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1.
Saudi Dent J ; 36(2): 364-367, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38419998

ABSTRACT

Loss of kidney function causes oral manifestations and multiple complications that have implications for dental treatment and patients' systemic conditions. We aimed to determine the clinical condition, epidemiological profile, and incidence of dental caries in patients with chronic kidney disease (CKD). This was an observational, cross-sectional, field study using a quantitative and epidemiological approach. The sample consisted of 45 randomly selected patients with CKD from a total of 114 patients. Data were collected through oral clinical examination, anamnesis, and medical records compiled in a clinical file specially developed for this research. Clinical evaluation was performed, including a Decayed, Missing, and Filled Teeth (DMFT) index examination. Data were analyzed using the Shapiro-Wilk test, Mann-Whitney test, and Spearman's rho coefficient. All analyses were performed using IBM SPSS Statistics software version 20.0, with a confidence interval of 95 % and significance level of 5 % (p < 0.05). The results indicated that CKD is more prevalent in the 5th decade of life, with a slight predilection for men. Oral cavity alterations were observed in 77.8 % of patients. The study population had a very high DMFT index, with a high number of missing teeth and a low number of decayed and filled teeth. Poor oral health in patients with CKD indicates a lack of care that supports the necessity of installing a preventive and therapeutic oral program and a regular follow-up aimed at this group of patients.

2.
Drug Chem Toxicol ; 47(2): 191-202, 2024 Mar.
Article in English | MEDLINE | ID: mdl-36803623

ABSTRACT

Aspergillus niger causes infections such as otitis and pulmonary aspergillosis in immunocompromised individuals. Treatment involves voriconazole or amphotericin B, and due to the increase in fungal resistance, the search for new compounds with antifungal activity has intensified. In the development of new drugs, cytotoxicity and genotoxicity assays are important, as they allow predicting possible damage that a molecule can cause, and in silico studies predict the pharmacokinetic properties. The aim of this study was to verify the antifungal activity and the mechanism of action of the synthetic amide 2-chloro-N-phenylacetamide against Aspergillus niger strains and toxicity. 2-Chloro-N-phenylacetamide showed antifungal activity against different strains of Aspergillus niger with minimum inhibitory concentrations between 32 and 256 µg/mL and minimum fungicides between 64 and 1024 µg/mL. The minimum inhibitory concentration of 2-chloro-N-phenylacetamide also inhibited conidia germination. When associated with amphotericin B or voriconazole, 2-chloro-N-phenylacetamide had antagonistic effects. Interaction with ergosterol in the plasma membrane is the probable mechanism of action.2-Chloro-N-phenylacetamide has favorable physicochemical parameters, good oral bioavailability and absorption in the gastrointestinal tract, crosses the blood-brain barrier and inhibits CYP1A2. At concentrations of 50 to 500 µg/mL, it has little hemolytic effect and a protective effect for type A and O red blood cells, and in the cells of the oral mucosa it promotes little genotoxic change. It is concluded that 2-chloro-N-phenylacetamide has promising antifungal potential, favorable pharmacokinetic profile for oral administration and low cytotoxic and genotoxic potential, being a promising candidate for in vivo toxicity studies.


Subject(s)
Antifungal Agents , Aspergillosis , Aspergillus , Humans , Antifungal Agents/toxicity , Amphotericin B/toxicity , Voriconazole/toxicity , Voriconazole/therapeutic use , Aspergillosis/drug therapy , Aspergillosis/microbiology , Acetanilides/therapeutic use , Microbial Sensitivity Tests
3.
Nat Prod Res ; : 1-9, 2023 Nov 07.
Article in English | MEDLINE | ID: mdl-37933528

ABSTRACT

The present study aimed to investigate the antifungal activity of citronellal (CIT) against clinical isolates of T. rubrum and to show the possible mechanism of action involved. The antifungal potential of CIT was evaluated from the Minimum Inhibitory Concentration (MIC), Minimum Fungicide Concentration (MFC) and assays with ergosterol and sorbitol, to elucidate the possible mechanisms of action, and molecular docking. MIC and MFC values ranged from 4 to 512 µg/mL. Regarding the mechanism of action, the monoterpene demonstrated interaction with fungal ergosterol. In addition, it is possible to observe that CIT acts on crucial enzymes for the biosynthesis and maintenance of the fungal cell membrane, due to the ability of the monoterpene to bind to CYP51. The results obtained in this research demonstrate that CIT has the potential to become, in the future, a product for the treatment of dermatophytosis.

4.
J Fungi (Basel) ; 9(2)2023 Feb 09.
Article in English | MEDLINE | ID: mdl-36836345

ABSTRACT

The ability of dermatophytes to develop biofilms is possibly involved in therapeutic failure because biofilms impair drug effectiveness in the infected tissues. Research to find new drugs with antibiofilm activity against dermatophytes is crucial. In this way, riparins, a class of alkaloids that contain an amide group, are promising antifungal compounds. In this study, we evaluated the antifungal and antibiofilm activity of riparin III (RIP3) against Trichophyton rubrum, Microsporum canis, and Nannizzia gypsea strains. We used ciclopirox (CPX) as a positive control. The effects of RIP3 on fungal growth were evaluated by the microdilution technique. The quantification of the biofilm biomass in vitro was assessed by crystal violet, and the biofilm viability was assessed by quantifying the CFU number. The ex vivo model was performed on human nail fragments, which were evaluated by visualization under light microscopy and by quantifying the CFU number (viability). Finally, we evaluated whether RIP3 inhibits sulfite production in T. rubrum. RIP3 inhibited the growth of T. rubrum and M. canis from 128 mg/L and N. gypsea from 256 mg/L. The results showed that RIP3 is a fungicide. Regarding antibiofilm activity, RIP3 inhibited biofilm formation and viability in vitro and ex vivo. Moreover, RIP3 inhibited the secretion of sulfite significantly and was more potent than CPX. In conclusion, the results indicate that RIP3 is a promising antifungal agent against biofilms of dermatophytes and might inhibit sulfite secretion, one relevant virulence factor.

5.
PLoS One ; 18(1): e0275835, 2023.
Article in English | MEDLINE | ID: mdl-36630475

ABSTRACT

An increase in the incidence of arboviral, microbial and parasitic infections, and to disorders related to oxidative stress has encouraged the development of adjuvant therapies based on natural formulations, such as those involving plant extracts. Thus, to expand the repertoire of the available therapeutic options, this study aimed to describe the versatility of Tephrosia toxicaria (Sw.) (Pers., 1807) extracts for the control of arbovirus vectors, as well as their antioxidant, antileishmanial, and antimicrobial potential. Among the aqueous and hydroethanolic extracts obtained, the hydroethanolic extract from roots (RHA) was identified as the most active larvicide extract demonstrating, respectively, the lowest lethal concentration (mg/mL) for 50%, 90% and 99% of Aedes aegypti (L., 1762) and Aedes albopictus (S., 1894) larvae, observed at 24 h (0.33, 0.84 and 1.80; 0.32, 0.70 and 1.32) and 48 h (0.17, 0.51 and 1.22; 0.26, 0.47 and 0.78) post-exposure. Field assays revealed that RHA (0.84 mg/mL) is a potential oviposition deterrent, reducing egg-laying by approximately 90%. RHA (0.1 mg/mL) also exhibited antioxidant activity for the following tests: total antioxidant capacity (286.86 mg AAE/g), iron (87.16%) and copper (25.64%) chelation, and superoxide scavenging (10%). In the cell culture assays, RHA (0.1 mg/mL) promoted regeneration of metabolic activity (92% cell viability) in cells exposed to oxidative stress. Furthermore, RHA displayed weak antileishmanial activity (IC50 = 3.53 mg/mL) against Leishmania amazonensis and not exhibit antimicrobial activity. The extraction favored the concentration of carbohydrates in RHA, in addition to lectins and protease inhibitors, with molecular masses estimated between 10 and 24 kDa. Cytotoxicity and phytotoxicity analyses of RHA suggested its biosecurity. Thus, RHA is a multivalent extract with insecticide and antioxidant properties at low and safe concentrations. However, others studies on its indirect toxic effects are ongoing to ensure the complete safety of RHA.


Subject(s)
Aedes , Anti-Infective Agents , Antiprotozoal Agents , Tephrosia , Animals , Female , Antioxidants/pharmacology , Mosquito Vectors , Plant Extracts/toxicity , Antiprotozoal Agents/pharmacology , Anti-Infective Agents/pharmacology
6.
Braz. J. Pharm. Sci. (Online) ; 58: e20075, 2022. tab, graf
Article in English | LILACS | ID: biblio-1403710

ABSTRACT

Abatsract Pseudomonas aeruginosa is an important nosocomial pathogen and its clinical importance is mainly related to nosocomial infections. Increased rates of bacterial resistance in recent years has led WHO to publish a global priority list to guide research and discovery of new antibiotics, where P. aeruginosa is among the group of bacteria for which there is a critical level of priority for new drugs to be discovered. In this context, isoeugenol appears as an interesting alternative and the objective of this study was to investigate its action against P. aeruginosa. Isoeugenol presented significant antibacterial activity, with minimum inhibitory concentration (MIC) of 64µg/mL and minimum bactericidal concentration (MBC) of 128µg/mL, and was considered bactericidal against this species. Molecular docking revealed interactions that suggest that isoeugenol may bind to the enzyme Penicillin-Binding Protein 3 and interfere with the bacterial cell wall synthesis process. This study reinforces the antibacterial potential of this compound and emphasizes that more studies are needed in order to better investigate its mechanism of antibacterial action.


Subject(s)
Pseudomonas aeruginosa/drug effects , Anti-Bacterial Agents/adverse effects , Bacteria/classification , World Health Organization , Microbial Sensitivity Tests/instrumentation , Penicillin-Binding Proteins/agonists , Reference Drugs , Molecular Docking Simulation/methods
7.
Rev. Ciênc. Méd. Biol. (Impr.) ; 20(2): 296-300, set 29, 2021.
Article in English | LILACS | ID: biblio-1354492

ABSTRACT

Introduction: tuberculosis is a bacteriosis caused by the etiological agent Mycobacterium tuberculosis, which initially affects the lungs, however it can become extrapulmonary. Although this infection is an important public health problem in Brazil, epidemiological studies on this disease are scarce. Objective: thus, the present study aimed to elucidate the epidemiological profile of people affected by tuberculosis in Campina Grande ­ PB, between the years 2014 to 2018. Methodology: this is an epidemiological, retrospective, analytical and documentary study, in which data were collected from the Department of Informatics of the "Sistema Único de Saúde". Results: Between 2014 and 2018, 795 cases of tuberculosis were reported in Campina Grande-PB, with 2018 having the highest number of cases (24.6%). The epidemiological profile of those affected was predominantly male, aged 20 to 39 years, with low schooling, mixed race and residents of the urban area. When associating sex with immunosuppressive factors, a statistically significant association was observed between, HIV, the state of acquired immunodeficiency syndrome (AIDS) and alcoholism (p <0.05). Conclusion: in this way, the data of this research can guide the development of indicators and public policies for the most susceptible population.


Introdução: a tuberculose é uma bacteriose causada pelo agente etiológico Mycobacterium tuberculosis, que inicialmente acomete os pulmões, entretanto pode tornar-se extrapulmonar. Mesmo esta infecção tratando-se de um importante problema de saúde pública no Brasil, há grande escassez de estudos epidemiológicos referentes a essa doença. Objetivo: o presente estudo teve como objetivo elucidar o perfil epidemiológico de acometidos por tuberculose em Campina Grande, PB, entre os anos de 2014 a 2018. Metodologia: trata-se de um estudo epidemiológico, retrospectivo, analítico e documental, em que os dados foram coletados a partir do Departamento de Informática do Sistema Único de Saúde. Resultados: entre 2014 a 2018, foram notificados 795 casos de tuberculose em Campina Grande, PB, sendo que o ano de 2018 foi aquele com o maior número de casos ­ 24,6%. O perfil epidemiológico de acometidos foi, predominantemente, de indivíduos do gênero masculino, com 20 a 39 anos de idade, baixa escolaridade, etnia parda e residentes da zona urbana. Ao associar o gênero com os fatores imunossupressores, observouse associação estatisticamente significativa entre VIH, estado de SIDA e alcoolismo (p<0,05). Conclusão: assim, os dados desta pesquisa podem nortear o desenvolvimento de indicadores e políticas públicas para a população mais susceptível.


Subject(s)
Humans , Male , Adult , Middle Aged , Aged , Tuberculosis , Epidemiology , Mycobacterium , Ethnicity , Epidemiologic Studies , Laboratory and Fieldwork Analytical Methods , Retrospective Studies , Educational Status
8.
Rev. Ciênc. Méd. Biol. (Impr.) ; 20(1): 120-124, maio 5, 2021. fig, tab
Article in Portuguese | LILACS | ID: biblio-1355053

ABSTRACT

Introduction: dermatophytoses or "tineas" are characterized by being mycoses caused by fungi of the genera Epidermophyton, Trichophyton and Microsporum. These mycotic infections can present themselves as a form of lesions that affect the skin, hair and nails of individuals of both genders and all ages. Objective: to elucidate the epidemiological profile of dermatophytoses in patients examined by a private clinical analysis laboratory in João Pessoa-PB, between 2015 and 2019. Methodology: this is an epidemiological, analytical, retrospective and documentary study, in which data collection took place at the Clinical Pathology Laboratory ­ "HEMATO", located in João Pessoa ­ PB. Results: the profile of those affected was predominantly female (58.5%), 18 to 59 years old (38.4%), white (53.6%) and with lesions, mainly in skin glabrous (38.5%), feet (33.3%) and nails (12.8%). When relating the age group to the injury site, it was noticed that injuries on glabrous skin, feet and nails, were more frequent in individuals aged 18 to 59 years, while injuries to the scalp were mostly found in individuals younger than 18 years old. The most prevalent species were M. canis (31.9%) and T.rubrum (31.9%). When correlating the fungal species with the lesion site, it was noted that M. canis was the main agent responsible for lesions in glabrous skin, scalp and hands, while T. rubrum was predominantly observed in nails and T. mentagrophytes in feet. Conclusion: it is concluded that the data present in this research can promote the development of indicators and public policies for the population most susceptible to dermatophytosis.


Introdução: dermatofitoses ou tineas se caracterizam por serem micoses causadas por fungos dos gêneros Epidermophyton, Trichophyton e Microsporum. Essas infecções micóticas podem se apresentar na forma de lesões que acometem pele, pelo e unhas de indivíduos de ambos os gêneros e todas as idades. Objetivo: elucidar o perfil epidemiológico de dermatofitoses de pacientes atendidos por um laboratório privado de análises clínicas em João Pessoa-PB, entre 2015 a 2019. Metodologia: trata-se de um estudo epidemiológico, analítico, retrospectivo e documental, em que a coleta de dados ocorreu no Laboratório de Patologia Clínica ­ HEMATO, localizado em João Pessoa ­ PB. Resultados: o perfil de acometidos foi predominantemente de indivíduos do sexo feminino (58,5%), com 18 a 59 anos de idade (38,4%), brancos (53,6%) e com lesões, principalmente, em pele glabra (38,5%), pés (33,3%) e unhas (12,8%). Ao relacionar a faixa etária com o local da lesão, percebeu-se que lesões em pele glabra, pés e unhas, foram mais frequentes em indivíduos de 18 a 59 anos, enquanto que lesões no couro cabeludo foram majoritariamente encontradas em indivíduos menos de 18 anos. As espécies mais prevalentes foram M. canis (31,9%) e T. rubrum (31,9%). Ao correlacionar a espécie fúngica com o local da lesão, notou-se que M. canis foi o principal agente responsável por lesões em pele glabra, couro cabeludo e mãos, enquanto T. rubrum foi predominantemente observado em unhas e T. mentagrophytes em pés. Conclusão: os dados obtidos nesta pesquisa podem fomentar o desenvolvimento de indicadores e políticas públicas para a população mais susceptível às dermatofitoses.


Subject(s)
Humans , Male , Female , Adolescent , Adult , Middle Aged , Aged , Tinea , Arthrodermataceae , Fungi , Laboratory and Fieldwork Analytical Methods , Epidemiologic Methods , Retrospective Studies
9.
Nat Prod Res ; 35(24): 6002-6006, 2021 Dec.
Article in English | MEDLINE | ID: mdl-32975125

ABSTRACT

Infections associated with biofilms developed by Candida spp. are becoming a great problem due to its resistance against the immune response of the host and the action of antifungal agents. Hence, finding substances that can inhibit the development of biofilms increases the likelihood that these compounds one day can become good antifungals applied in the clinic. The aim of this study was to evaluate the effect of ß-citronellol enantiomers on the biofilm formation by Candida albicans and Candida tropicalis isolated from bloodstream infections. Inhibition was evaluated by reading microplates treated with different concentrations of R-(+)-ß-citronellol, S-(-)-ß-citronellol and amphotericin B, compared to negative control, in spectrophotometer at 590 nm. All tested concentrations of ß-citronellol enantiomers inhibited the biofilm formation of Candida. However, it is still necessary to evaluate the behavior of these isomers on mature biofilms, so that they can become more viable as antifungal therapeutical agents.


Subject(s)
Antifungal Agents , Candida , Acyclic Monoterpenes , Antifungal Agents/pharmacology , Biofilms , Candida albicans , Microbial Sensitivity Tests
10.
Nat Prod Res ; 35(24): 6190-6193, 2021 Dec.
Article in English | MEDLINE | ID: mdl-33094646

ABSTRACT

The genus Candida is one of the main causes of otomycosis. The growing index of fungal strains resistant to antifungals makes necessary the search for new agents and α-pinene is a phytoconstituent present in plants with remarkable antimicrobial activity, which becomes an interesting object of study. Thus, the objective of this research was to evaluate the antifungal activity of α-pinene against Candida species isolated from otomycosis, determining the Minimum Inhibitory and Fungicide Concentrations, micromorphological analysis and verifying the effects of the association with boric acid. α-pinene showed significant antifungal activity, with greater inhibitory activity against C. parapsilosis, fungicidal action and proved to be effective in inhibiting fungal structures, such as pseudo-hyphae and promoting a marked decrease in blastoconidia. The combination of α-pinene with boric acid produced additive effects that may be interesting for use in clinical practice.


Subject(s)
Antifungal Agents , Otomycosis , Antifungal Agents/pharmacology , Bicyclic Monoterpenes , Boric Acids , Candida , Humans , Microbial Sensitivity Tests
11.
World J Gastroenterol ; 26(43): 6795-6809, 2020 Nov 21.
Article in English | MEDLINE | ID: mdl-33268962

ABSTRACT

BACKGROUND: (-)-Fenchone is a bicyclic monoterpene present in essential oils of plant species, such as Foeniculum vulgare and Peumus boldus, used to treatment of gastrointestinal diseases. Pharmacological studies report its anti-inflammatory, antioxidant, and antinociceptive activity. AIM: To investigate antidiarrheal activity related to gastrointestinal motility, intestinal secretion and antimicrobial activity. METHODS: A castor oil-induced diarrhea model was used to evaluate antidiarrheal activity. Intestinal transit and gastric emptying protocols were used to assess a possible antimotility effect. Muscarinic receptors, presynaptic α2-adrenergic and tissue adrenergic receptors, KATP channels, nitric oxide were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms. The antimicrobial activity was evaluated in the minimum inhibitory concentration model, the fractional inhibitory concentration index using the (-)-fenchone association method with standard antifungal agents. RESULTS: (-)-Fenchone (75, 150 and 300 mg/kg) showed antidiarrheal activity, with a significant decrease in the evacuation index. This activity is possibly related to a percentage of reduced intestinal transit (75, 150 and 300 mg/kg). The antimotility effect of (-)-fenchone decreased in the presence of pilocarpine, yohimbine, propranolol, L-NG-nitroarginine methyl ester or glibenclamide. In the enteropooling model, no reduction in intestinal fluid weight was observed. (-)- Fenchone did not show antibacterial activity; on the other hand, inhibits the growth of strains of fungi with a minimum fungicide concentration of 32 µg/mL. However, when it was associated with amphotericin B, no synergism was observed. CONCLUSION: The antidiarrheal effect of (-)-fenchone in this study involves antimotility effect and not involve antisecretory mechanisms. (-)-Fenchone presents antifungal activity; however, it did not show antibacterial activity.


Subject(s)
Antidiarrheals , Antifungal Agents , Antidiarrheals/pharmacology , Antidiarrheals/therapeutic use , Antifungal Agents/pharmacology , Antifungal Agents/therapeutic use , Camphanes , Diarrhea/chemically induced , Diarrhea/drug therapy , Gastrointestinal Motility , Humans , Models, Theoretical , Norbornanes , Plant Extracts/pharmacology , Plant Extracts/therapeutic use
12.
Rev. Ciênc. Méd. Biol. (Impr.) ; 19(3): 489-494, dez 5, 2020. tab
Article in Portuguese | LILACS | ID: biblio-1358023

ABSTRACT

Objetivo: investigar a suscetibilidade de cepas fúngicas de Candida parapsilosis isoladas de sangue humano frente ao timol, bem como seu mecanismo de ação. Metodologia: foram utilizadas técnicas de microdiluição em placas de 96 poços para determinar a concentração inibitória mínima (CIM) e concentração fungicida mínima (CFM). Além disso, foram realizados testes com o sorbitol e o ergosterol para investigar a ação do timol na parede e na membrana celular fúngica respectivamente. Resultados: nos testes de CIM e CFM, foi observado que as cepas de C. parapsilosis são resistentes ao fluconazol e a anfotericina B, no entanto, o timol desempenhou efeito fungicida com razão CFM/CIM entre 1 e 2. Além disso, a CIM do timol não aumentou quando o sorbitol ou o ergosterol foi adicionado no meio, sugerindo fortemente que este monoterpeno não age na parede celular fúngica ou por ligação ao ergosterol na membrana plasmática. Conclusão: portanto, esses resultados contribuem para a elucidação do mecanismo de ação do timol, sugerindo outros possíveis alvos de interação fármaco-receptor. No entanto, mais investigações de caráter enzimático e molecular em modelos in vitro são necessários para que se possa elucidar completamente o modo de ação desse promissor monoterpeno.


Objective: to investigate the susceptibility of fungal strains of Candida parapsilosis isolated from human blood against thymol, as well as its mechanism of action. Methodology: microdilution techniques were used in 96-well plates to determine minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). In addition, tests were performed with sorbitol and ergosterol to investigate the action of thymol on the wall and on the fungal cell membrane respectively. Results: in the CIM and CFM tests, it was observed that C. parapsilosis strains are resistant to fluconazole and amphotericin B, however, thymol had a fungicidal effect with MFC/MIC ratio between 1 and 2. In addition, thymol MIC did not increase when sorbitol or ergosterol was added in the medium, strongly suggesting that this monoterpene does not act on the fungal cell wall or by binding to ergosterol on the plasma membrane. Conclusion: therefore, these results contribute to the elucidation of the mechanism of action of thymol, suggesting other possible targets of drug-receptor interaction. However, further investigations of enzymatic and molecular character in in vitro models are necessary to fully elucidate the mode of action of this promising monoterpene.


Subject(s)
Humans , Thymol , Fluconazole , Amphotericin B , Candidiasis, Invasive , Candida parapsilosis , Anti-Infective Agents , Antifungal Agents , Sorbitol , Ergosterol
13.
Nat Prod Res ; 34(18): 2630-2633, 2020 Sep.
Article in English | MEDLINE | ID: mdl-30584769

ABSTRACT

Cryptococcus neoformans is a yeast fungus, which causes cryptococcosis, triggered by basidiospore inhalation and consequent dissemination to the central nervous system. In this study, we analyzed the antifungal action of thymol against 10 clinical strains of C. neoformans and analyzed the interaction of this monoterpene with sterols. The MICs of thymol ranged from 20 to 51 µg/ml, while the MFC values varied between 40 and 101 µg/ml. For the strains ICB-2601 and LM-39, in the presence of ergosterol, the MIC of thymol was 64 µg/ml, and in the presence of cholesterol, its MIC was 32 µg/ml. Based on the results, thymol presents antifungal action and seems to interact with ergosterol, but not with cholesterol. Complementary studies are needed to analyze its full effects.


Subject(s)
Antifungal Agents/pharmacology , Cryptococcosis/drug therapy , Cryptococcus neoformans/drug effects , Monoterpenes/pharmacology , Thymol/pharmacology , Cholesterol/pharmacology , Cryptococcosis/microbiology , Drug Interactions , Ergosterol/pharmacology , Microbial Sensitivity Tests
14.
Med Mycol ; 58(2): 272-274, 2020 Feb 01.
Article in English | MEDLINE | ID: mdl-31329906

ABSTRACT

This study investigated the monoterpene linalool and its resistance modulating activity involving ergosterol biosynthesis inhibitors (ketoconazole, fluconazole, and itraconazole) in strains of Microsporum spp. and Trichophyton spp. The minimum inhibitory concentration (MIC) of test-drugs were determined by microdilution. The modulating effect of linalool was evaluated by determining the MIC of the antifungals in the presence of subinhibitory concentrations of linalool. We also investigated the association effect (checkerboard) of linalool together with ketoconazole and itraconazole. The fungi became more sensitive to ketoconazole and itraconazole in the presence of linalool. The linalool and azole drug associations presented synergism.


Subject(s)
Acyclic Monoterpenes/pharmacology , Antifungal Agents/pharmacology , Azoles/pharmacology , Microsporum/drug effects , Trichophyton/drug effects , Drug Synergism , Itraconazole/pharmacology , Ketoconazole/pharmacology , Microbial Sensitivity Tests , Microsporum/growth & development , Trichophyton/growth & development
15.
Rev. Ciênc. Méd. Biol. (Impr.) ; 17(1): 57-60, jul.17,2018. tab
Article in Portuguese | LILACS | ID: biblio-909971

ABSTRACT

Introdução: aproximadamente 75% das mulheres saudáveis experimentam pelo menos um episódio sintomático de candidíase vulvovaginal (CVV) durante sua vida. Objetivo: avaliar a atividade antifúngica contra cepas de C. tropicalis dos enantiômeros (R)-(+) ­ e (S)-(-)-citronelal [(R)-(+) ­ e (S)-(-)-CT] em associação com cetoconazol. Metodologia: o efeito antifúngico de ambos os enantiômeros foram quantificados e classificados como fungicida ou fungistático a partir dos resultados obtidos da microdiluição em meio líquido RPMI1640 para a obtenção da concentração inibitória mínima (CIM) e da concentração fungicida mínima (CFM). Foram realizados ensaios de associação do antifúngico padrão, cetoconazol com os fitoconstituintes por difusão em Agar e os resultados foram classificados como sinérgicos, antagônicos e indiferentes. Resultados: a CIM50 e a CFM50 dos compostos (R)-(+) ­ e (S)-(-)-citronelal foram respectivamente 16 e 64µg/mL e 2×CIM. Houve sinergismo para todas as cepas testadas com ambos os compostos, porém com maior efeito do enantiômero (S)-(-)-CT sobre as cepas LM 665 e LM 255 em relação ao enantiômero (R)-(+)-CT. Conclusão: os compostos naturais deste estudo mostraram efeito fungicida sobre as cepas testadas, bem como efeito sinérgico significativo quando associado ao cetoconazol


Subject(s)
Female , Candida tropicalis
16.
Molecules ; 22(9)2017 Sep 17.
Article in English | MEDLINE | ID: mdl-28926981

ABSTRACT

We evaluated the antifungal and anti-biofilm activity, mechanism of action and cytotoxicity of chloramine T trihydrate (CAT) against Candida spp. The Minimum Inhibitory and Fungicidal Concentrations (MIC/MFC) of CAT were determined. Changes in CAT-treated C. albicans growth kinetics and micromorphology were evaluated, as well as the mechanism of action, and its effects on biofilm. Cytotoxicity was assessed by the hemolysis method. The data were analyzed by inferential statistics (p ≤ 0.05). CAT showed antifungal activity against all strains, with MIC values ranging between 1.38 and 5.54 mmol/L (MIC75%: 2.77 mmol/L). CAT demonstrated an immediate and sustained action on C. albicans growth kinetics, particularly at 2 × MIC. This compound likely acts on the cell wall and membrane permeability simultaneously and was found to cause changes in C. albicans micromorphology. Tha antibiofilm activity of CAT was similar to that of sodium hypochlorite (p > 0.05) against mature biofilms. CAT was more effective than NaOCl in reducing mature biofilm upon 1-min exposure at 2 × MIC (24 h) and 4 × MIC (48 h) (p < 0.05). Toxicological analysis revealed that CAT had hemolytic activity between 61 and 67.7% as compared to 100% by NaOCl. CAT has antifungal and anti-biofilm properties, probably acting on both cell wall and membrane permeability, and showed low toxicity in vitro.


Subject(s)
Antifungal Agents/pharmacology , Biofilms/drug effects , Candida albicans/drug effects , Chloramines/pharmacology , Disinfectants/pharmacology , Tosyl Compounds/pharmacology , Antifungal Agents/toxicity , Candida albicans/growth & development , Cell Line , Cell Survival/drug effects , Chloramines/toxicity , Disinfectants/toxicity , Hemolysis , Humans , Kinetics , Permeability , Tosyl Compounds/toxicity
17.
Biosci. j. (Online) ; 33(2): 494-506, mar./apr. 2017. ilus, tab, graf
Article in English | LILACS | ID: biblio-966207

ABSTRACT

Vulvovaginal candidiasis (VVC) is a common fungal infection that affects healthy women of all ages. At least 75% of women will develop one or more infections once during their lifetime, with 6 to 9% of those individuals developing recurrent infections. In view of this context, this study sought to evaluate the antifungal potential of the isolated (R)-(+)-citronellal [(R)-(+)-CT] and associated to therapeutic agents of clinical importance. The enantiomer was solubilized in tween 80 and dimethylsulfoxide (DMSO). Posteriorly diluted in sterile distilled water up to the concentration of 2048µg/mL. The minimum inhibitory concentration (MIC) of the product was determined by microdilution in RPMI-1640 obtaining dilutions of 1024-4µg/mL. The minimum fungicidal concentration (MFC) was determined by the Sabouraud dextrose agar (SDA) depletion technique from aliquots of 1µL of the MIC, MIC × 2 and MIC × 4. The MIC and the MFC values of (R)-(+)-CT for 90% of the C. albicans strains were 16 and 32µg/mL respectively. In the susceptibility test, C. albicans presented a high resistance to fluconazole and to itraconazole, 12 (92.30%) of the strains. However, for ketoconazole and miconazole the resistance was of 4 (30.76%) and 3 (23.07%) of the strains respectively. In the combination testing of the (R)-(+)-CT with ketoconazole and miconazole, the resistance was completely reverted. For fluconazole and itraconazole, the resistance was reverted in 9 (75%) and 7 (58.33%) of the strains respectively. The (R)-(+)-CT presented fungicide activity with MFC of MIC × 2. When in combination with ketoconazole, fluconazole, itraconazole and miconazole increased the inhibition zones of these antifungal drugs, reducing the resistance against C. albicans.


Candidíase vulvovaginal (CVV) é uma infecção fúngica comum que afeta mulheres saudáveis de todas as idades. Pelo menos 75% das mulheres irão desenvolver uma ou mais infecções uma vez durante a vida, com 6 a 9% dos indivíduos desenvolvendo infecções recorrentes. Diante deste contexto, buscou-se avaliar neste estudo o potencial antifúngico do (R)-(+)-citronelal [(R)-(+)-CT] isolado e associado a agentes terapêuticos de importância clínica. O enantiômero foi solubilizado em tween 80 e dimetilsulfóxido (DMSO). Posteriormente diluiu-se em água destilada estéril até a concentração de 2048µg/mL. A concentração inibitória mínima (CIM) do produto foi determinada por microdiluição em meio RPMI-1640 obtendo diluições de 4-1024µg/mL. A concentração fungicida mínima (CFM) foi determinada pela técnica de esgotamento em agar Sabouraud dextrose (ASD) a partir de alíquotas de 1mL da CIM, CIM × 2 e CIM × 4. A CIM e a CFM do (R)-(+)-CT para 90% das cepas de C. albicans foram 16 e 32µg/mL respectivamente. No ensaio de suscetibilidade, C. albicans apresentou alta resistência ao fluconazol e ao itraconazol, 12 (92.30%) das cepas. No em tanto, para o cetoconazol e o miconazol a resistência foi de 4 (30.76%) e 3 (23.07%) das cepas respectivamente. No ensaio de combinação do (R)-(+)-CT com cetoconazol e miconazol, a resistência foi completamente revertida. Para o fluconazol e o itraconazol, a resistências foi revertida em 9 (75%) e 7 (58.33%) das cepas respectivamente. O (R)-(+)-CT apresentou atividade fungicida com CFM igual à CIM × 2. Quando em combinação com cetoconazol, fluconazol, itraconazol e miconazol ampliou as zonas de inibição desses antifúngicos, diminuindo a resistência contra C. albicans.


Subject(s)
Candida albicans , Candidiasis, Vulvovaginal , Antifungal Agents
18.
Biosci. j. (Online) ; 33(1): 204-208, jan./feb. 2017. tab
Article in English | LILACS | ID: biblio-965892

ABSTRACT

The fungi of the genus Candida play a relevant role in the emergence of oral infections and are increasingly more frequent the cases of infections by non-albicans strains. In light of this context and the need for new alternatives to the antimicrobial therapy, the monoterpene [7-hidroxicitronelal] (7-HO) was evaluated for its antifungal effects. For the obtainment of the MIC and MFC values the broth microdilution method was used. The MIC and the MFC of this monoterpene for 60% of the tested strains was of 256µg/mL and 512µg/mL respectively. Furthermore, the standard antifungal nystatin (100UI/mL) was used as positive control for the inhibition of fungal growth. Therefore, were used 4 clinical strains of the species tropicalis (LM 06, LM 14, LM 31 and LM 36) and a standard strain (C. tropicalis ATCC 13803), originated from the Mycology collection of the Mycology Laboratory (LM) of the Health Sciences Center (CCS) of the Federal University of Paraiba (UFPB). The results obtained in this study showed fungicide activity of the compound (7-OH) against the strains of C. tropicalis.


Os fungos do gênero Candida tem um papel relevante no aparecimento de infecções orais e são cada vez mais frequentes os casos de infecções por cepas não-albicans. Diante deste contexto e da necessidade de novas alternativas para a terapia antimicrobiana, o monoterpeno [7-hidroxicitronelal] (7-HO) foi avaliado pelos seus efeitos antifúngicos. Para a obtenção dos valores da CIM e da CFM foi utilizado o método da microdiluição em caldo. A CIM e a CFM deste monoterpeno para 60% das cepas testadas foram de 256µg/mL e 512µg/mL respectivamente. Além disso, o antifúngico padrão nistatina (100UI/mL) foi utilizado como controle positivo para inibir o crescimento fúngico. Por tanto, foram utilizadas 4 cepas clínicas da espécie tropicalis (LM 06, LM 14, LM 31 e LM 36) e uma cepa padrão (C. tropicalis ATCC 13803), oriundas da Micoteca do Laboratório de Micologia (LM) do Centro de Ciências da Saúde (CCS) da Universidade Federal da Paraíba (UFPB). Os resultados obtidos neste estudo mostraram atividade fungicida do composto (7-OH) contra as cepas de C. tropicalis.


Subject(s)
In Vitro Techniques , Candidiasis, Oral , Monoterpenes , Antifungal Agents
19.
Rev. Inst. Adolfo Lutz (Online) ; 76: 1-8, 2017. tab, graf
Article in English | LILACS, Sec. Est. Saúde SP, SESSP-ACVSES, SESSP-IALPROD, Sec. Est. Saúde SP, SESSP-IALACERVO | ID: biblio-982799

ABSTRACT

Cladosporium spp. is a group of dematiaceous food-relevant fungi which are well dispersed in the environment causing food spoilage and poisoning. Considering the importance of fungalcontamination, natural drugs to control their growth have become important. Thus, the aim of this study was to evaluate the inhibitory effects of two monoterpenoids, (geraniol and citronellol), against strains of Cladosporium carrioni, C. cladosporioides, and C. oxysporum. Methods: The Minimum Inhibitory Concentration (MIC) and Minimum Fungicide Concentration (MFC) of the drugs were determined by microdilution. The effects of test drugs on mycelial dry weight, conidia germination, and conidiogenesis of Cladosporium spp. were also investigated using a hemacytometer. Respective MIC and MFC values of citronellol varied from 256 to 512 µg/mL, and from 256 to 2048 µg/mL. The MIC and MFC of geraniol varied similarly to citronellol. Conidia germination, mycelial dry weight, and conidiogenesis of Cladosporium spp. were reduced by the test-drugs at 1/2MIC, MIC and 2xMIC (p<0.05). These measurable cell events are essential for fungal infection and development infoods. The action of citronellol and geraniol against Cladosporium spp. suggest that the drugs may serveas effective agents for controlling fungal contamination and growth in foods.


Cladosporium spp. é um grupo de fungos dematiáceos relevantes para os alimentos, que podem ser dispersos pelo ambiente e causar deterioração e intoxicação alimentar. Considerando a importância da contaminação fúngica, os produtos naturais usados para controlar seu crescimentosão importantes. Neste contexto, o objetivo deste estudo foi avaliar os efeitos inibitórios de dois monoterpenoides, geraniol e citronelol, contra cepas de Cladosporium carrioni, C. cladosporioides eC. oxysporum. A Concentração Inibitória Mínima (CIM) e Concentração Fungicida Mínima (CFM) das drogas foram determinadas por microdiluição. Os efeitos das drogas-teste sobre a massa micelialseca, a germinação de conídios e a conidiogênese de Cladosporium spp. também foram investigados utilizando um hemocitômetro. Os valores de CIM e CFM do citronelol variaram de 256 a 512 μg/mLe de 256 a 2048 μg/mL, respectivamente. CIM e CFM de geraniol variaram de forma semelhante. A germinação de conídios, massa micelial seca e conidiogênese de Cladosporium spp. foram inibidaspelas drogas-teste 1/2CIM, CIM e 2xCIM (p<0,05). Esses eventos celulares são essenciais para a infecção e desenvolvimento fúngico em alimentos. A ação de citronelol e geraniol contra Cladosporium spp. sugere que podem servir como agentes eficazes para controlar a contaminação fúngica e o seucrescimento em alimentos.


Subject(s)
Humans , Biological Products , Cladosporium , Environmental Pollution , Food Supply , Monoterpenes , Mycotoxicosis
20.
Rev. Inst. Adolfo Lutz ; 762017. graf, tab
Article in English | LILACS, VETINDEX | ID: biblio-1489557

ABSTRACT

Cladosporium spp. is a group of dematiaceous food-relevant fungi which are well dispersed in the environment causing food spoilage and poisoning. Considering the importance of fungal contamination, natural drugs to control their growth have become important. Thus, the aim of this study was to evaluate the inhibitory effects of two monoterpenoids, (geraniol and citronellol), against strains of Cladosporium carrioni, C. cladosporioides,and C. oxysporum. Methods: The Minimum Inhibitory Concentration (MIC) and Minimum Fungicide Concentration (MFC) of the drugs were determined by microdilution. The effects of test drugs on mycelial dry weight, conidia germination, and conidiogenesis of Cladosporium spp. were also investigated using a hemacytometer. Respective MIC and MFC values of citronellol varied from 256 to 512 μg/mL, and from 256 to 2048 μg/mL. The MIC and MFC of geraniol varied similarly to citronellol. Conidia germination, mycelial dry weight, and conidiogenesis of Cladosporium spp. were reduced by the test-drugs at 1/2MIC, MIC and 2xMIC (p<0.05). These measurable cell events are essential for fungal infection and development in foods. The action of citronellol and geraniol against Cladosporium spp. suggest that the drugs may serve as effective agents for controlling fungal contamination and growth in foods.


Cladosporium spp. é um grupo de fungos dematiáceos relevantes para os alimentos, que podem ser dispersos pelo ambiente e causar deterioração e intoxicação alimentar. Considerando a importância da contaminação fúngica, os produtos naturais usados para controlar seu crescimento são importantes. neste contexto, o objetivo deste estudo foi avaliar os efeitos inibitórios de dois monoterpenoides, geraniol e citronelol, contra cepas de Cladosporium carrioni, C. cladosporioides e C. oxysporum. A Concentração Inibitória Mínima (CIM) e Concentração Fungicida Mínima (CFM) das drogas foram determinadas por microdiluição. os efeitos das drogas-teste sobre a massa micelial seca, a germinação de conídios e a conidiogênese de Cladosporium spp. também foram investigados utilizando um hemocitômetro. os valores de CIM e CFM do citronelol variaram de 256 a 512 μg/mL e de 256 a 2048 μg/mL, respectivamente. CIM e CFM de geraniol variaram de forma semelhante. A germinação de conídios, massa micelial seca e conidiogênese de Cladosporium spp. foram inibidas pelas drogas-teste 1/2CIM, CIM e 2xCIM (p<0,05). Esses eventos celulares são essenciais para a infecção e desenvolvimento fúngico em alimentos. A ação de citronelol e geraniol contra Cladosporium spp. sugere que podem servir como agentes eficazes para controlar a contaminação fúngica e seu crescimento em alimentos.


Subject(s)
Antifungal Agents/analysis , Cladosporium , Monoterpenes/therapeutic use , Food Safety , Biological Products/therapeutic use
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