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机构地区:[1]烟台市烟台山医院神经外科,山东烟台264000 [2]山东药品食品职业学院,山东威海264210 [3]沈阳药科大学药学院,辽宁沈阳110016
出 处:《沈阳药科大学学报》2013年第12期961-966,共6页Journal of Shenyang Pharmaceutical University
摘 要:目的研究雷公藤甲素与雷公藤红素抗炎作用量效关系。方法健康雄性Wistar大鼠灌胃给予雷公藤甲素与雷公藤红素的混合液,分别于给药前0h和给药后0.5、1.0、2.0、4.0、6.0、8.0和12.0h收集血清,利用液相色谱-质谱联用法检测大鼠血清中雷公藤甲素和雷公藤红素的浓度;采用小鼠腹腔巨噬细胞线RAW264.7,利用脂多糖(lipopolysaccharide,LPS)作为刺激剂构建炎症模型,向细胞模型中分别加入雷公藤甲素、雷公藤红素药液或含药血清,采用Griess试剂利用紫外分光光度法检测孵化液中一氧化氮(NO)的分泌情况。结果雷公藤甲素质量浓度高于200μg·L-1,即可抑制LPS对RAW264.7细胞的刺激,雷公藤红素药液质量浓度高于80μg·L-1时,也可产生此作用,并呈现浓度依赖关系。血清中雷公藤甲素的质量浓度在0.5和1.0h时高于300μg·L-1,雷公藤红素的血清质量浓度在0.5~6.0h内维持在200μg·L-1左右。大鼠服用雷公藤甲素和雷公藤红素后0.5~6.0h内的含药血清能明显抑制LPS对RAW264.7细胞的刺激作用,6.0h后含药血清抑制效果不显著。结论雷公藤甲素、雷公藤红素药液及大鼠服用雷公藤甲素和雷公藤红素后的含药血清均具有抗炎作用,该作用与这2种化合物体内浓度相关。Objective To investigate the effect of triptolide and tripterine as well as drug-containing serum on the secretion of nitric oxide of mouse macrophages. Methods Serum samples of healthy male Wistar rats were collected before(0 h)and at 0. 5,1.0,2. 0,4.0,6.0,8.0 and 12.0 h after dosing. Liquid chromatogra- phy-electrospray ionization mass spectrometry was applied for determination of triptolide and tripterine in rat serum. Mouse peritoneal macrophages RAW264. 7 cells were used to establish the inflammation model with the stimulating agents, lipopolysaccharide ( LPS ). Griess reagent was used to detect the secretion of nitric ox- ide in hatching fluids by ultraviolet spectrophotometry after adding triptolide, tripterine or drug-containing se- rum into the model. Results When the concentrations of triptolide and tripterine in serum were beyond 200 and 80 p^g-L-~, respectively, triptolide and tripterine can inhibit LPS stimulating RAW264. 7 cells which showed concentration dependence. The concentrations of triptolide in serum collected at 0.5 and 1.0 h were higher than 300 ~g. L- 1, and tripterine in serum collected between 0.5 h and 6. 0 h maintained at the level of 200 ~zg. L -1. The drug-containing serum between 0. 5 and 6.0 h after dosing can inhibit LPS stimulating RAW 264. 7 cells significantly, but the inhibition of the drug-containing serum collected after 6.0 h was not obvious. Conclusions Triptolide, tripterine and drug-containing serum after dosing triptolide and tripterine all show the anti-inflammatory effect, which was related to the concentration of the two compounds in vivo.
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