Takino Y
School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Yakugaku Zasshi. 1994 Aug;114(8):550-64.
The pharmacodynamics of ginsenoside-Rg1 (Rg1), -Rb1 (Rb1) and -Rb2 (Rb2) in rats were studied. In these studies, obvious differences were found in their pharmacodynamics. That is, Rg1 was easily hydrated to the same prospogenins in both rat stomach and 0.1 N HCl solution, but Rb1 and Rb2 were little decomposed (metabolised) in rat stomach and a small quantity of their hydroperoxide derivatives were found, but they were easily hydrated to their prosapogenins by 0.1 N HCl. These ginsenosides were decomposed (metabolised) to several prosapogenins by enteric bacteria and enteric enzymes. The modes of their decomposition (metabolism) were respectively different. In particular, the terminal sugar moiety at the C-20 hydroxy group was noted to affect the rates of their decomposition. The amount of Rg1 and Rb1 absorbed from the gastrointestinal tract of rat were 1.9% and 0.1% of the dose, respectively. And that of Rb2 was determined to be 3.7% of the dose by using 3H-labeled Rb2. Rg1 was excreted into the urine and bile in a 2:5 ratio. Rb1 and Rb2 were mainly excreted into the urine.
研究了人参皂苷-Rg1(Rg1)、-Rb1(Rb1)和-Rb2(Rb2)在大鼠体内的药效学。在这些研究中,发现它们的药效学存在明显差异。也就是说,Rg1在大鼠胃和0.1N盐酸溶液中都很容易水合为相同的原皂苷元,但Rb1和Rb2在大鼠胃中几乎不分解(代谢),仅发现少量的氢过氧化物衍生物,而它们在0.1N盐酸中很容易水合为原皂苷元。这些人参皂苷被肠道细菌和肠道酶分解(代谢)为几种原皂苷元。它们的分解(代谢)方式各不相同。特别值得注意的是,C-20羟基处的末端糖部分会影响它们的分解速率。大鼠胃肠道吸收的Rg1和Rb1的量分别为给药剂量的1.9%和0.1%。通过使用3H标记的Rb2测定,Rb2的吸收量为给药剂量的3.7%。Rg1以2:5的比例排泄到尿液和胆汁中。Rb1和Rb2主要排泄到尿液中。