Journal
JOURNAL OF ANTIBIOTICS
Volume 61, Issue 8, Pages 503-508Publisher
JAPAN ANTIBIOTICS RESEARCH ASSOC
DOI: 10.1038/ja.2008.67
Keywords
semisynthetic pyripyropene derivative; acyl-CoA : cholesterol acyltransferase (ACAT); ACAT isozyme; atherosclerosis
Funding
- National Institute of Biomedical Innovation (NIBIO)
- Ministry of Education, Culture, Sports, Science and Technology, Japan [18390008]
- Hoh-ansya Foundation, Japan
- Grants-in-Aid for Scientific Research [18390008] Funding Source: KAKEN
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Selectivity of 96 semisynthetic derivatives prepared from fungal pyripyropene A, originally isolated as a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), toward ACAT1 and ACAT2 isozymes was investigated in the cell-based assay using ACAT1- and ACAT2-expressing CHO cells. Eighteen derivatives including PR-71 (7-O-isocaproyl derivative) showed much more potent ACAT2 inhibition (IC(50): 6.0 to 62 nM) than pyripyropene A (IC(50): 70 nM). Among them, however, natural pyripyropene A showed the highest selectivity toward ACAT2 with a selectivity index (SI) of >1000, followed by PR-71 (SI, 667).
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