【摘要】 目的通过体内、体外实验筛选橙皮苷衍生物1～9的抗炎活性。方法放射免疫法、高效液相色谱法分别检测橙皮苷衍生物对佐剂性关节炎(AA)大鼠腹腔巨噬细胞(PMΦ)前列腺素E2(PGE2)和白三烯B4(LTB4)生物合成的影响,采用二甲苯诱导小鼠耳肿胀模型对系列衍生物进行抗炎活性筛选,并观察抗炎活性较好的衍生物2对AA大鼠的治疗作用。结果体外实验表明衍生物2和5均能显著抑制AA大鼠PMΦPGE2和LTB4的合成,并呈明显的剂量依赖关系;体内筛选实验结果表明衍生物2和5具有良好的抗炎效果,作用与萘普生相当;进一步研究发现衍生物2对AA大鼠的继发性炎症具有较好的治疗作用,且衍生物2(100mg/kg)组优于母体橙皮苷(80mg/kg)。结论通过体内、体外实验筛选得到的橙皮苷衍生物2和5抗炎活性较强,具有一定的研究开发前景。更多还原

【Abstract】 Objective To screen the anti-inflammatory activity of hesperidin derivatives 1~9 with experiment in vivo and in vitro.Methods The content of prostaglandin E2(PGE2)and leukotriene B4(LTB4)from peritoneal macrophage(PMΦ) of adjuvant arthritis(AA) rats were measured by radioimmunity and HPLC method respectively.We used the screening model(dimethylbenzene-induced mouse ear edema) to evaluate the anti-inflammatory activity of hesperidin derivates in vivo.Furthermore,we observed the effect of the derivative 2 on AA rats secondary paw swelling.Results Derivative 2 and 5 of hesperidin significantly decreased the productions of PGE2 and LTB4 from PMΦ of AA rats in a dose-dependent manner.In addition,derivative 2 and 5 remarkably inhibited the ear edema which induced by dimethylbenzene in mice,as the same with naproxen.Furthermore,100 mg/kg derivative 2 had better therapeutical effect on AA rat secondary inflammatory than its parent compound hesperidin(80mg/kg).Conclusion Derivative 2 and 5 have significant anti-inflammatory activity and need further research and development.更多还原