SRPIN340 和对磺酸杯[6]芳烃之间的复合物的 NMR 分析、细胞毒活性和理论研究。
NMR analysis, cytotoxic activity and theoretical study of a complex between SRPIN340 and p-sulfonic acid calix[6]arene.
发表日期：2024 Jul 01
作者：
Lívia Cristina de Souza Viol, Natália Aparecida Liberto Silva, Cristiane Isaac Cerceau, Marcus Vinícius de Andrade Barros, Raoni Pais Siqueira, Victor Hugo Sousa Gonçalves, Gustavo Costa Bressan, Sergio Antonio Fernandes, Elson Santiago Alvarenga, Róbson Ricardo Teixeira
来源：
Cellular & Molecular Immunology
摘要：
目的：本研究旨在提高 SRPK 抑制剂 N-(2-(哌啶-1-基)-5-(三氟甲基)苯基)异烟酰胺 (SRPIN340) 的水溶解度。材料
Aim: This study aimed to enhance the aqueous dissolution of SRPK inhibitor N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide (SRPIN340). Materials & Methods: A complex with p-sulfonic calix[6]arene (Host) and SRPIN340 (Guest) was prepared, studied via 1H nuclear magnetic resonance (NMR) and theoretical calculations and biologically evaluated on cancer cell lines. Results & conclusion: The 1:1 host (H)/guest (G) complex significantly enhanced the aqueous dissolution of SRPIN340, achieving 64.8% water solubility as determined by 1H NMR quantification analysis. The H/G complex reduced cell viability by 75% for HL60, ∼50% for Nalm6 and Jurkat, and ∼30% for B16F10 cells. It exhibited greater cytotoxicity than free SRPIN340 against Jurkat and B16F10 cells. Theoretical studies indicated hydrogen bond stabilization of the complex, suggesting broader applicability of SRPIN340 across diverse biological systems.