单酮类姜黄素:关于其合成和生物活性的最新综述

T. M. Vieira, Lívia S. Tanajura, V. C. Heleno, Lizandra G. Magalhães, A. E. M. Crotti
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引用次数: 0

摘要

姜黄素(或 diferuloylmethane)是姜黄根茎的一种成分,具有多种生物和药理活性。然而,它的生物利用率低,在生理 pH 值下不稳定。在这篇综述中,我们将介绍 2019 年至 2023 年间发表的有关更稳定、更有效的姜黄素类似物(称为单酮姜黄素(MKCs)或 "单羰基姜黄素")的合成和生物活性的论文。本文介绍了合成 MKCs 的标准程序--克莱森-施密特缩合法的最新进展,包括离子液体的使用。研究表明,MKCs 的抗菌、抗癌、抗氧化和抗寄生虫作用,以及其他不太常见的 MKC 生物和药理活性,与姜黄素相似或更高。MKCs 具有良好的生物和药理活性,加上其诱人的合成特点(如产量高、产品分离容易),使这类化合物成为进一步发现抗菌、抗癌和抗寄生虫药物的一个令人感兴趣的前景。
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Monoketone Curcuminoids: An Updated Review of Their Synthesis and Biological Activities
Curcumin (or diferuloylmethane), a component of Curcuma longa L. rhizomes, displays various biological and pharmacological activities. However, it is poorly bioavailable and unstable in physiological pH. In this review, we cover papers published between 2019 and 2023 on the synthesis and biological activities of more stable and effective curcumin analogs known as monoketone curcuminoids (MKCs) or “monocarbonyl curcuminoids.” Recent advances in Claisen–Schmidt condensation, the standard procedure to synthesize MKCs, including the use of ionic liquids, are addressed. MKCs’ antimicrobial, anticancer, antioxidant, and antiparasitic actions, as well as other less common MKC biological and pharmacological activities, have been shown to be similar or higher than curcumin. The promising biological and pharmacological activities, combined with the attractive synthetic aspects (e.g., good yields and an easiness of product isolation) to obtain MKCs, make this class of compounds an interesting prospect for further antimicrobial, anticancer, and antiparasitic drug discovery.
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