Ginseng (Panax ginseng C. A. Meyer) has been recorded to treat 'Xiao-ke' (emaciation and thirst) symptom in many ancient Chinese medical literatures (such as 'Shen Nong Ben Cao Jing') for thousands of years. 'Xiao-ke' symptom, in general, indicates diabetes mellitus. Malonyl ginsenosides (MGR) are natural ginsenosides which exist in both fresh and air-dried ginseng. The objective of this study is to determine the antidiabetic function of MGR on type 2 diabetes. High fat diet-fed and streptozotocin-induced diabetic rats were treated with 50 and 100mg/kg/d of MGR or vehicle for 3 weeks. The effects of MGR on fasting blood glucose (FBG), intraperitoneal glucose tolerance test (IPGTT), serum insulin (SI), insulin tolerance test (ITT), body weight, total cholesterol (TC), and triglyceride (TG) levels in type 2 diabetic rats were measured. After 3 weeks of treatment, MGR administration showed significantly lower FBG levels compared to the diabetic control group. In glucose tolerance test, IPGTT data showed that both MGR 50 and 100mg/kg groups significantly increased the glucose disposal after glucose load. The ITT also showed improvement of insulin sensitivity during 120 min of insulin treatment. In addition, MGR reduced TG and TC contents while showed no effect on body weight in diabetic rats. The findings from this study suggest that MGR can alleviate hyperglycemia, hyperlipemia and insulin resistance of type 2 diabetes. Crown Copyright © 2012. Published by Elsevier Ireland Ltd. All rights reserved.