Shikonin is the major bioactive component extracted from the roots of Lithospermum erythrorhizon which is also known as “Zicao” in Traditional Chinese Medicine (TCM). Recent studies have shown that shikonin demonstrates various bioactivities related to the treatment of cancer, inflammation, and wound healing. This review aimed to provide an updated summary of recent studies on shikonin. Firstly, many studies have demonstrated that shikonin exerts strong anticancer effects on various types of cancer by inhibiting cell proliferation and migration, inducing apoptosis, autophagy, and necroptosis. Shikonin also triggers Reactive Oxygen Species (ROS) generation, suppressing exosome release, and activate anti-tumor immunity in multiple molecular mechanisms. Examples of these effects include modulating the PI3K/AKT/mTOR and MAPKs signaling; inhibiting the activation of TrxR1, PKM2, RIP1/3, Src, and FAK; and regulating the expression of ERP57, MMPs, ATF2, C-MYC, miR-128, and GRP78 (Bip). Next, the anti-inflammatory and wound-healing properties of shikonin were also reviewed. Furthermore, several studies focusing on shikonin derivatives were reviewed, and these showed that, with modification to the naphthazarin ring or side chain, some shikonin derivatives display stronger anticancer activity and lower toxicity than shikonin itself. Our findings suggest that shikonin and its derivatives could serve as potential novel drug for the treatment of cancer and inflammation.

紫草素是从紫草紫草根中提取的主要生物活性成分。在中医中也被称为“紫草”。最近的研究表明，紫草素具有多种与癌症，炎症和伤口愈合相关的生物活性。这篇综述旨在提供有关紫草素的最新研究的最新摘要。首先，许多研究表明，紫草素通过抑制细胞增殖和迁移，诱导细胞凋亡，自噬和坏死性坏死而对各种类型的癌症发挥强大的抗癌作用。紫草素还可以触发活性氧（ROS）的产生，抑制外泌体释放，并通过多种分子机制激活抗肿瘤免疫力。这些效应的例子包括调节PI3K / AKT / mTOR和MAPKs信号转导；抑制TrxR1，PKM2，RIP1 / 3，Src和FAK的激活; 并调节ERP57，MMP，ATF2，C-MYC，miR-128和GRP78（Bip）。接下来，还回顾了紫草素的抗炎和伤口愈合特性。此外，综述了一些针对紫草素衍生物的研究，这些研究表明，经过修饰萘酚环或侧链，一些紫草素衍生物显示出比紫草素本身更强的抗癌活性和更低的毒性。我们的发现表明，紫草素及其衍生物可以作为潜在的新型药物用于治疗癌症和炎症。一些紫草素衍生物显示出比紫草素本身更强的抗癌活性和更低的毒性。我们的发现表明，紫草素及其衍生物可以作为潜在的新型药物用于治疗癌症和炎症。一些紫草素衍生物显示出比紫草素本身更强的抗癌活性和更低的毒性。我们的发现表明，紫草素及其衍生物可以作为潜在的新型药物用于治疗癌症和炎症。