2. Academic Validation
  3. Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent

Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent

  • Proc Natl Acad Sci U S A. 1980 Jul;77(7):3957-61. doi: 10.1073/pnas.77.7.3957.
A W Alberts,  J Chen,  G Kuron,  V Hunt,  J Huff,  C Hoffman,  J Rothrock,  M Lopez,  H Joshua,  E Harris,  A Patchett,  R Monaghan,  S Currie,  E Stapley,  G Albers-Schonberg,  O Hensens,  J Hirshfield,  K Hoogsteen,  J Liesch,  J Springer
PMID: 6933445 DOI: 10.1073/pnas.77.7.3957
Abstract

Mevinolin, a Fungal metabolite, was isolated from cultures of Aspergillus terreus. The structure and absolute configuration of mevinolini and its open acid form, mevinolinic acid, were determined by a combination of physical techniques. Mevinolin was shown to be 1,2,6,7,8,8a-hexahydro-beta, delta-dihydroxy-2,6-dimethyl-8-(2-methyl-1-oxobutoxy)-1-naphthalene-hepatanoic acid delta-lactone. Mevinolin in the hydroxy-acid form, mevinolinic acid, is a potent competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase [mevalonate: NADP+ oxidoreductase (CoA-acylating), EC 1.1.1.34]; its Ki of 0.6 nM can be compared to 1.4 nM for the hydroxy acid form of the previously described related inhibitor, ML-236B (compactin, 6-demethylmevinolin). In the rat, orally administered sodium mevinolinate was an active inhibitor of Cholesterol synthesis in an acute assay (50% inhibitory dose = 46 microgram/kg). Furthermore, it was shown that mevinolin was an orally active cholesterol-lowering agent in the dog. Treatment of dogs for 3 weeks with mevinolin at 8 mg/kg per day resulted in a 29.3 +/- 2.5% lowering of plasma Cholesterol.

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