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1.
Molecules ; 27(22)2022 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-36431841

RESUMO

The species Trattinnickia rhoifolia Willd, (T. rhoifolia), which belongs to the Burseraceae family, is widely used in ethnopharmacological cultural practices by traditional Amazonian people for anti-inflammatory purposes, sometimes as their only therapeutic resource. Although it is used in teas, infusions, macerations and in food, the species is still unexplored in regard to its pharmacophoric potential and chemical profile. Therefore, the aim of this study was to conduct a phytochemical characterization of the hydroethanolic extract of T. rhoifolia leaves (HELTr) and to evaluate the acute toxicity and anti-inflammatory activity of this species using zebrafish (Danio rerio). The extract was analyzed by gas chromatography−mass spectrometry (GC-MS). The evaluation of the acute toxicity of the HELTr in adult zebrafish was determined using the limit test (2000 mg/kg), with behavioral and histopathological evaluations, in addition to the analysis of the anti-inflammatory potential of HELTr in carrageenan-induced abdominal edema, followed by the use of the computational method of molecular docking. The phytochemical profile of the species is chemically diverse, suggesting the presence of the fatty acids, ester, alcohol and benzoic acid classes, including propanoic acid, ethyl ester and hexadecanoic acid. In the studies of zebrafish performed according to the index of histopathological changes (IHC), the HELTr did not demonstrate toxicity in the behavioral and histopathological assessments, since the vital organs remained unchanged. Carrageenan-induced abdominal edema was significantly reduced at all HELTr doses (100, 200 and 500 mg/kg) in relation to the negative control, dimethyl sulfoxide (DMSO), while the 200 mg/kg dose showed significant anti-inflammatory activity in relation to the positive control (indomethacin). With these activities being confirmed by molecular docking studies, they showed a good profile for the inhibition of the enzyme Cyclooxygenase-2 (COX-2), as the interactions established at the sites of the receptors used in the docking study were similar to the controls (RCX, IMN and CEL). Therefore, the HELTr has an acceptable degree of safety for acute toxicity, defined in the analysis of behavioral changes, mortality and histopathology, with a significant anti-inflammatory action in zebrafish at all doses, which demonstrates the high pharmacophoric potential of the species. These results may direct future applications and drug development but still require further elucidation.


Assuntos
Burseraceae , Peixe-Zebra , Animais , Carragenina/efeitos adversos , Simulação de Acoplamento Molecular , Anti-Inflamatórios/química , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Edema/induzido quimicamente , Edema/tratamento farmacológico , Edema/patologia , Ésteres
2.
Nat Prod Res ; 35(11): 1903-1908, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31339383

RESUMO

The gastroprotective effect of a turmeric acetone extract (TAE) (Curcuma longa L. [Zingiberaceae]) was evaluated and compared against its major curcuminoids; curcumin (CUR), demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC). Additionally, to demonstrate the importance of the metabolites' ratio in the extract on the synergistic effect, different mixtures were evaluated. An ethanol-induced gastric injury model was used to evaluate the gastroprotection activity in Wistar rats. The pharmacologic interaction analysis was performed using the Combination Index (CI)-Isobologram Equation method. The CI calculated at 0.5 of affected fraction (fa) for the TAE indicated a synergistic interaction between its components. However, when the proportion of curcuminoids changed from 3.7:1:10 in TAE to a 1:1:1 ratio, the CI implied an antagonistic effect. The binary combinations of curcuminoids (1:1) also showed an antagonistic interaction. The results of this work suggest that the proportion of curcuminoids in the TAE is crucial for the gastroprotective effect against ethanol-induced damage.


Assuntos
Curcuma/química , Curcumina/farmacologia , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Estômago/efeitos dos fármacos , Acetona , Animais , Curcumina/química , Diarileptanoides/farmacologia , Etanol , Extratos Vegetais/química , Ratos Wistar , Estômago/patologia
3.
Naunyn Schmiedebergs Arch Pharmacol ; 393(8): 1501-1513, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32242245

RESUMO

The co-administration of 3α-hydroxymasticadienoic acid (3α-OH MDA) and diligustilide (DLG) generates a synergist gastroprotective effect on indomethacin-induced gastric damage. However, the related protective activities of the compounds alone (or in combination) remain unclear. In the present study, we evaluated the anti-inflammatory and antioxidative activities, as well as the potential modulation of important gasotransmitters of each compound individually and in combination using the indomethacin-induced gastric damage model. Male Wistar rats were treated orally with the 3α-OH MDA, DLG, or their combination (at a fixed ratio of 1:1, 1:3, and 3:1) 30 min before the generation of gastric mucosal lesions with indomethacin (30 mg/kg, p.o.). Three hours later, the gastric injury (mm2) was determined. Results from these experiments indicate, in addition to maintaining basal levels of PGE2, the gastroprotective effect of the pre-treatment with 3α-OH MDA (70%), DLG (81%), and their combination (72%) which was accompanied by significant decreases in leukocyte recruitment, as well as decreases in TNF-α and LTB4 gastric levels (p < 0.05). We also found that the pre-treatment maintains the basal antioxidant enzyme activities (SOD) and gastric NO and H2S production even in the presence of indomethacin (p < 0.05). In conclusion, when 3α-OH MDA-DLG is given at a 1:1 combination ratio, the gastroprotective effect and the inflammatory, antioxidant, and gaso-modulation properties are not different from those of treatments using the maximum doses of each compound, revealing that this combination produces promising results for the treatment of gastric ulcers.


Assuntos
Anti-Inflamatórios/farmacologia , Antiulcerosos/farmacologia , Antioxidantes/farmacologia , Mucosa Gástrica/efeitos dos fármacos , Úlcera Gástrica/prevenção & controle , Triterpenos/farmacologia , Animais , Dinoprostona/metabolismo , Modelos Animais de Doenças , Quimioterapia Combinada , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Sulfeto de Hidrogênio/metabolismo , Indometacina , Leucotrieno B4/metabolismo , Masculino , Óxido Nítrico/metabolismo , Ratos Wistar , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patologia , Superóxido Dismutase/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
4.
Toxicol Rep ; 7: 217-232, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32042599

RESUMO

Endopleura uchi, is used for the treatment of inflammatory disease and related to the female reproductive tract. The aim of this study was to evaluate the acute toxicity of the Endopleura uchi stem bark hydroethanolic extract (EEu) in zebrafish, emphasizing the histopathological and biochemical parameters, as well as evaluating the in silico pharmacokinetic and toxicological parameters of the phytochemical/pharmacological marker, bergenin, as their metabolites. The animals were orally treated with EEu at a single dose of 75 mg/kg, 500 mg/kg, 1000 mg/kg and 3000 mg/kg. the oral LD50 of the EEu higher to the dose of 3000 mg/kg. Behavioral, biochemical and histopathological changes were dose dependent. In silico pharmacokinetic predictions for bergenin and its metabolites showed moderate absorption in high human intestinal absorption (HIA) and Caco-2 models, reduced plasma protein binding, by low brain tissue binding and no P-glycoprotein (P-Gp) inhibition. Their metabolism is defined by the CYP450 enzyme, in addition to bergenin inhibition of CYP2C9, CYP3A4 and CYP2C19. In the bergenin and its metabolites in silico toxicity test it have been shown to cause carcinogenicity and a greater involvement of the bergenin with the CYP enzymes in the I and II hepatic and renal metabolism's phases was observed. It is possible to suggest that the histopathological damages are involved with the interaction of this major compound and its metabolites at the level of the cellular-biochemical mechanisms which involve the absorption, metabolization and excretion of these possible prodrug and drug.

5.
J Appl Biomed ; 18(4): 126-135, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-34907765

RESUMO

Dyslipidemias are lipid metabolism alterations that cause increased levels of serum lipoprotein, cholesterol, and triglycerides. These alterations are associated with a higher incidence of cardiovascular diseases and are a risk factor for atherosclerosis development. This study aimed to evaluate the effect of Rosmarinus officinalis essential oil (EORO, 100 mg/kg) and its nanoemulsion (NEORO, 500 µg/kg) on Triton and coconut saturated-fat-induced (CSF) dyslipidemias using Wistar rats. The phytochemical evaluation of EORO performed by gas chromatography-mass spectroscopy (GC-MS) revealed 1,8-cineole (33.70%), camphor (27.68%), limonene (21.99%), and α-pinene (8.13%) as its major compounds. Triton-induced dyslipidemia significantly increased total cholesterol, LDL, and triglycerides levels. On the other hand, the groups treated with EORO and NEORO had significantly reduced total cholesterol, LDL, and triglycerides compared to the group treated only with Triton. Similar results were observed on the positive control treated with simvastatin. Dyslipidemia induced with coconut saturated-fat (CSF) caused abdominal fat gain, hypercholesterolemia, hypertriglyceridemia, increased LDL levels, and atherogenesis in the aorta. In contrast, the groups treated with EORO, NEORO, and simvastatin had significantly reduced hypercholesterolemia and hypertriglyceridemia, reduced abdominal fat gain, and absence of atherogenesis in the vascular endothelium. Overall, in the Triton-induced dyslipidemia model, EORO treatment had superior values than NEORO's (and simvastatin), although the differences were not too high, while in the CSF model, the values were mixed. In this manner, our results show an anti-dyslipidemic and anti-atherogenic activity effect by EORO and NEORO.


Assuntos
Aterosclerose , Dislipidemias , Hipercolesterolemia , Hipertrigliceridemia , Óleos Voláteis , Rosmarinus , Animais , Ratos , LDL-Colesterol , Dislipidemias/induzido quimicamente , Dislipidemias/tratamento farmacológico , Hipercolesterolemia/tratamento farmacológico , Hipertrigliceridemia/tratamento farmacológico , Sistemas de Liberação de Fármacos por Nanopartículas , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Ratos Wistar , Rosmarinus/química , Sinvastatina , Triglicerídeos
6.
Pharmaceuticals (Basel) ; 12(4)2019 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-31783553

RESUMO

Hydroethanolic preparations of the botanical species Acmella oleracea L. are used in the north of Brazil for the treatment of various diseases. However, few studies have been conducted to evaluate the toxicity of this species. The objective of this study was to evaluate the acute toxicity of the hydroethanolic extract of A. oleracea L. (EHFAo) flowers in zebrafish by immersion and oral administration. The extract was analyzed by ultra-performance liquid chromatography-mass spectrometry (UPLC-MS). EHFAo was administered orally (44.457, 88.915, 199.94, 281.83, and 448.81 mg/kg) and by immersion (250, 300, 350, 400, and 450 µg/L). Behavioral and histopathological analysis of gills, liver, intestine, and kidney were performed. The presence of (2E,6Z,8E)-N-isobutyl-2,6,8-decatrienamide (spilanthol) in EHFAo was identified by ultra-high-re.solution liquid chromatography-electrospray ionization mass spectrometry (UHPLC-ESI-MS). Treatment with EHFAo caused significant behavioral changes and death. The calculated median lethal dose (LD50) was 148.42 mg/kg, and the calculated median lethal concentration (LC50) was 320 µg/L. In the histopathological study, it was observed that upon oral treatment, the tissue alterations that compromised the normal functioning of the organism occurred with EHFAo doses of 88.915, 199.53, and 281.83 mg/kg, the intestine being the most affected. When the treatment was performed by immersion, the most toxic EHFAo concentrations according to the histopathological evaluation were 300, 350, and 400 µg/L, with the most affected organ being the gills. Finally, EHFAo in this study was shown to be more toxic to the liver, intestine, and kidneys when administered orally and to gills, liver, and kidneys when administered by immersion in water. Therefore, considering the results obtained and the chemical characteristics of the main phytochemical marker of EHFAo, spilanthol, it can be suggested that, depending on the dose, this compound can lead to histopathological damages in the organs highlighted in this study.

7.
Sci Rep ; 9(1): 16622, 2019 11 12.
Artigo em Inglês | MEDLINE | ID: mdl-31719599

RESUMO

The study of pharmacological interactions between herbal remedies and conventional drugs is important because consuming traditional herbal remedies as supplements or alternative medicine is fairly common and their concomitant administration with prescribed drugs could either have a favorable or unfavorable effect. Therefore, this work aims to determine the pharmacological interactions of a turmeric acetone extract (TAE) and its main metabolite (curcumin) with common anti-ulcer drugs (ranitidine and bismuth subsalicylate), using an ethanol-induced ulcer model in Wistar rats. The analysis of the interactions was carried out via the Combination Index-Isobologram Equation method. The combination index (CI) calculated at 0.5 of the affected fraction (fa) indicated that the TAE or curcumin in combination with ranitidine had a subadditive interaction. The results suggest that this antagonistic mechanism is associated to the mucoadhesion of curcumin and the TAE, determined by rheological measurements. Contrastingly, both the TAE and curcumin combined with bismuth subsalicylate had an additive relationship, which means that there is no pharmacological interaction. This agrees with the normalized isobolograms obtained for each combination. The results of this study suggest that mucoadhesion of curcumin and the TAE could interfere in the effectiveness of ranitidine, and even other drugs.


Assuntos
Antiulcerosos/uso terapêutico , Bismuto/uso terapêutico , Curcumina/farmacologia , Etanol/efeitos adversos , Compostos Organometálicos/uso terapêutico , Extratos Vegetais/farmacologia , Ranitidina/uso terapêutico , Salicilatos/uso terapêutico , Úlcera Gástrica/prevenção & controle , Animais , Antiulcerosos/antagonistas & inibidores , Curcuma , Modelos Animais de Doenças , Interações Medicamentosas , Mucosa Gástrica/efeitos dos fármacos , Interações Ervas-Drogas , Masculino , Compostos Organometálicos/antagonistas & inibidores , Ranitidina/antagonistas & inibidores , Ratos , Ratos Wistar , Salicilatos/antagonistas & inibidores , Úlcera Gástrica/induzido quimicamente
8.
Pharmaceuticals (Basel) ; 12(3)2019 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-31373315

RESUMO

Medicinal plants such as Aloysia polystachya are often used in the treatment of psychiatric diseases, including anxiety- and depression-related humor disturbances. In folk medicine, A. polystachya is used to treat digestive and respiratory tract disturbances, as a sedative and antidepressant agent, and as a tonic for the nerves. This study aimed to evaluate the antidepressant and anxiolytic effect from the hydroethanolic extract from the leaves of Aloysia polystachya (HELAp) in zebrafish. The extract was analyzed through ultra-performance liquid chromatography-mass spectroscopy (UPLC-MS) and the main compound detected was acteoside. HELAp was administered orally (10 mg/kg) and through immersion (mg/L). The anxiolytic activity was evaluated through the scototaxis (light-dark) test using caffeine as an anxiogenic agent and buspirone as a positive control. The parameters assessed were: period spent in the white compartment (s), latency (s), alternations (n), erratic swims (n), period of freezing (s), thigmotaxis (s), and risk evaluation (n). The antidepressant effect was evaluated through the novel tank diving test using 1% ethanol, unpredictable chronic stress, and social isolation as depressors; fluoxetine was used as a positive control. The parameters assessed were: period spent at the top of the tank, latency, quadrants crossed, erratic swim, period of freezing, and distance of swam. The main chemical compound of HELAp was acteoside. The administration of the extract on zebrafish managed to revert the anxiogenic effect of caffeine without impairing their locomotion. Additionally, the treatment exerted antidepressant activity similarly to fluoxetine. Overall, the results suggest a significant anxiolytic and antidepressant activity to the extract, which is probably due to the presence of the major compound, acteoside.

9.
Rev. bras. farmacogn ; 29(4): 441-444, July-Aug. 2019. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1042283

RESUMO

Abstract The present work investigates the chemical composition of seeds of Cascabela thevetioides (Kunth) Lippold, an ornamental shrub of México. Six thevetia cardiac glycosides or thevetosides (thevetin A, B, and C, acetylthevetin A, B and C) were identified from the methanol extract of seeds of C. thevetioides by High-Performance Liquid Chromatography-Mass Spectrometry and by comparison of mass spectral fragmentation patterns. Enzymatic hydrolysis of a sample of thevetosides from methanol extract of seeds and subsequent High-Performance Liquid Chromatography-Mass Spectrometry analysis yielded the monoglycosides neriifolin, acetylneriifolin and acetylperuvoside, previously reported for this plant. For the fisrt time thevetin A, B and C, and acetylthevetin A, B and C are reported as components of seeds of C. thevetioides.

10.
Inflammopharmacology ; 26(2): 611-619, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28879572

RESUMO

(Z,Z')-Diligustilide (DLG) or levistolide A is a dimeric phthalide isolated from Ligusticum porteri (Osha), the roots of which are used in the traditional treatment of many diseases including gastric aches. However, its action has not been completely elucidated. We analyzed the contributions of hydrogen sulfide and S-nitrosothiols to the action of DLG. Animals were pretreated with freshly formed in vitro nitrosothiol using Na2S and sodium nitroprusside to elucidate participation in the action of DLG. We also evaluated the production of H2S in vivo and in real time on the stomach via a specific electrode introduced into the stomachs of anaesthetized animals pretreated with DLG. Treatment with 10 mg/kg DLG increases gastric H2S production in vivo from 7.8 ± 0.81 ppm to 13.1 ± 3.01 ppm and prevents the decrease in gastric injury caused by absolute ethanol. In addition, it maintains endogenous concentrations of GSH and NO·. Exogenous S-nitrosothiols protect the gastric mucosa from damage, suggesting that the action of DLG might be associated with S-nitrosothiol and H2S formation.


Assuntos
Benzofuranos/farmacologia , Etanol/farmacologia , Mucosa Gástrica/diagnóstico por imagem , Sulfeto de Hidrogênio/metabolismo , S-Nitrosotióis/metabolismo , Animais , Mucosa Gástrica/metabolismo , Substâncias Protetoras/farmacologia , Ratos , Ratos Wistar , Sulfetos/metabolismo
11.
Biomed Pharmacother ; 96: 182-190, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28987941

RESUMO

INTRODUCTION: Portulaca pilosa L., belonging to the family Portulacaceae, is a common herbaceous plant in the Americas and in the Amazon, is popularly known as love-grown and is traditionally used as an aid in the treatment of burns, buds, insect bites and wound healing. This study aims to evaluate the non-clinical topical healing activity of the P. pilosa gel (GPP) and the propyleneglycol extract of P. pilosa (EPP) in Wistar rats. METHODS: For the healing activity, wistar rats were divided into the following groups: negative control (GVE - vehicle, 150mg/kg), positive control (Fibrinase®- FIB, 100U/kg), Portulaca pilosa gel 10%, (GPP, 150mg/kg), and propylenglycollic extract of Portulaca pilosa (EPP, 150 mg/kg), which were submitted to a surgical procedure to obtain the wounds, and were treated topically for 7days. After treatment, the treated area was removed and a histopathological analysis was performed. RESULTS: The EPP when analyzed in HPLC was able to identify the presence of gallic acid. EPP significantly modulated the tissue inflammatory response, presenting low number of inflammatory cells in the histopathological study. Treatment with EPP and GPP significantly stimulated angiogenesis and this response was superior to the fibrinase® group. Treatment with EPP and GPP significantly stimulated the proliferation of fibroblasts. The groups treated with EPP and GPP presented an organization pattern of the epidermis and dermis better than the control group, with a mild inflammatory process, with fibroblast proliferation and increased formation of collagen fibers. CONCLUSION: Thus, from the results obtained it can be suggested that the phytochemical marker of the P. pilosa species for healing activity is gallic acid and, together with the macroscopic and microscopic findings triggered by the topical applications of EPP and GPP, it can be concluded that this plant species has topical healing activity, with great potential for use, since this pharmacological action is associated with a possible topical anti-inflammatory activity.


Assuntos
Extratos Vegetais/uso terapêutico , Portulaca , Ferida Cirúrgica/tratamento farmacológico , Cicatrização/efeitos dos fármacos , Animais , Feminino , Géis , Masculino , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Distribuição Aleatória , Ratos , Ratos Wistar , Ferida Cirúrgica/patologia , Cicatrização/fisiologia
12.
Pharm Biol ; 55(1): 96-100, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27927103

RESUMO

CONTEXT: Agastache mexicana ssp. mexicana (Kunth) Lint & Epling (Lamiaceae), popularly known as 'toronjil morado', is used in Mexican traditional medicine for the treatment of several diseases such as hypertension, anxiety and respiratory disorders. OBJECTIVE: This study investigates the relaxant action mechanism of A. mexicana ssp. mexicana essential oil (AMEO) in guinea-pig isolated trachea model. MATERIALS AND METHOD: AMEO was analyzed by GC/MS. The relaxant effect of AMEO (5-50 µg/mL) was tested in guinea-pig trachea pre-contracted with carbachol (3 × 10 - 6 M) or histamine (3 × 10 - 5 M) in the presence or absence of glibenclamide (10 - 5 M), propranolol (3 × 10 - 6 M) or 2',5'-dideoxyadenosine (10 - 5 M). The antagonist effect of AMEO (10-300 µg/mL) against contractions elicited by carbachol (10 - 15-10 - 3 M), histamine (10 - 15-10 - 3 M) or calcium (10-300 µg/mL) was evaluated. RESULTS: Essential oil composition was estragole, d-limonene and linalyl anthranilate. AMEO relaxed the carbachol (EC50 = 18.25 ± 1.03 µg/mL) and histamine (EC50 = 13.3 ± 1.02 µg/mL)-induced contractions. The relaxant effect of AMEO was not modified by the presence of propranolol, glibenclamide or 2',5'-dideoxyadenosine, suggesting that effect of AMEO is not related to ß2-adrenergic receptors, ATP-sensitive potassium channels or adenylate cyclase activation. AMEO was more potent to antagonize histamine (pA2' = -1.507 ± 0.122) than carbachol (pA2' = -2.180 ± 0.357). Also, AMEO antagonized the calcium chloride-induced contractions. CONCLUSION: The results suggest that relaxant effect of AMEO might be due to blockade of calcium influx in guinea-pig trachea smooth muscle. It is possible that estragole and d-limonene could contribute majority in the relaxant effect of AMEO.


Assuntos
Agastache/química , Broncoconstrição/efeitos dos fármacos , Broncodilatadores/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Traqueia/efeitos dos fármacos , Animais , Broncodilatadores/isolamento & purificação , Sinalização do Cálcio/efeitos dos fármacos , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Cobaias , Técnicas In Vitro , Masculino , Músculo Liso/metabolismo , Óleos Voláteis/isolamento & purificação , Fitoterapia , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Traqueia/metabolismo
13.
Artigo em Inglês | MEDLINE | ID: mdl-27143986

RESUMO

Hepatotoxic chemicals damage liver cells primarily by producing reactive oxygen species. The decoction of the leaves of Tamarindus indica L. is used for liver disorders. In this work we evaluated the hepatoprotective activity of a tablet formulation of this plant. Thirty-five Sprague Dawley rats were randomly divided into five groups (n = 7). First group (I) is control group, fed with standard diet. Groups II to V (hepatotoxic groups) were subjected to a subcutaneous injection of CCl4 (0.5 mL/kg). Group II was negative control, fed with standard diet; group III was subjected to administration of Silymarin 150 mg/kg and groups IV and V were treated with tablets in dose of 100 mg/kg and 200 mg/kg, respectively. Lipid peroxidation and the activity of superoxide dismutase, catalase, and reduced glutathione were evaluated. Serum levels of alanine aminotransferase, aspartate aminotransferase, gamma-glutamine transferase, alkaline phosphatase, and a lipid profile were evaluated too. The tablets inhibit lipid peroxidation. The redox balance (SOD-CAT-GSH) remains normal in the experimental groups treated with tablets. The liver function using dose of 200 mg/kg of tablets was better than the other experimental groups. These results justify, scientifically, the ethnobotanical use of the leaves of Tamarindus indica L.

14.
Biomed Res Int ; 2013: 206581, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23509690

RESUMO

The crude ethanolic extract from aerial parts of Pothomorphe umbellata L. (Piperaceae) and fractions obtained by partitions sequentially among water-methanol, methylene chloride, and ethyl acetate, as well as the major constituent, 4-nerolidylcatechol, were, respectively, evaluated and evidenced for antioxidant and cytotoxic effects through fluorometric microplate and microculture tetrazolium assays in HL-60 cells. The crude ethanolic extract demonstrated the preeminent antioxidant activity (IC50 = 1.2 µg/mL) against exogenous cytoplasmic reactive oxygen species, followed by the water-methanolic (IC50 = 4.5 µg/mL), methylene chloride (IC50 = 5.9 µg/mL), ethyl acetate (IC50 = 8.0 µg/mL), 4-nerolidylcatechol (IC50 = 8.6 µg/mL), and the sterol fractions (IC50 > 12.5 µg/mL). Vitamin C, the positive control used in this assay, presented IC50 value equivalent to 1.7 µg/mL. 4-Nerolidylcatechol (IC50 = 0.4 µg/mL) and methylene chloride fraction (IC50 = 2.3 µg/mL) presented considerable cytotoxicity probably because of the presence of an o-quinone, an auto-oxidation by product of the catechol. Polar compounds, present in the ethanol extract, appear to increase the solubility and stability of the major active constituent, acting synergistically with 4-nerolidylcatechol, improving its pharmacokinetic parameters and increasing significantly its antioxidant activity which, in turn, suggests that the aqueous-ethanolic extract, used in folklore medicine, is safe and effective.


Assuntos
Antioxidantes/farmacologia , Catecóis/farmacologia , Piperaceae/química , Extratos Vegetais/farmacologia , Antioxidantes/análise , Ácido Ascórbico/metabolismo , Catecóis/análise , Citoplasma/metabolismo , Células HL-60 , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Oxigênio/metabolismo , Extratos Vegetais/análise , Folhas de Planta/química , Quinonas/metabolismo , Espécies Reativas de Oxigênio/metabolismo
15.
Pharmacognosy Res ; 3(2): 79-84, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21772750

RESUMO

BACKGROUND: Folk medicine uses preparations of Arrabidaea chica (pariri) leaves to treat various liver pathologies. We evaluated the effects of the hydroethanolic extract of these leaves (CHEE) on an in vivo model of liver intoxication. MATERIALS AND METHODS: Different groups of rats were treated orally for 7 days with CHEE at doses of 300, 500 or 600 mg/kg or silymarin at 35 mg/kg. The control group received only 0.5 ml of distilled water. After 7 days of treatment, both the groups received CCl(4), and activities of glutamic pyruvic transaminase (GPT), glutamic oxaloacetic transaminase (GOT) and bilirubin level were assessed. The ability of CHEE to suppress hepatic injury triggered by CCl(4) was evaluated based on suppression (%) of activities of GOT, GPT and bilirubin levels. RESULTS: The chromatograms of the CHEE obtained at 330 and 400 nm show features of two main classes of secondary metabolites: quinones and flavonoids. The administration of 300, 500 or 600 mg/kg of CHEE resulted in the reduction of GPT levels by 85.34%, 88.59% and 93.72%, respectively. The suppression of GOT levels was 56.86%, 65.27% and 68.95%, respectively, and that of plasma bilirubin was 83.81%, 83.12% and 84.14%, respectively. These results demonstrate the protective character of CHEE and its ability to maintain the functional integrity of hepatic cells. CONCLUSIONS: The results obtained are possibly due to the presence of quinones and flavonoids in A. chica CHEE, both detected using high performance liquid chromatography.

16.
Bol. latinoam. Caribe plantas med. aromát ; 10(2): 147-154, mar. 2011. ilus, tab
Artigo em Inglês | LILACS | ID: lil-686994

RESUMO

Gingko biloba has been one of the most used medicinal plants all over the world in the past years. In this study, our group has studied the effect of a hydroethanolic extract from the aerial parts of this plant on the growth and morphological differentiation of trypanosomatids. Herpetomonas samuelpessoai and Herpetomonas sp were used in this study. The extract was obtained in a Soxhlet apparatus (50 oC, 2 hours). This extract was aseptically added to Roitman’s medium in different concentrations (4, 20, 40, 60, 80 and 100 mg/ml). The growth rate was determined using a Newbauer chamber to count numbers of cells after the extract inoculation (24 and 72 hours later). Smears stained by the Panotic method was used to determine the percentages of pro, para and opisthomastigote forms. The extract inhibited Herpetomonas sp growth in concentrations higher than 20 mg/ml. H. samuelpessoai has been inhibited in doses higher than 40 mg/ml. No morphological differentiation was observed in Herpetomonas sp cell. However, morphological differentiations could be noticed in H. samuelpessoai cell using doses higher than 40 mg/ml. These alterations are probably related to the cell division process, since cells with 3 or 4 nucleus were observed. Also, cytoplasmatic expansions, representing unsuccessful process of cell division were frequently found out. Further ultrastructural analysis using a transmission electron microscope showed cells with homogeneous nucleus or the absence of it. Protozoan protein profile was also analyzed. It was possible to notice changes in both trypanosomatids used in this study. H. samuelpessoai has shown over expression and accumulation of proteins which its degradation is essential to continue the cell differentiation. Also, it is possible to suggest that this extract acts through the modulation of the genetic expression and may be harmful to human cells if not purified.


Gingko biloba es una de las plantas medicinales más utilizadas en todo el mundo en los últimos años. En este estudio, nuestro grupo ha estudiado el efecto de un extracto hidroetanólico de la parte aérea de esta planta sobre el crecimiento y la diferenciación morfológica de tripanosomátidos. Herpetomonas samuelpessoai y Herpetomonas sp se utilizaron en este estudio. El extracto se obtuvo en un aparato Soxhlet (50° C/2 horas). Este extracto se agregó asépticamente a medio Roitman en diferentes concentraciones (4, 20, 40, 60, 80 y 100 mg /ml). La tasa de crecimiento se determinó utilizando una cámara de Newbauer para contar el número de células después de la inoculación de extracto (24 y 72 horas más tarde). Frotis teñidos por el método Panotic se utilizó para determinar los porcentajes de pro, para y las formas opistomastigota. El extracto inhibió el crecimiento Herpetomonas sp en concentraciones superiores a 20 mg /ml. H. samuelpessoai se ha inhibido en dosis superiores a 40 mg /ml. No se observó diferenciación morfológica en la celda Herpetomonas sp. Sin embargo, las diferenciaciones morfológicas se pudo observar en la celda H. samuelpessoai con dosis superiores a 40 mg /ml. Estas alteraciones son probablemente relacionado con el proceso de división celular, ya que las células con 3 o 4 núcleos se observaron. Además, las expansiones citoplasmáticas, lo que representa el proceso fallido de la división celular se encontraron con frecuencia hacia fuera. Un análisis más detallado ultraestructural usando microscopio electrónico de transmisión mostró células con núcleo homogéneo o la ausencia de ella. El perfil de proteínas por Protozoarios también se ha analizado. Fue posible notar cambios tanto en tripanosomátidos utilizados en este estudio. H. samuelpessoai ha demostrado a lo largo de expresión y la acumulación de proteínas que su degradación es esencial para continuar con la diferenciación celular. Además, es posible sugerir que este extracto...


Assuntos
Extratos Vegetais/farmacologia , Ginkgo biloba/química , Trypanosomatina/crescimento & desenvolvimento , Trypanosomatina , Eletroforese , Folhas de Planta/química , Microscopia Eletrônica de Transmissão , Trypanosomatina/ultraestrutura
17.
J Pharm Pharmacol ; 59(8): 1151-8, 2007 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17725859

RESUMO

We have evaluated the anti-inflammatory and analgesic properties of the leaves (LCE) and stem bark (BCE) crude extracts of Zanthoxylum riedelianum (Rutaceae). Different fractions of the stem bark extract (hexane, BCEH; dichloromethane, BCED; ethyl acetate, BCEE; and lyophilized aqueous residual, BCEW) were also investigated. We studied the effects of the extracts and fractions using the rat paw oedema test induced by carrageenan, dextran, histamine or nystatin; the mouse abdominal constriction test; the mouse hot-plate test (only for LCE and BCE); and the mouse formalin test. Both extracts and all BCE fractions displayed anti-inflammatory activity in the carrageenan-induced oedema model, but not for dextran, histamine or nystatin. Considering the analgesic models, both extracts showed antinociceptive activity, but BCE was more active than LCE in models of central pain. All BCE fractions showed significant inhibition in the abdominal constriction test and in both phases of the formalin test. When BCED was submitted to phytochemical procedures it led to the isolation of six lignans (sesamin, methylpluviatolide, dimethylmatairesinol, piperitol-4(')-O-(gamma),(gamma)-dimethylallyl ether, kaerophyllin and hinokinin), and a triterpene (lupeol). Inhibition of cyclooxygenase and its metabolites may have been involved in the mechanism of action of this plant, considering previous studies reporting the anti-inflammatory and analgesic activity for the identified lignans, as well as anti-inflammatory activity for lupeol.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Dor/tratamento farmacológico , Zanthoxylum/química , Analgésicos/administração & dosagem , Analgésicos/química , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Lignanas/administração & dosagem , Lignanas/química , Lignanas/farmacologia , Masculino , Camundongos , Medição da Dor , Triterpenos Pentacíclicos , Casca de Planta , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta , Prostaglandina-Endoperóxido Sintases/efeitos dos fármacos , Prostaglandina-Endoperóxido Sintases/metabolismo , Ratos , Ratos Wistar , Triterpenos/administração & dosagem , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
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