The Hypolipidemic Activity of Metal Complexes of AmineCarboxyboranes in Rodents

Abstract

The metal complexes of amine-carboxyborane including copper, chromium, zinc, calcium amd cobalt were effective hypolipidemic agents lowering both serum cholesterol and triglyceride levels significantly in mice at 8 mg/kg/day, I.P. after 16 days. The agents reduced acetyl CoA synthetase, ATP-dependent citrate lyase, acyl CoA cholesterol acyl transferase, sn-glycerol-3-phosphate acyl transferase activities of rat liver and small intestinal mucosa after 14 days treatment. The neutral cholesterol ester hydrolase activity was elevated by the agents in both tissues. The metal complexes altered lipid levels in the bile of rats after treatment as well as the bile acid composition after 14 days administration, orally. The agents blocked enterohepatic absorption of cholesterol from rat isolated intestinal loops.

Synthesis of the first amine–dicarboxyboranes and their derivatives

“…Amine-carboxyboranes have been known for two decades, 1 and their biological and pharmaceutical activities have been extensively studied. 2 Amine-carboxyboranes and related compounds have shown anticancer, 3 antiosteoporotic, 4 anti-inflammatory 5 and hypolipidemic 6 properties. Since the preparation of the first representative of amine-carboxyboranes they have been generally considered to be the boron analogues of the protonated amino acids, 7 based on the isoelectronic relation between C-N + and B-N bonds.…”