scholarly journals A Promising Copper(II) Complex as Antifungal and Antibiofilm Drug against Yeast Infection

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 1856 ◽  
Author(s):  
Fabiana Gomes da Silva Dantas ◽  
Adriana Araújo de Almeida-Apolonio ◽  
Renata Pires de Araújo ◽  
Lis Regiane Vizolli Favarin ◽  
Pamella Fukuda de Castilho ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Ames Test ◽  
Inhibitory Concentration ◽  
Coordination Complexes ◽  
Antifungal Property ◽  
Candida Spp ◽  
Mutagenic Potential ◽  
Yeast Infection ◽  
Limited Option ◽  
Potential Complex

The high mortality rate of candidemia and the limited option for the treatment of Candida spp. infection have been driving the search for new molecules with antifungal property. In this context, coordination complexes of metal ions and ligands appear to be important. Therefore, this study aimed to synthesize two new copper(II) complexes with 2-thiouracil and 6-methyl-2-thiouracil ligands and to evaluate their mutagenic potential and antifungal activity against Candida. The complexes were synthesized and characterized by infrared vibrational spectroscopy, CHN elemental analysis, UV-Vis experiments and ESI-HRMS spectrometry studies. The antifungal activity was evaluated by broth microdilution against 21 clinical isolates of Candida species. The mutagenic potential was evaluated by the Ames test. The complexes were Cu(Bipy)Cl2(thiouracil) (Complex 1) and Cu(Bipy)Cl2(6-methylthiouracil) (Complex 2). Complex 1 showed fungicidal and fungistatic activities against all isolates. Furthermore, the Minimum Inhibitory Concentration (MIC) from 31 to 125 µg/mL and inhibition percentage of 9.9% against the biofilms of C. krusei and C. glabrata were demonstrated. At the concentrations tested, complex 1 exhibited no mutagenic potential. Complex 2 and the free ligands exhibited no antifungal activity at the concentrations evaluated. Since complex 1 presented antifungal activity against all the tested isolates and no mutagenic potential, it could be proposed as a potential new drug for anti-Candida therapy.

scholarly journals Antimicrobial and Antibiofilm Activities of 4,5-Dihydro-1H-pyrazole-1-carboximidamide Hydrochloride against Salmonella spp.

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Andressa C. Damim ◽  
Danilo Y. de Albuquerque ◽  
Fabiana G. S. Dantas ◽  
Fernanda Galvão ◽  
Melyssa Negri ◽  
...  
Keyword(s):  
Cell Viability ◽  
Biofilm Formation ◽  
Ames Test ◽  
Inhibitory Concentration ◽  
Vero Cells ◽  
Test Compound ◽  
Broth Microdilution ◽  
Salmonella Spp ◽  
Mutagenic Potential ◽  
Vero Cell Lines

In the present study, the antimicrobial and antibiofilm activities of two 4,5-dihydro-1H-pyrazole-1-carboximidamide hydrochloride, (trifluoromethyl) phenyl-substituted (compound 1) and bromophenyl-substituted (compound 2), were evaluated against four Salmonella spp. serotypes through broth microdilution and biofilm-forming activity. Further, the cytotoxicity of the compounds was evaluated by cell viability assays using cultures of HeLa and Vero cell lines, and the mutagenic potential was assessed by the Ames test. In the broth microdilution test, compound 1 inhibited 90% of the strains tested at the minimum inhibitory concentration of 62.5 μg mL−1. Furthermore, both compounds prevented biofilm formation, with a reduction of up to 5.2 log10. HeLa and Vero cells exhibited 100% viability in the presence of compound 1. In contrast, low cell viability was observed in the presence of 15 µg mL−1 of compound 2. Furthermore, no mutagenic potential was detected at any of the tested concentrations of compound 1.

Phytochemical Screening and Antifungal Activity of Kulantrillo De Allambre (Adiantum capillus-veneris) Extract as a Formulated Vaginal Cream Against Candida albicans

10.17158/234 ◽  
2012 ◽  
Vol 18 (1) ◽  
Author(s):  
Kathleen G. Bersabal ◽  
Kyrie Marie D. Deluao ◽  
Meg C. Ibarra ◽  
Nessa Karla C. Jerusalem
Keyword(s):  
Candida Albicans ◽  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Physical Properties ◽  
Inhibitory Concentration ◽  
Positive Control ◽  
Phytochemical Screening ◽  
Antifungal Property ◽  
Vaginal Cream ◽  
Adiantum Capillus Veneris

Candida albicans is a fungus that is normally present on the skin and in mucous membranes such as vagina, mouth, or rectum. This fungus also can travel through the blood stream and affect the throat, intestines, and heart valves. It becomes an infectious agent when there is some change in the body environment that allows it to grow out of control; thus, causing a modern day disease brought on by antibiotics, drugs, processed foods, sugar and poor diet. Folkloric practice suggests that Kulantrillo de Allambre (Adiantum capillus-veneris) is effective as antifungal medication against Candida albicans; therefore, this study was undertaken to verify such claim. This effort included the phytochemical screening of active constituents, susceptibility and minimum inhibitory concentration tests involving the plant. To prove that Kulantrillo de Allambre possesses antifungal activity, a formulation of vaginal cream out of the plant extracts was tested. Alkaloids, saponins, steroids, flavonoids, tannins and anthraquinones were performed following the method described by Guevara et al. (2005). Kirby-Bauer Method was employed for the susceptibility test and two-fold agar dilution was employed for the MIC. Vaginal cream was formulated following the method of Ansel (2004). Tests revealed the presence of flavonoids only, which exhibit the antifungal property. Kirby-Bauer Method revealed that both test extract and positive control showed strong inhibition equivalent to 17.71 ± 6.3183 mm and 23.54 ± 4.9629 mm, respectively. Minimum Inhibitory Concentration of the plant extract was 50,000 ug/mL. Statistical analysis showed that there is no significant difference between the antifungal property of plant extract and positive control. Both test drugs have similar antifungal property, suggesting that the plant material is a good antifungal agent. The physical properties of vaginal cream conformed to the standard of physical properties of commercialized product available in the market.

scholarly journals Chemical composition of essential oils from the apiaceae family, cytotoxicity, and their antifungal activity in vitro against candida species from oral cavity

2019 ◽  
Vol 79 (3) ◽  
pp. 432-437 ◽  
Author(s):  
J. N. Vieira ◽  
C. L. Gonçalves ◽  
J. P. V. Villarreal ◽  
V. M. Gonçalves ◽  
R. G. Lund ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Antifungal Activity ◽  
Essential Oils ◽  
Inhibitory Concentration ◽  
Anethum Graveolens ◽  
Candida Spp ◽  
Foeniculum Vulgare ◽  
Main Components ◽  
L929 Mouse

Abstract The aims of this research were: evaluate the chemical composition and the cytotoxicity of the Cuminum cyminum (cumin), Anethum graveolens (dill), Pimpinella anisum (anise) and Foeniculum vulgare (fennel) essential oils, as well as their antifungal activity in vitro against ten Candida spp. isolates. The chemical composition of the oils was analyzed by means of gas chromatography coupled with mass spectrometry (GC/MS). The cytotoxicity assays were performed, using the cell proliferation reagent WST-1 in L929 mouse fibroblasts (20x103 well-1). The determinate the Minimum Inhibitory Concentration (MIC), was performed through the Broth Microdilution technique (CLSI). The chemical main components were the cuminaldehyde (32.66%) for cumin, carvone (34.89%) for the dill, trans-anethole (94.01%) for the anise and anethole (79.62%) for the fennel. Anise and fennel did not were cytotoxic in all the tested concentrations, however the cumin oil was cytotoxic in the concentration of 20 mg.mL-1 and the dill in the concentrations of 20 and 8 mg.mL-1. All yeasts were susceptible against the evaluated essential oils. Cumin presented the lowest MIC against yeasts. We concluded that all the essential oils presented inhibitory action against Candida spp., and C . cyminum, P. anisum and F. vulgare were not cytotoxic in the same minimum inhibitory concentrations for the fungi.

scholarly journals Study of the antifungal activity of ibuprofen and its association with amphotericin B or ketoconazole against Candida spp.

2020 ◽  
Vol 49 (2) ◽  
Author(s):  
Paula Mariane Silva Sousa ◽  
Jefferson Rodrigues Nóbrega ◽  
Laísa Vilar Cordeiro ◽  
Francisco Patricio De Andrade Júnio ◽  
Wylly Araújo de Oliveira
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Candida Species ◽  
Inhibitory Concentration ◽  
Synergistic Effects ◽  
Candida Spp ◽  
Antagonistic Effects ◽  
Microdilution Method ◽  
Clinical Applicability ◽  
Checkerboard Assay

The objective was evaluating the antifungal activity of ibuprofen alone and when associated with amphotericin B or ketoconazole against Candida species. Strains of C. albicans, C. tropicalis, C. guilliermondii, C. krusei and C. parapsilosis were used. The minimum inhibitory concentration (MIC) was determined by the microdilution method and the association study performed through the checkerboard assay. The concentration of 512 µg/mL inhibited approximately 65% of the tested strains, while against 35% of the strains presented MIC values above 2048 µg/mL. Associations of ibuprofen with amphotericin B against C. tropicalis and ibuprofen with ketoconazole against C. krusei showed synergistic effect. Antagonistic effects were evidenced in the combination of ibuprofen with amphotericin B against C. guilliermondii and C. albicans, as well as in the association of ibuprofen with ketoconazole against C. albicans and C. tropicalis. Through the experiments, it was found that ibuprofen showed antifungal activity against most of the Candida species tested. The combinations of ibuprofen and antifungals had synergistic effects. However, antagonistic results were evidenced in the association with ibuprofen, which would make clinical applicability difficult. Therefore, studies of this combined activity should be investigated, considering that this association may be positive for antifungal therapy.

scholarly journals Evaluation of the Antifungal Activity of Mentha x piperita (Lamiaceae) of Pancalieri (Turin, Italy) Essential Oil and Its Synergistic Interaction with Azoles

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3148 ◽  
Author(s):  
Vivian Tullio ◽  
Janira Roana ◽  
Daniela Scalas ◽  
Narcisa Mandras
Keyword(s):  
Antifungal Activity ◽  
Fungicidal Activity ◽  
Inhibitory Concentration ◽  
Trichophyton Mentagrophytes ◽  
Candida Spp ◽  
Antimicrobial Drugs ◽  
Minimum Fungicidal Concentration ◽  
Fungistatic Activity ◽  
Mentha X Piperita ◽  
Infection Treatment

The promising antimicrobial activity of essential oils (EOs) has led researchers to use them in combination with antimicrobial drugs in order to reduce drug toxicity, side effects, and resistance to single agents. Mentha x piperita, known worldwide as “Mentha of Pancalieri”, is produced locally at Pancalieri (Turin, Italy). The EO from this Mentha species is considered as one of the best mint EOs in the world. In our research, we assessed the antifungal activity of “Mentha of Pancalieri” EO, either alone or in combination with azole drugs (fluconazole, itraconazole, ketoconazole) against a wide panel of yeast and dermatophyte clinical isolates. The EO was analyzed by GC-MS, and its antifungal properties were evaluated by minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) parameters, in accordance with the CLSI guidelines, with some modifications. The interaction of EO with azoles was evaluated through the chequerboard and isobologram methods. The results suggest that this EO exerts a fungicidal activity against yeasts and a fungistatic activity against dermatophytes. Interaction studies with azoles indicated mainly synergistic profiles between itraconazole and EO vs. Candida spp., Cryptococcus neoformans, and Trichophyton mentagrophytes. Thus, the “Mentha of Pancalieri” EO may act as a potential antifungal agent and could serve as a natural adjuvant for fungal infection treatment.

scholarly journals Attempts to Access a Series of Pyrazoles Lead to New Hydrazones with Antifungal Potential against Candida Species Including Azole-Resistant Strains

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5861
Author(s):  
Georgiana Negru ◽  
Laure Kamus ◽  
Elena Bîcu ◽  
Sergiu Shova ◽  
Boualem Sendid ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
Direct Reaction ◽  
Pyrazole Derivatives ◽  
Candida Spp ◽  
X Ray ◽  
Antifungal Potential ◽  
Resistant Strains

The treatment of benzylidenemalononitriles with phenylhydrazines in refluxing ethanol did not provide pyrazole derivatives, but instead furnished hydrazones. The structure of hydrazones was secured by X-ray analysis. The chemical proof was also obtained by direct reaction of 3,4,5-trimethoxybenzaldehyde with 2,4-dichlorophenylhydrazine. Newly synthesized hydrazones were tested against eight Candida spp. strains in a dose response assay to determine the minimum inhibitory concentration (MIC99). Five compounds were identified as promising antifungal agents against Candida spp. (C. albicans SC5314, C. glabrata, C. tropicalis, C. parapsilosis and C. glabrata (R azoles)), with MIC99 values ranging from 16 to 32 µg/mL and selective antifungal activity over cytotoxicity.

scholarly journals Facilitated diffusion of glucosamine-6-phosphate synthase inhibitors enhances their antifungal activity.

2002 ◽  
Vol 49 (1) ◽  
pp. 77-86 ◽  
Author(s):  
Agnieszka Janiak ◽  
Barbara Cybulska ◽  
Joanna Szlinder-Richert ◽  
Edward Borowski ◽  
Sławomir Milewski
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Synergistic Effects ◽  
Lipid Vesicles ◽  
Facilitated Diffusion ◽  
Candida Spp ◽  
Fungal Cell ◽  
Methyl Ester Derivative ◽  
Diaminopropanoic Acid ◽  
Phosphate Synthase

N3-(4-Methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP) and 2-amino-2-deoxy-D-glucitol-6-phosphate (ADGP) are strong inhibitors of the essential fungal enzyme, glucosamine-6-phosphate synthase, but their antifungal activity is poor, due to slow penetration of these agents through the cytoplasmic membrane. In the present studies we have exploited the possibility of enhancement of ADGP and FMDP antifungal activity by improving their transport properties. It has been found that membrane-permeabilising polyene macrolides amphotericin B (AMB) and its N-methyl-N-fructosyl methyl ester derivative (MF-AME), at subinhibitory concentrations, facilitate diffusion of ADGP through the fungal cell membrane, thus allowing a decrease of its minimal inhibitory concentration (MIC). Synergistic effects have been observed for combinations of ADGP with AMB or MF-AME. Fractional inhibitory concentration (FIC) indexes, determined against a number of Candida spp., have been in the 0.18-0.81 range. Weak antifungal synergistic effects have been found for combinations of FMDP with AMB or MF-AME. ADGP can be easily encapsulated into unilamellar lipid vesicles. Liposomal preparations of ADGP demonstrated stronger antifungal activity against some fungal strains than free ADGP.

Pre Clinical Evaluation of Lagnub (Ficus septica, Moraceae) Leaf Crude Extract

10.17158/235 ◽  
2012 ◽  
Vol 18 (1) ◽  
Author(s):  
Judee N. Nogodula ◽  
Preziel F. Gran ◽  
Lyn Venice I. Salamanca ◽  
Ellaine Ann S. Yeo
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Clinical Isolate ◽  
Crude Extract ◽  
Ames Test ◽  
Inhibitory Concentration ◽  
Direct Method ◽  
Fixed Dose ◽  
Dermal Toxicity ◽  
Significant Difference

Lagnub is popularly used by Ata Matigsalog in Arakan, North Cotabato in treating skin infections. Scientific investigation was done to prove its folkloric claim by determining the acute dermal toxicity level, mutagenic activity, antifungal property using Candida albicans ATCC and two clinical isolates and its Minimum Inhibitory Concentration (MIC). Acute dermal toxicity was performed using the fixed dose of dried leaves at 1000 mg/kg (Sighting study) and 1000, 2000 and 5000 mg/kg for the main study. The protocol was based on OECD guideline. Susceptibility test for antifungal activity was done using Kirby-Bauer Method. Two-fold agar dilution was followed for Minimum Inhibitory Concentration and Direct Method of Ames test was performed for mutagenicity. Results showed that the dried leaf crude extract was categorized as non-toxic because there were no deaths of rabbits or evident toxicity at the upper limit dose of 5000 mg/kg. However, Ames test revealed that the dried leaf extract was considered as mutagenic against Salmonella typhimurium TA98. Antifungal activity revealed that the leaf crude extract was interpreted as active having a zone of 16.67 mm ±5.3852 (C. albicans ATCC), clinical isolate 1 is 12.55 ±3.2974 mm, and clinical isolate 2 is 12.51 ±3.4278 mm. Statistically, there was a significant difference in the mean zones of inhibition exhibited by the plant material against the test organisms. Meanwhile, the minimum inhibitory concentration of lagnub was 52, 631.58 μg/mL

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