Suppr超能文献

自组装 pH 响应姜黄素-细菌胞外多糖胶束缀合物的构建及其作为生物活性递药系统的性能评价。

Development and performance evaluation of self-assembled pH-responsive curcumin-bacterial exopolysaccharide micellar conjugates as bioactive delivery system.

机构信息

Department of Biotechnology, Indian Institute of Technology Kharagpur, West Bengal, India.

Department of Chemistry, Indian Institute of Technology Kharagpur, West Bengal, India.

出版信息

Int J Biol Macromol. 2024 Apr;263(Pt 2):130372. doi: 10.1016/j.ijbiomac.2024.130372. Epub 2024 Feb 21.

Abstract

The present study reports the synthesis of micellar conjugates, wherein curcumin (Cur), a bioactive compound with poor bioavailability, was covalently bonded to a bacterial exopolysaccharide (EPS). These conjugates were synthesized by utilizing succinic acid that linked Cur to the pyranosyl moiety of the EPS. The Cur-EPS conjugates appeared as spherical micelles in aqueous solution and were found to have an average hydrodynamic diameter of 254 ± 2.7 nm. The micellar conjugates showed superior stability than Cur as evident from their negative surface charge (-27 ± 1.8 mV) and low polydispersity index (PDI) (0.33 ± 0.04). The in vitro studies on release kinetics helped elucidate the pH-responsive characteristics of the Cur-EPS conjugate, as 87.50 ± 1.45 % of Cur was released at an acidic pH of 5.6, in contrast to 30.15 ± 2.61 % at systemic pH of 7.4 at 150 h. The conjugates were hemocompatible and exhibited cytotoxic effect against the osteosarcoma cell line (MG-63) after 48 h treatment. They also demonstrated superior antibacterial, antibiofilm, and antioxidant activities in comparison to free Cur. Therefore, the Cur-EPS conjugates have potential pharmaceutical applications as therapeutic biomaterial that can be applied as a drug delivery system.

摘要

本研究报告了胶束缀合物的合成,其中姜黄素(Cur)是一种生物利用度较差的生物活性化合物,它通过琥珀酸共价键合到细菌胞外多糖(EPS)上。这些缀合物是通过利用将 Cur 连接到 EPS 的吡喃糖部分的琥珀酸合成的。Cur-EPS 缀合物在水溶液中呈现球形胶束,平均水动力直径为 254 ± 2.7nm。与 Cur 相比,胶束缀合物表现出更好的稳定性,其表面带负电荷(-27 ± 1.8mV)和低多分散指数(PDI)(0.33 ± 0.04)。释放动力学的体外研究有助于阐明 Cur-EPS 缀合物的 pH 响应特性,因为在酸性 pH 值 5.6 下,87.50 ± 1.45%的 Cur 被释放,而在系统 pH 值 7.4 下,150 小时后仅释放 30.15 ± 2.61%。缀合物具有血液相容性,并在 48 小时治疗后对骨肉瘤细胞系(MG-63)表现出细胞毒性作用。与游离 Cur 相比,它们还表现出优异的抗菌、抗生物膜和抗氧化活性。因此,Cur-EPS 缀合物具有作为治疗生物材料的潜在药物应用,可作为药物传递系统。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验