Evaluation of the biological effects of 5-Cl-8-oxyquinolinepropoxycalix[4]arene and 8-oxyquinolinepropoxycalix[4]arene in vitro and in vivo

• Remarkable cytotoxicity and fungicidal activities of (A) and (B) ligands.
• Slight inflammation were observed of A and B ligands in blood of Wistar male rats.
• The substance A depicted a potential microbicide effect against C. albicans.

The development of antibacterial and antifungal drugs has been the target of several pharmaceutical and chemical industries mainly due to the lack of effective drugs with low or no side effect. In this work, studies were conducted both in vitro and in vivo with 8-oxyquinolinepropoxycalix[4]arene (A) and 5-Cl-8-oxyquinolinepropoxycalix[4]arene (B) ligands, showing fairly good results. Cytotoxicity and fungicidal actions of compounds A and B were determined in Wistar male rats and peritoneal macrophages of mice. A slight change in the total of leukocytes and erythrocytes was observed on the hematologic assays, showing almost no inflammation after using both compounds in Wistar male rats. We have also noted some, but not significant, alteration in liver enzymes representing modest hepatotoxicity. Cytotoxicity of peritoneal macrophages, in the presence of compound A or B, showed 50% of survival of macrophages. On the other hand, macrophages previously infected with Candida albicans and treated with substance A or B exhibited an increased cytokine IL-10 at 24 h incubation. By checking the effect of substance A or B on growing C. albicans, the results pointed that these substances revealed antifungal activity against C. albicans, in 24 h culture with a reduction of yeast cells.

Substance A has better fungicidal activity than substance B, which represents a potential microbicide effect of these compounds.Figure optionsDownload as PowerPoint slide