The EtOAc fraction of Alpinia katsumadai seeds showed significant inhibition on glycogen phosphorylase a(GPa)with inhibitory ratios of 97.9%and 64.6%at concentrations of 200 and 100μg/mL,respectively.Bioactivity-guid...The EtOAc fraction of Alpinia katsumadai seeds showed significant inhibition on glycogen phosphorylase a(GPa)with inhibitory ratios of 97.9%and 64.6%at concentrations of 200 and 100μg/mL,respectively.Bioactivity-guided isolation afforded 15 new diarylheptanoid-flavanone hybrids,katsumadainols B_(1)-B_(15)(1-15),together with eight known ones(16-23).Compounds 4-10 and 12-21 exhibited activity against GPa with IC_(50) values of 10.1-95.4μmol/L;compounds 4,5,16,and 17 displayed inhibitory effects onα-glucosidase with IC_(50) values of 7.1,12.4,7.2,and 8.3μmol/L,obviously higher than acarbose(IC_(50),209.1μmol/L);compounds 4-6,14,16-20,22,and 23 were PTP1B/TCPTP selective inhibitors with IC_(50) values of 40.7-95.8μmol/L;compounds 4,5,16,and 17 showed DPP4 inhibitory effects with inhibitory ratios of 50.0%-54.2%(200μmol/L).Diarylheptanoid-flavanone hybrids(4,5,16,and 17)with a p-hydroxybenzyl at C-6 position represent a promising class of multiple-target antidiabetic agents inhibiting GPa,α-glucosidase,PTP1B,and DPP4.展开更多
基金This work was financially supported by the Yunnan Wanren Project(YNWR-QNBJ-2018-061)the Fund of State Key Laboratory of Phytochemistry and Plant Resources in West China(P2020-KF05)+3 种基金the Postdoctoral Oriented Training Program of Yunnan Province(E131821261)the Special Research Assistant Project of Chinese Academy of Sciences(E12D9211Q1)the Yunnan Science Fund for Excellent Young Scholars(2019FI017)the Reserve Talents of Young and Middle-aged Academic and Technical Leaders in Yunnan Province.
文摘The EtOAc fraction of Alpinia katsumadai seeds showed significant inhibition on glycogen phosphorylase a(GPa)with inhibitory ratios of 97.9%and 64.6%at concentrations of 200 and 100μg/mL,respectively.Bioactivity-guided isolation afforded 15 new diarylheptanoid-flavanone hybrids,katsumadainols B_(1)-B_(15)(1-15),together with eight known ones(16-23).Compounds 4-10 and 12-21 exhibited activity against GPa with IC_(50) values of 10.1-95.4μmol/L;compounds 4,5,16,and 17 displayed inhibitory effects onα-glucosidase with IC_(50) values of 7.1,12.4,7.2,and 8.3μmol/L,obviously higher than acarbose(IC_(50),209.1μmol/L);compounds 4-6,14,16-20,22,and 23 were PTP1B/TCPTP selective inhibitors with IC_(50) values of 40.7-95.8μmol/L;compounds 4,5,16,and 17 showed DPP4 inhibitory effects with inhibitory ratios of 50.0%-54.2%(200μmol/L).Diarylheptanoid-flavanone hybrids(4,5,16,and 17)with a p-hydroxybenzyl at C-6 position represent a promising class of multiple-target antidiabetic agents inhibiting GPa,α-glucosidase,PTP1B,and DPP4.
