Prolyl endopeptidase inhibitors from Caryophylli Flos

被引：26

作者：

Lee, KH

Kwak, JH

Lee, KB

Song, KS

机构：

[1] Kyungpook Natl Univ, Dept Agr Chem, Coll Agr, Taegu 702701, South Korea

[2] Sungkyunkwan Univ, Coll Pharm, Suwon 440746, South Korea

[3] KonYang Univ, Dept Chem, Nonsan 320800, Chungnam, South Korea

来源：

ARCHIVES OF PHARMACAL RESEARCH | 1998年 / 21卷 / 02期

关键词：

prolyl endopeptidase inhibitor; Eugenia caryophyllata; Caryophylli Flos; luteolin; quercetin; flavonoids; beta-sitosterol-3-O-beta-D-glucopyranoside;

D O I：

10.1007/BF02974029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three prolyl endopeptidase inhibitors were isolated and identified as luteolin, quercetin and beta-sitosterol-3-O-beta-D-glucopyranoside with IC50 of 0.17, 0.19 and 27.5 ppm, respectively. The inhibition of two flavonoids were non-competitive with substrate. Twenty authentic flavonoids were tested in order to investigate structure-activity relationship. No significant relationship was found in them, however, catechol moiety of B-ring and 7-OH group in flavonoid skeleton were seemed to be responsible for the stronger activity.

引用

页码：207 / 211

页数：5

共 23 条

[1]

AGRAWAL PK, 1988, CARBON 13 NMR FLAVON

[2] POSTSTATIN, A NEW INHIBITOR OF PROLYL ENDOPEPTIDASE, PRODUCED BY STREPTOMYCES-VIRIDOCHROMOGENES MH534-30F3 .1. TAXONOMY, PRODUCTION, ISOLATION, PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL-ACTIVITIES [J].