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Background  The continuous emergence of multidrug-resistant (MDR) bacteria drastically reduced the efficacy of our antibiotic armory and consequently, increased the frequency of therapeutic failure. The search for bioactive constituents from endophytic fungi against MDR bacteria became a necessity for alternative and promising strategies, and for the development of novel therapeutic solutions. We report here the isolation and structure elucidation of antibacterial and cytotoxic compounds from  Phomopsis  sp . , an endophytic fungus associated with  Garcinia kola  nuts.    Methods  The fungus  Phomopsis  sp .  was isolated from the nut of  Garcinia kola.  The crude extract was prepared from mycelium of  Phomopsis  sp .  by maceration in ethyl acetate and sequentially fractionated by column chromatography. The structures of isolated compounds were elucidated on the basis of spectral studies and comparison with published data. The isolated compounds were evaluated for their antibacterial and anticancer properties by broth microdilution and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide methods respectively. The samples were also tested spectrophotometrically for their hemolytic properties against human red blood cells.    Results  The fractionation of the crude extract afforded three known cytochalasins including 18-metoxycytochalasin J (1), cytochalasins H (2) and J (3) together with alternariol (4). The cytochalasin compounds showed different degrees of antibacterial activities against the tested bacterial pathogens.  Shigella flexneri  was the most sensitive microorganism while  Vibrio cholerae  SG24 and  Vibrio cholerae  PC2 were the most resistant. Ampicillin did not show any antibacterial activity against  Vibrio cholerae  NB2,  Vibrio cholerae  PC2 and  Shigella flexneri  at concentrations up to 512 μg/mL, but interestingly, these multi-drug resistant bacterial strains were sensitive to the cytochalasin metabolites. These compounds also showed significant cytotoxic properties against human cancer cells (LC 50  = 3.66–35.69 μg/mL) with low toxicity to normal non-cancer cells.    Conclusion  The three cytochalasin compounds isolated from the  Phomopsis  sp .  crude extract could be a clinically useful alternative for the treatment of cervical cancer and severe infections caused by MDR  Shigella  and  Vibrio cholerae.

Antibacterial and cytotoxic cytochalasins from the endophytic fungus Phomopsis sp. harbored in Garcinia kola (Heckel) nut