title: Antituberculosis compounds from a deep-sea-derived fungus Aspergillus sp. SCSIO Ind09F01.
abstract: Eleven diketopiperazine and fumiquinazoline alkaloids (1-11) together with a tetracyclic triterpenoid helvolic acid (12) were obtained from the cultures of a deep-sea derived fungus Aspergillus sp. SCSIO Ind09F01. The structures of these compounds (1-12) were determined mainly by the extensive NMR, ESIMS spectra data and by comparison with previously described compounds. Besides, anti-tuberculosis, cytotoxic, antibacterial, COX-2 inhibitory and antiviral activities of these compounds were evaluated. Gliotoxin (3), 12,13-dihydroxy-fumitremorgin C (11) and helvolic acid (12) exhibited very strong anti-tuberculosis activity towards Mycobacterium tuberculosis with the prominent MIC50values of <0.03, 2.41 and 0.894 μM, respectively, which was here reported for the first time. Meanwhile gliotoxin also displayed significant selective cytotoxicities against K562, A549 and Huh-7 cell lines with the IC50values of 0.191, 0.015 and 95.4 μM, respectively.
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.|b University of Chinese Academy of Sciences , Beijing , P.R. China.
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Luo
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Xuefeng
authors.initials: X
authors.lastname: Zhou
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Xiuping
authors.initials: X
authors.lastname: Lin
authors.affiliation: c Laboratory of Molecular Engineering and Laboratory of Natural Product Synthesis/State Key Laboratory of Respiratory Diseases , Center for Infection and Immunity, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou , China.
authors.forename: Xiaochu
authors.initials: X
authors.lastname: Qin
authors.affiliation: c Laboratory of Molecular Engineering and Laboratory of Natural Product Synthesis/State Key Laboratory of Respiratory Diseases , Center for Infection and Immunity, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou , China.
authors.forename: Tianyu
authors.initials: T
authors.lastname: Zhang
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Junfeng
authors.initials: J
authors.lastname: Wang
authors.affiliation: c Laboratory of Molecular Engineering and Laboratory of Natural Product Synthesis/State Key Laboratory of Respiratory Diseases , Center for Infection and Immunity, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou , China.
authors.forename: Zhengchao
authors.initials: Z
authors.lastname: Tu
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Bin
authors.initials: B
authors.lastname: Yang
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Shengrong
authors.initials: S
authors.lastname: Liao
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Yongqi
authors.initials: Y
authors.lastname: Tian
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.|b University of Chinese Academy of Sciences , Beijing , P.R. China.
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Pang
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.
authors.forename: Kumaravel
authors.initials: K
authors.lastname: Kaliyaperumal
authors.affiliation: d School of Pharmacy , Nantong University , Nantong , China.
authors.forename: Jian Lin
authors.initials: JL
authors.lastname: Li
authors.affiliation: e School of Traditional Chinese Medicine , Southern Medical University , Guangzhou , China.
authors.forename: Huaming
authors.initials: H
authors.lastname: Tao
authors.affiliation: a CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology , South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou , P.R. China.|f South China Sea Bio-Resource Exploitation and Utilization Collaborative Innovation Center , Guangzhou , China.
authors.forename: Yonghong
authors.initials: Y
authors.lastname: Liu
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology*; D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology; D059001:Aquatic Organisms; D001230:Aspergillus / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005672:Fusidic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D005912:Gliotoxin / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020014:K562 Cells; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects
chemical_list: D000470:Alkaloids; D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D000998:Antiviral Agents; D005672:Fusidic Acid; D005912:Gliotoxin; C011267:helvolic acid
keywords: Aspergillus sp; Deep sea fungi; alkaloids; anti-tuberculosis