Kido Toshitaka, Nakai Yoichiro, Kase Yoshio, Sakakibara Iwao, Nomura Masaaki, Takeda Shuichi, Aburada Masaki
Department of Medicinal Informatics, Graduate School of Medicine, Kanazawa University, Japan.
J Pharmacol Sci. 2005 Jun;98(2):161-7. doi: 10.1254/jphs.fpj04056x. Epub 2005 Jun 4.
We evaluated the effects of Rikkunshi-to and several of its ingredients on the delay of gastric emptying induced by a nitric oxide (NO) synthase inhibitor, N(G)-nitro-L-arginine (L-NNA). After oral administration of L-NNA to rats, the gastric emptying rate at 24 h was decreased from 82.8 +/- 2.4% to 53.3 +/- 5.7%. The decrease of the gastric emptying rate induced by L-NNA treatment was markedly ameliorated by administration of Rikkunshi-to (250 and 500 mg/kg, p.o.) in a dose-dependent manner. To identify the active ingredient of Rikkunshi-to, the components were separated according to polarity, and the effects of the respective fractions on gastric emptying were evaluated. Significant efficacy was found in the water and methanol fractions, but not in the 50% aqueous-methanol fraction. Furthermore, hesperidin (1 - 4.29 mg/kg, p.o.) contained in the methanol fraction and L-arginine (4.5 mg/kg, p.o.) contained in the water fraction ameliorated the decrease in the gastric emptying rate induced by L-NNA treatment. These results suggest that Rikkunshi-to ameliorated abnormalities of NO-mediated gastric functions such as delayed gastric emptying, and hesperidin and L-arginine were identified as two of the active ingredients contributing to the ability of Rikkunshi-to to facilitate gastric emptying.
我们评估了六君子汤及其几种成分对一氧化氮(NO)合酶抑制剂N(G)-硝基-L-精氨酸(L-NNA)诱导的胃排空延迟的影响。给大鼠口服L-NNA后,24小时的胃排空率从82.8±2.4%降至53.3±5.7%。通过口服给予六君子汤(250和500mg/kg),L-NNA治疗引起的胃排空率下降以剂量依赖性方式得到显著改善。为了确定六君子汤的活性成分,根据极性对其成分进行分离,并评估各个组分对胃排空的影响。在水相和甲醇相组分中发现了显著疗效,但在50%水-甲醇相组分中未发现。此外,甲醇相组分中含有的橙皮苷(1-4.29mg/kg,口服)和水相组分中含有的L-精氨酸(4.5mg/kg,口服)改善了L-NNA治疗引起的胃排空率下降。这些结果表明,六君子汤改善了NO介导的胃功能异常,如胃排空延迟,并且橙皮苷和L-精氨酸被确定为有助于六君子汤促进胃排空能力的两种活性成分。