scholarly journals In vitro antifungal activities and in vivo efficacies of 1,3-beta-D-glucan synthesis inhibitors L-671,329, L-646,991, tetrahydroechinocandin B, and L-687,781, a papulacandin.

1992 ◽  
Vol 36 (8) ◽  
pp. 1648-1657 ◽  
Author(s):  
K Bartizal ◽  
G Abruzzo ◽  
C Trainor ◽  
D Krupa ◽  
K Nollstadt ◽  
...  
Keyword(s):  
Antifungal Activities ◽  
Glucan Synthesis

scholarly journals Cispentacin, a new antifungal antibiotic. II. In vitro and in vivo antifungal activities.

1989 ◽  
Vol 42 (12) ◽  
pp. 1756-1762 ◽  
Author(s):  
TOSHIKAZU OKI ◽  
MINORU HIRANO ◽  
KOZO TOMATSU ◽  
KEI-ICHI NUMATA ◽  
HIDEO KAMEI
Keyword(s):  
Antifungal Activities ◽  
Antifungal Antibiotic

scholarly journals Current status of in vitro and in vivo antifungal activities of posaconazole

2013 ◽  
Vol 1 (1) ◽  
pp. 18-22
Author(s):  
He Sun ◽  
Xin Su ◽  
Yi Shi
Keyword(s):  
Animal Models ◽  
Broad Spectrum ◽  
Fungal Infections ◽  
Current Status ◽  
Dimorphic Fungi ◽  
Antifungal Activities ◽  
Endemic Fungi ◽  
Yeasts And Molds

Abstract Posaconazole (POS) is a new triazole drug with broad-spectrum in vitro activity against most yeasts and molds such as Candida, Cryptococcus neoformans, Aspergillus, Fusarium and Zygomycetes, as well as certain species of dimorphic fungi and endemic fungi. In immunocompetent or immunocompromised animal models with invasive fungal infections, POS has demonstrated highly effective, broad-spectrum antifungal activities. In vitro and in vivo antifungal activities of POS were superior to those of other azoles against Candida glabrata, Candida krusei, Aspergillus terrus, Fusarium and Zygomycetes. In vivo susceptibility studies have shown promising efficacy of POS against life-threatening fungal infections in animal models with different immune status and infection sites.

scholarly journals Chemical characterization and determination of in vivo and in vitro antifungal activity of essential oils from four Eucalyptus species against the Hemileia vastatrix Berk and Br fungus, the agent of coffee leaf rust

2020 ◽  
pp. 1379-1384
Author(s):  
Alex Rodrigues Silva Caetano ◽  
Sara Maria Chalfoun ◽  
Mario Lúcio Vilela Resende ◽  
Caroline Lima Angélico ◽  
Wilder Douglas Santiago ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Chemical Characterization ◽  
Eucalyptus Species ◽  
Hemileia Vastatrix ◽  
Antifungal Activities

Essential oils, also known as volatile oils, are substances produced through the secondary metabolism of plants. In this study, we determined the chemical composition and the in vitro and in vivo antifungal activity of the essential oils from four species of Eucalyptus, Eucalyptus citriodora, Eucalyptus camaldulensis, Eucalyptus grandis and Eucalyptus microcorys, against the Hemileia vastatrix fungus. The essential oils from these four species of Eucalyptus were extracted from their leaves by the hydrodistillation technique using a modified Clevenger apparatus. The chemical characterization was performed by gas chromatography coupled with a mass spectrometer detector and by gas chromatography using a flame ionization detector. The antifungal activities of the essential oils against H. vastatrix were studied by evaluating the percentage of spore germination using the microdilution test for in vitro assays. The curative and preventive effects were evaluated in in vivo tests. The principal constituents of the essential oil from E. citriodora were citronellal, citronellol and isopulegol, while E. camaldulensis produced 1,8-cineole, α-terpineol and α-pinene. 1,8-cineole, α-pinene and α-terpineol were obtained from E. grandis and 1,8-cineole, α-pinene and trans-pinocarveol were the principal components in the essential oil of E. microcorys. In vitro and in vivo antifungal activities against the fungus under study were observed for most of the essential oils, except the essential oil from E. microcorys, for which no preventive antifungal activity was observed. Only the curing of infection by the H. vastatrix fungus was observed with this oil.

Correlation between In Vitro and In Vivo Antifungal Activities in Experimental Fluconazole-Resistant Oropharyngeal and Esophageal Candidiasis

2000 ◽  
Vol 38 (6) ◽  
pp. 2369-2373
Author(s):  
Thomas J. Walsh ◽  
Corina E. Gonzalez ◽  
Steven Piscitelli ◽  
John D. Bacher ◽  
Joanne Peter ◽  
...  
Keyword(s):  
Esophageal Candidiasis ◽  
Antifungal Activities ◽  
Fluconazole Resistant

scholarly journals Application of Dithiocarbamates as Potential New Antitrypanosomatids-Drugs: Approach Chemistry, Functional and Biological

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2806 ◽  
Author(s):  
Johny Wysllas de Freitas Oliveira ◽  
Hugo Alexandre Oliveira Rocha ◽  
Wendy Marina Toscano Queiroz de Medeiros ◽  
Marcelo Sousa Silva
Keyword(s):  
Chagas Disease ◽  
Biomedical Applications ◽  
In Vitro Models ◽  
African Trypanosomiasis ◽  
Pharmacological Activities ◽  
Antifungal Activities ◽  
Pharmacological Control

Dithiocarbamates represent a class of compounds that were evaluated in different biomedical applications because of their chemical versatility. For this reason, several pharmacological activities have already been attributed to these compounds, such as antiparasitic, antiviral, antifungal activities, among others. Therefore, compounds that are based on dithiocarbamates have been evaluated in different in vivo and in vitro models as potential new antimicrobials. Thus, the purpose of this review is to present the possibilities of using dithiocarbamate compounds as potential new antitrypanosomatids-drugs, which could be used for the pharmacological control of Chagas disease, leishmaniasis, and African trypanosomiasis.

scholarly journals Combination Therapy with Ibrexafungerp (Formerly SCY-078), a First-in-Class Triterpenoid Inhibitor of (1→3)-β-D-Glucan Synthesis, and Isavuconazole for Treatment of Experimental Invasive Pulmonary Aspergillosis

2020 ◽  
Vol 64 (6) ◽  
Author(s):  
Vidmantas Petraitis ◽  
Ruta Petraitiene ◽  
Aspasia Katragkou ◽  
Bo Bo Win Maung ◽  
Ethan Naing ◽  
...  
Keyword(s):  
Invasive Pulmonary Aspergillosis ◽  
Rabbit Model ◽  
Prolonged Survival ◽  
Pulmonary Aspergillosis ◽  
Fungal Burden ◽  
Treatment Groups ◽  
Glucan Synthesis ◽  
Synthase Inhibitor

ABSTRACT Ibrexafungerp (formerly SCY-078) is a semisynthetic triterpenoid and potent (1→3)-β-d-glucan synthase inhibitor. We investigated the in vitro activity, pharmacokinetics, and in vivo efficacy of ibrexafungerp (SCY) alone and in combination with antimold triazole isavuconazole (ISA) against invasive pulmonary aspergillosis (IPA). The combination of ibrexafungerp and isavuconazole in in vitro studies resulted in additive and synergistic interactions against Aspergillus spp. Plasma concentration-time curves of ibrexafungerp were compatible with linear dose proportional profile. In vivo efficacy was studied in a well-established persistently neutropenic New Zealand White (NZW) rabbit model of experimental IPA. Treatment groups included untreated control (UC) rabbits and rabbits receiving ibrexafungerp at 2.5 (SCY2.5) and 7.5 (SCY7.5) mg/kg of body weight/day, isavuconazole at 40 (ISA40) mg/kg/day, or combinations of SCY2.5+ISA40 and SCY7.5+ISA40. The combination of SCY+ISA produced an in vitro synergistic interaction. There were significant in vivo reductions of residual fungal burden, lung weights, and pulmonary infarct scores in SCY2.5+ISA40, SCY7.5+ISA40, and ISA40 treatment groups versus those of the SCY2.5-treated, SCY7.5-treated, and UC (P < 0.01) groups. Rabbits treated with SCY2.5+ISA40 and SCY7.5+ISA40 had prolonged survival in comparison to that of the SCY2.5-, SCY7.5-, ISA40-treated, or UC (P < 0.05) groups. Serum galactomannan index (GMI) and (1→3)-β-d-glucan levels significantly declined in animals treated with the combination of SCY7.5+ISA40 in comparison to those of animals treated with SCY7.5 or ISA40 (P < 0.05). Ibrexafungerp and isavuconazole combination demonstrated prolonged survival, decreased pulmonary injury, reduced residual fungal burden, and lower GMI and (1→3)-β-d-glucan levels in comparison to those of single therapy for treatment of IPA. These findings provide an experimental foundation for clinical evaluation of the combination of ibrexafungerp and an antimold triazole for treatment of IPA.

scholarly journals Improved Cell Selectivity of Pseudin-2 via Substitution in the Leucine-Zipper Motif: In Vitro and In Vivo Antifungal Activity

Antibiotics ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 921
Author(s):  
Seong-Cheol Park ◽  
Heabin Kim ◽  
Jin-Young Kim ◽  
Hyeonseok Kim ◽  
Gang-Won Cheong ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Leucine Zipper ◽  
Pathogenic Fungi ◽  
Repeated Sequence ◽  
Antimicrobial Activities ◽  
Leucine Zipper Motif ◽  
Antifungal Activities ◽  
Cell Selectivity

Several antimicrobial peptides (AMPs) have been discovered, developed, and purified from natural sources and peptide engineering; however, the clinical applications of these AMPs are limited owing to their lack of abundance and side effects related to cytotoxicity, immunogenicity, and hemolytic activity. Accordingly, to improve cell selectivity for pseudin-2, an AMP from Pseudis paradoxa skin, in mammalian cells and pathogenic fungi, the sequence of pseudin-2 was modified by alanine or lysine at each position of two amino acids within the leucine-zipper motif. Alanine-substituted variants were highly selective toward fungi over HaCaT and erythrocytes and maintained their antifungal activities and mode of action (membranolysis). However, the antifungal activities of lysine-substituted peptides were reduced, and the compound could penetrate into fungal cells, followed by induction of mitochondrial reactive oxygen species and cell death. In vivo antifungal assays of analogous peptide showed excellent antifungal efficiency in a Candida tropicalis skin infection mouse model. Our results demonstrated the usefulness of selective amino acid substitution in the repeated sequence of the leucine-zipper motif for the design of AMPs with potent antimicrobial activities and low toxicity.

Chemical Composition and Combinatory Antifungal Activities of Ammoides verticillata, Allium sativum and Curcuma longa Essential Oils Against Four Fungi Responsible for Tomato Diseases

2020 ◽  
Vol 23 (3) ◽  
pp. 196-204 ◽  
Author(s):  
Hanane Senouci ◽  
Nassira G. Benyelles ◽  
Mohammed E.A. Dib ◽  
Jean Costa ◽  
Alain Muselli
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Allium Sativum ◽  
Curcuma Longa ◽  
Antifungal Effect ◽  
Antifungal Activities ◽  
Ammoides Verticillata

Background: Tomato is considered a model plant in genetics and is one of the most economically important crops of all those that exist in the world. Several species of fungi are reported on tomato fruit, causing damage both during cultivation and after harvest. Some of the appropriate actions that could be initiated to resolve the problem are to develop and search for new antimicrobial substances isolated from the bioactive natural products, such as essential oils. Aim and Objective: The aim of this work was to determine the chemical composition of essential oils of Ammoides verticillata, Allium sativum and Curcuma longa, to evaluate their in-vitro antifungal activities and in-vivo antifungal effect of essential oils to prevent the diseases caused by tomato. Materials and Methods: The essential oils obtained from aerial parts of plants were analyzed by GC/MS and tested for their antifungal activities against Penicillium expansum, Fusarium solani, Rhizopus stolonifer and Alternaria alternata using the radial growth technique method. The effectiveness in-vivo of the association between Allium sativum and Curcuma longa essential oils was also investigated on tomatoes inoculated by fungi. Results: The essential oil from A. verticilata was mainly composed of phenolic compounds (54.4%), the A. sativum oil was mainly composed of sulfur compounds (91.5%) and C. longa oil was dominated by oxygenated monoterpenes (82.0%). The obtained results in-vitro antifungal revealed that individual essential oils of A. verticillata and A. sativum were more active than the essential oil of C. longa against all screened microorganisms. An important antifungal effect of A. sativum and C. longa essential oils blend was obtained against P. expansum (100%), F. solani (95.2%), R. stolonifer (95.1%) and A. alternata (48.5%). Furthermore, A. sativum and C. longa essential oils blends have demonstrated promising in-vivo antifungal activity to control infection of tomato against P. expansum and R. stolonifer. Conclusion: A. sativum and C. longa essential oil blends can be used as a natural food preservative and alternative to chemical fungicides to protect stored tomato against many phytopathogens.

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