Antifungal Peptides

                                                                                                                                                                                                                                  Download data

4-methoxy-2,3,6-trimethylbenzensulfonyl-substituted D-octapeptide KN20IC(50) 4 microM) and chemosensitized AD/PDR5(+) to FLC, itraconazole, and ketoconazole, also inhibited the ATPase activity of other ABC transporters, such as Candida albicans Cdr1p (IC(50), 30 microM) and Cdr2p (IC(50), 2 microM), and chemosensitized clinical isolates of pathogenic Candida species and S. cerevisiaeChemosensitization of fluconazole resistance in Saccharomyces cerevisiae and pathogenic fungi by a D-octapeptide derivative15047528
(Ctn[1-14]) and (Ctn[15-34]), C-terminal peptide fragment of crotalicidinActive against pathogenic yeasts, including several Candida species, both clinical isolates and standard strains, with MICs as low as 5 microMLess cytotoxic to healthy HK-2 cells and less hemolytic to human erythrocytes than the standard-of-care amphotericin B Altogether, Ctn and its fragments, particularly Ctn[15-34], are promising leads, either alone or in combined regimen with amphotericin B, for the treatment of fungal diseases. 27876749
A-192411: a novel fungicidal lipopeptide (II)Efficacy demonstrated against Candida albicans In vivo characterization of A-192411: a novel fungicidal lipopeptide (II). The ability of the novel antifungal cyclic hexalipopetide A-192411 to treat fungal infections in rodents is presented.12565958
Analogous cyclic decapeptides produced by Bacillus aneurinolyticusTyrocidine peptide complex (Trc mixture) and purified tyrocidines exhibited minimum inhibition concentrations below 13 microg ml(-1) (around 10 microM) and was significantly more potent than that of the commercial imidazole fungicide, bifonazole Inhibition of agronomically relevant fungal phytopathogens by tyrocidines, cyclic antimicrobial peptides isolated from Bacillus aneurinolyticus.24996824
Antimicrobial peptides from norepinephrine-stimulated skin secretions from the foothill yellow-legged frog Rana boylii [Brevinin-1BYa (FLPILASLAA10KFGPKLF CLV20TKKC), peptides from ranatuerin-2 family temporin family ]Brevinin-1BYa particularly potent against C. albicans [minimal inhibitory concentration (MIC) = 3 microm] and also active against Escherichia coli (MIC = 17 microm) and Staphylococcus aureus (MIC = 2 microm)Strong hemolytic activity (HC50 = 4 microm) Isolation of peptides of the brevinin-1 family with potent candidacidal activity from the skin secretions of the frog Rana boylii. The emergence of strains of the human pathogen Candida albicans with resistance to commonly used antibiotics has necessitated a search for new types of antifungal agents.14531844
APS-1 (Glu, Asp, Tyr, Ser, Thr, Pro, Leu, Ile, Val and an unknown amino acid)Antifungal, strong inhibition on the germination of spores of the phytopathogens testedPurification and characterization of a novel antifungal peptide APS-1 produced by Bacillus cereus12555574
Beta-peptide with fluconazole or ketoconazoleEnhanced the biological activity of these azoles in planktonic and biofilm Candida, and also in a fluconazole-resistant strainOn vitro cytotoxicity of the dual treatment was evaluated towards the human hepatoma cell line, HepG2 Natural antimicrobial peptides, AMPs, in combination with other antifungal agents are a promising avenue to address the prevailing challenges.26470850
biofunctionalized polyelectrolyte multilayered films using CGA 47-66, chromofunginInhibit the growth of yeast Candida albicans by 65% and completely stop the proliferation of filamentous fungus Neurospora crassaCytotoxicity assessed by growing human gingival fibroblasts at its surfaceAntifungal coating by biofunctionalized polyelectrolyte multilayered films.15992921
CD101Potent activity against all Candida isolates tested, including azole-resistant strains, MICs were slightly higher at pH 4 versus 7 and at 48 versus 24 h of incubationIn vitro activity of the novel echinocandin CD101 at pH 7 and 4 against Candida spp. isolates from patients with vulvovaginal candidiasis28158577
Cilofungin (LY-121019), semi-synthetic lipopeptide The minimal inhibitory concentrations of cilofungin for C. albicans (N = 50) ranged from 0.039 to 5.0 micrograms/ml with a geometric mean of 0.47 micrograms/ml.: The same results were obtained with C. tropicalis but one strain showed higher resistance (40 micrograms/ml) suggesting an Eagle effect.: The MIC for T. glabrata ranged from 5.0-40.0 micrograms/ml.: C. parapsilosis and C. krusei were less susceptible (5.0-40.0 micrograms/ml). Susceptibility of Candida species to cilofungin (LY-121019). Torres-Rodriguez JM, Carrillo-Mu?oz A, Gallach-Bau C, Madrenys N. The antifungal activity of a new semi-synthetic lipopeptide named cilofungin (LY-121019) was studied in vitro on 102 strains of Candida and Torulopsis glabrata.2779613
D-beta-naphthylalanine-substituted antimicrobial peptide [P-113, Ac-KWRRWVRWI-NH(2), Pac-525, D-Nal-Pac-525] D-Nal-Pac-525 has the potential of becoming a promising antifungal agent, especially for fungal pathogens with intrinsic resistance to fluconazole Increased potency of a novel D-beta-naphthylalanine-substituted antimicrobial peptide against fluconazole-resistant fungal pathogens.19538482
Dipeptide-based amphiphilesRemarkable growth inhibiting activity on several Gram-positive (minimum inhibitory concentration (MIC)=0.1-10 microg/mL) and Gram-negative (MIC=5-150 microg/mL) bacteria as well as on fungus (MIC=1-50 microg/mL) The results show that the rational designing of short peptide-based cationic amphiphiles might serve as a promising strategy in the development of antimicrobial agents with greater cell specificities.19081951
DS6DS6 is membrane lytic and exhibits antibiofilm activity against Candida tropicalisIn conclusion, DS6 may have utility as an alternative antifungal therapy for C.?tropicalis.28120548
FK463MIC range, <==0.0039 to 2 microg/ml against Candida species and <==0.0039 to 0.0313 microg/ml against Aspergillus species also caused a 99% reduction in viability of C. albicans at concentrations above 0.0156 microg/ml In vitro activities of a new lipopeptide antifungal agent, FK463, against a variety of clinically important fungi. The in vitro antifungal activity and spectrum of FK463 were compared with those of amphotericin B, fluconazole, and itraconazole by using a broth microdilution method specified by National Committee for Clinical Laboratory Standards document M27-A (National Committee for Clinical Laboratory Standards, Wayne, Pa., 1997).10602723
FK463 MIC values of 0.010, 0.011 and 0.015 microg/ml against FLCZ susceptible, FLCZ susceptible-dose dependent and FLCZ resistant Candida albicans, respectively, Aspergillus fumigatus strains were inhibited at 0.0078 microg/ml or lower concentrations In vitro antifungal activity of a novel lipopeptide antifungal agent, FK463, against various fungal pathogens. The antifungal activities of FK463 against various pathogenic fungi were tested by standard broth microdilution methods, and compared with the activities of five currently available antifungal agents; viz., fluconazole (FLCZ), itraconazole, miconazole, amphotericin B and flucytosine.11132964
Hemocyanin-derived (poly)peptides? Antifungal peptides are generated from the C terminus of shrimp hemocyanin in response to microbial challenge. We report here the isolation from plasma of two penaeid shrimp species of novel peptides/polypeptides with exclusive antifungal activities.11598107
Histatin-5 Bioadhesive Hydrogel FormulationTreatment for Oral candidiasis (OC), caused by the fungal pathogen Candida albicans Histatin-5 (Hst-5) specifically has exhibited potent anticandidal activity indicating its potential as an antifungal agent.26596951
Human lactoferrin (hLF) and synthetic peptides representing N terminal cationic domains hLF(1-11) and hLF(21-31)hLF(1-11) more effective in killing fluconazole-resistant Candida albicans than hLF(21-31) and much more effective than lactoferrin Candidacidal activities of human lactoferrin peptides derived from the N terminus. In light of the need for new antifungal agents, the candidacidal activities of human lactoferrin (hLF) and synthetic peptides representing the first, hLF(1-11), and second, hLF(21-31), cationic domains of its N terminus were compared.11083624
Lactoferrin peptide (FKCRRWQWRM, Peptide 2; Pep2)Enhance the candidacidal activity of antifungal drugs by promoting anion channel-associated ATP efflux from Candida cells and decreasing efflux of the drugs, Antimicrobial peptides enhance the candidacidal activity of antifungal drugs by promoting the efflux of ATP from Candida cells. The examined peptides, especially Pep2 and Hst5, enhance the candidacidal activity of antifungal drugs by promoting anion channel-associated ATP efflux from Candida cells and decreasing efflux of the drugs, which could be useful clinical applications.16291868
Lipopeptide Pal-Lys-Lys-NH(2) (PAL)MICs ranged from < or = 0.25 to > 16 microg mL(-1) In vitro activity of the lipopeptide derivative (Pal-Lys-Lys-NH), alone and in combination with antifungal agents, against clinical isolates of dermatophytes. BACKGROUND: An increasing number of antimycotics have become available for the treatment of dermatophytoses; however, there are reports suggesting recalcitrance to therapy or resistance of a dermatophyte against conventional treatment.19438437
Lipopeptides synthesized by conjugating dodecanoic acid (DDA) to the N-termini of 12-mer peptides LXXLLXXLLXXL (L(6)X(6), X = Lys, His, Arg, and all the leucines are d-amino acid enantiomers)Active against both bacteria and fungi pH-dependent antifungal lipopeptides and their plausible mode of action. In this study we synthesized a new group of lipopeptides by conjugating dodecanoic acid (DDA) to the N-termini of 12-mer peptides LXXLLXXLLXXL (L(6)X(6), X = Lys, His, Arg, and all the leucines are d-amino acid enantiomers) and investigated their pH-dependent biological activity and a plausible mode of action by using model phospholipids mimicking bacterial, mammalian, and fungal membranes.16008362
LTX109 (arginine-tertbutyl tryptophan-arginine-phenylethan)Disrupt plasma membrane integrity. S. cerevisiae The synthetic amphipathic peptidomimetic LTX109 is a potent fungicide that disturbs plasma membrane integrity in a sphingolipid dependent manner. 23874964
LY121019, a new echinocandin derivativeStrong anti-Candida activity (in particular against Candida albicans)Low experimental toxicity A study of the antifungal activity of LY121019, a new echinocandin derivative. LY121019 is a cyclic peptide antibiotic of the echinocandin group, which is characterized by strong anti-Candida activity (in particular against Candida albicans) as well as by low experimental toxicity.3288366
LY303366 For amphotericin B-resistant (AF65), LY303366 at 10 and 25 mg/kg/day was superior to amphotericin B at 2 and 5 mg/kg/day in reducing tissue colony counts (P = 0.01 to 0.003), and for B-susceptible (AF210), amphotericin B at 5 mg/kg/day and at 5 mg/kg in four doses was more effective than all four regimens of LY303366 in reducing renal culture counts (P = 0.01 to 0.0001). Efficacy of LY303366 against amphotericin B-susceptible and -resistant Aspergillus fumigatus in a murine model of invasive aspergillosis. LY303366 is a novel antifungal echinocandin with excellent in vitro activity against Aspergillus spp.9559799
MK-0991 (L-743,872)Growth kinetic studies of MK-0991 against Candida albicans and Candida tropicalis isolates showed that the compound exhibited fungicidal activity (i.e., a 99% reduction in viability) within 3 to 7 h at concentrations ranging from 0.06 to 1 microg/ml (0.25 to 4 times the MIC) In vitro preclinical evaluation studies with the echinocandin antifungal MK-0991 (L-743,872). The echinocandin MK-0991, formerly L-743,872, is a water-soluble lipopeptide that has been demonstrated in preclinical studies to have potent activity against Candida spp., Aspergillus fumigatus, and Pneumocystis carinii.9371328
MUC7 D1Activity against azole-sensitive and azole-resistant C. albicans strains The MUC7 D1 candidacidal activity was assessed against azole-sensitive and azole-resistant C. albicans strains and was found, unlike that of the MUC7 D1-15mer, to be comparable with that of Hsn-5, indicating that in addition to Hsn-5, MUC7 D1 could provide an attractive alternative to the classical antifungal agents.11095181
Mucin MUC7-derived peptide and histatin 5Evaluated efficacy in vivo using the experimental model of murine vulvo-vaginal candidiasis Efficacy of human salivary mucin MUC7-derived peptide and histatin 5 in a murine model of candidiasis. MUC7 16-mer (residues 36-51 of human salivary mucin, MUC7) and histatin 5 possess potent in vitro antifungal activity.14659657
Novel Peptides from Skins of AmphibiansThese AMPs contain a C-terminus cyclic motif and most of them show obvious antimicrobial activities against 18 standard and clinically isolated strains of bacteria, including 4 Gram-positive bacteria, 11 Gram-negative bacteria, and 3 fungus. Novel Peptides from Skins of Amphibians Showed Broad-Spectrum Antimicrobial Activities.26452973
P11-6, 11-residue peptide Activity against fluconazole-resistant Candida albicans Antifungal peptides: a potential new class of antifungals for treating vulvovaginal candidiasis caused by fluconazole-resistant Candida albicans.28105725
Pantinin-1, Pantinin-2 and Pantinin-3All the three peptides possess relatively strong activities against Gram-positive bacteria and a fungus, but have very weak antimicrobial activities against Gram-negative bacteria Three new antimicrobial peptides from the scorpion Pandinus imperator.23624072
PMAP-36-derived peptides (18-mer peptide RI18)Exhibited excellent antimicrobial activity against both bacteria and fungiLow haemolytic activity Meanwhile, modification of AMPs is a promising strategy for developing novel antimicrobials to overcome drug-resistance. 27251456
Secreted lipopeptide fractions from Bacillus UCMB5113, together with synthetic peptide mimicsSuppressed growth of several fungal pathogens infecting Brassica plants Analysis by mass spectrometry identified the most potent compounds as novel linear forms of antifungal fengycins, with synthetic peptide mimics confirming the biological activity.28961818
Synthetic CAP37 peptide analogsThree of the peptides demonstrated strong antifungal activity for C. albicans, including fluconazole-resistant isolates of C. albicans and were active against C. guilliermondii, C. tropicalis, C. pseudotropicalis, C. parapsilosis, and C. dubliniensis Candidacidal activity of synthetic peptides based on the antimicrobial domain of the neutrophil-derived protein, CAP37. The primary bactericidal domain of CAP37, a cationic antimicrobial protein with potent activity against Gram-negative organisms was previously shown to reside between amino acids 20 through 44 (NQGRHFCGGALIHARFVMTAASCFQ) of the native protein.19626550
Synthetic cationic antimicrobial tripeptidesStrong general antifungal properties at low micromolar inhibitory concentrations Synthetic mimics of antimicrobial peptides are emerging as a promising class of compounds for antifungal treatment.27576445
Synthetic killer peptide (KP)Impairs Candida albicans biofilm The synthetic killer peptide KP impairs Candida albicans biofilm in vitro. This study provides the first evidence on the KP effectiveness against C. albicans biofilm, suggesting that KP may be considered as a potential novel tool for treatment and prevention of biofilm-related C. albicans infections. 28704490
Synthetic peptides Mo-CBP3-PepI (CPAIQRCC), Mo-CBP3-PepII (NIQPPCRCC), Mo-CBP3-PepIII (AIQRCC), RcAlb-PepI (AKLIPTIA), RcAlb-PepII (AKLIPTIAL), and RcAlb-PepIII (SLRGCC)Synthetic peptides at 50 microg/mL, a concentration 20-fold lower than griseofulvin, reduced the microconidia viability of Trichophyton mentagrophytes and Trichophyton rubrum by 100%Peptides also induced overproduction of reactive oxygen species (ROS) and enhanced the activity of griseofulvin 10-fold against both fungi, suggesting synergistic effects, and eliminated the toxicity of this drug to human erythrocytes.CONCLUSION: Therefore, our results strongly suggest six peptides with high potential to be employed alone as new drugs or as adjuvants to enhance the activity and decrease the toxicity of griseofulvin.32628303
1,3,4-oxadiazole and an endocyclic amine grafted within the peptide backboneAlthough few of the oxadiazole-containing macrocyclic peptides displayed activity against Candida albicans on their own, many increased the efficacy of fluconazole, resulting in a synergistic combination that was independent of efflux inhibition.Combination therapy has the potential to confer enhanced efficacy as well as mitigate the evolution of resistance.32269162
Synthetic antimicrobial peptides (SAMPs) : Mo-CBP3 -PepI (CPAIQRCC) and Mo-CBP3 -PepII (NIQPPCRCC)Anticandidal activity by induced the production of reactive oxygen species (ROS), cell wall degradation, and large poresSynthetic antimicrobial peptides (SAMPs) have attracted substantial attention as alternatives and/or adjuvants in therapeutic treatments due to their strong activity at low concentrations without apparent toxicity.32189445
Peptide gH625 analogue (gH625-M)gH625-M was effective in eradicating persister-derived biofilms both alone and in combination with conventional antifungals in Candida albicansBiofilm formation poses an important clinical trouble due to resistance to antimicrobial agents; therefore, there is an urgent demand for new antibiofilm strategies that focus on the use of alternative compounds also in combination with conventional drugs.32238858
Peptides isolated from the venom of bees and their synthetic analogues (lasioglossins, halictines and hylanines)Naturally occurring antimicrobial peptides and their synthetic analogues are promising candidates for new antifungal drugs.31376220
Rhesus theta defensin-1 (RTD-1)Papidly fungicidal against clinical isolates of MDR C. albicans in vitro. Here we found that RTD-1 was rapidly fungicidal against blastospores of fluconazole/caspofungin resistant C. albicans strains, and was active against established C. albicans biofilms in vitro. In vivo, promoted long term survival in candidemic mice whether infected with drug-sensitive or MDR strains of C. albicansResults of this study suggest that theta-defensins represent a new class of host-directed compounds for treatment of disseminated candidiasis.31729441
G(IIKK)3I-NH2 and (IIKK)3II-NH2G(IIKK)3I-NH2 and (IIKK)3II-NH2 were particularly potent against not only planktonic microbes but also fungal biofilms with low cytotoxicity to host cells.G(IIKK)3I-NH2 and (IIKK)3II-NH2 were particularly potent against not only planktonic microbes but also fungal biofilms with low cytotoxicity to host cells.Natural and synthetic antimicrobial peptides (AMPs) offer potential alternatives but require further development to overcome some of their current drawbacks.34626966
A library of 35 synthetic, linear, ternary polyacrylamides prepared by controlled/living radical polymerizationShort copolymers with a calculated log P of ?1.5 revealed optimal activity against the major human fungal pathogen Candida albicans and other pathogenic fungal speciesLimited toxicity to mammalian host cells (red blood cells and fibroblasts).Remarkably, selected copolymers outperformed the commercial antifungal drug amphotericin B, with respect to the therapeutic index, highlighting their potential as novel antifungal compounds.34060800