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苦参中异戊烯基黄酮对磷脂酶Cγ1的抑制作用

Inhibition of phospholipase C gamma 1 by the prenylated flavonoids from Sophora flavescens.

作者信息

Lee H S, Ko H R, Ryu S Y, Oh W K, Kim B Y, Ahn S C, Mheen T I, Ahn J S

出版信息

Planta Med. 1997 Jun;63(3):266-8. doi: 10.1055/s-2006-957670.

DOI:10.1055/s-2006-957670
PMID:9225612
Abstract

The effect on the phospholipase C gamma 1 activity of eleven prenylated flavonoids from Sophora flavescens was investigated. These flavonoids exhibited relatively strong inhibitory activity with IC50 values ranged from 7.5 x 10(-6) M to 35 x 10(-5) M with the exception of kushenol H (4) (IC50 value; > 5.3 x 10(-4) M). The presence of C3-OH resulted in a significant diminution of activity and the configuration of C3-OH is likely to be another factor influencing the activity. In addition, hydration of the C-4"'-C-5"' double bond of the lavandulyl side chain caused complete loss of activity. These data suggest that the presence and configuration of C3-OH are related to the inhibitory activity and the lavandulyl side chain is also important for high inhibitory activity against PLC gamma 1.

摘要

研究了苦参中11种异戊烯基黄酮对磷脂酶Cγ1活性的影响。除苦参醇H(4)(IC50值;>5.3×10−4 M)外,这些黄酮类化合物表现出较强的抑制活性,IC50值范围为7.5×10−6 M至35×10−5 M。C3-OH的存在导致活性显著降低,且C3-OH的构型可能是影响活性的另一个因素。此外,薰衣草基侧链的C-4″-C-5″双键水化导致活性完全丧失。这些数据表明,C3-OH的存在和构型与抑制活性有关,薰衣草基侧链对PLCγ1的高抑制活性也很重要。

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