Issue 4, 2022

Cryptochlorogenic acid and its metabolites ameliorate myocardial hypertrophy through a HIF1α-related pathway

Abstract

Cryptochlorogenic acid (4-CQA) is a phenolic acid that has antioxidant and anti-inflammatory activities. Our preliminary study found that 4-CQA has a good effect on isoproterenol (ISO)-induced myocardial hypertrophy, while the mechanism remains largely unknown. This study aimed at delineating the metabolites and metabolic pathways of 4-CQA using liquid mass spectrometry and molecular biotechnology, exploring possible active metabolites and the mechanism of myocardial hypertrophy amelioration in H9c2 cells, and finally, investigating the pharmacokinetics of 4-CQA and its active metabolites in vivo. In summary, 56 potential effective metabolites were distinguished in rat urine, feces, plasma samples and heart tissue after intragastric administration of 4-CQA, and the main metabolic reaction types of 4-CQA included hydrogenation, methylation, glucuronidation, sulfation, hydration and their composite reactions in in vivo biotransformation. Besides, 4-CQA and its main active metabolites, caffeic acid and 4-O-feruloylquinic acid, significantly ameliorated pathological cardiac hypertrophy of H9c2 cells treated with ISO based on the Akt/mTOR/HIF-1α pathway. In addition, this study demonstrated that the prototype drugs 4-CQA and 4-O-ferulylquinic acid generally exhibit similar pharmacokinetic characteristics and caffeic acid presents relatively late peak time and low peak concentration in rats, which make them suitable candidate drugs.

Graphical abstract: Cryptochlorogenic acid and its metabolites ameliorate myocardial hypertrophy through a HIF1α-related pathway

Supplementary files

Article information

Article type
Paper
Submitted
12 Nov 2021
Accepted
20 Jan 2022
First published
21 Jan 2022

Food Funct., 2022,13, 2269-2282

Cryptochlorogenic acid and its metabolites ameliorate myocardial hypertrophy through a HIF1α-related pathway

J. Li, X. Chen, X. Li, J. Tang, Y. Li, B. Liu and S. Guo, Food Funct., 2022, 13, 2269 DOI: 10.1039/D1FO03838A

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