Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 3, Pages 786-790Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.12.049
Keywords
Fusarithioamide B; Fusarium chlamydosporium; Benzamide derivative; Anvillea garcinii; Antimicrobial; Cytotoxic activity
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Fusarithioamide B (6), a new aminobenzamide derivative with unprecedented carbon skeleton and five known metabolites: stigmast-4-ene-3-one (1), stigmasta-4,6,8(14), 22-tetraen-3-one (2), p-hydroxyacetophenone (3), tyrosol (4), and fusarithioamide A (5) were separated from Fusarium chlamydosporium EtOAc extract isolated from Anvillea garcinii (Burm.f.) DC. leaves (Asteraceae). The structure elucidation and complete assignment of the isolated metabolites were performed mainly by the aid of various NMR and MS data. Fusarithioamide B (6) has been assessed for antibacterial and antifungal activities towards various microbial strains by disc diffusion assay. It exhibited selective antifungal activity towards C. albicans (MIC 1.9 mg/ml and IZD 14.5 mm), comparing to clotrimazole (MIC 2.8 mg/ml and IZD 17.9 mm). Also, it possessed high antibacterial potential towards E. coli, B. cereus, and S. aureus compared to ciprofloxacin. Furthermore, 6 was tested for the in vitro cytotoxic effect against KB, HCT-116, BT-549, MCF-7, SKOV-3, and SK-MEL cell lines. It had selective and potent effect towards BT-549, MCF-7, SKOV-3, and HCT-116 cell lines with IC(50)s 0.09, 0.21, 1.23, and 0.59 mu M, respectively compared to doxorubicin (IC(50)s 0.046, 0.05, 0.321, and 0.24 mu M, respectively). Fusarithioamide B may provide a lead molecule for future developing of antitumor and antimicrobial agents. (C) 2018 Elsevier Ltd. All rights reserved.
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