Inhibition of Human Platelet Aggregation by Amides and Ester of Salicylic Acid with Platelet-Activating Factor Analogs

V. I. Kulikov^* and G. I. Muzya

Research and Development Center for Medical Biotechnology, Ministry of Public Health of the Russian Federation, ul. Shchukinskaya 6, Moscow, 123182 Russia; fax: (095) 190-0100

^* To whom correspondence should be addressed.

Received October 23, 2000; Revision received December 18, 2000

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The influence of acetyl salicylic acid (ASA) derivatives with platelet-activating factor (PAF) lipid analogs on PAF-induced human platelet aggregation has been studied. It was found that the ASA amide with an ethanolamine plasmalogen PAF analog (1-0-alk-1´-enyl-2-acetyl-sn-glycero-3-phospho-(N-2´-acetoxybenzoyl)ethanolamine) and the ASA ester with a choline plasmalogen PAF analog (1-0-alk-1´-enyl-2-(2´-acetoxybenzoyl)-sn-glycero-3-phosphocholine) at concentrations of 10^-7-10^-6 M effectively inhibit PAF-induced aggregation of human platelets. In contrast to these compounds, the ASA amide with an alkyl PAF analog (1-0-alkyl-2-acetyl-sn-glycero-3-phospho-(N-2´-acetoxybenzoyl)ethanolamine) did not inhibit PAF-induced platelet aggregation. As possible mechanisms of action of the studied compounds, the blockade of PAF-receptor and cyclooxygenase inhibition are proposed.

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KEY WORDS: platelet-activating factor analogs, acetyl salicylic acid, platelets

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