Antithrombotic effects of YS-49 and YS-51--1-naphthylmethyl analogs of higenamine.

Abstract

The antiplatelet and antithrombotic effects of YS-49 and YS-51--l-naphthylmethyl analogs of higenamine, which is a benzyl-tetrahydroisoquinoline alkaloid isolated from Aconitum japonicum (Ranunculaceae)--were investigated. YS-49 and YS-51 showed inhibitory activities to both human and rat platelet aggregation induced by ADP, collagen and epinephrine. They were more inhibitory to epinephrine-induced aggregation (IC(50); 3.4 and 1.7 microM of YS-49, and 6.0 and 6.3 microM of YS-51 to human and rat platelets, respectively) than ADP- or collagen-induced aggregation. The antithrombotic effects of YS-49 and YS-51 were also observed in both mouse acute thrombosis model and rat arterio-venous shunt (AV shunt) model. The oral administration of YS-49 and YS-51 (50 or 100 mg/kg) increased the recovery rates from the acute thrombotic challenge in mice and lowered the weight of thrombus formed inside the AV shunt tube in rats.

• Authors: H S Yun-Choi, M K Pyo, K M Park, K C Chang, D H Lee
• Journal: Thrombosis research (Thromb Res) Vol. 104 Issue 4 Pg. 249-55 (Nov 15 2001) ISSN: 0049-3848 [Print] United States
• PMID: 11728526 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 1-(beta-naphthylmethyl)-6,7-dihydroxy-1,2,3,4-tetra-hydroisoquinoline
• Alkaloids
• Fibrinolytic Agents
• Isoquinolines
• Platelet Aggregation Inhibitors
• Tetrahydroisoquinolines
• YS 49
• higenamine

Topics

• Alkaloids
• Animals
• Disease Models, Animal
• Fibrinolytic Agents (administration & dosage, pharmacology)
• Humans
• Inhibitory Concentration 50
• Isoquinolines (administration & dosage, pharmacology)
• Mice
• Mice, Inbred ICR
• Platelet Aggregation (drug effects)
• Platelet Aggregation Inhibitors (administration & dosage, pharmacology)
• Rats
• Rats, Sprague-Dawley
• Tetrahydroisoquinolines
• Thrombosis (drug therapy, prevention & control)
• Treatment Outcome