生姜中有效部位及相关活性成分的止呕作用研究

Antiemetic activity of effective extract and bioactive compounds in ginger

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 investigate the antiemetic effect of the active extract（ ginger ether extract,GEE） and its bioactive compounds in ginger,the pica vomiting model in rats and the gastric emptying model in mice were used to observe the antiemetic effect of GEE in cisplatin-induced pica and gastric emptying,and the main components in GEE were detected by RP-HPLC; in vitro,the antagonist effect of GEE and the four components in it were explored by the contraction of guinea-pig ileum induced by SR57227 A and carbachol. The results showed that the amount of Kaolin ingested by rats were declined significantly in all the three groups of GEE（ 25,50,100 mg·kg^（-1））（ P〈0. 01）,while cisplatin-induced gastric emptying in mice was also suppressed in all the three groups（ P〈0. 01）,and6-gingerol,8-gingerol,10-gingerol and 6-shogaol were found mainly in GEE by RP-HPLC; the maximum contraction of isolated guineapig ileum could be reduced by addition of GEE（ 2. 3,4. 6,11. 5 mg·L^（-1））,6-gingerol,8-gingerol,10-gingerol or 6-shogaol（ 1,2,5μmol·L^（-1）） when the concentration of SR5727 A was 1 × 10-5mol·L^（-1）and that of carbachol was 1 × 10-4mol·L^（-1）（ P〈0. 05,P〈0. 01）. In conclusion,5-HT_3 and M_3 receptors could be antagonized by GEE and its bioactive compounds 6-gingerol,8-gingerol,10-gingerol and 6-shogaol,which may be correlated with the antiemetic mechanism of ginger maybe related to it.