Emerging Roles of Gossypol in Therapy: Innovations in Prodrug Design and Nanoformulation Frontiers.

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL ChemMedChem Pub Date : 2024-08-13 DOI:10.1002/cmdc.202400309

Arka Banerjee, Megha Biswas, Prakash Shukla, Rakesh Kumar Pathak

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Abstract

Stimuli activatable systems have the potential to deliver drugs to targeted areas by releasing therapeutic agents in response to diseased specific microenvironments such as the acidic environment commonly found in diseased tissues. This review article focuses on gossypol, a bioactive compound with inherent toxicity attributed to various factors, including the presence of its formyl groups. It highlights the potential of imine-linked gossypol-based prodrugs and nanoparticle formulations for targeted delivery and controlled release. The unique presence of polyphenolic cores on gossypol can be utilized to prepare nanoparticles. This review offers valuable insights into designing safer and more effective drug delivery systems by elucidating the masking effect and stimuli-responsive release mechanisms. Numerous examples demonstrate the conversion of formyl groups to imines, creating prodrugs that mask reactive functionalities and offer pH-responsive release. This insight can guide the design of combination therapeutics, where a second drug with an amine terminal group can form imine-linked prodrugs. Additionally, the second part discusses the use of polyphenolic moieties to create stable nanoparticles from infinite polymeric networks. Through a comprehensive examination of gossypol's properties and applications, this review emphasizes the broader implications of such a masking strategy for optimizing the therapeutic benefits of many similar bioactive compounds while minimizing adverse effects.

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戈西泊在治疗中的新作用：原药设计和纳米制剂的创新前沿。

可刺激激活的系统有可能根据疾病的特定微环境（如疾病组织中常见的酸性环境）释放治疗药物，从而将药物输送到目标区域。这篇综述文章的重点是棉酚，这是一种生物活性化合物，因其甲酰基团而具有固有毒性。文章强调了基于亚胺的棉酚原药和纳米颗粒制剂在靶向给药和控释方面的潜力。棉酚上独特的多酚核心可用于制备纳米颗粒。本综述通过阐明掩蔽效应和刺激响应释放机制，为设计更安全、更有效的给药系统提供了宝贵的见解。大量实例展示了将甲酰基转化为亚胺，从而制备出掩蔽反应性官能团并提供 pH 值响应释放的原药。这种见解可以指导组合疗法的设计，其中带有胺末端基团的第二种药物可以形成亚胺连接原药。此外，第二部分还讨论了如何利用多酚分子从无限聚合物网络中制造稳定的纳米颗粒。通过对棉酚特性和应用的全面研究，本综述强调了这种掩蔽策略的广泛意义，即优化许多类似生物活性化合物的治疗效果，同时最大限度地减少不良反应。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

期刊介绍： Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.