Instituto de Química de São Carlos, Universidade de São Paulo, Av. Trabalhador São Carlense, 400,13566-590 São Carlos, SP, Brazil.
Institute of Plant Biology and Biotechnology (IBBP), Westfälische Wilhelms-Universität Münster, Schlossplatz 8, 48143 Münster, Germany.
Int J Biol Macromol. 2020 Feb 15;145:417-428. doi: 10.1016/j.ijbiomac.2019.12.153. Epub 2019 Dec 20.
To improve biological activity of chitosans, new Zn(II), Pd(II) and Pt(II) complexes with biopolymeric amphiphilic Schiff bases anchored in different molecular weight chitosans matrices modified with salicylaldehyde and glycidol were prepared. Salicylaldehyde was introduced to generate complexing Schiff base sites in the chitosans matrix while glycidol is intended to increase the water solubility of the resulting biopolymeric complexes. These novel complexes were characterized using various techniques and assayed for antimicrobial and antitumor activity. The effectiveness of modification was evaluated using FTIR spectroscopy, and thermal behavior of the complexes by TG/DTG-DTA. XPRD showed that the crystallinity of the ligand diminished after the metal complexation. Surface morphologies, investigated by SEM, revealed that the complexes are rougher than chitosan matrix, and the presence of metallic ions was confirmed by EDX. Electronic spectra suggested square planar geometry for Pd(II) and Pt(II) complexes. Concerning antimicrobial activity, the novel complexes exhibited higher antibacterial efficiency against Pseudomonas syringae than against the Fusarium graminearum fungi regarding the free ligand. Complexes also exhibited high antitumor effects against the MCF-7 breast cancer cells, with certain selectivity regarding non-tumor cells (Balb/C 3T3 clone A31) depending on concentration and molar mass, indicating that they could potentially be used for antitumor applications.
为了提高壳聚糖的生物活性,我们制备了新的 Zn(II)、Pd(II) 和 Pt(II) 配合物,这些配合物带有生物聚合两亲性席夫碱,锚定在不同分子量的壳聚糖基质上,壳聚糖基质经过了水杨醛和缩水甘油修饰。水杨醛用于在壳聚糖基质中生成配位席夫碱位点,而缩水甘油则旨在提高所得生物聚合配合物的水溶性。使用各种技术对这些新型配合物进行了表征,并测试了它们的抗菌和抗肿瘤活性。通过傅里叶变换红外光谱(FTIR)评估了修饰的效果,通过热重分析/差示扫描量热法(TG/DTG-DTA)评估了配合物的热行为。X 射线粉末衍射(XPRD)表明,配体的结晶度在金属络合后降低。通过扫描电子显微镜(SEM)研究了表面形态,结果表明,与壳聚糖基质相比,配合物更粗糙,并且通过能谱分析(EDX)证实了金属离子的存在。电子光谱表明 Pd(II)和 Pt(II) 配合物具有正方形平面几何结构。关于抗菌活性,与游离配体相比,新型配合物对丁香假单胞菌的抗菌效率更高,而对禾谷镰刀菌的抗菌效率则较低。此外,配合物对 MCF-7 乳腺癌细胞也具有高抗肿瘤效果,并且根据浓度和摩尔质量对非肿瘤细胞(Balb/C 3T3 clone A31)具有一定的选择性,这表明它们可能具有用于抗肿瘤应用的潜力。