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1.
J Toxicol Environ Health A ; 87(14): 592-603, 2024 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-38712866

RESUMEN

Punica granatum, popularly known as pomegranate, is a fruit tree with wide worldwide distribution, containing numerous phytochemicals of great medicinal value. The aim of the present study was to determine the phytochemical profile and antioxidant potential of a protein fraction (PF) derived from P. granatum sarcotesta which is rich in lectin. In addition, the acute oral toxicity, genotoxicity and antigenotoxicity of this protein fraction (PF) from P. granatum sarcotesta was measured. The phytochemical profile of PF was determined using HPLC. The in vitro antioxidant effect was assessed using the methods of total antioxidant capacity (TAC) and DPPH and ABTS+ radical scavenging. Acute oral toxicity was determined in female Swiss mice administered a single dose of 2000 mg/kg. This PF was examined for genotoxicity and antigenotoxicity at doses of 500, 1000 and 2000 mg/kg, utilizing mouse peripheral blood cells. Phytochemical characterization detected a high content of ellagic acid and antioxidant capacity similar to that of ascorbic acid (positive control). PF was not toxic (LD50 >2000 mg/kg) and did not exert a genotoxic effect in mice. PF protected the DNA of peripheral blood cells against damage induced by cyclophosphamide. In conclusion, this PF fraction exhibited significant antioxidant activity without initiating toxic or genotoxic responses in mice.


Asunto(s)
Antioxidantes , Extractos Vegetales , Granada (Fruta) , Animales , Ratones , Antioxidantes/farmacología , Femenino , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Extractos Vegetales/farmacología , Granada (Fruta)/química , Lectinas/toxicidad , Pruebas de Mutagenicidad , Daño del ADN/efectos de los fármacos , Pruebas de Toxicidad Aguda
2.
J Toxicol Environ Health A ; 87(16): 662-673, 2024 Aug 17.
Artículo en Inglés | MEDLINE | ID: mdl-38808737

RESUMEN

Pseudobombax marginatum, popularly known as "embiratanha," is widely used by traditional communities as anti-inflammatory and analgesic agent. This study aimed to determine the phytochemical profile as well as cytotoxicity, acute oral toxicity, genotoxicity, and mutagenicity attributed to exposure to aqueous (AqEx) and ethanolic (EtEx) extracts of embiratanha bark. Phytochemical screening was conducted using thin-layer chromatography (TLC). Cell viability was analyzed using MTT assay with human mammary gland adenocarcinoma (MDA-MB-231) and macrophage (J774A.1) cell lines, exposed to concentrations of 12.5, 25, 50, or 100 µg/ml of either extract. For acute oral toxicity, comet assay and micronucleus (MN) tests, a single dose of 2,000 mg/kg of either extract was administered orally to Wistar rats. TLC analysis identified classes of metabolites in the extracts, including cinnamic acid derivatives, flavonoids, hydrolyzable tannins, condensed tannins, coumarins, and terpenes/steroids. In the cytotoxicity assay, the varying concentrations of extracts derived from embiratanha induced no significant alterations in the viability of MDA-MB-231 cells. The lowest concentration of EtEx significantly increased macrophage J774A.1 viability. However, the higher concentrations of AqEx markedly lowered macrophage J774A.1 viability. Animals exhibited no toxicity in the parameters analyzed in acute oral toxicity, comet assay, and MN tests. Further, EtEx promoted a significant reduction in DNA damage index and DNA damage frequency utilizing the comet assay, while the group treated with AqEx exhibited no marked differences. Thus, data demonstrated that AqEx or EtEx of embiratanha may be considered safe at a dose of 2,000 mg/kg orgally under our experimental conditions tested.


Asunto(s)
Extractos Vegetales , Ratas Wistar , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Animales , Humanos , Ratas , Línea Celular Tumoral , Masculino , Ensayo Cometa , Pruebas de Micronúcleos , Femenino , Supervivencia Celular/efectos de los fármacos , Fitoquímicos/toxicidad , Fitoquímicos/análisis , Ratones , Corteza de la Planta/química , Mutágenos/toxicidad , Pruebas de Mutagenicidad , Etanol/química
3.
Inflammopharmacology ; 32(1): 595-602, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37823930

RESUMEN

Wounds encompass physical, chemical, biological, induced damages to the skin or mucous membranes. In wound treatment, combating infections is a critical challenge due to their potential to impede recovery and inflict systemic harm on patients. Previously, the essential oil extracted from Psidium glaziovianum (PgEO) demonstrated antinociceptive and anti-inflammatory attributes, along with negligible oral toxicity. Hence, our study aimed to assess the effects of topically applying a gel formulation containing PgEO to excisional wounds in mice. Additionally, an in vitro antimicrobial assessment was conducted. The formulated gel underwent characterization and toxicological evaluation on erythrocytes, as well as a dermal irritation test. Its antimicrobial activity was tested against both gram-positive and gram-negative bacteria, as well as fungi. Subsequently, an assessment of its efficacy in excisional wound healing was conducted in mice. The findings of this investigation highlight the gel's efficacy against both gram-positive and gram-negative bacteria, as well as fungi. Moreover, this study underscores that the PgEO-gel treatment enhances skin wound healing, potentially due to its capacity to trigger antioxidant enzymes and suppress pro-inflammatory cytokines. Furthermore, the gel exhibited minimal toxicity to erythrocytes and skin irritation. These findings hold promise for prospective preclinical and clinical trials across diverse wound types. In conclusion, this study sheds light on the potential therapeutic applications of the gel formulation containing essential oil from P. glaziovianum in the context of wound healing.


Asunto(s)
Aceites Volátiles , Psidium , Humanos , Animales , Ratones , Antibacterianos , Estudios Prospectivos , Bacterias Gramnegativas , Bacterias Grampositivas , Cicatrización de Heridas , Aceites Volátiles/farmacología
4.
Inflammopharmacology ; 32(5): 3389-3398, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39126571

RESUMEN

Syagrus coronata, a native palm tree in the Caatinga domain, produces fixed oil (ScFO) used therapeutically and dietary by Northeast Brazilian communities. This study evaluated its anti-inflammatory potential of CFA-induced arthritis and its effect on behavioral parameters. In the acute model, ScFO at 25, 50, and 100 mg/kg showed edematogenic effects similar to indomethacin at 4 mg/kg (p > 0.05). In the arthritis model, 100 mg/kg ScFO treatment was comparable to indomethacin (4 mg/kg) (p > 0.05). TNF-α and IL-1ß levels were significantly reduced in ScFO-treated groups at 25, 50, and 100 mg/kg, and the indomethacin group (4 mg/kg) versus the positive control (p > 0.05). Radiographs showed severe soft-tissue swelling and bone deformities in the control group, while the 100 mg/kg ScFO group had few alterations, similar to the indomethacin group. Histopathological analysis revealed intense lymphocytic infiltration in the control group, mild diffuse lymphocytic infiltration in the indomethacin group, and mild lymphoplasmacytic infiltration with focal polymorphonuclear infiltrates in the 100 mg/kg ScFO group. Behavioral analysis showed improved exploratory stimuli in ScFO and indomethacin-treated mice compared to the positive control (p > 0.05). ScFO demonstrated anti-inflammatory effects in both acute and chronic arthritis models, reducing edema and pro-inflammatory cytokines, and improved exploratory behavior due to its analgesic properties.


Asunto(s)
Antiinflamatorios , Artritis Experimental , Adyuvante de Freund , Animales , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/patología , Ratones , Antiinflamatorios/farmacología , Masculino , Aceites de Plantas/farmacología , Arecaceae/química , Edema/tratamiento farmacológico , Factor de Necrosis Tumoral alfa/metabolismo , Interleucina-1beta/metabolismo , Aceite de Palma/farmacología , Indometacina/farmacología , Brasil , Relación Dosis-Respuesta a Droga
5.
J Appl Microbiol ; 134(7)2023 Jul 04.
Artículo en Inglés | MEDLINE | ID: mdl-37437916

RESUMEN

AIMS: We investigated the putative fungistatic and fungicidal activities of pomegranate sarcotesta lectin (PgTeL) against Cryptococcus neoformans B3501 (serotype D), specifically the ability of PgTeL to inhibit yeast capsule and biofilm formation in this strain. METHODS AND RESULTS: PgTeL showed a minimum inhibitory concentration of 172.0 µg ml-1, at which it did not exhibit a fungicidal effect. PgTeL concentrations of 4.0-256.0 µg ml-1 reduced biofilm biomass by 31.0%-64.0%. Furthermore, 32.0-256.0 µg ml-1 PgTeL decreased the metabolic activity of the biofilm by 32.0%-93.0%. Scanning electron microscopy images clearly revealed disruption of the biofilm matrix. Moreover, PgTeL disrupted preformed biofilms. At concentrations of 8.0-256.0 µg ml-1, PgTeL reduced metabolic activity in C. neoformans by 36.0%-92.0%. However, PgTeL did not inhibit the ability of B3501 cells to form capsules under stress conditions. CONCLUSIONS: PgTeL inhibited biofilm formation and disrupted preformed biofilms, demonstrating its potential for use as an anticryptococcal agent.


Asunto(s)
Criptococosis , Cryptococcus neoformans , Granada (Fruta) , Lectinas/farmacología , Granada (Fruta)/metabolismo , Plancton/metabolismo , Biopelículas , Pruebas de Sensibilidad Microbiana , Antifúngicos/farmacología , Antifúngicos/metabolismo
6.
Chem Biodivers ; 19(3): e202100853, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34990049

RESUMEN

The ethanolic extract from Croton blanchetianus leaves has been shown to have antinociceptive activity in mice. Here, we investigated the antinociceptive activity of an ethyl acetate fraction (EAF) from this extract in mice and the possible pathways involved in the analgesic effect. Adverse effects on behavior and motor coordination were also evaluated. The EAF was characterized by liquid chromatography coupled with mass spectrometry and evaluated (12.5, 25, and 50 mg/kg per os) in the acetic acid-induced abdominal writhing, formalin, hot plate, and tail immersion assays. Naloxone, atropine, glibenclamide, prazosin, or yohimbine was pre-administered to mice to investigate the involved pathways in the formalin test. The open-field, rotarod, and elevated plus-maze tests were used to assess behavior and locomotion. The main components of the EAF were quercetin-3-O-(2-rhamnosyl) rutinoside, hyperoside, quercetin rutinoside pentoside, and quercetin hexoside deoxyhexoside. EAF showed antinociceptive effects in all models and was effective against both neurogenic and inflammatory pain. The reversion of the effects in the formalin test by naloxone and atropine revealed that the EAF acted via the opioid and cholinergic systems. In the open-field test, the behavior of the animals treated with the EAF was like that of control, except at the highest dose, when hypnosis, eyelid ptosis, decreased walking, hygiene, and rearing behaviors were observed. No muscle relaxant effect was observed, but an anxiogenic effect was observed at all doses. This study provides new scientific evidence on the pharmacological properties of C. blanchetianus leaves and their potential for the development of phytomedicines with analgesic properties.


Asunto(s)
Croton , Euphorbiaceae , Analgésicos/farmacología , Analgésicos/uso terapéutico , Analgésicos Opioides/farmacología , Animales , Colinérgicos , Flavonoides , Ratones , Extractos Vegetales/uso terapéutico , Hojas de la Planta
7.
Inflammopharmacology ; 30(2): 599-607, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35257283

RESUMEN

Plants of the genus Psidium have been employed in "in natura" consumption and agroindustry, and owing to the diversity of phytochemicals, the development of new pharmaceutical forms has received remarkable research interest. In this study, the essential oil obtained from Psidium glaziovianum (PgEO) leaves were evaluated antinociceptive and anti-inflammatory activities were evaluated in mouse models. Initially, PgEO was characterized by gas chromatography-mass spectrometry and gas chromatography with flame ionization detection, and the profile was dominated by sesquiterpene compounds. In the evaluation of acute antinociceptive activity (abdominal contortions induced by acetic acid, formalin, tail immersion, and hot plate tests), PgEO promoted a reduction in nociception in the chemical and thermal models. Additionally, the potential underlying mechanism was investigated using pain pathway blockers, and the results revealed a combined action of opioidergic and muscarinic pathways. The anti-inflammatory potential was confirmed by anti-edematogenic action, reduced cell migration, pro-inflammatory cytokine production, and granuloma formation in chronic processes. This study provides evidence that PgEO can be effective for the treatment of pain and acute and chronic inflammation.


Asunto(s)
Aceites Volátiles , Psidium , Administración Oral , Analgésicos , Animales , Edema/inducido químicamente , Edema/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Ratones , Aceites Volátiles/farmacología , Dolor/tratamiento farmacológico , Extractos Vegetales , Hojas de la Planta/química , Psidium/química
8.
Inflammopharmacology ; 30(6): 2273-2284, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36094726

RESUMEN

Eugenia pohliana DC.(Myrtaceae) is used in folk medicine by communities in Brazil. However, there are no reports on its biological activity. This is the first study to identify the components of E. pohliana essential oil (EpEO) and evaluate their antinociceptive and anti-inflammatory activities in an in vivo model at doses of 25, 50, and 100 mg/kg. The essential oil (EO) was obtained by hydrodistillation, and the analysis was performed by gas chromatography coupled with mass spectrometry. Antinociceptive activity was evaluated by writhing tests, tail movement, and formalin (neurogenic and inflammatory pain); naloxone was used to determine the nociception mechanism. Anti-inflammatory activity was assessed by oedema and peritonitis tests. We found that (E)-ß-caryophyllene (BCP) (15.56%), δ-cadinene (11.24%) and α-cadinol (10.89%) were the major components. In the writhing test, there was a decrease in writing by 42.95-70.70%, in the tail movement, an increase in latency time by 69.12-86.63%, and in the formalin test, there was a reduction in pain neurogenic by 29.54-61.74%, and inflammatory pain by 37.42-64.87%. The antinociceptive effect of EpEO occurs through the activation of opioid receptors. In addition, a reduction in inflammation by 74.93‒81.41% was observed in the paw edema test and inhibition of the influx of leukocytes by 51.86‒70.38% and neutrophils by 37.74‒54.72% in the peritonitis test. It was concluded that EpEO has antinociceptive effect by the opioid pathway, as shown by the inhibitory effect of naloxone, and anti-inflammatory actions, and that its use does not cause hemolytic damage or behavioral change.


Asunto(s)
Eugenia , Myrtaceae , Aceites Volátiles , Peritonitis , Ratones , Animales , Eugenia/química , Aceites Volátiles/farmacología , Aceites Volátiles/uso terapéutico , Nocicepción , Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Edema/inducido químicamente , Edema/tratamiento farmacológico , Dolor/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Inflamación/tratamiento farmacológico , Peritonitis/tratamiento farmacológico , Naloxona/uso terapéutico
9.
An Acad Bras Cienc ; 93(3): e20201596, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33978069

RESUMEN

Moringa oleifera, a plant widely used in traditional medicine as well as for water purification, contains a lectin on its seeds named WSMoL which modulates several immune characteristics and has shown cardiac safe properties. Here, we tested the hypothesis that WSMoL is able to recover fasting glucose levels and to improve the cardiac left ventricular (LV) function in a type 2 diabetes mellitus (T2DM) mice model. T2DM was induced in adult C57BL/6 mice by combining a high fat diet and low doses of Streptozotocin. Mice were randomly divided in two groups: i. received WSMoL for 21 consecutive days by gavage (T2DM + WSMoL) and ii. received saline solution (T2DM). Metabolic parameters and LV function were assessed. WSMoL was able to reduce fasting blood glucose levels in T2DM mice after 2 weeks of treatment, when compared to T2DM untreated group. Regarding to cardiac LV function, the T2DM + WSMoL group depicted ejection fraction values comparable to non-diabetic group. Our results show: i. WSMoL treatment presented a potent hypoglycemic effect decreasing insulin resistance and ii. WSMoL was able to improve cardiac LV ejection fraction. Collectively, the results presented here show WSMoL as a potential hypoglycemic agent to be tested in T2DM patients.


Asunto(s)
Diabetes Mellitus Tipo 2 , Moringa oleifera , Animales , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Humanos , Lectinas , Ratones , Ratones Endogámicos C57BL , Semillas , Volumen Sistólico , Función Ventricular Izquierda , Agua
10.
Pestic Biochem Physiol ; 177: 104901, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34301362

RESUMEN

Lippia alba is an aromatic shrub known to produce a diversity of essential oils, which can be classified into chemotypes. This study reports on the insecticidal activity of essential oil from L. alba leaves collected at Caatinga and its major compound against termite Nasutitermes corniger and maize weevil Sitophilus zeamais. The chromatographic analysis revealed the presence of 19 compounds, with 1,8-cineole being the most common (70.01%). When ingested, the oil promoted the mortality of N. corniger (LC50: 18.25 and 8.4 nL/g for workers and soldiers, respectively). The compound 1,8-cineole was also termiticidal for workers (LC50: 13.7 nL/g). The oil inhibited the activity of N. corniger exoglucanase, xylanase, and proteases. Toxicity by ingestion to S. zeamais was detected for the oil (LC50: 0.297 µL/g) but not for 1,8-cineole; however, both the oil and 1,8-cineole showed anti-nutritional effects. Fumigant effects of the oil and 1,8-cineole against S. zeamais (LC50 of 78.0 and 13.64 µL/L in air, respectively) were detected. This is the first record of a chemotype VI oil from L. alba collected at Caatinga and the first report of the insecticidal activity of a chemotype VI oil. Our study demonstrates that essential oil from L. alba and 1,8 cineole have the potential for the development of natural insecticides.


Asunto(s)
Insecticidas , Isópteros , Lippia , Aceites Volátiles , Gorgojos , Animales , Eucaliptol , Insecticidas/farmacología , Aceites Volátiles/farmacología , Hojas de la Planta
11.
Chem Biodivers ; 18(6): e2100125, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33893724

RESUMEN

Previous studies have characterized a saline extract from Microgramma vacciniifolia rhizome and its lectin (MvRL)-rich fraction with low acute toxicity. In the present study, we evaluated these preparations for acute toxicity (1,000 mg/kg) and antinociceptive and anti-inflammatory activities (100-400 mg/kg for the extract and 25-50 mg/kg for the fraction). No signs of toxicity were observed. Both the extract and fraction increased the latency period for nociception in the hot plate assay, decreased writhing induced by acetic acid, and promoted analgesic effects in phases 1 and 2 of the formalin test. The antinociceptive mechanism was attributed to interactions with opioid receptors and K+ ATPase channels. The extract and fraction decreased carrageenan-induced paw edema in 46.15 % and 77.22 %, respectively, at the highest doses evaluated. Furthermore, the fraction was shown to act on the bradykinin pathway. The ability to decrease leukocyte migration after treatment was also verified in the peritonitis and air pouch models. In exudates collected from air pouches, decreased tumor necrosis factor (TNF)-α and increased interleukin (IL)-10 levels were noted. Both the extract and fraction also effectively inhibited the development of granulomatous tissue. In conclusion, the substances investigated in this study can be used for the development of novel therapeutic options for pain and inflammatory processes.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Edema/tratamiento farmacológico , Lectinas/química , Extractos Vegetales/farmacología , Rizoma/química , Analgésicos/química , Analgésicos/aislamiento & purificación , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Carragenina , Movimiento Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Leucocitos/efectos de los fármacos , Ratones , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Receptores Opioides/metabolismo , Salinidad , ATPasa Intercambiadora de Sodio-Potasio/antagonistas & inhibidores , ATPasa Intercambiadora de Sodio-Potasio/metabolismo
12.
Chem Biodivers ; 18(12): e2100538, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34609784

RESUMEN

The aim of this study was to evaluate the phytochemical composition, antioxidant, and antimicrobial potential of crude extract and fractions of Punica granatum leaves. The extract was produced by turbo extraction, after which hexanic, ethyl acetate, and aqueous fractions were obtained by partitioning. The chemical analyses were performed by thin layer chromatography and high-performance liquid chromatography, and the antioxidant activities were assayed by DPPH. and ABTS.+ . Minimal inhibitory and bactericidal concentrations (MIC/MBC) were applied to twenty-two bacteria. Most strains susceptible to extract/fractions and resistant to antibiotics were selected, and ampicillin, azithromycin, ciprofloxacin, and gentamicin were associated with the ethyl acetate fraction (EAF) against multidrug-resistant strains in modulatory and checkboard models. The data from chromatographic analyses showed flavonoids and tannins in the extract, as well as the enrichment of EAF in phenols, mainly flavonoids. The flavonoids were connected to the electron transfer activity demonstrated in the DPPH. and ABTS.+ assays. Gram-positive strains are more susceptible to EAF. The subinhibitory concentrations of P. granatum enhanced the antimicrobial activity of the agents and reduced the EAF individual MIC, and the combination of EAF and antibiotics demonstrated a synergistic effect. These results present a promising approach for developing a therapy in which antioxidant extracts and fractions can be used in combination with antibiotics.


Asunto(s)
Antibacterianos/farmacología , Antioxidantes/farmacología , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Lythraceae/química , Extractos Vegetales/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Benzotiazoles/antagonistas & inhibidores , Compuestos de Bifenilo/antagonistas & inhibidores , Escherichia coli/efectos de los fármacos , Klebsiella pneumoniae/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Picratos/antagonistas & inhibidores , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Pseudomonas aeruginosa/efectos de los fármacos , Ácidos Sulfónicos/antagonistas & inhibidores
13.
Pestic Biochem Physiol ; 165: 104464, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-32359546

RESUMEN

The glutathione S-transferases (GSTs) are enzymes involved in several distinct biological processes. In insects, the GSTs, especially delta and epsilon classes, play a key role in the metabolism of xenobiotics used to control insect populations. Here, we investigated its potential role in temephos resistance, examining the GSTE2 gene from susceptible (RecL) and resistant (RecR) strains of the mosquito Aedes aegypti, vector for several pathogenic arboviruses. Total GST enzymatic activity and the GSTE2 gene expression profile were evaluated, with the GSTE2 cDNA and genomic loci sequenced from both strains. Recombinant GSTE2 and mutants were produced in a heterologous expression system and assayed for enzyme kinetic parameters. These proteins also had their 3D structure predicted through molecular modeling. Our results showed that RecR has a profile of total GST enzymatic activity higher than RecL, with the expression of the GSTE2 gene in resistant larvae increasing six folds. Four exclusive RecR mutations were observed (L111S, I150V, E178A and A198E), which were absent in the laboratory susceptible strains. The enzymatic activity of the recombinant GSTE2 showed different kinetic parameters, with the GSTE2 RecR showing an enhanced ability to metabolize its substrate. The I150V mutation was shown to induce significant changes in catalytic parameters and a 3D modeling of GSTE2 mapped two of the RecR changes (L111S and I150V) near the enzyme's catalytic pocket, also implying an impact on its catalytic activity. Our results reinforce a potential role for GSTE2 in the metabolic resistance phenotype while contributing to the understanding of the molecular basis for the resistance mechanism.


Asunto(s)
Aedes , Insecticidas , Animales , Resistencia a los Insecticidas , Mosquitos Vectores , Temefós
14.
J Dairy Res ; 87(3): 309-314, 2020 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-32958093

RESUMEN

Our objectives were to identify genes of the multi-drug efflux system and to evaluate the antimicrobial activities of polypyrrole nanoparticles (PPy-NPs) and aqueous extract of Moringa oleifera against Staphylococcus spp. isolated from dairy farms in Northeast Brazil. Initially, 162 Staphylococcus spp. isolates were subjected to in vitro antimicrobial sensitivity tests. Of these, 35 presented antimicrobial multi-drug resistance phenotypes. These 35 isolates were then referred for the detection of norA, norB, norC, msrA, mgrA, tet-38, and lmrS genes, all of which feature in multi-drug efflux systems. In the isolates carrying the genes, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of PPy-NPs and Moringa oleifera aqueous extract were determined. In the molecular analysis of the 35 isolates norA, norC, tet-38, and msrA genes were detected and for the other genes norB, lmrS and mgrA there was no amplification. Antimicrobial activity was verified of PPy-NPs and aqueous extract of Moringa oleifera in Staphylococcus spp. carrying multi-drug efflux system genes. We concluded that there are multi-drug efflux system genes present in the Staphylococcus spp. from the agricultural environment in Northeast Brazil, and that aqueous extract of Moringa oleifera and PPy-NPs show bactericidal activity against these isolates.


Asunto(s)
Antibacterianos/farmacología , Moringa oleifera/química , Nanopartículas/química , Extractos Vegetales/farmacología , Polímeros/química , Pirroles/química , Staphylococcus/efectos de los fármacos , Animales , Antibacterianos/química , Bovinos , Industria Lechera , Farmacorresistencia Bacteriana Múltiple , Regulación Bacteriana de la Expresión Génica/efectos de los fármacos , Extractos Vegetales/química , Staphylococcus/genética
15.
Microb Pathog ; 131: 150-157, 2019 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-30965089

RESUMEN

In this study, essential oil extracted from Syagrus coronata seeds (SCEO) was evaluated for antibacterial and antibiofilm activities against Staphylococcus aureus; in addition, Galleria mellonella model was used as an in vivo infection model. SCEO was mainly composed by fatty acids (89.79%) and sesquiterpenes (8.5%). The major components were octanoic acid, dodecanoic acid, decanoic acid and γ-eudesmol. SCEO showed bactericidal activity (minimal bactericidal concentration from 312 to 1250 µg/mL) against all tested S. aureus clinical isolates, which showed distinct biofilm-forming and multiple drug resistance phenotypes. SCEO weakly reduced biomass but remarkably decreased cell viability in pre-formed biofilms of S. aureus isolate UFPEDA-02 (ATCC-6538). Electron microscopy analysis showed that SCEO treatments decreased the number of bacterial cells (causing structural alterations) and lead to loss of the roughness in the multiple layers of the three-dimensional biofilm structure. In addition, overproduction of exopolymeric matrix was observed. SCEO at 31.2 mg/kg improved the survival of G. mellonela larvae inoculated with UFPEDA-02 isolate and reduced the bacterial load in hemolymph and melanization. In conclusion, SCEO is an antibacterial agent against S. aureus strains with different resistance phenotypes and able to disturb biofilm architecture. Our results show SCEO as a potential candidate to drug development.


Asunto(s)
Antibacterianos/farmacología , Arecaceae/química , Biopelículas/efectos de los fármacos , Lepidópteros/microbiología , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Staphylococcus/efectos de los fármacos , Animales , Antibacterianos/química , Biopelículas/crecimiento & desarrollo , Brasil , Modelos Animales de Enfermedad , Pruebas de Sensibilidad Microbiana , Viabilidad Microbiana/efectos de los fármacos , Aceites Volátiles/química , Extractos Vegetales/química , Semillas/química , Infecciones Estafilocócicas/tratamiento farmacológico , Infecciones Estafilocócicas/microbiología , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo
16.
Ecotoxicol Environ Saf ; 183: 109583, 2019 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-31446169

RESUMEN

Aedes aegypti control is a key component of the prophylaxis of dengue fever and other diseases. Moringa oleifera seeds contain a water-soluble lectin (WSMoL) with larvicidal and ovicidal activities against this insect. In this study, A. aegypti individuals were exposed at the third larval instar for 24 h to the water extract (0.1-1.0 mg/mL of protein) or lectin-rich fraction (0.05-0.6 mg/mL of protein) containing WSMoL, and then their survival and development were followed for 9 days post-exposure. The feeding capacity of adult females that developed from the treated larvae and the hatching success of eggs laid by them were also evaluated. Further, any alterations to the midgut histology of treated larvae, pupae, and adults were investigated. The extract and fraction induced the death of A. aegypti larvae along the post-exposure period. Both preparations also delayed the developmental cycle. The midguts of treated larvae and pupae showed disorganization and epithelial vacuolization, while in treated adults, the epithelium was underdeveloped compared to control. Unlike in control mosquitos, proliferating cells were not detected in treated larvae, and appeared in lower numbers in treated pupae than in control pupae. Adult females that developed from larvae treated with the fraction gained less weight after a blood meal compared with control. The amount of eggs laid by females that developed from larvae treated with both the extract and fraction was significantly lower than in control. In addition, the eggs showed lower hatching rates. In conclusion, females that developed from larvae treated with both the water extract and lectin-rich fraction showed reduced engorgement after a blood meal, with the consequent impairment of their fertility and fecundity. These results were probably due to the damage to midgut organization and impairment of the remodeling process during metamorphosis.


Asunto(s)
Aedes/efectos de los fármacos , Lectinas/farmacología , Moringa oleifera/química , Extractos Vegetales/farmacología , Aedes/crecimiento & desarrollo , Aedes/fisiología , Animales , Femenino , Fertilidad/efectos de los fármacos , Insecticidas/química , Insecticidas/farmacología , Intestinos/efectos de los fármacos , Intestinos/crecimiento & desarrollo , Intestinos/patología , Larva/efectos de los fármacos , Larva/crecimiento & desarrollo , Larva/fisiología , Lectinas/química , Control de Mosquitos , Extractos Vegetales/química , Pupa/efectos de los fármacos , Pupa/crecimiento & desarrollo , Pupa/fisiología , Semillas/química , Agua/química
17.
Ecotoxicol Environ Saf ; 169: 669-677, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30500736

RESUMEN

The increase in urbanization and industrialization has contributed to the contamination of different environments by means of xenobiotic compounds, such as heavy metals, causing changes in microbial communities. Among these metals, the Mercury (Hg2+) is one the most prevalent toxic metals for the environment The present study aimed to evaluate the effect of mercury on the formation of biofilm by environmental (collected from urban stream water) and clinical isolates of Klebsiella pneumoniae. In addition, antibiotic resistance, virulence factors, and genetic diversity were investigated. Taxonomic identity of eight isolates (one reference, two clinical, and five environmental isolates) was performed by MALDI-TOF-MS, while the antibiotic susceptibility profile was assessed by the disc diffusion method. The ability to form biofilms was evaluated by culture on Congo red agar and by crystal violet staining. Biofilm structure was analyzed by scanning electron microscopy. The hydrophobicity profile and the presence of the virulence genes cps, fimH, and mrkD was investigated. The presence of merA and its relationship with antimicrobial resistance were also assessed. The identity of all isolates was confirmed by MALDI-TOF-MS, and different profiles of resistance to mercury and antibiotics as well as of biofilm formation were identified for the clinical and environmental isolates. All isolates were hydrophilic and positive for the virulence genes cps, fimH, and mrkD; only the clinical isolate K36-A2 was positive for merA. The diversity of the isolates was confirmed by ERIC-PCR, which revealed high heterogeneity among the isolates. In conclusion, the data demonstrate that the investigated isolates present different responses to exposure to Hg2+ and correspond to distinct populations of K. pneumoniae disseminated in the investigated environment. The data obtained in this work will aid in understanding the mechanisms of survival of this pathogen under adverse conditions.


Asunto(s)
Biopelículas/efectos de los fármacos , Contaminantes Ambientales/toxicidad , Klebsiella pneumoniae/efectos de los fármacos , Mercurio/toxicidad , Antibacterianos/farmacología , Biopelículas/crecimiento & desarrollo , Farmacorresistencia Bacteriana/efectos de los fármacos , Farmacorresistencia Bacteriana/genética , Hospitales , Humanos , Klebsiella pneumoniae/genética , Klebsiella pneumoniae/patogenicidad , Pruebas de Sensibilidad Microbiana , Factores de Virulencia/genética
18.
An Acad Bras Cienc ; 91(1): e20190916, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30994765

RESUMEN

Currently, the research of new natural compounds with biological potential demonstrates great ethnopharmacological importance. In this study, we evaluated the biological properties promoted by saline extract from Malpighia emarginata DC leaves, whose objective is to evaluate the antioxidant, antimicrobial and cytotoxicity potential. Phytochemical characterization was performed by UPLC-MS chromatography to identify the chemical compounds. For the antioxidant potential, DPPH, ATT and FRAP methods were used. The antibacterial and antifungal tests were performed evaluating the MIC50, MIC90, CMB and CMF parameters. Moreover, antibiofilm action was evaluated. Cytotoxicity and proliferation were performed using splenocytes from Balb/c mice and were evaluated by cytometry. We found a list of phenolic compounds among other bioactive compounds in the M. emarginata saline extract. In addition, higher antioxidant profile and antifungal activity against different strains of Candida spp. was promoted by the saline extract. Splenocytes showed greater cell viability (more than 90%) and showed higher proliferate index in 24 and 48 hours of incubation with the extract. Saline extract from Malpighia emarginata DC has potential action like antioxidant and antifungal agent without promote animal cell damage.


Asunto(s)
Antifúngicos/química , Antioxidantes/química , Proliferación Celular/efectos de los fármacos , Malpighiaceae/química , Extractos Vegetales/química , Hojas de la Planta/química , Polifenoles/química , Animales , Antifúngicos/farmacología , Antioxidantes/farmacología , Candida/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión/métodos , Femenino , Flavonoides/química , Ratones Endogámicos BALB C , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología , Polifenoles/farmacología , Valores de Referencia , Bazo/citología , Factores de Tiempo
19.
Microb Pathog ; 124: 152-162, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30142463

RESUMEN

The Alpinia purpurata inflorescence contains a lectin (ApuL), which has immunomodulatory activities on human cells. In the present work, it was evaluated the antibacterial and antifungal effects of ApuL against human pathogens. ApuL showed bacteriostatic activity against non-resistant (UFPEDA-02) and an oxacillin-resistant isolate (UFPEDA-672) of Staphylococcus aureus with minimal inhibitory concentrations (MIC50) of 50 and 400 µg/mL, respectively. In addition, it showed bactericidal effect on the non-resistant isolate (minimal bactericidal concentration: 200 µg/mL). For Candida albicans and Candida parapsilosis, ApuL showed fungistatic effect (MIC50: 200 and 400 µg/mL, respectively). The lectin was able to impair the viability of the microorganism cells, as indicated by propidium iodide (PI) staining. Analysis of growth curves, protein leakage, and ultrastructural changes supported that ApuL acts through distinct mechanisms on S. aureus isolates. Ultrastructural analysis of ApuL-treated Candida cells revealed malformations with elongations and bulges. ApuL-oxacillin combination showed synergistic effect on the oxacillin-resistant isolates UFPEDA-670 and 671, which were not sensitive to lectin alone. Synergism was also detected for ApuL-ceftazidime against a multidrug-resistant isolate of Pseudomonas aeruginosa. Synergistic action of ApuL-fluconazole was detected for C. parapsilosis, which was insensitive to the drug alone. Biofilm formation by S. aureus non-resistant isolate and C. albicans was remarkably inhibited by ApuL at sub-inhibitory concentrations. In conclusion, ApuL showed differential effects on non-resistant and resistant bacterial isolates, was active against Candida species, and showed synergistic action in combination with antibiotics.


Asunto(s)
Alpinia/química , Antibacterianos/farmacología , Antifúngicos/farmacología , Biopelículas/efectos de los fármacos , Candida albicans/efectos de los fármacos , Lectinas/farmacología , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/aislamiento & purificación , Antifúngicos/aislamiento & purificación , Candida albicans/crecimiento & desarrollo , Candida albicans/fisiología , Sinergismo Farmacológico , Lectinas/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Staphylococcus aureus/crecimiento & desarrollo , Staphylococcus aureus/fisiología
20.
Regul Toxicol Pharmacol ; 95: 289-297, 2018 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-29626561

RESUMEN

People broadly use medicinal plants although their safety and efficacy are often neglected. Several Cactaceae plants are used for medicinal purposes, but Pilosocereus gounellei (xique-xique) has been little studied for their pharmacological properties. In this study, a saline extract from Pilosocereus gounellei stem was evaluated for acute toxicity, effects on motor function, and antinociceptive activity in mice. Thin-layer chromatography and high-performance liquid chromatography revealed the presence of flavonoids and reducing sugars. No death of mice was noted with oral treatments at 2000 and 5000 mg/kg. Body weight gain, food intake, and water consumption were not affected with treatment at 2000 mg/kg. The number of segmented leukocytes was higher in the treated mice than in control, and reduced serum levels of cholesterol and triglycerides were detected after both extract treatments. No histological alterations in the liver, heart, lung, kidney, and spleen were detected. Open field and rotarod tests showed that the extract did not affect motor function and exploratory activity. Antinociceptive activity was detected in acetic acid-induced writhing, tail-immersion, and formalin tests, indicating interference with both non-inflammatory and inflammatory pain. In conclusion, the P. gounellei extract has antinociceptive activity in mice without showing toxicity and altering motor coordination.


Asunto(s)
Analgésicos/uso terapéutico , Cactaceae , Dolor/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Ácido Acético , Analgésicos/toxicidad , Animales , Artemia/efectos de los fármacos , Colesterol/sangre , Femenino , Formaldehído , Calor/efectos adversos , Masculino , Ratones , Dolor/etiología , Extractos Vegetales/toxicidad , Tallos de la Planta/química , Desempeño Psicomotor/efectos de los fármacos , Cloruro de Sodio/química , Triglicéridos/sangre
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