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1.
Saudi Dent J ; 36(1): 180-186, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38375400

RESUMEN

Objectives: This study aimed to analyze the knowledge of dental surgeons concerning the pharmacological effects of bisphosphonates (BP) and their impact on the health of patients undergoing oral surgery treatment. Materials and methods: A quantitative study was conducted with professionals in the Cariri region of Ceará, Brazil. The data were collected using a semi-structured questionnaire to interview the dental surgeons who met the inclusion criteria. The data were analyzed by Chi-square and Fischer's Exact tests using the SPSS program version 22.0. Results: The results indicated that most interviewed subjects have no experience with the dental treatment of individuals under treatment with bisphosphonates. When a sample of the medication was presented, a significant number of the participants (65.3%) did not recognize the drug. Among those who recognized it, 66.5% did not know how to treat bisphosphonate-using patients in the clinical routine. However, 95.1% of the professionals who recognized the need to discontinue these drugs admitted contacting the prescriber to establish the best dental conduct. Our results also showed that recently graduated professionals better understood the need to stop BP use before invasive treatment, although they did not know the protocol. Conclusion: In conclusion, a better knowledge of the pharmacological effects of BP is crucial for conducting adequate anamnesis, requesting additional tests, and performing medical monitoring, which has a significant impact on the clinical practice of dental surgeons.

2.
Chem Biodivers ; 21(4): e202301962, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38415915

RESUMEN

Stingless bees belong to the Meliponini tribe and are widely distributed in the tropics and subtropics, where they perform important ecological services. Among the best distributed groups of stingless bees is the genus Scaptotrigona, which includes 22 species distributed throughout the neotropical region, including the area from Mexico to Argentina. Bees of this genus are responsible for the production of products such as honey, propolis, geopropolis and fermented pollen ("saburá"). This review aimed to provide an overview of the chemical composition and biological activities associated with derived products from stingless bees of the genus Scaptotrigona. The bibliographic review was carried out through searches in the Scopus, Web of Science, ScienceDirect and PubMed databases, including publications from 2003 to January 2023. The study of the chemodiversity of products derived from Scaptotrigona demonstrated the mainly presence of flavonoids, phenolic acids, terpenoids and alkaloids. It was also demonstrated that products derived from bees of the genus Scaptotrigona exhibit a wide range of biological effects, such as antibacterial, antioxidant, anti-inflammatory and antifungal activities, among other bioactivities. This review provides an overview of phytochemical and pharmacological investigations of the genus Scaptotrigona. However, it is essential to clarify the toxicity and food safety of these products.


Asunto(s)
Miel , Himenópteros , Própolis , Animales , Antibacterianos/farmacología , Abejas , México , Própolis/farmacología , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Hidroxibenzoatos/química , Hidroxibenzoatos/aislamiento & purificación , Hidroxibenzoatos/farmacología , Terpenos/química , Terpenos/aislamiento & purificación , Terpenos/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología
3.
Chem Biodivers ; 21(3): e202301960, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38196022

RESUMEN

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.


Asunto(s)
Fluconazol , Malpighiales , Animales , Fluconazol/farmacología , Candida , Antifúngicos/farmacología , Antifúngicos/química , Drosophila melanogaster , Aceites de Plantas/farmacología , Aceites de Plantas/química , Candida albicans , Pruebas de Sensibilidad Microbiana
4.
Chem Biodivers ; 21(2): e202301407, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38116922

RESUMEN

Melipona subnitida (Ducke, 1911), a species of stingless bee, popularly known as Jandaíra, has a wide distribution in the Brazilian Northeast region, being an important pollinator of the Caatinga biome. This bee produces products such as honey, geopropolis, pollen (saburá) and wax that are traditionally used for therapeutic purposes and some studies report the biological properties, as well as its chemical composition. This review aimed to select, analyze and gather data published in the literature focusing on the chemical profile and bioactivities described for M. subnitida products. Data collection was carried out through the Capes Journal Portal platform, using the following databases: Web of Science, Scopus, and PubMed. Original articles published in English and Portuguese were included, with no time limitation. The chemical composition of M. subnitida products has been investigated through chromatographic analysis, demonstrating the presence of a variety of phenolic compounds, such as flavonoids and phenylpropanoids, among other classes of secondary metabolites. These products also have several biological activities, including antioxidant, healing, antinociceptive, anti-inflammatory, antidepressant, antidyslipidemic, antiobesity, antifungal, antibacterial and prebiotic. Among the biological activities reported, the antioxidant activity was the most investigated. These data show that products derived from the stingless bee M. subnitida have promising bioactive compounds. This review provides useful information about the bioactivities and chemical profile of Melipona subnitida bee products, and a direction for future research, which should focus on understanding the mechanisms of action associated with the already elucidated pharmacological activities, as well as the bioactive properties of the main isolate's constituents identified in the chemical composition of these products.


Asunto(s)
Miel , Abejas , Animales , Miel/análisis , Antibacterianos/farmacología , Antioxidantes/farmacología , Fenoles/análisis , Antifúngicos
5.
Curr Res Toxicol ; 5: 100120, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37744206

RESUMEN

Phytanic acid (PA: 3,7,11,15-tetramethylhexadecanoic acid) is an important biometabolite of the chlorophyll-derived diterpenoid phytol. Its biological sources (occurrence) and ADME (absorption, distribution, metabolism, and elimination) profile are well-discussed in the literature. Cumulative literature suggests that PA has beneficial as well as harmful biological roles in humans and other animals. This study aimed to sketch a brief summary of PA's beneficial and harmful pharmacological effects in test systems on the basis of existing literature reports. Literature findings propose that PA has anti-inflammatory and immunomodulatory, antidiabetic, anti-obesity, anticancer, and oocyte maturation effects. Although a high plasma PA-level mediated SLS remains controversial, it is evident to link it with Refsum's disease and other peroxisomal enzyme deficiency diseases in humans, including RCDP and LD; ZHDA and Alzheimer's disease; progressive ataxia and dysarthria; and an increased risk of some lymphomas such as LBL, FL, and NHL. PA exerts toxic effects on different kinds of cells, including neuronal, cardiac, and renal cells, through diverse pathways such as oxidative stress, mitochondrial disturbance, apoptosis, disruption of Na+/K+-ATPase activity, Ca2+ homeostasis, alteration of AChE and MAO activities, etc. PA is considered a cardiac biomarker in humans. In conclusion, PA may be one of the most important biometabolites in humans.

6.
Fundam Clin Pharmacol ; 37(4): 824-832, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36869661

RESUMEN

The rising of diseases caused by multidrug-resistant bacteria has encouraged researchers to explore more antimicrobial substances, as well as chemicals capable of potentiating the action of existing ones against multidrug-resistant bacteria. Anacardium occidentale produces a fruit known as cashew nut, filled with a dark, almost black, caustic, and flammable liquid called cashew nutshell liquid (CNSL). The goal of the study was to evaluate the intrinsic antimicrobial activity of the major compounds present in CNSL, called anacardic acids (AA), as well as their possible modulatory action as an adjuvant of Norfloxacin against a Staphylococcus aureus strain overproducing the NorA efflux pump (SA1199B). Microdilution assays were performed to determine the minimum inhibitory concentration (MIC) of AA against different microbial species. Norfloxacin and Ethidium Bromide (EtBr) resistance modulation assays were performed in the presence or absence of AA against SA1199-B. AA showed antimicrobial activity against Gram-positive bacterial strains tested but no activity against Gram-negative bacteria or yeast strains. At subinhibitory concentration, AA reduced the MIC values for Norfloxacin and EtBr against the SA1199-B strain. Furthermore, AA increased the intracellular accumulation of EtBr in this NorA overproducer strain, indicating that AA are NorA inhibitors. Docking analysis showed that AA probably modulates Norfloxacin efflux by spatial impediment at the same binding site of NorA.


Asunto(s)
Anacardium , Infecciones Estafilocócicas , Norfloxacino/farmacología , Antibacterianos/farmacología , Staphylococcus aureus , Anacardium/metabolismo , Ácidos Anacárdicos/farmacología , Ácidos Anacárdicos/metabolismo , Proteínas Asociadas a Resistencia a Múltiples Medicamentos , Infecciones Estafilocócicas/microbiología , Etidio/metabolismo , Etidio/farmacología , Pruebas de Sensibilidad Microbiana
7.
Microb Pathog ; 169: 105664, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-35803497

RESUMEN

A large number of infections are caused by multi-resistant bacteria worldwide, increasing to around 700,000 deaths per year. Because of that, many strategies are being developed to combat the resistance of microorganisms to drugs, and recently, chalcones have been studied for this purpose. Chalcones are known as α, ß-unsaturated ketones, characterized by having the presence of two aromatic rings that are joined by a three-carbon chain. They are a class of compounds considered an exceptional model due to chemical simplicity and a wide variety of biological activities, including anticancer, anti-inflammatory, antioxidants, antimicrobials, anti-tuberculosis, anti-HIV, antimalarial, anti-allergic, antifungal, antibacterial, and antileishmaniasis. The objective of this work was to evaluate the antibacterial and antibiotic modifying activity of chalcone (2E)-1-(4'-aminophenyl)-3-(4-methoxyphenyl)-prop-2-en-1-one against the bacteria Staphylococcus aureus carrying a NorA and MepA efflux pump. The results showed that chalcone showed no toxicity on macrophage cells and was able to synergistically modulate the action of Norfloxacin and Ethidium Bromide against the bacteria Staphylococcus aureus 1199B and K2068, respectively. Furthermore, the theoretical physicochemical and pharmacokinetic properties of chalcone showed that it did not present a severe risk of toxicity such as genetic mutation or cardiotoxicity, constituting an excellent pharmacological active ingredient.


Asunto(s)
Chalcona , Chalconas , Infecciones Estafilocócicas , Antibacterianos/química , Antibacterianos/farmacología , Proteínas Bacterianas/metabolismo , Chalcona/farmacología , Chalconas/farmacología , Humanos , Pruebas de Sensibilidad Microbiana , Proteínas Asociadas a Resistencia a Múltiples Medicamentos , Infecciones Estafilocócicas/tratamiento farmacológico , Infecciones Estafilocócicas/microbiología , Staphylococcus aureus/metabolismo
8.
Fundam Clin Pharmacol ; 36(6): 1066-1082, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-35475507

RESUMEN

In recent years, bacterial resistance to traditional drugs has increased, and the need to find new effective antibiotics to treat infections caused by multidrug-resistant bacteria has consequently become more important. The current study aimed to evaluate the potentiation of antibiotic activity and efflux pumps inhibition by (2E)-1-(4-aminophenyl)-3-(4-fluorophenyl)prop-2-en-1-one (PA-Fluorine) against the standard and resistant bacterial strains of Staphylococcus aureus and Escherichia coli. The association between PA-Fluorine and ampicillin reduced the minimum inhibitory concentration (MIC), showing a synergistic effect against S. aureus. For E. coli, PA-Fluorine did not show any significant results when associated with ampicillin. Ciprofloxacin and chlorpromazine showed synergy with PA-Fluorine on the two studied strains. An efflux pump mechanism was involved in the mechanism of action of chlorpromazine, norfloxacin, and ethidium bromide. PA-Fluorine synergistically modulated norfloxacin and bromide. It was thus concluded that PA-Fluorine has the potential to enhance antibacterial activity when combined with antibiotics. Molecular docking studies showed the effect of intermolecular interactions of PA-Fluorine on the NorA and MepA efflux pumps. Physicochemical and pharmacokinetic properties were also obtained by ADMET studies for this chalcone, which presents be a strong candidate as an efflux pump inhibitor.


Asunto(s)
Antibacterianos , Simportadores , Ampicilina/farmacología , Antibacterianos/farmacología , Proteínas Bacterianas/metabolismo , Clorpromazina/farmacología , Escherichia coli/metabolismo , Flúor/farmacología , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Proteínas Asociadas a Resistencia a Múltiples Medicamentos , Norfloxacino/farmacología , Staphylococcus aureus , Simportadores/metabolismo
9.
Bioorg Med Chem Lett ; 50: 128334, 2021 10 15.
Artículo en Inglés | MEDLINE | ID: mdl-34425202

RESUMEN

Compounds capable of inhibiting the efflux pump mechanism are a promising alternative against bacterial resistance because, when combined with antibiotics, they can increase the effectiveness of these drugs by inhibiting active efflux. Elaiophylin, derived from Streptomyces hygroscopicus, is a natural antibiotic that exhibits a variety of biological activities, including antibacterial activity. However, its potential as an inhibitor of the bacterial efflux mechanism has not been investigated. This study evaluated the ability of Elaiophylin to inhibit the NorA efflux pump in Staphylococcus aureus strains. Therefore, tests were performed to obtain the Minimum Inhibitory Concentration (MIC) and to verify the ability of Elaiophylin to potentiate the MIC of the antibiotic Norfloxacin and Ethidium Bromide (EtBr), known substrates of NorA efflux. Real-time PCR and molecular docking assays were also performed to assess the potential of Elaiophylin against NorA. The strains SA-1199 (wild type) and SA-1199B (NorA over-expressed) of S. aureus were used for this study. The results showed that Elaiophylin significantly decreased the MIC of Norfloxacin and EtBr, increasing the activity of these substrates against S. aureus, which carries the efflux protein NorA. However, Elaiophylin provided a non-significant reduction in norA gene expression, however, molecular docking demonstrated a high binding affinity between Elaiophylin and NorA efflux protein, indicating that Elaiophylin can act as a potential NorA in S. aureus.


Asunto(s)
Proteínas Bacterianas/metabolismo , Macrólidos/farmacología , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/metabolismo , Streptomyces/química , Antibacterianos/farmacología , Proteínas Bacterianas/genética , Sitios de Unión , Farmacorresistencia Bacteriana Múltiple , Regulación Bacteriana de la Expresión Génica/efectos de los fármacos , Macrólidos/química , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/genética , Conformación Proteica , Relación Estructura-Actividad
10.
Eur J Pharm Sci ; 158: 105695, 2021 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-33383131

RESUMEN

Chalcones and their derivatives are substances of great interest for medicinal chemistry due to their antibacterial activities. As the bacterial resistance to clinically available antibiotics has become a worldwide public health problem, it is essential to search for compounds capable of reverting the bacterial resistance. As a possibility, the chalcone class could be an interesting answer to this problem. The chalcones (2E)-1-(4'-aminophenyl)-3-(phenyl)­prop-2-en-1-one (APCHAL), and (2E)-1-(4'-aminophenyl)-3-(4-chlorophenyl)­prop-2-en-1-one (ACLOPHENYL) were synthesized by the Claisen-Schmidt condensation and characterized by 1H and 13C nuclear magnetic resonance (NMR), Fourier-transform infrared (FT-IR), and mass spectrometry (MS), In addition, microbiological tests were performed to investigate the antibacterial activity, modulatory potential, and efflux pump inhibition against Staphylococcus aureus (S. aureus) multi-resistant strains. Regarding the S. aureus Gram-positive model, the APCHAL presented synergism with gentamicin and antagonism with penicillin. APCHAL reduced the Minimum inhibitory concentration (MIC) of gentamicin by almost 70%. When comparing the effects of the antibiotic modifying activity of ACLOPHENYL and APCHAL, a loss of synergism is noted with gentamicin due to the addition of a chlorine to the substance structure. For Escherichia coli (E. coli) a total lack of effect, synergistic or antagonistic, was observed between ACLOPHENYL and the antibiotics. In the evaluation of inhibition of the efflux pump, both chalcones presented a synergistic effect with norfloxacin and ciprofloxacin against S. aureus, although the effect is much less pronounced with ACLOPHENYL. The effect of APCHAL is particularly notable against the K2068 (MepA overexpresser) strain, with synergistic effects with both ciprofloxacin and ethidium bromide. The docking results also show that both compounds bind to roughly the same region of the binding site of 1199B (NorA overexpresser), and that this region overlaps with the preferred binding region of norfloxacin. The APCHAL chalcone may contribute to the prevention or treatment of infectious diseases caused by multidrug-resistant S. aureus.


Asunto(s)
Chalcona , Chalconas , Staphylococcus aureus Resistente a Meticilina , Antibacterianos/farmacología , Proteínas Bacterianas/metabolismo , Chalconas/farmacología , Escherichia coli/metabolismo , Staphylococcus aureus Resistente a Meticilina/metabolismo , Pruebas de Sensibilidad Microbiana , Proteínas Asociadas a Resistencia a Múltiples Medicamentos , Espectroscopía Infrarroja por Transformada de Fourier , Staphylococcus aureus/metabolismo
11.
Int Immunopharmacol ; 86: 106766, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32652504

RESUMEN

BACKGROUND: Limonene (LIM) and its main metabolite perillyl alcohol (POH) are ingredients found in food with promising chemical entities due to their pharmacological profile. In this study, we hypothesized that LIM and POH are two molecules capable of accelerating the regenerative process and alleviating neuropathic pain. METHODS: Animals were treated daily (LIM, POH and saline) for 28 days and during this period evaluated for mechanical hyperalgesia, astrocyte participation by immunofluorescence for GFAP, and ELISA was used to quantify IL-1ß and TNF-α in the spinal cord. Western blot analysis of the following proteins was also performed: GFAP, GAP-43, NGF and ERK. For motor deficit analysis, tests were performed to assess hind paw muscle strength and footprints through gait (SFI). RESULTS: Both POH and LIM accelerated the regenerative process and improved motor deficits comparing to positive control; however, POH was more effective, particularly between the 2nd and 3rd week after the nerve injury, increasing GAP-43, NGF and the phosphorylated ERK immunocontent. Moreover, POH and LIM were able to reduce hyperalgesia and astrocytosis. CONCLUSIONS: Both substances, LIM and POH, improved the regeneration process and sensory and motor function recovery in the PNI model in mice by mitigating the inflammatory reactions and up-regulating the neurotrophic process.


Asunto(s)
Antiinflamatorios/uso terapéutico , Aditivos Alimentarios/uso terapéutico , Limoneno/uso terapéutico , Monoterpenos/uso terapéutico , Neuronas Motoras/fisiología , Neuralgia/terapia , Traumatismos de los Nervios Periféricos/terapia , Animales , Modelos Animales de Enfermedad , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Proteínas Activadoras de GTPasa/metabolismo , Humanos , Interleucina-1beta/metabolismo , Masculino , Ratones , Factor de Crecimiento Nervioso/metabolismo , Neuralgia/dietoterapia , Regeneración/efectos de los fármacos , Factor de Necrosis Tumoral alfa/metabolismo
12.
Saudi J Biol Sci ; 26(5): 873-880, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31303814

RESUMEN

Inflammation is a protective response of the organism against damaging agents, this process is considered beneficial, however in some situations, this response can be damage when exacerbated effect are present. This claim objective to evaluate the qualitative and quantitative chemical profile, acute toxic and anti-inflammatory effects of the hydroalcoholic extract of leaves from Tocoyena formosa (Cham. & Schlecht.) K. Schum. (HELTF). Quantitative and qualitative phytochemical analysis was performed by HPLC-DAD and colorimetric assay. The topical anti-inflammatory activity was determined in Croton oil-induced ear edema assay and systemic activity was performed in vascular permeability, paw edema induced by carrageenan and dextran. Phytochemical analysis of leaves from HELTF showed presence of tannin, flavonoid, saponins an other that confirmed by HPLC analysis. The extract did not cause significant with LD50 greater than 5000 mg/kg and did not promote significate reduction in topical inflammatory process. However, HELTF demonstrate significant reduction of paw edema induced by carrageenan and dextran. The HELTF (200 mg/kg) reduced the protein/cell migration in the intradermal carrageenan-induced inflammation. Our results demonstrated that the first time the chemical profile and describe the effective action in systemic anti-inflammatory, antiedematogenic activity and low acute toxicity. This activity presents, supporting its traditional use. However, new studies are necessary for the detection and clarification of the possible mechanism of action.

13.
Pathogens ; 7(4)2018 Dec 10.
Artículo en Inglés | MEDLINE | ID: mdl-30544654

RESUMEN

Mauritia flexuosa (buriti) is a typical Brazilian palm tree found in swampy regions with many plant forms. The fruit has various purposes with the pulps to the seeds being used for ice creams, sweets, creams, jellies, liqueurs, and vitamin production. A physicochemical characterization of the fixed pulp oil and its antibacterial and aminoglycoside antibiotic modifying activity against Gram-positive and Gram-negative multiresistant bacterial strains were performed using broth microdilution assays. Physical properties, such as moisture, pH, acidity, peroxide index, relative density, and refractive index, indicated oil stability and chemical quality. In the GC/MS chemical composition analysis, a high content of unsaturated fatty acids (89.81%) in relation to saturated fatty acids (10.19%) was observed. Oleic acid (89.81%) was the main fatty acid identified. In the antibacterial test, the fixed oil obtained the Minimum Inhibitory Concentration (MIC) ≥ 1024 µg/mL for all standard and multiresistant bacterial strains. The synergic effect of fixed pulp oil combined was observed only in Staphylococcus aureus SA⁻10, with an MIC reduction of the gentamicin and amikacin by 40.00% and 60.55%, respectively. The data indicates the M. flexuosa fixed oil as a valuable source of oleic acid and modulator of aminoglycoside activity.

14.
Pharm Biol ; 54(5): 863-7, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-26455352

RESUMEN

CONTEXT: Ocimum basilicum L. (Lamiaceae), popularly known as basil, is part of a group of medicinal plants widely used in cooking and known for its beneficial health properties, possessing significant antioxidant effects, antinociceptive, and others. OBJECTIVE: The objective of this study is to determine the pharmacological effects produced on the bacterial strains Staphylococcus aureus and Pseudomonas aeruginosa when standard antibiotics and O. basilicum essential oil are combined. MATERIALS AND METHODS: The extraction of O. basilicum (leaves) components was done by steam distillation. The Minimum inhibitory concentration (MIC) was calculated using microdilution technique, where the oil concentrations varied from 2 to 1024 µg/mL. The combinations of O. basilicum oil with ciprofloxacin or imipenem were analyzed by the checkerboard method where fractional inhibitory concentration (FIC) indices were calculated. RESULTS: Ocimum basilicum essential oil, imipenem, and ciprofloxacin showed respective MIC antibacterial activities of 1024, 4, and 2 µg/mL, against S. aureus. In S. aureus, the oil with imipenem association showed synergistic effect (FIC = 0.0625), while the oil with ciprofloxacin showed antagonism (FIC value = 4.25). In P. aeruginosa, the imipenem/oil association showed additive effect for ATCC strains, and synergism for the clinical strain (FIC values = 0.75 and 0.0625). The association of O. basilicum essential oil with ciprofloxacin showed synergism for clinical strains (FIC value = 0.09). CONCLUSION: Ocimum basilicum essential oil associated with existing standard antibiotics may increase their antibacterial activity, resulting in a synergistic activity against bacterial strains of clinical importance. The antibacterial activity of O. basilicum essential oil may be associated with linalool.


Asunto(s)
Antibacterianos/farmacología , Ocimum basilicum , Aceites de Plantas/farmacología , Pseudomonas aeruginosa/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/aislamiento & purificación , Ciprofloxacina/farmacología , Humanos , Pruebas de Sensibilidad Microbiana/métodos , Aceites Volátiles/aislamiento & purificación , Aceites Volátiles/farmacología , Hojas de la Planta , Aceites de Plantas/aislamiento & purificación , Pseudomonas aeruginosa/fisiología , Staphylococcus aureus/fisiología
15.
Oxid Med Cell Longev ; 2014: 696785, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25478063

RESUMEN

The guava fruit, Psidium guajava var. pomifera (Myrtaceae family), is a native plant from South America. Its leaves and fruits are widely used in popular medicine in tropical and subtropical countries. Drosophila melanogaster has been used as one of the main model organisms in genetic studies since the 1900s. The extensive knowledge about this species makes it one of the most suitable organisms to study many aspects of toxic compound effects. Due to the lack of studies on the effects of the bioactive compounds present in the P. guajava var. pomifera essential oil, we performed a phytochemical characterization by CG-MS and evaluated the toxicity induced by the essential oil in the D. melanogaster insect model. In order to understand the biochemical mechanisms of toxicity, changes on the Nrf2 signaling as well as hallmarks of oxidative stress response were followed in the exposed flies. Our results showed that exposure of insects to the P. guajava oil increased mortality and locomotor deficits in parallel with an oxidative stress response signaling. Therefore, it suggested a bioinsecticidal activity for P. guajava volatile compounds by means of oxidative stress. Further studies are ongoing to identify which oil compounds are responsible for such effect.


Asunto(s)
Drosophila melanogaster/efectos de los fármacos , Drosophila melanogaster/metabolismo , Myrtaceae/química , Aceites Volátiles/farmacología , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Psidium/química , Animales , Femenino , Fumigación/métodos , Masculino
16.
Jundishapur J Nat Pharm Prod ; 9(3): e13521, 2014 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-25237640

RESUMEN

BACKGROUND: Several studies have shown that species of the genus Hyptis, have promising antimicrobial and antifungal effects. OBJECTIVES: Identify of chemical constituents of essential oil from leaves of Hyptis martiusii and evaluate its effect against bacterial strains by direct and gaseous contact. MATERIALS AND METHODS: Essential oil was extracted from leaves of Hyptis martiusii Benth using hydro-distillation, and its composition was determined using gas chromatography-mass spectrometry (GC-MS). Chemical analysis showed that there was a predominance of sesquiterpenes. The leaf essential oil was screened for its minimal inhibitory concentration and modulatory effect of aminoglycoside by the direct (MIC) and gaseous (MID) micro-dilution assays for various pathogenic microorganisms. The essential oil remarkably inhibited the growth of all of the tested bacteria (MIC < 512 µg/mL) except S. aureus (SA358) multidrug resistant (MRSA) by direct contact. RESULTS: Twenty-four compounds representing 92.13% of the essential oil of leaves were characterized; δ -3-carene (6.88%), 1, 8-cineole (7.01%), trans-caryophyllene (9.21%), Cariophyllene oxide (7.47%) and bicyclogermacrene (10.61%) were found as the major components. Modulatory aminoglycoside effect, by direct contact, was showed antagonistic relationship with antimicrobial activity. The gaseous component of the oil inhibited the bacterial growth of all of the tested bacteria in 50% and 25% of oil concentration and demonstrated synergistic interactions can be attributed to the constituting the oil compounds. CONCLUSIONS: These results show that this oil influences the activity of the antibiotic and may be used as an adjuvant in the antibiotic therapy of respiratory tract bacterial pathogens.

17.
Biomed Res Int ; 2014: 305610, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24683545

RESUMEN

The Lippia origanoides H.B.K. ethanol extract (LOEE) and hexane (LOHEX), dichloromethane (LODCM), and ethyl acetate (LOEA) fractions were tested for their antimicrobial activity alone or in combination with antibiotics against a methicillin resistant Staphylococcus aureus (MRSA) strain. The natural products did not show antimicrobial activity against multidrug resistant strain at the clinically significant concentrations tested. However, a modulatory effect in the antibacterial activity of the neomycin and amikacin was verified when LOEE, LOHEX and LODCM were added to the growth medium at subinhibitory concentrations. A similar modulation was found when the natural products were changed for chlorpromazine, an inhibitor of bacterial efflux pumps, suggesting the involvement of resistance mediated by efflux system in the MRSA tested. The fractions LOHEX and LODCM showed a modulatory activity bigger than their majority compounds (carvacrol, thymol, and naringenin), indicating that this activity is not due to their majority compounds only, but it is probably due to a synergism between their chemical components. These results indicate that L. origanoides H.B.K. can be a source of phytochemicals able to modify the phenotype of resistance to aminoglycosides in MRSA.


Asunto(s)
Antibacterianos/farmacología , Lippia/química , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Fitoquímicos/farmacología , Acetatos/química , Clorpromazina/farmacología , Cimenos , Etanol/química , Flavanonas/farmacología , Cromatografía de Gases y Espectrometría de Masas , Hexanos/química , Cloruro de Metileno/química , Pruebas de Sensibilidad Microbiana , Monoterpenos/farmacología , Extractos Vegetales/farmacología , Timol/farmacología
18.
Artículo en Inglés | MEDLINE | ID: mdl-24302969

RESUMEN

Background. Phrynops geoffroanus is a small turtle that inhabits lakes, rivers, and streams throughout South America. The body fat of this animal is used as a folk medicine in Brazil for treating illnesses such as sore throats, ear aches, mumps, rheumatism, and arthritis. The present study evaluated the antimicrobial activity of oil extracted from Phrynops geoffroanus (OPG), determined its chemical composition, and discussed the implications of its use in traditional medicine. The OPG was obtained from the ventral region of this turtle using hexane as a solvent. The antimicrobial activity of OPG was tested against standard and multiresistance strains of bacteria and fungi and its composition was determined indirectly by analyzing the methyl esters of the component fatty acids. The OPG presented a clinically relevant antifungal activity against Candida krusei ATCC 6258 (MIC 128 µg/mL). When the OPG was associated with the antibacterial and antifungal drugs, was observed a synergistic effect when associated the OPG with the gentamicin against the strain Pseudomonas aeruginosa 22. Our results indicated that OPG has clinically relevant antifungal activity against C. krusei, and demonstrated synergetic antibacterial activity in combination with commercial antibiotics against Pseudomonas aeruginosa.

19.
Artículo en Inglés | MEDLINE | ID: mdl-23818919

RESUMEN

Knowledge of medicinal plants is often the only therapeutic resource of many communities and ethnic groups. "Erva-baleeira", Cordia verbenacea DC., is one of the species of plants currently exploited for the purpose of producing a phytotherapeutic product extracted from its leaves. In Brazil, its major distribution is in the region of the Atlantic Forest and similar vegetation. The crude extract is utilized in popular cultures in the form of hydroalcoholic, decoctions and infusions, mainly as antimicrobial, anti-inflammatory and analgesic agents. The aim of the present study was to establish a chemical and comparative profile of the experimental antibacterial activity and resistance modifying activity with ethnopharmacological reports. Phytochemical prospecting and HPLC analysis of the extract and fractions were in agreement with the literature with regard to the presence of secondary metabolites (tannins and flavonoids). The extract and fraction tested did not show clinically relevant antibacterial activity, but a synergistic effect was observed when combined with antibiotic, potentiating the antibacterial effect of aminoglycosides. We conclude that tests of antibacterial activity and modulating the resistance presented in this work results confirm the ethnobotanical and ethnopharmacological information, serving as a parameter in the search for new alternatives for the treatment of diseases.

20.
Artículo en Inglés | MEDLINE | ID: mdl-23864894

RESUMEN

Croton campestris A. St.-Hill., popularly known as "velame do campo," is a species native to the savannah area of Northeast Brazil, which is used by traditional communities in folk medicine for variety of health problems, especially detoxification, inflammation, and gastritis. The hydroalcoholic extract of C. campestris leaves (HELCC) was assessed for its antiulcerogenic effect in gastric lesion models and effect on intestinal motility in mice, and possible mechanisms of action were examined. HELCC showed significant gastroprotective action in all models of gastric ulcer evaluated; the results suggest that this action probably involves the nitric oxide pathway. HELCC did not show alteration of intestinal motility in mice. It was also found that C. campestris represents a promising natural source with important biological potential, justifying some of its uses in folk medicine.

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