A comprehensive review of ethnopharmacology, chemical constituents, pharmacological effects, pharmacokinetics, toxicology, and quality control of gardeniae fructus.

Ethnopharmacological Relevance: Gardeniae Fructus (GF), the desiccative mature fruitage of Gardenia jasminoides J. Ellis (G. jasminoides), belongs to the Rubiaceae family. It has abundant medicinal value, such as purging fire and eliminating annoyance, clearing heat and diuresis, cooling blood, and detoxifying. GF is usually used in combination with other drugs to treat diseases such as fever and jaundice in damp heat syndrome in traditional Chinese medicines (TCMs) clinical practice.

The Aim Of The Review: This review comprehensively summarizes the research progress in botany, traditional medical use, processing method, phytochemistry, pharmacological activity, quality control, pharmacokinetics, and toxicology, which aims to provide a scientific basis for the rational application and future research of GF.

Materials And Methods: ScienceDirect, PubMed, Web of Science, China National Knowledge Infrastructure (CNKI), Embase, Scopus etc. databases were retrieved to gain the comprehensive information of GF.

Results: At present, more than 215 compounds were isolated and identified from GF, including iridoids, diterpenes, triterpenoids, flavonoids, organic esters, and so on. The traditional application of GF mainly focused on clearing heat and detoxification. Pharmacological studies proved that GF had anti-inflammatory, antioxidation, antifatigue, antithrombotic, liver and gallbladder protection, and other pharmacological effects. In addition, many improved processing methods can alleviate the side effects and toxic reactions caused by long-term use of GF, so controlling its quality through multi-component content measurement has become an important means of research.

Conclusion: GF has a wide range of applications, the mechanisms by which some effective substances exert their pharmacological effects have not been clearly explained due to the complexity and diversity of its components. This review systematically elaborates on the traditional medical use, processing method, phytochemistry, pharmacological activity, quality control, and toxicology of GF, and it is expected to become a candidate drug for treating diseases, such as depression, pancreatitis, alcoholic or non-alcoholic fatty liver.