Tetronic 701-a novel hypocholesterolaemic agent.
The Tetronic series of polymeric surface-active agents were screened for hypocholesterolaemic activity in rats fed on a semi-synthetic hypercholesterolaemic diet. Only Tetronics 701 and 702 were active and the former was further investigated. Tetronic 701 lowered serum and liver cholesterol in rats fed on a semi-synthetic diet, with or without cholesterol, but not in rats fed on stock laboratory diet. A dose-related growth depression was observed. The compound was hypocholesterolaemic in chicks and rabbits fed on cholesterol-containing diets. The uptake of a single dose of cholesterol into liver and serum was inhibited in rats given Tetronic 701. Tetronics 701 and 702 were effective in precipitating cholesterol from mixed micelles in vitro. Non-hypocholesterolaemic Tetronics were inactive in this respect. A series of tetraesters of tetronic 701 were prepared and tested in rats fed on a semi-synthetic hypercholesterolaemic diet. Several were hypocholesterolaemic and the tetrabenzoate was of especial interest in that it depressed growth less than did Tetronic 701 itself.
D000818:Animals; D000924:Anticholesteremic Agents / Q000009:adverse effects / Q000494:pharmacology*; D001647:Bile Acids and Salts / Q000494:pharmacology; D001835:Body Weight / Q000187:drug effects; D002645:Chickens; D002784:Cholesterol / Q000097:blood* / Q000378:metabolism; D002791:Cholesterol, Dietary / Q000008:administration & dosage; D004305:Dose-Response Relationship, Drug; D004952:Esters; D005029:Ethylenediamines / Q000494:pharmacology*; D006128:Growth / Q000187:drug effects; D006937:Hypercholesterolemia / Q000097:blood; D007408:Intestinal Absorption / Q000187:drug effects; D008099:Liver / Q000378:metabolism; D008297:Male; D011092:Polyethylene Glycols / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D013501:Surface-Active Agents / Q000009:adverse effects / Q000494:pharmacology*
D000924:Anticholesteremic Agents; D001647:Bile Acids and Salts; D002791:Cholesterol, Dietary; D004952:Esters; D005029:Ethylenediamines; D013501:Surface-Active Agents; C012571:tetronic 701; D011092:Polyethylene Glycols; D002784:Cholesterol