《Table 1 Inhibitory activities, free energy of binding, H-bond interactions, and hydrophobic interac

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《"Protein tyrosine phosphatase 1B inhibitory activities of ursane-type triterpenes from Chinese raspberry, fruits of Rubus chingii"》

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a IC50 were determined by regression analyses and expressed as mean±SD of three replicates；b IC50 from reference[23].

Triterpenes 1-3 were evaluated PTP1B inhibitory activities at different concentrations.As a result，1-3 inhibited PTP1B in a concentration dependent manner，and the IC50were determined by regression analyses（Table 1）.The inhibition modes of compounds 1-3 were further elucidated by kinetics analyses with various concentrations of the compounds and the substrate p-nitrophenyl phosphate（p-NPP）.As shown in Fig.2，Lineweaver-Burk plots indicated compounds 1 was a non-competitive PTP1B inhibitors with the Ki of 25.8μmol·L-1，and compounds 2 and 3 inhibited PTP1B by a mixed mode.The secondary plots of compounds 1 and 2showed good linear relationship，when they were created by the slopes from the Lineweaver-Burk plots on the y-axis against the concentration on the x-axis.Meanwhile，the secondary plot of compound 3 showed good linear relationship，when plotting[I]2 on the x-axis，suggesting that two molecules of 3 were involved in the inhibition of PTP1B activity.