姜黄素非甾体抗炎药偶联物的合成及生物学评价

Sarika Chaudhary
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摘要

目前的研究工作包括四种姜黄素-非甾体抗炎药缀合物的合成及其对类风湿关节炎、抗炎和抗溃疡活性的生物学筛选。姜黄素是一种具有多种治疗潜力的植物化学物质。姜黄素与各种非甾体抗炎药结合的想法在某种程度上是新颖的,因为它有助于获得姜黄素中某些期望特性的目标,如增强生物利用度,减少副作用,并且在确定合成的偶联物的类风湿关节炎,抗炎和抗溃疡活性方面具有良好的治疗潜力,使用适当的动物模型。此外,还研究了姜黄素-非甾体抗炎药缀合物和姜黄素在Sprague-Dawley大鼠体内的生物利用度,以及姜黄素-非甾体抗炎药缀合物和姜黄素在改良的链球菌细胞壁诱导的Balb/c小鼠关节炎模型中的抗关节炎功效,该模型类似于人类类风湿关节炎。与姜黄素和姜黄素-非甾体抗炎药缀合物相比,姜黄素-非甾体抗炎药缀合物在所有提到的研究中都显示出更好的稳定性;与其他缀合物和姜黄素相比,它们还将姜黄素的生物利用度提高了5倍以上,并显著减轻了链球菌细胞壁诱导关节炎模型中的关节炎症状。所有合成化合物的结构特征都通过适当的光谱分析得到了证实。其它用于结构和纯度方面的辅助技术包括熔点测定、薄层色谱分析和重结晶。因此,将姜黄素与药用分子偶联是提高其生物利用度和增强其广泛药理作用的创新途径。
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Synthesis and Biological Evaluation of Curcumin-NSAIDs Conjugates
The present research work involves the synthesis of a total of four Curcumin-NSAIDs conjugates and their subsequent biological screening for Rheumatoid Arthritis, Anti-inflammatory, and Anti-ulcer activities. Curcumin is a phytochemical having versatile therapeutic potential. The idea of conjugating curcumin with various NSAIDs is somewhat novel in the sense that it helps in obtaining the target of incorporating certain desired properties in the curcumin like enhanced bioavailability, reduction in the side effects and also giving good therapeutic potential in terms of determination of rheumatoid arthritis, anti-inflammatory and anti-ulcer activities of synthesized conjugates using appropriate animal models. Additionally, studies have been done on the in vivo bioavailability of curcumin-NSAIDs conjugates and curcumin in Sprague-Dawley rats and on the antiarthritic efficacy of curcumin-NSAIDs conjugates and curcumin in a modified streptococcal cell wall-induced arthritis model in Balb/c mice to resemble rheumatoid arthritis in human. Curcumin-NSAID conjugates have shown improved stability in all of the studies mentioned when compared to curcumin and curcumin-NSAID conjugates; they also increased curcumin’s bioavailability by more than five folds and significantly reduced arthritis symptoms in a streptococcal cell wall-induced arthritis model when compared to other conjugates and curcumin. The structural features of all the synthesized compounds have been confirmed by appropriate spectral analysis. Other supporting techniques employed for structural and purity aspects include Melting point determination, Thin Layer Chromatography analysis, and Recrystallization. Therefore, conjugating curcumin with medicinal molecules proved to be a creative way to increase its bioavailability and enhance its wide range of pharmacological effects.
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