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1.
Chem Biodivers ; : e202400748, 2024 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-39146471

RESUMO

Genipa americana L. (Rubiaceae), genip tree, has therapeutic and nutritional potential. This revision aimed to gather information on botanical characteristics, popular uses, phytochemical, and pharmacological aspects of the tree. The methodology adopted integrated literature published between 2000 and 2024, as well as consultations with the World International Intellectual Property Organization (WIPO); resulting in 39 articles and 11 patents to promote this research. The species, which is native and not endemic to Brazil, is most prevalent in the Amazon biome as it is suitable for reconstructing degraded areas, as well as having various traditional applications. Iridoids are the main secondary metabolites present in the species, especially ginipin, geniposide acid, and geniposide, which are the most prevalent in the fruit. The patents registered with the WIPO indicate its use as a colorant, insecticide, anti-inflammatory, and antioxidant potential, in evidence of its antimicrobial and antioxidant activities. Further studies are needed on the mechanisms of the chemical components' action and on ethnopharmacology.

2.
Plants (Basel) ; 12(12)2023 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-37376002

RESUMO

Antimicrobial resistance has become a growing public health concern in recent decades, demanding a search for new effective treatments. Therefore, this study aimed to elucidate the phytochemical composition and evaluate the antibacterial activity of the essential oil obtained from the fruits of Piper tuberculatum Jacq. (EOPT) against strains carrying different mechanisms of antibiotic resistance. Phytochemical analysis was performed using gas chromatography-mass spectrometry (GC/MS). The antibacterial activity of EOPT and its ability to inhibit antibiotic resistance was evaluated through the broth microdilution method. The GC-MS analysis identified 99.59% of the constituents, with ß-pinene (31.51%), α-pinene (28.38%), and ß-cis-ocimene (20.22%) being identified as major constituents. The minimum inhibitory concentration (MIC) of EOPT was determined to assess its antibacterial activity against multidrug-resistant strains of Staphylococcus aureus (IS-58, 1199B, K2068, and K4100). The compound showed a MIC of ≥ 1024 µg/mL, suggesting a lack of intrinsic antibacterial activity. However, when the EOPT was associated with antibiotics and EtBr, a significant decrease in antibiotic resistance was observed, indicating the modulation of efflux pump activity. This evidence was corroborated with the observation of increased fluorescent light emission by the bacterial strains, indicating the involvement of the NorA and MepA efflux pumps. Additionally, the significant potentiation of ampicillin activity against the S. aureus strain K4414 suggests the ß-lactamase inhibitory activity of EOPT. These results suggest that the essential oil from P. tuberculatum fruits has antibiotic-enhancing properties, with a mechanism involving the inhibition of efflux pumps and ß-lactamase in MDR S. aureus strains. These findings provide new perspectives on the potential use of EOPT against antibiotic resistance and highlight the importance of Piper species as sources of bioactive compounds with promising therapeutic activities against MDR bacteria. Nevertheless, further preclinical (in vivo) studies remain necessary to confirm these in vitro-observed results.

3.
Plants (Basel) ; 12(8)2023 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-37111898

RESUMO

Species belonging to the genus Lippia are used worldwide as foods, beverages, and seasonings. Studies have demonstrated that these species have antioxidant, sedative, analgesic, anti-inflammatory, and antipyretic activities. This work aimed to evaluate the antibacterial activity and anxiolytic effect by different pathways of essential oils and ethanolic extracts of three species of Lippia (Lippia alba, Lippia sidoides, and Lippia gracilis). The ethanolic extracts were characterized by HPLC-DAD-ESI-MSn and their phenolics were quantified. The antibacterial activity was evaluated by determining the minimal inhibitory concentration and modulation of antibiotic activity, and toxic and anxiolytic effects were evaluated in the zebrafish model. The extracts showed compositions with a low ratio and shared compounds. L. alba and L. gracilis showed higher amounts of phenols and flavonoids, respectively. All extracts and essential oils presented antibacterial activity, especially those obtained from L. sidoides. On the other hand, L. alba extract presented the most significant antibiotic-enhancing effect. The samples were not toxic after 96 h of exposure, but showed an anxiolytic effect through modulation of the GABAA receptor, while L. alba extract acted via modulation of the 5-HT receptor. This new pharmacological evidence opens horizons for therapeutic approaches targeting anxiolytic and antibacterial therapies and food conservation using these species and their constituents.

4.
Curr Res Toxicol ; 4: 100103, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36970244

RESUMO

Medicinal plants have been used for many years by communities to treat illnesses. The need for scientific proof of these vegetable's curative effects is as necessary as the proof of the inexistence of toxicity related to the use of extracts with therapeutic potential. Annona squamosa L. (Annonaceae), popularly known as "pinha", "ata" or "fruta do conde", has been used in traditional medicine for its analgesic and antitumor activities. The toxic effects attributed to this plant have also been explored as a pesticide and an insecticide. The aim of the present study was to investigate the toxicity of the methanolic extract of A. squamosa seeds and pulp against human erythrocytes. Blood samples were treated with methanolic extract at different concentrations, osmotic fragility was determined using saline tension assays and morphological analyzes were performed using optical microscopy. The extracts were analyzed using high performance liquid chromatography with diode array detection (HPLC-DAD) for phenolic quantification. The seed's methanolic extract showed toxicity above 50% from a concentration of 100 µg/mL, while also presenting echinocytes in the morphological analysis. The pulp's methanolic extract did not show toxicity to red blood cells or morphological changes at the concentrations tested. HPLC-DAD analysis revealed the presence of caffeic acid in the seed extract and gallic acid in the pulp extract. The seed's methanolic extract is toxic and the pulp's methanolic extract showed no toxicity against human erythrocytes.

5.
Alkaloids Chem Biol ; 89: 39-171, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36731967

RESUMO

This study involves aporphine alkaloids identified through 13C Nuclear Magnetic Resonance (NMR) spectroscopic data. For the present publication, articles were selected from several databases on aporphine alkaloids from 1994 to 2021. In this class, more than 700 compounds have been registered, with 221 were included in this section, among which 122 were characterized for the first time in the investigated period. The study also addresses their biosynthetic pathways, classifying substances according to their structural characteristics based on established literature. Furthermore, pharmacological activities related to the aporphine alkaloids highlighted in this section are also presented, giving an overview of the various applications of these compounds.


Assuntos
Alcaloides , Aporfinas , Alcaloides/farmacologia , Alcaloides/química , Aporfinas/farmacologia , Aporfinas/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular
6.
Plants (Basel) ; 12(2)2023 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-36679128

RESUMO

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.

7.
Int J Ophthalmol ; 15(12): 1903-1907, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36536965

RESUMO

AIM: To investigate the anti-inflammatory effects of the sesquiterpenes α-humulene and ß-caryophyllene on pterygium fibroblasts. METHODS: Primary cultures of pterygium fibroblasts were established. Third passage pterygium fibroblasts were exposed to α-humulene and ß-caryophyllene separately and together. The cell viability was assessed by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay at 12, 24, 48, and 72h after exposure. The levels of the inflammatory cytokines interleukin (IL)-1ß, IL-6, IL-8, tumor necrosis factor (TNF)-α and IL-10 in the conditioned culture medium were assessed by enzyme-linked immunosorbent assay (ELISA) at 12, 24 and 48h after exposure. Data were statistically analyzed using Friedman repeated measures analysis of variances on ranks. RESULTS: The 25 µmol/L ß-caryophyllene induced significant decrease in the IL-6 production by pterygium fibroblasts 48h after the exposure (P=0.041). The levels of IL-1ß, IL-8, IL-10, and TNF-α were very low and had no statistically significant variations after exposure to α-humulene, ß-caryophyllene, or both compounds together. CONCLUSION: The exposure to 25 µmol/L of ß-caryophyllene significantly reduce the production of IL-6 by pterygium fibroblasts after 48h. This sesquiterpene may be a potential alternative adjuvant agent for the treatment of pterygium.

8.
Sci Rep ; 12(1): 20626, 2022 11 30.
Artigo em Inglês | MEDLINE | ID: mdl-36450779

RESUMO

Lippia sidoides Cham. (Verbenaceae) is a species often mentioned in traditional medicine due to the medicinal properties attributed to its leaves, which include antibacterial, antifungal, acaricidal and antioxidant. Several of these actions have been scientifically proven, according to reports in the literature; however, little is known about toxicological aspects of this plant. This work included studies to determine the chemical composition and toxicity tests, using several methods aiming to evaluate the safety for use of the aqueous extract of L. sidoides leaves, in addition, the anxiolytic effect on adult zebrafish was investigated, thus contributing to the pharmacological knowledge and traditional medicine concerning the specie under study. The chemical profile was determined by liquid chromatography coupled to mass spectrometry-HPLC/MS with electrospray ionization. Toxicity was evaluated by zebrafish, Drosophila melanogaster, blood cells, and Artemia salina models. 12 compounds belonging to the flavonoid class were identified. In the toxicity assays, the observed results showed low toxicity of the aqueous extract in all tests performed. In the analysis with zebrafish, the highest doses of the extract were anxiolytic, neuromodulating the GABAa receptor. The obtained results support the safe use of the aqueous extract of L. sidoides leaves for the development of new drugs and for the use by populations in traditional medicine.


Assuntos
Ansiolíticos , Lippia , Animais , Ansiolíticos/toxicidade , Peixe-Zebra , Drosophila melanogaster , Folhas de Planta
9.
Pharmaceuticals (Basel) ; 15(10)2022 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-36297389

RESUMO

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.

10.
Foods ; 11(15)2022 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-35954004

RESUMO

This study investigated the flavonoid content, antioxidant activity, and toxicological properties of the acetone-water fraction of stem bark of Stryphnodendron rotundifolium Mart. (TFSR). The total flavonoid content and antioxidant activity were determined, as typified by DPPH● and ABTS●+ radical scavenging abilities, Fe3+ reducing antioxidant power (FRAP), relative antioxidant capacity (RAC), and the inhibition of thiobarbituric acid reactive species (TBARs) in Drosophila melanogaster tissue. Toxicity and locomotor functions were evaluated in adult D. melanogaster flies through aging and survival assays, startle-induced negative geotaxis, and centrophobic responses with video-assisted open field motion tracking. The flavonoid content of dry TFSR (DF) was 3.36 mg quercetin/g. Furthermore, the significant antioxidant activity of TFSR was revealed through scavenging 95.3% of the ABTS●+ radical and 82.4% of the DPPH● radical, as well reducing 74.7% of Fe3+ in the FRAP assay and 80% Mo6+ in the RAC assay. TFSR conferred 70.25% protection against lipid peroxidation in Drosophila tissue. Survival rates ranged from 84.65 to 103.98% in comparison to the non-supplemented control and no evident deterioration of locomotor functions and centrophobia responses was observed. These results revealed that TFSR has potent antioxidant activity and low toxicity in vivo, profiling TFSR as a promising natural product in the treatment/management of iron overload and associated conditions.

11.
Plants (Basel) ; 11(13)2022 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-35807637

RESUMO

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.

12.
Molecules ; 27(13)2022 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-35807377

RESUMO

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.


Assuntos
Melastomataceae , Etnofarmacologia , Medicina Tradicional , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
13.
Folia Microbiol (Praha) ; 67(1): 15-20, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34417720

RESUMO

Bacterial resistance is a natural process carried out by bacteria, which has been considered a public health problem in recent decades. This process can be triggered through the efflux mechanism, which has been extensively studied, mainly related to the use of natural products to inhibit this mechanism. To carry out the present study, the minimum inhibitory concentration (MIC) tests of the compound limonene were performed, through the microdilution methodology in sterile 96-well plates. Tests were also carried out with the association of the compound with ethidium bromide and ciprofloxacin, in addition to the ethidium bromide fluorimetry, and later the molecular docking. From the tests performed, it was possible to observe that the compound limonene presented significant results when associated with ethidium bromide and the antibiotic used. Through the fluorescence emission, it was observed that when associated with the compound limonene, a greater ethidium bromide fluorescence was emitted. Finally, when analyzing the in silico study, it demonstrated that limonene can efficiently fit into the MepA structure. In this way, it is possible to show that limonene can contribute to cases of bacterial resistance through an efflux pump, so that it is necessary to carry out more studies to prove its effects against bacteria carrying an efflux pump and assess the toxicity of the compound.


Assuntos
Proteínas Associadas à Resistência a Múltiplos Medicamentos , Staphylococcus aureus , Antibacterianos/farmacologia , Proteínas de Bactérias/metabolismo , Limoneno , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Staphylococcus aureus/metabolismo
14.
Foods ; 10(11)2021 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-34828960

RESUMO

Stryphnodendron rotundifolium Mart., popularly known as "barbatimão", is a plant species traditionally used by topical and oral routes for the treatment of infectious and inflammatory diseases. Considering the well-described antioxidant properties of this species, this study investigated the protective effects of its keto-aqueous extract using an in vitro model of iron overload. Phenolic compounds were quantified and identified by Ultra-Performance Liquid Chromatography coupled with quadrupole Time-Of-Flight Electrospray Ionization Mass Spectrometry (UPLC-ESI-qTOF-MS/MS) in positive and negative ions mode analysis. Antioxidant activity was analyzed following the iron-chelating-reducing capacity and deoxyribose degradation (2-DR) protection methods. The analysis identified condensed tannins (54.8 mg catechin/g dry fraction (DF), polyphenols (25 mg gallic acid/g DF), and hydrolyzable tannins (28.8 mg tannic acid/g DF). Among the constituents, prodelphinidin, procyanidin, and prorobinetinidine were isolated and identified. The extract significantly protected 2-DR degradation induced by Fe2+ (72% protection) or •OH (43% protection). The ortho-phenanthroline test revealed Fe2+-chelating and Fe3+-reducing activities of 93% and 84%, respectively. A preliminary toxicological analysis using Artemia salina revealed mortality below 10%, at a concentration of 0.25 mg/mL, indicating low toxicity under the present experimental conditions. In conclusion, the findings of the present study indicate that Stryphnodendron rotundifolium is a source of antioxidant compounds with the potential to be used in drug development in the context of iron overload disorders, which remains to be further investigated in vivo.

15.
Foods ; 10(10)2021 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-34681391

RESUMO

This study presents the chemical profile of extracts from the pulp and seed of Annona squamosa L., as well as the evaluation of their antioxidant and acetylcholinesterase inhibition activities. In the chemical prospection, qualitative assays were performed, and the contents of total phenols, flavonoids, vitamin C, and carotenoids were quantified. For the compounds identification, analyses of the extracts were performed by liquid chromatography coupled to mass spectrometry. Antioxidant evaluation was performed using the DPPH, ABTS, Fe3+ reduction, 2-DR protection, and ß-carotene protection methods. The assay for inhibition of acetylcholinesterase activity was determined using the method described by Ellman. The secondary metabolites identified were anthocyanidins, flavones, flavonols, and alkaloids. Phenol analysis showed a higher quantitative value of total phenols and flavonoids for the seed extract, and the vitamin C content was higher in the pulp extract. There was no significant difference in relation to the carotenoids quantification. The best results obtained for antioxidant activity, for both seed and pulp extracts, were with the ABTS method with IC50 of 0.14 ± 0.02 and 0.38 ± 0.02 mg/mL, respectively. Compared to A. squamosa seed extract, the pulp extract demonstrates higher AChE inhibitory activity with IC50 of 18.82 ± 0.17 µg/mL. A. squamosa is a nutritious food source. The continuity of the studies is fundamental to relate the consumption of this food and its effects on neurodegenerative diseases.

16.
Molecules ; 26(7)2021 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-33918492

RESUMO

PURPOSE: Alternative methods for the use of animals in research have gained increasing importance, due to assessments evaluating the real need for their use and the development of legislation that regulates the subject. The principle of the 3R's (replacement, reduction and refinement) has been an important reference, such that in vitro, ex vivo and cord replacement methods have achieved a prominent place in research. METHODS: Therefore, due to successful results from studies developed with these methods, the present study aimed to evaluate the myorelaxant effect of the Dysphania ambrosioides essential oil (EODa) using a Sus scrofa domesticus coronary artery model, and the toxicity of both the Dysphania ambrosioides essential oil and its major constituent, α-terpinene, against Drosophila melanogaster in toxicity and negative geotaxis assays. RESULTS: The EODa relaxed the smooth muscle of swine coronary arteries precontracted with K+ and 5-HT in assays using Sus scrofa domesticus coronary arteries. The toxicity results presented LC50 values of 1.546 mg/mL and 2.282 mg/mL for the EODa and α-terpinene, respectively, thus showing the EODa and α-terpinene presented toxicity to these dipterans, with the EODa being more toxic. CONCLUSIONS: Moreover, the results reveal the possibility of using the EODa in vascular disease studies since it promoted the relaxation of the Sus scrofa domesticus coronary smooth muscle.


Assuntos
Chenopodiaceae/química , Vasos Coronários/fisiologia , Drosophila melanogaster/fisiologia , Relaxamento Muscular/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/toxicidade , Testes de Toxicidade , Animais , Vasos Coronários/efeitos dos fármacos , Monoterpenos Cicloexânicos/farmacologia , Modelos Animais de Doenças , Drosophila melanogaster/efeitos dos fármacos , Atividade Motora/efeitos dos fármacos , Contração Muscular/efeitos dos fármacos , Compostos Fitoquímicos/análise , Serotonina/farmacologia , Suínos
17.
Arch Microbiol ; 203(6): 3077-3087, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-33787988

RESUMO

This study aimed to investigate the chemical composition and antifungal potential of the essential oil of Baccharis trimera (Less.) DC. against Candida strains. The half maximal inhibitory concentration (IC50) was assessed by the microdilution method using the essential oil at a concentration range of 8192 to 8 µg/mL. The minimum fungicide concentration (MFC) was determined by subculture in solid medium. The ability of the essential oil to modulate the activity of antifungals was determined in wells treated simultaneously with the oil at a subinhibitory concentration (MFC/16) and fluconazole (FCZ). The fungal morphology was analyzed by microscopy. Gas chromatography coupled with mass spectrometry (GC/MS) was used to identify the chemical composition. The essential oil presented an CI50 of 11.24 and 1.45 µg/mL, which was found to potentiate the effect of FCZ against Candida albicans. On the other hand, this combined treatment resulted in antagonism against Candida tropicalis and no evident modulation against Candida krusei was observed. The essential oil significantly inhibited hyphae growth. However, with a MFC ≥ 16,384 µg/mL, it is assumed that it has a fungistatic action. The antifungal properties demonstrated in this study might be related to the presence of sesquiterpenes and monoterpenes, and the interaction between them. In conclusion, Baccharis trimera showed promising anti-Candida effects, in addition to potentiating the activity of FCZ against Candida albicans, affecting its morphological transition. Therefore, this species constitutes a source of chemical compounds with the potential to be used in the combat of fungal infections.


Assuntos
Baccharis , Candida , Óleos Voláteis , Antifúngicos/farmacologia , Baccharis/química , Candida/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/farmacologia , Pichia/efeitos dos fármacos
18.
Eur J Pharm Sci ; 160: 105753, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33581258

RESUMO

This study aimed to evaluate the antibacterial activity and to verify, in silico and in vitro, the inhibition of efflux mechanisms using a series of synthesized 1,8-naphthyridines sulfonamides against Staphylococcus aureus strains carrying MepA efflux pumps. The chemical synthesis occurred through the thermolysis of the Meldrum's acid adduct. The sulfonamide derivatives were obtained by the sulfonylation of 2-amino-5­chloro-1,8-naphthyridine with commercial benzenesulfonyl chloride. Antibacterial activity was assessed by the broth microdilution test. Efflux pump inhibitory capacity was evaluated in silico by molecular docking and in vitro by analyzing synergistic effects on ciprofloxacin and ethidium bromide (EtBr) and by EtBr fluorescence emission assays. The following 1,8-naphthyridines were synthesized: 4-methyl-N-(5­chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide (Compound 10a); 2,5-dichloro-N-(5­chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide (Compound 10b); 4-fluoro-N-(5­chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide (Compound 10c); 2,3,4-trifluoro-N-(5­chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide (Compound 10d); 3-trifluoromethyl-N-(5­chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide (Compound 10e); 4­bromo-2,5-difluoro-N-(5­chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide (Compound 10f). The 1,8-naphthyridines derivatives associated with sulfonamides did not show antibacterial activity. However, they showed a favorable pharmacokinetic profile with possible MepA efflux pump inhibitory action, demonstrated in molecular docking. In addition to the promising results in reducing the concentration of intracellular EtBr. 1,8-naphthyridines act as putative agents in the inhibitory action of the MepA efflux pump.


Assuntos
Proteínas Associadas à Resistência a Múltiplos Medicamentos , Naftiridinas , Antibacterianos/farmacologia , Proteínas de Bactérias/metabolismo , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Naftiridinas/farmacologia , Sulfonamidas/farmacologia
19.
Molecules ; 25(17)2020 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-32842529

RESUMO

Caesalpinia ferrea C. Mart., popularly known as "Jucá" or "Pau-ferro", belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of C. ferrea. The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from C. ferrea are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of C. ferrea most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of C. ferrea.


Assuntos
Anti-Infecciosos , Anti-Inflamatórios , Antioxidantes , Caesalpinia/química , Compostos Fitoquímicos , Extratos Vegetais , Animais , Anti-Infecciosos/química , Anti-Infecciosos/uso terapêutico , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Antioxidantes/química , Antioxidantes/uso terapêutico , Etnobotânica , Etnofarmacologia , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico
20.
Food Chem ; 315: 126277, 2020 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-32004983

RESUMO

This study reports the effects of seasonal variation on the total polyphenol and flavonoid content and the in vitro antioxidant activity of Secondatia floribunda A. DC. The extracts were prepared from the inner bark and heartwood of samples harvested in the 2015 to 2016. The total phenolic and flavonoid content was determined by specific qualitative tests. The in vitro antioxidant capacity was analyzed using the following tests: 1-1-diphenyl-2-picrylhydrazyl radical (DPPH), 2,2'-azinobis-3-ethylbenzenothiazoline-6-sulfonic acid (ABTS+), ferric reducing antioxidant power (FRAP) and iron (Fe2+) chelating activity. The total polyphenol and total flavonoid content varied over the harvest period. The DPPH and ABTS tests revealed that in the dry season had the most potent in vitro antioxidant activity, although the extracts obtained during the rainy season presented the higher Fe2+ chelating and Ferric reducing activities. In conclusion, the phenolic content and in vitro antioxidant activity are correlated, and both are influenced by seasonality.


Assuntos
Antioxidantes/análise , Apocynaceae/química , Polifenóis/análise , Flavonoides/química , Extratos Vegetais/química , Estações do Ano
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