School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
Beijing Research Institute of Chinese Medicine, Beijing University of Chinese Medicine, Beijing, China.
Pharm Biol. 2020 Dec;58(1):950-958. doi: 10.1080/13880209.2020.1818793.
Acetylshikonin, a naphthoquinone derivative, is mainly extracted from some species of the family Boraginaceae, such as Sieb. et Zucc., (Royle) Johnst., and Bunge. As a bioactive compound, acetylshikonin has attracted much attention because of its broad pharmacological properties.
This review provides a comprehensive summary of the pharmacology, toxicity, and pharmacokinetics of acetylshikonin focussing on its mechanisms on the basis of currently available literature.
The information of acetylshikonin from 1977 to 2020 was collected using major databases including Elsevier, Scholar, PubMed, Springer, Web of Science, and CNKI. Acetylshikonin, pharmacology, toxicity, pharmacokinetics, and naphthoquinone derivative were used as key words.
According to emerging evidence, acetylshikonin exerts a wide spectrum of pharmacological effects such as anticancer, anti-inflammatory, lipid-regulatory, antidiabetic, antibacterial, antifungal, antioxidative, neuroprotective, and antiviral properties. However, only a few studies have reported the adverse effects of acetylshikonin, with respect to reproductive toxicity and genotoxicity. Pharmacokinetic studies demonstrate that acetylshikonin is associated with a wide distribution and poor absorption.
Although experimental data supports the beneficial effects of this compound, acetylshikonin cannot be considered as a therapy drug without further investigations, especially, on the toxicity and pharmacokinetics.
乙酰紫草素是萘醌衍生物，主要从紫草科的一些物种中提取，如 Sieb. et Zucc.、 （罗伊勒）约翰斯通和 （Bunge）。作为一种生物活性化合物，乙酰紫草素因其广泛的药理学特性而备受关注。
本综述基于现有文献，对乙酰紫草素的药理学、毒性和药代动力学进行了全面总结，重点介绍其作用机制。
使用主要数据库（包括 Elsevier、Scholar、PubMed、Springer、Web of Science 和 CNKI）从 1977 年至 2020 年收集乙酰紫草素的信息。乙酰紫草素、药理学、毒性、药代动力学和萘醌衍生物被用作关键词。
根据新出现的证据，乙酰紫草素具有广泛的药理作用，如抗癌、抗炎、调脂、抗糖尿病、抗菌、抗真菌、抗氧化、神经保护和抗病毒作用。然而，只有少数研究报道了乙酰紫草素的不良反应，涉及生殖毒性和遗传毒性。药代动力学研究表明，乙酰紫草素具有广泛的分布和较差的吸收。
尽管实验数据支持这种化合物的有益作用，但乙酰紫草素不能被视为一种治疗药物，特别是在毒性和药代动力学方面，需要进一步研究。
