Zi Cao is an important traditional medicinal plant resource in China. Shikonin and its derivatives, as the purple-red naphthoquinones among natural products of its roots, are commonly used clinically in the treatment of sores and skin inflammations. Over the past few decades, due to their highly effective multiple biological activities, pharmacological effects, good clinical efficacy and high utilization value, shikonin and its derivatives have attracted increasing attention of domestic and foreign researchers. For this reason, the wild plant germplasm resources have been suffering a grievous exploitation, leading to a serious threat to the habitat. With the development of the biosynthesis, molecular metabolism and biotechnology, as well as the continuous innovation of research methods on the biological activities and pharmacological effects of plant natural products, significant progress has been made in the research on the biosynthetic pathways and related regulatory genes of shikonin. The pharmacological action and its mechanism of shikonin have also been deeply elucidated, which greatly promoted the basic research and clinical application development of shikonin. In this review, we briefly introduce and analyze the classification of Zi Cao, structure and composition of natural shikonin and its biosynthesis pathway, functional genes related to the regulation of shikonin biosynthesis, and biological activities and pharmacological functions of shikonin. Finally, we address possible prospective for the trend on the future research and development of natural shikonin and its derivatives, hoping to provide a useful reference for the deep mining and development of medicinal natural products from important Chinese medicinal materials, and to promote the modern development of traditional Chinese medicine.
紫草为我国传统的重要药用植物资源,其根部代谢产生的紫红色萘醌类天然产物—紫草素及其衍生物,临床上常被用于治疗疮疡和皮肤炎症。数十年来,紫草因具高效的多重生物活性、药理作用、良好的临床疗效、较高的利用价值,引起了国内外研究者的重视与关注,正由于此种原因,其野生植物种质资源常遭到大量采挖,生长环境受到严重威胁。随着植物天然产物的生物合成、分子代谢及其生物技术的发展,药用植物天然产物生物活性功能与药理作用研究手段的不断创新,紫草的生物合成途径和相关调控基因的研究取得了显著的进展,紫草素药理作用及其机制得到深入阐明或解析,极大地推进了紫草素的基础性研究及其临床应用开发的进程。本文从紫草分类、紫草素的结构与组成及其生物合成途径、调控紫草素生物合成代谢的功能相关基因以及紫草素生物活性与药理功能等方面综述了相关研究进展,并对未来可能的发展趋势进行了展望,以期为促进我国重要中药材源的药用天然产物的深度挖掘与开发提供有益参考,推动我国传统中药学的现代化发展。.
Keywords: Zi Cao; biosynthesis; gene regulation; pharmacological activity; shikonin.