A METHOD TO REDUCE IN VIVO THROMBUS FORMATION AND PLATELET AGGREGATION USING QUERCETIN 3, 3™, 4™, 5, 7-O- PENTASULFATE, AS A POTENTIAL ANTITHROMBOTIC AND ANTIPLATELET AGENT
MOHAMAD AMAN JAIRAJPURI,MOHAMMAD ABID,QUDSIA RASHID,NEHA GUPTA
申请号：
IN201611032665
公开号：
IN201611032665A
申请日:
2016.09.24
申请国别(地区):
IN
年份:
2018
代理人:
摘要：
The present disclosure provides a novel method to reduce in vivo thrombus formation and platelet aggregation with the use of a new polysulfated derivative of Quercetin-Quercetin 3, 3™, 4™, 5, 7-O- pentasulfate (QPS).In the present method the QPS was synthesized, characterized and evaluated for its in vitro and in vivo anticoagulant potential. QPS was tested for its in vitro anticoagulant activity using human plasma and clotting assays showed that APTT and PT got doubled at a concentration of 7mM and 4mM respectively, with no effect on TT. The in vivo observations demonstrated that intravenous administration of QPS, significantly reduced thrombus formation in rat model of venous thrombosis. Further, the infusion of rats with QPS prior to ligation also delayed APTT with profound effect on PT in comparison to non-sulfated Quercetin injected rats. The inhibition of ADP induced platelet aggregation for QPS injected rats also suggested its antiplatelet mechanism of action. Taking into consideration the non-toxic and highly soluble nature of Quercetin we suggest here that sulfation makes QPS as an effective antithrombotic lead compound with dual mode of action. In particular the method of administration of QPS can be used as a promising antithrombotic and antiplatelet strategy to treat thrombotic disorders.
