Produção Nacional
Revisado por pares
Characterization and Antiproliferative Activity of a Novel 2-Aminothiophene Derivative-β-Cyclodextrin Binary System
2018; Multidisciplinary Digital Publishing Institute; Volume: 23; Issue: 12 Linguagem: Inglês
10.3390/molecules23123130
ISSN1433-1373
AutoresElayne Barros Ferreira, Walter Ferreira da Silva Júnior, Jonas Gabriel de Oliveira Pinheiro, Aldilane Gonçalves da Fonseca, Telma Maria Araújo Moura Lemos, Hugo Alexandre Oliveira Rocha, Eduardo Pereira de Azevedo, Francisco Jaime Bezerra Mendonça, Ádley Antonini Neves de Lima,
Tópico(s)Analytical Chemistry and Chromatography
ResumoThe novel 2-aminothiophene derivative 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) has shown potential anti-proliferative activity in human cancer cell lines. However, the poor aqueous solubility of 6CN impairs its clinical use. This work aimed to develop binary 6CN-β-cyclodextrin (βCD) systems with the purpose of increasing 6CN solubility in water and therefore, to improve its pharmacological activity. The 6CN-βCD binary systems were prepared by physical mixing, kneading and rotary evaporation methods and further characterized by FTIR, XRD, DSC, TG and SEM. In addition, molecular modeling and phase solubility studies were performed. Finally, MTT assays were performed to investigate the cytostatic and anti-proliferative effects of 6CN-βCD binary systems. The characterization results show evident changes in the physicochemical properties of 6CN after the formation of the binary systems with βCD. In addition, 6CN was associated with βCD in aqueous solution and the solid state, which was confirmed by molecular modeling and the aforementioned characterization techniques. Phase solubility studies indicated that βCD forms stable 1:1 complexes with 6CN. The MTT assay demonstrated the cytostatic and anti-proliferative activities of 6CN-βCD binary systems and therefore, these might be considered as promising candidates for new anticancer drugs.
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