scholarly journals Antifungal activity of Propranolol against Fusarium keratitis isolates from the Mycotic Ulcer Treatment Trial (MUTT) and the United States

2021 ◽  
Author(s):  
Ruina Bao ◽  
Brandon S. Ross ◽  
Cecilia G. Perez ◽  
Galini Poimenidou ◽  
N. Venkatesh Prajna ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Fungicidal Activity ◽  
Inhibitory Concentration ◽  
The United States ◽  
Fungal Keratitis ◽  
Treatment Trial ◽  
Beta Adrenergic ◽  
Adrenergic Antagonists ◽  
Ulcer Treatment

SYNOPSISBackgroundFusarium keratitis is an infection of the cornea that often results in corneal perforation requiring corneal transplantation even with topical ocular antifungal therapy. The polyene natamycin remains the current antifungal of choice for Fusarium keratitis, but prompt sterilization of the cornea is often not achieved with contemporary therapy. Recently, natamycin synergy with the beta-adrenergic antagonist timolol against Fusarium species was reported.ObjectiveOur objective in this study was to characterize the in vitro antifungal effects of additional beta-adrenergic antagonists alone or in combination with natamycin on Fusarium keratitis isolates from the Mycotic Ulcer Treatment Trial (MUTT) and USA.MethodsMicrobroth dilution assays were used to determine the minimal inhibitory concentration (MIC) of beta-adrenergic antagonists against 18 Fusarium spp. keratitis (10 from MUTT, 8 from USA) and 3 Aspergillus fumigatus isolates. The fractional inhibitory concentration index (FICI) was calculated to assess interactions with natamycin.ResultsMost beta-blockers did not show antifungal activity or synergy with natamycin with the exception of propranolol. A racemic mix of propranolol had fungicidal activity with MIC between 31 and 83 μg/mL for the Fusarium isolates. The MIC of the less cardioactive R enantiomer was lower (27-83 μg/mL) than the MIC of the S enantiomer (42-104 μg/mL). The MICs of both propranolol and natamycin were lower in combination but were not synergistic. The MIC of propranolol was 156 μg/mL for the A. fumigatus isolates.ConclusionsPropranolol has intrinsic in vitro fungicidal activity and lowers the MIC of natamycin. Both the R and S enantiomers of propranolol had antifungal activity with the MIC modestly but significantly lower for R-propranolol. These findings have relevance both for the treatment of fungal keratitis and of glaucoma in the setting of fungal keratitis. Further study of propranolol’s antifungal activity may lead to a novel treatment for fungal keratitis and possibly other fungal infections.Trial RegistrationClinicalTrials.gov Identifier: NCT00997035 (MUTT Trial)

scholarly journals Time-Kill Kinetics of Rezafungin (CD101) in Vagina-Simulative Medium for Fluconazole-Susceptible and Fluconazole-ResistantCandida albicansand Non-albicans CandidaSpecies

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Jeffrey B. Locke ◽  
Amanda L. Almaguer ◽  
Joanna L. Donatelli ◽  
Ken F. Bartizal
Keyword(s):  
Antifungal Activity ◽  
Fungicidal Activity ◽  
Susceptibility Testing ◽  
Inhibitory Concentration ◽  
The Novel ◽  
Testing Conditions ◽  
Fluconazole Resistant ◽  
Time Kill ◽  
Kinetics Of

Background.While echinocandins demonstrate excellent efficacy againstCandidaspecies in disseminated infections and demonstrate potent minimal inhibitory concentration (MIC) values under standard susceptibility testing conditions, investigation under conditions relevant to the vaginal environment was needed. We assessed the antifungal activity and time-kill kinetics of the novel echinocandin rezafungin (formerly CD101) under such conditions, againstCandidaspecies relevant to vulvovaginal candidiasis (VVC).Methods. Susceptibility testing of fluconazole-susceptible and fluconazole-resistantC. albicans,C. glabrata,C. tropicalis,C. parapsilosis, andC. kruseiwas performed in RPMI at pH 7.0 and in vagina-simulative medium (VSM) at pH 4.2 for topical rezafungin, terconazole, fluconazole, and amphotericin B. Time-kill kinetics were evaluated for rezafungin and terconazole at 2, 8, 32, and 128 μg/ml over 72 hours.Results.Rezafungin MIC values were the same or 2-fold higher in VSM/pH 4.2 versus RPMI/pH 7.0. SomeC. albicansterconazole MIC values were lower, but most were significantly higher in VSM than in RPMI. Rezafungin was fungicidal against 11/14 strains and near-fungicidal against the others. Terconazole (128 μg/ml) was fungicidal againstC. kruseiand near-fungicidal against susceptibleC. parapsilosisbut fungistatic versus all other strains evaluated.Conclusion.Rezafungin retained anti-Candidaactivity and fungicidal activity under in vitro conditions relevant to VVC.

Aktivitas Antifungi Air Perasan Bawang Merah (Allium ascalonicum L.) Terhadap Candida albicans Secara In Vitro

2017 ◽  
Vol 9 (2) ◽  
pp. 71
Author(s):  
Nurhasanah Nurhasanah ◽  
Fauzia Andrini ◽  
Yulis Hamidy
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Allium Sativum ◽  
Fungicidal Activity ◽  
Positive Control ◽  
Negative Control ◽  
Randomized Design ◽  
Significant Difference ◽  
Completely Randomized Design

Shallot (Allium ascalonicum L.) has been known as traditional medicine. Shallot which has same genus with garlic(Allium sativum L.) contains allicin that is also found in garlic and has been suspected has fungicidal activity toCandida albicans. It is supported by several researches. Therefore, shallot is suspected has antifungal activity too.The aim of this research was to know antifungal activity of shallot’s water extortion againsts Candida albicans invitro. This was a laboratory experimental research which used completely randomized design, with diffusion method.Shallot’s water extortion was devided into three concentrations, there were 50%, 100% and 200%. Ketoconazole 2%was positive control and aquadest was negative control. The result of this research based on analysis of varians(Anova), there was significant difference between several treatments and was confirmed with Duncan New MultipleRange Test (DNMRT) p<0,05, there was significant difference between 100% shallot’s water extortion with othertreatments, but there was no significant difference between 50% shallot’s water extortion with 200% shallot’s. Theconclusion was shallot’s water extortion had antifungal activity againsts Candida albicans with the best concentration100%, but it was lower than ketoconazole 2%.

scholarly journals A Peptide Found in Human Serum, Derived from the C-Terminus of Albumin, Shows Antifungal Activity In Vitro and In Vivo

2020 ◽  
Vol 8 (10) ◽  
pp. 1627
Author(s):  
Tecla Ciociola ◽  
Pier Paolo Zanello ◽  
Tiziana D’Adda ◽  
Serena Galati ◽  
Stefania Conti ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Human Serum ◽  
Fungicidal Activity ◽  
Galleria Mellonella ◽  
Serum Proteins ◽  
Morphological Alterations ◽  
C Terminus ◽  
Different Sources

The growing problem of antimicrobial resistance highlights the need for alternative strategies to combat infections. From this perspective, there is a considerable interest in natural molecules obtained from different sources, which are shown to be active against microorganisms, either alone or in association with conventional drugs. In this paper, peptides with the same sequence of fragments, found in human serum, derived from physiological proteins, were evaluated for their antifungal activity. A 13-residue peptide, representing the 597–609 fragment within the albumin C-terminus, was proved to exert a fungicidal activity in vitro against pathogenic yeasts and a therapeutic effect in vivo in the experimental model of candidal infection in Galleria mellonella. Studies by confocal microscopy and transmission and scanning electron microscopy demonstrated that the peptide penetrates and accumulates in Candida albicans cells, causing gross morphological alterations in cellular structure. These findings add albumin to the group of proteins, which already includes hemoglobin and antibodies, that could give rise to cryptic antimicrobial fragments, and could suggest their role in anti-infective homeostasis. The study of bioactive fragments from serum proteins could open interesting perspectives for the development of new antimicrobial molecules derived by natural sources.

scholarly journals Triple oral beta-lactam containing therapy for Buruli ulcer treatment shortening

2018 ◽  
Author(s):  
María Pilar Arenaz Callao ◽  
Rubén González del Río ◽  
Ainhoa Lucía Quintana ◽  
Charles J. Thompson ◽  
Alfonso Mendoza-Losana ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Buruli Ulcer ◽  
Mycobacterium Ulcerans ◽  
Beta Lactam ◽  
Beta Lactams ◽  
Amoxicillin Clavulanate ◽  
Low Toxicity ◽  
Potential Use ◽  
Ulcer Treatment

ABSTRACTThe potential use of clinically approved beta-lactams for Buruli ulcer (BU) treatment was investigated with representative classes analyzed in vitro for activity against Mycobacterium ulcerans. Beta-lactams tested were effective alone and displayed a strong synergistic profile in combination with antibiotics currently used to treat BU, i.e. rifampicin and clarithromycin; this activity was further potentiated in the presence of the beta-lactamase inhibitor clavulanate. In addition, quadruple combinations of rifampicin, clarithromycin, clavulanate and beta-lactams resulted in multiplicative reductions in their minimal inhibitory concentration (MIC) values. The MIC of amoxicillin against a panel of clinical isolates decreased more than 200-fold within this quadruple combination. Amoxicillin/clavulanate formulations are readily available with clinical pedigree, low toxicity, and orally and pediatric available; thus, supporting its potential inclusion as a new anti-BU drug in current combination therapies.

scholarly journals Antifungal activity of thymol against clinical isolates of fluconazole-sensitive and -resistant Candida albicans

2009 ◽  
Vol 58 (8) ◽  
pp. 1074-1079 ◽  
Author(s):  
Na Guo ◽  
Jingbo Liu ◽  
Xiuping Wu ◽  
Xingming Bi ◽  
Rizeng Meng ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Concentration Index ◽  
Inhibitory Concentration ◽  
Clinical Isolates ◽  
Standard Strain ◽  
Antagonistic Action ◽  
Microdilution Method ◽  
Interaction Intensity

Thymol (THY) was found to have in vitro antifungal activity against 24 fluconazole (FLC)-resistant and 12 FLC-susceptible clinical isolates of Candida albicans, standard strain ATCC 10231 and one experimentally induced FLC-resistant C. albicans S-1. In addition, synergism was observed for clinical isolates of C. albicans with combinations of THY–FLC and THY–amphotericin B (AMB) evaluated by the chequerboard microdilution method. The interaction intensity was determined by spectrophotometry for the chequerboard assay, and the nature of the interactions was assessed using two non-parametric approaches [fractional inhibitory concentration index (FICI) and ΔE models]. The interaction between THY–FLC or THY–AMB in FLC-resistant and -susceptible strains of C. albicans showed a high percentage of synergism by the FICI method and the ΔE method. The ΔE model gave results consistent with FICI, and no antagonistic action was observed in the strains tested.

In vitro antifungal activity of luliconazole against nondermatophytic moulds

2019 ◽  
Vol 58 (5) ◽  
pp. 703-706 ◽  
Author(s):  
Jun Maeda ◽  
Hiroyasu Koga ◽  
Kou Yuasa ◽  
Daisuke Neki ◽  
Yasuko Nanjoh ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Drug Resistant ◽  
Fusarium Spp ◽  
Microdilution Method ◽  
In Vitro Antifungal Activity

Abstract In vitro antifungal activity of luliconazole against nondermatophytic moulds causing superficial infections was compared with that of five classes of 12 topical and systemic drugs. The minimum inhibitory concentration (MIC) of the drugs against the genera of Neoscytalidium, Fusarium, Aspergillus, Scedosporium, and Alternaria was measured via modified microdilution method. In results, the nondermatophytic moulds were found to be less susceptible to drugs to which Neoscytalidium spp. and Fusarium spp. were typically drug resistant. However, luliconazole was effective against all the genera tested, including afore-mentioned two species, and had the lowest MICs among the drugs tested.

scholarly journals Screening and Application of Chitin Synthase Inhibitors

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1029
Author(s):  
Xiaozai Shi ◽  
Shuo Qiu ◽  
Yingling Bao ◽  
Hanchi Chen ◽  
Yuele Lu ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Chitin Synthase ◽  
Fungal Cell ◽  
Ic50 Value ◽  
Further Development ◽  
Fungicide Target ◽  
Better Than

Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half–inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.

scholarly journals 7-Chloroquinolin-4-yl Arylhydrazone Derivatives: Synthesis and Antifungal Activity

2011 ◽  
Vol 11 ◽  
pp. 1489-1495 ◽  
Author(s):  
Auri R. Duval ◽  
Pedro H. Carvalho ◽  
Maieli C. Soares ◽  
Daniela P. Gouvêa ◽  
Geonir M. Siqueira ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Rational Design ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
First Line ◽  
Minimum Fungicidal Concentration ◽  
Starting Point ◽  
Line Drug ◽  
In Vitro Antifungal Activity

Fifteen 7-chloro-4-arylhydrazonequinolines have been evaluated for their in vitro antifungal activity against eight oral fungi:Candida albicans, C. parapsilosis, C. lipolytica, C. tropicalis, C. famata, C. glabrata, Rhodutorula mucilaginosa, andR. glutinis. Several compounds exhibited minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) activities comparable with the first-line drug fluconazole. These results could be considered as an important starting point for the rational design of new antifungal agents.

scholarly journals Uji Aktivitas Antifungi Ekstrak Rimpang Kencur (Kaempferia galanga L.) Terhadap Saprolegnia sp. Secara In Vitro [Antifungal Activity Test Of Kaempferia galanga L. Extract To Saprolegnia sp. By In Vitro]

2019 ◽  
Vol 5 (1) ◽  
pp. 23
Author(s):  
Rahayu Kusdarwati, Ayu Ratnaningtyas, Dewa Ketut Meles
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Positive Control ◽  
Negative Control ◽  
Fresh Water Fish ◽  
Minimum Fungicidal Concentration ◽  
Kaempferia Galanga ◽  
Activity Test

Abstract Saprolegnia sp. is a fungus that causes the Saprolegniasis disease can infection eggs and fresh water fish. Treatment Saprolegniasis done using chemical drugs, however the use of drugs is bad for the environment and biota. The purpose of the research was to determined the antifungal activity include a minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) from Kaempferia galanga L. to Saprolegnia sp. by in vitro. This research used 9 different concentrations of Kaempferia galanga L extract were 50%, 12.5%, 6.25%, 3.12%, 1.56%, 0.78%, 0, 39%, 0.2%, positive control used H2O2 3% and negative control used DMSO 10%. The results showed that the extract of Kaempferia galanga L had an antifungal activity were inhibits and kill with minimum inhibitory concentration (MIC) was 0.39% equivalen with 3,9 mg/ml and minimu fungicidal concentration (MBC) was 1.56% equivalen with 15,6 mg/ml. The existence of antifungal activity against Saprolegnia sp. by in vitro caused by some active compounds from the extracts of the Kaempferia galanga L. are polyphenolic compounds, flavonoin, saponins and essential oils.

scholarly journals Antifungal Activity of Plumericin and Isoplumericin

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Dharmendra Singh ◽  
Umakant Sharma ◽  
Parveen Kumar ◽  
Yogesh K Gupta ◽  
M. P. Dobhal ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Cryptococcus Neoformans ◽  
Inhibitory Concentration ◽  
Chloroform Extract ◽  
Drug Candidate ◽  
Minimum Fungicidal Concentration ◽  
In Vitro Antifungal Activity

This study evaluated the in vitro antifungal activity of the chloroform extract of Plumeria bicolor and its phytoconstituents plumericin and isoplumericin against Candida species and Cryptococcus neoformans by measuring the Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC). Plumericin's consistently high activity against Candida albicans, C. krusei, C. glabrata, C. tropicalis and Cryptococcus neoformans was more potent than isoplumericin and the standard antifungal drug nystatin suggesting its potential as a drug candidate for candidiasis and cryptococcosis.

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