K20 is a novel amphiphilic antifungal @entity4028 that is synthetically derived from the antibiotic @entity7913 . Reported here are investigations of K20's antimicrobial activities, @entity137 , and fungicidal mechanism of action. In vitro growth inhibitory activities against a variety of @entity1 and plant pathogenic @entity375 , filamentous fungi, and bacteria were determined using microbroth dilution assays and time-kill curve analyses, and hemolytic and animal cell cytotoxic activities were determined. Effects on @entity1327 H-99 infectivity were determined with a preventive @entity19 @entity358 model. The antifungal mechanism of action was studied using intact fungal cells, @entity375 lipid mutants, and small unilamellar lipid vesicles. K20 exhibited broad-spectrum in vitro antifungal activities but not antibacterial activities. Pulmonary, single dose-administration of K20 reduced @entity1327 @entity358 rates 4-fold compared to controls. @entity2142 and half-maximal cytotoxicities of @entity1 cells occurred at concentrations that were 10 to 32-fold higher than fungicidal MICs. With @entity2822 ( @entity2823 ), 20-25 mg/L K20 caused staining of >95% of @entity1327 and @entity12069 cells and at 31.3 mg/L caused rapid leakage (30-80% in 15 min) of @entity5384 from preloaded small unilamellar lipid vesicles. K20 appears to be a broad-spectrum fungicide, capable of reducing the infectivity of @entity1327 , and exhibits low hemolytic activity and @entity1 cell toxicity. It perturbs the plasma membrane by mechanisms that are lipid modulated. K20 is a novel amphiphilic @entity4028 amenable to scalable production and a potential lead antifungal for therapeutic and crop protection applications.

Antifungal amphiphilic XXXX K20: bioactivities and mechanism of action.

@entity1 :: ('9606', 'Species') :: ['mammalian', 'human'] @entity137 :: ('MESH:D064420', 'Disease') :: ['cytotoxicity'] @entity7913 :: ('MESH:D007612', 'Chemical') :: ['kanamycin A'] @entity19 :: ('10090', 'Species') :: ['murine'] @entity1327 :: ('5207', 'Species') :: ['C. neoformans', 'Cryptococcus neoformans'] @entity5384 :: ('MESH:C007740', 'Chemical') :: ['calcein'] @entity2822 :: ('CHEBI:37926', 'Chemical') :: ['fluorescein isothiocyanate'] @entity2823 :: ('MESH:D016650', 'Chemical') :: ['FITC'] @entity358 :: ('MESH:D008171', 'Disease') :: ['lung infection'] @entity12069 :: ('5518', 'Species') :: ['Fusarium graminearum'] @entity2142 :: ('MESH:D006461', 'Disease') :: ['Hemolysis'] @entity375 :: ('4932', 'Species') :: ['yeast', 'yeasts'] @entity4028 :: ('CHEBI:47779', 'Chemical') :: ['aminoglycoside']
@entity4028 :: (CHEBI:47779,Chemical) :: ['aminoglycoside']
