DNA topoisomerase I inhibitor, ergosterol peroxide from Penicillium oxalicum.
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].
Kuo
Li-Ming Yang
LM
National Research Institute of Chinese Medicine, Taipei, Taiwan, ROC.
Chen
Kuei-Yuh
KY
Hwang
Shy-Yuan
SY
Chen
Jin-Liang
JL
Liu
Yen-Yin
YY
Liaw
Chia-Ching
CC
Ye
Po-Ho
PH
Chou
Cheng-Jen
CJ
Shen
Chien-Chang
CC
Kuo
Yao-Haur
YH
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
D047072:Aromatase Inhibitors; D010936:Plant Extracts; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I; C036071:ergosterol-5,8-peroxide; D004875:Ergosterol