Anti-inflammatory and cytotoxic cyathane diterpenoids from the medicinal fungus Cyathus africanus.
Five novel cyathane diterpenes, cyathins D-H (1-5), as well as three known diterpenes, neosarcodonin O (6), cyathatriol (7),and 11-O-acetylcyathatriol (8), were isolated from the solid culture of Cyathus africanus. The structures of the new compounds were elucidated by spectroscopic methods. The absolute configurations of compounds 2 and 8 were determined by single-crystal X-ray crystallographic analysis, whereas the absolute configuration of C-14 in 1 was determined via the circular dichroism data of the [Rh(2)(OCOCF(3))(4)] complex. Compounds 3, 5, 6, 8, and 9 showed potent inhibition against nitric oxide production in lipopolysaccaride-activated macrophages with an IC(50) value of 2.57, 1.45, 12.0, 10.73, and 9.45μM, respectively. Compounds 6 and 8 showed strong cytotoxicity against Hela and K562 cell lines with the IC(50) value less than 10μM.
State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, No. 9 Beiertiao, Zhongguancun, Haidian District, Beijing 100190, PR China.
Junjie
J
Han
Yuhui
Y
Chen
Li
L
Bao
Xiaoli
X
Yang
Dailin
D
Liu
Shaojie
S
Li
Feng
F
Zhao
Hongwei
H
Liu
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D055365:Cyathus / Q000737:chemistry*; D004224:Diterpenes / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology*; D006801:Humans; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D004224:Diterpenes