Effects of myricetin and quercetin on ticagrelor metabolism and the underlying mechanism

doi:10.1016/j.cbi.2024.110924

科研成果详情

题名	Effects of myricetin and quercetin on ticagrelor metabolism and the underlying mechanism
作者	Wang, Jing 1,2; Hu, Yingying1; Li, Qingqing1,2; Liu, Ya-nan 1; Lin, Jingjing 1; Xu, Ren-ai1
发表日期	2024-04-01
发表期刊	Chemico-biological interactions 影响因子和分区
语种	英语
原始文献类型	Journal Article
关键词	Interaction Myricetin Pharmacokinetic Quercetin Ticagrelor
其他关键词	MYOCARDIAL-INFARCTION ; PHARMACOKINETICS ; PREVENTION ; PHARMACODYNAMICS ; INHIBITORS
摘要	The aim of this study was to investigate the potential drug-drug interactions (DDIs) between ticagrelor and other drugs as well as their underlying mechanisms. Rat liver microsome (RLM) reaction system was used to screen potential DDIs in vitro, and ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) was applied to detect the levels of ticagrelor and AR-C124910XX, the main metabolite of ticagrelor. A total of 68 drugs were screened, 11 of which inhibited the production of AR-C124910XX to 20% or less, especially two flavonoids (myricetin and quercetin). The half-maximal inhibitory concentration (IC50) of myricetin on ticagrelor was 11.51 ± 0.28 μM in RLM and 17.96 ± 0.54 μM in human liver microsome (HLM). The IC50 of quercetin in inhibiting ticagrelor in RLM and HLM was 16.92 ± 0.49 μM and 60.15 ± 0.43 μM, respectively. They all inhibited the metabolism of ticagrelor through a mixed mechanism. In addition, Sprague-Dawley (SD) rats were used to study the interactions of ticagrelor with selected drugs in vivo. We found that the main pharmacokinetic parameters including AUC (0-t), AUC (0-∞) and Cmax of ticagrelor were significantly increased when ticagrelor was combined with these two flavonoids. Our results suggested that myricetin and quercetin of flavonoids both had significant effects on the metabolism of ticagrelor, providing reference data for the clinical individualized medication of ticagrelor
出版者	ELSEVIER IRELAND LTD
ISSN	0009-2797
EISSN	1872-7786
卷号	392
DOI	10.1016/j.cbi.2024.110924
页数	7
WOS类目	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Toxicology
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Toxicology
WOS记录号	WOS:001194029400001
收录类别	PUBMED ; SCOPUS ; SCIE
在线发表日期	2024-02
URL	查看原文
PubMed ID	38401715
SCOPUSEID	2-s2.0-85186742215
通讯作者地址	[Xu, Ren-ai]The First Affiliated Hospital of Wenzhou Medical University,Zhejiang,Wenzhou,China ; [Lin, Jingjing]The First Affiliated Hospital of Wenzhou Medical University,Zhejiang,Wenzhou,China
Scopus学科分类	Toxicology
引用统计
文献类型	期刊论文
条目标识符	https://kms.wmu.edu.cn/handle/3ETUA0LF/207731
专题	药学院（分析测试中心）附属第一医院药学院（分析测试中心）_分子药理研究与教学中心
通讯作者	Lin, Jingjing; Xu, Ren-ai
作者单位	1.The First Affiliated Hospital of Wenzhou Medical University,Zhejiang,Wenzhou,China; 2.Institute of Molecular Toxicology and Pharmacology,School of Pharmaceutical Sciences,Wenzhou Medical University,Zhejiang,Wenzhou,China
第一作者单位	附属第一医院; 第一临床医学院（信息与工程学院）、附属第一医院; 药学院（分析测试中心）
通讯作者单位	附属第一医院; 第一临床医学院（信息与工程学院）、附属第一医院
第一作者的第一单位	附属第一医院
推荐引用方式 GB/T 7714	Wang, Jing,Hu, Yingying,Li, Qingqing,et al. Effects of myricetin and quercetin on ticagrelor metabolism and the underlying mechanism[J]. Chemico-biological interactions,2024,392.
APA	Wang, Jing, Hu, Yingying, Li, Qingqing, Liu, Ya-nan, Lin, Jingjing, & Xu, Ren-ai. (2024). Effects of myricetin and quercetin on ticagrelor metabolism and the underlying mechanism. Chemico-biological interactions, 392.
MLA	Wang, Jing,et al."Effects of myricetin and quercetin on ticagrelor metabolism and the underlying mechanism".Chemico-biological interactions 392(2024).