Liu Hai, Yang Jianqiong, Yang Wanqing, Hu Shaonan, Wu Yali, Zhao Bo, Hu Haiyan, Du Shouying
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, People's Republic of China.
College of Pharmacy, Gannan Medical University, Ganzhou, Jiangxi, People's Republic of China.
Drug Des Devel Ther. 2020 Feb 7;14:551-565. doi: 10.2147/DDDT.S240511. eCollection 2020.
Notoginsenoside (NG)-R1 is one of the main bioactive compounds from (PN) root, which is well known in the prescription for mediating the micro-circulatory hemostasis in human. In this article, we mainly discuss NG-R1 in metabolism and the biological activities, including cardiovascular protection, neuro-protection, anti-diabetes, liver protection, gastrointestinal protection, lung protection, bone metabolism regulation, renal protection, and anti-cancer. The metabolites produced by deglycosylation of NG-R1 exhibit higher permeability and bioavailability. It has been extensively verified that NG-R1 may ameliorate ischemia-reperfusion (IR)-induced injury in cardiovascular and neuronal systems mainly by upregulating the activity of estrogen receptor α-dependent phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT) and nuclear factor erythroid-2-related factor 2 (NRF2) pathways and downregulating nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) pathways. However, no specific targets for NG-R1 have been identified. Expectedly, NG-R1 has been used as a main bioactive compound in many Traditional Chinese Medicines clinically, such as Xuesaitong, Naodesheng, XueShuanTong, ShenMai, and QSYQ. These suggest that NG-R1 exhibits a significant potency in drug development.
三七皂苷（NG）-R1是三七（PN）根中的主要生物活性化合物之一，在用于调节人体微循环止血的方剂中广为人知。在本文中，我们主要讨论NG-R1的代谢和生物活性，包括心血管保护、神经保护、抗糖尿病、肝脏保护、胃肠道保护、肺保护、骨代谢调节、肾脏保护和抗癌作用。NG-R1去糖基化产生的代谢产物具有更高的通透性和生物利用度。大量研究证实，NG-R1可能主要通过上调雌激素受体α依赖性磷酸肌醇3激酶（PI3K）/蛋白激酶B（AKT）和核因子红细胞2相关因子2（NRF2）信号通路的活性，以及下调核因子κB（NF-κB）和丝裂原活化蛋白激酶（MAPK）信号通路，来减轻缺血再灌注（IR）诱导的心血管和神经系统损伤。然而，尚未确定NG-R1的具体靶点。不出所料，NG-R1已在临床上被用作许多中药的主要生物活性成分，如血塞通、脑得生、血栓通、参麦和芪参益气滴丸。这些表明NG-R1在药物开发中具有显著的潜力。
