Gymnemagenin is a potent and selective antagonist for the β isoform of LXR, it has antihyperglycemic activity.

Gymnemagenin exhibited strong antioxidant activity in the assays, including TBA (56%), SOD-like (92%), and ABTS (54%). Blood glucose levels in the diabetic rats fed G. Gymnemagenin decreased to normal levels. The presence of the antihyperglycemic compounds gymnemagenin and gymnemic acids in G. sylvestre extract was detected by LC/MS analysis. Lipid peroxidation levels were decreased by 31.7% in serum, 9.9% in liver, and 9.1% in kidney in the diabetic rats fed the extract. Feeding G. Gymnemagenin to the diabetic rats decreased the activity of glutathione peroxidase in cytosolic liver and glutamate pyruvate transaminase in serum to normal levels.

Diabetes was induced in overnight-fasted rats by intravenous injection of 200 mg/kg body weight streptozotocin using a 5% solution of freshly prepared streptozotocin in 0.1 M citrate buffer (pH 4.5). Rats in the normal group were injected with a 0.1 M citrate buffer (pH 4.5) solution alone. A total of 40 rats (20 STZ-treated diabetic rats, 20 normal rats) were fed a basal diet for 4 weeks. The rats were divided into four groups (10 rats/group): group 1 (control), rats were fed the basal diet alone; group 2 (G. sylvestre-fed), rats were fed the basal diet plus Gymnemagenin (100 mg/kg/bw/day); group 3 (STZ-treated), STZtreated rats were fed the basal diet alone; group 4 (STZ-treated?G. sylvestre-fed), STZ-treated rats were fed the basal diet plus Gymnemagenin (100 mg/kg/bw/day).