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新型杂交 3,5-二棕榈酰硝苯地平在模拟缺血/再灌注的心肌细胞培养中的保护作用。

Protective role of the novel hybrid 3,5-dipalmitoyl-nifedipine in a cardiomyoblast culture subjected to simulated ischemia/reperfusion.

机构信息

Graduate Program in Physiological Sciences, Comparative Animal Physiology, Institute of Biological Sciences, Universidade Federal do Rio Grande, FURG, Rio Grande, RS, Brazil; Institute of Biological Sciences, Universidade Federal do Rio Grande, FURG, Rio Grande, RS, Brazil.

Institute of Biological Sciences, Universidade Federal do Rio Grande, FURG, Rio Grande, RS, Brazil.

出版信息

Biomed Pharmacother. 2017 Aug;92:356-364. doi: 10.1016/j.biopha.2017.05.091. Epub 2017 May 26.

Abstract

This work investigated the acute effects of the calcium channel blocker nifedipine and its new fatty hybrid derived from palmitic acid, 3,5-dipalmitoyl-nifedipine, compared to endocannabinoid anandamide during the process of inducing ischemia and reperfusion in cardiomyoblast H9c2 heart cells. The cardiomyoblasts were treated in 24 or 96-well plates (according to the test being performed) and maintaining the treatment until the end of hypoxia induction. The molecules were tested at concentrations of 10 and 100μM, cells were treated 24h after assembling the experimental plates and immediately before the I/R. Cell viability, apoptosis and necrosis, and generation of reactive oxygen species were evaluated. Nifedipine and 3,5-dipalmitoyl-nifedipine were used to assess radical scavenging potential and metal chelation. All tested molecules managed to reduce the levels of reactive oxygen species compared to the starvation+vehicle group. In in vitro assays, 3,5-dipalmitoyl-nifedipine showed more antioxidant activity than nifedipine. These results indicate the ability of this molecule to act as a powerful ROS scavenger. Cell viability was highest when cells were induced to I/R by both concentrations of anandamide and the higher concentration of DPN. These treatments also reduced cell death. Therefore, it was demonstrated that the process of hybridization of nifedipine with two palmitic acid chains assigns a greater cardioprotective effect to this molecule, thereby reducing the damage caused by hypoxia and reoxygenation in cardiomyoblast cultures.

摘要

本研究旨在探讨钙通道阻滞剂硝苯地平及其与棕榈酸结合的新型脂肪酸衍生物 3,5-二棕榈酰硝苯地平在诱导心肌细胞 H9c2 缺血再灌注过程中的急性作用,与内源性大麻素花生四烯酸相比。心肌细胞分别在 24 孔和 96 孔板中进行处理(根据试验要求),并在缺氧诱导结束前维持处理。在浓度为 10 和 100μM 下对这些分子进行测试,在组装实验板 24 小时后和 I/R 之前对细胞进行处理。评估细胞活力、凋亡和坏死以及活性氧(ROS)的生成。使用硝苯地平和 3,5-二棕榈酰硝苯地平来评估自由基清除能力和金属螯合能力。与饥饿+载体组相比,所有测试的分子都能够降低 ROS 水平。在体外试验中,3,5-二棕榈酰硝苯地平比硝苯地平表现出更强的抗氧化活性。这些结果表明,该分子具有作为强大 ROS 清除剂的能力。当细胞受到两种浓度的花生四烯酸和更高浓度的 DPN 诱导发生 I/R 时,细胞活力最高。这些处理还减少了细胞死亡。因此,证明了硝苯地平与两个棕榈酸链的杂交过程赋予了该分子更大的心脏保护作用,从而减少了缺氧和再氧化对心肌细胞培养物造成的损伤。

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