Hu Xu-Xin, Liu Xiao, Chu Yu, Chen Wen-Xing, Zhang Ke-Wei, Wu Hao
College of Pharmacology, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Zhongguo Zhong Yao Za Zhi. 2016 Mar;41(5):904-909. doi: 10.4268/cjcmm20160524.
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 SR57227A 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), and 6-gingerol, 8-gingerol,10-gingerol and 6-shogaol were found mainly in GEE by RP-HPLC; the maximum contraction of isolated guinea-pig 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, 5 μmol•L⁻¹) when the concentration of SR5727A was 1×10⁻⁵ mol•L⁻¹ and that of carbachol was 1×10⁻⁴ mol•L⁻¹ (P<0.05, P<0.01). In conclusion, 5-HT3 and M3 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.
为研究生姜中活性提取物(姜醚提取物,GEE)及其生物活性成分的止吐作用,采用大鼠异食癖呕吐模型和小鼠胃排空模型,观察GEE对顺铂诱导的异食癖和胃排空的止吐作用,并用反相高效液相色谱法(RP-HPLC)检测GEE中的主要成分;体外实验通过观察SR57227A和卡巴胆碱诱导的豚鼠回肠收缩,探究GEE及其四种成分的拮抗作用。结果显示,GEE三个剂量组(25、50、100 mg•kg⁻¹)大鼠高岭土摄入量均显著下降(P<0.01),同时三个剂量组对顺铂诱导的小鼠胃排空均有抑制作用(P<0.01),RP-HPLC检测发现GEE中主要含有6-姜酚、8-姜酚、10-姜酚和6-姜烯酚;当SR5727A浓度为1×10⁻⁵ mol•L⁻¹、卡巴胆碱浓度为1×10⁻⁴ mol•L⁻¹时,加入GEE(2.3、4.6、11.5 mg•L⁻¹)、6-姜酚、8-姜酚、10-姜酚或6-姜烯酚(1、2、5 μmol•L⁻¹)均可使离体豚鼠回肠的最大收缩幅度降低(P<0.05,P<0.01)。综上所述,GEE及其生物活性成分6-姜酚、8-姜酚、10-姜酚和6-姜烯酚可拮抗5-HT3和M3受体,这可能与生姜的止吐机制相关。