Inhibition of plasminogen activator inhibitor-1 activity by two diketopiperazines, XR330 and XR334 produced by Streptomyces sp.

被引：54

作者：

Bryans, J ^{[1
]}

Charlton, P ^{[1
]}

ChicarelliRobinson, I ^{[1
]}

Collins, M ^{[1
]}

Faint, R ^{[1
]}

Latham, C ^{[1
]}

Shaw, I ^{[1
]}

Trew, S ^{[1
]}

机构：

[1] XENOVA LTD,SLOUGH SL1 4EF,BERKS,ENGLAND

来源：

JOURNAL OF ANTIBIOTICS | 1996年 / 49卷 / 10期

关键词：

D O I：

10.7164/antibiotics.49.1014

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Two diketopiperazines, XR334 (1) and the novel compound XR330 (2) were isolated from the lyophilised biomass of an unidentified Streptomyces sp. Their structures were elucidated on the basis of spectroscopic studies and confirmed by chemical synthesis. Both compounds inhibited plasminogen activator inhibitor-1 activity in an amidolytic assay of tissue plasminogen activator mediated plasmin generation. Compound 1 also enhanced fibrinolysis ex vivo and protected against thrombus formation in the rat. These diketopiperazines represent the first low molecular weight inhibitors of plasminogen activator inhibitor-1, a physiological regulator of fibrinolysis

引用

页码：1014 / 1021

页数：8

共 18 条

[1] AN ANTIBODY FRAGMENT AGAINST PAI-1 INHIBITS PAI-1 ACTIVITY AND STIMULATES FIBRINOLYSIS IN-VITRO AND IN-VIVO [J].