Obesity is a multi-factor chronic disease caused by the mixed influence of genetics, environments and an imbalance of energy intake and expenditure. Due to lifestyle changes, modern society sees a rapid increase in obesity occurrence along with an aggravated risk of metabolic syndromes in the general population, including diabetes, hepatic steatosis, cardiovascular diseases and certain types of cancer. Although obesity has become a serious worldwide public health hazard, effective and safe drugs treating obesity are still missing. Traditional Chinese medicine (TCM) has been implicated in practical use in China for thousands of years and has accumulated substantial front line experience in treating various diseases. Compared to western medicine that features defined composition and clear molecular mechanisms, TCM is consisted with complex ingredients from plants and animals and prescribed based on overall symptoms and collective experience. Because of their fundamental differences, TCM and western medicine were once considered irreconcilable. However, nowadays, sophisticated isolation technologies and deepened molecular understanding of the active ingredients of TCM are gradually bridging the gap between the two, enabling the identification of active TCM components for drug development under the western-style paradigms. Thus, studies on TCM open a new therapeutic avenue and show great potential in the combat against obesity, though challenges exist. In this review, we highlight six key candidate substances derived from TCM, including artemisinin, curcumin, celastrol, capsaicin, berberine and ginsenosides, to review their recent discoveries in the metabolic field, with special focus on their therapeutic efficacy and molecular mechanisms in treating obesity and metabolic diseases. In addition, we discuss the translational challenges and perspectives in implementing modern Chinese medicine into the western pharmaceutical industry.