Croton heliotropiifolius Kunth (Euphorbiaceae), whose occurrence has already been registered in the most varied Brazilian biomes, is commonly found in the Chapada do Araripe, Ceará. The species is ...traditionally used to treat fungal, parasitic, and degenerative diseases. This study investigated the chemical composition and pharmacological potential (antioxidant, antifungal, antiparasitic, and cytotoxic) of an aqueous extract obtained from the roots of C. heliotropiifolius. Following a qualitative phytochemical screening, the chemical constituents were identified by ultra-efficiency liquid chromatography coupled witha quadrupole/time-of-flight system (UPLC-QTOF). The antioxidant potential was verified by thin-layer chromatography (TLC). The direct and combined antifungal activity of the extract against opportunistic Candida strains was investigated using the microdilution method. The minimal fungicidal concentration (MFC) was determined by subculture, while the modulation of the morphological transition (fungal virulence) was evaluated by light microscopy. The in vitro antiparasitic activity was analyzed using epimastigotes of Trypanosoma cruzi and promastigotes of Leishmania braziliensis and Leishmania infantum, while cytotoxicity was determined in cultures of mouse fibroblasts. The phytochemical analysis identified the presence of acids, terpenes, flavonoids, lignans, and alkaloids. Among these constituents, the presence of polar and non-polar phenolic compounds with known antioxidant action was highlighted. While the extract showed clinically ineffective antifungal effects, it could enhance the effectiveness of fluconazole, in addition to inhibiting the morphological transition associated with increased virulence in Candida strains. Although the extract showed low cytotoxicity against fibroblasts, it also had weak antiparasitic effects. In conclusion, Croton heliotropiifolius is a source of natural products with antifungal and antioxidant potential.
Spondias mombin
is used in the folk medicine for the treatment of diarrhea and dysentery, indicating that extracts obtained from this species may present pharmacological activities against pathogenic ...microorganisms. The purpose of this work was to investigate the chemical composition and evaluate the antimicrobial activity of extracts obtained from the leaves (aqueous) and bark (hydroethanolic) of
S. mombin
both as single treatments and in combination with conventional drugs. Following a qualitative chemical prospection, the extracts were analyzed by HPLC–DAD. The antimicrobial activities were evaluated by microdilution. The combined activity of drugs and extracts was verified by adding a subinhibitory concentration of the extract in the presence of variable drug concentrations. The Minimum Fungicidal Concentration (MFC) was determined by a subculture of the microdilution test, while the effect of the in vitro treatments on morphological transition was analyzed by subculture in moist chambers. While the qualitative analysis detected the presence of phenols and flavonoids, the HPLC analysis identified quercetin, caffeic acid, and catechin as major components in the leaf extract, whereas kaempferol and quercetin were found as major compounds in the bark extract. The extracts showed effective antibacterial activities only against the Gram-negative strains. With regard to the combined activity, the leaf extract potentiated the action of gentamicin and imipenem (against
Staphylococcus aureus
), while the bark extract potentiated the effect of norfloxacin (against
S. aureus
), imipenem (against
Escherichia coli
), and norfloxacin (against
Pseudomonas aeruginosa
). A more significant antifungal (fungistatic) effect was achieved with the bark extract (even though at high concentrations), which further enhanced the activity of fluconazole. The extracts also inhibited the emission of filaments by
Candida albicans
and
Candida tropicalis
. Together, these findings suggest that that the extract constituents may act by favoring the permeability of microbial cells to conventional drugs, as well as by affecting virulence mechanisms in
Candida strains
.
A review on the antimicrobial properties of lectins Fonseca, Victor Juno Alencar; Braga, Ana Lays; Filho, Jaime Ribeiro ...
International journal of biological macromolecules,
01/2022, Letnik:
195
Journal Article
Recenzirano
Lectins are biologically versatile biomolecules with remarkable antimicrobial effects, notably against bacteria, fungi and protozoa, in addition to modulating host immunity. For this, the lectins ...bind to carbohydrates on the surface of the pathogen, which can cause damage to the cell wall and prevent the attachment of microorganisms to host cells. Thus, this study intends to review the biological activities of lectins, with an emphasis on antimicrobial activity. Lectins of plant stood out for its antimicrobial effects, demonstrating that they act against a variety of strains, where in vitro were able to inhibit their development and affect their morphology. In vivo, they modulated host immunity, signaling and activating defense cells. Some of these lectins were capable to modulate the action of antibiotics, indicating their potential to minimize the antibiotic resistance. The results suggest that lectins have antimicrobial activity with potential to be used in drug development.
sp. treatment has become a challenge due to the formation of biofilms which favor resistance to conventional antifungals, making the search for new compounds necessary. The objective of this study ...was to identify the composition of the
Benth. leaf ethanolic extract and to verify its antifungal activity against
sp. and its biofilms. The composition identification was performed using the ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS) technique. The antifungal activity of extract and fluconazole against planktonic cells and biofilms was verified through the minimum inhibitory concentration (MIC) following biofilm induction and quantification in acrylic resin discs by reducing tetrazolic salt, with all isolates forming biofilms within 48 h. Six constituents were identified in the extract, and the compounds identified are derivatives from phenolic compounds such as flavonoids (epi) gallocatechin Dimer, epigallocatechin and gallocatechin, Myricetin-O-hexoside, Myricitrin, and Quercetin-O-rhamnoside. The extract reduced biofilm formation in some of the strains analyzed, namely
URM5732,
INCQS40042, and
URM6352. This reduction was also observed in the treatment with fluconazole with some of the analyzed strains. The extract showed significant antifungal and anti-biofilm activities with some of the strains tested.
•The essential oil of Eugenia uniflora presented two components with proven antifungal activity: selina-1,3,7 (11)-trien-8-one and selina-1,3,7 (11)-trien-8-one.•Essential oil of Eugenia uniflora ...presented an antagonistic effect in association with Fluconazol.•The performance of E. uniflora essential oil was considered as a fungistatic agent.•The natural product inhibited one of the virulence mechanisms of Candida spp. which is the proliferation of filamentous structures.
The development of fungal resistance to antifungal drugs has been worsening over the years and as a result research on new antifungal agents derived from plants has intensified. Eugenia uniflora L. (pitanga) has been studied for its various biological actions. In this study the chemical composition and antifungal effects of the E. uniflora essential oil (EULEO) were investigated against Candida albicans (CA), Candida krusei (CK) and Candida tropicalis (CT) standard strains. The essential oil obtained through hydro-distillation was analyzed by gas chromatography coupled to mass spectrometry (GC-MS). To determine the IC50 of the oil, the cellular viability curve and the inhibitory effects were measured by means of the oil’s association with Fluconazole in a broth microdilution assay with spectrophotometric readings. The Minimum Fungicidal Concentration (MFC) was determined by solid medium subculture with the aid of a guide plate while the assays used to verify morphological changes emerging from the action of the fractions were performed in microculture chambers at concentrations based on the microdilution. Two major oil constituents stand out from the chemical analysis: selina-1,3,7(11)-trien-8-one (36.37%) and selina-1,3,7(11)-trien-8-one epoxide (27.32%). The concentration that reduced microorganismal growth was ≥8,192 μg/mL while the IC50 varied, this being between 1892.47 and 12491.80 μg/mL (oil), 10.07 – 80.78 μg/mL (fluconazole) and 18.53 – 295.60 μg/mL (fluconazole + oil). The combined activity (fluconazole + oil) resulted in indifference and antagonism. A MFC of the oil in association with fluconazole was recorded at the concentration of 8,192 μg/mL against CA and CK. The oil caused the inhibition of CA and CT morphological transition. In view of the results obtained, additional research is needed to elucidate the activity of the E. uniflora oil over genetic and biochemical processes regarding its effect on Candida spp. virulence.
Caryocar coriaceum, commonly known as ‘pequi’, is a medicinal species used traditionally for the herbal treatment of infectious and parasitic diseases in the Brazilian Northeast region. In this ...study, we investigated whether the fruits of C. coriaceum have bioactive chemical constituents against etiological agents of infectious diseases. The methanolic extract of the internal mesocarp of the fruits of C. coriaceum (MECC) was chemically analyzed and evaluated for its antimicrobial and drug-enhancing activity against multidrug-resistant pathogenic bacteria (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus), and Candida spp. strains. The extract had flavones, flavonols, xanthones, catechins, and flavanones as major classes. A total of 11.26 mg GAE/g of phenolics, and 5.98 mg QE/g of flavonoids were found. No intrinsic antibacterial activity was observed; however, the extract was able to intensify the action of gentamicin and erythromycin against multi-resistant strains. The anti-Candida effect observed in this study was mainly due to the formation of reactive oxygen species. The extract was capable of causing damage to the plasmatic membrane of Candida tropicalis through pores formation. Our findings partially support the ethnopharmacological uses of the fruit pulp of C. coriaceum against infectious and parasitic diseases.
•The traditional use of C. coriaceum against infectious diseases was partially supported by our findings.•The CC extract did not show a direct effect against pathogenic bacteria.•The CC intensified the action of antibiotics against MDR microorganisms.•The CC reduced the growth of Candida spp., acting through the formation of ROS.•The CC it was able to inhibit the morphological transition of the yeasts.
(1) Background:
is a genus of yeasts with notable pathogenicity and significant ability to develop antimicrobial resistance.
L., a medicinal plant that is traditionally used due to its antimicrobial ...properties, has demonstrated significant antifungal activity. Therefore, this study investigated the chemical composition and anti-
effects of aqueous (AELG) and hydroethanolic (HELG) extracts obtained from the leaves of this plant. (2) Methods: The extracts were chemically characterized by UPLC-QTOF-MS/MS, and their anti-
activities were investigated by analyzing cell viability, biofilm production, morphological transition, and enhancement of antifungal resistance. (3) Results: The UPLC-QTOF-MS/MS analysis revealed the presence of twenty-one compounds in both AELG and HELG, highlighting the predominance of flavonoids. The combination of the extracts with fluconazole significantly reduced its IC
values against
INCQS 40006,
INCQS 40042, and
URM 4262 strains, indicating enhanced antifungal activity. About biofilm production, significant inhibition was observed only for the AELG-treated
URM 4262 strain in comparison with the untreated control. Accordingly, this extract showed more significant inhibitory effects on the morphological transition of the INCQS 40006 and URM 4387 strains of
(4) Conclusions:
L. presents promising antifungal effects, that may be potentially linked to the combined activity of chemical constituents identified in its extracts.
The Malvaceae family, an important group of plants that have the Gossypium (cotton) genus has been used in folk medicine to treat microbial diseases and symptoms.
This article aims to understand its ...ethnobotany expression in communities and scientific elucidation of antimicrobial activities of this genus through literature review.
The bibliographic survey was carried out from 1999 to 2019 with keywords combinations such as "Gossypium + ethnobotanical", " Gossypium + medicinal ", "Gossypium + the biological activity" in scientific databases as Pubmed, Scopus, Web of Science, DOAJ, Scielo, Bireme.
After data analysis, we found that the Gossypium genus, specifically Gossypium hirsutum, G. barbadense, G. herbaceum, G. arboreum are the species most cited in the treatment of microbial diseases and symptoms in communities all over the world. In light of scientific elucidation of biological activities, the Gossypium genus has been used to treat protozoal, bacterial, fungal, and viral diseases.
The review demonstrated that the Gossypium genus is a promising source of biological activities against microbial diseases, especially in the treatment of protozoal diseases like malaria.
Display omitted
This study aimed to evaluate the antibiotic effects of the fixed oils of Acrocomia aculeata (FOAA) and Syagrus cearenses (FOSC) against the bacterial strains and the fungi strains of the genus ...Candida spp. The method of serial microdilution using different concentrations was used for measuring the individual biological activity of the fixed oils. The fixed oil of A. aculeata showed the presence of oleic acid (24.36%), while the oil of S. cearensis displayed the content of myristic acid (18.29%), compounds detected in high concentration. The combination FOAA + Norfloxacin, and FOSC + Norfloxacin showed antibacterial activity against E. coli and S. aureus strains, demonstrating possible synergism and potentiation of the antibiotic action against multidrug-resistant strains. The combination FOAA + Fluconazole displayed a significant effect against Candida albicans (IC50 = 15.54), C. krusei (IC50 = 78.58), and C. tropicalis (IC50 = 1588 μg/mL). Regarding FOSC + Fluconazole, it was also observed their combined effect against the strains of C. albicans (IC50 = 3385 μg/mL), C. krusei (IC50 = 26.67 μg/mL), and C. tropicalis (IC50 = 1164 μg/mL). The findings of this study showed a significant synergism for both fixed oils tested when combined with the antibiotic.
•– Were identifed the presence of eight fatty acids in the FOAA and FOSC.•– Were observed high percentages of oleic acid in FOAA and myristic acid in FOSC.•- Significant synergism was observed when the fixed oils were associated with Norfloxacin.•- Significant synergism was observed when the fixed oils were associated with Fluconazole.
•BISHDZHI, an isoniazid derivative was synthetized.•Structural, spectroscopic, and pharmacokinetic analysis was carried.•BISHDZHI presents maximum absorption at the wavelength of 346 nm.•BISHDZHI + ...Fluconazole possesses antifungal action against Candida tropicalis.•BISHDZHI has excellent oral bioavailability and metabolic stability.
In this work, the isoniazid derivative N',N'''-((1E,1′E)-1,4-phenylenebis(methaneylylidene))di(isonicotinohydrazide) (BISHDZHI) was synthesized and characterized by Nuclear Magnetic Resonance (NMR), Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR), Fourier Transform Raman (FT-Raman), and Ultraviolet-Visible (UV–Vis) spectroscopy, and its potential against fungal strains of Candida ssp. was evaluated by in vitro assays. The NMR spectrum confirmed the molecular structure of BISHDZHI. Quantum chemistry computational calculations allowed to obtain the potential energy surface, optimized molecular structure, and to identify all the bands of the Raman, infrared and UV spectra. The data calculated for isoniazid derivative BISHDZHI using the Functional Density Theory (DFT) are in accordance with the experimental values. Our in vitro studies showed that the BISHDZHI compound in association with Fluconazole possesses antifungal action against Candida tropicalis strain, with a reduction of the IC50 24 times to the host. In silico study of ADMET suggested that BISHDZHI has excellent oral bioavailability and metabolic stability, which allows therapeutic action without severe risk to the host. In addition, the molecular docking showed a high interaction potential between the Candida Albicans target. While the molecular dynamics simulations suggested that the BISHDZHI ligand occasioned a minor change in the structure target, indicating more excellent stability than the drug fluconazole.
Display omitted
PDF
