Department of Cardiology, Suzhou Kowloon Hospital of Shanghai Jiaotong University School of Medicine, #118 Wansheng Street, Suzhou 215021, Jiangsu, China.
Department of Pharmacology, School of Pharmacy, Nantong University,#19 Qixiu Road, Nantong 226001, Jiangsu, China; Key Laboratory of Inflammation and Molecular Drug Target of Jiangsu Province, #19 Qixiu Road, Nantong 226001, Jiangsu, China.
Eur J Pharmacol. 2017 Sep 15;811:21-29. doi: 10.1016/j.ejphar.2017.05.037. Epub 2017 May 23.
2,3,4',5-tetrahydroxystilbene 2-O-β-D-glucoside (TSG), a resveratrol analog with glucoside, is purified from a traditional Chinese herbal medicine polygonum multiflorum. It has been extensively studied in last decade and known to exert strong anti-inflammatory, anti-oxidative, anti-apoptotic, and free radical scavenging activities, and therefore has been listed as a potential agent for disease therapies. Recent studies extend well-beyond effects of TSG on the injury of neurons, cardiomyocytes and endothelial cells, and report important functions of TSG in a lot of pathophysiological conditions. For example, TSG has been shown to prevent the production of pro-inflammatory cytokines in microglia and macrophages in vitro, and ameliorate pro-inflammatory responses in animal models with neurodegeneration, atherosclerosis, and rat paw or ear oedema. TSG can prevent the proliferation of vascular smooth cells, gastrointestinal dysfunctions, platelet aggregation, osteoblastic injury, diabetic nephropathy and melanogenesis. TSG is also indicated to facilitate long-term potentiation and learning and memory in both normal and pathological conditions. These effects to some extent enrich the understanding about the role of TSG in disease prevention and therapy. However, to date, we still have no outlined knowledges about the pharmacological effects of TSG, though the role of TSG in aging and Alzheimer's disease has been reviewed in recent years. Here, we summarize the current pharmacological developments of TSG as well as its possible mechanisms in disease prevention and therapy, aiming to push the understanding about the protective role of TSG as well as its preclinical assessment of novel applications.
2,3,4',5-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(TSG),一种带有葡萄糖苷的白藜芦醇类似物,从传统中药何首乌中纯化得到。在过去十年中,它已被广泛研究,已知具有很强的抗炎、抗氧化、抗凋亡和自由基清除活性,因此被列为疾病治疗的潜在药物。最近的研究不仅扩展了 TSG 对神经元、心肌细胞和内皮细胞损伤的作用,还报告了 TSG 在许多病理生理条件下的重要功能。例如,TSG 已被证明可防止体外小胶质细胞和巨噬细胞中促炎细胞因子的产生,并改善神经退行性变、动脉粥样硬化、大鼠爪或耳水肿动物模型中的促炎反应。TSG 可防止血管平滑肌细胞增殖、胃肠功能障碍、血小板聚集、成骨细胞损伤、糖尿病肾病和黑色素生成。TSG 还表明可促进正常和病理条件下的长时程增强和学习记忆。这些作用在一定程度上丰富了对 TSG 在疾病预防和治疗中的作用的认识。然而,迄今为止,尽管近年来已经综述了 TSG 在衰老和阿尔茨海默病中的作用,但我们仍然没有关于 TSG 药理作用的概述知识。在这里,我们总结了 TSG 的当前药理学进展及其在疾病预防和治疗中的可能机制,旨在推动对 TSG 的保护作用以及其在新型应用中的临床前评估的理解。