Synthetic Phosphatidylethanolamines as Renin Inhibitors

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Abstract
Anti-renin and hypotensive effects of synthetic PE [phosphatidylethanolamine] were examined. PE (18) including optical isomers were newly synthesized. Arachidonic acid, linolenic acid and stearic acid were substituted at positions of .beta., .gamma. or both. Natural PE was extracted from porcine kidney, and the lyso form was prepared by treatment of phospholipase A. Anti-renin activity of these compounds was determined using high-renin plasma obtained from the dog. The inhibition of renin activity was expressed as a percentage of reduction in the production rate of angiotensin I as measured by radioimmunoassay. The inhibitory effects of .**GRAPHIC**. .gamma.-C18) series, D- and .**GRAPHIC**. .gamma.-C18) and DL- and L-PE(.beta.-C18, .**GRAPHIC**. were greater than that of the natural PE, but did not exceed the effect of lyso-PE. Hypotensive effect was evaluated in conscious normotensive, spontaneously hypertensive and renal hypertensive rats by daily i.m. injection of test compounds. Following repeated administration of natural PE, D-PE(.beta.-C18, .**GRAPHIC**. and D-PE(.beta.-C18, .**GRAPHIC**. to renal hypertensive rats, blood pressure decreased by > 30 mm Hg. D- and .**GRAPHIC**. DL-PE (.beta.-C18, .**GRAPHIC**. and DL-PE(.beta.-C18, .**GRAPHIC**. lowered pressure > 40 mm Hg. DL-PE(.beta.-C18, .**GRAPHIC**. showed hypotensive effects in renal hypertensive and spontaneously hypertensive rats, but not in normotensive rats.

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