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目的通过人全血培养方法筛选有潜在抗类风湿性关节炎作用的青藤碱衍生物。方法细菌酯多糖(LPS)刺激人全血诱导TNF-α产生,加入青藤碱衍生物,ELISA法检测其对TNF-α生成的抑制作用。结果浓度为10~4 mol/L时,青藤碱衍生物SIN-3、SIN-33对TNF-α的抑制率分别为22.9%和31.1%,其中SIN-33的抑制作用明显比强于青藤碱(24.2%),P<0.05。结论青藤碱衍生物SIN-33可明显抑制人全血中LPS诱导的TNF-α的生成,可作为抗类风湿性关节炎候选药物进一步研究。
Objective To screen sinomenine derivatives with potential anti-rheumatoid arthritis effect by human whole blood culture. Methods The lipopolysaccharide (LPS) stimulated human whole blood to induce the production of TNF-α. The sinomenine derivative was added to detect the inhibitory effect on TNF-α production by ELISA. Results The inhibitory rates of sinomenine derivatives SIN-3 and SIN-33 on TNF-α were 22.9% and 31.1% at the concentration of 10 ~ 4 mol / L, respectively. The inhibition effect of SIN-33 was stronger than that of cyanine Nicotine (24.2%), P <0.05. Conclusion Sinomenine derivative SIN-33 can significantly inhibit LPS-induced TNF-α production in human whole blood and can be used as a candidate drug for anti-rheumatoid arthritis.