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Prasoon Gupta Upasana Sharma Praveen Gupta Kiran Babu Siripurapu Rakesh Maurya 《Bioorganic & medicinal chemistry》2013,21(5):1116-1122
Phytochemical investigation of the n-butanol fraction of Evolvulus alsinoides (Linn.) led to the isolation of three new phenolic glycosides, evolvosides C, D and E (1–3) along with six known compounds (4–9). The structures of the compounds were elucidated on the basis of spectroscopic analysis, viz. 1D and 2D NMR experiments, chemical study, and comparison with literature data. Evolvoside C (1) was characterized as kaempferol 4′-O-β-d-glucopyranosyl-(1→2)-α-l-rhamnopyranosyl-(1→6)-β-d-glucopyranoside, whereas evolvosides D and E (2–3) were found to be mono and di-O-methyl derivatives of 1. The new compounds (1–3) represent rare triglycoside derivatives of flavonol at C-4′. The isolated compounds (1–6) were screened for acute stress-induced biochemical changes in male Sprague–Dawley rats at a dose of 40 mg/kg body weight. Compounds 1 and 2 displayed anti-stress effects by normalizing hyperglycemia, plasma corticosterone, plasma creatine kinase, and adrenal hypertrophy. Compounds 3 and 6 were also found to be effective in normalizing most of these stress parameters, whereas compounds 4 and 5 were ineffective in normalizing most of these effects. 相似文献
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KB Cullberg T Christiansen SK Paulsen JM Bruun SB Pedersen B Richelsen 《Obesity (Silver Spring, Md.)》2013,21(3):454-460
Background:
Vascular growth is a prerequisite for adipose tissue (AT) development and expansion. Some AT cytokines and hormones have effects on vascular development, like vascular endothelial growth factor (VEGF‐A), angiopoietin (ANG‐1), ANG‐2 and angiopoietin‐like protein‐4 (ANGPTL‐4).Methods:
In this study, the independent and combined effects of diet‐induced weight loss and exercise on AT gene expression and proteins levels of those angiogenic factors were investigated. Seventy‐nine obese males and females were randomized to: 1. Exercise‐only (EXO; 12‐weeks exercise without diet‐restriction), 2. Hypocaloric diet (DIO; 8‐weeks very low energy diet (VLED) + 4‐weeks weight maintenance diet) and 3. Hypocaloric diet and exercise (DEX; 8‐weeks VLED + 4‐weeks weight maintenance diet combined with exercise throughout the 12 weeks). Blood samples and fat biopsies were taken before and after the intervention.Results:
Weight loss was 3.5 kg in the EXO group and 12.3 kg in the DIO and DEX groups. VEGF‐A protein was non‐significantly reduced in the weight loss groups. ANG‐1 protein levels were significantly reduced 22‐25% after all three interventions (P < 0.01). The ANG‐1/ANG‐2 ratio was also decreased in all three groups (P < 0.05) by 27‐38%. ANGPTL‐4 was increased in the EXO group (15%, P < 0.05) and 9% (P < 0.05) in the DIO group. VEGF‐A, ANG‐1, and ANGPTL‐4 were all expressed in human AT, but only ANGPTL‐4 was influenced by the interventions.Conclusions:
Our data show that serum VEGF‐A, ANG‐1, ANG‐2, and ANGPTL‐4 levels are influenced by weight changes, indicating the involvement of these factors in the obese state. Moreover, it was found that weight loss generally was associated with a reduced angiogenic activity in the circulation. 相似文献4.
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Ahmad A Rasheed N Gupta P Singh S Siripurapu KB Ashraf GM Kumar R Chand K Maurya R Banu N Al-Sheeha M Palit G 《Phytomedicine》2012,19(7):639-647
Therapies targeting central stress mechanisms are fundamental for the development of successful treatment strategies. Ocimum sanctum (OS) is an Indian medicinal plant traditionally used for the treatment of various stress-related conditions. Previously, we have isolated and characterized three OS compounds; Ocimarin, Ocimumoside A and Ocimumoside B. However, their role in modulating chronic stress-induced central changes is unexplored. Thus, in the present study the efficacy of these OS compounds have been evaluated on the chronic unpredictable stress (CUS)-induced alterations in the monoaminergic and antioxidant systems in the frontal cortex, striatum and hippocampus, along with the changes in the plasma corticosterone levels. CUS (two different types of stressors daily for seven days) resulted in a significant elevation of plasma corticosterone level, which was reversed to control levels by pretreatment with Ocimumoside A and B (40 mg/kg p.o.), while Ocimarin showed no effect. The levels of NA, DA and 5-HT were significantly decreased in all the three brain regions by CUS, with a selective increase of DA metabolites. A significant decrease in the glutathione (GSH) content, the activities of superoxide dismutase and catalase with a significant increase in the glutathione peroxidase activity and lipid peroxidation was observed in all the three regions of the brain by CUS. The OS compounds alone did not cause any significant change in the baseline values of these parameters. However, Ocimumoside A and B (40 mg/kg body p.o.) attenuated these CUS-induced alterations with an efficacy similar to that of standard anti-stress (Panax quinquefolium; 100 mg/kg p.o.) and antioxidant (Melatonin; 20 mg/kg i.p.) drugs. While, Ocimarin failed to modulate these CUS-induced alterations. Therefore, this is the first report which identified the anti-stress activity of novel Ocimumoside A and B at the level of central monoamines and antioxidant properties, implicating their therapeutic importance in the prevention of stress-related disorders. 相似文献
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Siripurapu U Kolanos R Dukat M Roth BL Glennon RA 《Bioorganic & medicinal chemistry letters》2006,16(14):3793-3796
Comparison of several amine-substituted and methoxy-substituted analogs of N1-(4-aminobenzene)sulfonylindole suggests that these substituents might contribute to the 5-HT6 serotonin receptor affinity of these agents via their electronic effect on the indolic nucleus. Their 1,2,3,4-tetrahydrocarbazole counterparts behave differently. 相似文献
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KB Gudmundsdóttir S Sigurdarson J Kristinsson T Eiríksson T Jóhannesson 《Acta veterinaria Scandinavica》2006,48(1):16-5
This study was undertaken in order to examine whether any connection existed between the amounts of iron in forage and the
sporadic occurrence of scrapie observed in certain parts of Iceland. As iron and manganese are considered antagonistic in
plants, calculation of the Fe/Mn ratios was also included by using results from Mn determination earlier performed in the
same samples. Forage samples (n = 170) from the summer harvests of 2001–2003, were collected from 47 farms for iron and manganese
analysis. The farms were divided into four categories: 1. Scrapie-free farms in scrapie-free areas (n = 9); 2. Scrapie-free farms in scrapie-afflicted areas (n = 17); 3. Scrapie-prone farms (earlier scrapie-afflicted, restocked farms) (n = 12); 4. Scrapie-afflicted farms (n = 9). Farms in categories 1 and 2 are collectively referred to as scrapie-free farms. The mean iron concentration in forage samples from scrapie-afflicted farms was significantly higher than in forage samples
from farms in the other scrapie categories (P = 0.001). The mean Fe/Mn ratio in forage from scrapie-afflicted farms was significantly
higher than in forage from scrapie-free and scrapie-prone farms (P < 0.001). The results indicated relative dominance of iron
over manganese in forage from scrapie-afflicted farms as compared to farms in the other categories. Thus thorough knowledge
of iron, along with manganese, in soil and vegetation on sheep farms could be a pivot in studies on sporadic scrapie. 相似文献
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Scanning electron microscopy and gramicidin patch clamp recordings of microvillous receptor neurons dissociated from the rat vomeronasal organ 总被引:2,自引:1,他引:1
Vomeronasal organs from female rats were dissociated and isolated
microvillous receptor neurons were studied. The isolated receptor neurons
kept the typical bipolar shape which they have in situ as observed by
scanning electron microscopy. We applied the perforated patch-clamp
technique using the cation-selective ionophore gramicidin on freshly
isolated and well differentiated receptor neurons. The mean resting
potential was -58+/-14 mV (n=39). The contribution of the sodium pump
current to the resting potential was demonstrated by lowering the K+
concentration in the bath or by application of 100 microM dihydro-ouabain.
The input resistance was in the range of 1-6 GOmega and depolarizing
current pulses of a few pA were sufficient to trigger overshooting action
potentials. In voltage clamp conditions a fast transient sodium inward
current and a sustained outward potassium current were activated by
membrane depolarization. These observations indicate that freshly isolated
vomeronasal receptor neurons of rats can be recorded, using gramicidin,
with little modification of the intracellular content. Their
electrophysiological properties are very similar to those observed in situ.
Four out of eight female vomeronasal receptor cells were depolarized by
diluted rat male urine.
相似文献
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Dukat M Taroua M Dahdouh A Siripurapu U Damaj MI Martin BR Glennon RA 《Bioorganic & medicinal chemistry letters》2004,14(14):3651-3654
Several amine-substituted 8-amino-5,6,7,8-tetrahydroisoquinolines were examined as conformationally-constrained analogs of the nicotinic cholinergic (nACh) 3-(aminomethyl)pyridines. Although these ligands failed to bind at nACh receptors, the N-ethyl-N-methyl analog 3d was found to be at least equipotent with nicotine in rodent tests of antinociception. The mechanism of action of 3d is currently unknown. 相似文献