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首页> 外文期刊>Current opinion in lipidology >Molecular mechanisms underlying the antiatherosclerotic and antidiabetic effects of probucol, succinobucol, and other probucol analogues.
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Molecular mechanisms underlying the antiatherosclerotic and antidiabetic effects of probucol, succinobucol, and other probucol analogues.

机译：普罗布考，丁二酚和其他普罗布考类似物的抗动脉粥样硬化和抗糖尿病作用的分子机制。

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PURPOSE OF REVIEW: New therapies for the management of cardiovascular disease remain highly desirable, yet the recently developed agents, such as the cholesterylester transfer protein inhibitor torcetrapib, the antidiabetic agent rosiglitazone, and anti-inflammatory inhibitors of cyclooxygenase-2, have failed. In this review, the more recent developments in the molecular mechanisms underlying the beneficial activities of probucol and related compounds are described. RECENT FINDINGS: In-vivo and in-vitro studies have revealed that several of the protective activities of probucol can be explained by the ability of this drug to induce the enzyme heme oxygenase-1. It is now apparent that the sulfur atoms, rather than the phenol moieties of probucol, are required for its antiatherogenic and antirestenotic activities. Compounds related to probucol that have improved efficacy without the adverse effects offer promise as novel therapies of cardiovascular disease. Recent results suggest these compounds may also be used for the prevention of type-2 diabetes, a disease that is increasing in prevalence and importance worldwide. SUMMARY: The development of derivatives of probucol targeting anti-inflammatory and antioxidant processes, perhaps via induction of heme oxygenase-1, may add to the armamentarium of current agents used in treatment of atherosclerotic disease and diabetes.
机译：审查的目的：仍然非常需要用于治疗心血管疾病的新疗法，但是最近开发的药物，例如胆固醇酯转移蛋白抑制剂torcetrapib，抗糖尿病药罗格列酮和环氧合酶2的抗炎抑制剂都失败了。在这篇综述中，描述了普罗布考和相关化合物的有益活性的分子机制的最新进展。最新发现：体内和体外研究表明，该药诱导血红素加氧酶-1的能力可以解释普罗布考的几种保护作用。现在明显的是，其抗动脉粥样硬化和抗再狭窄活性需要硫原子而不是普罗布考的酚部分。与普罗布考有关的具有改善的功效而没有副作用的化合物有望作为心血管疾病的新疗法。最近的结果表明，这些化合物也可用于预防2型糖尿病，该疾病在世界范围内的患病率和重要性正在增加。概述：可能通过诱导血红素加氧酶-1来开发针对抗炎和抗氧化过程的普罗布考衍生物，这可能会增加用于治疗动脉粥样硬化疾病和糖尿病的现有药物的储备。

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