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1.
Pharm Dev Technol ; 27(8): 892-903, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36168940

RESUMO

Glioblastomas are tumors that present a high mortality rate. Artemether (ART) is a lactone with antitumor properties, demonstrating low bioavailability and water solubility. In the present study, we developed lipid-core nanocapsules (LNC) containing pequi oil (Caryocar brasiliense Cambess) as the oily core for ART-loaded LNCs (LNCART) and evaluated their effect on human glioblastoma cells (U-87 MG). LNCs were developed by interfacial deposition of a preformed polymer, followed by physicochemical characterization. LNCART revealed a diameter of 0.216 µm, polydispersity index of 0.161, zeta potential of -12.0 mV, and a pH of 5.53. Furthermore, mitochondrial viability, proliferation, total antioxidant status, and antioxidant enzyme activity were evaluated. ART reduced cell viability after 24 h and proliferation after 48 h of treatment at concentrations equal to or above 40 µg . mL-1. LNCART, at 1.25 µg . mL-1, reduced these parameters after 24 h of treatment. Furthermore, superoxide dismutase (SOD) activity was elevated, while glutathione reductase (GR) activity was reduced. These findings suggest that ART loaded into LNC may be a promising alternative to improve its pharmacological action and possible application as a therapeutic agent for glioblastoma.


Assuntos
Glioblastoma , Nanocápsulas , Humanos , Nanocápsulas/química , Antioxidantes/farmacologia , Artemeter , Sobrevivência Celular , Glioblastoma/tratamento farmacológico , Lipídeos/química , Polímeros
2.
J Environ Sci Health B ; 57(3): 211-219, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35240941

RESUMO

We evaluated the biological effects of ingestion by gavage, for 28 days, of the pesticides cypermethrin (CP) and emamectin benzoate (EB) and their mixtures in female Swiss mice. The groups were Control (water); CP; EB and three distinct concentrations of CP and EB mixture expressed in mg/kg/day. The biological effects were analyzed in the complete blood count and plasma (alkaline phosphatase (ALP), alanine aminotransferase (ALT) and creatinine); the biochemical parameters of oxidative stress (substances reactive to thiobarbituric acid (TBARS); reduced glutathione (GSH); catalase (CAT), superoxide dismutase (SOD) and glutathione-S-transferase (GST)), and bone marrow cells obtained from the femur for the micronucleus (MN) test. In the heart, there was a reduction in GSH in the groups (0.5 + 0.67 and 2.5 + 3.37), although in the brain this effect appeared for the other groups, except EB. Brain TBARS increased in CP and in the group (2.5 + 3.37) and platelets increased in the group (12.5 + 16.87). Genotoxic/mutagenic effects, showing a consistent increase dose-dependent effect on micronucleus counting for in the female mice. After 28 days of treatment, we can observe that the pesticide mixtures promoted genotoxic damage and oxidative brain damage in female mice, which can damage the health of these animals and possibly their future offspring.


Assuntos
Mutagênicos , Praguicidas , Animais , Antioxidantes/metabolismo , Benzoatos/farmacologia , Catalase/metabolismo , Dissacarídeos , Feminino , Glutationa/metabolismo , Glutationa Transferase/genética , Glutationa Transferase/metabolismo , Ivermectina/análogos & derivados , Fígado , Camundongos , Estresse Oxidativo , Praguicidas/toxicidade , Piretrinas , Superóxido Dismutase/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico
3.
J Environ Sci Health B ; 57(2): 153-163, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35275045

RESUMO

This study evaluated the long-term effect of biochar application on the sorption and desorption of thiamethoxam in a Haplic Plinthosol. The experiment was conducted in a randomized block design with combination of doses of mineral fertilizer NPK (0 and 300 kg·ha-1 formula 05-25-15) and biochar (0, 16 and 32 Mg ha-1). Deformed soil samples were collected in the field from the 0-0.10 m layer of all plots to determine the sorption and desorption of the thiamethoxam insecticide in the soil; fulvic acid (FA), humic acid (AH) and humin (HUM) carbon contents; and total organic carbon. The Batch slurry method was used to evaluate sorption and desorption. The Freundlich isotherm adequately described thiamethoxam sorption in all treatments. The application of biochar increased the sorption (Kfs) and decreased the desorption (Kfd) of thiamethoxam. The sorption intensity (1/n) showed reduction characteristics as the soil concentration of thiamethoxam increased. Biochar has a sorption effect on the soil through covalent bonds and H-bonds with the insecticide molecules, thereby indirectly increasing the sorption potential in the chemical fractions of the organic matter of soil. The application of 32 Mg ha-1 of biochar significantly reduced thiamethoxam in the soil solution. Altogether, the present study reveals that biochar application in soil is a promising tool for mitigating the contaminant potential of thiamethoxam in subsurface waters.


Assuntos
Inseticidas , Poluentes do Solo , Adsorção , Carbono/química , Carvão Vegetal/química , Solo/química , Poluentes do Solo/análise , Tiametoxam
4.
Ecotoxicol Environ Saf ; 106: 181-7, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-24840881

RESUMO

The aim of this study was to investigate the effects of acute glyphosate (active ingredient) exposure on the oxidative stress biomarkers and antioxidant defenses of a hybrid surubim (Pseudoplatystoma sp). The fish were exposed to different herbicide concentrations for 96 h. The thiobarbituric acid-reactive substances (TBARS), protein carbonyls and antioxidant responses were verified. The 15 mg a.pL(-1) of herbicide resulted in the death of 50% of the fish after 96 h. An increase in liver and muscle TBARS levels was observed when fish were exposed to the herbicide. The protein carbonyl content was also increased in the liver (4.5mg a.pL(-1) concentration) and brain (2.25 mg a.pL(-1) concentration). The antioxidant activities decreased in the liver and brain after exposure to herbicide. Levels of ascorbic acid in the liver (2.25 mg a.pL(-1) and 4.5 mg a.pL(-1) concentrations) and brain (2.25 mg a.pL(-1) concentration) were increased post-treatment. Levels of total thiols were increased in the liver and brain (2.25 mg L(-1) and 7.5mg a.pL(-1), respectively). Glyphosate exposure, at the tested concentrations affects surubim health by promoting changes that can affect their survival in natural environment. Some parameters as TBARS and protein carbonyl could be early biomarkers for Roundup exposure in this fish species.


Assuntos
Peixes-Gato/fisiologia , Glicina/análogos & derivados , Herbicidas/toxicidade , Fígado/efeitos dos fármacos , Músculos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Poluentes Químicos da Água/toxicidade , Animais , Ácido Ascórbico/análise , Biomarcadores/metabolismo , Glicina/toxicidade , Fígado/química , Fígado/metabolismo , Músculos/química , Músculos/metabolismo , Oxirredução , Carbonilação Proteica , Substâncias Reativas com Ácido Tiobarbitúrico/análise , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Glifosato
5.
Molecules ; 19(10): 16039-57, 2014 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-25299821

RESUMO

Caesalpinia ferrea Martius has traditionally been used in Brazil for many medicinal purposes, such as the treatment of bronchitis, diabetes and wounds. Despite its use as a medicinal plant, there is still no data regarding the genotoxic effect of the stem bark. This present work aims to assess the qualitative and quantitative profiles of the ethanolic extract from the stem bark of C. ferrea and to evaluate its mutagenic activity, using a Salmonella/microsome assay for this species. As a result, a total of twenty compounds were identified by Flow Injection Analysis Electrospray Ionization Ion Trap Mass Spectrometry (FIA-ESI-IT-MS/MSn) in the ethanolic extract from the stem bark of C. ferrea. Hydrolyzable tannins predominated, principally gallic acid derivatives. The HPLC-DAD method was developed for rapid quantification of six gallic acid compounds and ellagic acid derivatives. C. ferrea is widely used in Brazil, and the absence of any mutagenic effect in the Salmonella/microsome assay is important for pharmacological purposes and the safe use of this plant.


Assuntos
Caesalpinia/química , Mutagênicos/química , Mutagênicos/farmacologia , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Caules de Planta/química , Estrutura Molecular
6.
Toxicon ; 218: 57-65, 2022 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-36113683

RESUMO

Rhinella marina toad is abundant in Brazil. Its poison contains cardiac glycosides called bufadienolides, which are extensively investigated for their bioactivity. Our aim was to characterize the vasoactivity of Rhinella marina poison (RmP) on the aorta of male Wistar rats. For this, the RmP was first collected and processed to obtain an alcoholic extract. To determine cardiovascular effects of RmP, we performed in vivo tests by administering RmP intravenously in doses of 0.1-0.8 mg/kg. Vascular reactivity was also performed through concentration-response curves to RmP (10 ng/mL to 200 µg/mL) in aortic segments with and without endothelium. RmP induced a concentration-dependent contraction in rat aorta which was partly endothelium-mediated. Nitric oxide contributes with this response in view that incubation with L-NAME increased the contractile response. Additionally, treatment with indomethacin [cyclooxygenase, (COX) inhibitor], nifedipine (L-type voltage-gated calcium channels blocker), and BQ-123 (ETA receptors antagonist) decreased maximum response, and ketanserin (5-HT2 receptors antagonist) decreased pEC50, suggesting active participation of these pathways in the contractile response. On the other hand, apocynin (NADPH oxidase inhibitor) did not alter contractility. Incubation with prazosin (α1-adrenergic receptor antagonist) abolished the contractile response, suggesting that the RmP-induced contraction is dependent on the adrenergic pathway. In the Na+/K+ ATPase protocol, a higher Emax was observed in the RmP experimental group, suggesting that RmP potentiated Na+/K+ATPase hyperpolarizing response. When this extract was injected (i.v.) in vivo, increase in blood pressure and decrease in heart rate were observed. The results were immediate and transitory, and occurred in a dose-dependent manner. Overall, these data suggest that the poison extract of R. marina toad has an important vasoconstrictor action and subsequent vasopressor effects, and its use can be investigated to some cardiovascular disorders.


Assuntos
Bufanolídeos , Venenos , Adenosina Trifosfatases/metabolismo , Adenosina Trifosfatases/farmacologia , Adrenérgicos/farmacologia , Antagonistas Adrenérgicos/farmacologia , Animais , Bufanolídeos/toxicidade , Bufo marinus/metabolismo , Canais de Cálcio , Endotélio Vascular , Hemodinâmica , Indometacina/farmacologia , Ketanserina/farmacologia , Masculino , Metanol/farmacologia , NADPH Oxidases , NG-Nitroarginina Metil Éster , Nifedipino/farmacologia , Óxido Nítrico/metabolismo , Prazosina/farmacologia , Prostaglandina-Endoperóxido Sintases/metabolismo , Ratos , Ratos Wistar , Serotonina/farmacologia , Vasoconstritores
7.
Toxicon ; 182: 30-33, 2020 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-32387184

RESUMO

The secreted poisonin bufonids (Anura: Bufonidae) include proteins, biogenic amines, toxic bufadienolides and alkaloids. The chemical composition of the methanolic extract of parotoid gland secretions by the Amazonian toad Rhinella margaritifera was evaluated in a UFLC-DAD-micrOTOF system. Of the twenty three compounds found in the methanolic extract, eighteen were identified by the mass/charge ratio as: five arginine diacids, six bufagenins (telocinobufagin, marinobufagin, bufotalin, cinobufotalin, bufalin and cinobufagin), six bufotoxins, and an alkaloid (dehydrobufotenin).


Assuntos
Bufanolídeos/química , Bufonidae , Glândula Parótida/metabolismo , Venenos de Anfíbios , Animais , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão
8.
Toxicon ; 179: 101-106, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32209334

RESUMO

Amphibian cutaneous secretion has great potential for bioprospection and is a great tool in the development of bioproducts. Thus, the objective of the present work was to evaluate the comparative study of the chemical profile parotoid gland secretions from Rhaebo guttatus collected in two distinct regions of the Brazilian Amazon. For this, the chemical composition of six methanolic extracts of this species were analyzed by Liquid Chromatography in UV and MS Detection Ultra-Chromatography Systems (UFLC-DAD-micrOTOF). All obtained chromatograms presented two distinct regions; one referring to the more hydrophilic molecules (alkaloids), while the other refers to the more hydrophobic compounds (steroids). The steroid region resembles all samples, regardless of where they were collected. In the alkaloid region, there was a standardized variation for the samples from the southern Brazilian Amazon, but the same was not true for the samples collected in the Amazon-Cerrado transition region. Thus, the data suggest that the environment and diet of R. guttatus may be important in alkaloid production, but do not influence steroid content. These results add new information about the poison of the toad R. guttatus and raises new questions to be further investigated, thus contributing to the knowledge of the anuran fauna of the Brazilian Amazon.


Assuntos
Bufonidae/metabolismo , Glândula Parótida/metabolismo , Alcaloides , Animais , Brasil , Pele , Esteroides
9.
Eur J Pharm Sci ; 150: 105356, 2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-32389834

RESUMO

Cutaneous lesions lead to complications in patients, since they may be recurrent and also represent risk of progression to infection and/or amputation. Therefore, effective, protective, and topical treatments of easy application and removal need to be developed to provide effective alternatives to patients. The Caryocar brasiliense Cambess (CBC) presents important pharmacological activities and proved in the healing process. This paper reports the improvement of the CBC nanostructured (LNCCBC and LNCCBC+) activity in dermal wounds in vivo. The oil was physico-chemically characterized and used in the development of lipid-core nanocapsules (LNCs), coated (LNCCBC+) or without chitosan (LNCCBC), in concentration of 1.0 mg mL-1. Hydrogel (HG) was tested in vivo on lesions in the back of male Wistar rats for 14 days. The oil presented appropriate physico-chemical characteristics for its use, such as moisture 0.76 %, acidity 0.85 % and oleic acid 25.90 %. The LNCs showed nanometric size (around 200 nm), monomodal distribution, slight acid pH and zeta potential of + 22.1 mV in accordance with the composition. The nanostructured oil induced dermal healing in vivo showing significantly better improvement than free oil. LNCCBC+ showed best results showing the higher increase of the production of type 1 collagen, an important protein to the healing repair. These results suggest that development of formulations LNCCBC and LNCCBC+ are promising and important alternative for the treatment of dermal wounds, avoiding complications related to cutaneous lesions.


Assuntos
Hidrogéis/administração & dosagem , Malpighiales , Nanocápsulas/administração & dosagem , Óleos de Plantas/administração & dosagem , Pele/efeitos dos fármacos , Cicatrização/efeitos dos fármacos , Animais , Colágeno Tipo I/metabolismo , Liberação Controlada de Fármacos , Frutas , Hidrogéis/química , Lipídeos/administração & dosagem , Lipídeos/química , Masculino , Nanocápsulas/química , Óleos de Plantas/química , Polímeros/administração & dosagem , Polímeros/química , Ratos Wistar , Pele/lesões , Pele/metabolismo
10.
Artigo em Inglês | LILACS | ID: biblio-1532938

RESUMO

Aims: it was evaluated the antioxidant effect of the ethanolic extract of Caesal-pinia ferrea bark in a model of oxidative stress induced by paracetamol (PCM). Methods: male Swiss mice were subdivided into four groups (control; PCM; PCM+extract; extract; n=8) in which a dose of paracetamol (250 mg.kg-1) was administered and after 3 hours the treatment with the extract (100 mg.kg-1/day) was administered for seven days, via gavage. Oxidative stress biomarkers were determined, such as catalase, glutathione-S-transferase, reduced gluta-thione, ascorbic acid, thiobarbituric acid reactive substances and carbonylated proteins of liver, kidneys and brain and plasma parameters through the dosage of glucose, cholesterol, triglycerides, aspartate aminotransferase and alanine aminotransferase. Results: the Caesalpinia ferrea extract was able to reverse the lipid and protein damage caused by the drug in the liver tissue and caused the same effect in the renal and brain tissues in the carbonylated proteins. The extract alone decreased liver glutathione-S-transferase and increased catalase and brain glutathione-S-transferase activity, in addition to lowering glucose and cholesterol, but without altering the triglycerides. Conclusions: it was possible to conclude that the ethanolic extract of the bark of Caesalpinia ferrea has a good antioxidant activity, probably due to dose of paracetamol in the samples investigated. However, more studies are needed for a better understanding of the effects of this extract compared to the effects found in this research


Objetivos: foi avaliado o efeito antioxidante do extrato etanólico da casca de Caesalpinia ferrea em modelo de estresse oxidativo induzido por paracetamol (acetaminofeno, PCM). Métodos: camundongos Swiss machos foram subdivididos em quatro grupos (controle; PCM; PCM+extrato; extrato; n=8) nos quais foi administrada uma dose de paracetamol (250 mg.kg-1) e após três horas foi administrado o tratamento com o extrato (100 mg.kg-1/ dia) por sete dias, via gavagem. Foram determinados biomarcadores de estresse oxidativo, como catalase, glutationa-S-transferase, glutationa reduzida, ácido ascórbico, substâncias reativas ao ácido tiobarbitúrico e proteínas carboniladas do fígado, rins e cérebro, além de parâmetros plasmáticos através da dosagem de glicose, colesterol, triglicerídeos, aspartato aminotransferase e alanina aminotransferase. Resultados: o extrato de Caesalpinia ferrea foi capaz de reverter os danos lipídicos e proteicos causados pela droga no tecido hepático, e também causou o mesmo efeito nos tecidos renal e cerebral nas proteínas carboniladas. O extrato sozinho diminuiu a atividade da glutationa-S-transferase hepática e aumentou a da catalase e glutationa-S-transferase cerebral, além de diminuir a glicose e o colesterol, mas sem alterar os triglicerídeos. Conclusões: foi possível concluir que o extrato etanólico da casca de Caesalpinia ferrea apresenta uma boa atividade antioxidante, provavelmente devido à presença de taninos, tendo em vista os danos causados pela alta dose de paracetamol nas amostras investigadas. Entretanto, mais estudos são necessários para um melhor entendimento dos efeitos deste extrato frente aos efeitos encontrados nesta pesquisa


Assuntos
Animais , Bioquímica , Estresse Oxidativo , Caesalpinia , Extratos Vegetais , Acetaminofen
11.
Environ Sci Pollut Res Int ; 25(25): 25383-25389, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29951755

RESUMO

The toxicity of Roundup Original® (GLY), a glyphosate-based herbicide widely used in crops in Mato Grosso state, was determined in hybrid fish jundiara or pintado da Amazônia. The 96 h-LC50 of GLY was 13.57 mg L-1. Moreover, exposure to sublethal concentrations of GLY (0, 0.37, 0.75, 2.25, 4.5, 7.5 mg L-1) has not altered the survival rate (100% for all treatments). In fish liver, protein carbonyl (PC) levels as well as glutathione-S-transferase (GST) activity, reduced glutathione (GSH), and ascorbic acid (ASA) contents increased when compared to control group. Superoxide dismutase (SOD) activity was reduced and catalase (CAT) has not changed. PC content has grown in muscle and brain, and thiobarbituric acid-reactive species (TBARS) levels also increased in muscle, but in the brain, they remained unaltered. Acetylcholinesterase (AChE) activity reduced in muscle but increased in brain when compared to control group. Our results suggest that short-term exposure to GLY induced alterations in the oxidative stress biomarkers in fish and can be interfering with their survival in natural environment; besides, these findings may be considered of high ecotoxicological relevance.


Assuntos
Encéfalo/efeitos dos fármacos , Peixes-Gato/crescimento & desenvolvimento , Glicina/análogos & derivados , Herbicidas/toxicidade , Fígado/efeitos dos fármacos , Músculos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Acetilcolinesterase/metabolismo , Animais , Ácido Ascórbico/metabolismo , Biomarcadores/metabolismo , Encéfalo/metabolismo , Catalase/metabolismo , Peixes-Gato/metabolismo , Glicina/toxicidade , Fígado/metabolismo , Músculos/metabolismo , Carbonilação Proteica/efeitos dos fármacos , Superóxido Dismutase/metabolismo , Tiobarbitúricos , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Glifosato
12.
Chemosphere ; 185: 445-451, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28711796

RESUMO

The aim of this study was to investigate the effects of Roundup Original®, a glyphosate-based herbicide, against biochemical parameters including thiobarbituric acid-reactive substances (TBARS), protein carbonyl, enzymatic and nonenzymatic antioxidant responses and acetylcholinesterase (AChE) of jundiara fish (Leiarius marmoratus × Pseudoplatystoma reticulatum) at a sublethal concentration of 1.357 mg L-1. Fish exposed to the herbicide for different periods (6-96 h) showed a significant increase of both hepatic and muscular TBARS and protein carbonyl. Enzymatic antioxidant activity was decreased in the liver and brain after 48 h of exposure. Glutathione-S-tranferase (GST) had its levels raised in the brain and gills, probably as a toxicity event response. Non protein thiols (GSH) demonstrated a reduction after 6 and 24 h of exposure in the hepatic tissue, followed by an increase at 48 and 96 h in the same tissue. GSH brain levels, however, increased only after 96 h. AChE activity in muscle decreased for all the times tested (26.5, 45, 38 and 14% for 6, 24, 48 and 96 h respectively), but only at 96 h (34%) in the brain. We found that Roundup Original® is able to trigger important changes in the biochemical parameters tested, showing it can be a potential threat for the health and survival of fish in the environment.


Assuntos
Peixes-Gato/metabolismo , Herbicidas/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Acetilcolinesterase/metabolismo , Animais , Antioxidantes/metabolismo , Brânquias/metabolismo , Glicina/análogos & derivados , Fígado/metabolismo , Músculos/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Glifosato
13.
Environ Toxicol Pharmacol ; 56: 241-248, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29031220

RESUMO

Roundup Original® is an herbicide widely used in Mato Grosso's agriculture and it may contamine water bodies, being an unforeseen xenobiotic to aquatic organisms, particularly fish. This study investigated the effects on the hybrid fish jundiara (Leiarius marmoratus×Pseudoplatystoma reticulatum) of an environmentally relevant exposure to this herbicide. Glucose levels in liver, muscle and plasma decreased after exposure to 1.357mgL-1 of Roundup Original® (glyphosate nominal concentration), while glycogen levels reduced in liver and muscle for different times. Elevated cholesterol and triglycerides revealed an adaptive response. Protein and lactate levels also increased during the experiment, however no changes were observed for muscle lactate. Increment of the transaminases suggests damage to the liver cells. After 96hours of exposure, reductions in all hematological parameters were observed, whereas the micronucleus test findings showed genotoxic scenery. Histological analysis did not display pathological alterations of the hepatic tissue. The results obtained provide valuable data for noticing the effects of pollutants on non-target organisms.


Assuntos
Peixes/genética , Peixes/metabolismo , Glucose/metabolismo , Glicina/análogos & derivados , Herbicidas/toxicidade , Animais , Dano ao DNA , Monitoramento Ambiental , Proteínas de Peixes/metabolismo , Peixes/sangue , Regulação da Expressão Gênica/efeitos dos fármacos , Glicina/toxicidade , Ácido Láctico/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Músculos/efeitos dos fármacos , Músculos/metabolismo , Testes de Mutagenicidade , Poluentes Químicos da Água/toxicidade , Glifosato
14.
Biosci. j. (Online) ; 37: e37070, Jan.-Dec. 2021. ilus, tab, graf
Artigo em Inglês | LILACS | ID: biblio-1361398

RESUMO

Paracetamol (PCM) is a drug widely used by the population as an antipyretic and analgesic. If administered in high doses it can cause liver damage, leading to hepatoxicity. The genus Smilax, found in temperate and tropical regions, is traditionally used by the population through the extract of leaves and roots for several conditions, such as in the treatment of syphilis, diabetes, asthma and as a diuretic action. Through this, Smilax fluminensis leaf extracts were used to evaluate the protective effect against oxidative stress induced by a high dose of PCM in mice that received the drug and after receiving treatment with crude extract and fractions. Plasma analysis was performed using as partate aminotransferase (AST), alanine aminotransferase (ALT), glucose, triglycerides and cholesterol, in addition to biochemical techniques such as catalase (CAT), glutathione-S-transferase (GST), reduced glutathione (GSH), ascorbic acid (ASA), substances reactive to thiobarbituric acid (TBARS) and carbonylated proteins (CARBONYL) of liver, brain and kidneys. Fraction 1 of the extract was the most promising, decreasing the plasma levels of AST and ALT, the levels of CAT and GST of the liver, together with GSH and in the renal and brain tissue there was a decrease in carbonylated proteins (PCM + F1 versus PCM ). Besides, fraction 1 proved to be hypoglycemic and hypocholesterolemic. It is concluded that fraction 1 of Smilax fluminensis leaves has good antioxidant activity in the face of the damage caused by the high dose of paracetamol.


Assuntos
Smilax , Acetaminofen/toxicidade
15.
Sci. med. (Porto Alegre, Online) ; 30(1): e-34860, 2020.
Artigo em Inglês | LILACS | ID: biblio-1087374

RESUMO

Aims: The objective of this study was to identify the phytochemical profile and to evaluate the biological effects of the crude ethanolic extract (EE) and the ethanolic fraction (EF) of leaves of the species Cissus spinosa Cambess, after oxidative stress induced by cyclophosphamide (CP) in mice. Methods: Phytochemical profile was performed detecting functional groups and, analysis of total flavonoids and phenols concentration, as well as the antiradical activity in EE and EF. The phytochemical characterization was done for the identification of flavonoids present in the leaves of the plant. In the biochemical tests, hematological parameters, glucose, total cholesterol, creatinine, alkaline phosphatase and aminotransferases dosages in plasma, enzymatic and non--enzymatic antioxidants and lipid damage marker were evaluated in different tissues (liver, kidney and heart), besides genotoxic and immunological analyzes. The animals received 15 days of treatment, via gavage, with EE (50 mg kg-1) or EF (50 mg kg-1) and on the 15th day, an intraperitoneal injection of CP (100 mg kg-1) or saline (0.9%). After 24 h the last treatment, the animals were anesthetized for blood withdrawal, sacrificed and removal of the organs. Results: In the phytochemical analyzes, the presence of alkaloids, flavonoids and phenols was identified, the latter presented a higher concentration for EF. Eight flavonoids were identified - Rutin, Quercetin-3-ß-D-glucoside, Quercitrin, Taxifolin, Quercetin, Canferol, Luteolin and Apigenin. In the biochemical analyzes, in general, EE showed a better antioxidant action against oxidative damages, hypoglycemic and antitilipemic action when comparing with EF, probably due to the synergism caused by flavonoids. It was observed the reduction and an increase of micronucleated polychromatic erythrocytes, due to the action of antioxidant compounds and alkaloids present in the plant, also considering the question of the seasonal period that directly interferes in the production of these compounds. In the immunological analysis, the extracts did not stimulate the spontaneous production of oxygen peroxide (H2 O2) and nitric oxide (NO•). Conclusions: Other studies, such as the variation of the chemical composition of the plant by local seasonality, hypoglycemic and antilipemic action, should be carried out to better delineate the biological action present in this plant.


Objetivos: O objetivo deste estudo foi identificar o perfil fitoquímico e avaliar os efeitos biológicos do extrato etanólico bruto (EE) e da fração etanólica (EF) das folhas da espécie Cissus spinosa Cambess, após estresse oxidativo induzido pela ciclofosfamida. (CP) em camundongos. Métodos: O perfil fitoquímico foi realizado detectando grupos funcionais e, análise da concentração de flavonoides e fenóis totais, bem como a atividade antirradical em EE e EF. A caracterização fitoquímica foi realizada para a identificação de flavonoides presentes nas folhas da planta. Nos testes bioquímicos, os parâmetros hematológicos, as dosagens de glicose, colesterol total, creatinina, fosfatase alcalina e aminotransferases no plasma, os antioxidantes enzimáticos e não enzimáticos e o marcador de dano lipídico foram avaliados em diferentes tecidos (fígado, rim e coração), além de análises genotóxicas e imunológicas. Os animais receberam 15 dias de tratamento, via gavagem, com EE (50 mg kg-1) ou EF (50 mg kg-1) e no 15º dia, injeção intraperitoneal de CP (100 mg kg-1) ou soro fisiológico (0,9%) . Após 24 h do último tratamento, os animais foram anestesiados para retirada do sangue, sacrificados e após a retirada dos órgãos. Resultados: Nas análises fitoquímicas, identificou-se a presença de alcaloides, flavonoides e fenóis, estes últimos apresentaram maior concentração para EF. Oito flavonoides foram identificados - rutina, quercetina-3-ß--D-glicosídeo, quercitrina, taxifolina, quercetina, canferol, luteolina e apigenina. Nas análises bioquímicas, em geral, o EE apresentou melhor ação antioxidante contra os danos oxidativos, ação hipoglicemiante e antitilipêmica quando comparada à EF, provavelmente devido ao sinergismo causado pelos flavonoides. Observou-se a redução e um aumento de eritrócitos policromáticos micronucleados, devido à ação de compostos antioxidantes e alcaloides presentes na planta, considerando também a questão do período sazonal que interfere diretamente na produção desses compostos. Na análise imunológica, os extratos não estimularam a produção espontânea de peróxido de oxigênio (H2O2) e óxido nítrico (NO•). Conclusões: Outros estudos, como a variação da composição química da planta por sazonalidade local, ação hipoglicemiante e antilipêmica, devem ser realizados para melhor delineamento da ação biológica presente nesta planta.


Assuntos
Compostos Fitoquímicos , Fitoterapia , Flavonoides , Estresse Oxidativo
16.
Artigo em Inglês | LILACS | ID: biblio-1117416

RESUMO

AIMS: This study aimed to investigate the effects of crude extract of Carica papaya leaves on oxidative stress in mice induced by cyclophosphamide, as well as phytochemical profile characterization of this extract. METHODS: The male Swiss mice received 15 days of treatment with the extract (500 mg kg-1, via gavage) and intraperitoneal injection of cyclophosphamide (75 mg kg-1) or saline (0.9%) on the 15th day. After 24 h the last treatment, the animals were anesthetized for blood withdrawal, sacrificed and removal of the organs for analyses (liver, kidney and heart). In the biochemical tests were determined: hematological parameters in blood, aminotransferases, alkaline phosphatase, glucose and total cholesterol dosages in plasma, enzymatic and non-enzymatic antioxidants and lipid damage marker were evaluated in different tissues, besides genotoxic and histopathological analyzes. RESULTS: In the extract of Carica papaya leaves, the flavonoids quercetin-3ß-D-glucoside and rutin were identified, besides present positive results for alkaloids, saponins and tannins. This extract increased the activity of glutathione-S-transferase and catalase enzymes in the liver and reduced the levels of reduced glutathione in the kidneys and hematocrit levels, red cell count, and hemoglobin. It promoted the decrease of the reactive species of thiobarbituric acid (TBARS) in the kidneys and the activity of enzyme aspartate aminotransferase in the plasma and was antimutagenic in the micronucleus test. CONCLUSIONS: The study showed that extract of Carica papaya was beneficial against oxidative events and prevented DNA damage. The extract also showed hepatotoxicity, therefore prolonged infusion of papaya leaves is not advisable.


OBJETIVOS: O objetivo deste estudo foi investigar os efeitos do extrato bruto de folhas de Carica papaya sobre o estresse oxidativo em camundongos induzidos pela ciclofosfamida, bem como a caracterização do perfil fitoquímico deste extrato. MÉTODOS: Os camundongos Swiss machos receberam 15 dias de tratamento com o extrato (500 mg kg-1, via gavagem) e injeção intraperitoneal de ciclofos-famida (75 mg kg-1) ou salina (0,9%) no 15º dia. Após 24 h do último tratamento, os animais foram anestesiados para retirada do sangue, sacrificados e retirada dos órgãos para análises (fígado, rim e coração). Nos testes bioquímicos foram determinados: parâmetros hematológicos em sangue, aminotransferases, fosfatase alcalina, dosagens de glicose e colesterol total no plasma, antioxidantes enzimáticos e não enzimáticos e marcador de dano lipídico foram avaliados em diferentes tecidos, além de análises genotóxicas e histopatológicas. RESULTADOS: No extrato de folhas de Carica papaya foram identificados os flavonoides quercetina-3ß-D-glicosídeo e rutina, além de resultados positivos para alcaloides, saponinas e taninos. Este extrato aumentou a atividade das enzimas glutationa-S-transferase e catalase no fígado e diminuiu os níveis de glutationa reduzida nos rins, a concentração do hematócrito, a contagem dos glóbulos vermelhos e a hemoglobina. Promoveu a diminuição das espécies reativas de ácido tiobarbitúrico (TBARS) nos rins, a atividade da enzima aspartato aminotransferase no plasma e foi antimuta-gênico no teste do micronúcleo. CONCLUSÕES: O estudo mostrou que o extrato de Carica papaya foi benéfico contra eventos oxidativos e preveniu danos no DNA. O extrato também mostrou hepatotoxicidade, portanto, a infusão prolongada de folhas de mamão não é aconselhável.


Assuntos
Estresse Oxidativo , Farmacologia , Etnobotânica , Ciclofosfamida , Carica , Metabolismo
17.
Acta amaz ; 49(1): 41-47, jan. - mar. 2019.
Artigo em Inglês | LILACS | ID: biblio-1119222

RESUMO

Copaifera multijuga, commonly known as copaiba, is popularly used in the form of tea for various conditions due to the presence of antioxidant substances in its composition, which protect cells against damage caused by free radicals. Its oleoresin is also used as an anti-inflammatory and antitumoral agent. The present study investigated the antioxidant effect of the ethanolic extract of copaiba stem bark on Swiss mice inoculated with solid Ehrlich tumors. Mice were inoculated subcutaneously with 1x106 Ehrlich's tumor cells and treated via gavage with ethanolic extract of copaiba for thirty days, with doses varying between 100 and 200 mg kg-1. Biochemical analyses of enzymatic antioxidants [superoxide dismutase (SOD), catalase (CAT), glutathione-S-transferase (GST)], non-enzymatic antioxidants [reduced glutathione (GSH) and ascorbic acid (ASA)], substances reactive to thiobarbituric acid (TBARS) and protein carbonylation (carbonyl) in different tissues were significantly affected. The extract administered at 200 mg kg-1 presented higher antioxidant capacity in the liver, increased CAT, GST, GSH and decreased TBARS, as well as increased CAT activity and protein carbonylation in brain tissue. The results showed that the copaiba extract was able to reverse the oxidative stress caused by solid Ehrlich tumor, probably due to the presence of antioxidant compounds, and had potential antineoplasic effect after a 30-day treatment. (AU)


Assuntos
Estresse Oxidativo , Radicais Livres , Fabaceae , Neoplasias , Antineoplásicos
18.
Sci. med. (Porto Alegre, Online) ; 29(1): ID32408, 2019.
Artigo em Inglês | LILACS | ID: biblio-1009912

RESUMO

AIMS: Copaifera multijuga Hayne oleoresin is commonly used in traditional medicine owing to its anti-inflammatory, antiseptic, antitumor, and antibacterial properties. However, little is known about the effect of the compounds from the bark of this plant. In this study, the immunomodulatory effect of the ethanolic extract of C. multijuga bark via natural killer activity of non-adherent spleen cells of Ehrlich tumor-bearing mice was evaluated. METHODS: Male Swiss mice were inoculated subcutaneously with 1×106 Ehrlich tumor cells (Ehrlich and Ehrlich/C. multijuga group) or phosphate buffered saline solution (control group and C. multijuga group) and treated orally daily with C. multijuga extract (200 mg kg-1, 0.1 mL per mouse, for the Ehrlich/C. multijuga and C. multijuga groups) or phosphate buffered saline solution (control group and Ehrlich group). The four experimental groups consisted in eight mice each and were organized in two sets, one treated for seven days and another treated for 14 days, totalizing 64 mice throughout the experiment. Twenty-four hours after the last oral administration, the mice were euthanized and the spleen tissue was isolated to prepare a non-adherent spleen cell suspension and to evaluate natural killer activity. Data are presented as the cell lysis percentage of Yac.1 target cells by non-adherent spleen cells. RESULTS: Treatment for seven days increased natural killer activity in the Ehrlich/C. multijuga group (21.20±8.89, p<0.05) compared to the control group (3.14±2.71, p<0.05); however, this effect was not maintained in the groups treated for 14 days (Control: 6.02±6.98, Ehrlich: 4.82±7.72, C. multijuga: 2.07±2.10, Ehrlich/C. multijuga: 2.01±1.63, p>0.05). CONCLUSIONS: Treatment for seven days with an ethanolic extract of C. multijuga bark enhanced the natural killer activity of non-adherent spleen cells from Ehrlich tumor-bearing mice.


OBJETIVOS: O óleo-resina de Copaifera multijuga Hayne é popularmente utilizado na medicina tradicional por suas propriedades antiinflamatória, antisséptica, antitumoral e antibacteriana. Entretanto, há poucos estudos sobre o efeito dos compostos obtidos da casca da planta. Assim, o objetivo deste trabalho foi avaliar o efeito imunomodulador do extrato etanólico da casca da C. multijuga na atividade natural killer das células esplênicas não aderentes de animais portadores do tumor de Ehrlich. MÉTODOS: Camundongos Swiss machos foram inoculados subcutaneamente com 1×106 células do tumor de Ehrlich (grupo Ehrlich e Ehrlich/C. multijuga) ou com solução salina tamponada (grupo controle e C. multijuga) e tratados diariamente (gavagem) com extrato de C. multijuga (200 mg kg-1, 0,1mL cada um, para os grupos Ehrlich/C. multijuga e C. multijuga) ou com solução salina tamponada (grupo controle e grupo Ehrlich). Os quatro grupos experimentais consistiram de oito animais cada e foram organizados em dois conjuntos, um tratado por sete dias e outro tratado por 14 dias, totalizando 64 animais durante todo o experimento. Após 24 horas do término do tratamento, os animais foram eutanasiados para obtenção da suspensão de células esplênicas não aderentes e avaliação da atividade natural killer. Os resultados são apresentados como porcentagem da lise celular das células alvo Yac.1 pelas células esplênicas não aderentes. RESULTADOS: A análise dos resultados demonstrou que aos sete dias de tratamento a C. multijuga aumentou a atividade natural killer no grupo Ehrlich/C. multijuga (21,20±8,89, p<0,05) em comparação ao grupo controle (3,14±2,71, p<0,05), entretanto tal efeito não foi mantido nos grupos tratados por 14 dias (Controle: 6,02±6,98; EHR: 4,82±7,72; C. multijuga: 2,07±2,10; EHR/C. multijuga: 2,01±1,63, p>0,05). CONCLUSÕES: Os resultados demonstraram que o tratamento com o extrato etanólico da casca de C. multijuga favoreceu a atividade natural killer das células esplênicas não aderentes dos animais portadores do tumor de Ehrlich apenas aos sete dias de tratamento.


Assuntos
Carcinoma de Ehrlich , Células Matadoras Naturais , Fabaceae , Medicina , Neoplasias
19.
Biosci. j. (Online) ; 34(5): 1298-1307, sept./oct. 2018.
Artigo em Inglês | LILACS | ID: biblio-967319

RESUMO

Research has indicated the antifungal activity of ethanol extracts from propolis (EEP) on fungi of the genera Phakopsora, Colletotrichum, and Cercospora. Here, chemical compositions and antioxidant activity of three EEP (propolis from Scaptotrigona polysticta stingless bee and two types produced by Apis mellifera - red and brown) were evaluated and their action against Aspergillus flavus was investigated. Ash, dry extract, total phenolic and total flavonoid contents were determined. Phenolic composition was evaluated by high performance liquid chromatography, with using the following reference substances: gallic acid, caffeic acid, -coumaric acid, ferulic acid, quercetin, kaempferol, and apigenin. Tests on mycelial growth, sporulation, and germination of spores were performed to assess the biological activity of the EEP on A. flavus. All EEP showed low dry extract content (<11%) with adequate amounts of ash (<5%). The red EEP (Apis mellifera) showed the highest contents of total phenolic and total flavonoid (5.38 and 2.77 g 100 g-1), while the highest recorded antioxidant activity was exhibited by brown EEP (92.9%). The EEP of S. polysticta presented higher levels of -coumaric acid (10.99 mg g-1), while red and brown extracts from A. mellifera stood out with the highest levels of quercetin (27.26 mg g-1) and gallic acid (5.88 mg g-1), respectively. No extract was effective in inhibiting mycelial growth and sporulation of A. flavus, but red EEP inhibited spore germination. On the basis of these results, it is suggested that the inhibitory effect of red EEP on spore germination may be associated with increased levels of flavonoids found in it as compared with the other extracts investigated here.


Outros estudos apontaram a ação antifúngica dos extratos etanólicos de própolis (EEP) sobre fungos do gênero Phakopsora, Colletotrichum e Cercospora. Neste estudo, avaliou-se a composição química e a atividade antioxidante de três EEP (própolis produzido pela abelha sem ferrão Scaptotrigona polysticta e dois tipos de própolis produzida pela Apis melífera: marrom e vermelha) e sua ação contra o Aspergillus flavus. Foram determinados os teores de cinzas, extrato seco, fenólicos e flavonoides totais nos EEP. A composição fenólica foi determinada por cromatografia líquida de alta eficiência, empregando-se as seguintes substâncias de referência: ácido gálico, ácido p-cumárico, ácido ferrúlico, quercitina, kaempferol e apigenina. Para avaliar a atividade biológica dos EEP sobre A. flavus foram realizados os testes de crescimento micelial, esporulação e germinação de esporos. Todos os EEP apresentaram baixos teores de extrato seco (< 11%), porém quantidades de cinzas adequadas (< 5%). O EEP vermelha apresentou os maiores teores de fenólicos e flavonoides totais (5,38 e 2,77 g 100g-1), enquanto que a maior atividade antioxidante registrada foi do EEP marrom (92,9%). O EEP de S. polysticta apresentou maiores teores de ácido p-cumárico (10,99 mg g-1), enquanto que os de A. mellifera, vermelha e marrom, destacaram-se com os maiores níveis de quercetina (27,26 mg g-1) e de ácido gálico (5,88 mg g-1), respectivamente. Nenhum extrato foi eficaz na inibição do crescimento micelial e esporulação de A. flavus, porém observou-se inibição na germinação de esporos pelo EEP vermelha. Sugere-se que o efeito inibitório na germinação de esporos pode estar relacionado com os maiores níveis de flavonoides encontrados na própolis vermelha, quando comparado com os outros extratos investigados.


Assuntos
Própole , Aspergillus flavus , Abelhas , Germinação , Compostos Fenólicos , Fungos , Esporos , Flavonoides
20.
Acta amaz ; 48(4): 338-346, Oct.-Dec. 2018. tab, graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1455374

RESUMO

Capirona decorticans (Rubiaceae) is popularly used to treat warts, wounds, mycoses and scabies, and is also a component of the Ayahuasca tea. Despite its popular use, the phytochemical and pharmacological research on this species is limited. Therefore, this work quantified phenolic compounds in the ethanolic extract (EE) and hydromethanolic fraction (FM) (406, 293 mgEAG g-1, respectively) from leaves of C. decorticans. We identified flavonoids by LC-MS/MS-MMR-ESI (apigenin, rutin, luteolin, miricetin, quercetin, quercetin-3--D-glucoside, quercetrin), and evaluated oxidative stress and mutagenic/antimutagenic effect of EE and FM through an in vivo experiment using Swiss mice and cyclophosphamide (CP) as an inducer of DNA damage and oxidative stress. Mice were pretreated for 15 consecutive days with EE or FM (250 mg kg-1) and then intraperitoneally injected with CP (25 mg kg-1). Carbonylated proteins, ascorbic acid, catalase and thiobarbituric acid-reactive substances were measured in hepatic and renal tissues. The mutagenic/antimutagenic effect was evaluated through the Micronucleus Test. Protein carbonylation in the liver of animals exposed to CP was reduced by FM. There was no significant effect on other markers of oxidative stress. The groups treated with the extracts showed a significant percentage reduction (EE = 96% and FM = 71%) in the frequency of micronucleated polychromatic erythrocytes induced by CP. EE showed mutagenicity when used alone. The EE and FM of C. decorticans leaves showed antioxidant potential equivalent to that observed in other species, did not cause oxidative stress, nor toxicity, and had a protective and antimutagenic effect, although the EE showed signs of mutagenicity.


Capirona decorticans (Rubiaceae) é popularmente usada para tratar verrugas, feridas, micoses e sarna, e como um componente do chá de Ayahuasca. Apesar do uso popular, são limitadas as pesquisas fitoquímicas e farmacológicas sobre a espécie. Portanto, este estudo quantificou compostos fenólicos no extrato etanólico (EE) e na fração hidrometanólica (FM) (406 e 293 mgEAG g-1, respectivamente) de folhas de C. decorticans. Identificamos flavonoides por LC-MS / MS-MMR-ESI (apigenina, rutina, luteolina, miricetina, quercetina, quercetina-3--D-glicosídeo, quercetrina), e avaliamos o estresse oxidativo e o efeito mutagênico/antimutagênico de EE e FM em um experimento in vivo utilizando camundongos Swiss e ciclofosfamida (CP) como um indutor de danos no DNA e estresse oxidativo. Os camundongos foram pré-tratados por 15 dias consecutivos com EE ou FM (250 mg kg-1) e injetados intraperitonealmente com CP (25 mg kg-1). Proteínas carboniladas, ácido ascórbico, catalase e substâncias reativas ao ácido tiobarbitúrico foram dosadas em tecidos hepáticos e renais. O efeito mutagênico/antimutagênico foi avaliado através do Teste de Micronúcleo. Houve carbonilação protéica no fígado de animais expostos à CP, que foi reduzida pela FM. Não houve efeito significativo sobre outros marcadores de estresse oxidativo. Os grupos tratados com os extratos apresentaram uma redução percentual significativa (EE = 96% e FM = 71%) na frequência de eritrócitos policromáticos micronucleados induzidos pela PC. O EE também apresentou mutagenicidade quando utilizado isoladamente. O EE e FM das folhas de C. decorticans apresentaram potencial antioxidante equivalente ao observado em outras espécies, não causaram estresse oxidativo, nem toxicidade, e tiveram efeito protetor e antimutagênico, embora a EE tenha apresentado mutagenicidade.


Assuntos
Masculino , Animais , Camundongos , Compostos Fenólicos/análise , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Rubiaceae/química , Ciclofosfamida/administração & dosagem , Ciclofosfamida/efeitos adversos , Estresse Oxidativo , Modelos Animais
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