Transport and metabolic profiling studies of amentoflavone in Caco-2 cells by UHPLC-ESI-MS/MS and UHPLC-ESI-Q-TOF-MS/MS
Transport and metabolic profiling studies of amentoflavone in Caco-2 cells by UHPLC-ESI-MS/MS and UHPLC-ESI-Q-TOF-MS/MS
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DOI：
10.1016/j.jpba.2020.113441
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发表时间：
2020-09-10
影响因子：
3.4
通讯作者：
Wang, Hao
中科院分区：
文献类型：
--
作者：
Wang, Baolin;Lu, Yimeng;Wang, Hao
Amentoflavone是一种双黄酮类化合物，存在于卷柏、银杏等多种药用植物中，具有抗炎、抗氧化、抗病毒、抗肿瘤等活性。本研究开发了一种新的可靠且灵敏的UHPLC-ESI-MS/MS方法来测定不同条件下穗花果黄酮的渗透性，并通过UHPLC-Q-TOF-MS/MS方法鉴定了其在Caco-2细胞中的代谢物。结果表明，在Caco-2细胞模型中，穗花黄酮可以被认为是一种具有中等肠道吸收的化合物，其吸收特性可能涉及细胞旁被动渗透和网格蛋白介导的内吞作用，而没有外排转运蛋白的参与。在Caco-2细胞模型中鉴定出穗花果黄酮的8种代谢物，表明其主要代谢途径是氧化、还原、甲基化和葡萄糖醛酸结合。该研究可为深入了解穗花黄酮在肠道的吸收机制和转化提供有价值的证据。 (C) 2020 Elsevier B.V. 保留所有权利。
Amentoflavone, a kind of biflavonoid existing in several medicinal plants such as Selaginella moellendorfi and Gingko biloba, possesses anti-inflammatory, antioxidant, anti-virus, anti-tumor activities. In the present study, a new reliable and sensitive UHPLC-ESI-MS/MS method was developed to determine the permeability of amentoflavone under different conditions, and its metabolites in Caco-2 cells were identified by means of UHPLC-Q-TOF-MS/MS method. The results showed that amentoflavone could be considered as a compound with moderate intestinal absorption in Caco-2 cell model and its absorption characteristics might be involved in paracellular passive penetration and clathrin-mediated endocytosis with no participation of efflux transporters. Eight metabolites of amentoflavone were identified in Caco-2 cell model, indicating that the main metabolic pathways were oxidation, reduction, methylation and glucuronide conjugation. This study can provide valuable evidence for an in-depth understanding of absorption mechanism and transformation of amentoflavone in the intestine. (C) 2020 Elsevier B.V. All rights reserved.