Planta Med 2003; 69(12): 1109-1112
DOI: 10.1055/s-2003-45191
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Modulation of PAI-1 and tPA Activity and Thrombolytic Effects of Corilagin

Zhi-Qiang Shen1 , 2 , Ze-Jun Dong1 , Hua Peng1 , Ji-Kai Liu1
  • 1Kunming Institute of Botany, the Chinese Academy of Sciences, Kunming, P. R. China
  • 2Yunnan Pharmacological Laboratories of Natural Products, Kunming Medical College, Kunming, P. R. China
This project was supported by National Natural Science Foundation of China (30225048)
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Publikationsverlauf

Received: April 30, 2003

Accepted: August 24, 2003

Publikationsdatum:
29. Januar 2004 (online)

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Abstract

In this study, Charlton’s and Tomihisa’s methods were modified to investigate the thrombolytic effect of corilagin from the Chinese herbal plant Phyllanthus urinaria L., as well as its effect on carotid artery patency status. The activity of type 1 plasminogen activator inhibitor (PAI-1) in rat plasma or platelet-released substances and tissue-type plasminogen activator (tPA) in rat plasma was assayed by use of a chromogenic substrate. The results showed that corilagin had a dose-dependent thrombolytic effect in rats. 5 mg/kg of corilagin produced a nearly similar reperfusion rate to that of 20 000 U/kg of urokinase, whereas it produced a lower reocclusion rate than urokinase. Corilagin significantly inhibited PAI-1 activity in rat plasma or platelet-released substances while it elevated plasma tPA activity, in a concentration-dependent manner. Corilagin, however, had no influence on rabbit platelet aggregation. It is indicated that corilagin inhibited PAI-1 activity and increased tPA activity, and this property of corilagin is assumed to be responsible for the thrombolytic effect.

Abbreviations

PO:persistent occlusion

CR:cyclic reflow

PP:persistent patency

PAI-1:type 1 plasminogen activator inhibitor

tPA:tissue-type plasminogen activator

PBS:phosphate buffer solution

IC50:50 % of inhibitory concentration

PRP:platelet-rich plasma

ADP:adenosine diphosphate

AA:arachidonic acid

PAF:platelet-activating factor