title: Evaluation of the biological effects of 5-Cl-8-oxyquinolinepropoxycalix[4]arene and 8-oxyquinolinepropoxycalix[4]arene in vitro and in vivo.
abstract: 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 24h 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 24h culture with a reduction of yeast cells.
authors.affiliation: Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua Prof. Arthur Riedel, 275, CEP 09972-270, Diadema, SP, Brazil.
authors.forename: Marcos N
authors.initials: MN
authors.lastname: Soares
authors.affiliation: Fundação do ABC, Faculdade de Medicina, Av. Príncipe de Gales, 821, CEP 09060-650, Santo André, SP, Brazil.
authors.forename: Thais M
authors.initials: TM
authors.lastname: Gáscon
authors.affiliation: Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua Prof. Arthur Riedel, 275, CEP 09972-270, Diadema, SP, Brazil; Fundação do ABC, Faculdade de Medicina, Av. Príncipe de Gales, 821, CEP 09060-650, Santo André, SP, Brazil.
authors.forename: Fernando L A
authors.initials: FL
authors.lastname: Fonseca
authors.affiliation: Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua Prof. Arthur Riedel, 275, CEP 09972-270, Diadema, SP, Brazil.
authors.forename: Karen S
authors.initials: KS
authors.lastname: Ferreira
authors.affiliation: Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua Prof. Arthur Riedel, 275, CEP 09972-270, Diadema, SP, Brazil. Electronic address: ibagatin@unifesp.br.
authors.forename: Izilda A
authors.initials: IA
authors.lastname: Bagatin
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D047250:Calixarenes / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D002176:Candida albicans / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D016207:Cytokines / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D015125:Oxyquinoline / Q000737:chemistry*; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000935:Antifungal Agents; D016207:Cytokines; D010636:Phenols; C121325:calix(4)arene; D047250:Calixarenes; D015125:Oxyquinoline
keywords: 8-Hydroxiquinoline; Calix[4]arene; Cytotoxicity effect; Fungicidal activity; Iron depletion