Garcinia species, which have been studied for more than 70 years, comprise a large genus of tropical evergreen trees and shrubs that are widely distributed throughout Southeast Asia and Southern Africa. This genus consists of 450 species, of which 22 species are found across China. Xanthones, polycyclic polyprenylated acylphloroglucinols (PPAPs) and benzophenones are the major compounds obtained from these species, and exhibit anti-tumor, anti-inflammation and anti-virus activities. The research on Garcinia has become one of the hotspots in the field of natural compounds in recent years. Our in-depth comprehensive and systematic research on Chinese Garcinia plants could be traced back to 2005. So far, we have isolated more than 300 compounds, including over 150 components novel in structure. Through technologies and means of Analytical Chemistry, Molecular Biology, Proteomics, Computational Chemistry and Modern Pharmacology in our previous study, we have confirmed that PPAPs such as Oblongifolin C (OC) and Guttiferon K (GUTK) isolated from Garcinia yunnanensis Hu and Cambogin isolated from Garcinia esculenta have significant anti-tumor and anti-inflammation activities. In the past decade, we have published over 85 SCI papers on Garcinia species. We have also obtained 6 US patents and 15 Chinese patents and our research is supported by 10 of National Natural Science Foundation of China (NSFC). At present, we are focusing resources on large-scale preparation, chemical structure modification, anti-tumor and anti-inflammation molecular mechanism research of some bioactive compounds. Our study provides theoretical guidance for the comprehensive utilization of natural compounds and lays the ground work for the development of new drugs.