柴胡皂苷是柴胡中具有生物活性的一类五环三萜类齐墩果烷型衍生物，但因其口服时胃肠道的吸收能力差，生物利用度极低。主要通过对柴胡皂苷类化合物代谢途径及其相关代谢产物进行综述，探讨柴胡皂苷类化合物生物利用度低的原因，并提出柴胡皂苷类化合物发挥药理活性的物质基础可能与其胃肠道转化和催化氧化过程产生的皂苷元结构有关。因此对柴胡皂苷类化合物代谢途径的相关研究，尤其是胃肠道菌群对其的代谢作用研究，能够为临床应用提供更为关键的基础性数据，也具有更为重要的研究价值。

Saikosaponin is a kind of pentacyclic triterpenes oleanolic derivatives with biological activity in Bupleurum chinense. However, saikosaponin has very low bioavailability because of its poor absorption ability and unstable structure when taken orally. The metabolic pathways in vivo and their the metabolic pathways and related metabolites of saikosaponin are reviewed to make clear the reason of low bioavailability. And it was inferred that the material basis of the pharmacological activity of saikosaponin might be related to the structure of saponins generated through gastrointestinal transformation and catalytic oxidation. Therefore, relevant studies on the metabolic pathways of saponin, especially the study on the metabolic effects of gastrointestinal flora, can provide more critical basic data for clinical application and have more important research value.