一个稳定的姜黄素/β-环糊精/抗坏血酸三元包合物,对接研究,抗菌和抗癌试验

IF 1.6 4区 化学 Q2 Agricultural and Biological Sciences
Md Sajid Ali, Nur Sarah binti Zainal Shahrom, Thevashree Rajanderan, Ahmad Salawi, Fahad Y. Sabei, Ahmed H. Albariqi, Muhammad Hadi Sultan, Mohammad Intakhab Alam, Ayed A. Alshamrani, Arun Kumar, Lee Rhi Zhou, Shahnaz Majeed, Mohammed Tahir Ansari
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引用次数: 0

摘要

姜黄素(Curcumin, CUR)是一种以其治疗潜力而闻名的多酚,但由于其水溶性差和生物利用度低,在临床应用中受到限制。本研究设想以β-环糊精(βCD)和抗坏血酸(AA)为三元物质,制备稳定的三元包合物。采用揉捏和高压灭菌法制备包合物。相溶解度研究揭示了CUR与βCD的AL型关系。结果表明,AA提高了三元配合物的稳定性,其稳定常数为138.8M−1,配合效率为0.198,效用数为3.96,体积为4.80。溶解力由−17.42提高到1.33。用A549肺癌细胞系进行的细胞毒性试验表明,该三元配合物具有与纯CUR相当的抗癌活性,体外溶出试验表明,该三元配合物的CUR释放率显著增加。我们的研究表明,AA的加入显著提高了CUR的溶解度、稳定性和生物功效,而CUR-βCD-AA较高的稳定性常数和络合效率是由于AA促进了相互作用的改善。包合物对金黄色葡萄球菌和表皮葡萄球菌的抗菌活性增强,对A549肺癌细胞的溶出率提高,细胞毒性增强,进一步支持了该三元配合物克服CUR生物利用度限制的潜力。这些结果表明,CUR-βCD-AA三元配合物可以有效地提高姜黄素的溶解度、稳定性和抗癌活性,为克服姜黄素的生物利用度挑战和提高姜黄素的治疗潜力提供了一种有希望的配方策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

A stable curcumin/β-cyclodextrin/ascorbic acid ternary inclusion complexes, docking studies, antimicrobial and anticancer assays

A stable curcumin/β-cyclodextrin/ascorbic acid ternary inclusion complexes, docking studies, antimicrobial and anticancer assays

Curcumin (CUR) is a polyphenol known for its therapeutic potential, but faces limitations in clinical application due to its poor aqueous solubility and low bioavailability. This study envisaged developing stable ternary inclusion complexes of CUR with β-cyclodextrin (βCD) and ascorbic acid (AA) as the ternary substance. Inclusion complexes were prepared by kneading and autoclaving method. Phase solubility studies revealed that the AL type relation between CUR and βCD. We observed The AA improved the stability of the ternary complexes with its stability constant as 138.8M− 1, complexation efficiency as 0.198, utility number as 3.96 and the bulk as 4.80. The solubilization power improved from − 17.42 to 1.33. Cytotoxicity assays using the A549 lung cancer cell line demonstrated that the ternary complex exhibits potent anticancer activity, comparable to pure CUR. In vitro dissolution tests showed a marked increase in the release rate of CUR from the ternary complex. Our study demonstrates that the inclusion of AA significantly enhances the solubility, stability, and biological efficacy of CUR. The higher stability constant and complexation efficiency of CUR-βCD-AA was due to improved interaction facilitated by AA. The inclusion complexes showed improved antibacterial activity against Staphylococcus aureas and Staphylococcus epidermis Enhanced dissolution rates and strong cytotoxic effects against A549 lung cancer cells further support the potential of this ternary complex in overcoming CUR’s bioavailability limitations. These results suggest that the CUR-βCD-AA ternary complex effectively enhances curcumin’s solubility, stability, and anticancer activity, offering a promising formulation strategy to overcome curcumin’s bioavailability challenges and improve its therapeutic potential.

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来源期刊
CiteScore
3.30
自引率
8.70%
发文量
0
审稿时长
3-8 weeks
期刊介绍: The Journal of Inclusion Phenomena and Macrocyclic Chemistry is the premier interdisciplinary publication reporting on original research into all aspects of host-guest systems. Examples of specific areas of interest are: the preparation and characterization of new hosts and new host-guest systems, especially those involving macrocyclic ligands; crystallographic, spectroscopic, thermodynamic and theoretical studies; applications in chromatography and inclusion polymerization; enzyme modelling; molecular recognition and catalysis by inclusion compounds; intercalates in biological and non-biological systems, cyclodextrin complexes and their applications in the agriculture, flavoring, food and pharmaceutical industries; synthesis, characterization and applications of zeolites. The journal publishes primarily reports of original research and preliminary communications, provided the latter represent a significant advance in the understanding of inclusion science. Critical reviews dealing with recent advances in the field are a periodic feature of the journal.
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