title: Apoptosis-inducing effects of sterols from the dried powder of cultured mycelium of Cordyceps sinensis.
abstract: The methanolic extract and its ethyl acetate-soluble fraction from the dried powder of cultured Cordyceps sinensis mycelium showed cytotoxic effects on promyelocytic leukemia HL-60 cells. Sitosterol (1), 5 alpha,8 alpha-epidioxy-22E-ergosta-6,22-dien-3beta-ol (2), 5 alpha,8 alpha-epidioxy-22E-ergosta-6,9(11),22-trien-3beta-ol (3), 5 alpha,6 alpha-epoxy-5 alpha-ergosta-7,22-dien-3beta-ol (4), and ergosterol (5) were isolated from the ethyl acetate fraction. Among the isolated compounds, 2-4 with a peroxide ring or an epoxide ring showed substantial cytotoxic activity with IC(50) values of 7.3-7.8 microg/ml, but 1 and 5 showed only moderate activity. Furthermore, apoptosis of HL-60 cells was observed 24 h after treatment with 2-4 (10, 20 microg/ml) using the TdT-mediated dUTP nick-end labeling method, and their apoptosis-inducing activities are suggested to be dependent on the activation of caspases-3/7. To the best of our knowledge, this is the first report of the isolation of sterol constituents (1-5) from cultured C. sinensis mycelium.
authors.affiliation: Kyoto Pharmaceutical University, Kyoto, Japan.
authors.forename: Hisashi
authors.initials: H
authors.lastname: Matsuda
authors.forename: Junji
authors.initials: J
authors.lastname: Akaki
authors.forename: Seikou
authors.initials: S
authors.lastname: Nakamura
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Okazaki
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Kojima
authors.forename: Makoto
authors.initials: M
authors.lastname: Tamesada
authors.forename: Masayuki
authors.initials: M
authors.lastname: Yoshikawa