Abstract Context Acetylshikonin, a naphthoquinone derivative, is mainly extracted from some species of the family Boraginaceae, such as Lithospermum erythrorhizon Sieb. et Zucc., Arnebia euchroma (Royle) Johnst., and Arnebia guttata Bunge. As a bioactive compound, acetylshikonin has attracted much attention because of its broad pharmacological properties. Objective 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. Methods 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. Results 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. Conclusions 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.

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乙酰紫草素的药理学、毒性和药代动力学：综述

摘要 乙酰紫草素是萘醌衍生物，主要从紫草科紫草科植物中提取。等 Zucc.、Arnebia euchroma (Royle) Johnst. 和 Arnebia guttata Bunge。乙酰紫草素作为一种生物活性化合物，因其广泛的药理特性而备受关注。目的本综述在现有文献的基础上，对乙酰紫草素的药理学、毒性和药代动力学进行全面总结，重点阐述其作用机制。方法利用Elsevier、Scholar、PubMed、Springer、Web of Science、CNKI等主要数据库收集1977-2020年乙酰紫草素信息。以乙酰紫草素、药理学、毒性、药代动力学、萘醌衍生物为关键词。结果根据新出现的证据，乙酰紫草素具有广泛的药理作用，如抗癌、抗炎、调节血脂、抗糖尿病、抗菌、抗真菌、抗氧化、神经保护和抗病毒特性。然而，只有少数研究报告了乙酰紫草素在生殖毒性和遗传毒性方面的副作用。药代动力学研究表明，乙酰紫草素与广泛分布和吸收差有关。结论虽然实验数据支持该化合物的有益作用，但乙酰紫草素在没有进一步研究的情况下不能被视为治疗药物，特别是在毒性和药代动力学方面。抗炎、调节血脂、抗糖尿病、抗菌、抗真菌、抗氧化、神经保护和抗病毒特性。然而，只有少数研究报告了乙酰紫草素在生殖毒性和遗传毒性方面的副作用。药代动力学研究表明，乙酰紫草素与广泛分布和吸收差有关。结论虽然实验数据支持该化合物的有益作用，但乙酰紫草素在没有进一步研究的情况下不能被视为治疗药物，特别是在毒性和药代动力学方面。抗炎、调节血脂、抗糖尿病、抗菌、抗真菌、抗氧化、神经保护和抗病毒特性。然而，只有少数研究报告了乙酰紫草素在生殖毒性和遗传毒性方面的副作用。药代动力学研究表明，乙酰紫草素与广泛分布和吸收差有关。结论虽然实验数据支持该化合物的有益作用，但乙酰紫草素在没有进一步研究的情况下不能被视为治疗药物，特别是在毒性和药代动力学方面。关于生殖毒性和遗传毒性。药代动力学研究表明，乙酰紫草素与广泛分布和吸收差有关。结论虽然实验数据支持该化合物的有益作用，但乙酰紫草素在没有进一步研究的情况下不能被视为治疗药物，特别是在毒性和药代动力学方面。关于生殖毒性和遗传毒性。药代动力学研究表明，乙酰紫草素与广泛分布和吸收差有关。结论虽然实验数据支持该化合物的有益作用，但乙酰紫草素在没有进一步研究的情况下不能被视为治疗药物，特别是在毒性和药代动力学方面。