龙胆碱的解热作用及机制研究

Study on Antipyretic Effect and Its Mechanism of Gentianine

目的:比较龙胆水提液,龙胆碱及龙胆苦苷解热作用的差异,初步探讨龙胆碱的解热作用机制。方法:雄性SD大鼠,经筛选后随机分为空白对照组、发热模型组、龙胆碱组,龙胆苦苷组及龙胆水提组,采用干酵母皮下注射方法制备发热模型,于模型制备后6 h,分别ip龙胆碱溶液(100 mg.kg-1)、龙胆苦苷溶液(200 mg.kg-1)及ig龙胆水煎液(4 000 mg.kg-1)后分别于各个时间点监测直肠温度,比较三者作用的差异性;采用放射免疫法测定大鼠血清肿瘤坏死因子-α(TNF-α)、白介素-1(IL-1)、白介素-6(IL-6)及下丘脑内环磷酸腺苷(cAMP)、前列腺素E2(PGE2)含量。结果:龙胆碱、龙胆苦苷、龙胆水提液,均能降低发热模型大鼠体温,三者对体温指数(TRI9)的影响分别为:0.86±0.32,1.56±0.27,1.47±0.31,与模型组比较,其差异具有显著性(P≤0.05);放射免疫结果显示,给药组IL-6,PGE2含量分别为(42.46±3.84),(103.30±7.38)ng.L-1,含量明显低于模型组,其差异具有显著性(P<0.05)。结论:龙胆碱、龙胆苦苷及龙胆水提液均具有一定的解热作用,但龙胆碱的解热作用强于后者,龙胆碱可能是中药龙胆解热作用的更直接物质;龙胆碱的解热作用机制可能与降低血清中IL-6水平,进而影响下丘脑PGE2含量有关。

Objective： To study the antipyretic effect and the mechanism of gentianine by comparing with variances of the antipyretic effect among from water extract of Gentianae Radix Et Rhizoma,gentianine and gentiopcroside.Method： The rat febrile models induced by injecting fresh yeast subcutaneously and treated with gentianine,gentiopcroside intraperitoneally and fed with water extract of Gentianae Radix Et Rhizoma,then the rectal temperature was monitored to show the differences of effect from those groups.The contents of tumor necrosis factor（TNF-α）,interleukin-1（IL-1）,interleukin-6（IL-6） in blood serum and cyclic adenosine monophosphate（cAMP）,prostaglandin E2（PGE2） in the hypothalamus were measured by radioimmunoassav（RIA）,respectively.Result： Three drug administration groups（including gentianine,gentiopcroside and water extract of Gentianae Radix Et Rhizoma）showed marked antipyretic effect on the yeast-induced fever（P0.05） and the effects were stronger on the getianine group than other treated groups.Each treatment group showed remarkable decreased the contents of IL-6 in blood serum and PGE2 in the hypothalamus of febrile rats.Conclusion： Gentianine,gentiopcroside and water extract of Gentianae Radix Et Rhizoma all have obvious antipyretic effect,but the effect of gentianine is strongest of them and probably plays a more direct role in the antipyretic effect from Gentianae Radix Et Rhizoma,which might be related with decreasing the levels of IL-6 in serum and the interferencing the content of PGE2 in the hypothalamus.