Lignans from Piper cubeba

From the hot petrol extract of Piper cubeba ftuits, six lignans were isolated. Two of these, which have been obtained from a natural source for the first time, have been characterized as (2R,3R)-2-(3″,4″,5″-trimethoxybenzyl)-3-(3′,4′-methylenedioxybenzyl)-1,4-butanediol [(?)-dihydroclusin] and (3R,4R)-3,4-bis-(3,4,5-trimethoxybenzyl)tetra-hydro-2-furanol [(?)-cubebinin]. (?)Cubebin, (?)-hinokinin, (?)-clusin and (?)-dihydrocubebin were also found in this plant. Only (?)-cubebin has been reported so far from this source.     

Associations between Active Travel to Work and Overweight,Hypertension, and Diabetes in India: A Cross-Sectional Study

Background

Increasing active travel (walking, bicycling, and public transport) is promoted as a key strategy to increase physical activity and reduce the growing burden of noncommunicable diseases (NCDs) globally. Little is known about patterns of active travel or associated cardiovascular health benefits in low- and middle-income countries. This study examines mode and duration of travel to work in rural and urban India and associations between active travel and overweight, hypertension, and diabetes.

Methods and Findings

Cross-sectional study of 3,902 participants (1,366 rural, 2,536 urban) in the Indian Migration Study. Associations between mode and duration of active travel and cardiovascular risk factors were assessed using random-effect logistic regression models adjusting for age, sex, caste, standard of living, occupation, factory location, leisure time physical activity, daily fat intake, smoking status, and alcohol use. Rural dwellers were significantly more likely to bicycle (68.3% versus 15.9%; p<0.001) to work than urban dwellers. The prevalence of overweight or obesity was 50.0%, 37.6%, 24.2%, 24.9%; hypertension was 17.7%, 11.8%, 6.5%, 9.8%; and diabetes was 10.8%, 7.4%, 3.8%, 7.3% in participants who travelled to work by private transport, public transport, bicycling, and walking, respectively. In the adjusted analysis, those walking (adjusted risk ratio [ARR] 0.72; 95% CI 0.58–0.88) or bicycling to work (ARR 0.66; 95% CI 0.55–0.77) were significantly less likely to be overweight or obese than those travelling by private transport. Those bicycling to work were significantly less likely to have hypertension (ARR 0.51; 95% CI 0.36–0.71) or diabetes (ARR 0.65; 95% CI 0.44–0.95). There was evidence of a dose-response relationship between duration of bicycling to work and being overweight, having hypertension or diabetes. The main limitation of the study is the cross-sectional design, which limits causal inference for the associations found.

Conclusions

Walking and bicycling to work was associated with reduced cardiovascular risk in the Indian population. Efforts to increase active travel in urban areas and halt declines in rural areas should be integral to strategies to maintain healthy weight and prevent NCDs in India. Please see later in the article for the Editors'' Summary     

Ecdysteroid glycosides from Sida rhombifolia L

Seven ecdysteroids, including the three new compounds 1-3, were isolated from Sida rhombifolia L. Their structures and configurations were determined by extensive spectroscopic techniques in combination with chemical derivatization. The four known compounds--ecdysone (4), 20-hydroxyecdysone (5), 2-deoxy-20-hydroxyecdysone-3-O-beta-D-glucopyranoside (6), and 20-hydroxyecdysone-3-O-beta-D-glucopyranoside (7)--are reported for the first time from this plant.     

Fructose, 1,6-diphosphate mitigates CCl4 suppressed nitric oxide synthase activity in rats

Effect of fructose 1,6-diphosphate (FDP) and carbon tetrachloride (CCl4) were studied individually and in combination on rat endothelial (ET) and smooth muscle cell (SMC) nitric oxide synthase (NOS) activities in vivo, inhibition of ET and SMC NOS activity in CCl4 treated rats was reversed in FDP + CCl4 treated animals. Cellular based NOS activity was significantly increased in FDP treated group of rats when compared to non treated controls. The results suggest a significant increase in NOS in rats treated with a combination of FDP + CCl4 thus overcoming the suppression of NOS exposed to CCl4 alone.     

Deconvolution of the fluorescence spectra into its component Gaussians: a method to analyze the binding of coumarin to bovine serum albumin

7-N,N-Diethylamino-4-methylcoumarin, (cou-1), a readily available laser dye binding to bovine serum albumin (BSA), at room temperature has been studied by steady state fluorescence spectroscopy. Existing methods of analysis of the binding to obtain the binding parameters are based on the change in fluorescence intensity at a particular wavelength. These methods are not convenient when there is a gradual shift in the emission maxima for increasing protein concentration. In this paper we present a method to obtain the binding constants of cou-1 to BSA using a Windows '95 based package to deconvolute the asymmetrical spectrum (fluorescence intensity versus wave number curve) into two Gaussians, each corresponding to the binding of the fluorophore to a particular site. This method is convenient to analyze the binding constant data and obtain the binding parameters of each binding site, and can also provide information about the microenvironment of each site, relating micropolarity and microviscosity.     

Effect of prostaglandin F2alpha on gonadal carbohydrate metabolism of silkworm,Bombyx mori L

Effect of prostaglandin F2alpha (PGF2alpha) on carbohydrate accumulation in gonads of the multivoltine silkworm (hybrid: Xinhang x Keming) has been studied by means of topical application to larvae of the silkworm. Increased weights of larvae and reproduction organs, as well as carbohydrate metabolism in gonads of the silkworm, Bombyx mori L. was found after treatment with prostaglandin F2alpha. The increase in weight (larvae 21.9%, testis 28.9%, and ovary 33.3%) was associated with increases in the biomolecules (20-30%) and LDH and aldolase activity (18-25%). The results suggest that the accumulation of carbohydrates denotes a higher extent of utility of the energy sources in function of the testes and ovaries, and the routine application of prostaglandin F2alpha would be helpful in improving the reproductivity and egg quality of the silkworm.     

Synthesis,anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole–pyrrolobenzodiazepine conjugates

A series of 2,5-diaryloxadiazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates have been prepared and evaluated for their anticancer activity. These conjugates have shown promising activity with GI₅₀ values ranging from <0.1 to 0.29 μΜ. It is observed that some of these conjugates particularly 4a, 4d, 4i and 4l exhibit significant anticancer activity. Some detailed biological assays relating to the cell cycle aspects associated to Bax and caspases have been examined with a view to understand the mechanism of action of these conjugates.