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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 compare the antipyretic effects of gentian extract, gentianine and gentiopicroside, and to explore the mechanism of gentianin’s antipyretic effect. Methods: Male Sprague-Dawley rats were randomly divided into blank control group, fever model group, gentianin group, gentiopicroside group and gentian water extract group. Subcutaneous injection of dry yeast was used to prepare fever model. Six hours after the preparation, ip gentian solution (100 mg.kg-1), gentiopicroside solution (200 mg.kg-1) and ig gentian decoction (4 000 mg.kg-1) The rectal temperature was monitored at various time points to compare the difference of the three effects. The levels of tumor necrosis factor-α (TNF-α), interleukin-1 (IL-1), interleukin- -6), and cAMP and prostaglandin E2 (PGE2) levels in the hypothalamus. Results: Longchine, gentiopicroside and gentian extract all decreased the body temperature of rats with fever, the effects of three on the body temperature index (TRI9) were 0.86 ± 0.32, 1.56 ± 0.27 and 1.47 ± 0.31 (P <0.05). The results of radioimmunoassay showed that the levels of IL-6 and PGE2 in the treatment group were (42.46 ± 3.84) and (103.30 ± 7.38) ng.L-1, Content was significantly lower than the model group, the difference was significant (P <0.05). CONCLUSION: The extracts of gentian, gentiopicroside and gentian have certain antipyretic effect, but the antipyretic effect of gentian is stronger than that of gentian, gentian may be the antipyretic effect of gentian Direct substance; gentianine antipyretic mechanism may be related to lower serum IL-6 levels, thereby affecting the content of hypothalamic PGE2.