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1.
Chem Biodivers ; : e202401604, 2024 Aug 15.
Article in English | MEDLINE | ID: mdl-39145539

ABSTRACT

This study aims to investigate the essential oil from leaves of E. pohliana (EOEP) in regard to its chemical composition, antimicrobial and drug-enhancing activity, as well as the reduction of fungal virulence capacity. Chemical characterization using GC-MS showed as major components the sesquiterpenes δ-cadinene, Epi-α-Muurolol, and bicyclogermacrene. The results of antibacterial tests indicated that Staphylococcus aureus was more sensitive to EOEP, that also enhanced the efficacy of gentamicin, erythromycin, and norfloxacin. EOEP exhibited antifungal properties against Candida albicans, in addition to potentiating the effectiveness of fluconazole against Candida tropicalis. It showed anti-virulence effects in all fungal strains. These findings underscore Eugenia pohliana as a potential candidate for the prospection of novel therapeutic agents to treat infectious diseases caused by resistant microbes.

2.
Arch Microbiol ; 206(9): 368, 2024 Aug 06.
Article in English | MEDLINE | ID: mdl-39107625

ABSTRACT

This study investigated crotamine (CTA), a peptide derived from the venom of the South American rattlesnake Crotalus durissus terrificus, known for its exceptional cell penetration potential. The objective was to explore the antibacterial and antifungal activity of CTA, its ability to inhibit efflux pumps and evaluate the effectiveness of its pharmacological combination with antibiotics and antifungals. In microbiological assays, CTA in combination with antibiotics was tested against strains of S. aureus and the inhibition of NorA, Tet(K) and MepA efflux pumps was also evaluated. CTA alone did not present clinically relevant direct antibacterial action, presenting MIC > 209.7 µM against strains S. aureus 1199B, IS-58, K2068. The standard efflux pump inhibitor CCCP showed significant effects in all negative relationships to assay reproducibility. Against the S. aureus 1199B strain, CTA (20.5 µM) associated with norfloxacin diluted 10 × (320.67 µM) showed a potentiating effect, in relation to the control. Against the S. aureus IS-58 strain, the CTA associated with tetracycline did not show a significant combinatorial effect, either with 2304 or 230.4 µM tetracycline. CTA at a concentration of 2.05 µM associated with ciprofloxacin at a concentration of 309.4 µM showed a significant potentiating effect. In association with EtBr, CTA at concentrations of 2.05 and 20.5 µM potentiated the effect in all strains tested, reducing the prevention of NorA, Tet(K) and MepA efflux pumps. In the C. albicans strain, a potentiating effect of fluconazole (334.3 µM) was observed when combined with CTA (2.05 µM). Against the C. tropicalis strain, a significant effect was also observed in the association of fluconazole 334.3 µM, where CTA 2.05 µM considerably reduced fungal growth and decreased the potentiation of fluconazole. Against the C. krusei strain, no significant potentiating effect of fluconazole was obtained by CTA. Our results indicate that CTA in pharmacological combination potentiates the effects of antibiotics and antifungal. This represents a new and promising antimicrobial strategy for treating a wide variety of infections.


Subject(s)
Anti-Bacterial Agents , Antifungal Agents , Crotalid Venoms , Crotalus , Microbial Sensitivity Tests , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Anti-Bacterial Agents/pharmacology , Crotalid Venoms/pharmacology , Animals , Staphylococcus aureus/drug effects , Drug Synergism , Candida albicans/drug effects , Venomous Snakes
3.
Fundam Clin Pharmacol ; : e13007, 2024 May 13.
Article in English | MEDLINE | ID: mdl-38738393

ABSTRACT

Candida spp. is an opportunistic pathogen capable of causing superficial to invasive infections. Morphological transition is one of the main virulence factors of this genus and, therefore, is an important variable to be considered in pharmacological interventions. Riparins I, II, III, and IV are alkamide-type alkaloids extracted from the unripe fruit of Aniba riparia, whose remarkable pharmacological properties were previously demonstrated. This work aimed to evaluate in silico and in vitro the inhibitory effects of Riparins on the morphological transition of Candida albicans, Candida tropicalis, and Candida krusei. Molecular docking was applied to analyze the inhibitory effects of riparins against proteins such as N-acetylglucosamine, CYP-51, and protein kinase A (PKA) using the Ramachandran plot. The ligands were prepared by MarvinSketch and Spartan software version 14.0, and MolDock Score and Rerank Score were used to analyze the affinity of the compounds. In vitro analyses were performed by culturing the strains in humid chambers in the presence of riparins or fluconazole (FCZ). The morphology was observed through optical microscopy, and the size of the hyphae was determined using the ToupView software. In silico analysis demonstrated that all riparins are likely to interact with the molecular targets: GlcNAc (>50%), PKA (>60%), and CYP-51 (>70%). Accordingly, in vitro analysis showed that these compounds significantly inhibited the morphological transition of all Candida strains. In conclusion, this study demonstrated that riparins inhibit Candida morphological transition and, therefore, can be used to overcome the pathogenicity of this genus.

4.
Chem Biodivers ; 21(7): e202400444, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38670923

ABSTRACT

Fungal infections are a public health problem that mainly affects immunosuppressed people, Candida spp. have been responsible for most sources of contamination and invasive fungal infections described around the world. The need arises to find new therapeutic approaches to combat growing infections. Plants and natural products have been considered a valuable source for discovering new molecules with active ingredients. Diosgenin is a sapogenin found in the families of Leguminosae and Dioscoreaceae, it is obtained mainly from the dioscin saponin through the hydrolysis method, it is a phytochemical that has been highlighted in the treatment of various diseases, as well as in combating microbial resistance. The present study aimed to evaluate the susceptibility of fungal strains to diosgenin, as well as verify the association with the reference drug and evaluate the inhibition of the virulence factor through morphological changes in the yeast state to the filamentous form of hyphae and pseudohyphae in strains of Candida albicans, Candida tropicalis and Candida krusei using the broth microdilution method and microculture technique. Antifungal assays revealed that diosgenin was not able to inhibit the growth of the tested strains. However, it was able to inhibit the fungal dimorphism of the strains evaluated, however further studies are recommended to verify its effectiveness against other virulence factors.


Subject(s)
Antifungal Agents , Candida , Diosgenin , Microbial Sensitivity Tests , Diosgenin/pharmacology , Diosgenin/chemistry , Diosgenin/analogs & derivatives , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Candida/drug effects , Virulence/drug effects , Candida albicans/drug effects , Candida albicans/pathogenicity
5.
Acta Trop ; 253: 107168, 2024 May.
Article in English | MEDLINE | ID: mdl-38432404

ABSTRACT

The present article aims to evaluate the antifungal and antivirulence effect of the phytoconstituent Limonene against Candida spp. Antifungal assays were performed, where the concentration capable of inhibiting 50 % of fungal growth, the growth inhibition curve, the minimum fungicidal concentration, the evaluation of the modifying effect with fluconazole, the inhibitory effect of the substances on the morphological transition of Candida spp. and the statistical analysis of the results were determined. With this study, it was seen that limonene demonstrated growth inhibition for the strains tested and when associated the natural compound with Fluconazole, there was potentiation of the effect of the drug, since the inhibition of growth by the combination occurred at lower concentrations against all strains tested, when compared to the drug alone, which inhibited growth at the highest concentration. In the test to determine the Minimum Fungicidal Concentration of the products tested alone and in combination, it was found that in the case of Candida strains, growth inhibition by limonene occurred at a concentration of 1024 µg/mL. For Fluconazole, growth impairment ranged from > 1024 µg/mL to 256 µg/mL for the strains. And when combined, limonene potentiated the action of FCZ, making fungal colonization unfeasible at concentrations below 1024 µg/mL. Regarding the morphological transition from yeast to hyphae, limonene was used at concentrations of 1024 µg/mL and 512 µg/mL, and it was found that, for CA and CK, the filaments were reduced in number and size at the highest concentration and against CT, the morphological transition from yeast to hyphae/pseudohyphae was totally inhibited, and if compared to the growth control, limonene was able to reduce fungal growth at concentrations greater than 512 µg/mL. This compound has antimicrobial activity described, due to its ability to interfere in the gene expression of the fungus, the limited therapeutic options and the recent emergence of multidrug-resistant Candida species represent a significant challenge for human medicine and highlight the need for new therapeutic approaches, and in this study a great potential of limonene was revealed in relation to the perspective of increasing the efficiency of commercial drug. This work can bring an important contribution to the scientific database, while emphasizing that in-depth studies and tests on the subject, in order to better investigate its effectiveness and mechanisms by which they exert their effects, are still necessary.


Subject(s)
Antifungal Agents , Candida , Humans , Antifungal Agents/pharmacology , Fluconazole/pharmacology , Limonene/pharmacology , Saccharomyces cerevisiae , Virulence , Fungi , Microbial Sensitivity Tests
6.
Chem Biodivers ; 21(3): e202301960, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38196022

ABSTRACT

The fixed oil from the inner mesocarp of Caryocar coriaceum Wittm. is used in the Chapada do Araripe region of Brazil for the treatment of genitourinary candidiasis. This study aimed to evaluate the chemical composition, antifungal activity, reduction of fungal virulence, and the preliminary toxicity of the fixed oil from the inner mesocarp of C. coriaceum tested against three Candida yeasts. The oil was characterized by gas chromatography (GC-MS and GC-FID). Antifungal activity was assessed using the serial microdilution method. Additionally, the potential of the oil as an enhancer of fluconazole action was tested at sub-inhibitory concentrations (MIC/8). The mechanism of action of C. coriaceum fixed oil was determined by evaluating the inhibition of morphological transition in Candida spp. The chemical composition of the fixed oil of C. coriaceum comprised both unsaturated and saturated fatty acids. Oleic (61 %) and palmitic (33 %) acids were the major constituents. Regarding its anti-Candida activity, the oil inhibited the growth of C. albicans (IC50 : 371 µg/mL) and C. tropicalis (IC50 : 830 µg/mL). Furthermore, the oil reversed the antifungal resistance of C. albicans and C. tropicalis, restoring the susceptibility to fluconazole and reducing their IC50 from 12.33 µg/mL and 362 µg/mL to 0.22 µg/mL and 13.93 µg/mL, respectively. The fixed oil of C. coriaceum completely inhibited the morphological transition of C. albicans and C. tropicalis at a concentration of 512 µg/mL, but exhibited limited low antifungal potential against C. krusei. The observed antifungal activity may be attributed to the overproduction of reactive oxygen species. Additionally, the oil showed no toxic effect on the Drosophila melanogaster in vivo model. The fixed oil from the inner mesocarp of C. coriaceum emerge as a strong candidate for the development of new pharmaceutical formulations to treat infections caused by Candida spp.


Subject(s)
Fluconazole , Malpighiales , Animals , Fluconazole/pharmacology , Candida , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Drosophila melanogaster , Plant Oils/pharmacology , Plant Oils/chemistry , Candida albicans , Microbial Sensitivity Tests
7.
Antibiotics (Basel) ; 12(11)2023 Oct 26.
Article in English | MEDLINE | ID: mdl-37998767

ABSTRACT

The increasing antifungal resistance rates against conventional drugs reveal the urgent need to search for new therapeutic alternatives. In this context, natural bioactive compounds have a critical role in antifungal drug development. Since evidence demonstrates that abietic acid, a diterpene found in Pinus species, has significant antimicrobial properties, this study aimed to evaluate the antifungal activity of abietic acid against Candida spp and its ability to potentiate the activity of fluconazole. Abietic acid was tested both individually and in combination with fluconazole against Candida albicans (CA INCQS 40006), Candida krusei (CK INCQS 40095), and Candida tropicalis (CT INCQS 40042). The microdilution method was used to determine the IC50 and the cell viability curve. Minimum Fungicidal Concentration (MFC) was determined by subculture in a solid medium. The plasma membrane permeability was measured using a fluorescent SYTOX Green probe. While the IC50 of the drugs alone ranged between 1065 and 3255 µg/mL, the IC50 resulting from the combination of abietic acid and fluconazole ranged between 7563 and 160.1 µg/mL. Whether used in combination with fluconazole or isolated, abietic acid exhibited Minimum Fungicidal Concentration (MFC) values exceeding 1024 µg/mL against Candida albicans, Candida krusei and Candida tropicalis. However, it was observed that the antifungal effect of fluconazole was enhanced when used in combination with abietic acid against Candida albicans and Candida tropicalis. These findings suggest that while abietic acid alone has limited inherent antifungal activity, it can enhance the effectiveness of fluconazole, thereby reducing antifungal resistance.

8.
Microb Pathog ; 181: 106203, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37330178

ABSTRACT

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.


Subject(s)
Bacterial Infections , Plant Extracts , Plant Extracts/chemistry , Fruit/chemistry , Methanol , Anti-Bacterial Agents/pharmacology , Candida , Microbial Sensitivity Tests
9.
Microb Pathog ; 180: 106129, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37119940

ABSTRACT

The increased resistance of microorganisms to antimicrobial drugs makes it necessary to search for new active compounds, such as chalcones. Their simple chemical structure makes them molecules easy to synthesize. Therefore, the aim of this study was to evaluate the antimicrobial and potentiating activity of antibiotics and antifungals by synthetic chalcones against strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans and Candida tropicalis. The synthesis of chalcones was carried out by Claisen-Schimidt aldol condensation. Nuclear Magnetic Resonance (NMR) and Gas Chromatography Coupled to Mass Spectrometry (GC/MS) were also performed. Microbiological tests were performed by the broth microdilution method, using gentamicin, norfloxacin and penicillin as standard drugs for the antibacterial assay, and fluconazole for the antifungal assay. Three chalcones were obtained (1E,4E)-1,5-diphenylpenta-1,4-dien-3-one (DB-Acetone), (1E,3E,6E,8E)-1,9-diphenylnone-1,3,6,8-tetraen-5-one (DB-CNM), (1E,4E)-1,5-bis (4-methoxyphenyl) penta-1,4-dien-3-one (DB-Anisal). The compound DB-Acetone was able to inhibit P. aeruginosa ATCC 9027 at a concentration of 1.4 × 102 µM (32 µg/mL), while DB-CNM and DB-Anisal inhibited the growth of S. aureus ATCC 25923 at 17.88 × 102 µM and 2.71 × 101 µM (512 µg/mL and 8 µg/mL) respectively. In the combined activity, DB-Anisal was able to potentiate the effect of the three antibacterial drugs tested against E. coli 06, norfloxacin (128 for 4 µg/mL ±1) against P. aeruginosa 24 and penicillin (1,024 for 16 µg/mL ±1) against S. aureus 10. In antifungal assays, chalcones were not able to inhibit the growth of fungal strains tested. However, both showed potentiating activity with fluconazole, ranging from 8.17 x 10-1 µM (0.4909 µg/mL) to 2.35 µM (13.96 µg/mL). It is concluded that synthetic chalcones have antimicrobial potential, demonstrating good intrinsic activity against fungi and bacteria, in addition to potentiating the antibiotics and antifungal tested. Further studies are needed addressing the mechanisms of action responsible for the results found in this work.


Subject(s)
Anti-Infective Agents , Chalcones , Antifungal Agents/chemistry , Fluconazole/pharmacology , Chalcones/pharmacology , Chalcones/chemistry , Staphylococcus aureus , Norfloxacin/pharmacology , Escherichia coli , Acetone/pharmacology , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Anti-Bacterial Agents/chemistry , Candida albicans , Penicillins/pharmacology , Microbial Sensitivity Tests
10.
Chem Biol Interact ; 373: 110377, 2023 Mar 01.
Article in English | MEDLINE | ID: mdl-36754224

ABSTRACT

Trans-Caryophyllene (TC), a sesquiterpene, with proven biological activities, which in this work was tested alone, encapsulated in liposomes and associated with Fluconazole in vitro in an attempt to enhance the effect of the drug. Liposomes were characterized from vesicle size, polydispersity index, and Zeta potential, and imaging by scanning electron microscopy. Antifungal assays were performed against Candida albicans, Candida tropicalis and Candida krusei by microdilution to determine the IC50 values and the viability curve. The Minimum Fungicidal Concentration (MFC) was performed by subcultivation in solid medium and the inhibitory effect of the association of TC and Fluconazole and tests to verify morphological changes was performed in micro-cultivation chambers based on concentrations on microdilution plates. The corresponding IC50 data of the substances ranged from 34.4 to 65249 µg/mL, considerably high values compared to the control (Fluconazole). The MFC of all compounds showing fungistatic effect. The performance of the compounds on the cell viability curve was similar in all tested strains, as they showed no antifungal potential when compared to the control (FCZ), when associated with FCZ they showed no significant antifungal activity. The free and liposomal TC also managed to restrict 100% of the fungal dimorphism, in both concentrations, against C. albicans, and against C. tropicalis the isolated TC did not show a significant inhibitory effect; however, against the C. krusei strain inhibited 100% in filamentous growth in both concentrations, which is statistically relevant. The liposomes were homogeneous, with vesicles with diameters of 185.46 nm for the control and 143.8 nm for the liposomal TC, and a surface charge potential of - 42.6 mV. By scanning microscopy, the spherical shapes of the vesicles were verified.


Subject(s)
Fluconazole , Liposomes , Fluconazole/pharmacology , Candida , Antifungal Agents/pharmacology , Candida albicans , Microbial Sensitivity Tests
11.
Plants (Basel) ; 12(2)2023 Jan 16.
Article in English | MEDLINE | ID: mdl-36679128

ABSTRACT

Fungi of the Candida genus are responsible for invasive candidiasis, which affects people all over the world and has high mortality rates. This is due to their virulence factors, which give them great resistance and pathogenicity. In addition, the emergence of multidrug-resistant strains makes it difficult to treat these infections. In this way, natural products have emerged as an alternative to standard drugs, where plants known for their medicinal properties such as Turnera subulata become attractive to research. The present work aimed to analyze the ethanol extract of Turnera subulata leaves against standard strains of Candida albicans, Candida krusei and Candida tropicalis using broth microdilution techniques. The identification of the compounds in T. subulata leaves by LC-MS revealed the presence of a wide variety of substances such as carboxylic acids and terpenes, with flavonoids and fatty acids being more evident. The antifungal assays showed that the extract was not able to inhibit the growth of the tested strains at concentrations with a clinical relevance. However, at higher concentrations, it was able to inhibit the fungal dimorphism of C. albicans and C. tropicalis. It is possible that the T. subulata extract has potential as an inhibitor of fungal virulence factors without affecting the cell viability. Further research should be carried out in order to assess its inhibitory potential for other fungal virulence factors.

12.
Pharmaceuticals (Basel) ; 15(10)2022 Oct 17.
Article in English | MEDLINE | ID: mdl-36297389

ABSTRACT

Microbial resistance has become a worrying problem in recent decades after the abusive use of antibiotics causing the selection of resistant microorganisms. In order to circumvent such resistance, researchers have invested efforts in the search for promising natural substances, such as essential oils. Thus, the objective of this work was to determine the chemical composition of the essential oil of Acritopappus confertus leaves, to evaluate its intrinsic effect and its effects in combination with drugs against pathogenic fungi and bacteria, in addition to verifying the inhibition of virulence in Candida strains. To this end, the oil was verified by gas chromatography coupled with mass spectrometry (GC/MS). Candida strains were used for antifungal assays by means of the serial microdilution technique, in order to determine the average inhibitory concentration (IC50), and for the modification assays, sub-inhibitory concentrations (MIC/8) were used. Finally, the natural product's ability to inhibit the formation of filamentous structures was evaluated. In antibacterial tests, the MIC of the oil against strains of Staphylococcus aureus and Escherichia coli and its modifying effects in association with gentamicin, erythromycin, and norfloxacin were determined. The major constituent of the essential oil was the monoterpene myrcene (54.71%). The results show that the essential oil has an antifungal effect, with C. albicans strains being the most susceptible. Furthermore, the oil can potentiate the effect of fluconazole against strains of C. tropicalis and C. albicans. Regarding its effect on micromorphology, the oil was also able to inhibit the filaments in all strains. In combination with antibiotics, the oil potentiated the drug's action by reducing the MIC against E. coli and S. aureus. It can be concluded that the essential oil of A. confertus has potential against pathogenic fungi and bacteria, making it a target for the development of an antimicrobial drug.

13.
Molecules ; 27(13)2022 Jun 27.
Article in English | MEDLINE | ID: mdl-35807377

ABSTRACT

Species of the genus Miconia are used in traditional medicine for the treatment of diseases, such as pain, throat infections, fever, and cold, and they used as depuratives, diuretics, and sedatives. This work reviewed studies carried out with Miconia species, highlighting its ethnomedicinal uses and pharmacological and phytochemical potential. This information was collected in the main platforms of scientific research (PubMed, Scopus, and Web of Science). Our findings show that some of the traditional uses of Miconia are corroborated by biological and/or pharmacological assays, which demonstrated, among other properties, anti-inflammatory, analgesic, antimutagenic, antiparasitic, antioxidant, cytotoxic, and antimicrobial activities. A total of 148 chemical compounds were identified in Miconia species, with phenolic compounds being the main constituents found in the species of this genus. Such phytochemical investigations have demonstrated the potential of species belonging to this genus as a source of bioactive substances, thus reinforcing their medicinal and pharmacological importance.


Subject(s)
Melastomataceae , Ethnopharmacology , Medicine, Traditional , Phytochemicals/chemistry , Phytochemicals/pharmacology , Phytochemicals/therapeutic use , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/pharmacology
14.
Plants (Basel) ; 11(13)2022 Jun 25.
Article in English | MEDLINE | ID: mdl-35807637

ABSTRACT

Caryocar coriaceum is an endemic tree of Brazil, occurring mainly in the northeast region in the Cerrado environment. The species, popularly known as "pequi", produces fruits that are used in the manufacture of oil for food and medicinal purposes. This work reviewed studies conducted with the species, highlighting its ethnomedicinal use, its pharmacological potential, including its chemical constituents, and its cultural and socioeconomic importance. Information was obtained through the main scientific research platforms. The keyword "Caryocar coriaceum" was used as the main index for searching the following platforms: PubMed®, PubMed Central®, SciElo, Scopus® and Web of ScienceTM. The compiled papers demonstrate that C. coriaceum has great medicinal, economic and cultural importance for northeastern Brazil. Popularly, the fruits of C. coriaceum are used to treat broncho-pulmonary diseases (bronchitis, colds and flu). The fixed oil is widely used to relieve pain from various causes in the treatment of inflammation, flu, eczema, burns, fever, rickets, indigestion, heart murmurs, fatigue and erectile dysfunction. Some of these uses are corroborated by pharmacological trials, which have demonstrated the antioxidant, healing, anti-inflammatory, gastroprotective, antinociceptive and antimicrobial properties of the species. Chemically, fatty acids and phenolic compounds are the main constituents recorded for the species. Due to its medicinal properties, the fruits and oil of C. coriaceum have a high commercial demand and are one of the main forms of subsistence activities for local populations. On the other hand, the extractive practice of the fruits, associated with anthropic factors and its physiological nature, makes the species threatened with extinction. Thus, public management policies are highly necessary in order to avoid its extinction.

15.
Molecules ; 27(10)2022 May 20.
Article in English | MEDLINE | ID: mdl-35630757

ABSTRACT

One of the main global problems that affect human health is the development of bacterial resistance to different drugs. As a result, the growing number of multidrug-resistant pathogens has contributed to an increase in resistant infections and represents a public health problem. The present work seeks to investigate the chemical composition and antibacterial activity of the essential oil of Syzygium cumini leaves. To identify its chemical composition, gas chromatography coupled to mass spectrometry was used. The antibacterial activity test was performed with the standard strains Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 25853 and Staphylococcus aureus ATCC 25923 and multidrug-resistant clinical isolates E. coli 06, P. aeruginosa 24 and S. aureus 10. The minimum inhibitory concentration (MIC) was determined by serial microdilution as well as the verification of the modulating effect of the antibiotic effect. In this test, the oil was used in a subinhibitory concentration. The test reading was performed after 24 h of incubation at 37 °C. The results show that the major chemical constituent is α-pinene (53.21%). The oil showed moderate activity against E. coli ATCC 25922, with the MIC of 512 µg/mL; there was no activity against the other strains. The oil potentiated the effect of antibiotics demonstrating possible synergism when associated with gentamicin, erythromycin and norfloxacin against E. coli 06 and S. aureus 10.


Subject(s)
Oils, Volatile , Syzygium , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Escherichia coli , Gas Chromatography-Mass Spectrometry , Humans , Oils, Volatile/chemistry , Oils, Volatile/pharmacology , Phytochemicals/pharmacology , Pseudomonas aeruginosa , Staphylococcus aureus
16.
Arch Microbiol ; 204(6): 346, 2022 May 24.
Article in English | MEDLINE | ID: mdl-35608680

ABSTRACT

Lectins participate in the defense against microorganisms and in signaling the damage caused by pathogens to the cell surface and/or intracellular in plants. This study aims to analyze the antifungal potential of lectins extracted from seeds of Canavalia ensiformis (L.) DC and Canavalia rosea (Sw.) DC, against Candida albicans and Candida tropicalis. The antimicrobial tests were performed by microdilution against Candida spp. The test to verify the combined lectin/fluconazole effect was performed using subinhibitory concentrations of lectins and with antifungal ranging from 0.5 to 512 µg/mL. The ability to inhibit the morphological transition of Candida spp. was evaluated by microcultivation in a moist chamber. The results of the minimum inhibitory concentration revealed no antifungal activity against the tested strains. However, lectins modified the action of fluconazole, reducing the IC50 of the drug against C. albicans. Lectins were also able to discretely modulate the morphological transition of the tested strains.


Subject(s)
Candida albicans , Candida tropicalis , Antifungal Agents/pharmacology , Canavalia/metabolism , Candida/metabolism , Concanavalin A , Fluconazole/pharmacology , Lectins/pharmacology , Microbial Sensitivity Tests , Plankton
17.
Pharmaceutics ; 14(4)2022 Mar 24.
Article in English | MEDLINE | ID: mdl-35456532

ABSTRACT

(1) Background: Candida is a genus of yeasts with notable pathogenicity and significant ability to develop antimicrobial resistance. Gossypium hirsutum 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-Candida 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-Candida 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 IC50 values against Candida albicans INCQS 40006, Candida tropicalis INCQS 40042, and C. tropicalis URM 4262 strains, indicating enhanced antifungal activity. About biofilm production, significant inhibition was observed only for the AELG-treated C. tropicalis 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 C. albicans (4) Conclusions: Gossypium hirsutum L. presents promising antifungal effects, that may be potentially linked to the combined activity of chemical constituents identified in its extracts.

18.
Molecules ; 27(7)2022 Mar 27.
Article in English | MEDLINE | ID: mdl-35408565

ABSTRACT

Weeds are an important source of natural products; with promising biological activity. This study investigated the anti-kinetoplastida potential (in vitro) to evaluate the cytotoxicity (in vitro) and antioxidant capacity of the essential oil of Rhaphiodon echinus (EORe), which is an infesting plant species. The essential oil was analyzed by GC/MS. The antioxidant capacity was evaluated by reduction of the DPPH radical and Fe3+ ion. The clone Trypanosoma cruzi CL-B5 was used to search for anti-epimastigote activity. Antileishmanial activity was determined using promastigotes of Leishmania braziliensis (MHOM/CW/88/UA301). NCTC 929 fibroblasts were used for the cytotoxicity test. The results showed that the main constituent of the essential oil was γ-elemene. No relevant effect was observed concerning the ability to reduce the DPPH radical; only at the concentration of 480 µg/mL did the essential oil demonstrate a high reduction of Fe3+ power. The oil was active against L. brasiliensis promastigotes; but not against the epimastigote form of T. cruzi. Cytotoxicity for mammalian cells was low at the active concentration capable of killing more than 70% of promastigote forms. The results revealed that the essential oil of R. echinus showed activity against L. brasiliensis; positioning itself as a promising agent for antileishmanial therapies.


Subject(s)
Antiprotozoal Agents , Chagas Disease , Lamiaceae , Leishmaniasis, Mucocutaneous , Oils, Volatile , Trypanosoma cruzi , Animals , Antioxidants/pharmacology , Antiprotozoal Agents/pharmacology , Chagas Disease/drug therapy , Mammals , Oils, Volatile/pharmacology
19.
Article in English | MEDLINE | ID: mdl-35310039

ABSTRACT

Mesosphaerum suaveolens (L.) Kuntze is a species widely used traditionally in the treatment of ailments, such as stomach pain, hemorrhoids, cough, verminosis, ulcer, liver disease, fever, influenza, nasal congestion, and inflammation. This review aims to provide a survey of available information on seven international electronic databases (Google Scholar, Medline, ResearchGate, Web of Science, Scopus, Science Direct, and PubMed) about botanical aspects, traditional uses, phytochemistry, and biological activities of M. suaveolens. Mesosphaerum suaveolens is a tropical America native species, but it can be found in several parts of the world as a ruderal plant. The species is the most studied species of the genus Lamiaceae due its phytochemical aspect, especially regarding the chemical composition of its essential oil. Besides the essential oils, M. suaveolens is a source of numerous secondary compounds such as triterpenes, diterpenes, and phenolic compounds, which are related to its biological activities, such as allelopathic, antibacterial, antifungal, insecticidal, and larvicidal activities as described in the literature.

20.
Folia Microbiol (Praha) ; 67(3): 447-457, 2022 Jun.
Article in English | MEDLINE | ID: mdl-35112321

ABSTRACT

Due to the increase in fungal resistance to existing drugs, a need exists to search for new antifungals. This study aimed to evaluate the antifungal activity of α, ß, and δ-damascone and inclusion complexes with ß-cyclodextrin against different Candida spp. The inclusion complex of ß-damascone was prepared by the co-evaporation method using three molar proportions (1:1; 2:1; 3:1 (ßDA-ßCD)) and analyzed using Fourier transform infrared spectroscopy (FTIR). Standard Candida albicans (CA INCQS 40,006), Candida krusei (CK INCQS 40,095), and Candida tropicalis (CT INCQS 40,042) strains were used to evaluate antifungal activity. The substances were tested individually or in association with fluconazole (FCZ). The IC50 and cell viability curve constructions were performed using the microdilution method. The minimum fungicidal concentration (MFC) was determined by the subculture method in a solid medium. The α, ß, and δ-DA isolated or in combination with fluconazole (FCZ) showed significant antifungal activity. ß-damascone showed effective complexation in the three molar proportions assayed; however, none of the inclusion complexes was demonstrated clinically significant effects against the fungal tested. Then, all compounds have shown promising antifungal activities; however, in vivo assays are necessary to have therapeutical application in the future.


Subject(s)
Antifungal Agents , beta-Cyclodextrins , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Candida , Fluconazole/pharmacology , Microbial Sensitivity Tests , Norisoprenoids/pharmacology , beta-Cyclodextrins/pharmacology
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