Transport and metabolic profiling studies of amentoflavone in Caco-2 cells by UHPLC-ESI-MS/MS and UHPLC-ESI-Q-TOF-MS/MS

  • J Pharm Biomed Anal. 2020 Sep 10;189:113441. doi: 10.1016/j.jpba.2020.113441.
Baolin Wang  1 ,  Yimeng Lu  2 ,  Rong Wang  2 ,  Shumeng Liu  2 ,  Xiaolong Hu  2 ,  Hao Wang  3
Affiliations
  • 1. 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.
  • 2. 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.
  • 3. 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. Electronic address: [email protected].
PMID: 32615340 DOI: 10.1016/j.jpba.2020.113441
Abstract

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.

Keywords
Amentoflavone; Caco-2 cells; Metabolites; Transport.
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