Four new triterpenoid saponins, tigensides A–D (1–4), and one new C21 steroid, tipregnane A(9), together with six known compounds were isolated from the EtOAc fraction of the roots and stems of Gymnema tingens.

Two new C 21 steroids, named 12-O-acetyl-(20S)-O-(N-methyl)anthraniloyl sarcostin-5α,6β-hexahydroxypregnane (1) and 12-O-acetyl-(20S)-O-(N-methyl)anthraniloyl sarcostin 3-O-β-Dcymaropyranoside ( 2), together with eight known compounds (3-10) were isolated from the dried whole plants of Gymnema tingens. The structures of the new compounds were established by extensive 1D and 2D nuclear magnetic resonance (NMR) spectra with mass spectroscopy data. Compounds 1-9 were tested for glucose uptake in L6 cells, and compounds 3 and 4 showed the most potent glucose uptake activity with the enhancement by 2.98-and 3.36-fold.