【摘要】 目的 合成苦参碱-布洛芬有机盐，探究其抗菌抗炎活性及抗炎机制。方法 采用酸碱中和反应制备苦参碱-布洛芬有机盐，通过最低抑菌浓度（MIC）法检测其对金黄色葡萄球菌、枯草杆菌、大肠杆菌、变形杆菌和卡他莫拉菌的抑制作用；借助小鼠耳肿胀模型评价抗炎活性；测定其对脂多糖（LPS）刺激的巨噬细胞产生炎症因子[肿瘤坏死因子-α(TNF-α)、白细胞介素-2(IL-2)、一氧化氮（NO）]含量的影响，初步明确抗炎机制。结果 所得有机盐摩尔比1:1，产率为99.81%，水中溶解度为16.29 g。其对5种菌的MIC低于苦参碱和布洛芬，抗菌活性为苦参碱的2～4倍、布洛芬的16～128倍。50、100、200 mg/kg剂量肌内注射时，有机盐肿胀抑制率高于苦参碱和布洛芬。2.5～40μg/ml浓度范围内，三者均可降低致炎因子水平，且有机盐效果最优，呈剂量依赖性。结论 苦参碱-布洛芬有机盐水溶性提升，抗菌抗炎活性更强，抗炎机制可能与降低TNF-α、IL-2、NO分泌有关。更多还原

【Abstract】 Objective Synthesize the matrine-Ibuprofen organic salt, and investigate its antibacterial, anti-inflammatory activity and anti-inflammatory mechanism. Methods Matrine-Ibuprofen organic salt was prepared through acid-base neutralization reaction. The inhibitory effects on Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Proteus mirabilis and Moraxella catarrhalis were detected by the minimum inhibitory concentration(MIC) method, the anti-inflammatory activity was evaluated using a mouse ear swelling model, the effect of the organic salt on the production of inflammatory factors(tumor necrosis factor-α [TNF-α], interleukin-2 [IL-2], nitric oxide [NO]) by macrophages stimulated by lipopolysaccharide(LPS) was determined, and the anti-inflammatory mechanism was preliminarily clarified. Results The molar ratio of the obtained organic salt was 1:1, with a yield of 99.81%, and the water solubility was 16.29 g. Its MIC for the five bacteria was lower than those of matrine and Ibuprofen, and the antibacterial activity was 2-4 times that of matrine and16-128 times that of Ibuprofen. When injected intramuscularly at doses of 50, 100, and 200 mg/kg, the swelling inhibition rate of the organic salt was higher than those of matrine and ibuprofen. Within the concentration range of 2.5-40 μg/ml, all three could reduce the levels of inflammatory factors, and the organic salt had the best effect, showing a dose-dependent manner. Conclusion The water solubility of the matrine-Ibuprofen organic salt is improved, and its antibacterial and anti-inflammatory activity is stronger. The anti-inflammatory mechanism may be related to the reduction of TNF-α, IL-2,and NO secretion.更多还原