Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells

Journal of the Brazilian Chemical Society

article

Amaro, Bolivar R.¹  Denadai, Ângelo M. L.¹  Castro, Sandra B. R.¹  Alves, Caio C. S.²  Ferreira, Gabriella F.¹  Carvalho, Paloma E.¹  Silva, Jeferson G. da¹  Souza, Cleonice A.¹  Cardoso Jr., Oswaldo²  Carli, Alessandra P.²  Machado, Fabiana S.³ 

[1] Instituto de Ciências da Vida, Universidade Federal de Juiz de Fora;Universidade Federal dos Vales do Jequitinhonha e Mucuri;Departamento de Bioquímica e Imunologia, Universidade Federal de Minas Gerais

关键词: complexation;    MTT;    flow cytometry;    toxicity;    MIC;   

DOI  :  10.21577/0103-5053.20200145

学科分类：内科医学

来源: SciELO

【 摘 要 】

The ofloxacin (OFLOX) is a second-generation synthetic antibiotic that can be classified as a multifunctional drug, but is a poorly soluble drug, which influences its efficiency. The inclusion complexes of OFLOX with β-cyclodextrin (βCD) or hydroxypropyl-β-cyclodextrin (HPβCD) can improve the chemical characteristics of the drug; however, studies showing the biological activity of these inclusion complexes are still scarce. The present work aimed to investigate the multifunctionality of the OFLOX and their inclusion complexes. Thus, the 1:1 βCD/OFLOX or HPβCD/OFLOX were prepared and analyzed by Fourier transform infrared spectroscopy (FTIR), thermogravimetric and differential thermal analysis (TGA and DTA), 1 H nuclear magnetic resonance (NMR) and isothermal titration calorimetry (ITC). The antitumor and antibacterial effects were assessed. The results confirm the formation of the inclusion complexes, which had lower minimum inhibitory concentration (MIC) values, higher cytotoxicity and promoted the apoptosis. The present study showed, for the first time, the promising effects of the inclusion complexes as antitumor, improving the biological activities of the uncomplexed ofloxacin.

【 授权许可】

CC BY