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1.
Andrologia ; 53(6): e14047, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33756034

RESUMO

Ethanol consumption is a risk factor of male infertility. The use of medicinal plants offers an alternative for the treatment of male infertility in developing countries. This study aimed to evaluate the Rourea coccinea effect on ethanol-induced male infertility in Wistar rats. Twenty-five (25) male Wistar rats were randomised into five groups of five rats and treated by oesophageal gavage over a 28-day period. Group 1 (negative control) received distilled water; Group 2 (positive control) received 30% ethanol at 7 mg/kg body weight; Group 3 (reference control) received 30% ethanol co-treated with the reference drug, clomiphene citrate; Groups 4 and 5 (test groups) received 30% ethanol co-treated with Rourea coccinea hydro-ethanolic extract at 200 and 400 mg/kg respectively. Testosterone hormone, sperm parameters and testicular histopathology were evaluated. Ethanol treatment induced a significant reduction (p < .05) in sperm count, motility, viability and a significant increase in sperm abnormalities because of the significant decrease (p < .05) in testosterone levels. These data correlate with the alterations observed in the seminiferous tubule on histopathological examination of the testes. However, co-treatment of ethanol with Rourea coccinea extract or the reference drug restored the ethanol-induced toxic effects on the reproductive organs, sperm profile and testosterone level.


Assuntos
Connaraceae , Infertilidade Masculina , Animais , Etanol/toxicidade , Humanos , Infertilidade Masculina/induzido quimicamente , Infertilidade Masculina/tratamento farmacológico , Masculino , Extratos Vegetais , Ratos , Ratos Wistar , Contagem de Espermatozoides , Motilidade Espermática , Espermatozoides , Testículo , Testosterona
2.
PLoS One ; 15(11): e0241855, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33156835

RESUMO

Leishmaniasis is a disease impacting public health worldwide due to its high incidence, morbidity and mortality. Available treatments are costly, lengthy and toxic, not to mention the problem of parasite resistance. The development of alternative treatments is warranted and natural products demonstrate promising activity. This study investigated the activity of Connarus suberosus extracts and compounds against Leishmania species. Several C. suberosus extracts were tested against L. amazonensis promastigotes. Active and inactive extracts were analyzed by UHPLC-MS and data evaluated using a metabolomics platform, revealing an unknown neoflavonoid (connarin, 3), isolated together with the pterocarpans: hemileiocarpin (1) and leiocarpin (2). The aforementioned compounds (1-3), together with the benzoquinones: rapanone (4), embelin (5) and suberonone (6) previously isolated by our group from the same species, were tested against: (i) L. amazonensis and L. infantum promastigotes, and (ii) L. amazonensis intracellular amastigotes, with the most active compound (3) also tested against L. infantum amastigotes. Cytotoxicity against murine peritoneal macrophages was also investigated. Compounds 2 and 3 presented an IC50 33.8 µM and 11.4 µM for L. amazonensis promastigotes; and 44.3 µM and 13.3 µM for L. infantum promastigotes, respectively. For L. amazonensis amastigotes, the IC50 of 2 was 20.4 µM with a selectivity index (SI) of 5.7, while the IC50 of 3 was 2.9 µM with an SI of 6.3. For L. infantum amastigotes, the IC50 of 3 was 7.7 µM. Compounds 2 and 3 presented activity comparable with the miltefosine positive control, with compound 3 found to be 2-4 times more active than the positive control, depending on the Leishmania species and form. The extracts and isolated compounds showed moderate toxicity against macrophages. Compounds 2 and 3 altered the mitochondrial membrane potential (ΔΨm) and neutral lipid body accumulation, while 2 also impacted plasma membrane permeabilization, culminating in cellular disorder and parasite death. Transmission electron microscopy of L. amazonensis promastigotes treated with compound 3 confirmed the presence of lipid bodies. Leiocarpin (2) and connarin (3) demonstrated antileishmanial activity. This study provides knowledge of natural products with antileishmanial activity, paving the way for prototype development to fight this neglected tropical disease.


Assuntos
Connaraceae/química , Flavonoides/farmacologia , Metabolômica/métodos , Extratos Vegetais/farmacologia , Animais , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Antiprotozoários/farmacologia , Sobrevivência Celular , Cromatografia Líquida de Alta Pressão , Flavonoides/química , Flavonoides/isolamento & purificação , Leishmania mexicana/efeitos dos fármacos , Leishmania mexicana/crescimento & desenvolvimento , Macrófagos Peritoneais/citologia , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/parasitologia , Espectrometria de Massas , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
3.
J Ovarian Res ; 13(1): 83, 2020 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-32693841

RESUMO

BACKGROUND: Ovarian cancer (OvCa) is one of the most lethal tumors of gynecologic malignancies, due to lack of early detection, and a high rate of metastasis. The standard treatment for OvCa is surgery and cytotoxic chemotherapy. However, to overcome the high cost and side effects of these treatments, medicinal plants are widely used in developing countries to treat OvCa. Byrsocarpus coccineus plant preparation has been administered to patients traditionally in the management of tumors in Nigeria. In this study, we investigated the anti-proliferative effects of B. coccineus ethanol leaf extract against OVCAR-3 and SW 626 OvCa cell lines. After the treatment of the two cell lines with the extracts, analyses were carried out to determine inhibition of proliferation and expression of cell cycle markers, pro-apoptotic, and anti-apoptotic markers. RESULTS: Results showed that B. coccineus ethanol leaf extract, significantly inhibited cell migration and colony formation in OVCAR-3 and SW 626 treated cells in a dose-dependent manner. Results also show that B. coccineus ethanol leaf extract modulated the expression of tumor suppressor gene (p53), cell cycle progression, pro- and anti-apoptotic gene, and the pro-inflammatory cytokines. CONCLUSIONS: These results suggest that B. coccineus have anti-proliferative properties and could induce apoptosis. Further investigation will be carried out to isolate bioactive compounds for the treatment of ovarian cancer.


Assuntos
Proliferação de Células/efeitos dos fármacos , Connaraceae/química , Neoplasias Ovarianas/tratamento farmacológico , Extratos Vegetais/farmacologia , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Citocinas/metabolismo , Feminino , Humanos , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Neoplasias Ovarianas/metabolismo , Folhas de Planta/química
4.
J Ethnopharmacol ; 261: 112980, 2020 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-32422354

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: An interdisciplinary scientific investigation of biologically active agents is fundamental to search for natural substances with therapeutic action. This review collected the most relevant information on traditional knowledge related to the use of plants of the Connaraceae family. This work is the first to compile all the published ethnobotanical, chemical, pharmacological, and toxicological information about this important plant family. AIM OF THE STUDY: Our objective was to provide the scientific community with an up-to-date overview of the pharmacological potential of Connaraceae species. MATERIAL AND METHODS: We searched NCBI Pubmed Central, Google Scholar, Scientific Electronic Library Online (SciELO), ScienceDirect, SciFinder, and Scopus databases to review the research on ethnobotanical, chemical, pharmacognostical, pharmacological, and toxicological studies with Connaraceaes. Books that address the theme were also included. DISCUSSION AND CONCLUSION: The literature review indicated that 39 species of Connaraceaes have pharmacological potentiality. Ethnobotany reports listed 36 of the 39 species discussed. Pharmacognostical studies have been conducted with 23 species and isolates, and chemical compounds have been identified for only 15 species. At least one study has been published concerning the pharmacological activities for 20 of the 39 species analyzed. For Agelaea pentagyna, Cnestis ferruginea, Connars suberosus, and Rourea minor, pharmacological activity experiments were performed using isolated compounds, which have the highest current pharmacological potential. Studies employing a toxicological approach cover only 10 of the 39 Connaraceaes species. Thus, scientific community should conduct much more research for a broader understanding of this plant family.


Assuntos
Connaraceae , Etnobotânica , Etnofarmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Connaraceae/química , Connaraceae/classificação , Connaraceae/toxicidade , Humanos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Especificidade da Espécie
5.
J Ethnopharmacol ; 243: 112117, 2019 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-31351192

RESUMO

ETHNOPHARMACOLOGY RELEVANCE: the root decoction of Cnestis ferruginea Vahl ex DC (Connaraceae) is widely used in traditional African medicine for the treatment of various ailments including pain, inflammation and epilepsy. We have earlier reported anticonvulsant effect of Cnestis ferruginea root extract in mice. AIM OF THE STUDY: to evaluate the effect of ethanolic root extract of Cnestis ferruginea (CF) on kainic acid (KA)-induced temporal lobe epilepsy (TLE) in mice as well as the involvement of inflammatory mediators and oxidative stress. MATERIALS AND METHODS: mice were randomly divided into preventive treatment (vehicle (normal saline) or CF (400 mg/kg, p.o.) for 3 consecutive days before KA (5 mg/kg, i.p.) on days 4 and 5. In the reversal model, KA (5 mg/kg, i.p.) was administered on days 1 and 2 before vehicle or CF (400 mg/kg) administration on days 3-5. The effect of treatments on seizure severity was recorded using Racine scale. Animals were euthanized on day 5, 6 h after last KA exposure in preventive model and 1 h after CF administration in reversal model to estimate markers of oxidative stress and neuroinflammation. RESULTS: exposure of mice to KA induced TLE evidenced in increased severity of seizures which was significantly reduced by the pre- and post-treatment of mice with CF. Moreso, KA-induced malondialdehyde/nitrite generation and GSH deficit in the brain were attenuated by CF treatments. KA-induced up-regulation of inflammatory transcription factors; cyclooxygenase-2 (COX-2) and nuclear facor-kappaB (NF-κB) in the CA1, CA2, CA3 and dentate gyrus (DG) regions of the hippocampus regions were attenuated by CF treatments. CONCLUSION: findings from this study showed that Cnestis ferruginea root extract ameliorated KA-induced TLE through enhancement of antioxidant defense mechanism and attenuation of neuro-inflammatory transcription factors. Thus, could possibly be a potential phytotherapeutic agent in the management of temporal lobe epilepsy.


Assuntos
Anticonvulsivantes/uso terapêutico , Connaraceae , Epilepsia do Lobo Temporal/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Convulsões/tratamento farmacológico , Animais , Anticonvulsivantes/farmacologia , Ciclo-Oxigenase 2/metabolismo , Epilepsia do Lobo Temporal/induzido quimicamente , Epilepsia do Lobo Temporal/metabolismo , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Ácido Caínico , Masculino , Medicina Tradicional Africana , Camundongos , NF-kappa B/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Raízes de Plantas , Convulsões/induzido quimicamente , Convulsões/metabolismo
6.
Niger J Physiol Sci ; 34(2): 201-206, 2019 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-32343271

RESUMO

Diabetes mellitus is a devastating illness associated with alterations in the pancreatic islet of Langerhans and the islet volume constitutes a significant variable in diabetic investigations. This study investigates the volume of pancreatic islets in type 2 diabetic rats following treatment with aqueous extract Byrsocarpus coccineus leaves. Twenty-five male Wistar rats weighing between 100-120g were divided into five groups. Group 1 served as the normal control given distilled water while type 2 diabetes mellitus was induced by a high fat diet feeding for five weeks and a single dose of streptozotocin (35mg/kg, i.p.) in groups 2,3,4 and 5. After confirmation of diabetes, animals in groups 2,3,4 and 5 were administered normal saline, 50 mg/kg metformin, 800 mg/kg Byrsocarpus coccineus leaves leaf extract (BCLE) and 400 mg/kg BCLE respectively for 21 days. The pancreas was harvested, fixed in neutral buffered formalin and processed for stereological and histological analysis. Isotropic uniform random samples were obtained with the orientator grid. Serial sections were cut with a rotatory microtome and stained with Haematoxylin and Eosin. Pancreatic islet volumes were measured with the aid of a Cavalieri estimator grid. The result showed significant (p<0.05) increase in the blood glucose level of the diabetic control group, when compared to the normal control. But blood glucose levels from groups 4 and 5 were significantly (p<0.05) decreased when compared to the diabetic control. Pancreatic islet volume estimations showed a significant decrease in the diabetic control group when compared to the normal control (p<0.05), while pancreatic islet volumes in groups 3, 4 and 5 were significantly increased when compared to the diabetic control group (p<0.05). In a likewise manner the histology of the pancreas of the diabetic control shows damaged pancreatic islet cells and surrounding tissue that was reduced in all the treated group. In conclusion the aqueous extract of Byrsocarpus coccineus has shown an anti- hyperglycaemic effect in the experimental rats and increased the volumes of the pancreatic islet cells as well as ameliorated the pathological changes in the pancreas.


Assuntos
Connaraceae , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Ilhotas Pancreáticas/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Animais , Glicemia/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Masculino , Fitoterapia , Extratos Vegetais/farmacologia , Ratos Wistar
7.
Am J Bot ; 104(5): 685-693, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28500228

RESUMO

PREMISE OF THE STUDY: Permineralized wood is common in the Miocene beds exposed during the expansion of the Panama Canal. We describe a stem with the distinctive anatomy of a liana and evaluate the evolutionary, biogeographic, and ecological significance of this discovery. METHODS: The object of the study was obtained from a collection of fossil woods and fruits from a locality in the lower Miocene Cucaracha Formation, where the formation is exposed by the Culebra Cut of the Panama Canal. Thin sections were prepared using the cellulose acetate peel technique and examined using transmitted light microscopy. We described the anatomy and compared it with that of extant and fossil species. We also reviewed and evaluated published reports of fossils attributed to Connaraceae. KEY RESULTS: The anatomy of this fossil wood matches the genus Rourea (Connaraceae). The stem is only 1 cm in diameter, but vessels >200 µm in diameter also occur, indicating the perennial climbing habit. We evaluated 12 other pre-Quaternary occurrences attributed to Connaraceae. Four are accepted, three are rejected, and we consider five unknown or uncertain. CONCLUSIONS: The discovery of this Rourea stem confirms the presence of Connaraceae in the Neotropics by the early Miocene, provides the oldest evidence of the climbing habit in the family, and contributes to our understanding of the flora of Panama 19 mya. Although the fossil record of Connaraceae is sparse, reliable occurrences span three continents and indicate that the family originated as early as the Late Cretaceous-Paleocene and was widespread by the early Miocene.


Assuntos
Evolução Biológica , Connaraceae/classificação , Filogenia , Fósseis , Panamá , Caules de Planta
8.
Biomed Pharmacother ; 83: 340-348, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27399811

RESUMO

We have earlier reported antidepressant-like effect of Cnestis ferruginea and its bioflavonoid constituent, amentoflavone in behavioural paradigms but its effects on neurochemical and neuroendocrine systems are yet to be elucidated. This study sought to investigate the effect of subchronic treatment of C. ferruginea (CF) on monoamines system, hypothalamo-pituitary adrenal axis and nitrosative/oxidative stresses. Male albino rats (150-200g) randomly divided into seven groups; Group I: vehicle treated (0.2%v/v Tween 80 in normal saline (10ml/kg; p.o.; unstressed), Group II: vehicle treated+restraint stress, Group III: imipramine (20mg/kg; p.o.), Group IV-VI: CF (12.5, 50, or 100mg/kg; p.o., respectively), Group VII: CF 6.25+imipramine 5mg/kg. One hour post-treatment, animals were subjected to 20min restraint stress and 6min, forced swim test (FST) for a period of 14 days. CF (12.5, 50 and 100mg/kg) produced significant reduction in immobility time and an increase in climbing behaviour. CF attenuated repeated restraint stress×FST-induced serum corticosterone [F(6,28)=5.45,P<0.01]. Exposure of rats to FST+restraint stress paradigms produced significant (P<0.05) increase in malondialdehyde and nitrite level, also reduced the glutathione level and superoxide dismutase activity which was reversed by subchronic treatment of rats with CF. Restraint stress×FST significantly decreased NA, DA and 5-HT concentrations, with increased DA and 5-HT turnover ratios in discrete brain regions which was ameliorated by CF or imipramine subchronic treatment. These results suggest that the antidepressant-like effect of C. ferruginea involved enhancement of monoamines and antioxidant as well as normalization of neuroendocrine systems.


Assuntos
Antidepressivos/farmacologia , Antioxidantes/metabolismo , Monoaminas Biogênicas/metabolismo , Connaraceae/química , Sistemas Neurossecretores/metabolismo , Extratos Vegetais/farmacologia , Animais , Corticosterona/sangue , Masculino , Metaboloma/efeitos dos fármacos , Sistemas Neurossecretores/efeitos dos fármacos , Neurotransmissores/metabolismo , Nitrosação , Estresse Oxidativo/efeitos dos fármacos , Raízes de Plantas/química , Ratos Sprague-Dawley , Natação/fisiologia
9.
J Ethnopharmacol ; 183: 166-175, 2016 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-26940897

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The plant species Connarus favosus is used in folk medicine in the west of Pará state, Brazil, to treat snakebites. AIM OF THE STUDY: To investigate the potential of the aqueous extract of Connarus favosus (AECf) to inhibit hemorrhagic and phospholipase A2 activities induced by Bothrops atrox venom (BaV) and to determine the antioxidant and antimicrobial potentials of the extract. MATERIALS AND METHODS: AECf was analyzed phytochemically for phenolics (condensed tannins and hydrolyzable tannins) by colorimetry. Antioxidant activity was evaluated by quantitative assays using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and Fe(3+)/phenanthroline. Antimicrobial activity was evaluated by the minimal inhibitory concentration test, and cytotoxicity was evaluated using human fibroblast cells (MRC-5). Inhibition of BaV-induced hemorrhagic activity was assessed after oral administration of the extract using pre-treatment, post-treatment and combined (BA plus AECf) treatment protocols. Inhibition of indirect hemolysis caused by phospholipase A2 (PLA2) was investigated in vitro. Interaction between AECf and BaV was investigated by SDS-PAGE electrophoresis, Western blot (Wb) and zymography. RESULTS: The phytochemical profile of AECf revealed ten secondary metabolite classes, and colorimetry showed high total phenolic and total (condensed and hydrolyzable) tannin content. AECf exhibited high antioxidant and antimicrobial potentials. The IC50 for the cytotoxic effect was 51.91 (46.86-57.50)µg/mL. Inhibition of BaV-induced hemorrhagic activity was significant in all the protocols, and inhibition of PLA2 activity was significant with the two highest concentrations. The BaV/AECf mixture produced the same bands as BaV by itself in SDS-PAGE and Wb although the bands were much fainter. Zymography confirmed the proteolytic activity of BaV, but when the venom was pre-incubated with AECf this activity was blocked. CONCLUSION: AECf was effective in reducing BaV-induced hemorrhagic activity when administered by the same route as that used in folk medicine and exhibited antioxidant and antimicrobial potentials.


Assuntos
Antibacterianos/farmacologia , Antivenenos/farmacologia , Connaraceae/química , Venenos de Crotalídeos/administração & dosagem , Hemorragia/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Antibacterianos/química , Antioxidantes/farmacologia , Antivenenos/química , Bothrops , Brasil , Feminino , Hemorragia/metabolismo , Masculino , Medicina Tradicional/métodos , Camundongos , Fosfolipases A2/metabolismo , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Mordeduras de Serpentes/tratamento farmacológico , Taninos/metabolismo
10.
Drug Res (Stuttg) ; 66(5): 235-45, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-26789652

RESUMO

BACKGROUND: We have previously reported antidepressant effect of Cnestis ferruginea (CF) in behavioral models of depression. Due to the promise shown by this extract, this study was carried out to investigate the contribution of monoaminergic, cholinergic and nitrergic systems to the antidepressant-like effect elicited by CF. METHODS: Male albino mice were pretreated with monoaminergic or cholinergic receptor antagonists, L-arginine or N(G)-nitro-L-arginine (nitric oxide synthase inhibitor) (at doses reported to block the in vivo effect of the agonists), 15 min before oral administration of CF (100 mg/kg), 1 h later, the forced swim test (FST) in mice was carried out. RESULTS: CF treatment produced significant changes in the duration of swimming (F(5,42)=9.86, P<0.001), climbing behaviour (F(5,42)=4.51, P=0.004) and mean time spent immobile (F(5,42)=11.55, P<0.001) vs. vehicle-treated control. Co-administration of CF with fluoxetine or imipramine potentiated their effect. However, pretreatment of mice with reserpine (F(1,16)=119.20, P<0.001), prazosin (F(1,16)=68.98, P<0.001), sulpiride (F(1,16)=15.46, P<0.01), RS 127445 ((F(1,20)=8.22, P<0.01), SB 399885 ((F(1,20)=38.44, P<0.001), atropine (F(1,16)=53.77, P<0.001), or L-arginine (nitric oxide precursor) (F(1,16)=10.35, P<0.01) prevented CF-induced antidepressant-like effect in mice. In addition, pretreatment of mice with L-NNA (10 mg/kg) augmented the effect of CF. CONCLUSION: C. ferruginea exerts its antidepressant-like action through interaction with α-adrenoceptor, dopamine D2, 5-HT2B, 5-HT6 and muscarinic cholinergi1c receptors as well as L-arginine-nitric oxide systems. C. ferruginea could be used as adjuvant with conventional antidepressants in the treatment of major depressive disorder.


Assuntos
Antidepressivos/farmacologia , Connaraceae/química , Depressão/tratamento farmacológico , Medicina Tradicional Africana/métodos , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Antidepressivos/uso terapêutico , Arginina/metabolismo , Arginina/farmacologia , Comportamento Animal/efeitos dos fármacos , Antagonistas Colinérgicos/farmacologia , Modelos Animais de Doenças , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Nigéria , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase/antagonistas & inibidores , Nitroarginina/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Sprague-Dawley , Receptores Colinérgicos/metabolismo , Natação
11.
Nutrition ; 30(6): 713-8, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-24800671

RESUMO

OBJECTIVES: The aim of this study was to evaluate the flavonoid content of an ethanolic leaf extract from the medicinal plant Rourea induta Planch. (RIEE) and to investigate its hepatoprotective potential and in vivo antioxidant effects. METHODS: Using samples from carbon tetrachloride-treated Wistar female rats treated orally with or without RIEE, we evaluated the aspartate aminotransferase, alanine aminotransferase, and total bilirubin levels in plasma; the levels of the hepatic oxidative stress markers catalase, superoxide dismutase, glutathione peroxidase, and reduced glutathione in liver homogenates; and the thiobarbituric acid reactive substance levels. A histopathology study was performed. A quantitative analysis of the RIEE extract was performed using high-performance liquid chromatography to evaluate its flavonoid content. RESULTS: Oral administration of RIEE significantly reduced carbon tetrachloride-induced elevations in the levels of plasma markers of hepatic damage and lipid peroxidation. It also rescued histopathologic alterations observed in the liver and levels of oxidative stress markers. CONCLUSIONS: RIEE exhibits antioxidant and hepatoprotective activities in vivo, which may be attributable to its flavonoids composition [hyperin (2), quercetin-3-O-ß-xyloside (4), quercetin-3-O-α-arabinofuranoside (5), and quercetin (6)].


Assuntos
Antioxidantes/farmacologia , Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Connaraceae/química , Extratos Vegetais/farmacologia , Alanina Transaminase/sangue , Animais , Antioxidantes/química , Aspartato Aminotransferases/sangue , Bilirrubina/sangue , Catalase/metabolismo , Feminino , Flavonoides/química , Flavonoides/farmacologia , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Folhas de Planta/química , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo
12.
J Ethnopharmacol ; 153(3): 801-9, 2014 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-24680990

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Rourea induta Planch. is a small tree or shrub growing wild in Brazil and belonging to the Connaraceae family. It is used for the treatment of Chagas disease and as antirheumatic in folk medicine. This study was designed to investigate the antinociceptive activity of the aqueous extract (AERi) of Rourea induta leaves in rodents, as well as isolate and identify components that can be responsible for its effect. MATERIAL AND METHODS: The antinociceptive effect of orally administered AERi was evaluated in behavioral models of acute (formalin) and chronic [complete Freund׳s adjuvant (CFA)] pain in mice. We also investigated the possible involvement of opioid receptors and proinflammatory cytokines (interleukin-1ß and tumor necrosis factor-α) in the antinociceptive effect of the AERi. In addition, a nonspecific effect of AERi was evaluated by measuring locomotor activity and corporal temperature. Finally, we performed a phytochemical analysis of AERi. RESULTS: HPLC titration revealed the presence of hyperin (21.6 mg/g), quercetin-3-O-ß-xyloside (4.4 mg/g), quercetin-3-O-α-arabinofuranoside (12.0 mg/g), and quercetin (2.1 mg/g). It was also possible to isolate minor constituents׳ chlorogenic acid, neochlorogenic acid and procyanidin C1. The oral administration of AERi (100 mg/kg) significantly inhibited the neurogenic (37 ± 5%) and inflammatory (34 ± 7%) phases of formalin-induced pain. Acute and repeated treatment of animals with AERi (100 mg/kg, p.o.) once a day markedly reduced the mechanical hypersensitivity response induced by CFA, and this effect was evident until the day 10. Moreover, repeated treatment with AERi (100 mg/kg, p.o.) significantly reduced the levels of IL-1ß and TNF-α in the paw (22 ± 7% and 50 ± 19%) and in the spinal cord (100% and 100%) when compared to the CFA group. The AERi (100 mg/kg, p.o.) markedly reduced biting behavior induced by intrathecal injection of TNF-α (81 ± 11%). Finally, the effect of AERi was not associated with changes in locomotor activity or the corporal temperature of animals. CONCLUSION: These data show that aqueous extract of Rourea induta has significant antinociceptive action, which seems to be associated with an inhibition of pro-inflammatory cytokines activated pathways. These findings support the ethnomedical uses of this plant.


Assuntos
Analgésicos/uso terapêutico , Connaraceae , Dor/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Polifenóis/uso terapêutico , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Connaraceae/química , Feminino , Formaldeído , Adjuvante de Freund , Interleucina-1beta , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Dor/induzido quimicamente , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Fator de Necrose Tumoral alfa
13.
Chin J Nat Med ; 11(6): 628-37, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24345504

RESUMO

AIM: Diabetes Mellitus is associated with significant morbidity and mortality worldwide. The need for enhanced efficacy and safety, and cheaper and more readily available new drugs has increased the search for new antidiabetic drugs from plants. This study was conducted to investigate the antidiabetic activity of the hydroethanolic leaf extract of B. coccineus in rats. METHODS: The effect of B. coccineus extract (100-800 mg · kg(-1), p.o.) on blood glucose levels in normal and glucose loaded rats, and alloxan-induced diabetic rats was determined. After 10 days of treatment, blood samples were collected from rats for lipid and insulin profiling. Animals were thereafter sacrificed and the kidneys, heart, and liver were harvested for antioxidant indices assay. RESULTS: In normal rats, B. coccineus did not cause significant reduction in blood glucose. At the dose of 800 mg · kg(-1), significant increase in blood glucose level was not observed 30 min. after glucose load. B. coccineus administered acutely did not generally produce significant reduction in blood glucose level in diabetic rats. Administered subacutely, the extract significantly reduced blood glucose level in diabetic rats from the 3(rd) day with peak effect observed at the dose of 800 mg · kg(-1) on the 10(th) day. The extract generally preserved in vivo antioxidant levels in the kidneys, heart, and liver, increased the level of high density lipoprotein and insulin, and reduced the level of triglycerides and low density lipoprotein compared to diabetic control. CONCLUSION: The findings in this study suggest that the hydroethanolic leaf extract Byrsocarpus coccineus possesses antidiabetic activity possibly mediated through inhibition of intestinal glucose absorption, in vivo antioxidant activity, and enhancement of regeneration of beta cells of the pancreas and insulin secretion.


Assuntos
Antioxidantes/administração & dosagem , Connaraceae/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Extratos Vegetais/administração & dosagem , Animais , Antioxidantes/efeitos adversos , Antioxidantes/química , Glicemia/metabolismo , Diabetes Mellitus Tipo 2/metabolismo , Feminino , Humanos , Hipoglicemiantes/efeitos adversos , Hipoglicemiantes/química , Insulina/metabolismo , Masculino , Camundongos , Fitoterapia , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Folhas de Planta/química , Ratos , Ratos Wistar
14.
Mol Med Rep ; 8(5): 1493-8, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24026541

RESUMO

The antioxidant properties of robustaside B and para­hydroxyphenol isolated from Cnestis ferruginea were measured as the rate of inhibition of thiobarbituric acid reactive substance (TBARS) production in the Fe2+/ascorbate system. The modulatory effects of the compounds on mitochondrial membrane permeability transition (MMPT) were monitored spectrophotometrically as decreases in light scattering at 540 nm. The varying concentrations of robustaside B and para­hydroxyphenol (0.05, 0.1, 0.2, 0.25, 0.5, 0.75 and 1 mM) significantly reduced (P<0.05) the amount of TBARS generated by the Fe2+/ascorbate system by 85.3, 86.4, 86.0, 86.1, 86.0, 86.0 and 86.0% and 86.7, 81.3, 81.3, 80, 80, 82.6 and 83.1%, respectively. Similarly, quercetin, a standard antioxidant, was found to induce an 80% reduction in the amount of TBARS produced. The same IC50 value of 0.025 mM was observed for robustaside B, para­hydroxyphenol and quercetin. Pre­incubation of varying concentrations of robustaside B (0.125, 0.2, 0.5 and 1 mM) with succinate­energized mitochondria induced MMPT pore opening by 0, ­33.3, ­59.3 and ­218.5%, compared with control mitochondria. Para­hydroxyphenol at 0.1, 0.2, 0.25 and 0.5 mM induced MMPT pore opening in a concentration­dependent manner up to 0.25 mM by ­21, ­54.4 and ­107.0%, respectively. Quercetin at 0.05, 0.1, 0.25, 0.5, 0.75 and 1 mM also induced MMPT pore opening in the absence of calcium in a concentration­dependent manner by 5, 3.7, ­42.6, ­81.5, ­187 and ­161.1%, respectively. The current observations confirm the antioxidant properties of robustaside B and para­hydroxyphenol, and indicate a potential therapeutic use of the compounds for the treatment of diseases requiring the induction of cell death, including cancer.


Assuntos
Antioxidantes/farmacologia , Permeabilidade da Membrana Celular/efeitos dos fármacos , Connaraceae/química , Glicosídeos/farmacologia , Hidroquinonas/farmacologia , Mitocôndrias Hepáticas/efeitos dos fármacos , Proteínas de Transporte da Membrana Mitocondrial/efeitos dos fármacos , Fenóis/farmacologia , Animais , Cloreto de Cálcio/farmacologia , Masculino , Mitocôndrias Hepáticas/metabolismo , Poro de Transição de Permeabilidade Mitocondrial , Quercetina/farmacologia , Ratos , Ratos Wistar
15.
Pharm Biol ; 51(7): 825-35, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23627469

RESUMO

CONTEXT: Cnestis ferruginea Vahl ex DC (Connaraceae) (CF) is used in traditional African medicine in the management of CNS disorders. The degeneration and dysfunction of cholinergic neurons is closely associated with the cognitive deficits of Alzheimer's disease (AD) and oxidative stress has been implicated in its pathogenesis. However, the influence of C. ferruginea on the cholinergic system and oxidative stress parameters has not been explored. OBJECTIVE: The present study investigates the effect of methanol root extract of C. ferruginea and its active constituent amentoflavone (CF-2) on memory, oxidative stress and acetylcholinesterase (AChE) activity in scopolamine-induced amnesia. MATERIALS AND METHODS: Mice were orally treated with CF (25-200 mg/kg), CF-2 (6.25-25 mg/kg) for three days and memory impairment was induced by intraperitoneal injection of scopolamine (3 mg/kg). Memory function was evaluated by passive avoidance and Morris water maze tests. Biochemical parameters of oxidative stress and cholinergic function were estimated in brain after the completion of behavioral studies. RESULTS: Scopolamine caused memory impairment along with increased AChE activity and oxidative stress in mice brain. Oral administration of CF and CF-2 significantly prevented scopolamine-induced memory impairment, inhibited AChE and enhanced antioxidant enzyme activity in the brain following scopolamine injection as compared to vehicle administration in scopolamine (i.p.)-treated mice that were comparable to the effect of tacrine. DISCUSSION AND CONCLUSION: The study demonstrated that C. ferruginea and its constituent have significant protective effect against scopolamine-induced memory deficits in mice that can be attributed to their antioxidant and antiAChE activity.


Assuntos
Biflavonoides/farmacologia , Connaraceae/química , Transtornos da Memória/prevenção & controle , Extratos Vegetais/farmacologia , Acetilcolinesterase/metabolismo , Administração Oral , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Aprendizagem da Esquiva/efeitos dos fármacos , Biflavonoides/administração & dosagem , Biflavonoides/isolamento & purificação , Inibidores da Colinesterase/administração & dosagem , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Medicina Tradicional Africana , Transtornos da Memória/fisiopatologia , Camundongos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Escopolamina/toxicidade , Tacrina/farmacologia
16.
J Ethnopharmacol ; 146(2): 440-8, 2013 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-23376104

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cnestisferruginea (CF) Vahl ex DC (Connaraceae) is a shrub widely used in traditional African medicine for the treatment of various psychiatric illness and inflammatory conditions. AIM OF THE STUDY: This study was carried out to investigate the effect of amentoflavone isolated from methanolic root extract of CF on lipopolysaccharide (LPS)-induced neuroinflammatory cascade of events associated to the oxidative and nitrative stress, and TNF-α production in rat astrocytoma cell line (C6) and human monocytic leukemia cell line (THP-1), respectively. MATERIALS AND METHODS: Rat astrocytoma cells (C6) were stimulated with LPS (10µg/ml) alone and in the presence of different concentrations of amentoflavone (0.1-3µg/ml) for 24h incubation period. Nitrite release, reactive oxygen species (ROS), malondialdehyde (MDA) and reduced-glutathione (GSH) in C6 cells were estimated; while the TNF-α level was estimated in THP-1 cell lysate. In vivo analgesic activity was evaluated using mouse writhing and hot plate tests while the anti-inflammatory effect was investigated using carrageenan-induced oedema test. RESULTS: LPS (10µg/ml) significantly (P<0.05) stimulated C6 cells to release nitrite, ROS, MDA, and TNF-α generation while GSH was down regulated in comparison to control. However, amentoflavone significantly (P<0.05) attenuated nitrite, ROS, MDA and TNF-α generation and also up regulated the level of GSH. Amentoflavone per se did not have any significant effect on C6 and THP-1 cells. Amentoflavone (6.25-50mg/kg) significantly (P<0.05) reduced number of writhes and also increase pain threshold in hot plate test. It produced time course significant (P<0.05) decrease in oedema formation in rodents. DISCUSSION AND CONCLUSION: Findings in this study demonstrate the anti-neuroinflammatory and antinoceptive effects of amentoflavone which may suggest its beneficial roles in neuroinflammation associated disorders.


Assuntos
Anti-Inflamatórios/farmacologia , Biflavonoides/farmacologia , Connaraceae , Ácido Acético , Animais , Anti-Inflamatórios/uso terapêutico , Astrocitoma , Biflavonoides/uso terapêutico , Carragenina , Linhagem Celular , Linhagem Celular Tumoral , Sobrevivência Celular , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Glutationa/metabolismo , Temperatura Alta , Mediadores da Inflamação/metabolismo , Lipopolissacarídeos , Masculino , Malondialdeído/metabolismo , Camundongos , Nitritos/metabolismo , Dor/tratamento farmacológico , Dor/etiologia , Fitoterapia , Raízes de Plantas , Ratos , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
17.
Afr J Med Med Sci ; 41(2): 205-10, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23185920

RESUMO

OBJECTIVE: To evaluate the analgesic and antiinflammatory activities of the methanol extract of Cnestis ferruginea (CF) in rodents. MATERIALS AND METHODS: The antinociceptive activity of CF was evaluated using thermal (hot plate and tail flick tests) and chemical (acetic acid induced writhing and formalin tests) methods. The anti-inflammatory effects were studied using the cotton pellet granuloma and carrageenan induced paw edema tests. RESULTS: The extract (300-500 mg/kg, per oral), dissolved in normal saline produced a dose dependent analgesic effect on a hot plate maintained at 55 +/- 2 degrees C as well as on the early and late phases of formalin induced paw licking in rats. At the same doses, the plant extract also significantly (p < 0.05) inhibited the carrageenan induced paw edema and cotton pellet granuloma formation in rats. CONCLUSION: The results suggest that the methanol extract of CF possesses analgesic and antiinflammatory activities.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/uso terapêutico , Connaraceae/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Analgésicos/análise , Animais , Anti-Inflamatórios/análise , Carragenina , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/prevenção & controle , Masculino , Camundongos , Nigéria , Extratos Vegetais/análise , Ratos
18.
Pharmacol Biochem Behav ; 103(2): 322-31, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-22944105

RESUMO

The root decoction of Cnestis ferruginea (CF) Vahl DC (Connaraceae) is used in traditional African medicine in the management of psychiatric disorders. This study presents the antidepressant and anxiolytic effects of amentoflavone (CF-2) isolated from the root extract of C. ferruginea. The antidepressant effect was studied using the forced swimming (FST) and tail suspension tests (TST) while the hole-board, elevated plus maze (EPM) and light/dark tests were used to evaluate the anxiolytic effect. Acute treatment with CF extract and amentoflavone significantly (p<0.001) reduced the duration of immobility in FST and TST with peak effects observed at 100 and 50mg/kg respectively in comparison to control treated. Antidepressant effects of CF and amentoflavone were significantly higher (p<0.05) when compared to imipramine in FST but comparable to the fluoxetine treated group in TST. The pretreatment of mice with metergoline (4mg/kg, i.p., a 5-HT2 receptor antagonist), prazosin (62.5µg/kg, i.p., an α1-adrenoceptor antagonist), and yohimbine (1mg/kg, i.p., an α2-adrenoceptor antagonist), but not sulpiride (50mg/kg, i.p., a dopamine D2 receptor antagonist), cyproheptadine (3mg/kg, i.p., a 5-HT2 receptor antagonist), atropine (1mg/kg, i.p., a muscarinic receptor antagonist) 15mins before the administration of amentoflavone (50mg/kg; p.o.) significantly prevented its antiimmobility effect in the FST. CF extract and CF-2 significantly (p<0.05) attenuated anxiety by increasing the number of head-dips in the hole-board test, the time spent on the open arms in the EPM, and the exploration of the light chamber in the light/dark test. Pretreatment with flumazenil (3mg/kg, i.p., ionotropic GABA receptor antagonist) 15min before oral administration of amentoflavone (25mg/kg) significantly reduced the time spent in the open arms in EPM. It is concluded from the results obtained that amentoflavone produces its antidepressant effect through interaction with 5-HT2 receptor and α1-, and α2-adrenoceptors while the anxiolytic effect involved the ionotropic GABA receptor.


Assuntos
Ansiolíticos/farmacologia , Antidepressivos/farmacologia , Biflavonoides/farmacologia , Connaraceae/química , Extratos Vegetais/farmacologia , Animais , Ansiolíticos/isolamento & purificação , Antidepressivos/isolamento & purificação , Biflavonoides/isolamento & purificação , Masculino , Aprendizagem em Labirinto , Camundongos , Atividade Motora/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Teste de Desempenho do Rota-Rod
19.
Pharm Biol ; 50(8): 994-1006, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22775416

RESUMO

CONTEXT: Cnestis ferruginea (CF) Vahl ex DC (Connaraceae) is a shrub abundant in West Africa. Root preparations are used in traditional medicine to treat diverse conditions. OBJECTIVE: To evaluate the sub-chronic toxicological effects of the methanol root extract of CF. MATERIALS AND METHODS: Groups of adult rats of both sexes were treated daily with distilled water (DW) and CF at doses of 80 (sub-therapeutic dose), 400 (therapeutic dose), and 1000 (supra-therapeutic dose) mg/kg orally for 90 days. Animals were weighed weekly and observed for behavioral and morphological changes. At the end, rats were sacrificed and blood samples collected for hematological and biochemical analysis. Vital organs were harvested, weighed, and assessed for in vivo antioxidants and histopathological changes. Sperm analysis and reversibility study were done, and mortality was recorded. RESULTS: CF at the therapeutic dose did not produce any significant irreversible deleterious effects on the weight of animals and vital organs, in vivo antioxidants, histopathological presentation, hematological, biochemical, and sperm parameters. Platelet anomaly was elicited as a delayed effect. Effects at the sub- and supra-therapeutic doses were similar but with delayed anemia in females and weight reduction and sterility in males as possible side effects. CF generally showed a potential to induce in vivo antioxidants. DISCUSSION AND CONCLUSION: Findings suggest that CF given over an extended period possess the potential to cause induction of in vivo antioxidants especially in the ovary. Possible side effects identified with CF, which necessitate caution, include delayed platelet anomaly and anemia in females, weight reduction, and sterility in males.


Assuntos
Anemia/induzido quimicamente , Transtornos Plaquetários/induzido quimicamente , Connaraceae/química , Infertilidade Masculina/induzido quimicamente , Medicina Tradicional Africana , Extratos Vegetais/efeitos adversos , Raízes de Plantas/química , Animais , Peso Corporal/efeitos dos fármacos , Etnofarmacologia , Feminino , Dose Letal Mediana , Masculino , Metanol/química , Nigéria , Tamanho do Órgão/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Distribuição Aleatória , Ratos , Solventes/química , Testes de Toxicidade Subcrônica
20.
J Ethnopharmacol ; 142(2): 383-9, 2012 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-22613233

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cnestis ferruginea (CF) Vahl ex DC (Connaraceae) is a shrub widely used in Traditional African Medicine (TAM) for the treatment of various painful and inflammatory conditions. AIM OF THE STUDY: To isolate the active pharmacological constituents responsible for the anti-inflammatory and antinociceptive properties of the methanolic root extract of C. ferruginea. MATERIALS AND METHODS: The crude methanolic root extract of CF was sequentially fractionated into four sub extracts (chloroform, ethylacetate, n-butanol and the remaining aqueous fraction). The aqueous-butanol fractions, having showed significant inhibition of inflammation and pain, were subjected to fractionation through successive column chromatography on silica gel 60-120 mesh, eluted with a gradient of CHCl(3)-MeOH. Sixty five fractions were collected; fractions with similar TLC profiles were grouped into seven major fractions (1-7). Fraction 4 being the most active in bioassay was rechromatographed to obtain CF-2. Analgesic activity was evaluated using the acetic acid-induced writhing and hot plate tests in mice while carrageenan induced paw oedema test was used to investigate the anti-inflammatory actions of the fractions obtained. RESULT: Amentoflavone (CF-2) was isolated from the aqueous/n-butanol fraction. CF-2 (12.5, 25 and 100 mg/kg; p.o) produced significant (P<0.05) dose dependent inhibition of pain response elicited by acetic acid and increased nociceptive reaction latency in hot plate test. In addition it produced significant (P<0.05) dose-dependent inhibition of oedema in the carrageenan-induced inflammation. CONCLUSION: This study showed that amentoflavone is responsible for the analgesic and anti-inflammatory activity of Cnestis ferruginea.


Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Biflavonoides/uso terapêutico , Connaraceae/química , Inflamação/tratamento farmacológico , Dor/tratamento farmacológico , Fitoterapia , Ácido Acético , África , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Biflavonoides/isolamento & purificação , Biflavonoides/farmacologia , Carragenina , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/tratamento farmacológico , Temperatura Alta , Inflamação/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos , Dor/induzido quimicamente , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Raízes de Plantas , Ratos , Ratos Sprague-Dawley
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