State Key Laboratory of Natural Medicines, Department of TCM Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China; Nanchang Key Laboratory of Quality Control and Safety Evaluation of TCM, Nanchang Institute for Food and Drug Control, Nanchang 330012, People's Republic of China.
State Key Laboratory of Natural Medicines, Department of TCM Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
J Pharm Biomed Anal. 2020 Sep 10;189:113441. doi: 10.1016/j.jpba.2020.113441. Epub 2020 Jun 24.
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.
穗花杉双黄酮是一种存在于卷柏和银杏等几种药用植物中的双黄酮类化合物，具有抗炎、抗氧化、抗病毒、抗肿瘤等活性。本研究建立了一种新的可靠、灵敏的 UHPLC-ESI-MS/MS 方法，用于测定不同条件下穗花杉双黄酮的渗透性，并采用 UHPLC-Q-TOF-MS/MS 方法鉴定其在 Caco-2 细胞中的代谢物。结果表明，穗花杉双黄酮可被认为是一种在 Caco-2 细胞模型中具有中等肠道吸收特性的化合物，其吸收特征可能涉及细胞旁被动渗透和网格蛋白介导的内吞作用，而不涉及外排转运体。在 Caco-2 细胞模型中鉴定出穗花杉双黄酮的 8 种代谢物，表明其主要代谢途径为氧化、还原、甲基化和葡萄糖醛酸缀合。本研究可为深入了解穗花杉双黄酮在肠道中的吸收机制和转化提供有价值的证据。
