Screening and identification of potent α-glycosidase inhibitors from Gardenia jasminoides Ellis
2018
Hua, D.; Luo, W.; Duan, J.; Jin, D.; Zhou, X.; Sun, C.; Wang, Q.; Shi, C.; Jiang, Z.; Wang, R.; Rao, C.; Yu, S.; Li, S.; Tang, S.
https://dx.doi.org/10.1016/j.sajb.2018.10.004
The α-glycosidase inhibition assay is used to examine the inhibition activity of traditional Chinese medicines through extraction with methanol. The α-glycosidase inhibition activity of the isolated compounds is measured by α-glycosidase inhibition assay and compared with Acarbose. Molecular docking is implemented to study the interaction between isolated compounds and CtMGAM (maltase–glucoamylase-C) or NtMGAM (maltase–glucoamylase-N). Compared with those of Acarbose, the methanol extract of Gardenia jasminoides Ellis has a higher activity to inhibit α-glycosidase among the 74 traditional Chinese medicines. Geniposide and Gardenoside, isolated compounds from Gardenia jasminoides Ellis, have better inhibition activity (IC50 values of 0.35 and 0.46 mg/ml, respectively) than Acarbose (IC50 values of 0.75 mg/ml). The molecular docking results show that Geniposide and Gardenoside have specific binding affinities with CtMGAM and can be considered comparable to those of Acarbose. Our findings illuminate the possible anti-diabetic mechanism of Gardenia jasminoides Ellis and support its use for the treatment of diabetes.
[screening, glycosidases, chemical constituents of plants, acarbose, α-Glycosidase assay, Virtual screening, Molecular docking, Geniposide, Gardenia jasminoides, binding capacity, enzyme inhibition, α-Glycosidase inhibitor, methanol, computer simulation, Oriental traditional medicine, inhibitory concentration 50, enzyme inhibitors, diabetes, Gardenoside]
[South African journal of botany]
2019/US/US2019_0.rdf
The α-glycosidase inhibition assay is used to examine the inhibition activity of traditional Chinese medicines through extraction with methanol. The α-glycosidase inhibition activity of the isolated compounds is measured by α-glycosidase inhibition assay and compared with Acarbose. Molecular docking is implemented to study the interaction between isolated compounds and CtMGAM (maltase–glucoamylase-C) or NtMGAM (maltase–glucoamylase-N). Compared with those of Acarbose, the methanol extract of Gardenia jasminoides Ellis has a higher activity to inhibit α-glycosidase among the 74 traditional Chinese medicines. Geniposide and Gardenoside, isolated compounds from Gardenia jasminoides Ellis, have better inhibition activity (IC50 values of 0.35 and 0.46 mg/ml, respectively) than Acarbose (IC50 values of 0.75 mg/ml). The molecular docking results show that Geniposide and Gardenoside have specific binding affinities with CtMGAM and can be considered comparable to those of Acarbose. Our findings illuminate the possible anti-diabetic mechanism of Gardenia jasminoides Ellis and support its use for the treatment of diabetes.
