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来自属海洋海绵的可体松抑制素和普拉基那明甾体生物碱:对其化学、药理学、药代动力学及构效关系(SARs)的深入研究

Cortistatin and plakinamine steroidal alkaloids from the marine sponges of the genus : insights into their chemistry, pharmacology, pharmacokinetics and structure activity relationships (SARs).

作者信息

Tammam Mohamed A, Aouidate Adnane, Mahmoud Manar M, Gamal El-Din Mariam I, El-Demerdash Amr

机构信息

Department of Biochemistry, Faculty of Agriculture, Fayoum University Fayoum 63514 Egypt.

School of Applied Sciences-Ait Melloul, Ibn Zohr University Agadir Morocco.

出版信息

RSC Adv. 2025 Mar 25;15(12):9092-9107. doi: 10.1039/d4ra08718f. eCollection 2025 Mar 21.

Abstract

Cortistatins and plakinamines represent a unique class of marine-derived steroidal alkaloids, renowned for their structural diversity and potent pharmacological activities. This review provides a comprehensive overview of their chemical characteristics, pharmacological profiles, pharmacokinetics, and drug-likeness properties, with a particular focus on structure-activity relationships (SARs). Indeed, we explored their distinct molecular architectures and classification within the broader family of marine alkaloids, highlighting key subclasses and derivatives identified through advanced analytical techniques. Their broad-spectrum bioactivities, including anticancer, anti-inflammatory, antimicrobial, and antiviral effects, are discussed in detail, supported by insights into SARs and pharmacophore identification that illuminate the molecular basis of their bioactivity. Additionally, we evaluate their pharmacokinetic attributes, including absorption, distribution, metabolism, and elimination (ADME), alongside their compliance with drug-likeness criteria, offering a holistic perspective on their potential for drug development.

摘要

可体他汀类化合物和普拉基胺类化合物是一类独特的海洋来源甾体生物碱,以其结构多样性和强大的药理活性而闻名。本综述全面概述了它们的化学特征、药理概况、药代动力学和类药性质,特别关注构效关系(SARs)。事实上,我们探讨了它们在更广泛的海洋生物碱家族中的独特分子结构和分类,强调了通过先进分析技术鉴定的关键亚类和衍生物。详细讨论了它们的广谱生物活性,包括抗癌、抗炎、抗菌和抗病毒作用,并通过对构效关系和药效团识别的深入了解来支持,这些了解阐明了它们生物活性的分子基础。此外,我们评估了它们的药代动力学属性,包括吸收、分布、代谢和消除(ADME),以及它们符合类药标准的情况,为它们在药物开发中的潜力提供了一个全面的视角。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/519d/11934034/f39623618111/d4ra08718f-f1.jpg

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