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天然与合成辣椒素类似物:生物学效应与合成途径的全面综述

Natural and Synthetic Capsaicin Analogues: A Comprehensive Review of Biological Effects and Synthetic Pathways.

作者信息

Borges Lara Gimenez, de Oliveira Alves Thais Nascimento, Vassiliades Sandra Valeria, Parise-Filho Roberto

机构信息

Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Prof. Lineu Prestes Avenue, 580, Bl.13, São Paulo, SP, Brazil.

出版信息

Curr Med Chem. 2025;32(24):4963-4991. doi: 10.2174/0109298673310050240821054652.

Abstract

Capsaicin analogs, whether sourced from natural origins or synthesized de novo, have garnered significant attention across diverse scientific disciplines. This comprehensive investigation explores the expansive domain of medicinal chemistry and pharmacology, focusing on capsaicin and its analogs. Notably, these analogs exhibit a wideranging pharmacological spectrum, with a particular emphasis on their potent antitumor properties. Researchers frequently explore structural modifications, particularly in region C, consistently enhancing their pharmacological activities. A highlighted finding is that analogs with alterations in both regions A and C manifest a diverse array of effects, spanning from anti-obesity to protection against ischemia. They also demonstrate anti- Alzheimer's, anti-fibrotic, anti-inflammatory, anti-diabetic, antimalarial, and anti-epileptic properties. This underscores the potential of structural adaptations in these regions, expanding the therapeutic applications of capsaicin-like compounds. Additionally, manipulations in regions B and C result in compounds that possess antioxidant and anti-obesity properties, providing valuable insights for the development of novel compounds. The therapeutic potential of capsaicin analogs opens innovative avenues for drug design and development, promising to address a broad spectrum of diseases and enhance global quality of life. Moreover, this article meticulously examines various synthetic methodologies for synthesizing capsaicin analogs, complementing the main review. These methodologies distinguish themselves through their simplicity, mild reaction conditions, and reliance on readily available commercial reagents. The accessible synthesis pathways enable researchers from diverse backgrounds to explore these compounds, fostering investigations and potential therapeutic applications.

摘要

辣椒素类似物,无论源自天然还是从头合成,都已在不同科学学科中引起了广泛关注。这项全面的研究探索了药物化学和药理学的广阔领域,重点关注辣椒素及其类似物。值得注意的是,这些类似物展现出广泛的药理谱,尤其强调其强大的抗肿瘤特性。研究人员经常探索结构修饰,特别是在区域C,不断增强它们的药理活性。一个突出的发现是,在区域A和C都有改变的类似物表现出从抗肥胖到抗缺血保护等一系列不同的效应。它们还表现出抗阿尔茨海默病、抗纤维化、抗炎、抗糖尿病、抗疟疾和抗癫痫特性。这突出了这些区域结构适应性的潜力,扩大了辣椒素样化合物的治疗应用。此外,对区域B和C的操作产生了具有抗氧化和抗肥胖特性的化合物,为新型化合物的开发提供了有价值的见解。辣椒素类似物的治疗潜力为药物设计和开发开辟了创新途径,有望解决广泛的疾病并提高全球生活质量。此外,本文详细研究了合成辣椒素类似物的各种合成方法,作为主要综述的补充。这些方法以其简单性、温和的反应条件以及对易于获得的商业试剂的依赖而独具特色。易于获得的合成途径使来自不同背景的研究人员能够探索这些化合物,促进研究和潜在的治疗应用。

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