Cellulose & Paper Department, National Research Centre, 33 El-Bohouth St. Former (El-Tahrir St.), Dokki, Giza, P.O. 12622, Egypt.
Botany and Microbiology Department, Faculty of Science, Al-Azhar University, Cairo 11884, Egypt.
Carbohydr Polym. 2022 Feb 1;277:118823. doi: 10.1016/j.carbpol.2021.118823. Epub 2021 Oct 29.
The conjugation between drug and biopolymers through an easily hydrolysable bond such as ester linkage, disulfide linkage, or imine-bond have been extensively employed to control the drug release pattern and improve its bioavailability. This work described the conjugation of 9-aminoacridine (9-AA) to Gum Arabic (GA) via Schiff's base, as a pH-responsive bond. First, GA was oxidized to Arabic Gum dialdehyde (AGDA), then a different amount of 9-AA (10, 25, and 50 mg 9-AA) was coupled to defined amount of AGDA, the coupling was confirmed by elemental analysis and different spectroscopic tools. In addition, the physical features of Schiff's base conjugates including surface morphology, thermal stability, and crystalline structure were examined. The thermogravimetric analysis revealed that the incorporation of 9-AA slightly improved the thermal stability. The coupling of 9-AA to AGDA dramatically enhanced its in vitro antimicrobial and antitumor activities. All conjugates exhibited broad-spectrum activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, and Candida albicans. Moreover, AGA 25 and AGA 50 demonstrated promising capability to suppress the proliferation of human colon cancer cell line (Caco-2), with IC 190.10 and 180.80 μg/mL respectively.
通过酯键、二硫键或亚胺键等易于水解的键将药物与生物聚合物连接,已被广泛用于控制药物释放模式并提高其生物利用度。本工作通过席夫碱将 9-氨基吖啶(9-AA)连接到阿拉伯树胶(GA)上,作为一种 pH 响应键。首先,将 GA 氧化为阿拉伯树胶二醛(AGDA),然后将不同量的 9-AA(10、25 和 50mg 9-AA)与一定量的 AGDA 偶联,通过元素分析和不同的光谱工具确认偶联。此外,还研究了席夫碱缀合物的物理特性,包括表面形貌、热稳定性和晶体结构。热重分析表明,引入 9-AA 略微提高了热稳定性。9-AA 与 AGDA 的偶联极大地增强了其体外抗菌和抗肿瘤活性。所有缀合物均对大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌、枯草芽孢杆菌和白色念珠菌表现出广谱活性。此外,AGA 25 和 AGA 50 表现出抑制人结肠癌细胞系(Caco-2)增殖的良好能力,IC 50 分别为 190.10 和 180.80μg/mL。