Department of Chemistry, Faculty of Science and Arts, Najran University, Najran, Saudi Arabia.
Department of Chemistry, College of Science, Qassim University, Buraidah 51452, Saudi Arabia; Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.
Int J Biol Macromol. 2023 Dec 31;253(Pt 6):127277. doi: 10.1016/j.ijbiomac.2023.127277. Epub 2023 Oct 6.
For chemical modification, p-aminobenzoic acid was incorporated into chitosan Schiff base (ACsSB) and chitosan (ACs). Two ACs-based CuO nanoparticles composites; ACs/CuONPs-1 % and ACs/CuONPs-5 %, were also synthesized. Their structures were emphasized utilizing several analytical techniques; elemental analysis, FTIR, H NMR, XRD, SEM, EDX and TEM. Compared with standard cyclooxygenase (COX) inhibitor, Celecoxib, the prepared biomaterials showed in vitro selective inhibitory effectiveness against COX-2 enzyme that could be sorted, according to their MIC values that produce 50 % inhibition of COX-2 enzyme activity, as follows: Celecoxib (0.28 μg/mL) > ACs/CuONPs-5 % (4.1 μg/mL) > ACs/CuONPs-1 % (14.8 μg/mL) > ACs (38.5 μg/mL) > ACsSB (58.9 μg/mL) > chitosan (>125 μg/mL). Further, ACs/CuONPs-5 % has more in vitro inhibition efficiency towards Helicobacter pylori (H. pylori) than the other prepared biomaterials. Interestingly, the MIC value of 100 % growth inhibition of H. pylori for ACs/CuONP-5 % is equal to that of drug Clarithromycin (1.95 μg/mL). Thus, ACs/CuONPs-5 % has a promising potential as anti-H. pylori and selective anti-inflammatory agent. ACs/CuONPs-5 % is safe on the human gastric normal cells (GES-1). Therefore, amalgamation of both p-aminobenzoic acid and CuONPs into chitosan extremely promoted its anti-inflammatory and anti-H. pylori activity. This is a promising approach to achieve methods successful to compete the conventional antibiotics.
对于化学修饰,将对氨基苯甲酸掺入壳聚糖席夫碱(ACsSB)和壳聚糖(ACs)中。还合成了两种基于 ACs 的氧化铜纳米粒子复合材料;ACs/CuONPs-1%和 ACs/CuONPs-5%。利用元素分析、FTIR、H NMR、XRD、SEM、EDX 和 TEM 等几种分析技术强调了它们的结构。与标准环氧化酶(COX)抑制剂塞来昔布相比,所制备的生物材料在体外对 COX-2 酶表现出选择性抑制作用,可以根据其 MIC 值进行分类,MIC 值产生 COX-2 酶活性抑制 50%,如下所示:塞来昔布(0.28μg/mL)>ACs/CuONPs-5%(4.1μg/mL)>ACs/CuONPs-1%(14.8μg/mL)>ACs(38.5μg/mL)>ACsSB(58.9μg/mL)>壳聚糖(>125μg/mL)。此外,ACs/CuONPs-5%对幽门螺杆菌(H. pylori)的体外抑制效率高于其他制备的生物材料。有趣的是,ACs/CuONP-5%对 H. pylori 的 100%生长抑制的 MIC 值等于药物克拉霉素(1.95μg/mL)。因此,ACs/CuONPs-5%具有作为抗 H. pylori 和选择性抗炎剂的巨大潜力。ACs/CuONPs-5%对人胃正常细胞(GES-1)安全。因此,将对氨基苯甲酸和 CuONPs 合并到壳聚糖中极大地促进了其抗炎和抗 H. pylori 活性。这是实现成功对抗传统抗生素的方法的有前途的方法。