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为研究生姜中有效部位(ginger ether extract,GEE)及其中生理活性成分的止呕作用,该研究在整体动物模型水平,大鼠、小鼠分别腹腔注射顺铂,建立大鼠异食癖呕吐模型和小鼠胃排空模型。观察GEE预防给药对顺铂所致大鼠异食癖及小鼠胃排空的止呕作用,并用RP-HPLC检测分析GEE中主要成分;在离体水平,观察GEE及其主要成分对5-HT3受体激动剂SR57227A和M3胆碱受体激动剂卡巴胆碱(carbachol)引起的离体豚鼠回肠收缩的影响。结果显示GEE(25,50,100 mg·kg-1)3个剂量组均可显著减少大鼠摄食高岭土的量(P<0.01),同时GEE(50,100,200mg·kg-1)3个剂量组均能显著对抗顺铂所致的小鼠胃排空抑制(P<0.01);RP-HPLC检测结果表明,GEE中主要含有4种姜辣素类成分,分别为6-gingerol,8-gingerol,6-shogaol,10-gingerol;在5-HT3受体激动剂SR57227A浓度为1×10-5mol·L-1和M3胆碱受体激动剂carbachol浓度为10-4mol·L-1时,分别加入GEE(2.3,4.6,11.5 mg·L-1),6-gingerol,8-gingerol,6-shogaol,10-gingerol(1,2,5μmol·L-1)均可降低离体豚鼠回肠的最大收缩张力(P<0.05,P<0.01)。由此可知,生姜中的有效部位GEE及其中的主要成分6-gingerol,8-gingerol,6-shogaol,10-gingerol产生止呕作用的机制可能与其拮抗5-HT_3和M_3胆碱受体有关。
To study the antiemetic effects of ginger ether extract (GEE) and its physiologically active components in rats, the rats were injected intraperitoneally with cisplatin at the level of the whole animal model to establish a rat model of pica vomiting And mouse gastric emptying model. To observe the preventive effect of GEE on cisplatin-induced vomiting in rats and gastric emptying in mice. The main constituents of GEE were detected by RP-HPLC. At the level of exogenous GEE, -HT3 receptor agonist SR57227A and carbachol-induced withdrawal of guinea pig ileum. The results showed that all three doses of GEE (25, 50, 100 mg · kg-1) could significantly reduce the amount of kaolin in rats (P <0.01) (P <0.01). The results of RP-HPLC showed that GEE mainly contains four kinds of gingerol components, namely 6-gingerol, 8-gingerol and 6-shogaol , 10-gingerol. When the concentrations of SR-5 receptor agonist SR57227A were 1 × 10-5mol·L-1 and the concentration of carbachol was 10-4mol·L-1, GEE (2.3 , 4.6, 11.5 mg · L-1), 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol (1,2,5 μmol·L-1) all decreased the maximum contractile tension of guinea pig ileum <0.05, P <0.01). It can be seen that the mechanism of antiemetic effect of GEE, which is the active site in ginger, and the main components of 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol may be related to the antagonism of 5-HT_3 and M_3 cholinergic receptors.