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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and characterization of some bioactive conjugates of curcumin with glycine, glutamic acid, valine and demethylenated piperic acid and study of their antimicrobial and antiproliferative properties.
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Design, synthesis and characterization of some bioactive conjugates of curcumin with glycine, glutamic acid, valine and demethylenated piperic acid and study of their antimicrobial and antiproliferative properties.

机译：姜黄素与甘氨酸，谷氨酸，缬氨酸和去甲基化的哌酸的某些生物活性缀合物的设计，合成和表征，以及其抗微生物和抗增殖特性的研究。

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摘要

The monoesters of curcumin, a symmetric diphenol with valine and glycine have been prepared by a novel solid phase synthesis and its diesters with valine, glutamic acid and demethylenated piperic acid have been prepared by solution phase method. The assessment of their antimicrobial and anticancer (antiproliferative) activities suggested that diesters of curcumin are relatively more active than curcumin itself due to their increased solubility, slow metabolism and better cellular uptake. Furthermore, significant observation was that monoesters of curcumin have even better antimicrobial activity than their corresponding diesters, emphasizing the role of free phenolic group. The conjugate of curcumin with demethylenated piperic acid in which methylenedioxy ring was open also shows enhanced activity than the corresponding piperic acid conjugate, emphasizing the role of free phenolics in the transport or in the binding processes.
机译：姜黄素，具有缬氨酸和甘氨酸的对称二酚的单酯通过新颖的固相合成制备，并且其具有缬氨酸，谷氨酸和去甲基化的哌酸的二酯通过溶液相法制备。对它们的抗微生物和抗癌（抗增殖）活性的评估表明，姜黄素二酯由于其增加的溶解度，缓慢的代谢和更好的细胞吸收而比姜黄素本身具有更高的活性。此外，重要的观察结果是姜黄素单酯比其相应的二酯具有更好的抗菌活性，强调了游离酚基的作用。姜黄素与其中亚甲基二氧基环打开的去甲基化的哌酸的缀合物也显示出比相应的哌酸缀合物更高的活性，强调了游离酚类在运输或结合过程中的作用。

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