Discovery of Efficient Hypoxia-Targeted NO Donor Compounds to Alleviate Hypoxia Cardiac Disease,Journal of Medicinal Chemistry

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Discovery of Efficient Hypoxia-Targeted NO Donor Compounds to Alleviate Hypoxia Cardiac Disease
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2023-11-16 , DOI: 10.1021/acs.jmedchem.3c01421
Wanxiang Yang ₁ , Wen Zhou _{1,

2} , Shaohua Gou _{1,

2}

Affiliation

In order to obtain efficient NO donor drugs to treat hypoxic cardiac disease, a series of hypoxia-targeted NO donor compounds were prepared and screened. Among them, a representative compound H3 was found to selectively release NO under hypoxia with a higher ratio than isosorbide dinitrate (ISDN). In vitro study indicated that H3 had a strong capability of alleviating vascular dilation and reducing myocardial hypoxic injury due to its effective regulation of vascular dilatation and myocardial injury-related proteins in H9c2 cells even at low concentrations. By intraperitoneal injection or intragastric administration, in vivo animal tests revealed that H3 possessed a potent antimyocardial hypoxic injury effect superior to ISDN. These findings suggest that H3 has a better effect on alleviating hypoxic cardiac disease than the conventional drug, owing to its hypoxia-targeted release of NO.

中文翻译：

发现有效的针对缺氧的 NO 供体化合物以缓解缺氧性心脏病

为了获得高效的NO供体药物来治疗缺氧性心脏病，制备并筛选了一系列针对缺氧的NO供体化合物。其中，代表性化合物H3被发现在缺氧条件下选择性释放NO，释放比例高于硝酸异山梨酯（ISDN）。体外研究表明， H3即使在低浓度下也能有效调节H9c2细胞中的血管扩张和心肌损伤相关蛋白，因此具有很强的缓解血管扩张和减轻心肌缺氧损伤的能力。通过腹腔注射或灌胃给药，体内动物试验表明H3具有优于ISDN的强效抗心肌缺氧损伤作用。这些发现表明， H3由于其针对缺氧的 NO 释放，比传统药物具有更好的缓解缺氧性心脏病的效果。

更新日期：2023-11-16

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