2. Academic Validation
  3. Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178

Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178

  • J Nat Prod. 2016 Jun 24;79(6):1500-7. doi: 10.1021/acs.jnatprod.5b00961.
Patima Phainuphong,  Vatcharin Rukachaisirikul,  Saowanit Saithong,  Souwalak Phongpaichit,  Kawitsara Bowornwiriyapan,  Chatchai Muanprasat 1,  Chutima Srimaroeng 2,  Acharaporn Duangjai 3,  Jariya Sakayaroj 4
Affiliations

Affiliations

  • 1 Department of Physiology, Faculty of Science, Mahidol University , Rajathevi, Bangkok 10400, Thailand.
  • 2 Department of Physiology, Faculty of Medicine, Chiang Mai University , Muang, Chiang Mai 50200, Thailand.
  • 3 Division of Physiology, School of Medical Sciences, University of Phayao , Muang, Phayao 56000, Thailand.
  • 4 National Center for Genetic Engineering and Biotechnology (BIOTEC) , Thailand Science Park, Klong Luang, Pathumthani 12120, Thailand.
PMID: 27228159 DOI: 10.1021/acs.jnatprod.5b00961
Abstract

Three new lovastatin analogues (1, 4, and 5) together with four known lovastatin derivatives, namely, lovastatin (2), α,β-dehydrolovastatin (3), α,β-dehydrodihydromonacolin K (6), and α,β-dehydro-4a,5-dihydromonacolin L (7), were isolated from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178. Their structures were established using spectroscopic evidence. Compound 5 exhibited the most potent activity against HMG-CoA reductase, with an IC50 value of 387 μM. In addition, the present study indicated the direct interaction of compound 5 with HMG-CoA reductase. Compound 5 was considered to be noncytotoxic against noncancerous Vero cells, with an IC50 value of 40.0 μM, whereas compound 2 displayed much stronger activity, with an IC50 value of 2.2 μM.

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