体外研究孕激素对糖蛋白- P活性的影响

详细

研究现实性。糖蛋白- P(Pgp,ABCB1)是一种参与药物药代动力学和肿瘤细胞化疗耐药发展的转运蛋白。

目的:目的:研究黄体酮对体外培养的人小肠上皮细胞模型中Pgp活性的影响。

材料与方法:对Caco-2细胞系进行了研究。在特殊的Transwell体系中,通过非索非那定转运评价Pgp的活性。高效液相色谱法测定非索非那定的浓度。采用免疫酶测定法测定Pgp的含量。我们进行了四个系列的实验:对照组细胞在不添加任何物质的清洁运输介质中孵育;预孵育3天,10 mcmol / L浓度利福平对Pgp活性及合成的影响(诱导控制);孕酮在1、10和100 mol / L预潜伏30分钟时对Pgp活性的影响;孕酮在1、10、100 mcmol / L预潜伏3天后对Pgp活性及合成的影响。

结果:黄体酮与细胞潜伏30 分钟时,浓度为1和10的黄体酮对Pgp的活性没有显著影响,但浓度为100的黄体酮会降低转运蛋白的活性。

将Caco-2细胞与黄体酮浓度分别为1,10和100微米的水杨酸潜伏3天后,Pgp的活性没有变化。与对照指标相比,孕酮在潜伏3天后,浓度为100微米的孕酮可显著提高肠上皮细胞Pgp的合成,提高114.3%,但在剩余的使用浓度(1和10微米)中效果不显著。

结论:体外实验中,在Caco-2细胞系细胞中,孕激素浓度为100微米时,对Pgp活性有直接抑制作用,但在潜伏3天后,孕酮增加了转运蛋白的合成,使其抑制活性减弱。

作者简介

Pelageya Erokhina

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0003-4802-5656

Student

俄罗斯联邦, Ryazan

Yulia Abalenikhina

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0003-0427-0967
SPIN 代码: 4496-9027
Researcher ID: L-8965-2018

PhD in Biological Sciences, Assistant Professor of the Department of Biological Chemistry

俄罗斯联邦, Ryazan

Alexey Shchulkin

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0003-1688-0017
SPIN 代码: 2754-1702
Researcher ID: N-9143-2016

MD, PhD, Assistant Professor of the Department of Pharmacology with a Course of Pharmacy of Continuing Professional Education Faculty

俄罗斯联邦, Ryazan

Ivan Chernykh

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0002-5618-7607
SPIN 代码: 5238-6165
Researcher ID: R-1389-2017

PhD in Biological Sciences, Head of the Department of Pharmaceutical Chemistry

俄罗斯联邦, Ryazan

Natalia Popova

Ryazan State Medical University

编辑信件的主要联系方式.
Email: p34-66@yandex.ru
ORCID iD: 0000-0002-5166-8372
SPIN 代码: 7553-9852
Researcher ID: B-1130-2016

MD, PhD, Assistant Professor of the Department of Pharmacology with a Course of Pharmacy of Continuing Professional Education Faculty

俄罗斯联邦, Ryazan

Alexandr Slepnev

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0003-0696-6554

PhD in Biological Sciences, Assistant Professor of the Department of Pharmacology with a Course of Pharmacy of Continuing Professional Education Faculty

俄罗斯联邦, Ryazan

Elena Yakusheva

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0001-6887-4888
SPIN 代码: 2865-3080
Researcher ID: T-6343-2017

MD, PhD, Professor, Head of the Department of Pharmacology with a Course of Pharmacy of Continuing Professional Education Faculty

俄罗斯联邦, Ryazan

参考

  1. Yakusheva EN, Shulkin AV, Popova NM, et al. Structure, functions, of P-glycoprotein and its role in rational pharmacotherapy. Reviews on Clinical Pharmacology and Drug Therapy. 2014;(2):3-11. (In Russ).
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  3. Gatsanoga MV, Chernykh IV, Shchulkin AV, et al. The method of assessment of drugs belonging to the substrates of P-glycoprotein on female rabbits. Nauka Molodykh (Eruditio Juvenium). 2016;(3):5-10. (In Russ).
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版权所有 © Erokhina P., Abalenikhina Y., Shchulkin A., Chernykh I., Popova N., Slepnev A., Yakusheva E., 2020

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