Effects of phytochemicals of Flemingia vestita (Fabaceae) on glucose 6-phosphate dehydrogenase and enzymes of gluconeogenesis in a cestode (Raillietina echinobothrida).

The crude root-peel extract of Flemingia vestita, containing genistein as the major isoflavone, has a vermifugal/vermicidal effect. It acts by causing flaccid paralysis accompanied by alterations in the activities of several tegumental enzymes and other metabolic activities in the fowl tapeworm, Raillietina echinobothrida. To elucidate the mode of action of the putative phytochemicals on energy metabolism, crude root-peel extract, pure genistein and praziquantel were tested on glucose 6-phosphate dehydrogenase (G6PDH) and enzymes of gluconeogenesis--pyruvate carboxylase (PC), phosphoenolpyruvate carboxykinase (PEPCK) and fructose 1,6-bisphosphatase (FBPase)--in R.

99mTc-Tetraethylenepentamine-Folate--a new 99mTc-based folate derivative for the detection of folate receptor positive tumors: synthesis and biological evaluation.

A new radiopharmaceutical, 99mTc-Tetraethylenepentamine(TEPA)-Folate has been synthesized introducing TEPA to the gamma-carboxyl group of folic acid. This binds with 99mTc high efficiency at ambient temperature. The resulting 99mTc-N5-Folate is stable under physiological conditions at least for 24 h after radiocomplexation.

Anthelmintic efficacy of Flemingia vestita (Fabaceae): alterations in glucose metabolism of the cestode, Raillietina echinobothrida.

The root-tuber peel of Flemingia vestita and its active component, genistein, were tested in respect of glucose metabolism in the cestode, Raillietina echinobothrida. Live R. echinobothrida, collected from the intestine of freshly slaughtered domestic fowl, were incubated at 39+/-1 degrees C in defined concentrations of the root-peel crude extract (5 mg/ml), genistein (0.

Anthelmintic efficacy of genistein, the active principle of Flemingia vestita (Fabaceae): alterations in the free amino acid pool and ammonia levels in the fluke, Fasciolopsis buski.

The crude root-peel extract of Flemingia vestita, its active principle genistein and the reference flukicide oxyclozanide were tested against Fasciolopsis buski, the giant intestinal trematode. The amino acid composition of F. buski was demonstrated using HPLC and it was observed that the free amino acid (FAA) pool of the control worm consisted of aspartate, threonine, serine, glutamic acid, glutamine, proline, glycine, alanine, valine, methionine, isoleucine, leucine, tyrosine, lysine, histidine, arginine, phosphoserine, taurine, citrulline, ornithine, beta-alanine, and gamma-amino butyric acid (GABA).

Synthesis and anti-implantation activity of new stilbene derivatives.

New stilbene (CAS 56-53-1) derivatives have been synthesized by reductive elimination of desoxybenzoin analogs which were obtained by Fries rearrangement of the corresponding phenolic esters. The chemical structures of the compounds obtained were confirmed by 1H-NMR, IR and elemental analysis. Anti-implantation activity of the compounds was determined by performing experiments with adult male and female Spargue-Dawley rats of proven fertility.

Nuclear localization and in situ DNA damage by Mycobacterium tuberculosis nucleoside-diphosphate kinase.

Nucleoside-diphosphate kinase of Mycobacterium tuberculosis (mNdK) is a secretory protein, but the rationale behind secreting an enzyme involved in the maintenance of cellular pool of nucleoside triphosphates is not clearly understood. To elucidate the biological significance of mNdK secretion, we expressed mNdK fused to green fluorescent protein in HeLa and COS-1 cells. Interestingly, mNdK was detected in the nuclei of HeLa and COS-1 cells.

Efficient oxidizing methods for the synthesis of oxandrolone intermediates.

Mild, efficient and eco-friendly oxidation of 17alpha-methylandrostan-3beta-17beta-diol (1) has been studied with three different reagents viz. pentavalent iodine reagent 2-iodoxy benzoic acid (IBX) in DMSO at 65 degrees C, sodium hypochlorite and H2O2/Na2WO4 under phase transfer conditions to give 17beta-hydroxy-17alpha-methylandrostan-3-one (mestanolone 2), a drug intermediate as oxidized product. The H2O2/Na2WO4/PTC gave mestanolone in high yield and purity whereas sodium hypochlorite/PTC system yielded some chlorinated material along with the mestanolone.

Oropharyngeal leiomyosarcoma.

A unique case of Oropharyngeal leiomyosarcoma in a 32 years old male is presented with the review of literature The details of clinical, radiological, histopathological and operative findings are discussed The treatment of choice is complete tumor removal The patient was symptom free with no evidence of loco regional or distant metastasis at one-year follow up.

Potential hypotensive agents: synthesis and hypotensive activity of oxime ethers derived from 1-naphthoxepines and related compounds.

The synthesis and pharmacological evaluation of substituted oximino-ethers 1 and 2 of naphth[1,2-b]- and naphth[2,1-b]-oxepin-5-ones (4 and 8) were carried out. The hypotensive activity of oximino-ethers 1 and 2 was evaluated on anaesthetized cats. The results indicated that 1c caused a fall of 80 mm/Hg for >100' at a dose of 5mg/kg iv in anaesthetized cats.

Anthelmintic efficacy of Flemingia vestita (Fabaceae): alteration in the activities of some glycolytic enzymes in the cestode, Raillietina echinobothrida.

The crude root-peel extract of Flemingia vestita, genistein and praziquantel were tested against some selected glycolytic enzymes--hexokinase (HK), phosphofructokinase (PFK), phosphoenolpyruvate carboxykinase (PEPCK), pyruvate kinase (PK), lactate dehydrogenase (LDH), malate dehydrogenase (MDH) and malic enzyme (ME)--of the fowl tape worm, Raillietina echinobothrida. Following exposure to the various treatments, the activities of HK, PFK, PEPCK and LDH increased by 33-39%, 41-125%, 44-49% and 55-67%, respectively, and that of PK decreased by 14-26% in the parasite at the time of paralysis. The MDH and ME activities of the tissue homogenate were also found to be higher by 22-43% and 28-59%, respectively, in the treatments.

Synthesis and evaluation of novel 1,4-naphthoquinone derivatives as antiviral, antifungal and anticancer agents.

The synthesis and evaluation of some 2-substituted-1,4-naphthoquinones 2, S-(1,4-naphthoquinon-2-yl)-mercaptoalkanoic acid amides 4, related benzoquinone and naphthoquinone derivatives 6-9 and 2,3-disubstituted 1,4-naphthoquinones 10-11 were carried out. The antifungal, antibacterial, antiviral and anticancer activities were determined by using the standard assay. The results show that compounds 2b and 10a showed in vitro antiviral activity against Influenza-A Virus and Herpes Simplex Virus and possess pronounced antifungal profile whereas 4a showed anticancer activities against Lymphoid Leukaemia P 388.

Chemo- and stereoselective synthesis of benzocycloheptene and 1-benzoxepin derivatives as alpha-sympathomimetic and anorexigenic agents.

The synthesis and pharmacological evaluation of cis- and trans-6-amino-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ols 4a-c and 5a-c and cis- and trans-4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ols 4d-f and 5d-f were carried out. Chemo- and stereoselective synthesis of 5a-f was achieved by reduction of corresponding alpha-amino ketones 3a-f with LiAl(t-BuO)3H. cis-4-Amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol 4d and trans-4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol 5d exhibited marked anorexigenic activity in mice at a dose of LD50 800 and 500 mg/kg and ED50 75 and 55 mg/kg, respectively, while the analog cis-2,3-dihydroxy-6-amino-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol 8 showed typical alpha-sympathomimetic activity.

1- and 2-substituted naphthalenes: a new class of potential hypotensive agents.

A series of 2-substituted aminomethyloxy naphthalenes 1 and 4-(1-naphthoxy-2-substituted aminomethyl)-butanoic acids 2 were synthesized by Mannich reaction of 4-(2-naphthoxy)-butanoic acid 3 and 4-(1-naphthoxy)-butanoic acid 4 with appropriate secondary amines and para-formaldehyde. The newly synthesized compounds were tested for their hypotensive activity at 5 mg/kg i.v.

Filarial chyluria: long-term experience of a university hospital in India.

Background: Filariasis is an endemic problem in various Indian states. We evaluated the results of long-term follow up (10-20 years) of patients with filarial chyluria.

Methods: We conducted a retrospective analysis of 160 patients treated for filarial chyluria who presented to the Banaras Hindu University Hospital from 1982 to 1992.

Design, synthesis and evaluation of novel 1,4-naphthoquinone derivatives as antifungal and anticancer agents.

A series of 1,4-naphthoquinone derivatives were synthesized and tested for antifungal and antitumor activity against a number of fungal disease causative species and Walker 256 carcinoma cell lines. The results show that the compounds 8a,e and 11b possess pronounced antifungal profile where as 7b and f were found to be active against Walker 256 carcinoma cell lines. Moreover 7c and 11a showed inhibitory effect against reverse transcriptase enzyme from Rauscher Murine Leukemia Virus.

Primary Sjogren's syndrome: rarity in India.

Objective: Primary Sjogren's syndrome (SS) is rarely reported from India. We have studied the clinical spectrum and immunological profile of patients with primary SS.

Methods: A prospective analysis of patients with primary Sjogren's syndrome fulfilling San Francisco criteria, seen at our clinic in the last 10 years was carried out.

Conformational fluctuations in anthrax protective antigen: a possible role of calcium in the folding pathway of the protein.

Protective antigen (PA) is the central receptor binding component of anthrax toxin, which translocates catalytic components of the toxin into the cytosol of mammalian cells. Ever since the crystal structure of PA was solved, there have been speculations regarding the possible role of calcium ions present in domain I of the protein. We have carried out a systematic study to elucidate the effect of calcium removal on the structural stability of PA using various optical spectroscopic techniques, limited proteolysis and mutational analysis.

Minor groove binding DNA ligands with expanded A/T sequence length recognition, selective binding to bent DNA regions and enhanced fluorescent properties.

DNA minor groove ligands provide a paradigm for double-stranded DNA recognition, where common structural motifs provide a crescent shape that matches the helix turn. Since minor groove ligands are useful in medicine, new ligands with improved binding properties based on the structural information about DNA-ligand complexes could be useful in developing new drugs. Here, two new synthetic analogues of AT specific Hoechst 33258 5-(4-methylpiperazin-1-yl)-2-[2'-(3,4-dimethoxyphenyl)-5'-benzimidazolyl] benzimidazole (DMA) and 5-(4-methylpiperazin-1-yl)-2-[2'[2''-(4-hydroxy-3-methoxyphenyl)-5' '-benzimidazolyl]-5'-benzimidazolyl] benzimidazole (TBZ) were evaluated for their DNA binding properties.

Acid induced unfolding of anthrax protective antigen.

Acidic pH plays an important role in the membrane insertion of protective antigen (PA) of anthrax toxin leading to the translocation of the catalytic moieties. The structural transitions occurring in PA as a consequence of change in pH were investigated by fluorescence and circular dichroism measurements. Our studies revealed the presence of two intermediates on-pathway of acid induced unfolding; one at pH 2.

Influence of phenyl ring disubstitution on bisbenzimidazole and terbenzimidazole cytotoxicity: synthesis and biological evaluation as radioprotectors.

DNA minor groove binders, Hoechst 33258 and Hoechst 33342, have been reported to protect against radiation-induced DNA-strand breakage, but their mutagenicity and cytotoxicity limit their use as protectors of normal tissue during radiotherapy and as biological radioprotectors during accidental radiation exposure. On the basis of these observations, two new nontoxic disubstituted benzimidazoles were synthesized, one having two methoxy groups (5-(4-methylpiperazin-1-yl)-2-[2'-(3,4-dimethoxyphenyl)-5'-benzimidazolyl]benzimidazole, 5) and another having a methoxy and a hydroxyl group (5-(4-methylpiperazin-1-yl)-2-[2'[2''-(4-hydroxy-3-methoxyphenyl)-5' '-benzimidazolyl]-5'-benzimidazolyl]benzimidazole, 6) ortho to each other on the phenyl ring. The radiomodifying effects of these nontoxic ligands were investigated with a human glioma cell line exposed to low linear energy transfer radiation by determining cell survival and cell proliferation compared with effects of the parent compound, Hoechst 33342.

Anthelmintic efficacy of Flemingia vestita (Fabaceae): Effect of genistein on glycogen metabolism in the cestode, Raillietina echinobothrida.

The edible root-tuber peel of Flemingia vestita and its major active component, genistein, have been earlier shown to have a vermifugal/vermicidal effect on cestodes in vitro by causing a flaccid paralysis and alterations in the tegumental architecture and activity of several enzymes associated with the tegumental interface of the parasite. Pursuing further investigation on the mode of action of this putative anthelmintic, the crude peel extract and pure genistein were further tested in respect of glycogen metabolism in the fowl tapeworm, Raillietina echinobothrida. On exposure to the plant root peel crude extract (5 mg/ml) and genistein (0.

Artificial neural networks in predicting optimum renal stone fragmentation by extracorporeal shock wave lithotripsy: a preliminary study.

Objective: To assess the ability of artificial neural networks (ANNs) to predict optimum renal stone fragmentation in patients being managed by extracorporeal shock wave lithotripsy (ESWL).

Patients And Methods: The study included 82 patients with renal stones who were being treated by ESWL. Data (input and output values) from 60 patients in whom there was optimum fragmentation of stones by ESWL were used for training the ANN.

Synthesis and pharmacological studies of some 2-t-amino and 2,3-di-t-amino substituted 1,4-naphthoquinones and related compounds.

Series of 2-t-amino and 2,3-di-t-amino substituted-1,4-naphthoquinones have been synthesised from corresponding 1,4-naphthoquinones by reaction with secondary amines. The compounds have been evaluated for their broad spectrum antimicrobial, antiviral and anticancer activity. In the preliminary screening results 8a and 9a have shown profile of an antimicrobial agent.

Anthelmintic efficacy of Flemingia vestita: genistein-induced effect on the activity of nitric oxide synthase and nitric oxide in the trematode parasite, Fasciolopsis buski.

The root-tuber peel of Flemingia vestita, an indigenous leguminous plant of Meghalaya (Northeast India), has usage in local traditional medicine as curative against worm infections. The peel and its active component, genistein, have been shown to cause flaccid paralysis, deformity of tegumental architecture and alterations in the activity of several enzymes in platyhelminth parasites. To investigate further the mode of action and anthelmintic efficacy of the plant-derived components, the crude peel extract of F.

Embolization of cranial/spinal tumours and vascular malformations with hydrogel microspheres. An experience of 69 cases.

Objective: To evaluate polymethyl methacrylate hydrogel microspheres (HMs) as an embolization material in the management of hypervascular craniofacial and spinal lesions.

Material And Methods: Sixty-nine patients with vascular lesions of the craniofacial and spinal regions underwent embolization with HM. The pathologies included craniofacial tumours (n=38), cranial arteriovenous malformations (AVMs) (n=7), dural AVM (n=1), cavernous carotid fistula (n=1), spinal tumours (n=7), spinal AVMs (n=6), orbital lesions (n=4) and scalp AVMs (n=5).