ABSTRACT
Objective:To prepare water-soluble graphene-based itraconazole antifungal eye drops and evaluate its antifungal activity against Fusarium solani. Methods:By oxidative modification of graphene and modification of polymer materials, water-soluble graphene oxide-modified polyethylene glycol (GO-PEG) composites were prepared.The composites were characterized by scanning electron microscopy, zeta potential, and Raman spectroscopy.The antifungal drug itraconazole was loaded onto the GO-PEG vector by solvent evaporation method, and itraconazole eye drops were obtained.The drug loading of itraconazole eye drops was measured using a UV and visible spectrophotometer.The antifungal effect in vitro was assessed by the microdilution method and light microscopy. Results:Scanning electron microscopy showed that GO-PEG had a two-dimensional nanosheet structure and many wrinkles.The zeta potential of GO-PEG was -42.40 mV.Raman spectroscopy showed that the ID/ IG of GO-PEG was 1.003.Using the water-soluble GO-PEG vector, a maximum itraconazole concentration of 10 mg/ml was achieved with a 10 000-fold increase in apparent solubility (10 mg/ml vs 0.001 mg/ml). The antifungal results showed that the minimum inhibitory concentration of itraconazole eye drops against Fusarium solani was approximately 1.88 μg/ml, but the GO-PEG vector has no significant antifungal activity against Fusarium solani. Conclusions:GO-PEG achieves effective loading and solubilization of itraconazole, demonstrating an in vitro inhibitory effect on Fusarium solani.
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Objective: To evaluate the anti Candida activity of Hyptis martiusii decoction and its major compound, caffeic acid alone or in the presence of fluconazole, as well as their cytotoxic effect. Methods: The decoction was characterized using high performance liquid chromatography coupled with diode array detector. For the antifungal activity, the minimum inhibitory concentration (MIC) and the potential effect of the decoction with the fluconazole were evaluated by microdilution method using 96-well microtiter trays. The osmotic fragility test was performed using erythrocytes under saline stress. All tests were performed in triplicate. Results: The chemical characterization of the decoction was performed by high performance liquid chromatography and revealed the presence of seven compounds, including caffeic acid as major constituent. The antifungal tests demonstrated that both decoction (DHm) and caffeic acid obtained from Hyptis martiusii presented MIC and MFC ≥ 4096 μg/mL against Candida albicans and Candida tropicalis strains. However, in the presence of fluconazole, DHm and caffeic acid presented IC
ABSTRACT
Objective: To evaluate the anti Candida activity of Hyptis martiusii decoction and its major compound, caffeic acid alone or in the presence of fluconazole, as well as their cytotoxic effect. Methods: The decoction was characterized using high performance liquid chromatography coupled with diode array detector. For the antifungal activity, the minimum inhibitory concentration (MIC) and the potential effect of the decoction with the fluconazole were evaluated by microdilution method using 96-well microtiter trays. The osmotic fragility test was performed using erythrocytes under saline stress. All tests were performed in triplicate. Results: The chemical characterization of the decoction was performed by high performance liquid chromatography and revealed the presence of seven compounds, including caffeic acid as major constituent. The antifungal tests demonstrated that both decoction (DHm) and caffeic acid obtained from Hyptis martiusii presented MIC and MFC ≥ 4096 μg/mL against Candidaalbicans and Candida tropicalis strains. However, in the presence of fluconazole, DHm and caffeic acid presented IC50 of 2.60 and 2.53 μg/mL respectively, demonstrating significant synergistic effects against Candida strains. The modulator activity of DHm might be due to the presence of caffeic acid. Moreover, DHm and caffeic acid did not cause significant hemolytic effects, indicating that they present low cytotoxicity. Conclusions: These data indicate that DHm potentiates the activity of the fluconazole, without enhancement of the toxicity, encouraging further toxicological, pharmacological and phytochemical studies to provide consistent evidence of the potential of this plant to be used in drug development.
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Objective: To evaluate antimicrobial and antioxidant properties of saline extract from Tithonia diversifolia leaves by phytochemical bioprospecting, and investigate its safety against animal cells. Methods: The saline extract was prepared, with NaCl (0.15 M), by constant stirring of the dried and pulverized leaves, followed by volume reduction by lyophilization. The extract was phytochemical characterized using ultra-performance liquid chromatography, and total phenol and flavonoid analysis also was performed.The antioxidant capacity was determined through DPPH? radical, the antimicrobial property was evaluated against standard bacteria and fungi, and the viability assays were performed against mice splenocytes. Results: Fifteen compoundswereidentifiedbelongingtotwomainclassesterpenoidsandphenolics.Theextract showed 22.185 mg GAE/g of total phenolic compounds and 3.220 mg QE/g of flavonoid. Moreover, extract showed higher antioxidant ability similar to butylated hydroxytoluene a standard molecule [(3.042±0.019) mg AAE/g and (4.12±0.10) mg AAE/g to saline extract and butylated hydroxytoluene, respectively].The antimicrobial assays demonstrated that the extract had a significant antifungal potential against Candida species and could be used with safety against mice splenocytes, in concentrations lower than 50 μg/mL, promoting higher proliferation in these cells. Conclusions: Saline extract from Tithonia diversifolia leaves presents potential antioxidant, antifungal properties and induces immunostimulation in mice splenocytes.
ABSTRACT
Objective: To evaluate antimicrobial and antioxidant properties of saline extract from Tithonia diversifolia leaves by phytochemical bioprospecting, and investigate its safety against animal cells. Methods: The saline extract was prepared, with NaCl (0.15 M), by constant stirring of the dried and pulverized leaves, followed by volume reduction by lyophilization. The extract was phytochemical characterized using ultra-performance liquid chromatography, and total phenol and flavonoid analysis also was performed. The antioxidant capacity was determined through DPPH· radical, the antimicrobial property was evaluated against standard bacteria and fungi, and the viability assays were performed against mice splenocytes. Results: Fifteen compounds were identified belonging to two main classes terpenoids and phenolics. The extract showed 22.185 mg GAE/g of total phenolic compounds and 3.220 mg QE/g of flavonoid. Moreover, extract showed higher antioxidant ability similar to butylated hydroxytoluene a standard molecule [(3.042±0.019) mg AAE/g and (4.12±0.10) mg AAE/g to saline extract and butylated hydroxytoluene, respectively]. The antimicrobial assays demonstrated that the extract had a significant antifungal potential against Candida species and could be used with safety against mice splenocytes, in concentrations lower than 50 μg/mL, promoting higher proliferation in these cells. Conclusions: Saline extract from Tithonia diversifolia leaves presents potential antioxidant, antifungal properties and induces immunostimulation in mice splenocytes.
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Antifungal properties of extracts from eight Brazilian plants traditionally used in popular Brazilian medicine were tested against five clinically relevant Candida species, Cryptococcus neoformans, and Sporothrix schenckii. Results demonstrate that almost all extracts exhibited antifungal activity, at least against one of the microorganisms tested. The ethanolic extract from the leaves of Schinus terebinthifolius exhibited potential antifungal activity against C. glabrata and S. schenckii. Preliminary phytochemical analysis of extract from S. terebinthifolius showed the presence of biologically active compounds, namely saponins, flavonoids, triterpenes, steroids and tannins.
A propriedade antifúngica de extratos de oito plantas utilizadas na medicina tradicional brasileira foi testada contra cinco espécies de Candida, com relevância clínica, Cryptococcus neoformans e Sporothrix schenckii. Os resultados mostraram que todos os extratos exibiram atividade antifúngica contra pelo menos um dos microrganismos testados. O extrato etanólico das folhas de Schinus terebinthifolius apresentou potencial atividade antifúngica contra C. glabrata e S. schenckii. Na análise fitoquímica preliminar dos extratos de S. terebinthifolius observou-se a presença de compostos biologicamente ativos como, flavonóides, triterpenos, esteróides e taninos.