Preparation, characterizations and evaluation of antifungal activity of eugenol-linalool emulgel against anthrophilic dermatophytic trichophyton rubrum

2021 ◽  
pp. 1-15
Author(s):  
Abdullah Akram ◽  
Muhammad Khalid Khan ◽  
Barkat Ali Khan
Keyword(s):  
Antifungal Activity ◽  
Skin Infection ◽  
Trichophyton Rubrum ◽  
Sem Analysis ◽  
Antifungal Drugs ◽  
In Vivo Studies ◽  
Stability Studies ◽  
Antifungal Activities

Trichophyton rubrum (T. Rubrum) is responsible for chronic cases of dermatophytosis which have high rates of resistance to antifungal drugs worldwide. The aim of this study was to formulate an emulgel of Eugenol-Linalool for the treatment of T. Rubrum infections. The emulgel was prepared by slow emulsification method and characterized for physical examination, pH analysis, swelling index, stability studies, spreading coefficient, SEM analysis, thermal analysis and PXRD studies. In-vitro antifungal activities were performed by growing T. rubrum on specialized media in petri dishes. In-vivo antifungal activity was performed in rabbits by inducing the skin infection by application of fungal strain. Results indicated that the emulgel formulation is highly stable and the physical properties of the emulgel remained quite feasible. No deterioration was observed in the formulation and the pH remained the same as the pH of skin. The viscosity and spreadability of the emulgel remained highly compatible. The results of in vitro and in vivo studies indicated that the Eugenol and Linalool both inhibited the growth of T. rubrum. Eugenol was more effective in inhibition of zone (38±0.01 mm) of T. rubrum as compared to Linalool (32.9±0.03 mm). Similarly it was observed that when the combination of both Linalool and Eugenol was used, the growth of T. rubrum (42±0.01 mm) was significantly (P <  0.05) inhibited. It is hence concluded that the emulgel containing Eugenol and Linalool possess strong in vitro and in vivo antifungal activities against the commercial strains of anthrophilic dermophytic T. Rubrum.

scholarly journals IN VITRO AND IN VIVO ANTIFUNGAL ACTIVITY OF ALKALOID 3,5-bis(4,4’’-dimethoxy- [1,1’:2’,1’’-terphenyl]-4’-yl)-4H-pyrazole-4,4-diol FROM DERRIS INDICA (LAM) BENNETT SEEDS

2021 ◽  
pp. 133-140
Author(s):  
NUZHAT TABASSUM ◽  
VIDYASAGAR G. M. ◽  
RAGHUNANDAN D ◽  
SHIVAKUMAR I
Keyword(s):  
Antifungal Activity ◽  
Fungal Pathogens ◽  
Antifungal Drugs ◽  
Hexane Extract ◽  
In Vivo Studies ◽  
Antifungal Compound ◽  
In Vivo Evaluation ◽  
Derris Indica

Objectives: The aim of the present study is to isolate an antifungal compound from Derris indica (Lam) Bennett seed oil with various solvents and evaluation of its antifungal activity against the clinical species of Candida. Methods: D. indica seed hexane extract was tested against Trichophyton rubrum, Trichophyton tonsurans and Candida albicans. Hexane extract was fractioned using different solvents through column chromatography (CC). Isolated compound D1 was identified and characterized using ultraviolet, Fourier-transform infrared, 1HNMR, and mass spectroscopy. In vitro evaluation of D1 carried out against 12 Candida strains. In vivo evaluation of D1 carried out against T. rubrum, T. tonsurans, and C. albicans using an excision wound healing model on male Wistar rats. Results: Different concentrations of hexane extract showed antimicrobial activity against tested microorganism with varying minimum inhibitory concentration values. On fractionation with hexane-petroleum ether through CC, it yielded a crystalline fraction. Compound D1 characterized as a 3,5-bis (4,4’’-dimethoxy-[1,1’: 2’,1’’-terphenyl]-4’-yl)-4H-pyrazole-4,4-diol. A novel alkaloid compound from D. indica is a new report and proved to be inhibitory against C. albicans MTCC 3017 (14.83±0.28), MTCC 1637 (16.0±0.0), Candida glabrata MTCC 3814 (16.83±0.28) and MTCC 3014 (16.66±0.57), Candida tropicalis MTCC 230 (20.0±0.0), MTCC 1406 (12.33±0.57). C. glabrata MTCC 3981 was found to be resistant to the compound. In vivo studies showed no visual symptoms at the end of treatment indicating the therapeutic property of the compound. Conclusion: The D1 was found to be effective against human fungal pathogens and can be used as a base molecule in designing new antifungal drugs.

scholarly journals Non-toxic Cobalt(III) Schiff Base Complexes with Broad Spectrum Antifungal Activity

2020 ◽  
Author(s):  
Angelo Frei ◽  
A. Paden King ◽  
Gabrielle J. Lowe ◽  
Amy K. Cain ◽  
Francesca L. Short ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antifungal Activity ◽  
Broad Spectrum ◽  
Bacterial Infections ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Schiff Base Complexes ◽  
In Vivo Studies

Resistance to currently available antifungal drugs has quietly been on the rise but overshadowed by the alarming spread of antibacterial resistance. There is a striking lack of attention to the threat of drug resistant fungal infections, with only a handful of new drugs currently in development. Given that metal complexes have proven to be useful new chemotypes in the fight against diseases such as cancer, malaria, and bacterial infections, it stands to reason to explore their possible utility in treating fungal infections. Herein we report a series of cobalt(III) Schiff base complexes with broad spectrum antifungal activity. Some of these complexes (1-3) show minimum inhibitory concentrations (MIC) in the low micro- to nanomolar range against a series of Candida and Cryptococcus yeasts. Additionally, we demonstrate that these compounds show no cytotoxicity against both bacterial and human cells. Finally, we report first in vivo toxicity data on these compounds in Galleria mellonella, showing that doses as high as 266 mg/kg are tolerated without adverse effects, paving the way for further in vivo studies of these complexes. <br>

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.

scholarly journals The celecoxib derivative AR-12 has broad spectrum antifungal activity in vitro and improves the activity of fluconazole in a murine model of cryptococcosis

2016 ◽  
pp. AAC.01061-16 ◽  
Author(s):  
Kristy Koselny ◽  
Julianne Green ◽  
Louis DiDone ◽  
Justin P. Halterman ◽  
Annette W. Fothergill ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Small Molecules ◽  
Broad Spectrum ◽  
Murine Model ◽  
Antifungal Drugs ◽  
Dimorphic Fungi ◽  
New Class ◽  
Cancer Agent

Only one new class of antifungal drugs has been introduced into clinical practice in the last thirty years and, thus, the identification of small molecules with novel mechanisms of action is an important goal of current anti-infective research. Here, we describe the characterization of the spectrum of in vitro activity and in vivo activity of AR-12, a celecoxib-derivative which has been tested in a Phase I clinical trial as an anti-cancer agent. AR-12 inhibits fungal acetyl CoA synthetase in vitro and is fungicidal at concentrations similar to those achieved in human plasma. AR-12 has a broad spectrum of activity including active against yeasts (e.g.,C. albicans, non-albicansCandidaspp.,C. neoformans); molds (e.g.,Fusarium,Mucor), and dimorphic fungi (Blastomyces,Histoplasma, andCoccidioides) with minimum inhibitory concentrations of 2-4 μg/mL. AR-12 is also active against azole- and echinocandin-resistantCandidaisolates and sub-inhibitory AR-12 concentrations increase susceptibility of fluconazole- and echinocandin-resistantCandidaisolates. Finally, AR-12 also increases the activity of fluconazole in a murine model of cryptococcosis. Taken together, these data indicate that AR-12 represents a promising class of small molecules with broad spectrum antifungal activity.

scholarly journals Strong Antifungal Activity of SS750, a New Triazole Derivative, Is Based on Its Selective Binding Affinity to Cytochrome P450 of Fungi

2002 ◽  
Vol 46 (2) ◽  
pp. 308-314 ◽  
Author(s):  
Masaru Matsumoto ◽  
Kazuya Ishida ◽  
Akihiro Konagai ◽  
Kazunori Maebashi ◽  
Takemitsu Asaoka
Keyword(s):  
Cytochrome P450 ◽  
Antifungal Activity ◽  
In Vivo Studies ◽  
Dependent Manner ◽  
Strong Affinity ◽  
Dose Dependent ◽  
Potent Inhibitory Activity ◽  
In Vitro Antifungal Activity

ABSTRACT SS750 [(R)-(−)-2-(2,4-difluorophenyl)-1-(ethylsulfonyl)-1,1-difluoro-3-(1H-1,2,4-triazol-1-yl)-2-propanol] is a new triazole, and its potential as an antifungal agent was evaluated by in vitro and in vivo studies. In a comparison of the MICs at which 50% of isolates are inhibited (MIC50s) for all strains of Candida species and Cryptococcus neoformans tested, SS750 was four times or more active than fluconazole and had activity comparable to that of itraconazole. The most important advantage of SS750 was that, when the MIC90s were compared, SS750 had 64 and 32 times greater antifungal activities than fluconazole against Candida krusei and Candida glabrata, respectively, which are intrinsically less susceptible to fluconazole. In cyclophosphamide-immunosuppressed mouse models of systemic and pulmonary candidiasis caused by C. albicans, oral SS750 prolonged the number of days of survival of infected animals in a dose-dependent manner and was 4 and ≥64 times more potent than fluconazole and itraconazole, respectively. In a safety profile, SS750, like fluconazole, had less of an affinity for binding to mammalian cytochrome P450 compared with that of ketoconazole, despite its strong affinity for binding to fungal cytochrome P450. The mechanism for the increased in vitro antifungal activity of SS750 against C. krusei is partially due to the potent inhibitory activity (3.7 times versus that of fluconazole) of C. krusei cytochrome P450 sterol 14α-demethylase; SS750 showed a strong affinity for binding to cytochrome P450 of C. krusei, indicating that SS750 acts by inhibiting the cytochrome P450 sterol 14α-demethylase of fungal cells.

scholarly journals Antifungal Activity and Potential Mechanism of 6,7, 4′-O-Triacetylscutellarein Combined With Fluconazole Against Drug-Resistant C. albicans

2021 ◽  
Vol 12 ◽  
Author(s):  
Liu-Yan Su ◽  
Guang-Hui Ni ◽  
Yi-Chuan Liao ◽  
Liu-Qing Su ◽  
Jun Li ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Signaling Pathway ◽  
Treatment Method ◽  
Inhibitory Effect ◽  
Antifungal Drugs ◽  
Infection Model ◽  
Drug Resistant ◽  
Mycelium Growth

The increased resistance of Candida albicans to conventional antifungal drugs poses a huge challenge to the clinical treatment of this infection. In recent years, combination therapy, a potential treatment method to overcome C. albicans resistance, has gained traction. This study assessed the effect of 6,7,4′-O-triacetylscutellarein (TA) combined with fluconazole (FLC) on C. albicans in vitro and in vivo. TA combined with FLC showed good synergistic antifungal activity against drug-resistant C. albicans in vitro, with a partial inhibitory concentration index (FICI) of 0.0188–0.1800. In addition, the time-kill curve confirmed the synergistic effect of TA and FLC. TA combined with FLC showed a strong synergistic inhibitory effect on the biofilm formation of resistant C. albicans. The combined antifungal efficacy of TA and FLC was evaluated in vivo in a mouse systemic fungal infection model. TA combined with FLC prolonged the survival rate of mice infected with drug-resistant C. albicans and reduced tissue invasion. TA combined with FLC also significantly inhibited the yeast-hypha conversion of C. albicans and significantly reduced the expression of RAS-cAMP-PKA signaling pathway-related genes (RAS1 and EFG1) and hyphal-related genes (HWP1 and ECE1). Furthermore, the mycelium growth on TA combined with the FLC group recovered after adding exogenous db-cAMP. Collectively, these results show that TA combined with FLC inhibits the formation of hyphae and biofilms through the RAS-cAMP-PKA signaling pathway, resulting in reduced infectivity and resistance of C. albicans. Therefore, this study provides a basis for the treatment of drug-resistant C. albicans infections.

DESIGN OF PRONIOSOMAL GEL CONTAINING EUGENOL AS AN ANTIFUNGAL AGENT FOR THE TREATMENT OF ORAL CANDIDIASIS

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (09) ◽  
pp. 55-57
Author(s):  
T. S Vishnu ◽  
◽  
A. Dubey ◽  
G.S Ravi ◽  
S. Hebbar
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Release Kinetics ◽  
Oral Candidiasis ◽  
In Vivo Studies ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
Release Study

The objective of this study was to design and investigate the antifungal activity of proniosomal gel of eugenol for the treatment of oral candidiasis. The proniosomal gel was prepared by coacervation phase separation method using different surfactants like spans 20, 60, 80, soya lecithin and cholesterol. The proniosomal gel formulations were evaluated for visual inspection, pH detection, viscosity, spreadability, in vitro drug release and kinetics study, and in vivo studies. The compatibility study indicated that the drug and the excipients were compatible with each other. The results showed that pH, viscosity and spreadability were all acceptable for topical preparation. In vitro drug release study and drug release kinetics were conducted to check the release study and drug release patterns of the formulation. Amongst the formulations, an optimized formulation was selected to conduct an in vivo study. Candida albicans was used to induce oral candidiasis for the evaluation of therapeutic efficacy of proniosomal gel in immunosuppressed rats. Activity was analysed by microbiological and histopathological techniques and was compared with the marketed product. It is evident from the study that the proniosomal gel shows sustained release trend with strong antifungal activity.

Carvacrol essential oil stimulates growth performance, immune response, and tolerance of Nile tilapia to Cryptococcus uniguttulatus infection

2020 ◽  
Vol 141 ◽  
pp. 1-14 ◽  
Author(s):  
HH Mahboub ◽  
YH Tartor
Keyword(s):  
Antifungal Activity ◽  
Growth Performance ◽  
Nile Tilapia ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
Fish Growth ◽  
Immunological Parameters ◽  
Species Production

This study investigated the antifungal activity of 5 essential oils (EOs) towards yeasts recovered from diseased fishes; and focused on the efficacy of one EO (carvacrol) on growth performance, non-specific immunity, and disease resistance of Nile tilapia Oreochromis niloticus against Cryptococcus uniguttulatus challenge. Thymoquinone, thymol, carvacrol, eugenol, and cinnamon were first tested in vitro against 20 clinical yeast strains in comparison with antifungal drugs (fluconazole, ketoconazole, itraconazole, amphotericin B, nystatin, and clotrimazole) using disc diffusion and broth microdilution methods. For the in vivo challenge, fish (n = 150) were divided into 5 groups (carvacrol prophylaxis, carvacrol treatment, itraconazole treatment, unchallenged control, and positive control; 30 fish group-1) with 3 replicates. Phagocytic activity, reactive oxygen species production, reactive nitrogen species production, myeloperoxidase, lysozyme activity, and total immunoglobulins were tested before and after challenge. Relative percent survival (RPS) and mortality percent were determined as indicators for functional immunity. EOs displayed divergent degrees of antifungal activity, and carvacrol was the most effective against the tested yeasts. The dietary additive of carvacrol significantly enhanced growth performance, all immunological parameters, and the RPS values (90%) compared to other treatments. This unique experimental model indicates that carvacrol seems promising not only for enhancing immunity and promoting fish growth, but also for controlling emerging fungal infections. Future studies should investigate different concentrations of carvacrol as well as its antifungal activity in different fish species.

Antifungal Activity of Essential Oil and Hydrosol Extract of Ballota nigra L. and their Protective Effects Against the Black Rot of Tomatoes

2019 ◽  
Vol 15 (7) ◽  
pp. 662-671 ◽  
Author(s):  
Nabila A. Sebaa ◽  
Amina T. Zatla ◽  
Mohammed E.A. Dib ◽  
Boufeldja Tabti ◽  
Jean Costa ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Alternaria Alternata ◽  
Penicillium Expansum ◽  
Protective Effects ◽  
Antifungal Activities

Background: Bellota species are used to treat various diseases in traditional folk medicine. Objectives: This study aimed to chemically characterize the essential oils and the hydrosol extract and regional specificity of the major components of Ballota nigra essential oil and to evaluate their in vitro and in vivo antifungal activities. Methods: Essential oils were obtained by a Clevenger-type apparatus and analyzed by using Gas Chromatography (GC) and Gas Chromatography Mass Spectroscopy (GC/MS). The antifungal activities were tested to three phytopathogenic stains (Penicillium expansum, Aspergillus niger and Alternaria alternata). Results: Altogether, 38 compounds were identified in the essential oils, representing 92.1-96.8% of the total oil composition. Their main constituents were E-β-caryophyllene (4.8-24.6%), E-β-farnesene (3.3-22.9%), β-bisabolene (7.6-30.2%), α-humulene (2.1-13.3%) and geranyl linalool (1.1-8.2%). The statistical methods deployed confirmed that there is a relation between the essential oil compositions and the harvest locations. Hydrosol extract was constituted by seven components, represented principally by methyl eugenol (75.2%) and caryophyllene oxide (12.5%). The results of in vitro antifungal activity with essential oil and hydrosol extract have shown very interesting antifungal activities on Penicillium expansum and Alternaria alternata strains with percentage reductions up to 80%. Additionally, in in vivo assays, Ballota nigra essential oil and hydrosol extract significantly reduce decay in artificially inoculated tomato by Alternaria alternata. Conclusion: The essential oil and hydrosol extract can be used as a potential source of sustainable eco-friendly botanical fungicides to protect stored tomatoes from pathogens, saprophytic fungi causing bio-deterioration to a variety of food commodities.

scholarly journals EVALUATION OF ANTIFUNGAL AND ANTIBACTERIAL ACTIVITY OF SOME NEW BENZIMIDAZOLE DERIVATIVES

2018 ◽  
Vol 48 (2) ◽  
pp. 125-129
Author(s):  
K. ZOMORODIAN ◽  
S. KHABNADIDEH ◽  
L. ZAMANI ◽  
K. PAKSHIR ◽  
M. TAJADDOD
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
Antifungal Drugs ◽  
In Vivo Studies ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Gram Positive ◽  
Meta Position

The extensive use of antifungal drugs and their resistance against fungal infections have led to discover new antimicrobial compounds. We previously described synthesis of some new derivatives of 2-methylbenzimidazole (1a-5a) and 5,6dimethylbenzimidazol (1b-5b). Here we evaluated the antimicrobial activities of these compounds against different species of micro organisms including gram positive and gram negative bacteria as well as fungi. Broth micro-dilution method as recommended by clinical and laboratory standard institute (CLSI) was used for this purpose. The results show compounds 2-Methyl-1-(3-methylbenzyl)-1H-benzo [d]imidazole (5a) and 5,6-Dimethyl-1-(3-methyl benzyl)-1H-benzo[d]imidazole (5b) had the best antifungal activity against the examined fungi and gram positive bacteria. Moreover these two compounds inhibited the growth of azole resistant strains. By comparison the relationship between the structures and activities of the tested compounds revealed that the presence of methyl residue in meta position of benzyl group enhance the antifungal activity. Regarding a broad spectrum antifungal activities of some of the tested compounds, they might be a good candidate for further in vivo studies to evaluate their pharmacological activity and toxicity as a novel antifungal agents.

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