Eight previously undescribed lanostane triterpenoids,including five nortriterpenoids with 26carbons,ganothenoids A-E(1-5),and three lanostanoids,ganothenoids F-H(6-8),along with 24 known ones(9-32),were isolated from ...Eight previously undescribed lanostane triterpenoids,including five nortriterpenoids with 26carbons,ganothenoids A-E(1-5),and three lanostanoids,ganothenoids F-H(6-8),along with 24 known ones(9-32),were isolated from the fruiting bodies of Ganodrma theaecolum.The structures of the novel compounds were elucidated using comprehensive spectroscopic methods,including electronic circular dichroism(ECD)and nuclear magnetic resonance(NMR)calculations.Compounds 1-32 were assessed for their neuroprotective effects against H_(2)O_(2)-induced damage in human neuroblastoma SH-SY5Y cells,as well as their inhibitory activities against protein tyrosine phosphatase 1B(PTP1B)andα-glucosidase.Compound 4demonstrated the most potent neuroprotective activity against H_(2)O_(2)-induced oxidative stress by suppressing G_0/G_1 phase cell cycle arrest,reducing reactive oxygen species(ROS)levels,and inhibiting cell apoptosis through modulation of B-cell lymphoma 2 protein(Bcl-2)and Bcl-2 associated X-protein(Bax)protein expression.Compounds 26,12,and 28 exhibited PTP1B inhibitory activities with IC_(50)values ranging from 13.92 to 56.94μmol·L~(-1),while compound12 alone displayed significant inhibitory effects onα-glucosidase with an IC_(50)value of 43.56μmol·L~(-1).Additionally,enzyme kinetic analyses and molecular docking simulations were conducted for compounds 26 and 12 with PTP1B andα-glucosidase,respectively.展开更多
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 elucidat...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.展开更多
基金supported by the National Natural Science Foundation of China (No.81973568)the Earmarked Fund for China Agriculture Research System (No.CARS-21)the Special Financial Project of the Ministry of Agriculture and Rural Areas (No.NFZX2024)。
文摘Eight previously undescribed lanostane triterpenoids,including five nortriterpenoids with 26carbons,ganothenoids A-E(1-5),and three lanostanoids,ganothenoids F-H(6-8),along with 24 known ones(9-32),were isolated from the fruiting bodies of Ganodrma theaecolum.The structures of the novel compounds were elucidated using comprehensive spectroscopic methods,including electronic circular dichroism(ECD)and nuclear magnetic resonance(NMR)calculations.Compounds 1-32 were assessed for their neuroprotective effects against H_(2)O_(2)-induced damage in human neuroblastoma SH-SY5Y cells,as well as their inhibitory activities against protein tyrosine phosphatase 1B(PTP1B)andα-glucosidase.Compound 4demonstrated the most potent neuroprotective activity against H_(2)O_(2)-induced oxidative stress by suppressing G_0/G_1 phase cell cycle arrest,reducing reactive oxygen species(ROS)levels,and inhibiting cell apoptosis through modulation of B-cell lymphoma 2 protein(Bcl-2)and Bcl-2 associated X-protein(Bax)protein expression.Compounds 26,12,and 28 exhibited PTP1B inhibitory activities with IC_(50)values ranging from 13.92 to 56.94μmol·L~(-1),while compound12 alone displayed significant inhibitory effects onα-glucosidase with an IC_(50)value of 43.56μmol·L~(-1).Additionally,enzyme kinetic analyses and molecular docking simulations were conducted for compounds 26 and 12 with PTP1B andα-glucosidase,respectively.
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)。
文摘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.
