Sesquiterpene lactones of Aucklandia lappa: Pharmacology, pharmacokinetics, toxicity, and structure–activity relationship
10.1016/j.chmed.2020.11.005
- Author:
Xin-nan LIU
1
;
Xin-nan LIU
2
;
Hui-min LI
2
;
Jing-ze ZHANG
2
;
Dai-lin LIU
2
;
Shu-ping WANG
3
Author Information
1. Tianjin University of Traditional Chinese Medicine
2. Department of Pharmacy, Logistics College of Chinese People's Armed Police Forces
3. Department of Pharmacy, Tianjin Provincial Corps Hospital, Chinese People's Armed Police Forces
- Publication Type:Journal Article
- Keywords:
Aucklandia lappa Dence;
pharmacokinetic;
pharmacological activities;
sesquiterpene lactones;
structure–activity relationship
- From:
Chinese Herbal Medicines
2021;13(2):167-176
- CountryChina
- Language:Chinese
-
Abstract:
The medicinal part of Aucklandia lappa (Asteraceae) is its dried root, which is one of the commonly used Chinese medicinal materials. Here we reviewed sesquiterpene lactones isolated from A. lappa over the past ten years in the following aspects of pharmacological activities, pharmacokinetics, toxicology, structure–activity relationship. Pharmacological activities consist of anti-cancer, anti-inflammatory activity, anti-immunity activity, anti-oxidant activity, antimicrobial activity, spasmolytic activity and so on. The extractive, showing similar pharmacokinetics parameters, may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacromolecules through Michael-addition. However, the poor aqueous solubility, non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class. In order to evaluate the potential effect of the extractive applied in clinical trial, the present review outlines information on pharmacological activities, pharmacokinetics, toxicology, and structure–activity relationship, as well as the future research directions of the extractive for further development and utilization of A. lappa.
