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北美金缕梅单宁及相关多酚对5-脂氧合酶和溶血血小板活化因子:乙酰辅酶A乙酰转移酶的双重抑制活性。

Dual inhibitory activities of tannins from Hamamelis virginiana and related polyphenols on 5-lipoxygenase and lyso-PAF: acetyl-CoA acetyltransferase.

作者信息

Hartisch C, Kolodziej H, von Bruchhausen F

机构信息

Institut für Pharmazie II, Pharmazeutische Biologie, Freie Universität Berlin, Germany.

出版信息

Planta Med. 1997 Apr;63(2):106-10. doi: 10.1055/s-2006-957623.

DOI:10.1055/s-2006-957623
PMID:9140221
Abstract

In the present study, the effects of tannins obtained from various plant sources on the activity of 5-LOX and AT were examined. With IC50 values ranging from 1.0 to 18.7 muM, hamamelitannin and the galloylated proanthocyanidins isolated from Hamamelis virginiana L. were found to be most potent inhibitors of 5-LOX. Unlike the 5-LOX study, hamamelitannin proved to be ineffective in the AT assay. Potent candidates are represented by the group of B-type proanthocyanidins. Structure-activity relationships regarding the in vitro inhibitory potency of the polyphenols in the biological assays are discussed.

摘要

在本研究中,检测了从各种植物来源获得的单宁对5-脂氧合酶(5-LOX)和抗胰蛋白酶(AT)活性的影响。北美金缕梅单宁和从北美金缕梅中分离出的没食子酰化原花青素的IC50值在1.0至18.7μM之间,被发现是5-LOX最有效的抑制剂。与5-LOX研究不同,北美金缕梅单宁在AT检测中被证明无效。B型原花青素组是有效的候选物。讨论了生物测定中多酚体外抑制效力的构效关系。

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