Studies on new nicotinic acid ester derivatives

Abstract

The effects of 2,2,6,6-tetrakis(nicotinoyloxymethyl) cyclohexanol (K-31) on cholesterol-fed rabbits were compared with those of meso-inositol hexanicotinate and nicotinic acid.

In the regressive studies using oral K-31 after inducing experimental atherosclerosis, the drug suppressed the elevation of serum total cholesterol, phospholipid and triglyceride levels, and also decreased the deposition of total cholesterol and phospholipids in the liver. In the progressive studies, oral K-31 exhibited a marked serum cholesterol lowering effect.

The effect of K-31 on intestinal absorption of cholesterol was studied in thoracic-duct fistula rats administered labeled cholesterol. K-31 significantly depressed the absorption of [4-¹⁴C]cholesterol into lymph, and caused more absorbed [4-¹⁴C]-cholesterol to appear as ester.

The hypocholesterolemic action of K-31 is thought to be due to inhibition of exogenous sterol absorption.