Wang Yan, Zhang Shu-Yan, Ma Xiao-Feng, Tian Wei-Xi
Department of Biology, Graduate University of Chinese Academy of Sciences, Beijing 100049, China.
J Enzyme Inhib Med Chem. 2006 Feb;21(1):87-93. doi: 10.1080/14756360500472829.
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.
在我们之前的研究中,发现筛检中的药用植物桑寄生可抑制脂肪酸合酶(EC 2.3.1.85,FAS)并降低大鼠体重。现在我们已确定了桑寄生[Taxillus chinensis (DC.) Danser]提取物的抑制特性和动力学参数。桑寄生提取物(PLE)对FAS具有可逆和不可逆抑制作用,IC50值为0.48微克/毫升,似乎是迄今为止报道的最有效的抑制剂。PLE含有多种有效抑制剂,可能与FAS上的不同位点发生反应。不可逆抑制呈现出时间依赖性的双相过程,包括在最初几分钟内迅速的快相。快相抑制似乎是由提取物中某些强效但低浓度的成分引起的。此外,我们发现该草药中存在的杨梅苷可有效抑制FAS。这种糖基化黄酮和槲皮素在桑寄生抑制FAS中发挥有效作用。