首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Potent inhibition of fatty acid synthase by parasitic loranthus (Taxillus chinensis (dc.) danser) and its constituent avicularin.
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Potent inhibition of fatty acid synthase by parasitic loranthus (Taxillus chinensis (dc.) danser) and its constituent avicularin.

机译:寄生天牛(Taxillus chinensis(dc。)danser)及其组成的avicularin对脂肪酸合酶的有效抑制作用。

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摘要

The medicinal herb parasitic loranthus in a screen was found to inhibit fatty acid synthase (EC 2.3.1.85, FAS) and reduce body weight of rats in our previous study. Now we have determined the inhibitory characteristics and kinetic parameters of extracts of parasitic loranthus [Taxillus chinensis (DC.) Danser]. The parasitic loranthus extracts (PLE) inhibits FAS reversibly and irreversibly and with an IC50 value of 0.48 microg/ml, appears to be the most potent inhibitor reported to date. PLE contains various potent inhibitors and may react with different sites on FAS. The irreversible inhibition exhibits a time-dependent biphasic process including a speedy fast-phase during the initial several minutes. The fast-phase inhibition seems to be caused by some potent but low-concentration component(s) in the extracts. In addition, we have found that avicularin existing in this herb can potently inhibit FAS. This glycosylated flavonoid and quercetin play an effective role in inhibiting FAS by parasitic loranthus.
机译:在我们先前的研究中,发现筛选中的药用寄生寄生狼能够抑制脂肪酸合酶(EC 2.3.1.85,FAS)并减轻大鼠体重。现在,我们已经确定了寄生的狼rant(Taxillus chinensis(DC。)Danser]提取物的抑制特性和动力学参数。寄生的狼毒提取物(PLE)可逆和不可逆地抑制FAS,IC50值为0.48 microg / ml,似乎是迄今为止报道的最有效的抑制剂。 PLE包含各种有效的抑制剂,并且可能与FAS上的不同部位发生反应。不可逆的抑制在最初的几分钟内表现出时间依赖性的双相过程,包括快速的快速相。快速相抑制似乎是由提取物中某些有效的但低浓度的成分引起的。另外,我们已经发现该草药中存在的鸟卵磷脂可以有效抑制FAS。这种糖基化的类黄酮和槲皮素在抑制寄生龙虾的FAS中起着有效的作用。

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