Phi Hung Nguyen


Phytochemical analysis of the methanol extract of the aerial parts of Orthosiphon stamineus Benth. led to the isolation of four flavone compounds including 5-hydroxy-3,7,3′,4′-tetramethoxyflavone (1), 3,5,7,3′,4′-pentamethoxyflavone (2), 3,3′-dihydroxy-5,7,4′-trimethoxyflavone (3), and 3,5,3′-trihydroxy-7,4ʹ-dimethoxyflavone (4). Their chemical structures were determined from the spectroscopic evidences, including 1D-NMR and MS, respectively. The inhibitory effects of the isolates (14) against protein tyrosine phosphatase 1B (PTP1B) enzyme were investigated in vitro using ursolic acid as positive control. Among the isolates, compound 4 exhibited potential activity with IC50 value of 10.12 ± 0.19 μM, the others showed weak activity. In this assay, ursolic acid displayed an IC50 value of 3.42 ± 0.25 μM. This is indicated that 3,3′-dihydroxy-5,7,4′-trimethoxyflavone (4) maybe useful for discovery of PTP1B inhibitors as antidiabetic agent.


Orthosiphon stamineus Benth.; flavone; ursolic acid; PTP1B inhibitor; type 2 diabetes

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