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1.
Chem Biodivers ; 20(5): e202200969, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36973180

RESUMO

Distictis buccinatoria is used for inflammatory-related diseases. From a dichloromethane extract were obtained five different fractions called F1 to F5, and sub-fractions F4-1, F5-1, F5-2, and F5-3; and were evaluated as anti-neuroinflammatory, antioxidant, and nootropic agents in mice exposed to lipopolysaccharide. Also, were isolated herniarin, daphnoretin, and fraction's terpenes with an anti-inflammatory activity using 12-O-tetradecanoylphorbol-13-acetate-induced auricular edema. The inhibition of local edema was: F1 (73.6 %), F2 (57 %), F3 (62.61 %), F4 (87.3 %), and F5 (93.57 %). Terpene fraction inhibited at 89.60 %, herniarin at 86.92 % (Emax 99.01 %, ED50 0.35 mg ear-1 ), and daphnoretin at 86.41 %. Fractions F4-1 and F5-2 (10 mg kg-1 ) enhancer spatial memory acquisition and spontaneous motor activity; reduced IL-1ß, TNF-α, and IL-6; increased IL-10, enhanced the activity of CAT and GR. D. buccinatoria has neuroprotective activity and contains daphnoretin and herniarin, with anti-inflammatory activity.


Assuntos
Fármacos Neuroprotetores , Extratos Vegetais , Camundongos , Animais , Extratos Vegetais/farmacologia , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Edema/induzido quimicamente , Edema/tratamento farmacológico
2.
Molecules ; 28(14)2023 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-37513187

RESUMO

The negative impact on worldwide social well-being by the increasing rate of psychiatric diseases has led to a continuous new drug search. Even though the current therapeutic options exert their activity on multiple neurological targets, these have various adverse effects, causing treatment abandonment. Recent research has shown that Coriandrum sativum offers a rich source of metabolites, mainly terpenes and flavonoids, as useful agents against central nervous system disorders, with remarkable in vitro and in vivo activities on models related to these pathologies. Furthermore, studies have revealed that some compounds exhibit a chemical interaction with γ-aminobutyric acid, 5-hydroxytryptamine, and N-methyl-D-aspartate receptors, which are key components in the pathophysiology associated with psychiatric and neurological diseases. The current clinical evaluations of standardized extracts of C. sativum are scarce; however, one or more of its compounds represents an area of opportunity to test the efficacy of the plant as an anxiolytic, antidepressant, antiepileptic, or sleep enhancer. For this, the aim of the review was based on the pharmacological activities offered by the compounds identified and isolated from coriander and the processes involved in achieving their effect. In addition, lines of technological research, like molecular docking and nanoparticles, are proposed for the future development of phytomedicines, based on the bioactive molecules of C. sativum, for the treatment of psychiatric and neurological disorders addressed in the present study.


Assuntos
Ansiolíticos , Coriandrum , Transtornos Mentais , Humanos , Coriandrum/química , Simulação de Acoplamento Molecular , Ansiolíticos/farmacologia , Ansiolíticos/uso terapêutico , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , Antidepressivos/metabolismo , Transtornos Mentais/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/metabolismo
3.
Molecules ; 27(21)2022 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-36364031

RESUMO

Agave angustifolia is a xerophytic species widely used in Mexico as an ingredient in sweet food and fermented beverages; it is also used in traditional medicine to treat wound pain and rheumatic damage, and as a remedy for psoriasis. Among the various A. angustifolia extracts and extract fractions that have been evaluated for their anti-inflammatory effects, the acetonic extract (AaAc) and its acetonic (F-Ac) and methanolic (F-MeOH) fractions were the most active in a xylene-induced ear edema model in mice, when orally administered. Four fractions resulting from chemically resolving F-Ac (F1-F4) were locally applied to mice with phorbol 12-myristate 13-acetate (TPA)-induced ear inflammation; F1 inhibited inflammation by 70% and was further evaluated in a carrageenan-induced mono-arthritis model. When administered at doses of 12.5, 25, and 50 mg/kg, F1 reduced articular edema and the spleen index. In addition, it modulated spleen and joint cytokine levels and decreased pain. According to a GC-MS analysis, the main components of F1 are fatty-acid derivatives: palmitic acid methyl ester, palmitic acid ethyl ester, octadecenoic acid methyl ester, linoleic acid ethyl ester, and oleic acid ethyl ester.


Assuntos
Agave , Camundongos , Animais , Anti-Inflamatórios/uso terapêutico , Extratos Vegetais/uso terapêutico , Ácidos Graxos/uso terapêutico , Edema/induzido quimicamente , Edema/tratamento farmacológico , Carragenina/efeitos adversos , Dor/tratamento farmacológico , Ésteres , Fitoterapia
4.
Euro Surveill ; 26(47)2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34823642

RESUMO

IntroductionKnowing the factors associated with HIV transmission is necessary in order to design preventive programmes tailored to the epidemiological situation in each region and population.AimOur objective was to study the sociodemographic, clinical and behavioural characteristics of men who have sex with men (MSM) who were newly diagnosed with HIV infection.MethodsWe carried out an observational, descriptive, study on all MSM newly diagnosed with HIV infection in one clinic for sexually transmitted infections (STI) and HIV clinic in Madrid between 2014 and 2019. Information on sociodemographic, clinical, and behavioural characteristics of participants per year of diagnosis was collected.ResultsWe detected a total of 1,398 people with HIV infection, 253 of whom were recent seroconverters (rSCV) with a median duration of documented seroconversion of 6 months. From the total, 97.9% infections were sexually transmitted and 2.1% involved injected drugs, i.e. slam practices. The average age was 32.9 years (range: 15.6-74.9), 51.8% were Spanish and 40% Latin American. These diagnoses decreased in Spanish people and increased in Latin Americans during the study period. Of the rSCV, 73.9% had condomless sex under the influence of drugs and 28.9% participated in chemsex sessions. Apps were used by 92.6% rSCV for sexual encounters and 70.4% of them attributed HIV transmission to their use.ConclusionsCombination of HIV prevention strategies, as pre-exposure prophylaxis, should be reinforced among young MSM, especially those born in Latin America, those who use drugs for sex, and those who use apps in search of sexual contacts.


Assuntos
Infecções por HIV , Minorias Sexuais e de Gênero , Infecções Sexualmente Transmissíveis , Adulto , Infecções por HIV/diagnóstico , Infecções por HIV/epidemiologia , Homossexualidade Masculina , Humanos , Masculino , Comportamento Sexual , Infecções Sexualmente Transmissíveis/diagnóstico , Infecções Sexualmente Transmissíveis/epidemiologia , Sexo sem Proteção
5.
Chem Biodivers ; 18(3): e2000790, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33527713

RESUMO

Argemone mexicana L. is a widely used plant in Mexican traditional medicine to treat inflammatory and nervous medical conditions. It has been subjected to several pharmacological and chemical studies in which acute anti-inflammatory activity is indicated. This work aimed at finding an extract and fraction with anti-inflammatory activity by means of 2-O-tetradecanoylphorbol-13-acetate (TPA)-induced auricular edema. Afterward, the extract and the fraction were tested on neuroinflammation caused by lipopolysaccharides (LPS). Treatments obtained from A. mexicana included the methanolic extract (AmMeOH), a fraction extracted with ethyl acetate (AmAcOEt), and four sub-fractions (AmF-1 to AmF-4), which were evaluated in auricular edema with the TPA assay. Both treatments with the most significant inhibitory effect were employed to test these in the LPS neuroinflammation model. AmAcOEt and AmF-3 induced a higher inhibition of edema (%), and both diminished ear inflammation when viewed under a microscope. These treatments also raised an increase in spleen, but not in brain of mice with neuroinflammation. They were able to decrease the concentration of proinflammatory cytokines (TNF-α, IL-1ß, and IL-6) in both organs. Furthermore, the accumulation of amyloid-ß (Aß) in hippocampus was not visible. AmF-3 contains the flavonoids isoquercetin, luteolin, and rutin, the former being the most concentrated.


Assuntos
Anti-Inflamatórios/farmacologia , Argemone/química , Edema/tratamento farmacológico , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/patologia , Inflamação/induzido quimicamente , Inflamação/patologia , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
6.
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
7.
Molecules ; 26(15)2021 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-34361655

RESUMO

Pterygium is a corneal alteration that can cause visual impairment, which has been traditionally treated with the sap of Sedum dendroideum D.C. The pharmacological effect of a dichloromethane extract of S. dendroideum was demonstrated and implemented in a pterygium model on the healing process of corneal damage caused by phorbol esters. In mice of the ICR strain, a corneal lesion was caused by intravitreal injection of tetradecanoylphorbol acetate (TPA). The evolution of the corneal scarring process was monitored with vehicle, dexamethasone, and dichloromethane extract of S. dendroideum treatments by daily ophthalmic administration for fifteen days. The lesions were evaluated in situ with highlighted images of fluorescence of the lesions. Following treatment levels in eyeballs of IL-1α, TNF-α, and IL-10 cytokines were measured. The effective dose of TPA to produce a pterygium-like lesion was determined. The follow-up of the evolution of the scarring process allowed us to define that the treatment with S. dendroideum improved the experimental pterygium and had an immunomodulatory effect by decreasing TNF-α, IL-1α, and maintaining the level of IL-10 expression, without difference with respect to the healthy control. Traditional medical use of S. dendroideum sap to treat pterygium is fully justified by its compound composition.


Assuntos
Anti-Inflamatórios/farmacologia , Túnica Conjuntiva/anormalidades , Cloreto de Metileno/farmacologia , Extratos Vegetais/farmacologia , Pterígio/tratamento farmacológico , Cicatrização/efeitos dos fármacos , Animais , Masculino , Camundongos , Camundongos Endogâmicos ICR , Sedum/química
8.
Med Princ Pract ; 29(2): 113-120, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31466071

RESUMO

OBJECTIVE: To evaluate the antidepressant effect of Bauhinia blakeana and a standardized fraction in the forced swimming test (FST) on mice with neuroinflammation induced with lipopolysaccharides (LPS). MATERIALS AND METHODS: Evaluation of the antidepressant effect of Bauhinia blakeana hydroalcoholic extract (BbHA) and its fractions was carried out in behavioral tests on mice with LPS-induced neuroinflammation. RESULTS: BbHA had a significant antidepressant effect, measured on healthy mice in the FST. Bio-guided chemical separation of the extract produced a methanolic fraction (BbMe), which decreased the immobility time in FST. In this test, the intraperitoneal administration of LPS induced depression in mice, and BbHA and BbMe counteracted this effect, significantly decreasing the induced depression. Quantification of inflammatory mediators (IL-10, IL-4, IL-6, IL-1ß, and TNF-α) in the brain demonstrated that BbHA and BbMe effectively decreased the effect of LPS on the brain concentration of all measured cytokines. CONCLUSIONS: Bauhinia blakeana produced an antidepressant effect, while BbMe also exerted a modulating effect, on the damage induced by LPS. Rutin, a glycosylated flavonoid, was identified as the main compound in the active fraction, which could mediate in the antidepressant and immunomodulatory effect.


Assuntos
Antidepressivos/farmacologia , Bauhinia/efeitos dos fármacos , Encéfalo/efeitos dos fármacos , Depressão/tratamento farmacológico , Animais , Citocinas/análise , Modelos Animais de Doenças , Inflamação , Masculino , Camundongos , Camundongos Endogâmicos ICR , Natação
9.
J Neuroinflammation ; 16(1): 143, 2019 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-31291963

RESUMO

BACKGROUND: Alzheimer's disease (AD) is a neuropathology strongly associated with the activation of inflammatory pathways. Accordingly, inflammation resulting from obesity exacerbates learning and memory deficits in humans and in animal models of AD. Consequently, the long-term use of non-steroidal anti-inflammatory agents diminishes the risk for developing AD, but the side effects produced by these drugs limit their prophylactic use. Thus, plants natural products have become an excellent option for modern therapeutics. Malva parviflora is a plant well known for its anti-inflammatory properties. METHODS: The present study was aimed to determine the anti-inflammatory potential of M. parviflora leaf hydroalcoholic extract (MpHE) on AD pathology in lean and obese transgenic 5XFAD mice, a model of familial AD. The inflammatory response and Amyloid ß (Aß) plaque load in lean and obese 5XFAD mice untreated or treated with MpHE was evaluated by immunolocalization (Iba-1 and GFAP) and RT-qPCR (TNF) assays and thioflavin-S staining, respectively. Spatial learning memory was assessed by the Morris Water Maze behavioral test. Microglia phagocytosis capacity was analyzed in vivo and by ex vivo and in vitro assays, and its activation by morphological changes (phalloidin staining) and expression of CD86, Mgl1, and TREM-2 by RT-qPCR. The mechanism triggered by the MpHE was characterized in microglia primary cultures and ex vivo assays by immunoblot (PPAR-γ) and RT-qPCR (CD36) and in vivo by flow cytometry, using GW9662 (PPAR-γ inhibitor) and pioglitazone (PPAR-γ agonist). The presence of bioactive compounds in the MpHE was determined by HPLC. RESULTS: MpHE efficiently reduced astrogliosis, the presence of insoluble Aß peptides in the hippocampus and spatial learning impairments, of both, lean, and obese 5XFAD mice. This was accompanied by microglial cells accumulation around Aß plaques in the cortex and the hippocampus and decreased expression of M1 inflammatory markers. Consistent with the fact that the MpHE rescued microglia phagocytic capacity via a PPAR-γ/CD36-dependent mechanism, the MpHE possess oleanolic acid and scopoletin as active phytochemicals. CONCLUSIONS: M. parviflora suppresses neuroinflammation by inhibiting microglia pro-inflammatory M1 phenotype and promoting microglia phagocytosis. Therefore, M. parviflora phytochemicals represent an alternative to prevent cognitive impairment associated with a metabolic disorder as well as an effective prophylactic candidate for AD progression.


Assuntos
Doença de Alzheimer , Encéfalo/efeitos dos fármacos , Disfunção Cognitiva/patologia , Microglia/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Encéfalo/patologia , Disfunção Cognitiva/etiologia , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Malva , Aprendizagem em Labirinto/efeitos dos fármacos , Camundongos , Camundongos Transgênicos , Microglia/metabolismo , PPAR gama/metabolismo , Fagocitose/efeitos dos fármacos , Folhas de Planta
10.
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
11.
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
12.
Acta Neurochir (Wien) ; 160(12): 2489-2500, 2018 12.
Artigo em Inglês | MEDLINE | ID: mdl-30413938

RESUMO

BACKGROUND: Stereoelectroencephalography (SEEG) is an effective technique to help to locate and to delimit the epileptogenic area and/or to define relationships with functional cortical areas. We intend to describe the surgical technique and verify the accuracy, safety, and effectiveness of robot-assisted SEEG in a newly created SEEG program in a pediatric center. We focus on the technical difficulties encountered at the early stages of this program. METHODS: We prospectively collected SEEG indication, intraoperative events, accuracy calculated by fusion of postoperative CT with preoperative planning, complications, and usefulness of SEEG in terms of answering preimplantation hypothesis. RESULTS: Fourteen patients between the ages of 5 and 18 years old (mean 10 years) with drug-resistant epilepsy were operated on between April 2016 and April 2018. One hundred sixty-four electrodes were implanted in total. The median entry point localization error (EPLE) was 1.57 mm (1-2.25 mm) and the median target point localization error (TPLE) was 1.77 mm (1.2-2.6 mm). We recorded seven intraoperative technical issues. Two patients suffered complications: meningitis without demonstrated germ in one patient and a right frontal hematoma in the other. In all cases, the SEEG was useful for the therapeutic decision-making. CONCLUSION: SEEG has been useful for decision-making in all our pediatric patients. The robotic arm is an accurate tool for the insertion of the deep electrodes. Nevertheless, it is an invasive technique not risk-free and many problems can appear at the beginning of a robotic arm-assisted SEEG program that must be taken into account beforehand.


Assuntos
Epilepsia Resistente a Medicamentos/cirurgia , Eletroencefalografia/métodos , Complicações Pós-Operatórias/epidemiologia , Robótica/métodos , Técnicas Estereotáxicas/efeitos adversos , Adolescente , Criança , Pré-Escolar , Tomada de Decisão Clínica , Epilepsia Resistente a Medicamentos/diagnóstico , Eletrodos Implantados/efeitos adversos , Eletrodos Implantados/normas , Eletroencefalografia/efeitos adversos , Eletroencefalografia/instrumentação , Eletroencefalografia/normas , Feminino , Humanos , Masculino , Robótica/instrumentação , Robótica/normas , Técnicas Estereotáxicas/instrumentação , Técnicas Estereotáxicas/normas
13.
Molecules ; 22(6)2017 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-28587079

RESUMO

In this work, the immunomodulatory activity of the acetone extract and the fructans obtained from Agave tequilana were evaluated, on the systemic autoimmunity type-SLE model generated by the administration of 2,6,10,14-tetramethylpentadecane (TMPD, also known as pristane) on Balb/c female mice. The systemic autoimmunity type-SLE was observed seven months after the application of TMPD, in which the animals from the negative control group (animals with damage and without any other treatment) developed articular inflammation, proteinuria, an increment of the antinuclear antibody titters and tissue pro-inflammatory cytokines levels (IL-1ß, IL-6, TNF-α e IFN-γ) as well as the anti-inflammatory cytokine IL-10. The administration of the different treatments and the extracts of A. tequilana, provoked the decrease of: articular inflammation, the development of proteinuria, ssDNA/dsDNA antinuclear antibody titters and cytokines IL-1ß, IL-6, TNF-α, IFN-γ and IL-10. The phytochemical analysis of the acetone extract identified the presence of the following compounds: ß-sitosterol glycoside; 3,7,11,15-tetramethyl-2-hexadecen-1-ol (phytol); octadecadienoic acid-2,3-dihydroxypropyl ester; stigmasta-3,5-dien-7-one; cycloartenone and cycloartenol. Therefore, A. tequilana contains active compounds with the capacity to modify the evolution of the systemic autoimmunity type-SLE on a murine model.


Assuntos
Agave/química , Autoimunidade/efeitos dos fármacos , Fatores Imunológicos/farmacologia , Lúpus Eritematoso Sistêmico/imunologia , Extratos Vegetais/farmacologia , Terpenos/efeitos adversos , Animais , Autoanticorpos/sangue , Autoanticorpos/imunologia , Citocinas/metabolismo , Modelos Animais de Doenças , Ensaio de Imunoadsorção Enzimática , Feminino , Articulação do Joelho/efeitos dos fármacos , Articulação do Joelho/imunologia , Articulação do Joelho/metabolismo , Articulação do Joelho/patologia , Lúpus Eritematoso Sistêmico/tratamento farmacológico , Lúpus Eritematoso Sistêmico/metabolismo , Lúpus Eritematoso Sistêmico/patologia , Camundongos , Camundongos Endogâmicos BALB C
14.
Molecules ; 22(8)2017 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-28749448

RESUMO

An anxiolytic fraction of Tilia americana standardized in tiliroside, rutin, quercitrin, quercetin glucoside, and kaempferol was obtained. After oral administration of the fraction, the above-mentioned flavonoids were not detected in plasma over 24 h. However, meta and para hydroxyphenylacetic acid and dihydroxyphenylacetic acid (m-HPAA, p-HPAA and DOPAC) were monitored. These are the biotransformation compounds of the aglycones of kaempferol and quercetin; these aglycones are products of the other flavonoids present in the anxiolytic fraction. The analytical methods (HPLC) for flavonoids and the related compounds (m-HPAA, p-HPAA and DOPAC) were validated, determining the parameters of accuracy, precision, specificity or selectivity, limit of detection, quantification range, and robustness. The pharmacokinetic assay was performed with ICR mice strains, which were given 200 mg/kg of the standardized active fraction. The results of validation of the analytical methods were obtained, allowing it to be established in a validated way that no flavonoids present in the anxiolytic fraction of T. americana were detected in plasma. However, detection and follow up was possible for the serum levels of m-HPAA, p-HPAA, and DOPAC. The three compounds follow a two-compartment model with very similar parameters between m-HPAA and p-HPAA, some being different from the ones characterized in the pharmacokinetics of DOPAC.


Assuntos
Ansiolíticos/farmacocinética , Extratos Vegetais/farmacocinética , Tilia/química , Administração Oral , Análise de Variância , Animais , Ansiolíticos/administração & dosagem , Biotransformação , Fracionamento Químico , Cromatografia Líquida de Alta Pressão , Flavonoides/sangue , Flavonoides/química , Camundongos Endogâmicos ICR , Extratos Vegetais/administração & dosagem , Padrões de Referência
15.
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
16.
Neurol India ; 65(4): 808-813, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28681757

RESUMO

Chordoid glioma (CG) of the third ventricle is an unusual neoplasm of glial nature, which is almost exclusively located in the anterior wall of the third ventricle, in close relation with the hypothalamus. Magnetic resonance images show CG as a suprasellar, hypo- to isointense mass, homogeneously enhancing after the administration of gadolinium. Since its description in 1998 by Brat et al., approximately 85 cases have been reported. Some of its pathological features are under discussion and its histological origin still remains unclear. In this study, we present a patient having this rare entity. We review the management of CG reported in literature. We also studied its pathological features, the postoperative mortality and morbidity related to radical surgical resection, and the implemented adjuvant therapies. Due to its classical clinical features and its close resemblance to other lesions in the region, it is an entity unlikely to be suspected prior to its histological diagnosis. Despite the benign nature of this tumor, the clinical outcome might be poor. Its treatment may represent a real challenge because it involves critical anatomical areas, leading to high postoperative morbidity and mortality rates. An initial minimally invasive management and adjuvant therapies, such as radiosurgery, in case of symptomatic recurrences, can be effective handling strategies.


Assuntos
Neoplasias do Ventrículo Cerebral/terapia , Glioma/terapia , Terceiro Ventrículo , Neoplasias do Ventrículo Cerebral/patologia , Neoplasias do Ventrículo Cerebral/cirurgia , Terapia Combinada , Gerenciamento Clínico , Feminino , Glioma/patologia , Glioma/cirurgia , Humanos , Imageamento por Ressonância Magnética , Pessoa de Meia-Idade , Procedimentos Neurocirúrgicos , Complicações Pós-Operatórias/epidemiologia , Complicações Pós-Operatórias/mortalidade , Síndrome das Pernas Inquietas/etiologia , Resultado do Tratamento
17.
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
18.
Acta Neurochir (Wien) ; 157(9): 1495-503; discussion 1503, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26163258

RESUMO

BACKGROUND: When performing a transplanum transtuberculum approach, dealing with the anterior communicating artery (ACoA) complex is inevitable. The aim of this study is to provide quantitative anatomical information regarding the ACoA complex and its bony and neural relationships, when exposed through this approach. METHOD: The endoscopic endonasal transplanum transtuberculum approach was performed on ten human cadaver heads. In each specimen, radiological studies were performed. A three-dimensional model of the approach was reconstructed. Measured parameters were: exposure of the vessels; distance between the proximal anterior cerebral artery (A1) and the optic chiasm; dimension of the bone opening. The feasibility to perform clip placement was graded as "possible" or "not possible". RESULTS: Dimension of bone opening varied from 88 to 53 mm(2). The ACoA was exposed for 3 mm ± 2 mm, A1 for 17 mm ± 9 mm, the distal anterior cerebral artery (A2) for 12 mm ± 3 mm, the recurrent artery of Heubner (RAH) for 16 mm ± 4 mm. Clip placement was possible on the ACoA, A2, and distal segment of A1 in all cases, and on the proximal segment of A1 in one instance. The distance between A1 and the optic chiasm measured 9 mm ± 2 mm. CONCLUSIONS: The ACoA, A2, and the distal segment of A1 can be visualized and controlled through the transplanum transtuberculum approach. The relationship between A1, gyrus rectus, and optic chiasm is the main determinant for the exposure and control of the vessel. The olfactory nerve can represent a surgical landmark for the identification of the A1 origin. The whole course of the RAH can be visualized trough this approach.


Assuntos
Artéria Cerebral Anterior/cirurgia , Cirurgia Endoscópica por Orifício Natural/métodos , Procedimentos Neurocirúrgicos/métodos , Artéria Cerebral Anterior/anatomia & histologia , Humanos
19.
Planta Med ; 80(1): 90-6, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24338551

RESUMO

Galphimia glauca, commonly known as "flor de estrella", is a plant species used in Mexican traditional medicine for the treatment of different diseases that have an acute or chronic inflammatory process in common. Aerial parts of this plant contain nor-seco-triterpenoids with anxiolytic properties, which have been denominated galphimines. Other compounds identified in the plant are tetragalloyl-quinic acid, gallic acid, and quercetin, which are able to inhibit the bronchial obstruction induced by platelet-activating factor. The objective of this work was to evaluate the anti-inflammatory effect of crude extracts from G. glauca and, by means of bioguided chemical separation, to identify the compounds responsible for this pharmacological activity. n-Hexane, ethyl acetate, dichloromethane, and methanol extracts showed an important anti-inflammatory effect. Chemical separation of the active methanol extract allowed us to identify the nor-seco-triterpenes galphimine-A (1) and galphimine-E (3) as the anti-inflammatory principles. Analysis of structure-activity relationships evidenced that the presence of an oxygenated function in C6 is absolutely necessary to show activity. In this work, the isolation and structural elucidation of two new nor-seco-triterpenes denominated as galphimine-K (4) and galphimine-L (5), together with different alkanes, fatty acids, as well as three flavonoids (17-19), are described, to our knowledge for the first time, from Galphimia glauca.


Assuntos
Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Galphimia/química , Extratos Vegetais/química , Animais , Edema/induzido quimicamente , Edema/tratamento farmacológico , Galphimia/metabolismo , Masculino , Medicina Tradicional , Camundongos , Camundongos Endogâmicos ICR , Estrutura Molecular , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Metabolismo Secundário , Relação Estrutura-Atividade , Acetato de Tetradecanoilforbol/toxicidade , Triterpenos/química , Triterpenos/farmacologia
20.
Molecules ; 19(3): 3120-34, 2014 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-24625685

RESUMO

The aim of this study was to obtain pharmacokinetic data for the anxiolytic compound galphimine-A (G-A) from Galphimia glauca. G-A is the most abundant anxiolytic compound in this plant, while Galphimine-E (G-E) is the most abundant galphimine, but inactive. G-E was transformed chemically into G-A. The pharmacokinetic study was carried out in ICR mice, which were orally administered a single 200 mg/kg dose of G-A. Samples of blood and brain were taken at different times after administration of G-A. Previously, we established the validation of methods for determining the concentration of G-A. The G-A was detected in plasma 5 min after oral administration, and its concentration reached 2.47 µg/mL. Data from concentration-time curves allowed us to establish the main pharmacokinetic parameters in two models: one- and/or two-compartment. C(max) values were 3.33 and 3.42 µg/mL respectively, likewise AUC(0→1440 min) were 1,951.58 and 1,824.95 µg/mL·min. The G-A in brain tissue was noted to cross the blood-brain barrier, reaching C(max) 2.74 µg/mL, T(max) 81.6 min, and then drop gradually to 0.32 µg/mL detected at 24 h. The presence of G-A in brain tissue, confirmed that this anxiolytic compound can access the target organ and acts directly on the CNS.


Assuntos
Ansiolíticos/química , Ansiolíticos/farmacocinética , Galphimia/química , Triterpenos/química , Triterpenos/farmacocinética , Administração Oral , Animais , Encéfalo/metabolismo , Cromatografia Líquida de Alta Pressão , Estabilidade de Medicamentos , Camundongos , Extratos Vegetais/química , Reprodutibilidade dos Testes
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