The molecular basis of the antiplatelet action of ajoene: direct interaction with the fibrinogen receptor.
Ajoene, the major antiplatelet compound derived from garlic inhibits the fibrinogen-supported aggregation of washed human platelets (ID50 = 13 microM) and, inhibits binding of 125I-fibrinogen to ADP-stimulated platelets (ID50 = 0.8 microM). In both cases, the inhibition is of the mixed non-competitive type. Furthermore, fibrinogen-induced aggregation of chymotrypsin-treated platelets is also inhibited by ajoene in a dose-dependent manner (ID50 = 2.3 microM). Other membrane receptors such as ADP or epinephrine receptors are not affected by ajoene. Ajoene strongly quenches the intrinsic fluorescence emission of purified glycoproteins IIb-IIIa (ID50 = 10 microM). These results indicate that the antiaggregatory effect of ajoene is causally related to its direct interaction with the putative fibrinogen receptor.
D000244:Adenosine Diphosphate / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects*; D004220:Disulfides / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D010936:Plant Extracts / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects; D010980:Platelet Membrane Glycoproteins / Q000187:drug effects* / Q000378:metabolism*; D013454:Sulfoxides
D004220:Disulfides; D010936:Plant Extracts; D010980:Platelet Membrane Glycoproteins; D013454:Sulfoxides; D000244:Adenosine Diphosphate; C048980:ajoene