The present work deals with the potential of Garcinia mangostana L. (Mangosteen, Clusiaceae) for modulation of digestive and plasma lipid transfer protein as an approach to discover novel inhibitors. Garcinia mangostana (in methanol, dicholromethane and hexane) extracts were screened for alpha amylase, alpha glucosidase and Cholesteryl ester transfer protein (CETP) inhibition assays. TLC, HPLC, LC-MS analysis were performed and was compared with reference standard. Alpha amylase results obtained were 39.4 µg/ml, 11.87 µg/ml and 9.048 µg/ml respectively. For CETP inhibition assay the dose response was done only for the hexane extract as others were not showing potent inhibition. Thus an IC50 of 10.89 µg/ml was obtained and the hexane extract was taken for further analysis to discover the compound responsible for the activity. Alpha mangosteen was found to be the active compound in Garcinia mangostana responsible for the potent inhibitor activity of alpha amylase and CETP enzyme in plant raw material.