Steroidal carbonitriles as potential aromatase inhibitors.

Estrogens, responsible for the growth of hormone-dependant breast cancer are biosynthesized from androgens involving aromatase enzyme in the last rate limiting step. Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. Novel 4-phenylthia derivatives (2, 3 and 7) have been synthesized as aromatase inhibitors.

An open-label study on the effect of flax seed powder (Linum usitatissimum) supplementation in the management of diabetes mellitus.

Diabetes mellitus is characterized by hyperglycemia and associated with aberrations in the metabolism of carbohydrate, protein, and lipid that result in development of secondary complications. Extensive studies have indicated that nutritional therapy plays a pivotal role in the controlling or postponing of development of these secondary complications. Several functional foods have been shown to possess hypoglycemic and hypolipidemic properties.

Traditional uses, phytochemistry and pharmacology of Clerodendron glandulosum Coleb--a review.

Present review for the first time provides a complete botanical description and information on ethnomedicinal uses of Clerodendron glandulosum.Coleb (CG; Fam, Verbenaceae). Recent studies conducted from our laboratory provide pharmacological evidence for its anti-hypertensive, anti-diabetic and anti-obesity potentials.

Molecular characterization of Bacillus thuringiensis isolated from diverse habitats of India.

Bacillus thuringiensis (Bt) strains were isolated from 94 samples from different geographical regions. Novel types of crystalline inclusion bodies were observed from some of the isolates. Crystalline inclusions of bipyramidal, spherical and cuboidal morphology were found produced by most of the isolates.

High-resolution quantitative phase microscopic imaging in deep UV with phase retrieval.

High-resolution three-dimensional (3D) microscopic imaging requires the use of short wavelengths. Quantitative 3D imaging techniques, such as digital holographic microscopy, require interference between the object beam and a known reference background for the extraction of phase information. At shorter wavelengths, due to short coherence lengths, it may be difficult to implement a two-beam off-axis setup.

Synthesis, spectroscopic characterization and DNA nuclease activity of Cu(II) complexes derived from pyrazolone based NSO-donor Schiff base ligands.

Two neutral mononuclear Cu(II) complexes have been prepared in EtOH using Schiff bases derived from 4-toluoyl pyrazolone and thiosemicarbazide. Both the ligands have been characterized on the basis of elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data. The molecular geometry of one of these ligands has been determined by single crystal X-ray study.

Clerodendron glandulosum.Coleb extract prevents in vitro human LDL oxidation and oxidized LDL induced apoptosis in human monocyte derived macrophages.

This study reports the protective role of Clerodendron glandulosum (CG) extract against in vitro LDL oxidation and Ox-LDL induced macrophage apoptosis using various experimental models. Effect of CG extract on Cu(2+) mediated LDL oxidation kinetics and formation of various intermediary products and its ability to prevent human monocyte derived macrophage mediated LDL oxidation have been investigated. Ox-LDL induced macrophage apoptosis was evaluated by nuclear condensation, cell cycle analysis, and annexin V-FITC/PI staining in presence or absence of CG extract.

Antihyperglycaemic and renoprotective effect of Boerhaavia diffusa L. in experimental diabetic rats.

The present study evaluates the efficacy of ethanolic extract of Boerhaavia diffusa L (BD) administered orally at a dose of 500mg/kg body weight for a period of 30 days to alloxanized diabetic rats and its efficacy compared with the standard hypoglycaemic drug metformin. Diabetic animals showed glycemic dysregulation, altered ionic balance, increased levels of serum markers of kidney function, and reduced Na+-K+ ATPase activity and endogenous antioxidant status. Administration of BD not only maintained the ionic balance and renal Na+-K+ ATPase activity but also significantly minimized diabetic hyperglycaemia.

Therapy with methanolic extract of Pterocarpus marsupium Roxb and Ocimum sanctum Linn reverses dyslipidemia and oxidative stress in alloxan induced type I diabetic rat model.

Methanolic extracts of Pterocarpus marsupium Roxb (P. marsupium) and Ocimum sanctum Linn (O. sanctum) were prepared separately and then administered to both non-diabetic and alloxan induced diabetic adult female Wistar rats as a mixture of both at a dosage of 500mg/kg body weight, and its effect was checked on serum and tissue lipids together with corticosterone, estrogen and progesterone profile.

Clerodendron glandulosum.Coleb extract ameliorates high fat diet/fatty acid induced lipotoxicity in experimental models of non-alcoholic steatohepatitis.

This study evaluates the protective role of Clerodendron glandulosum.Coleb (CG) aqueous extract against high fat diet/fatty acid induced lipotoxicity in experimental models of non-alcoholic steatohepatitis (NASH). Supplementation of NASH mice with CG extract (1% and 3% in high fat diet for 16 weeks) prevented high fat diet induced elevation in liver enzymes, plasma and hepatic lipids, mitochondrial oxidative stress and compromised enzymatic and non-enzymatic antioxidant status and histopathological damage to hepatocytes.

Three-dimensional microscopy with single-beam wavefront sensing and reconstruction from speckle fields.

Generally, 3D digital holographic microscopy requires the interference of the object wave with a known reference beam under coherent illumination to perform numerical focusing. This configuration may be challenging for some applications, including the use of exotic wavelengths such as x rays, miniaturized instrumentation, etc. Single-beam intensity measurement followed by phase retrieval techniques is attractive for wavefront sensing and reconstruction, including applications with low coherence.

A novel itraconazole bioadhesive film for vaginal delivery: design, optimization, and physicodynamic characterization.

The purpose of this work was to design and optimize a novel vaginal drug delivery system for more effective treatment against vaginal candidiasis. Itraconazole was formulated in bioadhesive film formulations that could be retained in the vagina for prolonged intervals. The polymeric films were prepared by solvent evaporation and optimized for various physicodynamic and aesthetic properties.

Monodispersed superparamagnetic FeO4 nanoparticles: synthesis and characterization.

Monodispersed Fe3O4 (magnetite) nanoparticles are synthesized by non-aqueous thermal decomposition route. The powder XRD reveals single phase spinel structure with 60 angstroms particle size. The TEM image shows nearly monodispersed spherical particles with log-normal median diameter of 49 A and size distribution in In(D) 0.

A novel triterpenoid isolated from the root bark of Ailanthus excelsa Roxb (Tree of Heaven), AECHL-1 as a potential anti-cancer agent.

Background: We report here the isolation and characterization of a new compound Ailanthus excelsa chloroform extract-1 (AECHL-1) (C(29)H(36)O(10); molecular weight 543.8) from the root bark of Ailanthus excelsa Roxb. The compound possesses anti-cancer activity against a variety of cancer cell lines of different origin.

Influence of chitosan crosslinking on bitterness of mefloquine hydrochloride microparticles using central composite design.

The present work examines the influence of various process and product parameters on mefloquine hydrochloride (MFL) entrapped in crosslinked chitosan microparticles for masking the bitterness. A central composite design (CCD) was employed to investigate the effect of three process and product variables, namely amount of MFL, chitosan and sodium hydroxide (crosslinking agent) on the incorporation efficiency, particle size, drug release at pH 6.8 and bitterness score.

Anti-oxidant activity mediated neuroprotective potential of trimetazidine on focal cerebral ischaemia-reperfusion injury in rats.

1. The present study was designed to investigate the neuroprotective effect of trimetazidine (TMZ) following focal cerebral ischaemia-reperfusion (I/R) injury in rat forebrain. 2.

Formulation, characterization, and in vitro evaluation of bioadhesive gels containing 5-Fluorouracil.

The objective of this study was to prepare and evaluate in vitro the bioadhesive gels of 5-Fluorouracil (FU) for the treatment of oropharyngeal cancer. In preformulation study, the physicochemical interactions between FU and polymers were investigated by X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectrophotometry, and differential scanning calorimetry (DSC). According to FTIR, XRD, and DSC studies, the drug did not show any evidence of an interaction with the polymers used and was present in an unchanged state.

Excision of Anabaena PCC 7120 nifD element in Escherichia coli: Growth kinetics and RecA regulated xisA expression and DNA rearrangement.

Anabaena PCC 7120 nifHDK operon is interrupted by an 11 kb DNA element which is excised during the development of heterocysts by Excisase A, encoded by the xisA gene residing on the element. The excision is a site-specific recombination event that occurs at the 11 base pair direct repeats flanking the element. Earlier work showed the excision of the 11 kb element in Escherichia coli at a frequency 0.

Optimization of formulation components and characterization of large respirable powders containing high therapeutic payload.

The aim of the study was to optimize and characterize high therapeutic payload large respirable powders prepared by spray-drying technique for maximum fine particle fraction with minimum quantities of excipients. Influence of formulation components was optimized by a three-factor, five-level central composite design having different proportions of L-leucine (X1), tobramycin sulfate (X2), and poloxamer-188 (X3) as the independent variables and fine particle fraction as a response variable (Y). Large respirable powders were characterized for particle size, size distribution, moisture, crystallinity, and morphology.

Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability.

The main purpose of this work was to develop an oral microemulsion formulation for enhancing the bioavailability of acyclovir. A Labrafac-based microemulsion formulation with Labrasol as surfactant and Plurol Oleique as cosurfactant was developed for oral delivery of acyclovir. Phase behavior and solubilization capacity of the microemulsion system were characterized, and in vivo oral absorption of acyclovir from the microemulsion was investigated in rats.

Understanding the antitumor activity of novel tricyclicpiperazinyl derivatives as farnesyltransferase inhibitors using CoMFA and CoMSIA.

3D-QSAR studies of some tricyclicpiperazinyl derivatives as farnesyltransferase inhibitors were performed by comparative molecular field analysis (CoMFA) and comparative molecular similarity indices (CoMSIA) methods to rationalize the structural requirements responsible for the inhibitory activity of these compounds. The global minimum energy conformer of the template molecule 35, the most active and pharmacokinetically stable molecule of the series, was obtained by simulated annealing method and used to build structures of the molecules in the dataset. The CoMFA model obtained after the removal of outliers produced statistically significant results with cross-validated and conventional correlation coefficients of 0.

Profile of non communicable disease risk factors in an industrial setting.

Aim: The profile of non communicable diseases (NCD) risk factors was identified in an industry by pre tested WHO's STEPS questionnaire.

Settings And Design: A cross-sectional survey of all employment categories of an Industry (2000 employees) was done after randomly selecting subjects (220) from worker (52%) and non worker categories (47.4%), after informed consent.

Thermoluminescence dosimetric characteristics of beta irradiated salt.

The thermoluminescence (TL) characteristics of sodium chloride (NaCl), known as common salt, used for cooking purposes (iodised salt), have been studied in the present paper considering its usage as an 'accidental dosemeter' in the case of a nuclear fallout. TL characteristics of common salt have been examined under excitation with a beta dose of 20 Gy from a 90Sr beta source. The salt specimens are used in the form of discs.

Role of calcium in gene delivery.

The treatment of genetic diseases using therapeutic gene transfer is considered to be a significant development. This development has brought with it certain limitations, and the process of overcoming these barriers has seen a drastic change in gene delivery. Many metal ions such as Mg2+, Mn2+, Ba2+ and, most importantly, Ca2+ have been demonstrated to have significant roles in gene delivery.