scholarly journals ANTI-CANDIDA ALBICANS ACTIVITY OF THE ASSOCIATION OF CITRONELAL WITH ANFOTERICIN B OR WITH CETOCONAZOLE

2019 ◽  
Vol 16 (31) ◽  
pp. 250-257
Author(s):  
Patrícia Duarte Costa SILVA ◽  
Brenda Lavínia Calixto dos SANTOS ◽  
Gustavo Lima SOARES ◽  
Wylly Araújo de OLIVEIRA
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Amphotericin B ◽  
Inhibitory Concentration ◽  
Fungal Infections ◽  
Pathogenic Fungi ◽  
Mortality Rates ◽  
New Drugs ◽  
High Morbidity ◽  
Isolated Species

Fungal infections caused by species of the genus Candida are responsible for high morbidity and mortality rates, mainly affecting immunocompromised individuals. Among fungi, Candida albicans is the most frequently isolated species of clinical specimens. A problem associated with increased resistance of pathogenic fungi to the agents used in the therapeutic regimen and the limited number of drugs to cure these infections. As a result, the search for new drugs with antifungal activity has become increasingly important. The aim of this study is to study the antifungal activity of citronellal alone and in combination with amphotericin B or ketoconazole. The Minimal Inhibitory Concentration of citronellal, amphotericin B and ketoconazole against strains of Candida albicans were evaluated by the microdilution technique, and the Minimum Fungicide Concentration of citronellal against the same strains was also performed. Through the checkerboard methodology the effect of the combination of citronelal with amphotericin B or with ketoconazole was determined. This study showed that the association of citronellal with ketoconazole was shown to be an additive against one of the strains of C. albicans and indifferent to another strain. While the combined activity of citronellal and amphotericin B demonstrated an indifferent effect on the strains tested.

Efficacy of Novel Schiff base Derivatives as Antifungal Compounds in Combination with Approved Drugs Against Candida Albicans

2019 ◽  
Vol 15 (6) ◽  
pp. 648-658 ◽  
Author(s):  
Manzoor Ahmad Malik ◽  
Shabir Ahmad Lone ◽  
Parveez Gull ◽  
Ovas Ahmad Dar ◽  
Mohmmad Younus Wani ◽  
...  
Keyword(s):  
Schiff Base ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Fungal Infections ◽  
Total Sterol ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Ergosterol Biosynthesis ◽  
Dependent Manner ◽  
Schiff Base Derivatives

Background: The increasing incidence of fungal infections, especially caused by Candida albicans, and their increasing drug resistance has drastically increased in recent years. Therefore, not only new drugs but also alternative treatment strategies are promptly required. Methods: We previously reported on the synergistic interaction of some azole and non-azole compounds with fluconazole for combination antifungal therapy. In this study, we synthesized some non-azole Schiff-base derivatives and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drugs- fluconazole (FLC) and amphotericin B (AmB) against four drug susceptible, three FLC resistant and three AmB resistant clinically isolated Candida albicans strains. To further analyze the mechanism of antifungal action of these compounds, we quantified total sterol contents in FLC-susceptible and resistant C. albicans isolates. Results: A pyrimidine ring-containing derivative SB5 showed the most potent antifungal activity against all the tested strains. After combining these compounds with FLC and AmB, 76% combinations were either synergistic or additive while as the rest of the combinations were indifferent. Interestingly, none of the combinations was antagonistic, either with FLC or AmB. Results interpreted from fractional inhibitory concentration index (FICI) and isobolograms revealed 4-10-fold reduction in MIC values for synergistic combinations. These compounds also inhibit ergosterol biosynthesis in a concentration-dependent manner, supported by the results from docking studies. Conclusion: The results of the studies conducted advocate the potential of these compounds as new antifungal drugs. However, further studies are required to understand the other mechanisms and in vivo efficacy and toxicity of these compounds.

scholarly journals Biofabricated Silver Nanoparticles Synergistically Activate Amphotericin B Against Mature Biofilm Forms of Candida Albicans

2017 ◽  
Vol 4 (1) ◽  
pp. 1-16 ◽  
Author(s):  
Shivkrupa D. Halbandge ◽  
Supriya P. Mortale ◽  
Sankunny Mohan Karuppayil
Keyword(s):  
Silver Nanoparticles ◽  
Candida Albicans ◽  
Amphotericin B ◽  
Hemolytic Activity ◽  
Biofilm Formation ◽  
Inhibitory Concentration ◽  
Fungal Infections ◽  
Fractional Inhibitory Concentration ◽  
Planktonic Growth ◽  
Concentration Indices

Background: Biofilm formation by Candida albicans is a significant clinical challenge. Fungal biofilms are resistant to most of the currently available antifungal agents. Amphotericin-B (AmB) is an antifungal agent used for the treatment of systematic fungal infections but it is well known for its toxicities and side-effects. Novel approaches are needed to treat these infections that can reduce its toxicities. Objectives: Current study aims to evaluate the efficacy of silver nanoparticles (SNPs) alone and in combination with AmB against growth and biofilm formation in C. albicans. Methods: Combinations of SNP-AmB were tested against planktonic growth and biofilm formation in vitro. Micro broth dilution method was used to study planktonic growth and biofilm formation. The fractional inhibitory concentration indices (FICI) were calculated by using a checkerboard format. Biofilm formation was analyzed by using XTT-metabolic assay. Results: MIC of AmB for developing biofilm was lowered by 16 fold in combination with SNPs. The calculated fractional inhibitory concentration indices were 0.1875 suggesting that this interaction is synergistic. Similarly, the mature biofilms were significantly prevented by SNPs-AmB combination. This interaction was synergistic. Furthermore, interaction between SNPs and AmB against planktonic growth was additive. Hemolytic activity assay was carried out on these drugs and combinations. Drug required for inhibition alone as well as in combination did not exhibit hemolytic activity. Conclusion: The combinations with SNPs lead to decreases in the dosage of AmB required for anti-Candida activity. SNPs-AmB combination could be an effective strategy against biofilm formed by C. albicans.

scholarly journals Antifungal Activity of Amphotericin B Cochleates against Candida albicans Infection in a Mouse Model

2000 ◽  
Vol 44 (6) ◽  
pp. 1463-1469 ◽  
Author(s):  
Leila Zarif ◽  
John R. Graybill ◽  
David Perlin ◽  
Laura Najvar ◽  
Rosie Bocanegra ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Amphotericin B ◽  
Blood Cells ◽  
Inhibitory Concentration ◽  
Human Red Blood Cells ◽  
Unique Shape ◽  
Tissue Burden ◽  
Candida Albicans Infection

ABSTRACT Cochleates are lipid-based supramolecular assemblies composed of natural products, negatively charged phospholipid, and a divalent cation. Cochleates can encapsulate amphotericin B (AmB), an important antifungal drug. AmB cochleates (CAMB) have a unique shape and the ability to target AmB to fungi. The minimal inhibitory concentration and the minimum lethal concentration against Candida albicans are similar to that for desoxycholate AmB (DAMB; Fungizone). In vitro, CAMB induced no hemolysis of human red blood cells at concentrations of as high as 500 μg of AmB/ml, and DAMB was highly hemolytic at 10 μg of AmB/ml. CAMB protect ICR mice infected with C. albicans when the agent is administered intraperitoneally at doses of as low as 0.1 mg/kg/day. In a tissue burden study, CAMB, DAMB, and AmBisome (liposomal AmB; LAMB) were effective in the kidneys, but in the spleen CAMB was more potent than DAMB at 1 mg/kg/day and was equivalent to LAMB at 10 mg/kg/day. In summary, CAMB are highly effective in treating murine candidiasis and compare well with AmBisome and AmB.

scholarly journals ANTIFUNGAL ACTIVITY OF THE ASSOCIATION OF CARVACROL WITH AMPHOTERICIN B OR WITH KETOCONAZOLE

2019 ◽  
Vol 16 (31) ◽  
pp. 12-17
Author(s):  
Gustavo Lima SOARES ◽  
Brenda Lavínia Calixto dos SANTOS ◽  
Brenna Ravena Araújo LUZ ◽  
Wylly Araújo de OLIVEIRA
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Inhibitory Concentration ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
Aspergillus Species ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Antifungal Action

Aspergillus species are a cause of a high number of fungal infections of difficult treatment, presenting an expressive number of deaths due to the complications in the severe cases of infection. The objective was to evaluate the antifungal action of carvacrol against Aspergillus species, as well as to evaluate the interactions when associated with amphotericin B or ketoconazole. The antifungal activity of carvacrol was evaluated by the broth microdilution method. The combinations of the substances were performed by the checkerboard methodology, to determine the Index of Fractional Inhibitory Concentration. Carvacrol showed antifungal activity against all Aspergillus strains used in the trials. In combinations of substances, only a combination of carvacrol and amphotericin B presented satisfactory results. Combinations of carvacrol and ketoconazole have not shown good. It is concluded that carvacrol is a good candidate for the antifungal drug because of its good activity against Aspergillus demonstrated in the present study, as well as in other studies in the literature. Their combination in vitro with amphotericin B or ketoconazole did not present any advantages over the use of antifungal drugs alone.

scholarly journals Structural and Bioactivity Characterization of Filipin Derivatives from Engineered Streptomyces filipinensis Strains Reveals Clues for Reduced Haemolytic Action

Antibiotics ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 413
Author(s):  
Eva G. Barreales ◽  
Ángel Rumbero ◽  
Tamara D. Payero ◽  
Antonio de Pedro ◽  
Ester Jambrina ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
Pathogenic Fungi ◽  
New Drugs ◽  
Metabolic Intermediates ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Opportunistic Pathogenic

The rise in the number of immunocompromised patients has led to an increased incidence of fungal infections, with high rates of morbidity and mortality. Furthermore, misuse of antifungals has boosted the number of resistant strains to these agents; thus, there is urgent need for new drugs against these infections. Here, the in vitro antifungal activity of filipin III metabolic intermediates has been characterized against a battery of opportunistic pathogenic fungi—Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans, Trichosporon cutaneum, Trichosporon asahii, Aspergillus nidulans, Aspergillus niger, and Aspergillus fumigatus—using the Clinical and Laboratory Standards Institute broth microdilution method. Structural characterization of these compounds was undertaken by mass spectrometry (MS) and nuclear magnetic resonance (NMR) following HPLC purification. Complete NMR assignments were obtained for the first time for filipins I and II. In vitro haemolytic assays revealed that the haemolytic action of these compounds relies largely on the presence of a hydroxyl function at C26, since derivatives lacking such moiety show remarkably reduced activity. Two of these derivatives, 1′-hydroxyfilipin I and filipin I, show decreased toxicity towards cholesterol-containing membranes while retaining potent antifungal activity, and could constitute excellent leads for the development of efficient pharmaceuticals, particularly against Cryptococcosis.

scholarly journals Antifungal activities of the rhizome extract of five member Zingiberaceae against Candida albicans and Trichophyton rubrum

2021 ◽  
Vol 22 (3) ◽  
Author(s):  
Muhammad Evy Prastiyanto ◽  
NI’MATUR ROHMAH ◽  
LESITA EFENDI ◽  
RAHMATIA ARIFIN ◽  
FANDHI ADI WARDOYO ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Fungal Infections ◽  
Curcuma Longa ◽  
Ethanol Extract ◽  
Pathogenic Fungi ◽  
Zingiber Officinale ◽  
Diffusion Method ◽  
Antifungal Activities

Abstract. Prastiyanto ME, Rohmah N, Efendi L, Arifin R, Wardoyo FA, Wilson W, Mukaromah AH, Dewi SS, Darmawati S. 2021. Antifungal activities of the rhizome extract of five member Zingiberaceae against Candida albicans and Trichophyton rubrum. Biodiversitas 22: 1509-1513. Fungal infections have now become serious health issues. One of the strategies to avoid the problems of fungal infections is by using natural product from plants that are effective against many human pathogenic fungi. The study portrayed the use of the extracts of plant rhizomes as the alternatives to fight against number of human pathogenic fungi. This research aimed to investigate the antifungal activities of crude ethanol extract of five member of the family Zingiberaceae (Curcuma longa, Alpinia galanga Zingiber officinale. var. rubrum, Zingiber officinale var. officinarum and Zingiber officinale var. amarum), which are widely used as folk medicines against Candida albicans and Trichophyton rubrum. Crude ethanol extracts of five members of Zingiberaceae were evaluated for their antifungal activities and the results were calculated based on the zones of inhibition using the diffusion method. The extract showed antifungal activity against Candida. albicans in the agar well diffusion assay (10.2-27.1 mm inhibition diameter) and against T. rubrum (27.3-44.3 mm inhibition diameter). The data have revealed that all rhizomes have the potential to be developed as antifungal agents, particularly against C. albicans and T. rubrum. Studies on the antifungal activity against yeast-like (C. albicans) and filamentous (T. rubrum) can provide new information about the benefits of members Zingiberaceae as a source of natural antifungal. Researchers can select the type of rhizome that has more potential for further extraction to obtain pure compounds that can be used as antifungals.

scholarly journals Herbal Extracts with Antifungal Activity Against Candida albicans: A Systematic Review

2020 ◽  
Vol 20 ◽  
Author(s):  
Hsuan Hsu ◽  
Chirag C. Sheth ◽  
Veronica Veses
Keyword(s):  
Systematic Review ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
High Throughput Screening ◽  
Fungal Infections ◽  
Natural Compounds ◽  
New Drugs ◽  
Mentha Piperita ◽  
Herbal Extracts ◽  
Antifungal Activities

Background: In the era of antimicrobial resistance, fungal pathogens are not an exception. Several strategies, including antimicrobial stewardship programs and high throughput screening of new drugs are being implemented. Several recent studies have demonstrated effectiveness of plant compounds with antifungal activity. Objective: In this systematic review we examine the use of natural compounds as a possible avenue to fight fungal infections produced by Candida albicans, the most common human fungal pathogen. Method: Electronic literature searches were conducted through PubMed/MEDLINE, Cochrane, and Science Direct limited to the 5 years. A total of 131 articles were included with 186 plants extracts evaluated. Results: Although the majority of the natural extracts exhibited antifungal activities against C. albicans (both in vivo and in vitro), the strongest antifungal activity was obtained from Lawsonia inermis, Pelargonium graveolens, Camellia sinensis, Mentha piperita, and Citrus latifolia. Conclusion: The main components with proven antifungal activities were phenolic compounds such as gallic acid, thymol, and flavonoids (specially catechin), polyphenols such as tannins, terpenoids and saponins. The incorporation of nanotechnology enhances greatly the antifungal properties of these natural compounds. Further research is needed to fully characterize the composition of all herbal extracts with antifungal activity as well as the mechanisms of action of the active compounds.

Antifungal efficacy of atorvastatin-containing emulgel in the treatment of oral and vulvovaginal candidiasis

2020 ◽  
Author(s):  
Ari Soares de Oliveira Neto ◽  
Israel Lucas Antunes Souza ◽  
Maria Eliza Samuel Amorim ◽  
Thalita de Freitas Souza ◽  
Vinicius Novaes Rocha ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Fungal Infections ◽  
Drug Repositioning ◽  
Oral Candidiasis ◽  
Vulvovaginal Candidiasis ◽  
Antifungal Drugs ◽  
Sterol Synthesis ◽  
In Vitro Tests

Abstract Drug repositioning has been an important ally in the search for new antifungal drugs. Statins are drugs that act to prevent sterol synthesis in both humans and fungi and for this reason they are promissory candidates to be repositioned to treat mycoses. In this study we evaluated the antifungal activity of atorvastatin by in vitro tests to determine the minimum inhibitory concentration against azole resistant Candida albicans and its mechanisms of action. Moreover, the efficacy of both atorvastatin-loaded oral and vaginal emulgels (0.75%, 1.5% and 3% w/w) was evaluated by means of in vivo experimental models of oral and vulvovaginal candidiasis, respectively. The results showed that atorvastatin minimal inhibitory concentration against C. albicans was 31.25 μg/ml. In oral candidiasis experiments, the group treated with oral emulgel containing 3.0% atorvastatin showcased total reduction in fungal load after nine days of treatment. Intravaginal delivery atorvastatin emulgel showed considerable effectiveness at the concentration of 3% (65% of fungal burden reduction) after nine days of treatment. From these findings, it is possible to assert that atorvastatin may be promising for drug repositioning towards the treatment of these opportunistic mycoses. Lay Summary Atorvastatin is a statin drug that presents antifungal activity. This study showed that atorvastatin-containing oral and vaginal emulgels were able to treat vulvovaginal and oral candidiasis of infected animal model. Therefore, we showcased that atorvastatin may be a possible therapeutic agent in order to be a used to control opportunistic mucosal fungal infections caused by Candida albicans.

scholarly journals Increasing Susceptibility of Drug-Resistant Candida albicans to Fluconazole and Terbinafine by 2(5H)-Furanone Derivative

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 642 ◽  
Author(s):  
Irshad S. Sharafutdinov ◽  
Georgii D. Ozhegov ◽  
Alina E. Sabirova ◽  
Valentina V. Novikova ◽  
Svetlana A. Lisovskaya ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Laser Scanning ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
Fungal Infections ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Drug Resistant ◽  
Drug Resistant Strains

The frequency of mycoses caused by drug-resistant fungal pathogen Candida albicans has increased drastically over the last two decades. The spread of drug-resistant strains, along with the limitations of currently available antifungals, complicates the management of fungal infections, thereby representing great challenges for clinical healthcare. Among various antimicrobial pharmacophores, 2(5H)-furanone derivatives have demonstrated antimicrobial, antifungal, and antibiofilm activities. In this study, we report the antifungal activity of the 2(5H)-furanone derivative F105, consisting of three pharmacophores, namely chlorinated 2(5H)-furanone, sulfonyl group, and l-menthol moiety. Although exhibiting moderate antifungal activity alone with the minimum inhibitory concentration (MIC) values of 32–256 μg/mL, F105 potentiates the activity of fluconazole and terbinafine with fractional inhibitory concentration index (FICI) values of 0.27–0.50. Thus, 16 μg/mL of F105 reduced the MICs of these antifungals against fluconazole-resistant C. albicans isolates four-fold, achieving similar values as for the intermediately susceptible phenotype. Confocal laser scanning microscopy revealed that the fluorescent 2(5H)-furanone derivative F145 was also able to penetrate through biofilms formed by C. albicans. Indeed, in the presence of F105, even sub-MIC concentrations of both fluconazole and terbinafine led to significant reduction of C. albicans CFUs in the mature biofilm. Thus, F105 appears to be a promising candidate for the development of novel antifungal agents as well as enhancers of current antifungal agents, particularly for the treatment of drug-resistant C. albicans infections.

Antifúngicos poliénicos. Mecanismo de acción y aplicaciones

2020 ◽  
Vol 63 (2) ◽  
pp. 7-17
Author(s):  
Evelyn Rivera-Toledo ◽  
Alan Uriel Jiménez-Delgadillo ◽  
Patricia Manzano-Gayosso
Keyword(s):  
Antifungal Activity ◽  
Key Words ◽  
Secondary Metabolism ◽  
Amphotericin B ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Variable Number ◽  
Therapeutic Failure ◽  
Morbidity And Mortality ◽  
Clinical Use

The first compounds with specific antifungal activity were identified in the middle of the last century as a product of the secondary metabolism of bacteria of the order Actinomycetales, and their clinical use significantly diminished the morbidity and mortality associated with severe fungal infections. Many of such biosynthetic compounds are characterized by a chemical polygenic structure, with a variable number of carbon-carbon double bonds. Currently, besides polygenic antimycotics, there are other antifungal agents, such as the azole compounds, that have less toxicity in patients; however, cases of therapeutic failure with such compounds have been documented, therefore, the use of polygenics is still the best alternative in such cases. This review presents data about the properties and applications of antifungal-polygenic compounds using amphotericin B as a model. Key words: Amphotericin B; antifungal polyenes; ergosterol

Sign in / Sign up

Export Citation Format

Share Document