title: Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178.
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.
authors.forename: Patima
authors.initials: P
authors.lastname: Phainuphong
authors.forename: Vatcharin
authors.initials: V
authors.lastname: Rukachaisirikul
authors.forename: Saowanit
authors.initials: S
authors.lastname: Saithong
authors.forename: Souwalak
authors.initials: S
authors.lastname: Phongpaichit
authors.forename: Kawitsara
authors.initials: K
authors.lastname: Bowornwiriyapan
authors.affiliation: Department of Physiology, Faculty of Science, Mahidol University , Rajathevi, Bangkok 10400, Thailand.
authors.forename: Chatchai
authors.initials: C
authors.lastname: Muanprasat
authors.affiliation: Department of Physiology, Faculty of Medicine, Chiang Mai University , Muang, Chiang Mai 50200, Thailand.
authors.forename: Chutima
authors.initials: C
authors.lastname: Srimaroeng
authors.affiliation: Division of Physiology, School of Medical Sciences, University of Phayao , Muang, Phayao 56000, Thailand.
authors.forename: Acharaporn
authors.initials: A
authors.lastname: Duangjai
authors.affiliation: National Center for Genetic Engineering and Biotechnology (BIOTEC) , Thailand Science Park, Klong Luang, Pathumthani 12120, Thailand.
authors.forename: Jariya
authors.initials: J
authors.lastname: Sakayaroj
mesh_terms: D000818:Animals; D001230:Aspergillus / Q000737:chemistry*; D002522:Chlorocebus aethiops; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007624:KB Cells; D008148:Lovastatin / Q000031:analogs & derivatives / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015359:Mycobacterium scrofulaceum / Q000187:drug effects; D019906:Nuclear Magnetic Resonance, Biomolecular; D010963:Plasmodium falciparum / Q000187:drug effects; D012988:Soil Microbiology; D013785:Thailand; D014709:Vero Cells
chemical_list: D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008148:Lovastatin