Phyllanthus niruri is used in herbal medicine for treatment of diabetes. The objective of this study was to investigate the antidiabetic potential of P. niruri, using assays for alpha-glucosidase, muscle glucose transport, liver glucose production and adipogenesis. alpha-Glucosidase inhibitory activity was performed on aqueous and ethanolic extract of aerial parts of P. niruri. The aqueous and ethanolic extract of P. niruri showed alpha-glucosidase inhibitory activity with IC50 values of 3.7 +/- 1.1 and 6.3 +/- 4.8 mu g/mL, respectively. HR-bioassay/HPLC-HRMS and NMR analysis was used for identification of compounds. Corilagin (1) and repandusinic acid A (2) were identified as alpha-glucosidase inhibitors in the water extract of P. niruri with IC50 values of 0.9 +/- 0.1 and 1.9 +/- 0.02 mu M, respectively. In in vitro cell-based bioassays, cells were treated for 18 h with maximal non-toxic concentrations of the ethanolic extract of P. niruri, which were determined by the lactate dehydrogenase cytotoxicity assay. The ethanolic extract of P. niruri was not able to reduce glucose-6-phosphatase activity. However, the extract increased deoxyglucose uptake in C2C12 muscle cells and enhanced adipogenesis in 3T3-L1 fat cells which has been reported for the first time. The present study demonstrated that P. niruri may thus have potential application for treatment and/or management of type 2 diabetes. (C) 2017 Elsevier Inc. All rights reserved.