何首乌中二苯乙烯苷类成分 2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的抗骨关节炎体内外作用研究
In Vitro and In Vivo Anti-Osteoarthritis Effects of 2,3,5,4'-Tetrahydroxystilbene-2-O-β-d-Glucoside from Polygonum Multiflorum.
机构信息
School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan.
Department of Medical Sciences Industry, College of Health Sciences, Chang Jung Christian University, Tainan 71101, Taiwan.
出版信息
Molecules. 2018 Mar 3;23(3):571. doi: 10.3390/molecules23030571.
Thunb. is a traditional herbal medicine that is rich in polyphenols. The major compound, 2,3,5,4'-tetrahydroxystilbene-2--β-d-glucoside (THSG) has many pharmacological activities, such as antioxidative and free radical-scavenging properties, and the abilities to reduce hyperlipidemia, prevent lipid peroxidation, and protect the cardiovascular system. In this study, the anti-osteoarthritis (OA) effects of THSG were explored using in vitro and in vivo models. THSG inhibited nitric oxide (NO) and prostaglandin E₂ (PGE₂) production and inducible NO synthase (iNOS) and cyclooxygenase-2 expressions by lipopolysaccharide-stimulated RAW 264.7 cells. On the other hand, THSG inhibited PGE₂ production and iNOS and matrix metalloproteinase-13 expressions by interleukin-1β-stimulated primary rat chondrocytes. Through a mono-iodoacetate-induced rat OA model assay, THSG reduced paw edema and improved the weight-bearing distribution. Therefore, THSG has anti-inflammatory activity and could be applied as a lead compound for the development as an OA drug.
虎杖是一种富含多酚的传统草药。其主要化合物 2,3,5,4'-四羟基二苯乙烯-2-β-D-葡萄糖苷（THSG）具有多种药理活性，如抗氧化和清除自由基的特性，以及降低高血脂、预防脂质过氧化和保护心血管系统的能力。在这项研究中，使用体外和体内模型探讨了 THSG 对骨关节炎（OA）的治疗作用。THSG 抑制了脂多糖刺激的 RAW 264.7 细胞中一氧化氮（NO）和前列腺素 E₂（PGE₂）的产生以及诱导型一氧化氮合酶（iNOS）和环氧化酶-2 的表达。另一方面，THSG 抑制了白细胞介素-1β刺激的原代大鼠软骨细胞中 PGE₂的产生以及 iNOS 和基质金属蛋白酶-13 的表达。通过单碘乙酸诱导的大鼠 OA 模型测定，THSG 减轻了爪肿胀并改善了负重分布。因此，THSG 具有抗炎活性，可作为开发 OA 药物的先导化合物。
Zotero 插件