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

Gymnemagenin在各项实验中展现出强大的抗氧化活性，包括TBA（56%）、SOD-like（92%）、ABTS（54%）。喂食G. Gymnemagenin的糖尿病大鼠血糖水平降至正常。G. sylvestre提取物中含有降血糖化合物gymnemagenin和gymnemic酸，通过LC/MS分析检测到。喂食该提取物的糖尿病大鼠，在血清中的脂质过氧化水平降低了31.7%，在肝脏中降低了9.9%，在肾脏中降低了9.1%。给糖尿病大鼠喂食G. Gymnemagenin还能将肝细胞质内的谷胱甘肽过氧化物酶活性和血清中的谷丙转氨酶活性降至正常水平。

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).