亲爱的研友该休息了!由于当前在线用户较少,发布求助请尽量完整地填写文献信息,科研通机器人24小时在线,伴您度过漫漫科研夜!身体可是革命的本钱,早点休息,好梦!

Rapid high performance liquid chromatography method for erlotinib quantification in vitro: Application to study the effect of resveratrol on metabolism and cellular uptake of erlotinib

埃罗替尼 药理学 白藜芦醇 化学 微粒体 药物代谢 代谢物 表皮生长因子受体 体外 医学 药品 生物化学 受体
作者
Aref Zayed,Jomana Al Hroot,Abdulraouf Mayyas,Belal Al‐Husein
出处
期刊:Fundamental & Clinical Pharmacology [Wiley]
卷期号:37 (5): 983-993 被引量:2
标识
DOI:10.1111/fcp.12914
摘要

Erlotinib is a selective epidermal growth factor receptor inhibitor that is used for the treatment of non-small cell lung cancer and pancreatic cancer. Its metabolism is mainly mediated by cytochrome P450 3A (CYP 3A). Resveratrol, a natural compound found in many plants and supplements, is known to inhibit CYP3A enzyme, therefore, it may act as an inhibitor for the metabolism of erlotinib.Development of a rapid high performance liquid chromatography with photodiode array detection (HPLC-PDA) method for the quantification of erlotinib in liver microsomes and cancer cells and its application to study resveratrol effect on metabolism and cellular uptake of erlotinib.HPLC-PDA was used to develop an efficient bioanalytical method with a 2.5-min runtime preceded by a simple protein precipitation step. The method was validated according to the European Medicines Agency guidelines. Erlotinib metabolic stability and resveratrol effect on erlotinib metabolite formation were evaluated in rat liver microsomes. Furthermore, the method was used to measure the intracellular concentrations of erlotinib in cancer colorectal cells and investigating resveratrol effect on the cellular uptake of erlotinib.A rapid HPLC-PDA method was developed and validated for the first time to address potential drug interaction of erlotinib with resveratrol. Resveratrol was a strong inhibitor of erlotinib metabolism in vitro with IC50 = 4.03 μM. Resveratrol, however, had no effect on erlotinib cellular uptake after 1 h incubation in human colorectal cancer cells.The study suggests that resveratrol may produce a potential herb-drug interaction with erlotinib at the metabolism level and should be investigated in patients in the clinic.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
34秒前
36秒前
Sisyphus发布了新的文献求助10
42秒前
59秒前
1分钟前
Sisyphus完成签到,获得积分10
1分钟前
arsenal完成签到 ,获得积分10
1分钟前
1分钟前
yukk完成签到,获得积分10
1分钟前
1分钟前
11发布了新的文献求助10
1分钟前
2分钟前
2分钟前
yukk发布了新的文献求助10
2分钟前
2分钟前
11完成签到,获得积分10
3分钟前
斯文败类应助科研通管家采纳,获得10
3分钟前
cadcae完成签到,获得积分10
4分钟前
4分钟前
h0jian09完成签到,获得积分10
4分钟前
科研通AI2S应助科研通管家采纳,获得10
5分钟前
Akim应助科研通管家采纳,获得10
5分钟前
5分钟前
风清月明已深秋完成签到,获得积分10
5分钟前
5分钟前
5分钟前
5分钟前
脑洞疼应助tanliulong采纳,获得10
6分钟前
6分钟前
6分钟前
tanliulong发布了新的文献求助10
6分钟前
檸123456发布了新的文献求助30
6分钟前
tanyaru完成签到,获得积分10
6分钟前
6分钟前
打打应助合适小刺猬采纳,获得10
6分钟前
xingsixs完成签到 ,获得积分10
6分钟前
6分钟前
6分钟前
6分钟前
檸123456完成签到,获得积分10
7分钟前
高分求助中
The Mother of All Tableaux: Order, Equivalence, and Geometry in the Large-scale Structure of Optimality Theory 3000
A new approach to the extrapolation of accelerated life test data 1000
Indomethacinのヒトにおける経皮吸収 400
基于可调谐半导体激光吸收光谱技术泄漏气体检测系统的研究 370
Phylogenetic study of the order Polydesmida (Myriapoda: Diplopoda) 370
Robot-supported joining of reinforcement textiles with one-sided sewing heads 320
Aktuelle Entwicklungen in der linguistischen Forschung 300
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 3995599
求助须知:如何正确求助?哪些是违规求助? 3535409
关于积分的说明 11267260
捐赠科研通 3275108
什么是DOI,文献DOI怎么找? 1806536
邀请新用户注册赠送积分活动 883367
科研通“疑难数据库(出版商)”最低求助积分说明 809782