From Orthosiphon stamineus Benth, seven pimarane diterpenes (1–7) have been isolated. By isolation by assay-guided. Both isolates had a 2-deoxy-2-((7-nitro-2,1,3-benzoxadiazole-4-yl)amino)-d-glucose absorption effect at 5 and 10 μM concentrations in 3T3-L1 adipocytes. Most of them demonstrated potent protein tyrosine phosphatase 1B inhibition with IC50 values ranging from 0.33 to 9.84...