title: Non-cytotoxic antifungal agents: isolation and structures of gageopeptides A-D from a Bacillus strain 109GGC020.
abstract: Antifungal resistance and toxicity problems of conventional fungicides highlighted the requirement of search for new safe antifungal agents. To comply with the requirement, we discovered four new non-cytotoxic lipopeptides, gageopeptides A-D, 1-4, from a marine-derived bacterium Bacillus subtilis. The structures and stereochemistry of gageopeptides were determined by NMR data analysis and chemical means. Gageopeptides exhibited significant antifungal activities against pathogenic fungi Rhizoctonia solani, Botrytis cinerea, and Colletotrichum acutatum with minimum inhibitory concentration (MIC) values of 0.02-0.06 μM. In addition, these lipopeptides showed significant motility inhibition and lytic activities against zoospores of the late blight pathogen Phytophthora capsici. These compounds also showed potent antimicrobial activity against Gram positive and Gram negative bacteria with MIC values of 0.04-0.08 μM. However, gageopeptides A-D did not exhibit any cytotoxicity (GI50 > 25 μM) against cancer cell lines in sulforhodamine B (SRB), 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT), and WST-1 ((4-[3-4-iodophenyl]-2-(4-nitrophenyl)-2H-5-tetrazolio)-1,3-benzene disulfonate)) assays, demonstrating that these compounds could be promising candidates for the development of non-cytotoxic antifungal agents.
authors.affiliation: Department of Marine Biotechnology, Korea University of Science and Technology , Daejeon 350-360, Republic of Korea.
authors.forename: Fakir Shahidullah
authors.initials: FS
authors.lastname: Tareq
authors.forename: Min Ah
authors.initials: MA
authors.lastname: Lee
authors.forename: Hyi-Seung
authors.initials: HS
authors.lastname: Lee
authors.forename: Yeon-Ju
authors.initials: YJ
authors.lastname: Lee
authors.forename: Jong Seok
authors.initials: JS
authors.lastname: Lee
authors.forename: Choudhury M
authors.initials: CM
authors.lastname: Hasan
authors.forename: Md Tofazzal
authors.initials: MT
authors.lastname: Islam
authors.forename: Hee Jae
authors.initials: HJ
authors.lastname: Shin
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000935:Antifungal Agents / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000737:chemistry*; D020171:Botrytis / Q000187:drug effects; D045744:Cell Line, Tumor; D020231:Colletotrichum / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D055666:Lipopeptides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D010838:Phytophthora / Q000187:drug effects; D012232:Rhizoctonia / Q000187:drug effects; D012235:Rhodamines / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D055666:Lipopeptides; D012235:Rhodamines; C022027:lissamine rhodamine B