Triflavin, an Arg-Gly-Asp-containing peptide, prevents platelet plug formation in in vivo experiments.
Triflavin, an Arg-Gly-Asp-containing peptide from Trimeresurus flavoviridis snake venom (M(r) of 7500 Da) inhibits platelet aggregation through the blockade of fibrinogen binding to activated platelets. The present study demonstrated that the intravenous injection of triflavin (0.1 and 0.25 mg/kg) significantly prolonged the bleeding time about 1.8- to 2.4-fold as compared with control (normal saline) of severed mesenteric arteries in rats, whereas the injection of Gly-Arg-Gly-Asp-Ser (GRGDS) (2-8 mg/kg) failed to increase the bleeding time in this model. Continuous infusion of triflavin (0.08 mg/kg/min) significantly increased the bleeding time about 2.6-fold, and the bleeding time returned to normal within 20 min after the cessation of triflavin infusion. Triflavin (10-20 mg/kg) significantly prolonged the occlusion time of platelet plug formation induced by irradiation of mesenteric venules of fluorescein sodium-pretreated mice. In contrast, trigramin (10-20 mg/kg) and GRGDS (500 and 1000 mg/kg) showed no significant effect. These results suggest that triflavin has an effective antiplatelet effect in vivo and this peptide may be a useful therapeutic agent for arterial thrombosis.
Sheu
J R
JR
Graduate Institute of Medical Science, Taipei Medical College, Taiwan.
Yen
M H
MH
Peng
H C
HC
Chang
M C
MC
Huang
T F
TF
D000595:Amino Acid Sequence; D000818:Animals; D001760:Bleeding Time; D001772:Blood Cell Count / Q000187:drug effects; D003435:Crotalid Venoms / Q000008:administration & dosage / Q000494:pharmacology*; D019793:Fluorescein; D005452:Fluoresceins; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D008638:Mesenteric Arteries / Q000187:drug effects; D051379:Mice; D008813:Mice, Inbred ICR; D008969:Molecular Sequence Data; D010455:Peptides / Q000008:administration & dosage / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D003435:Crotalid Venoms; D005452:Fluoresceins; D010455:Peptides; D010975:Platelet Aggregation Inhibitors; C070025:triflavin; D019793:Fluorescein