Antihyperlipidemic activity of o-chlorobenzylsulfonamide in rodents.

o-Chlorobenzylsulfonamide was observed to be a potent hypolipidemic agent in rodents, reducing serum cholesterol levels 71% and triglyceride levels 49% at 60 mg/kg/d. The agent was effective both in normal and hyperlipidemic mice and was active both orally and intraperitoneally. o-Chlorobenzylsulfonamide significantly inhibited phosphatidate phosphohydrolase activity and marginally inhibited sn-glycerol-3-phosphate acyl transferase activity both in vitro and in vivo. The lowering of serum cholesterol levels appeared to be correlated with the accelerated excretion of cholesterol via the bile into the feces, with a marginal reduction of cholesterol absorption from the intestine. Reduced concentrations of lipids, e.g., cholesterol, triglycerides, and neutral lipids, were observed in the liver, small intestine, and blood lipoprotein fractions of rats.