Title:Advance in Anti-tumor Mechanisms of Shikonin, Alkannin and their Derivatives
Volume: 18
Issue: 2
Author(s): Xu Zhang, Jia-Hua Cui, Qing-Qing Meng, Shao-Shun Li, Wen Zhou*Sui Xiao*
Affiliation:
- School of Chinese Meteria, Medica, Guangzhou University of Chinese Medicine, E. 232, Waihuan Rd, University Town, Panyu, Guangzhou, 510006,China
- Guangdong Key Laboratory for Innovative Development and Utilization of Forest Plant Germplasm, College of Forestry and Landscape Architecture, South China Agricultural University, Guangzhou 510642,China
Keywords:
Alkannin, anti-tumor mechanisms, bioalkylation, DNA, ROS, shikonin.
Abstract: Shikonin, alkannin and their derivatives, the main ingredient of Lithospermum erythrorhizon
and Arnebia euchroma (Royle) Johnst native to Inner Mongolian and Northwest of China respectively,
hold promising potentials for antitumor effects via multiple-target mechanisms. This review will emphasize
the importance of their antitumor activity in apoptosis, necroptosis and immunogenic cell
death, and expound the relationship of their antitumor activity and naphthoquinone scaffold that could
generate ROS and alkylating agent. Meanwhile, the antitumor mechanisms of naturally-occurring
shikonin, alkannin and their derivatives, which were divided into the direct interaction involved in alkylating
agent, covalently binding the DNA and protein, as well as the indirect interaction mediated by
ROS, nonspecifically influencing the mitochondria or multiple signal pathways, will be systematically
summarized and discussed.
