水飞蓟中的水飞蓟素和异水飞蓟素A对VA和VII碳酸酐酶的双重抑制:一种潜在的抗肥胖策略

IF 4.3 3区 医学 Q2 CHEMISTRY, MEDICINAL
Emanuele Liborio Citriniti, Roberta Rocca, Giosuè Costa, Gioele Renzi, Fabrizio Carta, Claudiu T. Supuran, Stefano Alcaro, Francesco Ortuso
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引用次数: 0

摘要

肥胖是一种全球健康危机,与心血管疾病和2型糖尿病等慢性疾病有关。它的流行,甚至在低收入国家,凸显了传统干预措施的失败。由于许多现有的抗肥胖药物由于严重的副作用而被撤回,留下了严重的治疗空白,迫切需要更安全的药物治疗。在这种情况下,一个有希望的目标是人类碳酸酐酶V (hCA V),这是一种在葡萄糖稳态中起关键作用的线粒体酶。抑制hcav已被证明可以减少脂肪生成并改善代谢状况。天然植物提取物,如水飞蓟中的水飞蓟素,已被证明具有通过降低甘油三酯、降低胆固醇水平和改善肝功能来控制肥胖相关代谢综合征的潜力。我们的计算研究已经确定了水飞蓟素中有效抑制hCA V的活性化合物,揭示了其抗肥胖作用的潜在机制。基于这些发现,我们的研究进一步揭示了这些化合物还能抑制碳酸酐酶VII (hCA VII),增强其治疗潜力。这种双重抑制作用解决了代谢失调和氧化应激。值得注意的是,hCA VII的抗氧化特性通过减轻氧化应激(代谢综合征发展的关键因素),为肥胖相关并发症提供了额外的保护。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Dual inhibition of carbonic anhydrases VA and VII by silychristin and isosilybin A from Silybum marianum: A potential antiobesity strategy

Dual inhibition of carbonic anhydrases VA and VII by silychristin and isosilybin A from Silybum marianum: A potential antiobesity strategy

Obesity is a global health crisis linked to chronic diseases like cardiovascular disease and type 2 diabetes. Its prevalence, even in low-income countries, highlights the failure of traditional interventions. Safer pharmacological treatments are urgently needed, as many existing antiobesity drugs have been withdrawn due to severe side effects, leaving a critical therapeutic gap. A promising target in this context is human carbonic anhydrase V (hCA V), a mitochondrial enzyme that plays a key role in glucose homeostasis. Inhibiting hCA V has been shown to reduce lipogenesis and improve metabolic conditions. Natural plant extracts, such as silymarin from milk thistle, have demonstrated potential in managing obesity-related metabolic syndromes by lowering triglycerides, reducing cholesterol levels, and improving liver function. Our computational studies have identified active compounds in silymarin that effectively inhibit hCA V, shedding light on a potential mechanism for its antiobesity effects. Building on these findings, our research further reveals that these compounds also inhibit carbonic anhydrase VII (hCA VII), enhancing their therapeutic potential. This dual inhibitory action addresses both metabolic dysregulation and oxidative stress. Notably, the antioxidant properties of hCA VII provide additional protection against obesity-related complications by mitigating oxidative stress, a key contributor to the development of metabolic syndrome.

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来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
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