title: Inhibition of Candida albicans adhesiveness to human buccal and vaginal cells by sub-inhibitory concentrations of rilopirox.
abstract: Candida albicans is an opportunistic dimorphic pathogenic yeast which is present on the human mucosal epithelial cell surface. Its adhesion is considered to be an important first step in colonization and in the subsequent symptomatic or asymptomatic infection of buccal or vaginal mucosa. Because the ability to adhere is an important element of the pathogenicity of Candida we investigated in this study the compared effects of sub-inhibitory concentrations (sub-MICs) of rilopirox (CAS 104153-37-9) with those of ciclopirox olamine (CAS 41621-49-2) in inhibiting Candida adhesion to human buccal (BEC) and vaginal cells (VEC). Rilopirox is a new hydroxypyridone antimycotic agent with strong activity, especially against Candida albicans. There was a significant reduction in the mean number of Candida adhering to both buccal and vaginal cells with up to 1/8 MIC rilopirox for buccal and 1/16 MIC for vaginal cells, while for ciclopirox olamine reduction was significant up to 1/16 MIC for buccal and 1/8 MIC for vaginal cells. There were no significant differences in the dose-effect curves for BEC and VEC with either rilopirox and ciclopirox olamine, but on a molar basis, rilopirox was more active than ciclopirox olamine. The present in-vitro results support the developmental concept of an oropharyngeal and vaginal preparation of rilopirox. It can be expected that even sub-inhibitory concentrations of rilopirox exert an important additional effect in the treatment of oral and vaginal candidosis by impairing the pathogenic adhesion process of the fungus.
authors.affiliation: Department of Pharmacology, School of Medicine, University of Milan, Italy.
authors.forename: P C
authors.initials: PC
authors.lastname: Braga
authors.forename: M
authors.initials: M
authors.lastname: Dal Sasso
authors.forename: S
authors.initials: S
authors.lastname: Maci
authors.forename: G
authors.initials: G
authors.lastname: Piatti
authors.forename: D R
authors.initials: DR
authors.lastname: Dannhorn
authors.forename: M
authors.initials: M
authors.lastname: Bohn
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D002448:Cell Adhesion / Q000187:drug effects; D002478:Cells, Cultured; D000077768:Ciclopirox; D004847:Epithelial Cells; D004848:Epithelium / Q000187:drug effects; D005260:Female; D006801:Humans; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D009061:Mouth Mucosa / Q000166:cytology* / Q000187:drug effects; D011728:Pyridones / Q000494:pharmacology*; D014621:Vagina / Q000166:cytology* / Q000187:drug effects
chemical_list: D000935:Antifungal Agents; D011728:Pyridones; D000077768:Ciclopirox; C066307:rilopirox