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作 者:Luting DAI Qingyi XIE Jiaocen GUO Qingyun MA Li YANG Jingzhe YUAN Haofu DAI Zhifang YU Youxing ZHAO
机构地区:[1]College of Food Science and Technology,Nanjing Agricultural University,Nanjing 210095,China [2]Key Laboratory of Research and Development of Natural Product from Li Folk Medicine of Hainan Province,Institute of Tropical Bioscience and Biotechnology,Chinese Academy of Tropical Agricultural Sciences&Hainan Academy of Tropical Agricultural Resource,Haikou 571101,China
出 处:《Journal of Oceanology and Limnology》2024年第3期905-914,共10页海洋湖沼学报(英文)
基 金:Supported by the China Agriculture Research System of MOF and MARA(CARS-21);the Financial Fund of the Ministry of Agriculture and Rural Affairs,China(No.NFZX2021);the National Natural Science Foundation of China(No.81973568)。
摘 要:A new isochromanone,cladosporinisochromanone(1),accompanied by 15 known compounds(2–16)were obtained from secondary metabolites produced by marine-derived fungus Cladosporium sp.DLT-5.NMR and HRESIMS spectra elucidation determined the planar structure of 1.Subsequent electronic circular dichroism(ECD)experiment assigned the absolute configuration of 1.Compounds 1,2,4–6,and 10 displayed different degrees of neuroprotective activities on human neuroblastoma cells SH-SY5Y.Five compounds(1,3–5,and 13)emerged resistance to protein tyrosine phosphatase 1B(PTP1B),further kinetic analysis and molecular docking study indicated that the most potent compound 13(IC50value of 10.74±0.61μmol/L)was found as a noncompetitive inhibitor for PTP1B.Surface plasmon resonance(SPR)and molecular docking studies also demonstrated the interaction between compound 12 and Niemann-Pick C1 Like 1(NPC1L1),which has been identified as significant therapeutic target for hypercholesteremia.In addition,compounds 3,6,and 14 showed attractive inhibitory activity against the phytopathogenic fungi:Colletotrichum capsici.Therefore,library of Cladosporium metabolites is enriched and new active uses of known compounds are explored.
关 键 词:Cladosporium sp. marine-derived fungus neuroprotective effects protein tyrosine phosphatase 1B(PTP1B) Niemann-Pick C1 Like 1(NPC1L1) antifungal activity
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