Abstract
SummaryNovelty: Known and previously disclosed 10-membered lactone decanolides and diploalides are disclosed and are said to exhibit an inhibitory action on HMG-CoA reductase. The compounds are potentially useful hypocholesterolaemic and anti-arterioscleroic agents.Biology: Inhibition of HMG-CoA reductase by the compounds was demonstrated in cell cultures of HEP-G2 hepatocytes, where the preferred compound gave an IC50 = 0.1 μM for cholesterol synthesis. In vivo rodent studies showed an elevation of HDL/LDL plasma lipoprotein ratio at a daily dose of 15 mg/kg po, an action comparable with the known agents lovastatin and clofibrate.Chemistry: The ten-membered lactones were isolated from the fermentation medium of penicillium species, followed by derivatization by conventional methods as disclosed in EP0333024-A.Structure:
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
