[Screening of drugs inhibiting cholesterol synthesis].
The biosynthesis of fusidin, an antibiotic of steroid structure, was used as a model of steroid synthesis. Screening of compounds modifying the fusidin synthesis included 80 strains of mycelial fungi. A high frequency of such fungal cultures was observed. 9 cultures forming compounds which inhibited the synthesis of cholesterol in the cell culture of human hepatocytes were screened. A method for biological estimation of the activity of cholesterol synthesis inhibitors was developed on rabbits with high blood levels of cholesterol. It was shown that the cholesterol synthesis inhibitors, isolated as a result of the specific screening were not toxic and markedly lowered the cholesterol blood levels.
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D000818:Animals; D000900:Anti-Bacterial Agents / Q000096:biosynthesis* / Q000302:isolation & purification / Q000494:pharmacology*; D000924:Anticholesteremic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D001414:Bacitracin / Q000494:pharmacology; D002460:Cell Line; D002682:Chinchilla; D002784:Cholesterol / Q000096:biosynthesis* / Q000097:blood; D002994:Clofibrate / Q000494:pharmacology; D003470:Culture Media / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D005658:Fungi / Q000187:drug effects* / Q000378:metabolism; D005672:Fusidic Acid / Q000031:analogs & derivatives / Q000096:biosynthesis*; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000378:metabolism; D011817:Rabbits; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000924:Anticholesteremic Agents; D003470:Culture Media; D001414:Bacitracin; D005672:Fusidic Acid; D002784:Cholesterol; D002994:Clofibrate