Development of Poly Unsaturated Fatty Acid Derivatives of Aspirin for Inhibition of Platelet Function S
Supplemental material to this article can be found at: http://jpet.aspetjournals.org/content/suppl/2016/08/03/jpet.116.234781.DC1 1521-0103/359/1/134–141$25.00 http://dx.doi.org/10.1124/jpet.116.234781 THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS J Pharmacol Exp Ther 359:134–141, October 2016 Copyright ª 2016 by The American Society for Pharmacology and Experimental Therapeutics Development of Poly Unsaturated Fatty Acid Derivatives of Aspirin for Inhibition of Platelet Function s Jahnabi Roy, Reheman Adili, Richard Kulmacz, Michael Holinstat, and Aditi Das Department of Chemistry (J.R.), Division of Nutritional Sciences, Departments of Comparative Biosciences, Biochemistry, and Bioengineering, Center for Biophysics and Quantitative Biology, Beckman Institute for Advanced Science (A.D.), University of Illinois at Urbana-Champaign, Urbana, Illinois; Division of Cardiovascular Medicine (M.H.), Department of Pharmacology (R.A., M.H.), University of Michigan Medical School, Ann Arbor, Michigan; and Department of Internal Medicine, Texas Health Science Center, McGovern Medical School, Houston, Texas (R.K.) Received April 27, 2016; accepted August 1, 2016 Downloaded from ABSTRACT The inhibition of platelet aggregation is key to preventing particular, the aspirin-DHA anhydride displayed similar effective- conditions such as myocardial infarction and ischemic stroke. ness to aspirin. Platelet aggregation studies conducted in the Aspirin is the most widely used drug to inhibit platelet aggre- presence of various platelet agonists indicated that the aspirin-lipid gation. Aspirin absorption can be improved further to increase conjugates act through inhibition of the cyclooxygenase (COX)– jpet.aspetjournals.org its permeability across biologic membranes via esterification thromboxane synthase (TXAS) pathway.
[Show full text]