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他莫昔芬与燕麦酰胺B对肝脏酯酶的抑制活性比较及基于猪和人肝脏酯酶叠加结构的相关性研究

Compared Inhibitory Activities of Tamoxifen and Avenanthramide B on Liver Esterase and Correlation Based on the Superimposed Structure Between Porcine and Human Liver Esterase.

作者信息

Lim Hakseong, Hwang Sungbo, Cho Seung-Hak, Bak Young-Seok, Yang Woong-Suk, Park Daeui, Kim Cheorl-Ho

机构信息

Department of Biological Science, Sungkyunkwan University, Suwon 16419, Republic of Korea.

Division of Advanced Predictive Research, Center for Biomimetic Research, Korea Institute of Toxicology, Daejeon 34114, Republic of Korea.

出版信息

Int J Mol Sci. 2024 Dec 11;25(24):13291. doi: 10.3390/ijms252413291.

DOI:10.3390/ijms252413291
PMID:39769055
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11675837/
Abstract

Exposure to tamoxifen can exert effects on the human liver, and esterases process prodrugs such as antibiotics and convert them to less toxic metabolites. In this study, the porcine liver esterase (PLE)-inhibitory activity of tamoxifen has been investigated. PLE showed inhibition of a PLE isoenzyme (PLE5). In addition, avenanthramides, which have a similar structure to that of tamoxifen, have been used to determine the PLE-inhibitory effect. Among the avenanthramide derivatives, avenanthramide B has been shown to inhibit PLE. Avenanthramide B interacts with Lys284 of PLE, whereas avenanthramide A and C counteract with Lys284. Avenanthramide B has shown a similar inhibitory effect to that of tamoxifen. Given that avenanthramide B can modulate the action of PLE, it can be used in pharmaceutical and industrial applications for modulating the effects of PLE. Based on superimposed structures between PLE and human liver esterase, the impact of tamoxifen use in humans is discussed. In addition, this study can serve as a fundamental basis for future investigations regarding the potential risk of tamoxifen and other drugs. Thus, this study presents an insight into the comparison of structurally similar tamoxifen and avenanthramides on liver esterases, which can have implications for the pharmaceutical and agricultural industries.

摘要

他莫昔芬的暴露会对人体肝脏产生影响，酯酶会处理抗生素等前体药物并将它们转化为毒性较小的代谢物。在本研究中，已对他莫昔芬的猪肝酯酶（PLE）抑制活性进行了研究。PLE对一种PLE同工酶（PLE5）表现出抑制作用。此外，结构与他莫昔芬相似的燕麦酰胺已被用于确定PLE抑制作用。在燕麦酰胺衍生物中，燕麦酰胺B已被证明可抑制PLE。燕麦酰胺B与PLE的Lys284相互作用，而燕麦酰胺A和C与Lys284相互拮抗。燕麦酰胺B已显示出与他莫昔芬相似的抑制作用。鉴于燕麦酰胺B可调节PLE的作用，它可用于制药和工业应用中以调节PLE的作用。基于PLE与人体肝脏酯酶之间的叠加结构，讨论了他莫昔芬在人体中的使用影响。此外，本研究可为未来关于他莫昔芬和其他药物潜在风险的调查提供基础依据。因此，本研究深入比较了结构相似的他莫昔芬和燕麦酰胺对肝脏酯酶的影响，这可能对制药和农业产业具有启示意义。

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Int J Biol Macromol. 2022 Jun 15;210:172-181. doi: 10.1016/j.ijbiomac.2022.05.009. Epub 2022 May 6.
2
gmx_MMPBSA: A New Tool to Perform End-State Free Energy Calculations with GROMACS.gmx_MMPBSA：一种使用GROMACS进行终态自由能计算的新工具。
J Chem Theory Comput. 2021 Oct 12;17(10):6281-6291. doi: 10.1021/acs.jctc.1c00645. Epub 2021 Sep 29.
3
Pig Liver Esterases Hydrolyze Endocannabinoids and Promote Inflammatory Response.
猪肝酯酶水解内源性大麻素并促进炎症反应。
Front Immunol. 2021 May 17;12:670427. doi: 10.3389/fimmu.2021.670427. eCollection 2021.
4
A De Novo Designed Esterase with p-Nitrophenyl Acetate Hydrolysis Activity.具有对硝基苯乙酸酯水解活性的从头设计酯酶。
Molecules. 2020 Oct 13;25(20):4658. doi: 10.3390/molecules25204658.
5
Hot spot profiles of SARS-CoV-2 and human ACE2 receptor protein protein interaction obtained by density functional tight binding fragment molecular orbital method.通过密度泛函紧束缚片段分子轨道方法获得的 SARS-CoV-2 病毒和人血管紧张素转换酶 2 受体蛋白相互作用的热点图谱。
Sci Rep. 2020 Oct 8;10(1):16862. doi: 10.1038/s41598-020-73820-8.
6
Recent developments in the general atomic and molecular electronic structure system.通用原子和分子电子结构系统的最新进展。
J Chem Phys. 2020 Apr 21;152(15):154102. doi: 10.1063/5.0005188.
7
Investigation of Hot Spot Region in XIAP Inhibitor Binding Site by Fragment Molecular Orbital Method.用片段分子轨道法研究XIAP抑制剂结合位点的热点区域
Comput Struct Biotechnol J. 2019 Aug 21;17:1217-1225. doi: 10.1016/j.csbj.2019.08.004. eCollection 2019.
8
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Sci Rep. 2019 Oct 29;9(1):15564. doi: 10.1038/s41598-019-51580-4.
9
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Chemosphere. 2020 Jan;239:124705. doi: 10.1016/j.chemosphere.2019.124705. Epub 2019 Aug 29.
10
Use of the Multilayer Fragment Molecular Orbital Method to Predict the Rank Order of Protein-Ligand Binding Affinities: A Case Study Using Tankyrase 2 Inhibitors.使用多层片段分子轨道方法预测蛋白质-配体结合亲和力的排名顺序：以端锚聚合酶2抑制剂为例的研究。
ACS Omega. 2018 Apr 24;3(4):4475-4485. doi: 10.1021/acsomega.8b00175. eCollection 2018 Apr 30.