Longfei Lin,1,* Yuling Liu,1,* Ruying Tang,1 Shilan Ding,1 Hongmei Lin,2,3 Hui Li1,4 

1Institute Chinese Materia Medica China Academy of Chinese Medical Sciences, Beijing, People’s Republic of China; 2Beijing Research Institute of Chinese Medicine, Beijing University of Chinese Medicine, Beijing, People’s Republic of China; 3National Medical Products Administration Key Laboratory for Research Evaluation of Traditional Chinese Medicine, Beijing University of Chinese Medicine, Beijing, People’s Republic of China; 4Institute of Traditional Chinese Medicine Health Industry, China Academy of Chinese Medical Sciences, Nanchang, People’s Republic of China

*These authors contributed equally to this work

Correspondence: Hui Li, Institute Chinese Materia Medica China Academy of Chinese Medical Sciences, Beijing, 100700, People’s Republic of China, Email lihuizys@126.com Hongmei Lin, Beijing Research Institute of Chinese Medicine, Beijing University of Chinese Medicine, Beijing, 100029, People’s Republic of China, Email lhmtcm@126.com

Abstract: Evodiamine (EVO) is a tryptamine indole alkaloid and the main active ingredient in Evodia rutaecarpa. In recent years, the antitumor, cardioprotective, anti-inflammatory, and anti-Alzheimer’s disease effects of EVO have been reported. EVO exerts antitumor effects by inhibiting tumor cell activity and proliferation, blocking the cell cycle, promoting apoptosis and autophagy, and inhibiting the formation of the tumor microvasculature. However, EVO has poor solubility and low bioavailability. Several derivatives with high antitumor activity have been discovered through the structural optimization of EVO, and new drug delivery systems have been developed to improve the solubility and bioavailability of EVO. Current research found that EVO could have toxic effects, such as hepatotoxicity, nephrotoxicity, and cardiac toxicity. This article reviews the pharmacological activity, derivatives, drug delivery systems, toxicity, and pharmacokinetics of EVO and provides research ideas and references for its further in-depth development and clinical applications.

Keywords: evodiamine, pharmacology, derivatives, drug delivery systems