Kim Kyung-Ah, Yoo Hye Hyun, Gu Wan, Yu Dae-Hyung, Jin Ming Ji, Choi Hae-Lim, Yuan Kathy, Guerin-Deremaux Laetitia, Kim Dong-Hyun
Department of Pharmacy, College of Pharmacy, Kyung Hee University, Dongdaemun-gu, Seoul 130-701, Korea ; Department of Food Science and Nutrition, College of Natural Science, Songwon University, 73, Songamro, Nam-gu, Gwangju 503-742, Korea.
Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 426-791, Korea.
J Ginseng Res. 2015 Apr;39(2):183-7. doi: 10.1016/j.jgr.2014.11.002. Epub 2014 Nov 24.
Gut microflora play a crucial role in the biotransformation of ginsenosides to compound K (CK), which may affect the pharmacological effects of ginseng. Prebiotics, such as NUTRIOSE, could enhance the formation and consequent absorption of CK through the modulation of gut microbial metabolic activities. In this study, the effect of a prebiotic fiber (NUTRIOSE) on the pharmacokinetics of ginsenoside CK, a bioactive metabolite of ginsenosides, and its mechanism of action were investigated.
Male Sprague-Dawley rats were given control or NUTRIOSE-containing diets (control diet + NUTRIOSE) for 2 wk, and ginseng extract or vehicle was then orally administered. Blood samples were collected to investigate the pharmacokinetics of CK using liquid chromatography-tandem mass spectrometry. Fecal activities that metabolize ginsenoside Rb1 to CK were assayed with fecal specimens or bacteria cultures.
When ginseng extract was orally administered to rats fed with 2.5%, 5%, or 10% NUTRIOSE containing diets, the maximum plasma concentration (C max) and area under the plasma concentration-time curve values of CK significantly increased in a NUTRIOSE content-dependent manner. NUTRIOSE intake increased glycosidase activity and CK formation in rat intestinal contents. The CK-forming activities of intestinal microbiota cultured in vitro were significantly induced by NUTRIOSE.
These results show that prebiotic diets, such as NUTRIOSE, may promote the metabolic conversion of ginsenosides to CK and the subsequent absorption of CK in the gastrointestinal tract and may potentiate the pharmacological effects of ginseng.
肠道微生物群在人参皂苷向化合物K(CK)的生物转化中起关键作用,这可能会影响人参的药理作用。益生元,如NUTRIOSE,可通过调节肠道微生物代谢活性来增强CK的形成及后续吸收。在本研究中,研究了一种益生元纤维(NUTRIOSE)对人参皂苷生物活性代谢产物CK的药代动力学及其作用机制的影响。
将雄性Sprague-Dawley大鼠给予对照或含NUTRIOSE的饮食(对照饮食 + NUTRIOSE)2周,然后口服人参提取物或赋形剂。采集血样,采用液相色谱-串联质谱法研究CK的药代动力学。用粪便标本或细菌培养物检测将人参皂苷Rb1代谢为CK的粪便活性。
当给喂食含2.5%、5%或10% NUTRIOSE饮食的大鼠口服人参提取物时,CK的最大血浆浓度(Cmax)和血浆浓度-时间曲线下面积值以NUTRIOSE含量依赖的方式显著增加。摄入NUTRIOSE可增加大鼠肠内容物中的糖苷酶活性和CK形成。NUTRIOSE显著诱导体外培养的肠道微生物群的CK形成活性。
这些结果表明,益生元饮食,如NUTRIOSE,可能促进人参皂苷在胃肠道中向CK的代谢转化以及CK的后续吸收,并可能增强人参的药理作用。