DEVELOPMENT OF NEW ANTI-PLATELET AGGREGATING AGENTS

PLATELET AGGREGATION PLAYS A MAJOR ROLE IN CARDIOVASCULAR DISEASE. MUCH OF THE PRESENT PHARMACEUTICAL RESEARCH IS FOCUSED ON INHIBITORS OF THE FORMATION OF THROMBOXANE A2, A PROSTAGLANDIN DERIVED FROM ARACHIDONIC ACID. THE DIETARY INTAKE OF AN ESSENTIAL FATTY ACID, EICOSAPENTAENOIC ACID (EPA), HAS BEEN SHOWN TO DECREASE THROMBOXANE A2. ALSO, OTHER ESSENTIAL FATTY ACIDS, GAMMA LINOLENIC ACID (GLA) AND DIHOMO GAMMA LINOLENIC ACID (DGLA), HAVE BEEN SHOWN TO DECREASE PLATELET AGGREGATION BY A DIFFERENT MECHANISM: THE INCREASE IN THE PLASMA LEVELS OF PGE1. THE GOAL OF THIS RESEARCH IS TO PREPARE A PHARMACEUTICAL-GRADE EDIBLE OIL CONTAINING GLA THAT CAN BE TESTED IN CLINICAL TRIALS FOR ITS ABILITY TO REDUCE PLATELET AGGREGATION. THE RARE SEED SOURCE THAT HAS THE HIGHEST CONCENTRATION OF GLA ALSO CONTAINS A POTENTIALLY TOXIC ALKALOID. THE SUCCESSFUL COMPLETION OF PHASE I WILL BE TO DEMONSTRATE THAT A PHARMACEUTICAL-GRADE OIL CAN BE PRODUCED THAT IS ALSO DEVOID OF THE TOXIC ALKALOID. IF PHASE I IS SUCCESSFUL, THEN PHASE II WILL FOCUS ON CLINICAL TRIALS WITH SUCH A GLA-CONTAINING EDIBLE OIL TO INVESTIGATE THE REDUCTION OF PLATELET AGGREGATION.