Mechanism of the inhibitory effect of cepharanthine on the aggregation of platelets.

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Abstract
Human platelet aggregation elicited by collagen or thrombin was inhibited by cepharanthine in a concentration-dependent manner. The inhibition of thrombin-induced aggregation was correlated with the inhibition of arachidonate release from the phospholipids of the membrane, notably from phosphatidylcholine. The normal disc shape of the washed platelets with a few pseudopods was transformed to a sphere due to treatment with cepharanthine at a concentration which as considerably inhibited aggregation. Washing the cepharanthine-treated platelets with a Ca-free solution changed the spherical shape back to the disc shape and abolished the inhibition of aggregation. Apparently, cepharanthine disturbs the plasma membrane due to its incorporation into the membrane, which results in the change in shape of the membrane and the inhibition of aggregation.

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