Center of Drug Absorption and Transport, Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, Germany.
Pharmazie. 2024 Aug 1;79(7):151-158. doi: 10.1691/ph.2024.4014.
Substances metabolised by the intestinal microbiota can be used as colon markers and are gaining importance. The flavonoid glycoside baicalin has been described in the literature to be metabolised by the intestinal microbiota. The aim of this work was to investigate how the biotransformation of baicalin to baicalein is related to the intestinal microbiota. For this purpose, stool samples from healthy volunteers with different dietary habits were used. From the pre-cultured stool samples, different standard microbiota were obtained which were used for the subsequent metabolism studies in the model MimiCol. MimiCol represents the ascending section of the colon, the , in terms of available volume, pH-value, redox potential and bacterial abundance. While during the experiments with added standard microbiota a metabolism of baicalin to baicalein could be detected, this was not the case in a series of experiments without added microbiota. This confirmed the hypothesis that the metabolism of baicalin relies on the bacterial species that are present in the colon. The data collected in the MimiCol therefore support the use of baicalin as a potential marker for the determination of the colon arrival. This can be explained by the fact that baicalin in its native form is poorly absorbed from the gastrointestinal tract. Enzymes of the colonic microbiota, namely β-glucuronidases, hydrolyze baicalin to the aglycone baicalein. The resulting aglycone can be absorbed through the intestinal mucosa and detected in blood plasma. This potentially enables the use of baicalin as a marker to determine the time of arrival in the colon.
肠道微生物群代谢的物质可用作结肠标志物,其重要性日益增加。文献中描述了黄酮糖苷黄芩苷被肠道微生物群代谢。本工作旨在研究黄芩苷生物转化为黄芩素与肠道微生物群的关系。为此,使用了具有不同饮食习惯的健康志愿者的粪便样本。从预培养的粪便样本中获得了不同的标准微生物群,用于随后在模型 MimiCol 中的代谢研究。MimiCol 代表结肠的升结肠部分,在可用体积、pH 值、氧化还原电位和细菌丰度方面。虽然在添加标准微生物群的实验中可以检测到黄芩苷向黄芩素的代谢,但在没有添加微生物群的一系列实验中则不然。这证实了黄芩苷代谢依赖于结肠中存在的细菌种类的假设。因此,MimiCol 中收集的数据支持将黄芩苷用作确定结肠到达的潜在标志物。这可以解释为黄芩苷在其天然形式下从胃肠道吸收不良。结肠微生物群的酶,即β-葡萄糖醛酸酶,将黄芩苷水解为苷元黄芩素。生成的苷元可以通过肠黏膜吸收并在血浆中检测到。这可能使黄芩苷能够用作标记物来确定在结肠中的到达时间。