Abstract
A new set of compounds containing indole nucleus appended with carefully selected amino acids via a triazole linker are identified. These compounds showed substantial antifungal activities against the BWP17 strain of candida albicans. The preliminary screening of the compounds was done by docking in the active site of lanosterol 14-α demethylase enzyme (pdb ID - 3JUS) with ArgusLab.exe software. Subsequently the screened compounds were subjected to in-vivo antifungal assays. The probable mechanism of action of the test compounds was studied by GC analysis of the membrane metabolites. The compounds with tryptophan and histidine substitution were found to be most effective with MIC80 of 50.2 μg/ml and 78.81 μg/ml respectively. In the fungal cells treated with compound 3b the lanosterol levels were found to increase indicating that lanosterol 14-α demethylase enzyme could be the probable target. Additionally, the R6G influx/efflux assay provided the evidence for the fungicidal properties of the test compounds.
Highlights
Diseases caused by fungus are one of the major global challenges today
Ten successive dilutions of the test compounds were prepared alongwith the solvent control with yeast extract peptone dextrose (YEPD) medium in a 96-well plate
The overnight grown cells of the BWP 17 strain of the fungus Candida Albicans were resuspended in a 0.9% saline solution to give a resultant optical density of 0.1 at a wavelength of 570 nm (OD570) These cells were further diluted 100 times in SDM medium. 100 μl of these diluted cells were added to each of the wells in the 96 well plate except the column 11 which was taken as media control to examine any kind of contamination while performing the assay
Summary
Diseases caused by fungus are one of the major global challenges today. Starting from local infections to systemic mycosis the fungi are causing more deaths compared to malaria and tuberculosis. [4-(3-Methyl-indol-1-ylmethyl)-[1,2,3]triazol-1-yl]-acetic acid (3a): The compound (2) was dissolved in 9:1 solution of EtOH:H2O and allowed to stir till a clear solution is obtained.
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