Amit Kumar

A Molecular docking study on novel Acetamide derivatives as specific Mono amino oxidase (MAO) A inhibitory agents was performed with a set of 40 compounds to analyze their inhibitory action.  For this, compounds were designed on the basis of available literature and used as Ligands for molecular interaction. The structure of molecular target Mono Amino Oxidase A (MAO A) was retrieved from the PDB database (PDB ID 2Z5X). For comparative analysis Clorgyline, a well-known specific MAO A inhibitor was taken as the standard. Computational docking analysis was performed using PyRx, AutoDock Vina option based on scoring functions. Among 40 compounds the top 11 hits were recognized as promising MAO A inhibitors, according to their docking scores and selected for further study of interaction and visualization. Phenyl sulphanyl derivative with chlorobenzyl amino moiety (Code AD31) showed an optimum binding affinity and stable complex with a molecular target MAO A  with the binding energy of -8.3  kcal/mol as compared to the standard (-7.6 kcal/mol). These results indicated that proposed modification in Acetamide derivatives may produce potent and specific MAO A inhibitors to treat depression with lesser side effects.

Jatropha curcas in spite of having many medicinal effects is not used usually as medicine because of the presence of toxic components like phorbol ester. In this study, we have compared many chemical and biochemical parameters between plant extract (MEMJC) Methanolic extract of mechanical cake of Jatropha curcas seeds and without the presence of phorbol ester (MEHJCAT). Alkali treated mechanical cake of Jatropha curcas seeds .The phorbol ester was removed by alkali treatment. Phytochemical analyses were done to determine composition. The survival study was evaluated using Kaplan Meier Chart. SOD activity was assayed by the method of McCord and Fridovich and Catalase activity was assayed by Aebi’s method. Urea, Creatinine, triglyceride level in plasma was measured using their respective kits. The removal of phorbol ester through alkali treatment makes the MEHJCAT less toxic or less vulnerable to generate free radical in rats. Through oral fat tolerance test, we have found that MAHJCAT reduces the absorption of triglyceride in blood. The results of renal function test also favored MEMJC as more toxic then MEHJCAT. Also from kaplen meier survival curve, it has been found that both drugs MEMJC and MEHJCAT have no mortality significance proved by the measurement of LD50. So, we have concluded that MEHJCAT as better medicinal plant product through the study of all biochemical parameters.

Bioanalytical methods of Reverse Phase-High performance liquid chromatography (HPLC) was developed and validated for simultaneous estimation of Isoniazid (INH) and Ciprofloxacin Hydrochloride (CIP HCl) encapsulated in lipid polymeric hybrid nanoparticles (LPNs) in plasma and in organ homogenates of lung, liver, spleen and kidney of mice. Chromatographic separation was done using Agilent® C18 bonded silica column of dimensions 150 × 4.6 mm, 5μmwith flow rate 1.0 ml/min, injection volume 20 µland column temperature 40°C. The mobile phase consists of a mixture of 70 volumes of 0.1 percent v/v of trifluoroacetic acid(TFA) and 30 volumes of acetonitrile (ACN). The results indicated that the developed method was linear and selective for all matrices studied. Analysis of accuracy and precision showed adequate values, with relative standard deviation values lower than 5, which are in accordance with USFDA guidelines for bioanalytical method validation. Isoniazid (INH) and Ciprofloxacin Hydrochloride (CIP HCl) were stable in plasma and tissue homogenates under different storage and processing conditions. This method was applied to study the pharmacokinetic and biodistribution profile of both drugs in free form and in bound state with lipid nanoparticles. The results showed that polymeric nanoparticles showed higher drug accumulation in the target site i.e. lung as compared to non-target organs fulfilling our aim of developing a HPLC method for the simultaneous estimation of both drugs and their application in determination of pharmacokinetic and pharmacodynamic potential of the lipid nanoparticles.

Salvadora persica L. (family- Salvadoraceae) is an evergreen small tree commonly known as Pilu, Jal and toothbrush tree. It is used in the treatment of pain, low fever, toothache, nose trouble, piles, scabies, inflammation, scurvy, gonorrhoea, chest disease and boils.  The present study was undertaken to evaluate the antinociceptive activity of the successive extracts (chloroform, ethyl acetate, ethanol and aqueous extracts) of powdered leaves of Salvadora persica L. at the dose of 500 mg/kg b. w. using eddy’s hot plate method. The results of the statistical analysis showed that chloroform and ethyl acetate extracts have significant antinociceptive activity. From the results of antinociceptive effects it can be concluded that the chloroform extract of the powdered leaves of Salvadora persica has shown significant activity (P < 0.05) at 30 min and significant activity (P < 0.01) at 60 and 120 minutes. The ethyl acetate extract has shown significant activity (P < 0.01) at 30, 60 and 120 minutes when compared to the control group. While the standard drug (Morphine Sulphate) shown significant activity (P < 0.01) at 30, 60, 120 and 180 minutes. Other successive extracts (ethanol and aqueous extracts) could not produce the significance of the difference from the control as antinociceptives. Hence present investigation reveals the antinociceptive activity of chloroform and ethyl acetate extracts of leaves of Salvadora persica L Key Words: Salvadora persica L. antinociceptive activity, chloroform and ethyl acetate extracts

Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Poorly water soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities. Any drug to be absorbed must be present in the form of an aqueous solution at the site of absorption. The ability to increase aqueous solubility can thus be a valuable aid to increasing efficiency and/or reducing side effects for certain drugs. This is true for parenterally, topically and orally administered solutions. The solubility of drugs is defined according to (bio-pharmaceutical classification system) BCS classification system which divides drugs to different class according to its solubility. Solid dispersion is defined as dispersion of one or more active ingredients in an inert carrier or matrix known as solid dispersion. Solid dispersion reduces the particle size and changes the micro environment of the drug particle, increases the rate of dissolution and absorption and thus changes the biopharmaceutical properties of poorly water soluble drugs. The solid dispersion method, by which a drug is dispersed in a carrier to make it amorphous, is one of the pharmaceutical approaches most commonly employed to enhance bioavailability of poorly water soluble drugs. Various pharmaceutical approaches for the preparation of SDs, including co-precipitation, lyophilization, spray drying, solvent evaporation, fusion and powder mixing methods, have been reported. It’s a new and efficient technique to improve the solubility of poorly soluble drugs.