title: Aspernigrins with anti-HIV-1 activities from the marine-derived fungus Aspergillus niger SCSIO Jcsw6F30.
abstract: Two new 2-benzylpyridin-4-one containing metabolites, aspernigrins C (3) and D (4), together with six known compounds (1, 2, and 5-8), were isolated from the marine-derived fungus Aspergillus niger SCSIO Jcsw6F30. The structures of the new compounds were determined by NMR, MS, and optical rotation analyses. All the isolated compounds were evaluated for their inhibitory activities against infection with HIV-1 SF162 in TZM-bl cells. Malformin C (5) showed the strongest anti-HIV-1 activity with IC50 of 1.4±0.06μM (selectivity index, 11.4), meanwhile aspernigrin C (3) also exhibited potent activity with IC50 of 4.7±0.4μM (selectivity index, 7.5).
authors.affiliation: CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China.
authors.forename: Xuefeng
authors.initials: X
authors.lastname: Zhou
authors.affiliation: Center of Bio-pesticide Engineering Research, Hubei Academy of Agricultural Science, Wuhan 430064, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Fang
authors.affiliation: State Key Laboratory of Organ Failure Research, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, South Medical University, Guangzhou 510515, China.
authors.forename: Suiyi
authors.initials: S
authors.lastname: Tan
authors.affiliation: CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China.
authors.forename: Xiuping
authors.initials: X
authors.lastname: Lin
authors.affiliation: State Key Laboratory of Organ Failure Research, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, South Medical University, Guangzhou 510515, China.
authors.forename: Tianrong
authors.initials: T
authors.lastname: Xun
authors.affiliation: CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China; State Key Laboratory of Organ Failure Research, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, South Medical University, Guangzhou 510515, China.
authors.forename: Bingjie
authors.initials: B
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Organ Failure Research, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science, South Medical University, Guangzhou 510515, China. Electronic address: liusw@smu.edu.cn.
authors.forename: Shuwen
authors.initials: S
authors.lastname: Liu
authors.affiliation: CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China. Electronic address: yonghongliu@scsio.ac.cn.
authors.forename: Yonghong
authors.initials: Y
authors.lastname: Liu
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001234:Aspergillus niger / Q000737:chemistry*; D002460:Cell Line; D004354:Drug Screening Assays, Antitumor; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D011728:Pyridones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D011728:Pyridones; C000611445:aspernigrin C; D009536:Niacinamide
keywords: Aspergillus niger; Aspernigrins; HIV-1 SF162; Malformin C