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The well-known plant components for their anti-diabetic properties are Azadirachta indica leaves, Pterocarpus marsupium heartwood, Picrorhiza kurroa rhizomes and Withania coagulans berries and fruit coat. The current study's objective was to create a polyherbal dosage form and assess its effectiveness and stability. The various methanolic extracts of all four medicines were combined in the 1:1:1:1 ratios to create the polyherbal extract. Both in vitro antioxidant and in vitro antidiabetic activity of the extract were evaluated. For their preformulation investigations, a total of six polyherbal compositions were examined. Through Fourier transform infrared spectroscopic analysis, the phytochemicals present were identified. The medication was then put into capsules with a 0 size and evaluated for every aspect of a capsule. The stability of the most recent medicine was examined under diverse circumstances. The 2,2-diphenyl-1- picrylhydrazyl half maximal inhibitory concentration value for the polyherbal extract was 60.56 µg/ml indicating in vitro antioxidant activity. The anti-diabetic action was equivalent to the industry standard and dose-dependent, with an half maximal inhibitory concentration value of 59.82 µg/ml for inhibiting alpha-amylase and 67.28 µg/ml for inhibiting alpha-glucosidase. The polyherbal formulation 1 displayed the best flow qualities. According to Fourier transform infrared spectroscopic data, granules may include terpenes, tannins, phenols and flavonoids. In 30 min, the capsules with polyherbal formulation 1 had a 95.77 % cumulative drug release value. The capsules were discovered to be stable under many types of lighting, however they disintegrate above 70 % humidity and over 55°. As a result, it was discovered that the polyherbal capsules were stable and effective in treating hyperglycemia. [ABSTRACT FROM AUTHOR]

The present study was designed to investigate the role of estrogen receptor and KATP channel in cardioprotective effect of remote aortic preconditioning in rat heart. Remote preconditioning is a phenomenon in which brief episodes of ischemia and reperfusion to remote organs protect the target organ against sustained ischemia/reperfusion induced injury. Protective effects of remote aortic preconditioning are well established in the heart, but their mechanisms still remain to be elucidated. Remote aortic preconditioning in rats was produced by introducing four episodes of ischemia and reperfusion, each comprising of 5 min occlusion and 5 min reperfusion, through abdominal aorta. Perfused rat heart was isolated and subjected to global ischemia for 30 min followed by reperfusion for 120 min. The degree of cardiac injury was assessed by analysing the level of lactate dehydrogenase, creatin kinase, reactive oxygen species and nitrite in coronary effluent. Myocardial infarct size was also estimated macroscopically using tetrazolium tri chloride staining. Ethylinestradiol (10 µg/kg, orally) as estrogen receptor agonist was noted to reproduce remote aortic preconditioning mediated cardioprotection in ovariectomized rat. However, administration of glibenclamide along with or prior to ethylinestradiol abolished cardioprotection. Moreover, glibenclamide a KATP channel blocker, abolish cardioprotective effect of remote aortic preconditioning with daidzein a caveolin inhibitor (0.2 mg/kg subcutaneous). Ethylinestradiol significantly increased the release of nitric oxide and restored the attenuated cardioprotective effect of remote aortic preconditioning. These data provide the evidence that estrogen receptor activation involved in cardioprotective effect of remote aortic preconditioning-mediated trough opening of KATP channels. [ABSTRACT FROM AUTHOR]

The aim of present study was to formulate and evaluate self-microemulsifying drug delivery system containing piroxicam and to use the ability of porous magnesium alumina metasilicate as a solid carrier for self-microemulsifying drug delivery system. It was developed to resolve the problems of piroxicam such as low water solubility, low bioavailability and gastrointestinal irritation. Self-microemulsifying drug delivery system containing varying proportions of Capmul MCM, Cremophor EL and Transcutol-P were prepared and optimized using response surface methodology of Design-Expert® software version 10. Liquid self-microemulsifying drug delivery systems were subjected to in vitro evaluation, including self-emulsification efficiency study, droplet size, zeta potential measurement and in vitro drug release studies. Solid selfmicroemulsifying drug delivery system was prepared by adding liquid self-microemulsifying drug delivery system with Neusilin US2 and filled in hard gelatin capsule. The optimized formulation consists of 28.26 % of Capmul MCM, 44.16 % of Cremophor EL and 27.58 % of Transcutol-P. The results showed that the drug release profile of piroxicam from the self-microemulsifying drug delivery formulations was higher than the pure piroxicam powder. The release of piroxicam was rapid and complete. Solid self-microemulsifying drug delivery systems after filled in hard gelatin capsule, predicted to be a promising technique to deliver a liquid formulation in solid dosage form. [ABSTRACT FROM AUTHOR]

A library of 3,4,6,7-tetrahydro-3,3,6,6-tetramethyl-9,10-diphenylacridine-1,8-dione derivatives were synthesized via microwave-assisted three-component reaction employing silica supported sulphuric acid under solvent free conditions and tested for in vitro cholesterol esterase inhibitory activity. All synthesized compounds exhibited moderate to good inhibition of cholesterol esterase enzyme. Among all the synthesized acridinedione derivatives, compound HSM-1a showed the most promising activity with IC50 value of 1.53 μM against cholesterol esterase enzyme. Enzyme kinetic studies carried out for HSM-1a, revealed its mixed-type inhibition approach. Molecular protein-ligand docking studies were also performed to figure out the key binding interactions of HSM-1a with the amino acid residues of the enzyme's active site. Furthermore, acquiescence of some potent compounds to the Lipinski rule was also determined. [ABSTRACT FROM AUTHOR]

In an effort to search for more active antiinflammatory agent, a series of pyrazolinylbenzidines and isoxazolylbenzidines was designed, synthesized, and screened for their potential as novel orally inflammation inhibitors. Compounds 4,4'-bis-(1"-acetyl-5"-substitutedaryl-2"-pyrazolin-3"-yl)benzidines (8-13) and 4,4'-bis-(2"-substitutedaryl-isoxazolin-4'-yl)benzidines (14-19) have been synthesized from 4,4'-bis-(substituted benzylidenyl-acetyl)benzidines (2-7). The structures of the products have been delineated by spectral and elemental analysis. Compounds 2-19 evaluated for antiinflammatory activity and acute toxicity and results are reported. The compound 4,4'-bis-[1"-acetyl-5"-(p-methoxyphenyl)-2"-pyrazolin-3'-yl)benzidine (9) showed more potent and dose-dependent antiinflammatory activity in comparison to reference drug. [ABSTRACT FROM AUTHOR]

In the present studies, two series of 4-substituted-imidazolidines (IIIa-i and IIIj,k) were synthesized by reacting different tetrahydro-di-Schiff bases (IIa-i and IIj,k) with p-diethylaminobenzaldehyde/ dimethylaminobenzaldehyde. The title compounds were evaluated for their antibacterial and antifungal actions against some selected microbes. The results of microbiological evaluation revealed that two compounds, 4-(1,3-bis(benzo[d][1,3]dioxol-5-ylmethyl)-4-methylimidazolidin-2-yl)-N,N-diethyl aniline (IIIj), 4-(1,3-bis(benzo[d][1,3]dioxol-5-ylmethyl)-4-methylimidazolidin-2-yl)-N,N-dimethyl aniline (IIIk) were good in their antibacterial as well as antifungal actions. Minimum inhibitory concentration values (MIC) of the compounds are reported. [ABSTRACT FROM AUTHOR]

The c-Jan N-terminal kinases are members of the mitogen activated protein kinase family of signaling proteins. Amino pyridine based compounds, 4-anilino pyrimidine derivatives, and 2-pyridine carboxamide derivatives have been identified as potent JNK inhibitors with good cellular activity. In this study we calculated molecular topological and quantum chemical descriptors of 15 training compounds and three quantitative structure activity relationships models have been constructed. The significance of three models is judged on the basis of correlation, Fischer F test and quality factor (Q). This study is helpful for screening potent inhibitors of protein kinases. [ABSTRACT FROM AUTHOR]

A three dimensional quantitative structure-activity relationship study using the comparative molecular field analysis method was performed on a series of 3-aryl-4-[a-(1H-imidazol-1-yl) aryl methyl] pyrroles for their anticandida activity. This study was performed using 40 compounds, for which comparative molecular field analysis models were developed using a training set of 33 compounds. Database alignment of all 33 compounds was carried out by root-mean-square fit of atoms and field fit of the steric and electrostatic molecular fields. The resulting database was analyzed by partial least squares analysis with cross-validation; leave one out and no validation to extract optimum number of components. The analysis was then repeated with bootstrapping to generate the quantitative structure-activity relationship models. The predictive ability of comparative molecular field analysis model was evaluated by using a test set of 7 compounds. The 3D- quantitative structure-activity relationship model demonstrated a good fit, having r² value of 0.964 and a cross validated coefficient r² value as 0.598. Further comparison of the coefficient contour maps with the steric and electrostatic properties of the receptor has shown a high level of compatibility and good predictive capability. [ABSTRACT FROM AUTHOR]

This present work is an investigation of anticancer activities of the nitrogen mustards possessing quinazolinone, benzimidazole, benzoxazole, and benzothiazole nuclei by the three-dimensional Quantitative Structure Activity paradigm, Comparative Molecular Field Analysis. A total of 39 compounds were modelled in SYBYL 6.7 (Tripos, USA). The molecules were aligned by root-mean-square fit of atoms and field fit of the steric and electrostatic molecular fields and the resulting databases analysed by partial least squares analysis with cross-validation, leave-one-out and no validation to extract the optimum number of components. The analysis was then repeated with bootstrapping to give the final Quantitative Structure Activity Relationship models. Eight compounds, which were kept separately as test set, were used to test the predictive ability of the Comparative Molecular Field Analysis models. Out of the two models generated, one was found to be useful. The predicted activities of the test set were in good agreement with experimentally determined values. [ABSTRACT FROM AUTHOR]