Transformation of Psoralen and Isopsoralen by Human Intestinal Microbial In Vitro, and the Biological Activities of Its Metabolites
Transformation of Psoralen and Isopsoralen by Human Intestinal Microbial In Vitro, and the Biological Activities of Its Metabolites
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人肠道微生物对补骨脂素和异补骨脂素的体外转化及其代谢产物的生物活性
DOI：
10.3390/molecules24224080
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发表时间：
2019-11-01
期刊：
影响因子：
4.6
通讯作者：
Yang, Xiu-Wei
中科院分区：
文献类型：
--
作者：
Liu, Lu;Zhang, Lei;Yang, Xiu-Wei
补骨脂素（P）和异补骨脂素（IP）是补骨脂干果中的主要活性成分。(PC)，具有广泛的药理学活动。肠道细菌的生物转化在中药复杂成分的代谢过程中起着核心作用。我们的研究目的是调查在肠道条件下，与人粪便细菌厌氧共培养的P和IP的代谢谱。结果表明，该菌株可转化6，7-呋喃基羟基香豆酸（P-1）和6，7-呋喃基羟基香豆酸甲酯（P-2），以及5，6-呋喃基羟基香豆酸（IP-1）和5，6-呋喃基羟基香豆酸甲酯（IP-2）。值得一提的是，IP-2是一种尚未发表的新化合物。根据光谱数据分析了它们的结构。此外，一个高灵敏度的超高效液相色谱串联质谱（UPLC-MS/MS）方法被用来表征的代谢途径的P，IP，和它们的生物转化产物的反应样品。此外，通过人结肠直肠细胞（HCT 116）和异质性人上皮结肠直肠腺癌细胞（Caco-2）细胞系，体外评估人肠道植物群对P、IP及其生物转化产物的氧化应激的抑制作用。结果表明，代谢产物的活性强于P和IP，这可能为阐明PC提取物抗炎症性肠病的作用机制提供了依据。
Psoralen (P) and isopsoralen (IP) are the main active ingredients in the dried fruit of Psoralen corylifolia L. (PC), with a wide range of pharmacology activities. The intestinal bacteria biotransformation plays a central role in the metabolism of the complex ingredients in traditional Chinese medicine (TCM). Our study aimed to investigated the metabolic profile of P and IP in the intestinal condition, co-cultured with human fecal bacteria anaerobically. Four bio-transforming products were obtained, including 6,7-furano-hydrocoumaric acid (P-1) and 6,7-furano-hydro- coumaric acid methyl ester (P-2), which transformed from P, and 5,6-furano-hydrocoumaric acid (IP-1) and 5,6-furano-hydrocoumaric acid methyl ester (IP-2), which were transformed from IP. It is worth mentioning that IP-2 is a new compound that has not been published. Their structures were analyzed based on their spectroscopic data. Moreover, a highly sensitive ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was used to characterize the metabolic pathways of P, IP, and their bio-transforming products in the reaction samples. In addition, the dampening effects against the oxidative stress of P, IP, and their bio-transforming products by human intestinal flora were estimated in vitro via the human colorectal cells (HCT116) and heterogeneous human epithelial colorectal adenocarcinoma cells (Caco-2) cell lines. The results showed that the metabolites have stronger activity than P and IP, which possibly provides a basis for elucidating the treating mechanisms of PC extract against inflammatory bowel disease.