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Stability, Structure, and Permeability Studies of Copper Tripeptide Species in Aqueous Solution
Australian Journal of Chemistry ( IF 1.0 ) Pub Date : 2021-06-22 , DOI: 10.1071/ch21040
Ahmed N. Hammouda , Fatin M. Elmagbari , Graham E. Jackson , Giselle M. Vicatos , Raffaele P. Bonomo , Gabriele Valora

The use of copper complexes to alleviate inflammation associated with rheumatoid arthritis (RA) is well known. This study focuses on designing a new drug that could be used to increase the bioavailability of copper and hence be more effective. The ligand chosen was sarcosyl-l-lysyl-l-lysine (Sar-Lys-Lys). The thermodynamic stability of H+, CuII, NiII, and ZnII complexes of Sar-Lys-Lys was measured in an aqueous solution at 298 ± 0.01°C and an ionic strength of 0.15 M (NaCl) using glass electrode potentiometry. UV-Vis, ESR, and 1H NMR spectroscopy was used to investigate the solution structures of the different species. At physiological pH, the ligand was found to coordinate via two amide nitrogens, the terminal amine, and the terminal carboxy group. The ε-amino group of lysine did not coordinate with the metal ion. Dermal absorption is the preferred method of administration and so this study used partition coefficients and tissue permeability studies to assess the bioavailability of the different complexes. Sar-Lys-Lys was found to increase the copper lipophilicity by a factor of 10 and increased tissue permeability by 30 %.



中文翻译:

铜三肽在水溶液中的稳定性、结构和渗透性研究

使用铜络合物减轻与类风湿性关节炎 (RA) 相关的炎症是众所周知的。这项研究的重点是设计一种可用于提高铜的生物利用度并因此更有效的新药。选择的配体是肌氨酰-1-赖氨酰-1-赖氨酸(Sar-Lys-Lys)。Sar-Lys-Lys的 H +、Cu II、Ni II和 Zn II复合物的热力学稳定性在 298 ± 0.01°C 和 0.15 M (NaCl) 离子强度的水溶液中使用玻璃电极电位测定法测量。紫外-可见光、ESR 和1H NMR光谱用于研究不同物种的溶液结构。在生理 pH 值下,发现配体通过两个酰胺氮、末端胺和末端羧基进行配位。赖氨酸的ε-氨基不与金属离子配位。皮肤吸收是首选的给药方法,因此本研究使用分配系数和组织渗透性研究来评估不同复合物的生物利用度。发现 Sar-Lys-Lys 将铜的亲脂性提高了 10 倍,并将组织渗透性提高了 30%。

更新日期:2021-06-24
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