School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Key Laboratory of Standardization for Chinese Herbal Medicine, Ministry of Education, National Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, Chengdu, China; School of Basic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Key Laboratory of Standardization for Chinese Herbal Medicine, Ministry of Education, National Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, Chengdu, China.
Pharmacol Res. 2019 Nov;149:104463. doi: 10.1016/j.phrs.2019.104463. Epub 2019 Sep 22.
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.
紫草素是从紫草的根中提取的主要生物活性成分，紫草在中药（TCM）中也被称为“紫草”。最近的研究表明，紫草素具有多种与癌症治疗、炎症和伤口愈合相关的生物活性。本综述旨在提供对紫草素的最新研究的更新总结。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、自噬和坏死来发挥对各种类型癌症的强烈抗癌作用。紫草素还通过多种分子机制触发活性氧（ROS）的产生，抑制外泌体的释放，并激活抗肿瘤免疫。这些作用的例子包括调节 PI3K/AKT/mTOR 和 MAPKs 信号通路；抑制 TrxR1、PKM2、RIP1/3、Src 和 FAK 的激活；调节 ERP57、MMPs、ATF2、C-MYC、miR-128 和 GRP78（Bip）的表达。接下来，还综述了紫草素的抗炎和伤口愈合特性。此外，还对一些专注于紫草素衍生物的研究进行了综述，这些研究表明，通过对萘并萘醌环或侧链进行修饰，一些紫草素衍生物比紫草素本身具有更强的抗癌活性和更低的毒性。我们的研究结果表明，紫草素及其衍生物可能成为治疗癌症和炎症的潜在新型药物。
