DRUG ENHANCEMENT, SYNERGISM AND ANTIFUNGAL ACTIVITY OF MICONAZOLE ASSOCIATED POLYGODIAL AGAINST CANDIDA ALBICANS

Miconazole has low toxicity, however, there is a high incidence resistance of Candida sp. In the search for new drugs or improve existing ones, the originating products of medicinal plants has been the target of constant studies. The aim of this work was to verifyinvitrosynergismand antifungal activity of miconazole associated with poligodial. Miconazole (MCZ) and Poligodial (P) were dissolved in dimethylsulfoxide (DMSO) 1% done successive dilutions of each product ranging from 25mg to 0,19mg/mL (Polygodial)(10-1 to 10-9mg / ml); 14mg to 0,10mg/mL (miconazole). Antifungal test were based by CLSI diffusion agar against C. albicans (ATCC 18804), C. albicans (LMB01) and C. albicans (LMB02), C. tropicalis (ATCC 18807),C. lusitaniae (ATCC 42720), C. krusei (ATCC 20405). The results had shown all compounds that were effective in inhibiting Candida species. However, the zones of inhibition in agar diffusion test were higher for Miconazole (16,83mm) and Polygodial (15,16mm) while the MIX showed lower inhibition zones (14,43mm) when compared with controls. MIX was more effective in MIC test, and lowest concentration were at 10-6 dilution (0,60mg / ml) compared to MCZ and P controls.

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

Medicinal Chemistry ◽

10.2174/1573406415666181203115957 ◽

2019 ◽

Vol 15 (6) ◽

pp. 648-658 ◽

Cited By ~ 1

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.

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Antifungal Activity Directed Toward the Cell Wall by 2-Cyclohexylidenhydrazo- 4-Phenyl-Thiazole Against Candida albicans

Infectious Disorders - Drug Targets ◽

10.2174/1871526518666180531101605 ◽

2019 ◽

Vol 19 (4) ◽

pp. 428-438 ◽

Cited By ~ 1

Author(s):

Nívea P. de Sá ◽

Ana P. Pôssa ◽

Pilar Perez ◽

Jaqueline M.S. Ferreira ◽

Nayara C. Fonseca ◽

...

Keyword(s):

Cell Wall ◽

Candida Albicans ◽

Antifungal Activity ◽

Mammalian Cells ◽

C Elegans ◽

Buccal Epithelial Cells ◽

Mutant Strains ◽

Low Toxicity ◽

High Concentrations ◽

Mic Value

Background: The increasing incidence of invasive forms of candidiasis and resistance to antifungal therapy leads us to seek new and more effective antifungal compounds. Objective: To investigate the antifungal activity and toxicity as well as to evaluate the potential targets of 2- cyclohexylidenhydrazo-4-phenyl-thiazole (CPT) in Candida albicans. Methods: The antifungal activity of CPT against the survival of C. albicans was investigated in Caenorhabditis elegans. Additionally, we determined the effect of CPT on the inhibition of C. albicans adhesion capacity to buccal epithelial cells (BECs), the toxicity of CPT in mammalian cells, and the potential targets of CPT in C. albicans. Results: CPT exhibited a minimum inhibitory concentration (MIC) value of 0.4-1.9 µg/mL. Furthermore, CPT at high concentrations (>60 x MIC) showed no or low toxicity in HepG2 cells and <1% haemolysis in human erythrocytes. In addition, CPT decreased the adhesion capacity of yeasts to the BECs and prolonged the survival of C. elegans infected with C. albicans. Analysis of CPT-treated cells showed that their cell wall was thinner than that of untreated cells, especially the glucan layer. We found that there was a significantly lower quantity of 1,3-β-D-glucan present in CPT-treated cells than that in untreated cells. Assays performed on several mutant strains showed that the MIC value of CPT was high for its antifungal activity on yeasts with defective 1,3-β-glucan synthase. Conclusion: In conclusion, CPT appears to target the cell wall of C. albicans, exhibits low toxicity in mammalian cells, and prolongs the survival of C. elegans infected with C. albicans.

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Antifungal activity of components used for decontamination of dental prostheses on the growth of Candida albicans

Revista de Odontologia da UNESP ◽

10.1590/rou.2014.018 ◽

2014 ◽

Vol 43 (2) ◽

pp. 137-142 ◽

Cited By ~ 2

Author(s):

Cíntia Lima Gouveia ◽

Isabelle Cristine Melo Freire ◽

Maria Luísa de Alencar e Silva Leite ◽

Rebeca Dantas Alves Figueiredo ◽

Leopoldina de Fátima Dantas de Almeida ◽

...

Keyword(s):

Candida Albicans ◽

Antifungal Activity ◽

Sodium Bicarbonate ◽

Fungal Growth ◽

Antifungal Effect ◽

Dental Prostheses ◽

Diffusion Technique ◽

Zones Of Inhibition ◽

And Control

Introduction: The effectiveness of antimicrobial solutions employed in dental prosthesis decontamination is still uncertain. Aim: To evaluate the antifungal activity of cleaners used in the decontamination of dental prostheses on the growth of Candida albicans. Material and method: The evaluated products were: Corega Tabs(r) (S1), Sodium Hypochlorite 1% (S2), Sodium Bicarbonate 1% (S3), Hydrogen Peroxide 1% (S4), Chlorhexidine Digluconate 0.12% - Periogard (r) (S5), Mouthrinse based on essential oils - Listerine(r) (S6), essential oil from Rosmarinus officinalis (rosemary) at concentrations of 1% (S7) and 2% (S8). The antifungal activity of the products was evaluated by agar diffusion technique and the determination of microbial death curve of samples of C. albicans (ATCC 90028) in concentration 1.5 × 106 CFU/mL. The tests were performed in triplicate and statistical analysis was made by ANOVA Two-Way and Tukey tests, with the confidence level of 95%. Result: The average of the zones of inhibition growth, in millimeters, obtained for the products were: 0.0 (S1), 44.7 (S2), 0.0 (S3), 21.6 (S4), 10.0 (S5), 6.1 (S6), 0.0 (S7) and 2.4 (S8). Considering the determination of microbial death curve, all products showed a statistical difference (p<0.01) from control (0.85% sodium chloride) and S3 groups. Fungal growth less than 2×104 CFU/mL and an accentuation of the microbial death curve were observed after 30 minutes, with exception for S3 and control groups. Conclusion: The studied compounds, with the exception of Sodium Bicarbonate, have antifungal effect against C. albicans, which contribute for dental prostheses hygiene.

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

Periódico Tchê Química ◽

10.52571/ptq.v16.n31.2019.256_periodico31_pgs_250_257.pdf ◽

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.

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Comparative studies of the antimicrobial effect of ethanolic and aqueous extracts of Garcinia kola on Klebsiella pneumonia and Candida albicans in vitro

Nigerian Journal of Technological Research ◽

10.4314/njtr.v16i1.7 ◽

2021 ◽

Vol 16 (1) ◽

pp. 52-58

Author(s):

Elizabeth Winful ◽

Olanikpekun Idowu ◽

Opeoluwa O. Fasanya ◽

Nkechi E. Egbe

Keyword(s):

Antimicrobial Activity ◽

Candida Albicans ◽

Ethanol Extract ◽

Antimicrobial Effect ◽

Klebsiella Pneumonia ◽

Disc Diffusion ◽

Diffusion Test ◽

Garcinia Kola ◽

Zones Of Inhibition

Antimicrobial resistance has become a global health problem. Although a wide range of chemotherapeutic antimicrobials are available for treatment of microbial related infections and diseases, development of resistance to these chemotherapeutic agents is rapidly on the increase. Extracts from some plants have shown some promise in antimicrobial activity. This has led to the screening of several medicinal plants for their potential antimicrobial activity. Therefore, this study was aimed at evaluating the antimicrobial effect of ethanolic and aqueous extracts of Garcinia kola against Klebsiella pneumonia and Candida albicans in vitro. The Garcinia kola seeds extracts were obtained using 70% ethanol and distilled water respectively. Phytochemical screening of Garcinia kola revealed the presence of various potent phytochemicals such as tannins, saponins, flavonoids, alkaloids and glycosides. Both extracts of the seeds were investigated for antimicrobial activity using disc diffusion and agar well diffusion sensitivity tests. The ethanol extract produced zones of inhibition of about 7.3 mm for Candida albicans only at a concentration of 800mg/ml for the disc diffusion test. For the agar well diffusion test, the aqueous extract produced zones of inhibition of about 9.5 mm, while the ethanol extract produced zone of inhibition of 19 mm against Candida albicans at a concentration of 800 mg/ml. However, at the same concentration, the ethanol extract produced zones of inhibition of about 8.5 mm against Klebsiella pneumoniae. The findings of this study revealed that Garcinia kola was not effective in treating Klebsiella pneumonia infections but has potential in treating Candida albicans infections. Keywords: Garcinia kola, Klebsiella pneumonia, Candida albicans

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Commercial AHAS-inhibiting herbicides are promising drug leads for the treatment of human fungal pathogenic infections

Proceedings of the National Academy of Sciences ◽

10.1073/pnas.1809422115 ◽

2018 ◽

Vol 115 (41) ◽

pp. E9649-E9658 ◽

Cited By ~ 14

Author(s):

Mario D. Garcia ◽

Sheena M. H. Chua ◽

Yu-Shang Low ◽

Yu-Ting Lee ◽

Kylie Agnew-Francis ◽

...

Keyword(s):

Candida Albicans ◽

Antifungal Drug ◽

New Drugs ◽

Acetohydroxyacid Synthase ◽

Drug Candidates ◽

New Class ◽

Branched Chain Amino Acid ◽

Low Toxicity ◽

Chlorimuron Ethyl ◽

Branched Chain

The increased prevalence of drug-resistant human pathogenic fungal diseases poses a major threat to global human health. Thus, new drugs are urgently required to combat these infections. Here, we demonstrate that acetohydroxyacid synthase (AHAS), the first enzyme in the branched-chain amino acid biosynthesis pathway, is a promising new target for antifungal drug discovery. First, we show that several AHAS inhibitors developed as commercial herbicides are powerful accumulative inhibitors of Candida albicans AHAS (Ki values as low as 800 pM) and have determined high-resolution crystal structures of this enzyme in complex with several of these herbicides. In addition, we have demonstrated that chlorimuron ethyl (CE), a member of the sulfonylurea herbicide family, has potent antifungal activity against five different Candida species and Cryptococcus neoformans (with minimum inhibitory concentration, 50% values as low as 7 nM). Furthermore, in these assays, we have shown CE and itraconazole (a P450 inhibitor) can act synergistically to further improve potency. Finally, we show in Candida albicans-infected mice that CE is highly effective in clearing pathogenic fungal burden in the lungs, liver, and spleen, thus reducing overall mortality rates. Therefore, in view of their low toxicity to human cells, AHAS inhibitors represent a new class of antifungal drug candidates.

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Chemical Analysis and Antioxidant and Antimicrobial Activity of Essential oils from Artemisia negrei L. against Drug-Resistant Microbes

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2021/5902851 ◽

2021 ◽

Vol 2021 ◽

pp. 1-9

Author(s):

Khalid Chebbac ◽

Abdelfattah EL Moussaoui ◽

Mohammed Bourhia ◽

Ahmad Mohammad Salamatullah ◽

Abdulhakeem Alzahrani ◽

...

Keyword(s):

Antioxidant Activity ◽

Antibacterial Activity ◽

Candida Albicans ◽

Antifungal Activity ◽

Gram Negative ◽

E Coli ◽

Phytochemical Composition ◽

Total Antioxidant ◽

Inhibition Zones ◽

Β Carotene

Background. Artemisia negrei L. (A. negrei) is a medicinal and aromatic plant belonging to the family Asteraceae that is more widespread in the folded Middle Atlas Mountains, Morocco. Materials and Methods. This study was run to investigate the phytochemical composition and antioxidant, antibacterial, and antifungal activities of Artemisia negrei L. essential oil. This oil was extracted from the fresh plant material by using the Clevenger apparatus. The phytochemical composition was characterized by GC-MS. The antioxidant activity was evaluated using different methods including DPPH, β-carotene bleaching, and total antioxidant capacity. The antibacterial activity was tested vs. multidrug-resistant bacteria including both Gram-negative and Gram-positive using inhibition zones in agar media and minimum inhibitory concentration (MIC) bioassays. The antifungal activity was conducted on Candida albicans, Aspergillus niger, Aspergillus flavus, and Fusarium oxysporum using a solid medium assay. Results. The chromatographic characterization of essential oils of A. negrei revealed the presence of 34 compounds constituting 99.91% of the total essential oil. The latter was found to have promising antioxidant activity by all bioassays used such as DPPH, β-carotene bleaching, and total antioxidant capacity. The results obtained showed that our plant oils had potent antibacterial activity towards Gram-negative (E. coli 57, E. coli 97, K. pneumonia, and P. aeruginosa) and Gram-positive (S. aureus), so that the maximum inhibition zones and MIC values were around 18–37 mm and 3.25 to 12.5 mg/mL, respectively. The oil also showed antifungal activity towards Candida albicans, Fusarium oxysporum, and Aspergillus Niger except for flavus species. Conclusion. The findings obtained in the work showed that A. negrei can serve as a valuable source of natural compounds that can be used as a new weapon to fight radical damage and resistant microbes.

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Antimicrobial Potential of Strontium Hydroxide on Bacteria Associated with Peri-Implantitis

Antibiotics ◽

10.3390/antibiotics10020150 ◽

2021 ◽

Vol 10 (2) ◽

pp. 150

Author(s):

Hatem Alshammari ◽

Jessica Neilands ◽

Gunnel Svensäter ◽

Andreas Stavropoulos

Keyword(s):

Antimicrobial Properties ◽

Fusobacterium Nucleatum ◽

Diffusion Test ◽

Agar Diffusion ◽

Antimicrobial Potential ◽

Viability Assay ◽

Patient Morbidity ◽

Agar Diffusion Test ◽

Zones Of Inhibition ◽

Strontium Hydroxide

Background: Peri-implantitis due to infection of dental implants is a common complication that may cause significant patient morbidity. In this study, we investigated the antimicrobial potential of Sr(OH)2 against different bacteria associated with peri-implantitis. Methods: The antimicrobial potential of five concentrations of Sr(OH)2 (100, 10, 1, 0.1, and 0.01 mM) was assessed with agar diffusion test, minimal inhibitory concentration (MIC), and biofilm viability assays against six bacteria commonly associated with biomaterial infections: Streptococcus mitis, Staphylococcus epidermidis, Aggregatibacter actinomycetemcomitans, Porphyromonas gingivalis, Escherichia coli, and Fusobacterium nucleatum. Results: Zones of inhibition were only observed for, 0.01, 0.1, and 1 mM of Sr(OH)2 tested against P. gingivalis, in the agar diffusion test. Growth inhibition in planktonic cultures was achieved at 10 mM for all species tested (p < 0.001). In biofilm viability assay, 10 and 100 mM Sr(OH)2 showed potent bactericidal affect against S. mitis, S. epidermidis, A. actinomycetemcomitans, E. coli, and P. gingivalis. Conclusions: The findings of this study indicate that Sr(OH)2 has antimicrobial properties against bacteria associated with peri-implantitis.

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Increased itraconazole antifungal activity by agar diffusion test

Journal of Microbiological Methods ◽

10.1016/0167-7012(94)90063-9 ◽

1994 ◽

Vol 20 (1) ◽

pp. 47-54 ◽

Cited By ~ 5

Author(s):

F.D. D'Auria ◽

N. Simonetti ◽

V. Strippoli

Keyword(s):

Antifungal Activity ◽

Diffusion Test ◽

Agar Diffusion ◽

Agar Diffusion Test

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Antibacterial effects of new endodontic materials based on calcium silicates

Vojnosanitetski pregled ◽

10.2298/vsp161231130t ◽

2019 ◽

Vol 76 (4) ◽

pp. 365-372

Author(s):

Dijana Trisic ◽

Bojana Cetenovic ◽

Nemanja Zdravkovic ◽

Tatjana Markovic ◽

Biljana Dojcinovic ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Enterococcus Faecalis ◽

Antibacterial Effects ◽

Diffusion Test ◽

Highly Active ◽

Agar Diffusion Test ◽

Active Calcium ◽

Calcium Silicates ◽

Inhibition Zones ◽

Antibacterial Potential

Background/Aim. The main task of endodontic treatment is to eliminate pathologically altered tissue, to disinfect root canal space and to obtain its three-dimensional hermetic obturation. The main purpose of this study was to evaluate antimicrobial activity of new endodontic nano-structured highly active calcium silicates based materials albo-mineral plyoxide carbonate aggregate (ALBO-MPCA) and calcium silicates (CS) in comparison to mineral trioxide aggregate (MTA+) and UltraCal XS (CH). Methods. The antimicrobial activity of materials was tested against Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 14506) strains, and following clinical isolates: Rothia dentocariosa, Enterococcus faecalis, Staphylococcus aureus, Streptococcus anginosus and Streptococcus vestibularis using a double layer agar diffusion test. The pH measurements were performed using the pH meter. Total amount of released ions was determined by inductively coupled plasma optical emission spectrometry (ICP-OES). Results. All tested materials showed the best antibacterial potential after 1 h of incubation. After 3h and 24h of the incubation period, the antibacterial potential of all tested materials were similar. The Agar diffusion test showed that ALBO-MPCA, CS and MTA+ had similar inhibition zones (p > 0.05), except in the activity against Staphylococcus aureus where ALBO-MPCA showed better antimicrobial properties than MTA+ in 3h and 24h of the incubation period (p < 0.05). Following 24h of the incubation, the inhibition zones were the strongest with CH against Staphylococcus aureus (16.67 ? 2.34 mm) followed by ALBO-MPCA (14.67 ? 1.21 mm) and the weakest with CS against Enterococcus faecalis (6.50 ? 1.76 mm). CH showed the highest pH, followed by ALBO-MPCA, CS and MTA+. Conclusion. The expressed antibacterial effects indicate that materials based on nano-structured highly active calcium silicates represent effective therapeutic agents for root canal obturation in one-visit apexification treatment, therefore they are recommend for further examination and clinical trials as they are proposed for MTA substitution.

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