title: Ophiobolins P-T, five new cytotoxic and antibacterial sesterterpenes from the endolichenic fungus Ulocladium sp.
abstract: Five ophiobolane sesterterpenes, ophiobolins P-T, and three known compounds, 6-epi-21,21-O-dihydroophiobolin G, 6-epi-ophiobolin G and 6-epi-ophiobolin K, were isolated from the acetone extract of the endolichenic fungus Ulocladium sp. by using OSMAC method. Their structures were elucidated on the basis of spectroscopic analysis. The absolute configuration of the 18,19-diol moieties in ophiobolin Q was assigned using the Frelek's method. The cytotoxic effects on KB and HepG2 cell lines, antibacterial activity against Bacillus subtilis, methicillin-resistant Staphylococcus aureus, and Bacille Calmette-Guerin were evaluated for all isolated compounds. Ophiobolin T and 6-epi-ophiobolin G exhibited the most potent cytotoxic activity against HepG2 with IC₅₀ of 0.24 and 0.37 μM, respectively. In antibacterial assay, ophiobolins P and T showed moderate antibacterial activity against B. subtilis and meticillin-resistant S. aureus. Ophiobolin T also displayed moderate antibacterial activity against the Bacille Calmette-Guerin strain.
authors: State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, No.1 Beichen West Road, Chaoyang District, Beijing 100101, PR China; School of Life Sciences, University of Science and Technology of China, No. 96 Jinzhai-Road, Hefei 230026, PR China; CAS Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, No.1 Beichen West Road, Chaoyang District, Beijing 100101, PR China.
authors: Quan-Xin
authors: QX
authors: Wang
authors: Li
authors: L
authors: Bao
authors: Xiao-Li
authors: XL
authors: Yang
authors: Dai-Lin
authors: DL
authors: Liu
authors: Hui
authors: H
authors: Guo
authors: Huan-Qin
authors: HQ
authors: Dai
authors: Fu-Hang
authors: FH
authors: Song
authors: Li-Xin
authors: LX
authors: Zhang
authors: Liang-Dong
authors: LD
authors: Guo
authors: Shao-Jie
authors: SJ
authors: Li
authors: Hong-Wei
authors: HW
authors: Liu
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D001203:Ascomycota / Q000737:chemistry*; D001412:Bacillus subtilis / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D056945:Hep G2 Cells; D006801:Humans; D007624:KB Cells; D008011:Lichens / Q000737:chemistry*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009163:Mycobacterium bovis / Q000187:drug effects; D009369:Neoplasms / Q000188:drug therapy*; D054830:Sesterterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D001688:Biological Products; D054830:Sesterterpenes; C002884:ophiobolins
keywords: Antibacterial activity; Cytotoxicity; Endophytic fungi; Ophiobolane sesterterpenes; Ulocladium sp.