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壳聚糖纳米粒中β-和γ-CD/姜黄素负载的抗氧化、抗菌和抗癌活性。

Antioxidant, antibacterial and anti-cancer activities of β-and γ-CDs/curcumin loaded in chitosan nanoparticles.

机构信息

Department of Chemistry, Faculty of Science, University of Guilan, P.B. 41335-1914, Rasht, Iran; Department of Chemistry, Faculty of Science, University Campus 2, University of Guilan, Rasht, Iran.

Department of Chemistry, Faculty of Science, University Campus 2, University of Guilan, Rasht, Iran.

出版信息

Int J Biol Macromol. 2020 Mar 15;147:778-791. doi: 10.1016/j.ijbiomac.2020.01.206. Epub 2020 Jan 23.

Abstract

Curcumin, as a naturally occurring polyphenol, has been extensively used as anticancer and antioxidant agent due to its ability to protect cells from oxidative damage. In the present study, we have prepared highly soluble CUR-β-cyclodextrin (β-CD) and γ-cyclodextrin (γ-CD) hollow spheres. UV-Vis method was employed to approve the successful formation of the inclusion complex where the aromatic ring of CUR has been encapsulated by the hydrophobic cavity of CDs. CUR-CDs were then encapsulated into positively charged biodegradable chitosan (CUR-CDs-CS) nanoparticles. The CUR-CD-CS were characterized by UV-Vis, FTIR, HNMR, XRD, SEM analysis. Antibacterial efficacy was evaluated by measuring the zone of inhibition scale and MIC value which was recorded as 32 μg/mL and 64 μg/mL for both Gram positive S. aureus and Gram negative E. coli bacteria respectively. We tested the efficacy of these CUR-CD-CS nanoparticles in A549 cell lines using MTT assay and investigated its cellular uptake mechanism. Our results demonstrated that CUR-CD-CS nanoparticles showed superior in vitro release performance and higher cytotoxicity in A549 cell line among all tested formulations. Antioxidant activity and release behavior of the curcumin-loaded CDs-CS was investigated. The IC value for CUR/CD-CS was estimated based on their inhibition percent-concentration curves using DPPH assay.

摘要

姜黄素作为一种天然存在的多酚,因其能够保护细胞免受氧化损伤,而被广泛用作抗癌和抗氧化剂。在本研究中,我们制备了高水溶性的 CUR-β-环糊精(β-CD)和 γ-环糊精(γ-CD)空心球。采用紫外可见分光光度法证实了包合物的成功形成,其中 CUR 的芳环被 CDs 的疏水性腔包裹。然后将 CUR-CDs 包封到带正电荷的可生物降解壳聚糖(CUR-CDs-CS)纳米粒子中。通过紫外可见分光光度法、傅里叶变换红外光谱(FTIR)、HNMR、X 射线衍射(XRD)、扫描电子显微镜(SEM)分析对 CUR-CD-CS 进行了表征。通过测量抑菌圈的大小和 MIC 值来评估 CUR-CD-CS 的抗菌功效,结果表明,CUR-CD-CS 对革兰氏阳性菌金黄色葡萄球菌和革兰氏阴性菌大肠杆菌的抑菌圈大小分别为 32 μg/mL 和 64 μg/mL。我们通过 MTT 测定法在 A549 细胞系中测试了这些 CUR-CD-CS 纳米粒子的功效,并研究了其细胞摄取机制。结果表明,与所有测试配方相比,CUR-CD-CS 纳米粒子在体外具有更好的释放性能和更高的 A549 细胞系细胞毒性。研究了载有姜黄素的 CDs-CS 的抗氧化活性和释放行为。根据 DPPH 测定法的抑制百分比浓度曲线,估算了 CUR/CD-CS 的 IC 值。

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