Inhibition of Plasminogen Activator Inhibitor-1 Activity by Two Diketopiperazines, XR330 and XR334 Produced by Streptomyces sp.

JUSTIN BRYANS; PETER CHARLTON; INÊS CHICARELLI-ROBINSON; MARK COLLINS; RICHARD FAINT; CHRIS LATHAM; IAN SHAW; SALLY TREW

doi:10.7164/antibiotics.49.1014

Inhibition of Plasminogen Activator Inhibitor-1 Activity by Two Diketopiperazines, XR330 and XR334 Produced by Streptomyces sp.

JUSTIN BRYANS, PETER CHARLTON, INÊS CHICARELLI-ROBINSON, MARK COLLINS, RICHARD FAINT, CHRIS LATHAM, IAN SHAW, SALLY TREW

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JOURNAL FREE ACCESS

1996 Volume 49 Issue 10 Pages 1014-1021

DOI https://doi.org/10.7164/antibiotics.49.1014

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Abstract

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

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