An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) inhibition.Bioassay guided fractionation resulted in the isolati...An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) inhibition.Bioassay guided fractionation resulted in the isolation of PTP1B inhibitory activity of triterpenes(1-4).These four compounds were identified as aceriphyllic acid C(1),aceriphyllic acid D(2),aceriphyllic acid E(3) and aceriphyllic acid F(4).The isolated 1-4 compounds inhibited PTP1B with IC50 values ranged from(2.1±1.5) μmol/L to(11.2±2.5) μmol/L.Kinetic analysis of PTP1B inhibition by aceriphyllic acid C(1) and aceriphyllic acid D(2) suggested that oleanane-type triterpenes inhibited PTP1B activity in a mixed-type manner.展开更多
基金The Scientific Research Foundation for the Returned Overseas Chinese Scholars(Grant No.20091590)State Education Ministry and Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules(Yanbian University),Ministry of Education,China(Grant No.201003)
文摘An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) inhibition.Bioassay guided fractionation resulted in the isolation of PTP1B inhibitory activity of triterpenes(1-4).These four compounds were identified as aceriphyllic acid C(1),aceriphyllic acid D(2),aceriphyllic acid E(3) and aceriphyllic acid F(4).The isolated 1-4 compounds inhibited PTP1B with IC50 values ranged from(2.1±1.5) μmol/L to(11.2±2.5) μmol/L.Kinetic analysis of PTP1B inhibition by aceriphyllic acid C(1) and aceriphyllic acid D(2) suggested that oleanane-type triterpenes inhibited PTP1B activity in a mixed-type manner.