可溶性鸟苷酸环化酶刺激剂BAY41-8543:一种治疗压力和容量过载引起的慢性心力衰竭的有前途的方法。

IF 2.3 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Adriana Martišková, Matúš Sýkora, Natália Andelová, Miroslav Ferko, Olga Gawrys, Katarína Andelová, Petr Kala, Luděk Červenka, Barbara Szeiffová Bačová
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引用次数: 0

摘要

心力衰竭(HF)是发病率和死亡率的主要原因,通常由长期暴露于病理性刺激(如压力和容量过载)引起。这些因素导致过度氧化应激、不良心脏重构和一氧化氮-可溶性鸟苷环化酶-环鸟苷单磷酸(NO-sGC-cGMP)信号通路失调。鉴于迫切需要有效的治疗,本研究探讨了sGC刺激剂减缓HF进展的潜力。我们利用转人-2基因(TGR)的雄性高血压大鼠和由主动脉腔瘘(ACF)引起的容量过载HF模型。大鼠给予sGC刺激剂BAY 41-8543 (3 mg/kg/d),连续30周,对照组为正常血压的汉诺威Sprague-Dawley大鼠。在研究终点(40周龄),使用质谱法、Western blotting和组织学评估分析左心室组织。经sGC刺激剂处理的TGR大鼠显示出关键抗氧化蛋白(SOD1、CH10、ACSF2、NDUS1、DHE3、GSTM2和PCCA)显著增加,表明其抗氧化应激能力增强。然而,sGC刺激剂治疗也上调了细胞外基质重塑标志物(MMP-2、TGF-β和SMAD2/3),这些标志物通常与纤维化相关。尽管如此,马松三色染色显示,接受sGC刺激剂的TGR和TGR- acf大鼠的胶原沉积减少。值得注意的是,所有未经治疗的TGR-ACF大鼠在研究终点前死亡,无法直接评估sGC刺激剂在晚期心衰中的作用。这些发现强调了sGC刺激剂在HF中的治疗潜力,特别是通过它们的抗氧化作用。然而,它们对纤维化的同时影响需要进一步研究以优化治疗策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Soluble Guanylate Cyclase Stimulator, BAY41-8543: A Promising Approach for the Treatment of Chronic Heart Failure Caused by Pressure and Volume Overload.

Heart failure (HF) is a leading cause of morbidity and mortality, often driven by prolonged exposure to pathological stimuli such as pressure and volume overload. These factors contribute to excessive oxidative stress, adverse cardiac remodeling, and dysregulation of the nitric oxide-soluble guanylate cyclase-cyclic guanosine monophosphate (NO-sGC-cGMP) signaling pathway. Given the urgent need for effective treatments, this study investigated the potential of sGC stimulators to mitigate HF progression. We utilized male hypertensive Ren-2 transgenic (TGR) rats and a volume-overload HF model induced by an aortocaval fistula (ACF). Rats received the sGC stimulator BAY 41-8543 (3 mg/kg/day) for 30 weeks, while normotensive Hannover Sprague-Dawley rats served as controls. At the study endpoint (40 weeks of age), left ventricular tissue was analyzed using mass spectrometry, Western blotting, and histological assessment. TGR rats treated with sGC stimulators exhibited a significant increase in key antioxidant proteins (SOD1, CH10, ACSF2, NDUS1, DHE3, GSTM2, and PCCA), suggesting enhanced resistance to oxidative stress. However, sGC stimulator treatment also upregulated extracellular matrix remodeling markers (MMP-2, TGF-β, and SMAD2/3), which are typically associated with fibrosis. Despite this, Masson's trichrome staining revealed reduced collagen deposition in both TGR and TGR-ACF rats receiving sGC stimulators. Notably, all untreated TGR-ACF rats succumbed before the study endpoint, preventing direct assessment of sGC stimulator effects in advanced HF. These findings highlight the therapeutic potential of sGC stimulators in HF, particularly through their antioxidant effects. However, their concurrent influence on fibrosis warrants further investigation to optimize treatment strategies.

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来源期刊
Pharmacology Research & Perspectives
Pharmacology Research & Perspectives Pharmacology, Toxicology and Pharmaceutics-General Pharmacology, Toxicology and Pharmaceutics
CiteScore
5.30
自引率
3.80%
发文量
120
审稿时长
20 weeks
期刊介绍: PR&P is jointly published by the American Society for Pharmacology and Experimental Therapeutics (ASPET), the British Pharmacological Society (BPS), and Wiley. PR&P is a bi-monthly open access journal that publishes a range of article types, including: target validation (preclinical papers that show a hypothesis is incorrect or papers on drugs that have failed in early clinical development); drug discovery reviews (strategy, hypotheses, and data resulting in a successful therapeutic drug); frontiers in translational medicine (drug and target validation for an unmet therapeutic need); pharmacological hypotheses (reviews that are oriented to inform a novel hypothesis); and replication studies (work that refutes key findings [failed replication] and work that validates key findings). PR&P publishes papers submitted directly to the journal and those referred from the journals of ASPET and the BPS
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