Anti-HIV activity of semisynthetic derivatives of andrographolide and computational study of HIV-1 gp120 protein binding.

Andrographolide, a diterpene lactone of the Andrographis paniculata, displays anti-HIV activity in vitro. A series of andrographolide derivatives have been synthesized and evaluated for their anti-HIV activity in a cell-free virus infectivity assay using TZM-bl cells. As compared to andrographolide, 3-nitrobenzylidene derivative 6 showed higher in vitro anti-HIV activity, whereas 2',6'-dichloro-nicotinoyl ester derivative 9 showed higher Therapeutic Index.

Antimicrobial potential of 3-hydroxy-2-methylene-3-phenylpropionic acid derivatives.

Twenty Baylis-Hillman adducts were synthesized from different aromatic aldehydes and activated vinyl derivatives. The adducts, which are differently substituted 3-hydroxy-2-methylene-3-phenylpropionic acid derivatives, were screened for their antimicrobial activity in vitro by the serial dilution method. Many of these molecules displayed potent antibacterial and antifungal activities.

Antibacterial potential of citral derivatives.

Nine conjugated acid derivatives from monoterpene citral have been synthesized using ester, amide condensations, Wittig, Knoevenagel, Baylis-Hillman reactions and their antimicrobial activities were evaluated through disc diffusion and serial dilution methods. Several derivatives displayed interesting antimicrobial activity. Particularly, the Baylis-Hillman adducts 8-10 were found to have more potent antibacterial and antifungal activities than standard drugs namely chloramphenicol and nystatin respectively.

Anti-infective Potential of Hot-spring Bacteria.

Aim And Background: Antibiotic resistance currently spans most of the known classes of natural and synthetic antibiotics; limiting our options for treatment of infections and demanding discovery of new classes of antibiotics. Much effort is being directed towards developing new antibiotics to overcome this problem. Success in getting novel chemical entities from microbial sources depends essentially on novelty of its habitat.

Synthesis and antitumor activity of new retinobenzoic acids.

New retinobenzoic acid derivatives have been synthesized starting from 1,2,3,4-tetrahydro-1,1,2,4,4,6-hexamethylnaphthalene and 1,1,2,3,3-pentamethylindane. Four of the synthetic compounds displayed potent cytotoxic activities in vitro against human breast cancer and leukemic cell lines. Thus, these molecules can be further evaluated for the treatment of human leukemia and breast cancer.

Radiosensitization in human breast carcinoma cells by thymoquinone: role of cell cycle and apoptosis.

TQ (thymoquinone), the bioactive constituent of black seed (Nigella sativa), has been shown to inhibit the growth of various human cancers both in vitro and in vivo. This study reports the radiosensitizing effect of TQ on human breast carcinoma cells (MCF7 and T47D). TQ in combination with single dose of ionizing radiation (2.

An evaluation of the antidiabetic effects of Elaeocarpus ganitrus in experimental animals.

Objective: To evaluate the antidiabetic effects of the aqueous extract of Elaeocarpus ganitrus (EAG) in experimental animals.

Materials And Methods: The hypoglycemic activity of the EGA was evaluated in normoglycemic rats by single dose at three graded dose levels, viz. 250, 500 and 1000 mg/kg of body weight.

Development and validation of UPLC tandem mass spectrometry assay for separation of a phase II metabolite of ramipril using actual study samples and its application to a bioequivalence study.

In this paper, we present a validated UPLC-MS/MS assay for determination of ramipril and ramiprilat from human plasma samples. The assay is capable of isolating phase II metabolites (acylglucornides) of ramipril from in vivo study samples which is otherwise not possible using conventional HPLC conditions. Both analytes were extracted from human plasma using solid-phase extraction technique.

In vitro and in vivo immunostimulatory activity of Woodfordia fruticosa flowers on non-specific immunity.

Context: Woodfordia fruticosa Kurz. (Lythraceae), a non-rasayana immunomodulatory Indian medicinal plant, used traditionally as an anthelmintic, in dysentery, leprosy, blood diseases, leucorrhea, and menorrhagia.

Objective: To investigate the effect of ethanol extract of W.

Anticancer activity of andrographolide semisynthetic derivatives.

Andrographolide 1, a diterpene lactone of Andrographis paniculata, displays in vitro and in vivo antitumor activity against breast cancer models and mouse myeloid leukemia (M1) cells. In the present study, we report the semi-synthesis of andrographolide derivatives and their in vitro activity against A549 (ATCC) (NSCL cancer) cell line. Amongst the derivatives tested, compounds 3-5 displayed maximum activity, with IC50 values of 22-31 microg/mL.

Determination of free and liposomal amphotericin B in human plasma by liquid chromatography-mass spectroscopy with solid phase extraction and protein precipitation techniques.

Amphotericin B is available in various drug delivery systems such as cholesteryl sulfate complex, as lipid complex, and as liposomal formulation. The separation and measurement of free drug (drug which is not bound with liposomal lipids) and liposomal drug (drug which is entrapped in liposomes) in the human plasma after injection of liposomal Amphotericin B is of prime importance due to toxicity concerns. A robust, specific and sensitive method has been developed to effectively separate and then quantify the free drug and liposomal drug, present in human plasma.

IVUS-guided management of late stent malaposition with peri-stent restenosis with coronary artery aneurysm following drug-eluting stent implantation (paxlitaxel-eluting stent).

Late stent malapposition (LSM) within a coronary artery aneurysm is an unusual intravascular ultrasound (IVUS) finding at follow up, and has been reported to be more common after drug-eluting stent implantation than after bare-metal stenting. We describe a case of LSM with coronary artery aneurysm 6 months after paclitaxeleluting stent implantation. This unusual case was successfully managed under IVUS guidance.

Effect of Alstonia scholaris (Linn.) R. Br. on stress and cognition in mice.

Effect of stress and its modulation by methanolic extract of bark of Alstonia scholaris was studied using acute restraint stress model in mice. The extract was also evaluated for nootropic and antioxidant potential to support anti-stress activity testing. Acute restraint stress resulted in significant increase of plasma corticosterone, glucose, protein, cholesterol and triglyceride levels in stress group of animals.

Validated LC-MS/MS method for determination of Alverine and one of its hydroxy metabolites in human plasma along with its application to a bioequivalence study.

The present research work involves a first of its kind rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method developed and validated for simultaneous analysis of Alverine (ALV) and one of its hydroxy metabolites, para hydroxy Alverine (PHA) in human plasma. The analytes were extracted from the matrix using a simple solid-phase extraction procedure. Mebeverine was used as the internal standard for both analytes.

Effect of matrix treatment on spectroscopic properties of HCl catalysed sol-gel glasses containing coumarin laser dyes.

Coumarin 1, Coumarin 2 and Coumarin 120 are embedded in transparent sol-gel glass samples prepared by sol-gel process using dip method. The sol-gel matrix is given dip treatment with Methanol /Distilled Water (50/50 vol) for 1 to 16 h before dipping into dye solution. The effect of dipping time of matrix in Methanol/ Distilled Water on spectroscopic properties of coumarin dye doped glass samples has been studied.

Protective effect of Piper longum L. on oxidative stress induced injury and cellular abnormality in adriamycin induced cardiotoxicity in rats.

Effect of methanolic extract of fruits of P. longum (PLM) on the biochemical changes, tissue peroxidative damage and abnormal antioxidant levels in adriamycin (ADR) induced cardiotoxicity in Wistar rats was investigated. PLM was administered to Wistar albino rats in two different doses, by gastric gavage (250 mg/kg and 500 mg/kg) for 21 days followed by ip ADR (15 mg/kg) on 21st day.

Immunomodulatory activity of methanolic extract of Murraya koenigii (L) Spreng. leaves.

Immunomodulatory activity of methanolic extract of M. koenigii leaves was evaluated on humoral and cell mediated immune response to ovalbumin, phagocytic activity by carbon clearance test, nitric oxide (NO) release from murine peritoneal macrophages and cyclophosphamide induced myelosuppression. Significant increase in the NO production by mouse peritoneal macrophages was detected in culture supernatants indicated increased phagocytic activity of macrophages.

Liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for simultaneous determination of tenofovir and emtricitabine in human plasma and its application to a bioequivalence study.

A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for simultaneous quantification of Tenofovir (TEN) and Emtricitabine (EMT) in human plasma using Chromolith Speed Rod RP18. The mass transition ion-pair has been followed as m/z 288.10-->176.

Bioadhesive ranitidine hydrochloride for gastroretention with controlled microenvironmental pH.

Ranitidine hydrochloride is a H(2) receptor blocker used in the treatment of gastric ulcers. Pharmacological factors, in addition to the dosage regimen, favor development of a sustained-release system for ranitidine especially in the therapeutic condition of erosive esophagitis. This investigation delves into the development of bioadhesive type of gastroretentive formulation (tablets) of ranitidine.

Attenuation of Acute and Chronic Restraint Stress-induced Perturbations in Experimental Animals by Nelumbo nucifera Gaertn.

Aqueous extract of leaves of Nelumbo nucifera was investigated on acute stress (immobilization stress)-induced biochemical alterations in Swiss mice. The animals were also subjected to acute physical stress (swimming endurance test) and acute chemical stress (writhing test) to gauge the antistress potential of the extract. Further to evaluate the antistress activity of Nelumbo nucifera in chronic stress condition, fresh Wistar rats were subjected to cold restraint stress (4 degrees for 1 h) for 7 days after 21 days of pretreatment with the extract.

Rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of clonidine in human plasma.

A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the estimation of clonidine in human plasma. Clonidine was extracted from human plasma by using solid-phase extraction technique. Nizatidine was used as the internal standard.

Effects of Chlorophytum borivilianum on sexual behaviour and sperm count in male rats.

This study was designed to evaluate the aphrodisiac and spermatogenic potential of the aqueous extract of dried roots of Chlorophytum borivilianum (CB) in rats. Male Wistar albino rats were divided into four groups. Rats were orally treated with (1) CONTROL GROUP: distilled water; (2) CB 125 mg/kg/day; (3) CB 250 mg/kg/day; and (4) Viagra((R)) group: 4 mg/kg/day sildenafil citrate and their sexual behaviour was monitored 3 h later using a receptive female.

Anti-stress and anti-oxidant effects of roots of Chlorophytum borivilianum (Santa Pau & Fernandes).

The aqueous extract of C. borivilianum (250 mg/kg for 7 days) significantly reverted the elevated levels of plasma glucose, triglycerides, cholesterol and serum corticosterone and also reduced the ulcer index, adrenal gland weight more as effectively as the standard drug (diazepam) in rats. At 125 mg/kg po, it showed a mild anti-stress activity.

Physicochemical, in silico and in vivo evaluation of a danazol-beta-cyclodextrin complex.

Inclusion complexation of danazol with beta-cyclodextrin (BCD) in aqueous solution, in solid state and in silico state was investigated to examine the interactions of danazol with BCD. The study also explored the potential application of danazol-beta-cyclodextrin complex as an oral antiovulatory agent. Phase solubility analysis suggested formation of first-order soluble complex with stability constant 972.

Danazol-beta-cyclodextrin binary system: a potential application in emergency contraception by the oral route.

This study explored the potential of beta-cyclodextrin to improve the aqueous solubility and dissolution of danazol, investigated a simple and less expensive method for preparation of a danazol-beta-cyclodextrin binary system, and explored the potential application of a danazol-beta-cyclodextrin binary system as a single-dose emergency contraceptive. Phase solubility analysis indicated formation of a first-order soluble complex with stability constant 972.03 M(-1), while Job's plot affirmed 1:1 stoichiometry.