Trypsin inhibitory potential and microbial transformation of rutin isolated from Citrus sinensis

Muhammad Asam Raza; Durre Shahwar

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Trypsin inhibitory potential and microbial transformation of rutin isolated from Citrus sinensis

机译：柑橘中芦丁的胰蛋白酶抑制潜能和微生物转化

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This study was designed to determine the trypsin inhibitory potential of rutin (1) and its biotransformed metabolite, quercetin (2). Rutin (1) was purified from the methanolic extract of Citrus sinensis and biotransformed in the culture of Streptomyces griseus, which yielded quercetin (2) as the major product. Both 1 and 2 showed significant trypsin inhibitory potential with IC50 = 0.016 ± 0.002 and 0.019 ± 0.003 mM, respectively. Kinetic studies were carried out using GraFit 7.0 software. Lineweaver-Burk and Dixon plots and their secondary replots indicated that these compounds are non-competitive inhibitors. The Ki values of 1 and 2 were found to be 17.5 ± 0.7 and 3.1 ± 0.5 nuM, respectively.

机译：本研究旨在确定芦丁（1）及其生物转化的代谢产物槲皮素（2）对胰蛋白酶的抑制潜力。从柑桔的甲醇提取物中纯化芦丁（1），并在灰链霉菌的培养物中进行生物转化，从而产生槲皮素（2）作为主要产物。 1和2均显示出显着的胰蛋白酶抑制潜能，IC50分别为0.016±0.002和0.019±0.003 mM。使用GraFit 7.0软件进行了动力学研究。 Lineweaver-Burk和Dixon图及其二级重复图表明这些化合物是非竞争性抑制剂。发现1和2的Ki值分别为17.5±0.7和3.1±0.5 nuM。

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《Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents》 |2013年第8期|共5页
作者
Muhammad Asam Raza; Durre Shahwar;
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正文语种 eng
中图分类药学;
关键词
Trypsin inhibition; Flavonoids; Enzyme kinetics; Citrus sinensis;

机译：胰蛋白酶抑制;类黄酮;酶动力学;柑橘;

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1. Trypsin inhibitory potential and microbial transformation of rutin isolated from Citrus sinensis [J] . Muhammad Asam Raza, Durre Shahwar Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2013,第8期

机译：柑橘中芦丁的胰蛋白酶抑制潜能和微生物转化
2. Microbial inhibitory and radical scavenging activities of cold-pressed terpeneless Valencia orange (Citrus sinensis) oil in different dispersing agents [J] . Chalova Vesela I., Crandall Philip G., Ricke Steven C. Journal of the Science of Food and Agriculture . 2010,第5期

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Trypsin inhibitory potential and microbial transformation of rutin isolated from Citrus sinensis

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