title: DNA topoisomerase I inhibitor, ergosterol peroxide from Penicillium oxalicum.
abstract: Recently, we found that the MeOH extract of Penicillium oxalicum showed inhibitory activity towards DNA topoisomerase I. Subsequently, ergosterol peroxide, ergosterol, palmitoleic acid, and linoleic acid were isolated from the cultured mycelia of P. oxalicum. The structural determinations were based on physical and spectral analyses. Biological evaluation revealed that ergosterol peroxide inhibited the relaxation of supercoiled DNA (pBR322) induced by DNA topoisomerase I, and also showed marginal, selective cytotoxic activity against human colon tumor cells [COLO-205 (ED50=8.56 microg/mL].
authors.affiliation: National Research Institute of Chinese Medicine, Taipei, Taiwan, ROC.
authors.forename: Li-Ming Yang
authors.initials: LM
authors.lastname: Kuo
authors.forename: Kuei-Yuh
authors.initials: KY
authors.lastname: Chen
authors.forename: Shy-Yuan
authors.initials: SY
authors.lastname: Hwang
authors.forename: Jin-Liang
authors.initials: JL
authors.lastname: Chen
authors.forename: Yen-Yin
authors.initials: YY
authors.lastname: Liu
authors.forename: Chia-Ching
authors.initials: CC
authors.lastname: Liaw
authors.forename: Po-Ho
authors.initials: PH
authors.lastname: Ye
authors.forename: Cheng-Jen
authors.initials: CJ
authors.lastname: Chou
authors.forename: Chien-Chang
authors.initials: CC
authors.lastname: Shen
authors.forename: Yao-Haur
authors.initials: YH
authors.lastname: Kuo
mesh_terms: D047072:Aromatase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D004264:DNA Topoisomerases, Type I / Q000187:drug effects; D004875:Ergosterol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010407:Penicillium; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D059004:Topoisomerase I Inhibitors
chemical_list: D047072:Aromatase Inhibitors; D010936:Plant Extracts; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I; C036071:ergosterol-5,8-peroxide; D004875:Ergosterol