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1.
J Med Food ; 25(4): 443-455, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35085011

RESUMO

Systemic arterial hypertension (SAH) is a health problem of great importance worldwide, and endothelial dysfunction underlies SAH development. This condition's main characteristics include vasoconstriction, inflammation, oxidative stress, and procoagulant and proliferative states. This study's objective was to evaluate the antihypertensive, anti-inflammatory, and antioxidant effects of the whole extract and fractions of Agave tequilana in a murine model of SAH. SAH was induced in male ICR or CD-1 (Strain obtained from animals from Charles River Laboratories, Massachusetts) mice by intraperitoneal administration of angiotensin II (AGII) (0.1 µg/kg) for 4 weeks, and then A. tequilana treatments were co-administered with AGII. At the end of the experiment, systolic and diastolic blood pressure were measured and the kidneys were dissected to quantify interleukin (IL)-1ß, IL-6, tumor necrosis factor-alpha, IL-10, and malondialdehyde (MDA). The whole extract and the fractions of A. tequilana were chemically characterized using gas chromatography-mass spectrometry. The results indicate that the whole extract (At-W) and At-AcOEt fraction treatment are the most efficient in lowering blood pressure, although all the treatments had an immunomodulatory effect on the cytokines evaluated and an antioxidant effect on lipid peroxidation. Finally, the chromatographic profile shows that the integral extract and fractions of A. tequilana contained phytol (M)3,7,11,15-Tetramethyl-2-hexadecen-1-ol; 9,12-octadecadienoic acid; hentriacontane; 9,19-cyclolanost-24-en-3-ol,(3b); t-sitosterol; and stigmasta-3,5-dien-7-one.


Assuntos
Agave , Hipertensão , Agave/química , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Hipertensão/tratamento farmacológico , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/farmacologia
2.
Sci Rep ; 11(1): 21193, 2021 10 27.
Artigo em Inglês | MEDLINE | ID: mdl-34707201

RESUMO

Endothelial dysfunction (ED) is a key factor for the development of cardiovascular diseases. Due to its chronic, life-threatening nature, ED only can be studied experimentally in animal models. Therefore, this work was aimed to characterize a murine model of ED induced by a daily intraperitoneal administration of angiotensin II (AGII) for 10 weeks. Oxidative stress, inflammation, vascular remodeling, hypertension, and damage to various target organs were evaluated in treated animals. The results indicated that a chronic intraperitoneal administration of AGII increases the production of systemic soluble VCAM, ROS and ICAM-1 expression, and the production of TNFα, IL1ß, IL17A, IL4, TGFß, and IL10 in the kidney, as well as blood pressure levels; it also promotes vascular remodeling and induces non-alcoholic fatty liver disease, glomerulosclerosis, and proliferative retinopathy. Therefore, the model herein proposed can be a representative model for ED; additionally, it is easy to implement, safe, rapid, and inexpensive.


Assuntos
Angiotensina II/administração & dosagem , Modelos Animais de Doenças , Endotélio Vascular/metabolismo , Doenças Vasculares/metabolismo , Angiotensina II/toxicidade , Animais , Endotélio Vascular/efeitos dos fármacos , Endotélio Vascular/patologia , Infusões Parenterais , Molécula 1 de Adesão Intercelular/metabolismo , Interleucinas/metabolismo , Rim/metabolismo , Rim/patologia , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Estresse Oxidativo , Fator de Crescimento Transformador beta/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Molécula 1 de Adesão de Célula Vascular/metabolismo , Doenças Vasculares/etiologia , Doenças Vasculares/patologia , Remodelação Vascular
3.
Molecules ; 26(3)2021 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-33494340

RESUMO

Pharmacodynamic interactions between plant isolated compounds are important to understand the mode of action of an herbal extract to formulate or create better standardized extracts, phytomedicines, or phytopharmaceuticals. In this work, we propose binary mixtures using a leader compound to found pharmacodynamic interactions in inhibition of the NF-κB/AP-1 pathway using RAW-Blue™ cells. Eight compounds were isolated from Castilleja tenuiflora, four were new furofuran-type lignans for the species magnolin, eudesmin, sesamin, and kobusin. Magnolin (60.97%) was the most effective lignan inhibiting the NF-κB/AP-1 pathway, followed by eudesmin (56.82%), tenuifloroside (52.91%), sesamin (52.63%), and kobusin (45.45%). Verbascoside, a major compound contained in wild C. tenuiflora showed an inhibitory effect on NF-κB/AP-1. This polyphenol was chosen as a leader compound for binary mixtures. Verbacoside-aucubin and verbascoside-kobusin produced synergism, while verbascoside-tenuifloroside had subadditivity in all concentrations. Verbascoside-kobusin is a promising mixture to use on NF-κB/AP-1 related diseases and anti-inflammatory C. tenuiflora-based phytomedicines.


Assuntos
Anti-Inflamatórios , Glucosídeos , Iridoides , Lignanas , NF-kappa B/antagonistas & inibidores , Orobanchaceae/química , Fenóis , Fator de Transcrição AP-1/antagonistas & inibidores , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Linhagem Celular , Glucosídeos/química , Glucosídeos/farmacologia , Iridoides/química , Iridoides/farmacologia , Lignanas/química , Lignanas/farmacologia , Camundongos , NF-kappa B/metabolismo , Fenóis/química , Fenóis/farmacologia , Fator de Transcrição AP-1/metabolismo
4.
Naunyn Schmiedebergs Arch Pharmacol ; 393(7): 1281-1291, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32342135

RESUMO

Malva parviflora is used as food in the gastronomy of some regions of Mexico and, also, in Mexican traditional medicine for inflammation-related conditions like rheumatoid arthritis. The objective of this work was to evaluate its antiarthritic activity in a mice model. In ICR, female mice were tested the dichloromethane extract (MpD) and fractions MpF4 (extracted with a dichoromethane:methanol system) and MpFphy (a precipitate by acetone:methanol) by using the mono-arthritis with kaolin/carrageenan model. During the treatment, joint inflammation was measured daily, and hyperalgesia was measured using the hot plate test. The treatments diminished both joint inflammation and pain. At the end of the evaluation, the left joint and spleen were extracted for determination of pro- and anti-inflammatory cytokines. The results showed that the MpD, MpF4, and MpFphy treatments modulated the concentration of these proteins. Specifically, MpFphy at 1.0 mg/kg increased IL-4 and IL-10 and decreased IL-17, IL-1ß, and TNF-α. GC-MS analysis showed that MpF4 contained a mixture of a total of nine compounds, three of them newly reported for the species. The studies confirmed the presence of five sterols in the MpFphy fraction, including stigmasterol and ß-sitosterol. These results confirm the anti-rheumatoid and anti-inflammatory activities of a fraction rich in sterols from Malva parviflora. Graphical abstract.


Assuntos
Anti-Inflamatórios/farmacologia , Antirreumáticos/farmacologia , Malva/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Antirreumáticos/isolamento & purificação , Artrite Experimental/tratamento farmacológico , Artrite Experimental/patologia , Artrite Reumatoide/tratamento farmacológico , Artrite Reumatoide/patologia , Carragenina , Citocinas/metabolismo , Feminino , Inflamação/tratamento farmacológico , Inflamação/patologia , Caulim , Camundongos , Camundongos Endogâmicos ICR , Esteróis/isolamento & purificação , Esteróis/farmacologia
5.
Biomed Pharmacother ; 118: 109349, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31545221

RESUMO

Neuroinflammation, a centralized immune response, is a physiological process by which the organism attempts to remove an injurious stimulus in the central nervous system. Nonetheless, it is known that chronic inflammatory processes play an important role in the onset and progression of neurodegenerative disorders, such as Alzheimer´s disease (AD). Based on this, new strategies to treat AD have been proposed. Among them, the use of non-steroidal anti-inflammatory drugs (NSAIDs) decreases the incidence of this disease. Unfortunately, the prolonged use of NSAIDs results in adverse secondary effects. In this context, plants secondary metabolites have become of great interest. Particularly, our group has demonstrated that the hydroalcoholic extract of Malva parviflora (MpHA) has anti-inflammatory effect and is capable of improving the cognitive deficit present in an AD model. To further characterize the Malva parviflora compounds with anti-inflammatory properties, here we generated a fraction from a dichloromethane extract, which constitutes a less complex mix of compounds than the MpHA. This approach allowed us to isolate a fraction (MpF10) with anti-inflammatory activity, able to ameliorate the spatial learning and memory impairment, and to reduce both astrogliosis as well as IL-1ß and TNF production in a murine model of LPS-mediated neuroinflammation. Among the identified compounds in the MpF10, we found daucosterol (MpDau), which prevented LPS-induced neuroinflammation. Interestingly, MpF10 and MpDau inhibit NFκB activity in macrophages exposed to LPS. Therefore, we propose that the compounds present in the MpF10 represent an alternative to treat neuroinflammation, an important process developed during neurodegenerative diseases such as AD.


Assuntos
Encéfalo/patologia , Inflamação/tratamento farmacológico , Malva/química , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Encéfalo/fisiopatologia , Inflamação/patologia , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Macrófagos/patologia , Memória/efeitos dos fármacos , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia
6.
Biol Pharm Bull ; 42(2): 201-211, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30713252

RESUMO

The main objective of treatment against hypertension is not only to reduce blood pressure levels, but also to reduce vascular risk in general. In the present work, administering angiotensin II (AGII; 0.2 µg/kg intraperitoneally (i.p.) for 12 weeks) activates the hypothalamic-pituitary-adrenal (HPA) axis, which caused an increase in corticosterone levels, as well as in proinflammatory cytokines (interleukin 1ß (IL-1ß), interleukin 6 (IL-6), and tumor necrosis factor alpha (TNF-α)) and macrophage chemotactic protein 1 (MCP-1), and decreased anti-inflammatory cytokines (interleukin 10 (IL-10) and interleukin 4 (IL-4)). On observing the behavior in the different models, an anxiogenic effect (elevated plus maze (EPM)) and cognitive impairment (water Morris maze (WMM)) was observed in animals with AGII. By administering organic extracts from Ocimum basilicum (Oba-EtOAc) and Ocimum selloi (Ose-EtOAc), and some doses of rosmarinic acid (RA) (6 weeks per os (p.o.)), the damage caused by AGII was stopped by re-establishing corticosterone serum levels and by decreasing the proinflammatory cytokines and MCP-1.


Assuntos
Cinamatos/farmacologia , Depsídeos/farmacologia , Hipertensão/tratamento farmacológico , Ocimum/química , Extratos Vegetais/farmacologia , Angiotensina II/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Corticosterona/sangue , Citocinas/metabolismo , Relação Dose-Resposta a Droga , Hipertensão/induzido quimicamente , Hipertensão/metabolismo , Sistema Hipotálamo-Hipofisário/efeitos dos fármacos , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Camundongos Endogâmicos ICR , Ocimum basilicum/química , Sistema Hipófise-Suprarrenal/efeitos dos fármacos , Distribuição Aleatória , Navegação Espacial/efeitos dos fármacos , Ácido Rosmarínico
7.
Biol Pharm Bull ; 42(1): 18-25, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30606987

RESUMO

Hypertension is a disease of high prevalence and morbidity where vascular inflammation and associated oxidative stress (endothelial dysfunction) is the underlying cause of this pathology. We are reporting the antihypertensive activity of extracts and fractions of Malva parviflora in mice with chronic and acute hypertension. Also, the treatments of this plant were able to counteract the kidney inflammation and associated oxidative stress. The chronic hypertension model consisted of administration of angiotensin II (AGII) during 12 weeks, causing a sustained increase in systolic (SBP) or diastolic (DBP) pressure, with values of pharmacological constants of: ED50 = 0.038 mg/kg y Emax = 135 mmHg for SBP and ED50 = 0.046 mg/kg y Emax = 98 mmHg for DBP. The chronic hypertension caused the inflammation and lipid peroxidation in kidneys, measured by of tissue level of cytokines such as interleukin-1ß (IL-1ß), IL-6, Tumor Necrosis Factor-α (TNF-α), IL-10 and malondialdehyde, and treatments for M. parviflora were able to modulate these parameters. The chemical fractionation allowed to identify three compounds: oleanolic acid, tiliroside and scopoletin, which were tested in a model of acute hypertension. The pharmacodynamic parameters for SBP were ED50 = 0.01 and 0.12 mg/kg while Emax = 33.22 and 37.74 mmHg for scopoletin and tiliroside, respectively; whereas that for DBP data were ED50 = 0.01 and 0.02 mg/kg; with an Emax = 7.00 and 6.24 mmHg, in the same order. M. parviflora, is able to counteract the effect of chronic and acute administration of AGII, on hypertension, but also the inflammatory and oxidative damage in the kidney. The oleanolic acid, scopoletin and tiliroside are the compounds responsible for such activities.


Assuntos
Anti-Hipertensivos/uso terapêutico , Flavonoides/uso terapêutico , Hipertensão/tratamento farmacológico , Malva , Extratos Vegetais/uso terapêutico , Escopoletina/uso terapêutico , Angiotensina II/toxicidade , Animais , Anti-Hipertensivos/isolamento & purificação , Anti-Hipertensivos/farmacologia , Pressão Sanguínea/efeitos dos fármacos , Pressão Sanguínea/fisiologia , Relação Dose-Resposta a Droga , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Hipertensão/sangue , Hipertensão/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/isolamento & purificação , Escopoletina/isolamento & purificação , Escopoletina/farmacologia
8.
Nutrients ; 10(3)2018 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-29495578

RESUMO

Inflammation and oxidative stress play major roles in endothelial dysfunction, and are key factors in the progression of cardiovascular diseases. The aim of this study was to evaluate in vitro the effect of three subfractions (SFs) from the Cucumis sativus aqueous fraction to reduce inflammatory factors and oxidative stress induced by angiotensin II (Ang II) in human microvascular endothelial cells-1 (HMEC-1) cells. The cells were cultured with different concentrations of Ang II and 0.08 or 10 µg/mL of SF1, SF2, or SF3, or 10 µmol of losartan as a control. IL-6 (Interleukin 6) concentration was quantified. To identify the most effective SF combinations, HMEC-1 cells were cultured as described above in the presence of four combinations of SF1 and SF3. Then, the effects of the most effective combination on the expression of adhesion molecules, the production of reactive oxygen species (ROS), and the bioavailability of nitric oxide (NO) were evaluated. Finally, a mass spectrometry analysis was performed. Both SF1 and SF3 subfractions decreased the induction of IL-6 by Ang II, and C4 (SF1 and SF3, 10 µg/mL each) was the most effective combination to inhibit the production of IL-6. Additionally, C4 prevented the expression of adhesion molecules, reduced the production of ROS, and increased the bioavailability of NO. Glycine, arginine, asparagine, lysine, and aspartic acid were the main components of both subfractions. These results demonstrate that C4 has anti-inflammatory and antioxidant effects.


Assuntos
Aminoácidos/farmacologia , Angiotensina II/toxicidade , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Cucumis sativus , Células Endoteliais/efeitos dos fármacos , Inflamação/prevenção & controle , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Aminoácidos/isolamento & purificação , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Moléculas de Adesão Celular/metabolismo , Linhagem Celular , Cucumis sativus/química , Relação Dose-Resposta a Droga , Células Endoteliais/metabolismo , Humanos , Inflamação/induzido quimicamente , Inflamação/metabolismo , Mediadores da Inflamação/metabolismo , Interleucina-6/metabolismo , Óxido Nítrico/metabolismo , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Espécies Reativas de Oxigênio/metabolismo
9.
Molecules ; 22(6)2017 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-28587132

RESUMO

The ethyl acetate extract (SsAcOEt) from Serjania schiedeana, select fractions (F-6, F-12, F-13, F-14), and one isolated compound, were evaluated in 12-O-tetradecanoylphorbol 13-acetate (TPA) ear edema and kaolin/carrageenan (KC)-induced monoarthritis assays. SsEtOAc induced edema inhibition of 90% (2.0 mg/ear), fractions showed activity within a range of 67-89%. Due to the fact F-14 showed the highest effect, it was separated, yielding a proanthocyanidin-type called epicatechin-(4ß â†’ 8)-epicatechin-(4ß â†’ 8, 2ß â†’ O → 7) epicatechin (ETP). This compound (2.0 mg/ear) provoked 72% of edema inhibition (ED50 = 0.25 mg/ear, Emax = 52.9%). After 9 days of treatment, joint inflammation was decreasing, and on the last day, SsEtOAc (400 mg/kg), F-14 and ETP (10 mg/kg), SsEtOAc (200 mg/kg), methotrexate (MTX) 1.0 mg/kg and meloxicam (MEL) 1.5 mg/kg, produced an inhibition articulate edema of 94, 62, 36, 21, 80, and 54%, respectively. In the joint, pro-inflammatory molecules were elevated in animals without treatment (vehicle group, VEH). Treatments from S. schiedeana induced a decrease in the concentration of interleukin (IL)-1ß, IL-17, and IL-6, and SsEtOAc at a higher dose diminished tumor necrosis factor (TNF-α). IL-10 and IL-4 were fewer in the VEH group in comparison with healthy mice; the animals with treatments from S. schiedeana induced an increment in the levels of these cytokines in joint and spleen.


Assuntos
Anti-Inflamatórios/farmacologia , Extratos Vegetais/farmacologia , Polímeros , Proantocianidinas/farmacologia , Sapindaceae/química , Animais , Anti-Inflamatórios/química , Artrite/tratamento farmacológico , Artrite/metabolismo , Artrite/patologia , Citocinas/metabolismo , Edema/tratamento farmacológico , Edema/metabolismo , Edema/patologia , Feminino , Mediadores da Inflamação/metabolismo , Camundongos , Estrutura Molecular , Extratos Vegetais/química , Proantocianidinas/química
10.
Planta Med ; 81(14): 1240-7, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26166136

RESUMO

In the present work, the antiarthritic activity of hautriwaic acid is reported. This ent-clerodane diterpene isolated from Dodonaea viscosa was evaluated in mice using a kaolin/carrageenan-induced monoarthritis model. The inflammation observed in the joint (knee) on days 1-8 ranged from 50-70 %. After 10 days of treatment with different doses of hautriwaic acid (5, 10, 20 mg/kg), a decrease in knee inflammation was detected. This recovery was observed with both reference drugs, methotrexate (1 mg/kg) and diclofenac (0.75 mg/kg). In these groups of mice, the concentration of proinflammatory cytokines interleukin-1 beta, interleukin-6, and tumor necrosis factor alpha in the joint was significantly lower than that of the negative control group (animals with damage without any treatment). The negative control group presented a decrease in the concentration of interleukin-10, while the groups that received hautriwaic acid at different dose exhibited an increase in this interleukin. This anti-inflammatory cytokine was not modified in the joint of mice with diclofenac, but in mice that received methotrexate, a significant decrease was observed. Hautriwaic acid isolated from D. viscosa diminished the joint edema induced by this mixture of polysaccharides (carrageenan), possibly by acting as immunomodulator of the inflammatory response.


Assuntos
Artrite Experimental/tratamento farmacológico , Diterpenos/farmacologia , Sapindaceae/química , Administração Oral , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Artrite Experimental/induzido quimicamente , Carragenina/toxicidade , Diclofenaco/farmacologia , Diterpenos/administração & dosagem , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Feminino , Interleucina-10/metabolismo , Caulim/efeitos adversos , Metotrexato/farmacologia , Camundongos Endogâmicos , Fator de Necrose Tumoral alfa/metabolismo
11.
Arch Pharm Res ; 38(7): 1369-79, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25740217

RESUMO

Bouvardia ternifolia has been used medicinally to treat inflammation. In the present study, we investigate the anti-Alzheimer's potential effect of the hydroalcoholic extract of B. ternifolia through evaluation of anti-inflammatory and antioxidant activities, quantification of the percentage inhibition of acetylcholinesterase activity, protection effect against ß-amyloid fibrillar-induce neurotoxicity, and the identification of the main constituents. Our results show that B. ternifolia extract and ethyl acetate fraction induced anti-inflammatory effects by reducing inflammation by >70 %, while antioxidant test revealed significant IC50 values for flavonoid content fraction (30.67 ± 2.09 µg/ml) and ethyl acetate fraction (42.66 ± 0.93 µg/ml). The maximum inhibition of acetylcholinesterase was exhibited by scopoletin content fraction (38.43 ± 3.94 %), while ethyl acetate fraction exerted neuroprotective effect against ß-amyloid peptide (83.97 ± 5.03 %). Phytochemical analysis, showed the presence of 3-O-quercetin glucopyranoside (415 mg/g), rutin (229.9 mg/g), ursolic and oleanolic acid (54 and 20.8 mg/g respectively), 3-O-quercetin rhamnopyranoside (12.8 mg/g), chlorogenic acid (9.5 mg/g), and scopoletin (1.38 mg/g). Our findings support the use of B. ternifolia since the extract induced significant neuroprotection against ß-amyloid peptide, anti-inflammatory, antioxidant and anti-acetylcholinesterase effects that could be attributed to its contents of polyphenols, coumarins, and triterpenes, and encourage further studies for development of this extract as therapeutic agent in treatment of Alzheimer's disease.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Rubiaceae/química , Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/antagonistas & inibidores , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/isolamento & purificação , Cumarínicos/isolamento & purificação , Cumarínicos/farmacologia , Flavonoides/farmacologia , Humanos , Fármacos Neuroprotetores/isolamento & purificação , Fragmentos de Peptídeos/antagonistas & inibidores , Fenóis/isolamento & purificação , Fenóis/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
12.
J Ethnopharmacol ; 150(3): 1032-7, 2013 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-24145005

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Castilleja tenuiflora Benth. (Orobanchaceae) is a perennial shrub used since the 16(th) century in Mexican traditional medicine for the treatment of a number of health disorders including inflammation, stomach pain and tumors. The aim of the present study was to evaluate the cytotoxic, anti-inflammatory and anti-ulcerogenic activities of ethyl acetate (EaE), methanol (ME) and aqueous extracts (AE) of Castilleja tenuiflora wild grown (CtW) and in vitro plants (CtIv). MATERIAL AND METHOD: Phytochemical analysis of the phenylethanoid glycoside (PhG) and iridoid glycoside (IG) components was carried out by chromatographic methods. In vitro cytotoxic activity of the extracts was evaluated in the following four carcinoma cell lines: colon (HF-6), breast (MCF-7), prostate (PC-3), and nasopharyngeal (KB). The topical anti-inflammatory activity was evaluated in mouse ear edema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). Anti-ulcerogenic activity was evaluated in rats using an absolute ethanol-induced acute gastric ulcer model. RESULTS: The main compounds in the extracts were isoverbascoside, verbascoside and aucubin and their concentration depended both on the solvent used and on the plant material origin. None of the extracts showed cytotoxicity against the tested cell lines. In contrast, CtWEaE, CtWAE and CtIvEaE (1.6 mg/ear) showed moderate anti-inflammatory activity similar to dexamethasone (1 mg/ear) with a 38.2, 39.3 and 49.1% decrease of inflammation, respectively. CtWEaE and CtIvEaE (100 mg/kg) showed high anti-ulcerogenic activity with 88.3 and 83.1% inhibition, respectively, compared to famotidine (20 mg/kg, 32.8% inhibition). CONCLUSION: Castilleja tenuiflora extracts provided significant gastric protection in an acute ulcer induction model and topical anti-inflammatory activity in a mouse ear edema model. These activities are related to verbascoside and may explain the traditional use of Castilleja tenuiflora in the treatment of anti-inflammatory and gastrointestinal disorders. Cultured Castilleja tenuiflora plants (in vitro) exhibited pharmacological activities and also have the potential to produce bioactive compounds.


Assuntos
Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Orobanchaceae , Extratos Vegetais/uso terapêutico , Úlcera Gástrica/tratamento farmacológico , Animais , Anti-Inflamatórios/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Etanol , Feminino , Humanos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Fitoterapia , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-Dawley , Estômago/efeitos dos fármacos , Estômago/patologia , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia
13.
J Ethnopharmacol ; 150(1): 275-9, 2013 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-24001890

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Infusions of Solanum chrysotrichum (Schldl.) or "sosa" are employed in Traditional Mexican Medicine for the local and systemic treatment of skin and mucosal infections. Different studies have verified its antifungal effectiveness and therapeutic safety in superficial mycosis caused by dermatophytes or yeasts, and have identified a group of spirostanic saponins, denominated SC-2-SC-6, as responsible for the antifungal activity. Of these, SC-2 is the most active molecule. Electron microscopy studies showed that SC-2 disintegrates cell wall and internal membranes of the fungi studied. In order to continue the systematic study of Solanum chrysotrichum, the goal of the present study was to evaluate the toxicity, genotoxicity, and cytotoxicity of the three different extracts of Solanum chrysotrichum. MATERIALS AND METHODS: From the dried leaves of Solanum chrysotrichum, we obtained the aqueous, hydroalcoholic, and ethanolic extracts. Saponins (SC-2-SC-6) were quantified by High-performance liquid chromatography (HPLC). For the toxicology study, we formed four groups: three experimental groups, treated with each of the extracts at 1-g/kg doses per os (po) during 4 weeks, and a negative control group treated with the vehicle. For the genotoxicity study, we added another group, which was treated with cyclophosphamide for 1 week. The cytotoxicity study was carried out with international methods and employing the nasopharyngeal cancer (KB) and breast cancer (MDA) cell lines. RESULTS: The three evaluated extracts did not modify either of the behavioral parameters, and on the hepatic-function biochemical tests (alanine aminotransferase [ALT] and aspartate aminotransferase [AST]), did not showed significant increase on comparing to placebo. The genotoxicity parameters did not exhibit differences between the experimental groups and the placebo (control) group. Histologic analysis showed that the three extracts caused amyloidosis and moderate necrosis in liver, and focal tumefaction in kidney, as well as significant, but clinically irrelevant, elevations of creatinine with the aqueous and hydroalcoholic, but not with the ethanolic, extracts. In addition, the aqueous and ethanolic extracts exhibited interesting cytotoxic activity against the KB cell line. CONCLUSIONS: At the doses administered, the ethanolic extract of Solanum chrysotrichum showed a slightly toxic effect on liver and kidney, without biochemical or genotoxic repercussions and with cytotoxic activity against the KB cell line.


Assuntos
Extratos Vegetais/toxicidade , Solanum , Alanina Transaminase/metabolismo , Animais , Aspartato Aminotransferases/metabolismo , Comportamento Animal/efeitos dos fármacos , Linhagem Celular Tumoral , Feminino , Humanos , Rim/efeitos dos fármacos , Rim/enzimologia , Rim/patologia , Fígado/efeitos dos fármacos , Fígado/enzimologia , Fígado/patologia , Camundongos , Camundongos Endogâmicos BALB C , Testes para Micronúcleos , Folhas de Planta
14.
Planta Med ; 79(8): 622-7, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23599006

RESUMO

The aerial parts of Ageratina pichinchensis are used in Mexican traditional medicine for the treatment of skin wounds. Recently, it was demonstrated that the aqueous extract of this plant reduced the time required to cicatrize a wound induced in the rat. The same extract showed a capability to induce overgrowth in normal fetal lung cells (MRC-5). The objective of the present study was isolating and identifying the active compounds in A. pichinchensis that are capable of inducing cellular overgrowth, as well as performing a preliminary evaluation of their anti-inflammatory and toxic effects. By means of bioguided chemical separation of an aqueous extract of A. pichinchensis, the most active compound capable of inducing cellular overgrowth was identified as 7-O-(ß-D-glucopyranosyl)-galactin. In vivo inflammation induced with carrageenan in mice was significantly reduced by the aqueous extract of A. pichinchensis, reaching a decrease of up to 60.6 %. Acute (2 g/kg) and subchronic (1 g/kg for 28 days) oral administration of the aqueous extract of this plant did not affect hepatic function (through alanine aminotransferase and aspartate aminotransferase activity evaluation), while no alterations of the histologic samples of liver and kidney were evidenced.


Assuntos
Ageratina/química , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Feminino , Humanos , Técnicas In Vitro , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/química
15.
Bol. latinoam. Caribe plantas med. aromát ; 11(6): 526-541, nov. 2012. ilus, tab
Artigo em Inglês | LILACS | ID: lil-723583

RESUMO

The hydroalcoholic extract (BtHA) and its fractions of Bouvardia ternifolia were evaluated as inhibitors of the activity of the acetylcholinesterase enzyme utilizing the in vitro method (Ellman). BtHA inhibited the acetylcholinesterase enzyme competitively (IC50 = 0.6 ug/ml); the ethyl acetate fraction (BtF-AcOEt) caused mixed-type inhibition (IC50 = 0.96 ug/ml). A fraction insoluble on methanol (Bt-Faq-1) showed a mixed-type inhibition (CI50 = 0.96 ug/ml). Finally, the methanol-soluble fraction (Bt-Faq-2), presented complex, mixed-type inhibition that corresponds to the C5 system ( alpha= 0.740 and beta = 0.842). Rutin, quercetin, kaempferol and ursolic acid were detected by HPLC and the concentration of these compounds was different in each fraction.


El extracto hidroalcohólico (BtHA) y fracciones provenientes de Bouvardia ternifolia fueron evaluadas como inhibidores de la enzima acetilcolinesterasa utilizando el método enzimático propuesto por Ellman. BtHA inhibe a la enzima de manera competitiva (IC50 = 0.6 ug/ml); la fracción de acetato de etilo (BtF-AcOEt) provoca una inhibición mixta (IC50 = 0.96 ug/ml). La fracción insoluble en metanol (Bt-Faq-1) mostró una inhibición tipo mixta (CI50 = 0.96 ug/ml). Finalmente la fracción soluble en metanol, Bt-Faq-2, inhibe a la enzima presentando una inhibición mixta que corresponde a un sistema C5 ( alfa= 0.740 and beta= 0.842). Mediante HPLC se detectó rutina, quercetina, canferol y ácido ursólico la concentración de estos compuestos fue diferente en cada fracción.


Assuntos
Animais , Ratos , Acetilcolinesterase , Extratos Vegetais/farmacologia , Inibidores da Colinesterase/farmacologia , Rubiaceae/química , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Solução Hidroalcoólica , Metanol , Triterpenos/análise
16.
J Altern Complement Med ; 18(6): 607-11, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22784348

RESUMO

OBJECTIVES: Interdigital tinea pedis is the most frequent presentation, as well as the most severe clinical form of tinea pedis, constituting a therapeutic challenge. The aim of the study was to evaluate the effectiveness and tolerability of two concentrations of Ageratina pichinchensis extract (encecalin content, 0.76 and 1.52%, respectively) on patients with clinical and mycological diagnosis of chronic interdigital tinea pedis. DESIGN: By means of a randomized, double-blind clinical trial, three groups of patients were treated topically for 4 weeks with a cream containing the following: Group I-the lower concentration of A. pichinchensis extract, group II-the higher concentration, group III-2% ketoconazole. SUBJECTS: One hundred and sixty (160) ambulatory patients of either sex between the ages of 18 and 65 years were enrolled. OUTCOME MEASURES: The primary outcome variables were: clinical effectiveness, mycological effectiveness, therapeutic cure, tolerability, and treatment compliance. The secondary outcome variable was therapeutic success. RESULTS: At the end of treatment, therapeutic cure was achieved by 34.1, 41.8, and 39.53% of Groups I, II, and III, respectively. No statistical difference between the groups was observed. CONCLUSIONS: Both treatments were effective for the treatment of interdigital-type tinea pedis, while better results were observed on patients that received the higher concentration of the extract.


Assuntos
Ageratina , Antifúngicos/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Tinha dos Pés/tratamento farmacológico , Administração Tópica , Adolescente , Adulto , Idoso , Antifúngicos/farmacologia , Método Duplo-Cego , Esquema de Medicação , Feminino , Humanos , Cetoconazol/farmacologia , Cetoconazol/uso terapêutico , Masculino , Pessoa de Meia-Idade , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Tinha dos Pés/microbiologia , Dedos do Pé , Resultado do Tratamento , Adulto Jovem
17.
Planta Med ; 78(4): 304-10, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22174074

RESUMO

The aerial parts of the species Ageratina pichinchensis, popularly known as "axihuitl", have been empirically used in Mexico for wound-healing purposes. The evaluation of an extract from A. pichinchensis (in an in vivo model) demonstrated its capacity to reduce, in a significant manner, the time required for wound healing in rodent skin. This same extract showed (in vitro) a capacity of encouraging proliferation of normal human fetal lung fibroblasts (MRC-5). This study's objective was to evaluate, in a clinical trial, the effectiveness and tolerability of the topical administration of a product elaborated with the standardized extract from the aerial parts of A. pichinchensis in patients with chronic venous leg ulcers, and to compare the effect with a control group treated with 7 % propylene glycol alginate. In this study, a total of 34 patients were included (50 % in each group). Six patients of the control group withdrew from the treatment, three of these because of lack of recovery. In the experimental group, 2 participants withdrew from the study, but none of these due to treatment or clinical-evolution reasons. The A. pichinchensis extract showed therapeutic effectiveness in one hundred percent of the patients treated with it, while the control treatment achieved this condition in 81.8 % of the control group patients. Ulcer size reduction resulted significantly higher (p < 0.010) in the group of patients administered the experimental treatment, which allows us to assure that the A. pichinchensis standardized extract is effective in the treatment of chronic venous leg ulcers and, compared with the 7 % propylene glycol alginate formula, achieves a significant reduction of the time required for the ulcers to heal.


Assuntos
Ageratina/química , Fitoterapia/métodos , Extratos Vegetais/uso terapêutico , Úlcera Varicosa/tratamento farmacológico , Alginatos/uso terapêutico , Anti-Infecciosos/uso terapêutico , Doença Crônica , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Componentes Aéreos da Planta/química , Resultado do Tratamento
18.
Am J Chin Med ; 35(6): 1037-46, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-18186589

RESUMO

Insulin resistance, which precedes type 2 diabetes mellitus (T2DM), is a widespread pathology associated with the metabolic syndrome, myocardial ischemia, and hypertension. Finding an adequate treatment for this pathology is an important goal in medicine. The purpose of the present research was to investigate the effect of an extract from Aloe vera gel containing a high concentration of polyphenols on experimentally induced insulin resistance in mice. A polyphenol-rich Aloe vera extract (350 mg/kg) with known concentrations of aloin (181.7 mg/g) and aloe-emodin (3.6 mg/g) was administered orally for a period of 4 weeks to insulin resistant ICR mice. Pioglitazone (50 mg/kg) and bi-distilled water were used as positive and negative controls respectively. Body weight, food intake, and plasma concentrations of insulin and glucose were measured and insulin tolerance tests were performed. The insulin resistance value was calculated using the homeostasis model assessment for insulin resistance (HOMA-IR) formula. Results showed that the polyphenol-rich extract from Aloe vera was able to decrease significantly both body weight (p < 0.008) and blood glucose levels (p < 0.005) and to protect animals against unfavorable results on HOMA-IR, which was observed in the negative control group. The highest glucose levels during the insulin tolerance curve test were in the negative control group when compared to the Aloe vera extract and pioglitazone treated mice (p < 0.05). In conclusion, Aloe vera gel could be effective for the control of insulin resistance.


Assuntos
Aloe , Flavonoides/farmacologia , Resistência à Insulina/fisiologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Animais , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Peso Corporal/efeitos dos fármacos , Peso Corporal/fisiologia , Modelos Animais de Doenças , Ingestão de Alimentos/efeitos dos fármacos , Ingestão de Alimentos/fisiologia , Hipoglicemiantes/farmacologia , Insulina/sangue , Masculino , Camundongos , Camundongos Endogâmicos ICR , Pioglitazona , Polifenóis , Distribuição Aleatória , Tiazolidinedionas/farmacologia
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