Title:Evodiamine: A Privileged Structure with Broad-ranging Biological Activities
Volume: 22
Issue: 21
Author(s): Deping Li, Yan Li, Xiaowen Jiang, Wenwu Liu*Qingchun Zhao*
Affiliation:
- Department of Pharmacy, General Hospital of Northern Theater Command, Shenyang 110840, People’s Republic of
China
- School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People’s
Republic of China
- Department of Pharmacy, General Hospital of Northern Theater Command, Shenyang 110840, People’s Republic of
China
- School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People’s
Republic of China
Keywords:
Evodiamine, alkaloid, natural products, bioactivity, structure-activity relationship, rutaecarpine, β-carboline.
Abstract: Evodiamine (EVO) is a natural quinolone alkaloid firstly isolated from the fruit of Evodia rutaecarpa,
which is one of the most frequently used traditional Chinese herb for treating a variety of ailments,
including headaches, abdominal pain, vomiting, diarrhea, amenorrhea difficult menstruation,
postpartum hemorrhage, and other diseases. Latest pharmacological studies showed that EVO possesses a
broad spectrum of pharmacological activities through different mechanisms. However, its moderate activities
and poor physicochemical properties have hampered its clinical application. In this regard, the
modification of EVO aiming at seeking derivatives with more potency and better physicochemical properties
has been extensively emerging. These derivatives exhibit diverse biological activities, including
antitumor, anti-Alzheimer's disease, anti-pulmonary hypertension, anti-fungi, and thermogenic activities
via a variety of mechanisms. Moreover, they are described to act as single, dual, or multiple inhibitors or
agonists of many proteins, such as topoisomerase I, topoisomerase II, tubulin, histone deacetylase,
sirtuins, butyrylcholinesterase, phosphodiesterase 5, and transient receptor potential vanilloid 1. However,
hitherto, there is no comprehensive review to systematically summarize the derivatives of EVO. Considering
this perspective, this paper aims to provide a comprehensive description of them by focusing on
their diverse biological activities. For each biological activity, the mechanisms and the main structureactivity
relationships (SARs) will be presented in cases where adequate information is available. Finally,
future directions of this class of compounds will be discussed. This review will be helpful in understanding
and encouraging further exploration of EVO.
