Key Laboratory of Quality Evaluation of Chinese Medicine of the Guangdong Provincial Medical Products Administration, The Second Clinical College, Guangzhou University of Chinese Medicine, Guangzhou, China.
Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome, Guangdong Provincial Hospital of Chinese Medicine, Guangzhou, China.
Biomed Chromatogr. 2022 Dec;36(12):e5493. doi: 10.1002/bmc.5493. Epub 2022 Sep 12.
Ginsenosides have poor oral bioavailability and undergo rapid biological transformation in the complex gastrointestinal environment. Most studies on the metabolism of ginsenosides have focused on gut bacteria, yet gastric juice remains a nonnegligible factor. Metabolic profiles of ginsenoside monomers formed in artificial gastric juice were separately investigated and qualitatively identified using ultra-high-pressure liquid chromatography coupled with linear ion trap-Orbitrap mass spectrometry (UHPLC-LTQ-Orbitrap MS ). A common pattern of their metabolic pathways was established, showing that ginsenosides were transformed via deglycosylation, hydration, and dehydration pathways. Two major structure types, 20(S), 20(R)-protopanaxatriols and 20(S), 20(R)-protopanaxadiols, basically shared similar transformation pathways and yielded deglycosylated, hydrated, and dehydrated products. Fragmentation patterns of major ginsenosides were also discussed. Consequently, gastric juice, as the primary link in ginsenoside metabolism and as important as the intestinal flora, produces considerable amounts of degraded ginsenosides, providing a partial explanation for the low bioavailabilities of primary ginsenosides.
人参皂苷的口服生物利用度较差，在复杂的胃肠道环境中会迅速发生生物转化。大多数关于人参皂苷代谢的研究都集中在肠道细菌上，但胃液仍然是一个不可忽视的因素。使用超高效液相色谱-线性离子阱轨道阱质谱联用技术（UHPLC-LTQ-Orbitrap MS）分别研究了人工胃液中形成的人参皂苷单体的代谢谱，并进行了定性鉴定。建立了它们的代谢途径的共同模式，表明人参皂苷通过去糖基化、水合和脱水途径转化。两种主要结构类型，20（S），20（R）-原人参三醇和 20（S），20（R）-原人参二醇，基本上都具有相似的转化途径，生成去糖基化、水合和脱水产物。主要人参皂苷的裂解模式也进行了讨论。因此，胃液作为人参皂苷代谢的主要环节，与肠道菌群同样重要，会产生大量降解的人参皂苷，这部分解释了原人参皂苷生物利用度低的原因。
