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目的研究腰痛宁及其衍生方中几种皂苷有效部位的细胞抗炎、免疫调节与骨细胞修复活性,为风湿骨病处方候选药物筛选提供依据。方法在马钱子、麻黄生物碱与甘草等5种药材黄酮混合物的基础上,分别加入50%的甘草皂苷、三七皂苷、人参皂苷、川牛膝皂苷组成新的中药有效部位组方。采用半数有效浓度(EC50)或半数抑制浓度(IC50)评价各样品对巨噬细胞Ana-1分泌白介素(IL)-1β、IL-6、肿瘤坏死因子-α(TNF-α)的促进作用;对脂多糖(LPS)诱导的Ana-1释放前列腺素(PG)E2的抑制作用;对IL-1β诱导的软骨细胞增殖的影响。同时采用最小二乘优化方法,计算各样品的EC50或IC50叠加值,根据EC50或IC50叠加值与实验值之间的差异分析各有效部位间的相互作用关系。结果 25%生物碱+25%黄酮+50%甘草皂苷组方的细胞抗炎、免疫和促进骨细胞修复活性优于其他组方,且该方中的各有效部位之间产生了较强的协同增效作用。结论以甘草皂苷为主的I号样品有良好的细胞抗炎、免疫调节及骨细胞修复活性,提示甘草皂苷可作为生物碱+黄酮+皂苷的风湿骨病处方中皂苷的优选有效部位。
Objective To study the cellular anti-inflammatory, immunoregulatory and osteoclast repair activities of several effective fractions of Yaotongning and its derivatives in rheumatoid bone disease. Methods Fifty percent of glycyrrhizin, notoginseng saponin, ginsenoside and dichoganenoside were added to the active ingredients of Chinese traditional medicine on the basis of 5 flavonoids mixture of Strychnos nux vomica, Ephedra alkaloids and Glycyrrhiza uralensis. The effects of each sample on the secretion of interleukin-1β, IL-6 and tumor necrosis factor-α (TNF-α) by macrophages were evaluated by EC50 or IC50. On lipopolysaccharide (LPS) -induced Ana-1 release of prostaglandin (PG) E2; IL-1β-induced chondrocyte proliferation. At the same time, the least square method was used to calculate the EC50 or IC50 superposition value of each sample. The interaction between the effective parts was analyzed according to the difference between the EC50 or IC50 superposition value and the experimental value. Results The anti-inflammatory, immune and osteoclast repair activities of 25% alkaloids + 25% flavonoids + 50% Glycyrrhizin group were better than those of other groups, and strong synergism was found among the effective sites Synergy. Conclusion Glycyrrhizin-based sample I has good cell anti-inflammatory, immunomodulatory and osteoclast repair activities, suggesting that glycyrrhizin can be used as alkaloids + flavonoids + saponins rheumatoid bone prescription saponins in the preferred effective site.