Metabolic syndrome is coexistence of abdominal obesity, hyperglycemia, hyperlipidemia and hypertension that causes cardiovascular diseases, diabetes and their complications, low quality and short lifespan. Garcinia mangostana and its xanthones such as α-mangostin have been shown desirable effects such as anti-obesity, anti-hyperglycemic, anti-dyslipidemia, anti-diabetic and antiinflammatory effects in experimental studies. Various databases such as PubMed, Scopus and Web of Science with keywords of 'Garcinia mangostana', 'mangosteen', 'α-mangostin', 'metabolic syndrome', 'hypoglycemic', 'antihyperglicemic', 'antidiabetic', 'hypotensive', 'antihypertensive', 'atherosclerosis', 'arteriosclerosis' and 'hyperlipidemia' have been investigated in this search without publication time limitation. This study reviewed all pharmacological effects and molecular pathways of G. mangostana and its xanthones in the management of metabolic syndrome and its complications in in-vitro and in-vivo studies. Based on these studies, mangosteen and its xanthones have good potential to design human studies for controlling and modification of metabolic syndrome and its related disorders such as obesity, disrupted lipid profile, diabetes and its complications. Copyright © 2017 John Wiley & Sons, Ltd.