Yi Lang, Luo Jin-Fang, Xie Bing-Bing, Liu Jian-Xin, Wang Jun-Yue, Liu Liang, Wang Pei-Xun, Zhou Hua, Dong Yan
*Department of Immunology, Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou; and †State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau, China.
Shock. 2015 Aug;44(2):188-95. doi: 10.1097/SHK.0000000000000389.
Sinomenine (SIN), an alkaloid derived from the plant Sinomenium acutum, has anti-inflammatory and analgesic effects and has been used for rheumatoid arthritis treatment in China. This study aims to verify the hypothesis that SIN acts on α7 nicotinic acetylcholine receptor (α7nAChR) to inhibit the activation of macrophages stimulated by lipopolysaccharide. The prototypical α7nAChR antagonist α-bungarotoxin and mecamylamine attenuated the effect of SIN on tumor necrosis factor-α and interleukin-6 in RAW264.7 murine macrophage-like cells and primary peritoneal macrophages of mouse induced by lipopolysaccharide. With the knockdown of α7nAChR expression in RAW264.7 cells by small interfering RNA, the inhibitory effect of SIN on tumor necrosis factor-α and interleukin-6 was reversed. Sinomenine decreased p65 expression in nuclear and increased IκBα expression in cytoplasm, and these effects were reversed by the α7nAChR small interfering RNA as well. These results indicate that the anti-inflammatory effects of SIN on macrophages in vitro depend on α7nAChR.
青藤碱（SIN）是从植物青风藤中提取的一种生物碱，具有抗炎和镇痛作用，在中国已被用于治疗类风湿性关节炎。本研究旨在验证青藤碱作用于α7烟碱型乙酰胆碱受体（α7nAChR）以抑制脂多糖刺激的巨噬细胞活化这一假说。典型的α7nAChR拮抗剂α-银环蛇毒素和美加明减弱了青藤碱对脂多糖诱导的RAW264.7小鼠巨噬细胞样细胞和小鼠原代腹腔巨噬细胞中肿瘤坏死因子-α和白细胞介素-6的作用。通过小干扰RNA敲低RAW264.7细胞中α7nAChR的表达后，青藤碱对肿瘤坏死因子-α和白细胞介素-6的抑制作用被逆转。青藤碱降低了细胞核中p65的表达并增加了细胞质中IκBα的表达，而这些作用也被α7nAChR小干扰RNA逆转。这些结果表明，青藤碱在体外对巨噬细胞的抗炎作用依赖于α7nAChR。
