School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 102488, China.
School of Life Sciences, Beijing University of Chinese Medicine, Beijing 102488, China.
J Pharm Biomed Anal. 2022 Sep 20;219:114906. doi: 10.1016/j.jpba.2022.114906. Epub 2022 Jun 23.
Lonicera japonica Flos (LJF) is taken orally as a health food and medicinal plant in China for a long time. The gastrointestinal metabolism of LJF was investigated in vitro by three independent models (gastric juice, intestinal juice, and human intestinal bacteria), qualitative analyzed by UPLC-LTQ-Orbitrap-MS and quantified by HPLC-DAD. 72 prototype compounds were detected in LJF water extraction (LJF-WE), including 14 organic acids, 43 iridoids, 14 flavonoids and one other compound. The prototype and metabolic components of LJF-WE bio-transformed by simulated gastric fluid (70 and 12), intestinal fluid (69 and 12) and human fecal bacteria (29 and 70) were characterized, respectively. The metabolites were formed through desaccharization, isomerization, hydrogenation, methylation, dehydration, and then cyclization, glucuronization and dimethylation followed. 8 bioactive compounds including neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, sweroside, secoxyloganin, isochlorogenic acid B, isochlorogenic acid A and isochlorogenic acid C were much stable in simulated gastric fluid and intestinal fluid, compared with human fecal bacteria. Especially, sweroside and secoxyloganin with glucoside bonds degradated extraordinarily fast, because of the abundant β-glucosidases in human fecal bacteria.
忍冬花（LJF）在中国长期以来一直被作为一种保健食品和药用植物口服使用。本研究采用三种独立模型（胃液、肠液和人肠菌）体外研究了忍冬花的胃肠道代谢情况，通过 UPLC-LTQ-Orbitrap-MS 进行定性分析，通过 HPLC-DAD 进行定量分析。在忍冬花水提物（LJF-WE）中检测到 72 种原型化合物，包括 14 种有机酸、43 种环烯醚萜、14 种黄酮类化合物和 1 种其他化合物。模拟胃液（70 种和 12 种）、肠液（69 种和 12 种）和人粪便细菌（29 种和 70 种）转化的忍冬花-WE 的原型和代谢成分分别进行了特征描述。这些代谢物通过去糖基化、异构化、加氢、甲基化、脱水、然后环化、葡萄糖醛酸化和二甲化形成。8 种生物活性化合物，包括新绿原酸、绿原酸、隐绿原酸、蝶芪、木樨草苷、异绿原酸 B、异绿原酸 A 和异绿原酸 C，在模拟胃液和肠液中比人粪便细菌更稳定。特别是，由于人粪便细菌中含有丰富的β-葡萄糖苷酶，蝶芪和木樨草苷糖苷键降解速度非常快。
