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Effect of Lactic Acid Bacteria on the Pharmacokinetics and Metabolism of Ginsenosides in Mice
Pharmaceutics ( IF 4.9 ) Pub Date : 2021-09-17 , DOI: 10.3390/pharmaceutics13091496
Ji-Hyeon Jeon 1 , Jaehyeok Lee 1 , Jin-Hyang Park 1 , Chul-Haeng Lee 2 , Min-Koo Choi 2 , Im-Sook Song 1
Affiliation  

This study aims to investigate the effect of lactic acid bacteria (LAB) on in vitro and in vivo metabolism and the pharmacokinetics of ginsenosides in mice. When the in vitro fermentation test of RGE with LAB was carried out, protopanaxadiol (PPD) and protopanaxadiol (PPD), which are final metabolites of ginsenosides but not contained in RGE, were greatly increased. Compound K (CK), ginsenoside Rh1 (GRh1), and GRg3 also increased by about 30%. Other ginsenosides with a sugar number of more than 2 showed a gradual decrease by fermentation with LAB for 7 days, suggesting the involvement of LAB in the deglycosylation of ginsenosides. Incubation of single ginsenoside with LAB produced GRg3, CK, and PPD with the highest formation rate and GRd, GRh2, and GF with the lower rate among PPD-type ginsenosides. Among PPT-type ginsenosides, GRh1 and PPT had the highest formation rate. The amoxicillin pretreatment (20 mg/kg/day, twice a day for 3 days) resulted in a significant decrease in the fecal recovery of CK, PPD, and PPT through the blockade of deglycosylation of ginsenosides after single oral administrations of RGE (2 g/kg) in mice. The plasma concentrations of CK, PPD, and PPT were not detectable without change in GRb1, GRb2, and GRc in this group. LAB supplementation (1 billion CFU/2 g/kg/day for 1 week) after the amoxicillin treatment in mice restored the ginsenoside metabolism and the plasma concentrations of ginsenosides to the control level. In conclusion, the alterations in the gut microbiota environment could change the ginsenoside metabolism and plasma concentrations of ginsenosides. Therefore, the supplementation of LAB with oral administrations of RGE would help increase plasma concentrations of deglycosylated ginsenosides such as CK, PPD, and PPT.

中文翻译:


乳酸菌对小鼠体内人参皂苷药代动力学和代谢的影响



本研究旨在探讨乳酸菌(LAB)对小鼠体外和体内代谢的影响以及人参皂苷的药代动力学。当进行RGE与LAB的体外发酵试验时,RGE中不含有的人参皂苷最终代谢产物原人参二醇(PPD)和原人参二醇(PPD)大大增加。化合物K(CK)、人参皂苷Rh1(GRh1)和GRg3也增加了约30%。其他糖数超过 2 的人参皂苷在 LAB 发酵 7 天后逐渐减少,表明 LAB 参与了人参皂苷的去糖基化。单一人参皂苷与 LAB 一起孵育,在 PPD 型人参皂苷中产生了形成率最高的 GRg3、CK 和 PPD,以及形成率较低的 GRd、GRh2 和 GF。 PPT型人参皂苷中,GRh1和PPT的形成率最高。阿莫西林预处理(20 mg/kg/天,每天两次,持续 3 天)通过单次口服 RGE(2 g)后阻断人参皂苷的去糖基化,导致 CK、PPD 和 PPT 粪便回收率显着下降/kg)在小鼠中。在该组中,在GRb1、GRb2和GRc没有变化的情况下,检测不到CK、PPD和PPT的血浆浓度。小鼠接受阿莫西林治疗后补充 LAB(10 亿 CFU/2 g/kg/天,持续 1 周)可将人参皂苷代谢和人参皂苷血浆浓度恢复至对照水平。总之,肠道微生物环境的改变可能会改变人参皂苷的代谢和人参皂苷的血浆浓度。因此,口服 RGE 补充 LAB 将有助于增加去糖基化人参皂苷(如 CK、PPD 和 PPT)的血浆浓度。
更新日期:2021-09-17
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