In vitro evaluation of the inhibition potential of echinacoside on human cytochrome P450 isozymes

doi:10.1186/s12906-022-03517-0

科研成果详情

题名	In vitro evaluation of the inhibition potential of echinacoside on human cytochrome P450 isozymes
作者	Wu, Yujie; Qiao, Aiqing; Lin, Shu; Chen, Lijia
发表日期	2022-02-18
发表期刊	BMC COMPLEMENTARY MEDICINE AND THERAPIES 影响因子和分区
语种	英语
原始文献类型	Article
关键词	Herb-drug interaction
其他关键词	HUMAN LIVER-MICROSOMES ; DRUG-DRUG INTERACTION ; INDUCTION ; APOPTOSIS ; PRODUCTS ; CYP2C19 ; CYP1A2 ; CELLS ; 3A4
摘要	Background Echinacoside (ECH) possesses a wide range of biological activity. This present study analyzes the effect of ECH on cytochrome P450 isozymes (CYPs) activities of human liver microsomes. Methods The effect of ECH on CYPs enzyme activities were studied using the enzyme-selective substrates phenacetin (1A2), chlorzoxazone (2E1), S-mephenytoin (2C19), testosterone (3A4), coumarin (2A6), diclofenac (2C9), paclitaxel (2C8), and dextromethorphan (2D6). The IC50 values for CYP1A2, CYP2E1, CYP2C19, and CYP3A4 isoforms were examined to express the strength of inhibition. Further, the inhibition of CYPs was checked for time-dependent or not, and then fitted with competitive or non-competitive inhibition models. The corresponding parameters were also obtained. Results ECH caused inhibitions on CYP1A2, CYP2E1, CYP2C19 and CYP3A4 enzyme activities in HLMs with IC50 of 21.23, 19.15, 8.70 and 55.42 mu M, respectively. The obtained results showed that the inhibition of ECH on CYP3A4 was time-dependent with the KI/K-inact value of 6.63/0.066 min(- 1)center dot mu M- 1. Moreover, ECH inhibited the activity of CYP1A2 and CYP2E1 via non-competitive manners (K-i = 10.90 mu M and K-i = 14.40 mu M, respectively), while ECH attenuated the CYP2C19 activity via a competitive manner (K-i = 4.41 mu M). Conclusions The results of this study indicate that ECH inhibits CYP1A2, CYP2E1, CYP2C19 and CYP3A4 activities in vitro. In vivo and clinical studies are warranted to verify the relevance of these interactions.
出版者	BMC
出版地	LONDON
ISSN	2662-7671
EISSN	2662-7671
卷号	22 期号:1 页码:46
DOI	10.1186/s12906-022-03517-0
页数	8
WOS类目	Integrative & Complementary Medicine
WOS研究方向	Integrative & Complementary Medicine
WOS记录号	WOS:000757825700001
收录类别	SCIE ; PUBMED ; SCOPUS
URL	查看原文
PubMed ID	35180866
PMC记录号	PMC8857812
SCOPUSEID	2-s2.0-85124924944
通讯作者地址	[Chen, Lijia]Department of Pharmacy,The Second Affiliated Hospital of Wenzhou Medical University,No. 109, West Xueyuan Road,Wenzhou,325027,China
Scopus学科分类	Complementary and Alternative Medicine
引用统计	被引频次：1[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	https://kms.wmu.edu.cn/handle/3ETUA0LF/14087
专题	第二临床医学院，附属第二医院、育英儿童医院附属第二医院
通讯作者	Chen, Lijia
作者单位	Department of Pharmacy,The Second Affiliated Hospital of Wenzhou Medical University,Wenzhou,325027,China
第一作者单位	第二临床医学院，附属第二医院、育英儿童医院; 附属第二医院
通讯作者单位	第二临床医学院，附属第二医院、育英儿童医院; 附属第二医院
第一作者的第一单位	第二临床医学院，附属第二医院、育英儿童医院; 附属第二医院
推荐引用方式 GB/T 7714	Wu, Yujie,Qiao, Aiqing,Lin, Shu,et al. In vitro evaluation of the inhibition potential of echinacoside on human cytochrome P450 isozymes[J]. BMC COMPLEMENTARY MEDICINE AND THERAPIES,2022,22(1):46.
APA	Wu, Yujie, Qiao, Aiqing, Lin, Shu, & Chen, Lijia. (2022). In vitro evaluation of the inhibition potential of echinacoside on human cytochrome P450 isozymes. BMC COMPLEMENTARY MEDICINE AND THERAPIES, 22(1), 46.
MLA	Wu, Yujie,et al."In vitro evaluation of the inhibition potential of echinacoside on human cytochrome P450 isozymes".BMC COMPLEMENTARY MEDICINE AND THERAPIES 22.1(2022):46.