ruber3). Independently, the same compound (named mevinolin) was isolated by ALBERTS et al.1) from Aspergillus terreus. 4a, 5-Dihydromevinolin (Fig. 2)* was also isolated from the same culture.5) All of these five structurally-related entities are potent competitive inhibitors of 3-hydroxy-3-methylglutaryl (HMG)-CoA reductase (EC 1.1.1.34)2-1), the rate-limiting enzyme in cholesterol synthesis, with mevinolin being the most potent. However, compactin is the most extensively studied. Its hypocholesteremic acitivity in several animal species including human subjects has been demonstrated8~12) and a review of its pharmacology was also publi-shed13). In our search for new microbial metabolites having HMG-CoA reductase inhibition and ultimately hypocholesteremic activities, we have regrown P. citrinum in our laboratories and discovered a new component, designated as 4a,5dihydrocompactin. This new compound apparently cannot be derived from compactin stereospecifically without lengthy chemical conversions. The present communication describes the isolation, physical and chemical properties of this unique compound. The inhibition of HMG-CoA reductase is also described.
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