.

The purpose of the present research was to synthesize a new series of acetanilide derivatives that would have analgesic and anti-inflammatory properties in laboratory animals (rats). IR spectroscopy, 1HNMR spectroscopy and Mass spectroscopy were used to confirm the structures of freshly synthesised compounds. The goal of the computer analysis of synthesized compounds was to see how similar they were in terms of physicochemical properties. For this, physiochemical parameters were calculated. The result suggested the reasonable physiochemical similarity with diclofenac sodium and Indomethacin. Molecular docking studies showed that the all the test compounds perfectly docked with COX-2 enzyme with all the drug-likeness characteristics. Before start of in-vivo evaluation, in vitro cyclooxygenase (COX) inhibition assays was performed with an aim to evaluate the compounds against the protein target COX-2 which would exhibit their inhibitory activity. The test compounds (C1-C6) were subjected to analgesic activity evaluation by Eddy’s hot plate method and anti-inflammatory activity evaluation by Carageenan induced edema method respectively.

Ayurvedic literature claims that Inula racemosa Hook. f. roots are beneficial for the liver. The study’s aim was to test the hepatoprotective effect of Inula racemosa Hook. f. roots ethanolic extract (IRE) against paracetamol (PCM) induced hepatotoxicity in rats. Silymarin (100 mg/kg/day) was used for 7 days, then PCM was orally administered (3 g/kg b.wt.) on the eighth day. 24 hours after the last PCM dosing, blood was withdrawn from the retro-orbital plexus and later on the rats were sacrificed. Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Albumin (ALB), Total Protein (TP), liver weight and relative liver weight were determined. Histopathology of the liver was performed. In the study, IRE was found to have comparable protective effects against PCM-induced hepatotoxicity as Silymarin. Gallic acid was isolated for the first time from Inula racemosa Hook. f. roots. IRE exhibited a hepatoprotective effect because gallic acid was present in it.

Electric and magnetic fields (EMFs) are indefinable regions of energy that are often referred to as Radiation and are linked to the use of electricity as well as various natural and man-made phenomena. Due to continuous exposure to Unexplained and negative EMF, people experienced stress, anxiety, Hypoxia, and even long-term exposure result in Cancer to patients. On the other hand, Rudraksha seeds are globally known as electromagnetic seeds due to their positive electromagnetic healing effect. This research was conducted to find the consequence of the Negative EMF effect on human pulse rate and Oxygen carrying capacity in blood and the use of Rudraksha to study cut off harmful effect of negative EMF by this Electromagnetic property. This topic constitutes a new domain with the largely unstudied potential of Rudraksha seeds shielding effect on Unexplained Negative Electromagnetic Radiation. Keywords: EMF, Rudraksha, electromagnetic seeds, human pulse rate, Oxygen carrying capacity, Negative Electromagnetic Radiation.

The present work includes extraction of Betula alnoides bark using ethyl acetate as a solvent, preliminary phytochemical test, quantification of phytochemicals and quantification of lupeol in Betula alnoides by High Performance Thin Layer Chromatography (HPTLC) instrument along with the assessment of the antimicrobial potential of Ethyl Acetate Extract (EAE). The marc obtained after defatting of the coarsely powdered crude drug in Petroleum ether (60-80) was extracted using ethyl acetate. Afterward, preliminary phytochemical tests were done. For High Performance Thin Layer Chromatography (HPTLC), the solvent used was n-hexane: ethyl acetate (8:2 v/v) and scanning was performed at wavelength 254 nm. EAE was screened for antimicrobial potential. The extraction yield was 3.45% w/w. The result of the phytochemical analysis confirmed the presence of some important phytochemicals in EAE. A clear and resolved peak of lupeol was observed at Rf 0.61. The developed method was validated as per ICH guidelines. The concentration (%) of the marker compound (lupeol) was found to be 0.0168. Disk diffusion method using Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis as bacterial strains and Candida albicans, Aspergillus flavus and Epidermophyton floccosum as fungal strains against ciprofloxacin (for antibacterial activity) and fluconazole (for antifungal activity) as standard drugs was employed. The finding suggested that EAE possess significant antibacterial and antifungal activity when comparison was made with standard drugs. The proposed elucidated mechanism behind this action may be due to the presence of triterpenoids in EAE.

Aims: The aim of present investigation was to evaluate the traditional claim of Ficus retusa as an anti-diarrheal and anti-spasmodic agent using different pharmacological models. Background: Diarrhea is considered as major cause of mortality, especially in children and aged persons. Because of diarrhoea, 17% of admitted children get die. In order to treat the diarrhea, natural drugs may be useful. Objective: In order to prove the traditional claim of Ficus retusa, present work was undertaken with objective to prove antidiarrheal and antispasmodic activity. Methods: The anti-diarrhoeal activity was evaluated by magnesium sulphate induced diarrhea and 5-hydroxy tryptamine(5HT) induced diarrhea. Further, the exact were subjected to gastrointestinal motility test using standard procedure. Conclusion: The response towards bioactivity was dose dependent. It was concluded that 400mg/kg bw of ethanolic extract is most potent in antidiarrhoeal and antispasmodic activity.

Benzothiazole is a heterocyclic aromatic and bicyclic compound in which, benzene ring is attached with thiazole ring. This nucleus is established in marine as well as terrestrial natural compounds. The benzothiazole skeleton is established in a broad variety of bioactive heterocycles and natural products. The benzothiazole nucleus is considered as the principle moiety in several biologically active compounds. Over the decade, chemists are paying more attention towards the revision of the biological and therapeutic activities such as antimicrobial, analgesic, antiinflammatory, antitubercular, antiviral and antioxidant of benzothiazole containing compounds. The molecular structures of a number of potent drugs including Frentizole, Pramipexole, Thioflavin T and Riluzole etc., are based on benzothiazole skeleton. The present work is the compilation and presentation of all available information in a systematic manner with an aim to present the findings in a way, which may be beneficial for future research.

The present work was aimed to synthesize eight new diphenylamine derivatives by the reactions of 2-chloro-N-(4-(diphenyl amino) thiazol-2-yl)acetamide with substituted phenols in the chloroform along with anhydrous potassium carbonate and potassium iodide. The structures of newly synthesized compounds were characterized by IR, NMR, Mass and elemental analysis techniques. Toxicity profile (acute and subacute oral toxicity) and biological activity (analgesic and anti-inflammatory activity) of the synthesized derivatives was performed. Findings of the present work suggested that the synthesized compounds may be one of the excellent potent compounds to treat pain and inflammation. Therefore compounds of this group especially AK-4 (N-(4-(diphenylamino)thiazol-2-yl)-2-(2- nitrophenoxy)acetamide) could be an excellent starting point to build up new lead compounds in the management of pain and inflammation.

Oxadiazole moiety, which is one of the heterocyclic aromatic groups of the azole family; with the molecular formula C2H2N2O, exists in four isomeric form; out of which, 1,2,4-oxadiazole; 1,2,5-oxadiazole and 1,3,4-oxadiazole are common isomers. The stable isomeric forms of oxadiazoles are observed in a variety of pharmaceutical important potent drugs including raltegravir, butalamine, fasiplon, oxolamine and pleconaril. An attempt has been made to emphasize the chemistry and pharmacology associated with oxadiazole and its derivatives. A number of oxadiazole derivatives are very popular and common in use as potential therapeutic agents. However, a number of researchers are working and have worked to find out more synthetic analogues for anticancer and antifungal, anti-HIV agents using biological and in-silico models.

Background: Currently, ringworm treatment drugs include two major categories: first, propylene amine drugs, such as terbinafine, butenafine and naftifine, which exert their bactericidal effects through inhibiting squalene cyclase, causing the lack of ergosterol and accumulation of squalene. The second category of imidazole drugs includes miconazole, econazole, clotrimazole, ketoconazole and bifonazole. Mechanism: These synthetic antifungal agents exhibits their action by inhibiting the lanosterol 14α- demethylation activity of fungal cell, leading to the prevention of the ergosterol synthesis of cell membrane, changing the cell membrane permeability, and resulting in the loss of important intracellular fungal material and causing fungal death. Applications: At present, Imidazole antifungal agents are commonly used drugs in clinical treatment of ringworm with extensive clinical applications. Conclusion: The present review covers the chemistry and detailed pharmacology aspects of luliconazole.

The present work was aimed to synthesize some novel 2-chloro-N,N-diphenylacetamide derivatives conjugated with various benzaldehydes in multistep synthesis and further to undergo the process of docking on COX-1 and COX-2 enzymes. All the targeted synthesized compounds were subjected to evaluation of analgesic activity using hot plate model. Sophisticate analytical techniques via infrared spectroscopy, NMR, Mass spectroscopy and elemental analysis were employed to characterize the newly synthesized compounds. All the synthesized derivatives were evaluated for their analgesic activity. The synthesized compound AKM-2 (N-(4-(diphenylamino) thiazol-2-yl)-2-((4-((3methylbenzylidene)amino)phenyl)amino)acetamide) exhibited significant analgesic response when comparison was made with diclofenac sodium as standard drug. Molecular docking study was used to discover the possibility of binding site and binding strength of new derivatives of acetamide. The present study offers insight for compound AKM-2, as a new lead compound as analgesic agent because of significant docking and similar amino acid residue. The biological activity performed by in-vivo method confirmed the same.

Objective: Firstly, Deflazacort was synthesized in 1969 and has the structural similarity with cortisol. The present review is an attempt to summarize the updated information related to chemistry and pharmacology of Deflazacort. Development: Deflazacort a synthetic compound synthesized by derivatization in the chemical structure of prednisolone with an aim to improve its potency. Deflazacort is under global development with Marathon Pharmaceuticals, was approved by the U.S. Food and Drug Administration in year 2017 to treat patients with Duchenne muscular dystrophy (DMD). Chemistry and Pharmacology: DMD is one of the rare and genetic disorders with the symptoms of progressive degeneration of muscle tissue. Chemically, it is deacetylated at position 21 to produce active metabolite 21-desacetyl deflazacort (21-desDFZ), which acts through the glucocorticoid receptor. The predominant side effects are cushingoid appearance, increased appetite, upper respiratory tract infection (URTI), pollakiuria, hirsutism, and nasopharyngitis. Conclusion: The present article summarizes the available updated information and work done so far on Deflazacort with special emphasis on its chemistry, pharmacology with detailed mechanism of action, pharmacodynamics, pharmacokinetics, metabolism and clinical trials etc.

Acetanilide or N-phenylacetamide is an aromatic compound having phenyl ring attached to an acetamido group (–NHCOCH3). In 1886, acetanilide was introduced as an analgesic and antipyretic drug into medical practice by A. Cahn and P. Hepp. Since then, many acetanilide derivatives have been found to have antimicrobial, analgesic, anti-inflammatory, antipyretic, antioxidant, anticonvulsant, anti- cancer, antihyperglycaemic and antimalarial activities. Acetanilide also plays an important role in the synthesis of a number of chemicals as intermediates and precursors. The chief objective of the present article is to highlight the chemistry and pharmacological aspects of various derivatives of acetanilide and their pharmacological activities to assist the future discovery of more efficacious derivatives with less toxicity.

The objective of the study is to access the safety of Calendula essential oil by studying acute and sub-chronic dermal toxicity. The dermal toxicities of Calendula essential oil were evaluated in accordance with OECD guidelines number 402 and 411 respectively. The animals were exposed to Calendula officinalis (CO) essential oil dose of 20 mL/kg body weight for acute dermal toxicity, whereas for dermal sub-chronic toxicity study, rats were exposed to CO oil 2.5, 5 and 10 mL/kg body weight, respectively, for 7 times in a week for 90 days. The parameters studies included CNS stimulation, depression, hematological parameters (RBC, WBC, Hb, Lymphocyte % etc), biochemical parameters (total protein, albumin, total bilirubin, ALP, AST, etc), relative organ weight, necropsy and histopathology. In toxicity studies, all animals exhibited normal behavior without any change in hematology, blood biochemistry, necroscopical and histopathology. The no observed effect level (NOEL) and no observed adverse effect level (NOAEL) of CO oil were 2.5 and 10 mg/kg/day, respectively. CO oil is under the herbal medicinal product according to the European Medicines Agency with the claim of an LD50 value of 20 mL/kg body weight. The result indicates that CO essential oil did not produce any significant toxic effects.

The present investigation was aimed to find out the sun protection factor (SPF) and antioxidant potential of geranium essential oil (GEO) and calendula essential oil (CEO) because having a combination of these two properties moves up the oils as an active ingredient of various cosmeceutical formulations for their preventive and protective properties. Essential oils were obtained by hydrodistillation of Pelargonium graveolens leaves (GEO) and Calendula officinalis flowers (CEO). The composition and identification of chemical constituents of oils were determined by GCMS analysis. Free radical scavenging activity was measured by nitric oxide scavenging activity and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. It was observed that both GEO and CEO have the potential to reduce or prevent oxidative stress and can be used in skin care regimen to slow down skin aging via its antioxidant properties. In vitro SPF was determined by a very simple and rapid spectroscopic method. SPF value of GEO and CEO was found to 6.45 and 8.36, respectively. The SPF of CEO was higher than GEO, and the results of SPF show that these essential oils can be employed in sunscreen formulations to protect the skin from sunburn. From the results, it can be concluded that the combined antioxidant and SPF property of GEO and CEO can provide synergistic photoprotective effect or lift up the additional value of the cosmeceutical formulation.

Aim The current study presents the first report of isolation of bioactive compound (salicylic acid) from seeds of Cleome viscosa L. confirmed by its characterization by infrared (IR) spectroscopy, nuclear magnetic resonance (1H NMR and 13C NMR) spectroscopy and mass spectroscopy. The present work is the first report of HPTLC densitometric method, which has been developed and validated for quantification of a marker compound (salicylic acid) from ethyl acetate extract using the solvent system of ethyl acetate: acetonitrile (1.1:0.9, v/v). Material and methods TLC glass plates pre-coated with silica gel F366 (stationary phase) were used. Densitometric analysis of salicylic acid was performed in reflectance mode at 366 nm. Result The developed compact spot for salicylic acid at Rf 0.51. ICH guidelines were used to validate this method in terms of precision, repeatability and accuracy. Linearity range for salicylic acid was 10–50 ng/spot and the content of salicylic acid was found to be 0.9 ± 0.04 μg/g of seed. The limit of detection (LOD) and limit of quanitification (LOQ) values for salicylic acid were 4 ng and 8 ng, respectively. Better resolution from other present constituents present in the extract were obtained by this developed simple, precise and accurate method. Conclusion The study concluded the presence of Salicylic acid as active compound present in seeds of C viscosa. The present HPTLC-densitometric method may be used for routine quality control analysis for salicylic acid quantification from Cleome viscosa L.

The present study deals with the evaluation of antiaging potential of carrot seed oil-based cosmetic emulsions. Briefly, cosmetic emulsions composed of carrot seed oil in varying proportions (2, 4, and 6% w/v) were prepared using the hydrophile-lipophile balance (HLB) technique. Coconut oil, nonionic surfactants (Tween 80 and Span 80), and xanthan gum were used as the oil phase, emulgent, and emulsion stabilizer, respectively. The formed emulsions were evaluated for various physical, chemical, and biochemical parameters such as the zeta potential, globule size measurement, antioxidant activity, sun protection factor (SPF), skin irritation, and biochemical studies. The zeta potential values ranged from -43.2 to -48.3, indicating good stability. The polydispersity index (PDI) of various emulsion formulations ranged from 0.353 to 0.816. 1,1-Diphenyl-2-picrylhydrazyl- (DPPH) and nitric oxide-free radical scavenging activity showed the antioxidant potential of the prepared carrot seed oil emulsions. The highest SPF value (6.92) was shown by F3 having 6%w/v carrot seed oil. Histopathological data and biochemical analysis (ascorbic acid (ASC) and total protein content) suggest that these cosmetic emulsions have sufficient potential to be used as potential skin rejuvenating preparations.

Introduction The wound is defined as an injury of a living tissue, arose due to either an accidental injury like cut of the cells or skin or sometime, maybe broken the tissue, which may cause the anomalies in the cellular ability to exhibit the protective mechanism. Wound healing is process of regaining the integrity of cell structure and layers of the skin. The normal healing process of wounds are categorized in 4 phases which includes hemostatic, inflammatory, fibrolastic and maturation. Purpose The present manuscript embarks on up to date information on different methods being used for wound healing assessment including incision, excision, burn wound and dead space models. The biochemical parameter which acts as wound healing markers are collagen estimation (hydroxyproline), hexosamine, DNA estimation, total protein estimation, wound Index, contraction area, epithelization period and tensile strength etc. Histologic evaluations is also an integral part of wound healing evaluation which, help in evaluating the cellular and matrix detail within the wound. Conclusion At present, molecular approaches are important to heal the wound. For assessment of potential of any herbal drug/synthetic compound, incision wound model, excision wound model, burn wound model and dead space model and their parameter are used.

Objective Brahmi vati (BV) is an Ayurvedic polyherbal formulation used since ancient times and has been prescribed in seizures associated with schizophrenia and related memory loss by Ayurvedic practitioners in India. The aim of the study was to investigate these claims by evaluation of anticonvulsant, antischizophreniac, and memory-enhancing activities. Antioxidant condition of brain was determined by malondialdehyde (MDA) and reduced glutathione (GSH) levels estimations. Acetylcholinesterase (AChE) was quantitatively estimated in the brain tissue. Methods Brahmi vati was prepared in-house by strictly following the traditional Ayurvedic formula. Bacoside A rich fraction (BA) of Bacopa monnieri was prepared by extraction and fractionation. It was than standardized by High Performance Liquid Chromatography (HPLC) and given in the dose of 32.5 mg/kg body weight to the different groups of animals for 7 days. On the seventh day, activities were performed adopting standard procedures. Key findings Brahmi vati showed significant anticonvulsant, memory-enhancing and antischizophrenia activities, when compared with the control groups and BA. It cause significantly higher brain glutathione levels. Acetylcholinesterase activity was found to be significantly low in BV-treated group. Conclusion The finding of the present study suggests that BV may be used to treat seizures associated with schizophrenia and related memory loss.

BACKGROUND: Recent advances in the field of bionanomedicine make us not only to produce biomaterials but also to manipulate them at molecular level. Viruses particularly bacteriophages are a promising nanomaterial that can be functionalized with great precision. Bacteriophages are the natural antimicrobial agents that fight against antibiotic resistant bacteria which causes infections in animals, in humans, or in crops of agricultural value. OBJECTIVE: The idea of utilizing bacteriophages as therapeutic agents is due to their ability to kill bacteria at the end of the infectious cycle. This paper reviewed on the general biology of bacteriophages, presence of receptors on the bacteria which are necessary for the recognition and adsorption of bacteriophages. Pharmacokinetics and therapeutic potential of bacteriophages administered through various routes in treating diverse bacterial infections is also reviewed along with the problems associated with bacteriophage therapy. CONCLUSION: By engineering the phages or by making a cocktail of phages it would become easy to treat various bacterial infections which are as such resistant to the current generations of antibiotics available in the market. Among various routes of administration parenteral route is found to be the most thriving route for the treatment of systemic infections whereas oral route is meant to treat gastrointestinal infections whereas; local delivery (skin, nasal, ears) of phages has proven their potency to treat topical infections.

Ethnopharmacological relevance Cleome viscosa Linn., commonly known as Hurhur, is used in traditional system of medicine in healing of wounds. Aim There was no scientific proof confirming the use of Cleome viscosa Linn. seeds in wound healing, therefore the present study was aimed to evaluate the wound healing potential of Cleome viscosa Linn. seeds extract. Materials and methods In the present study, quantitative estimation of phytochemicals was done according to standard procedures. The seeds of Cleome viscosa Linn, were studied for wound healing activity by assimilating petroleum ether extract, ethyl acetate extract, methanol extract and aqueous extract respectively in simple ointment base B.P. in 0.5% (w/w), 1% (w/w) and 2% (w/w) concentrations. Three models were used to evaluate the wound healing potential which included excision wound model, incision wound model and model based on biochemical parameter estimation. In excision wound model, contraction of wound and epithelization period was studied. Estimation of tensile strength and content of hydroxyproline in eschar were determined in incision wound model. Petroleum ether extract was chromatographed using column chromatography. A compound was isolated which was characterized by IR, 1 H NMR, 13 C NMR and Mass spectroscopy. Results Secondary metabolites estimated quantitatively were terpenoids, tannins, alkaloids, phenols, flavonoids and saponins. Wound treated with ointment containing 2% (w/w) petroleum ether extract (PEE), exhibited potent wound healing activity in comparison to 2% (w/w) ethyl acetate extract (EAE), 2% (w/w) methanol extract (MEE), 2% (w/w) aqueous extract (AEE). No significant difference was observed in 2% (w/w) petroleum ether extract treated group and standard group. All the extracts were analyzed for hydroxyproline content equivalent to 4-hydroxy- l -proline. Hydroxyproline content (μg/500 g) was found to be 43.58 ± 0.45, 39.45 ± 0.15, 37.86 ± 0.90 and 40.09 ± 0.49 in 2% (SO). PEE, 2% (SO). EAE, 2% (SO). MEE and 2% (SO). AEE respectively. A triterpenoid compound (Lupeol) was isolated from PEE of Cleome viscosa L. seeds which may be responsible for maximum wound healing potential of ointment prepared by PEE. Conclusion It was concluded that PEE shows excellent wound healing activity.

The symptoms of Staphylococcal scalded skin syndrome (SSSS) include blistering of skin on superficial layers due to the exfoliative toxins released fromStaphylococcus aureus. After the acute exfoliation of skin surface, erythematous cellulitis occurs. The SSSS may be confined to few blisters localized to the infection site and spread to severe exfoliation affecting complete body. The specific antibodies to exotoxins and increased clearence of exotoxins decrease the frequency of SSSS in adults. Immediate medication with parenteral anti-staphylococcal antibiotics is mandatory. Mostly, SSSS are resistant to penicillin. Penicillinase resistant synthetic penicillins such as Nafcillin or Oxacillin are prescribed as emergency treatment medicine. If Methicillin-resistantStaphylococcus aureus(MRSA) is suspected), antibiotics with MRSA coverage (e.g., Vancomycin or Linezolid) are indicated. Clindamycin is considered as drug of choice to stop the production of exotoxin from bacteria ribosome. The use of Ringer solution to to balance the fluid loss, followed by maintainence therapy with an objective to maintain the fluid loss from exfoliation of skin, application of Cotrimoxazole on topical surface are greatlly considered to treat the SSSS. The drugs that reduce renal function are avoided. Through this article, an attempt has been made to focus the source, etiology, mechanism, outbreaks, mechanism, clinical manisfestation, treatment and other detail of SSSS.

The aryl propionic acid derivatives belong to an important class of NSAIDs (Non Steroidal Anti-inflammatory Drugs). Ibuprofen, chemically called 2-(4-isobutyl phenyl) propionic acid, is a well known NSAID. Aryl propionic acid derivatives possesses a wide range of biological activities including anti-bacterial, anti-convulsant, anti-cancer, analgesic and anti-inflammatory activities. Apart from very potent compounds in the field of analgesics and antipyrectics as Ibuprofen, Oxaprozin, Ketoprofen, Fenoprofen; aryl propionic acid derivatives plays important role to treat other ailments also. Through this review, an attempt has been made to emphasize on recent work done and recent advancements in arena of aryl propionic acid derivatives in view of medicinal chemistry.

The objective of this work was to develop quantitative structure activity relationship (QSAR) models from sulfonamide derivatives against anticonvulsant activity. For developing the model, multiple linear regression and artificial neural network (ANN) have been employed as effective and efficient methods and these models have been validated with statistical analysis such as fraction of variance, cross-validation test, quality factor, Fischer’s test, and internal validation test (Y-randomization test), where applicable. A regression-based QSAR model (linear model) has been developed with cross-validation test q 2 = 0.8324 and fraction of variance r 2 = 0.8327, all the statistical tests have validated this model. An ANN (nonlinear model)-based model has also been developed with fraction of variance r 2 = 0.8710 and cross validation test q 2 = 0.7032. So, with the help of the developed models we can predict the logKi values of novel designed molecules and alter their structural properties accordingly before synthesizing them.

Objective Ayurvedic formulations are preferred over other formulations as well as commercialized on broad level to treat various ailments. The World Health Organization has established certain guidelines for quality control of heavy metals and pesticide residues. Bacopa monnieri, a popular herb with immunomodulator and memory-enhancing properties is the chief constituent of several Ayurvedic formulations, which include Brahmi Vati (BV), Brahmi Ghrita (BG) and Saraswat Churna (SC), etc. In view of the World Health Organization guidelines, two products of each formulation from six different manufacturers were purchased from Ayurvedic Pharmacy, Bulanala-Varanasi, India for testing heavy metal and pesticide residue. Methods In the present study, all the formulations—BV, BG and SC—were selected for estimation of four heavy metals namely lead (Pb), cadmium (Cd), chromium (Cr) and nickel (Ni) by a plasma emission spectrophotometer. Organochlorine pesticidal residues were estimated for dichlorodiphenyl trichloroethane, isomers of hexachlorocyclohexane (HCH) and α-endosulfan, etc. in total 12 samples of test formulations containing Bacopa monnieri L. using gas chromatography technique. Results Out of 12 samples, Pb, Cd, Cr and Ni were present in all samples but below the permissible limit. Although atrazine, aldrin, dialdrin were in below detection limit, but other pesticides were detected in some samples as oxamyl, hexachlorocyclohexanes (α-HCH, β-HCH and γ-HCH), dichlorodiphenyl trichloroethane and dichlorodiphenyl dichloroethylene. Conclusion The presence of heavy metals in the formulations was low to cause toxicity. However evaluation of heavy metals and pesticide residue in every batch is necessary.

Background Tridax procumbens(L.) leaves are traditionally used in wound healing by tribal people. The matured leaves are crushed to make a paste and applied on the surface of the wound. Purpose The aim of the present investigation was to evaluate the wound healing activity of ethanolic extract of Tridax procumbens (L.) (EETP) in streptozotocin induced diabetic and non- diabetic laboratory animals. There is no scientific literature, claiming the use of leaves of Tridax procumbens (L.) in diabetic wounds. Study Design The simple ointment base (2.5 % and 5% w/w) of EETP was formulated to evaluate the wound healing potential on diabetic and non-diabetic rats, using incision, excision and burn wound model. Methods In incision wound model, epithelization period, wound index, % contraction area, hydroxyproline content, DNA estimation, total protein and histopathological evaluations were done. In excision wound model, tensile strength was measured. In burn model, contraction rate, wound contraction (%) and epithelization period were evaluated. Results Secondary metabolite as tannin, flavonoids were present. In the excision model, animals treated with 2.5 % and 5% w/w EETP showed significant result in wound contraction, epithelization period and wound index. Hydroxyproline, total protein and DNA concentration in healing tissue were more in comparison to control and as well as standard in diabetic and non- diabetic. The parameters evaluated showed significant response at 2.5 % and 5% w/w EETP. Conclusion Flavonoids and tannin were accountable for wound healing. The findings confirmed the ethanomedicinal claim of Tridax procumbens(L.) in wound healing in diabetic and nondiabetic conditions.

Objective: Aripiprazole, a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole. Development: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S. Food and Drug Administration (USFDA) by the end of 2002 with an aim to treat patients with schizophrenia. This drug got approved by European Commission in February 2013 to treat the patients having severe manic episodes in bipolar I disorder Additionally, it got approval in Japan in January 2006 and in Canada in 2014. Pharmacology: Aripiprazole shows high specificity for dopamine receptor especially D2 and D3, serotonin 5-HT1A and serotonin 5-HT2A receptors, reasonable specificity for dopamine D4, serotonin 5- HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors. It also shows moderate specificity for the serotonin reuptake. The major side effects include headache, agitation, akithesia, anxiety, tachycardia, insomnia, postural hypotension, constipation, vomiting, dizziness, nervousness and somnolence. Conclusion: The present article embarks the available information on Aripiprazole with emphasis on its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism and clinical trials.

Objective: Ozenoxacin is one of the potent quinolone antibiotics, recently approved by the United States Food and Drug Administration (USFDA) with reported pharmacology to treat the impetigo. The demand for better acting topical formulation is increasing day by day. The present review is an attempt to summarize the facts behind the chemistry and biological applications of Ozenoxacin. Mechanism of Action: This novel drug being a quinolone antibiotic compound, acts by inhibiting DNA gyrase A and topoisomerase IV and affects supercoiling, supercoil relaxation, chromosomal condensation, chromosomal decatenation and many others. Mechanism of Action: This novel drug being a quinolone antibiotic compound, acts by inhibiting DNA gyrase A and topoisomerase IV and affects supercoiling, supercoil relaxation, chromosomal condensation, chromosomal decatenation and many others. Pharmacology: Ozenoxacin has demonstrated to have a bactericidal activity against organisms, such as Staphylococcus aureus and Staphylococcus pyogenes. Ozenoxacin is non-fluorinated quinolone and being developed for the other dermatological bacterial infections as well. No sign of genotoxicity was observed when tested experimentally. Conclusion: The present review also covers the complete picture of pharmacokinetics, clinical trials, toxicity and future scope and possible avenues in this arena.

Background The brain is a vital part of the central nervous system (CNS), characterized by the presence of soft tissue in its internal structure which protects itself. Research on design of drugs for CNS disorders is in progress and up to date information is required for further investigation. Objective The present paper is written with the objective to compile all the available data and information on CNS disorders and CNS acting drugs. CNS acting drugs are important to consider because some drugs get ineffective owing to incapability to efficiently deliver and sustain them within the brain for effective treatment. Cns disorders The current trend to design therapeutic drugs for CNS disorders focuses on neurotransmitters release and their reuptake, including Parkinson's, Alzheimer's, and other CNS disorders. The disorders associated with CNS are characterized by the progressive loss of gray matter and/or white matter structures. Drugs CNS stimulants are the class of drugs, producing response to alleviate a particular medical condition. CNS stimulants improve the brain function in patients with schizophrenia and related diseases. CNS stimulants are a class of therapeutic drugs used to treat CNS disorder including the conditions like lack of adrenergic stimulation, symptoms of narcolepsy and neonatal apnea, etc. Apart from drugs, a number of smart tools including Multi-Target Designed Ligands (MTDL) and "predictor" models are contemporarily used to design therapeutic agents for CNS disorders. Mechanism The majority of CNS stimulants causes stimulation of the traditional "fight or flight" syndrome which is concerned with activation of sympathetic nervous system. These neurotransmitters associated receptors are concerned in drug abuse and addiction withdrawal related phenomenon. Conclusion The present review embarks on detail up-to-date information on CNS stimulant drugs, their mechanism of action, in vivo models for biological evaluations with major emphasis on tools in design of therapeutic drugs for CNS disorders.

Background Since ancient times, species of Cleome genus are used to cure various ailments in human beings and same is stated in traditional treatises. Each part of the plant has its own significance, therefore, in background of its significance, upto date information in systematic manner is required. Purpose The present review embarks on variety of naturally occurring compounds that have been isolated from various species of Cleome genus. The present study furnishes an overview of all naturally isolated compounds diterpenes, triterpenoids, trinorterpenoids, flavonol glycoside, coumarinolignoids, dipyridodiazepinone, essential oils, sesquiterpenes, flavonoids, carboxylic acid derivatives, lactone derivatives, sterols and pharmacological activities of various species of Cleome genus. These plants of Cleome genus are often used as conventional drugs to treat several ailments therefore information on analgesic, anti-inflammatory, antifungal, antimicrobial, anti-diarrheal, anticancer, anti-arthritic, hepatoprotective, antinociceptive, wound healing and psychopharmacological activity etc were compiled. Method Literature regarding the compounds isolated and pharmacological studies performed by various researchers in the last 40 years who worked on different species belonging to genus Cleome was summarized in the present review. Results On the basis of references, this review covers the phytochemistry and pharmacology of Cleome species, describing compounds previously reported current trends and future prospects. Conclusion From a wellbeing point of view, species belonging toCleome genus presents an excellent option for curing variety of ailments in human beings due to its isolated phytocompounds that reveal significant biological activities or for developing a variety of new pharmaceutical products. Future Perspective The observed pharmacological activities and no toxicity profile of extracts obtained from species of Cleome genus support the statement that these extracts might be used in the formation of new formulations that can be beneficial to treat various ailments.

Aim The aim of present work was to study the pharmacognostic standardization, physicochemical, phytochemical and pharmacological evaluation of the stem of Bacopa monnieri L. Method Standard method was followed for pharmacognostic, physicochemical, and phytochemical study. For quantitative analysis, HPTLC technique was employed. Maximal electroconvulsive shock (MES) and pentylenetetrazole (PTZ) method was used for anticonvulsant evaluation. Result Microscopic study of the stem showed presence of epidermis and cortex having large intercellular spaces. The oval shaped starch grains were present in cells of cortex and endodermis. Total ash (5.98%), water-soluble ash (4.91%), acid-insoluble ash (3.96%), water soluble extractive (15.31%) and ethanol soluble extractive (6.74%) values were evaluated for physicochemical evaluations. Quantitative estimation of Bacoside A (marker compound) by HPTLC technique was performed. The linearity (100–600 ng), the % recovery (97.81% w/w) were estimated. The Bacoside A in the alcoholic extract was found to be higher than that of the other extracts. The proposed HPTLC method was found to be simple and accurate. The anticonvulsant activities of all the extracts were evaluated by MES and PTZ models in mice. Conclusion The least anticonvulsant potential was recorded for acetone extract in dose of 100 mg/kg and maximum anticonvulsant action was recorded for ethanolic extract in dose of 300 mg/kg.

In search of new leads toward potent antimicrobial agent, an array of novel derivatives of 2-hydrazinyl -N-N, diphenyl acetamide has been synthesized from the chloroacetylation reaction of diphenylamine (DPA). For this, a series of DPA derivatives were prepared by replacing chlorine with hydrazine hydrate in alcoholic medium and 2-hydrazino-N, N-diphenylacetamide was synthesized. The 2-hydrazino-N, N-diphenylacetamide was further subjected to reaction with various aromatic aldehydes in presence of glacial acetic acid in methanol. The synthesized compounds were characterized by their IR, 1HNMR spectral data and elemental analysis. The compounds were screened for antibacterial and antifungal activity by cup plate method. 2-(2-Benzylidenehydrazinyl)-N, N-diphenylacetamide (A1); 2-(2-(3-methylbenzylidene) hydrazinyl)-N, N-diphenyl-acetamide (A5) and 2-(2-(2-nitrobenzylidine) hydrazinyl)-N, N-diphenyl-acetamide compounds (A7) showed significant antimicrobial as well as antifungal activity. Diphenylamine compounds may be explored as potent antimicrobial and antifungal compounds.

P

A series of Schiff bases of diphenylamine derivatives have been synthesized and evaluated in vitro for their antibacterial activity against pathogenic both Gram-positive bacteria B. subtilis and Gram-negative bacteria E. coli using ciprofloxacin as standard drug at conc. of 50 µg/ml and 100 µg/ml. The structures of these compounds were established on the basis of IR and 1H-NMR spectral analysis. The compound (3d) displayed potent antibacterial activity against Bacillus subtilis (17 and 15mm) and Escherichia coli (19 and 17mm) by disc diffusion method.

The aim of the present study was to standardize Brahmi vati (BV) by simultaneous quantitative estimation of Bacoside A3 and Piperine adopting HPLC-UV method. BV very important Ayurvedic polyherbo formulation used to treat epilepsy and mental disorders containing thirty eight ingredients including Bacopa monnieri L. and Piper longum L.An HPLC-UV method was developed for the standardization of BV in light of simultaneous quantitative estimation of Bacoside A3 and Piperine, the major constituents of B. monnieri L. and P. longum L. respectively. The developed method was validated on parameters including linearity, precision, accuracy and robustness.The HPLC analysis showed significant increase in amount of Bacoside A3 and Piperine in the in-house sample of BV when compared with all three different marketed samples of the same. Results showed variations in the amount of Bacoside A3 and Piperine in different samples which indicate non-uniformity in their quality which will lead to difference in their therapeutic effects.The outcome of the present investigation underlines the importance of standardization of Ayurvedic formulations. The developed method may be further used to standardize other samples of BV or other formulations containing Bacoside A3 and Piperine.

The causative agent of tuberculosis (TB), Mycobacterium tuberculosis, remains an important worldwide health threat. Although TB is one of the oldest infectious diseases of man, a detailed understanding of the mycobacterial mechanisms underlying pathogenesis remains elusive. Here, we studied the role of the α(1→2) mannosyltransferase MptC in mycobacterial virulence, using the Mycobacterium marinum zebrafish infection model. Like its M. tuberculosis orthologue, disruption of M. marinum mptC (mmar_3225) results in defective elongation of mannose caps of lipoarabinomannan (LAM) and absence of α(1→2)mannose branches on the lipomannan (LM) and LAM mannan core, as determined by biochemical analysis (NMR and GC-MS) and immunoblotting. We found that the M. marinum mptC mutant is strongly attenuated in embryonic zebrafish, which rely solely on innate immunity, whereas minor virulence defects were observed in adult zebrafish. Strikingly, complementation with the Mycobacterium smegmatis mptC orthologue, which restored mannan core branching but not cap elongation, was sufficient to fully complement the virulence defect of the mptC mutant in embryos. Altogether our data demonstrate that not LAM capping, but mannan core branching of LM/LAM plays an important role in mycobacterial pathogenesis in the context of innate immunity.

Cardiac glycosides are used in the treatment of congestive heart failure and arrhythmia. Current trend shows use of some cardiac glycosides in the treatment of proliferative diseases, which includes cancer. Nerium oleander L. is an important Chinese folk medicine having well proven cardio protective and cytotoxic effect. Oleandrin (a toxic cardiac glycoside of N. oleander L.) inhibits the activity of nuclear factor kappa-light-chain-enhancer of activated B chain (NF-κB) in various cultured cell lines (U937, CaOV3, human epithelial cells and T cells) as well as it induces programmed cell death in PC3 cell line culture. The mechanism of action includes improved cellular export of fibroblast growth factor-2, induction of apoptosis through Fas gene expression in tumor cells, formation of superoxide radicals that cause tumor cell injury through mitochondrial disruption, inhibition of interleukin-8 that mediates tumorigenesis and induction of tumor cell autophagy. The present review focuses the applicability of oleandrin in cancer treatment and concerned future perspective in the area.

Cyanobacteria are rich source of array of bioactive compounds. The present study reports a novel antibacterial bioactive compound purified from cyanobacterium Nostoc sp. MGL001 using various chromatographic techniques viz. thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Further characterization was done using electrospray ionization mass spectroscopy (ESIMS) and nuclear magnetic resonance (NMR) and predicted structure of bioactive compound was 9-Ethyliminomethyl-12-(morpholin - 4 - ylmethoxy) -5, 8, 13, 16–tetraaza–hexacene - 2, 3 dicarboxylic acid (EMTAHDCA). Structure of EMTAHDCA clearly indicated that it is a novel compound that was not reported in literature or natural product database. The compound exhibited growth inhibiting effects mainly against the gram negative bacterial strains and produced maximum zone of inhibition at 150 μg/mL concentration. The compound was evaluated through in silico studies for its ability to bind 30S ribosomal fragment (PDB ID: 1YRJ, 1MWL, 1J7T, and 1LC4) and OmpF porin protein (4GCP, 4GCQ, and 4GCS) which are the common targets of various antibiotic drugs. Comparative molecular docking study revealed that EMTAHDCA has strong binding affinity for these selected targets in comparison to a number of most commonly used antibiotics. The ability of EMTAHDCA to bind the active sites on the proteins and 30S ribosomal fragments where the antibiotic drugs generally bind indicated that it is functionally similar to the commercially available drugs.

Thallus growth and development in the coenocyti alga Caulerpa sertularioides (Gmelin) Howe have been studied quantitatively. In unsupplemented seawater at 26 C and in a 12:12 hr light/dark cycle, new rhizomes formed near the old growing points on thalli transplanted from the ocean. Adjacent to the apices of new rhizomes, rhizoids were produced downward, regularly spaced and at a rate of about 1.5/day. Upright. shoots developed irregularly in acropetal succession behind the tips of either the parent or the new rhizomes, which arose as branches of the old. Rates of rhizome, rhizoid, and upright shoot elongation were 0.4, 0.81, and 0.54 cm/day, respectively. Thalli survived up to 2 months in unsupplemented seawater. Long-term growth was obtained by varying culture conditions. A substratum of sand, apparently rich in microorganisms, produced long-term thallus growth in seawater, and the form of development changed so that upright shoot formation was promoted and rhizome elongation halved. Similar effects were elicited by indole-3-acetic acid, 5 × 10(-5) , M in seawater and by sap expressed from C. racemosa or C. sertularioides and added to seawater at 2.5-10% by volume. The regulation of development in an algal coenocyte is discussed and analogies with regulation in multicellular plants are drawn.