RESUMO

The antihyperglycemic activity of ethanolic extract from Salvia polystachya (EESpS) and its products was evaluated using in vivo, ex vivo and in silico assays; additionally, an acute toxicity assay was evaluated. EESpS was classified as a nontoxic class 5 drug. EESpS, ethyl acetate fraction (EtOAcFr), secondary-6-fraction (SeFr6), ursolic acid (UA), and oleanolic acid (OA) reduced the hyperglycemia in DM2 mice. α-glucosidase inhibition was evaluated with oral sucrose and starch tolerance tests (OSuTT and OStTT), an intestinal sucrose hydrolysis (ISH) assay and molecular docking studies using acarbose as control. SGLT1 inhibition was evaluated with oral glucose and galactose tolerance tests (OGTT and OGaTT), an intestinal glucose absorption (IGA) assay and molecular docking studies using canagliflozin as the control. During the carbohydrate tolerance tests, all the treatments reduced the postprandial peak, similar to the control drugs. During the ISH, IC50 values of 739.9 and 726.3 µM for UA and OA, respectively, were calculated. During the IGA, IC50 values of 966.6 and 849.3 for UA, OA respectively, were calculated. Finally, during the molecular docking studies, UA and OA showed ∆G values of -6.41 and -5.48 kcal/mol-1, respectively, on α-glucosidase enzymes. During SGLT1, UA and OA showed ∆G values of -10.55 and -9.65, respectively.

RESUMO

Abstract Metabolic syndrome (MetS), an epidemic defined as a group of interconnected physiological, biochemistry, clinical, and metabolic factors, directly increases the risk of cardiovascular disease, atherosclerosis, type 2 diabetes, and death. MetS therapy includes diet, physical exercise, and a poly-pharmacological intervention. Cannabis is mainly recognized for its recreational uses and has several medical applications for neurological diseases, due to its hypnotic, anxiolytic, antinociceptive, anti-inflammatory, and anticonvulsant activities. Although several clinical observations in Cannabis smokers suggest metabolic effects, its utility in metabolic disorders is unclear. This review aims to determine under what conditions Cannabis might be useful in the treatment of MetS. Cannabis contains 120 phytocannabinoids, of which Δ9-THC mediates its psychoactive effects. Cannabinoids exert biological effects through interactions with the endocannabinoid system, which modulates several physiologic and metabolic pathways through cannabinoid receptors (CB1/CB2). Signaling through both receptors inhibits neurotransmitter release. In general, endocannabinoid system stimulation in Cannabis smokers and Δ9-THC signaling through CB1 have been implicated in MetS development, obesity, and type 2 diabetes. In contrast, CB1 antagonists and non-psychotropic phytocannabinoids like cannabidiol reduce these effects through interactions with both cannabinoid and non-cannabinoid receptors. These pharmacological approaches represent a source of new therapeutic agents for MetS. However, more studies are necessary to support the therapeutic potential of Cannabis and cannabinoids in metabolic abnormalities

Assuntos

Cannabis/efeitos adversos , Síndrome Metabólica/tratamento farmacológico , Bioquímica/classificação , Canabinoides/efeitos adversos , Doenças Cardiovasculares , Receptores de Canabinoides/análise , Receptor CB1 de Canabinoide/antagonistas & inibidores , Diabetes Mellitus/patologia , Aterosclerose/patologia , Anticonvulsivantes/classificação

RESUMO

OBJECTIVE: To determine the involvement of TNF-α and glycine receptors in the inhibition of pro-inflammatory adipokines in 3T3-L1 cells. METHODS: RT-PCR evidenced glycine receptors in 3T3-L1 adipocytes. 3T3-L1 cells were transfected with siRNA for the glycine (Glrb) and TNF1a (Tnfrsf1a) receptors and confirmed by confocal microscopy. Transfected cells were treated with glycine (10 mM). The expressions of TNF-α and IL-6 mRNA were measured by qRT-PCR, while concentrations were quantified by ELISA. RESULTS: Glycine decreased the expression and concentration of TNF-α and IL-6; this effect did not occur in the absence of TNF-α receptor due to siRNA. In contrast, glycine produced only slight changes in the expression of TNF-α and IL-6 in the absence of the glycine receptor due to siRNA. A docking analysis confirmed the possibility of binding glycine to the TNF-α1a receptor. CONCLUSION: These findings support the idea that glycine could partially inhibit the binding of TNF-α to its receptor and provide clues about the mechanisms by which glycine inhibits the secretion of pro-inflammatory adipokines in adipocytes through the TNF-α receptor.

Assuntos

Adipócitos/metabolismo , Citocinas/metabolismo , Glicina/farmacologia , Receptores Tipo II do Fator de Necrose Tumoral/antagonistas & inibidores , Receptores Tipo I de Fatores de Necrose Tumoral/antagonistas & inibidores , Células 3T3-L1 , Adiponectina/genética , Animais , Citocinas/genética , Expressão Gênica , Camundongos , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , RNA Mensageiro/metabolismo , RNA Interferente Pequeno/genética , Receptores de Glicina/genética , Receptores Tipo I de Fatores de Necrose Tumoral/genética , Receptores Tipo II do Fator de Necrose Tumoral/genética

RESUMO

Jatropha neopauciflora is an endemic species of Mexico. Its latex is used to treat wounds, scarring, oral infections, and loose teeth. To date, there are no studies that validate at a morphological level a wound-healing use in diabetes. The present research aimed to evaluate the wound-healing capacity of the latex of J. neopauciflora in the skin of healthy and streptozotocin-induced diabetic mice. Also, a chemical analysis of the latex through molecular exclusion chromatography and HPLC were performed. Male mice (Mus musculus) of 7-week-old CD1 strain were used. Groups of healthy and diabetic mice were formed. A longitudinal cut of 1 cm was performed on the depilated skin. All treatments were topically applied to the wound area twice a day for ten days. At the end of the experiments, the skin sections were obtained from the wound area and stained with Hematoxylin-Eosin. Then we counted the number of active fibroblasts in all the experimental groups. In normal mice, the latex accelerated the wound-healing process and decreased the number of active fibroblasts, similarly to Recoveron. In diabetic mice, the latex and Recoveron increased the number of active fibroblasts. In normal and diabetic mice, a thin and orderly epidermis was observed. Molecular exclusion chromatography exhibited 58 fractions, 14 of which were subjected to HPLC, to detect catechin, a flavonoid with antioxidant, antimicrobial, and anti-inflammatory properties. J. neopauciflora latex can be useful for wound treatment in patients with diabetes mellitus because it accelerates and promotes the wound-healing process.

Assuntos

Diabetes Mellitus Experimental , Jatropha , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Humanos , Látex , Camundongos , Pele , Cicatrização

RESUMO

In Central and South American traditional medicine, people use Cecropia obtusifolia Bertol (Cecropiaceae) for the treatment of diabetes mellitus. However, its hypoglycemic action mechanism at pancreatic and liver level has been poorly explored. The present research aimed to establish the influence of the aqueous extract of C. obtusifolia, standardized in its content of chlorogenic acid, on insulin secretion in RINm5F cells and over the liver carbohydrates and lipids metabolism, and to determine concomitantly its hepatoprotective effect on mice with streptozotocin-induced diabetes. In RINm5F cells, concentrations 5, 50, 100, and 200 µg/mL of aqueous extract of C. obtusifolia were used to determine [Ca2+]i and insulin secretion. In an acute study, the extract was administered at doses of 500 mg/kg. In another test (subacute), the extract was daily administrated to diabetic mice (200 mg/kg/day) for 30 days. Blood glucose levels and other biochemical parameters were determined, and a liver histological analysis was performed. In RINm5F cells, C. obtusifolia increased [Ca2+]i and insulin secretion, whereas in diabetic mice exhibited acute and subacute hypoglycemic effects. Daily administration of C. obtusifolia to diabetic mice also increased liver glycogen storage and glycogen synthase levels, without apparent changes in gluconeogenesis. Besides, it increased peroxisome proliferator-activated receptor-α (PPAR-α) and long-chain-fatty-acid-CoA ligase 1 (ACSL-1) expression and reduced triglycerides, transaminases (alanine aminotransferase and aspartate aminotransferase), and collagen fibers, modifying anti-inflammatory (adiponectin and interleukin-10) and inflammatory (tumor necrosis factor-α) cytokines in serum. Therefore, the hypoglycemic effect of C. obtusifolia implicates a dual action, promoting insulin secretion, liver glycogen accumulation, and hepatoprotection by decreasing collagen fibers and inflammatory markers, whereas it improves lipid metabolism, due in part to PPAR-α.

Assuntos

Cecropia/química , Diabetes Mellitus Experimental , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Glicemia , Diabetes Mellitus Experimental/tratamento farmacológico , Fígado/efeitos dos fármacos , Camundongos , Fitoterapia , Substâncias Protetoras/uso terapêutico

RESUMO

Ayahuasca (caapi, yajé), is a psychoactive brew from the Amazon Basin region of South America traditionally considered a "master plant." It is prepared as a decoction from Banisteriopsis caapi and Psychotria viridis, which it is thought that it stimulates creative thinking and visual creativity. Native healers of the Orinoco and Amazon basins have used traditionally ayahuasca as a healing tool for multiple purposes, particularly to treat psychological disorders in the patients, with some beneficial effects experimentally and clinically validated. Recently, several syncretic religions, as the "União de Vegetal" (UDV) group in Brazil, have been spread around the world. The use of ayahuasca has been popularized by internet and smart-shops, bringing the psychoactive substance to new highs, emerging new "ayahuasqueros." Ayahuasca has alkaloids as ß-carbolines and dimethyltryptamines, which inhibit the monoamine oxidase and active the 5-HT2A (5-hydroxytryptamine) receptor, respectively, resulting in hallucinations in the users. Ayahuasca induces a psychedelic change in the anteroposterior coupling of the electrophysiological brain oscillations in humans. Traditional ayahuasca beverage is generating pharmacological, commercial and spiritual interest among the scientific community, government people, and different populations worldwide. The goal of this article is to report about the uses, chemistry and biological activities of ayahuasca.

RESUMO

Tillandsia L. genus comprises 649 species, with different uses at different times. T. usneoides L. uses are reported since the late- archaic and pre-Columbian cultures. In XIX-XX centuries, T. usneoides was used in some manufactured products, as polish and packing fruit. Tillandsia has a favorable reputation as medicine: for leucorrhea, rheumatism, ulcers, hemorrhoid treatment, as an anti-diabetic remedy, emetic, analgesic, purgative, contraceptive, antispasmodic and diuretic. Tillandsia chemical composition includes cycloartane triterpenes and hydroxy-flavonoids, which are present in at least 24 species. Several extracts and compounds from Tillandsia spp. have been reported with pharmacological actions, as anti-neoplasia, hypolipidemic, antifungal, anti-HSV-1, hypoglycemic and microbicide. This review communicates the economic importance, ethnobotany, chemistry composition and biological activities of the Tillandsia genus, and analyze its biological and economic perspective. Tillandsia genus has cultural, economic and pharmacological relevance, with a high potential in many essential aspects of the modern society.

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El género Tillandsia L. comprende 649 especies, con diferentes usos en diferentes épocas. T. usneoides L. se han reportado desde el arcáico tardío hasta las culturas precolombinas. En los siglos XIX-XX, T. usneoides se usó en productos manufacturados: como abrasivo y embalaje de fruta. Como medicina tradicional, el género Tillandsia se reporta para leucorrea, reumatismo, úlceras, hemorroides, remedio antidiabético, emético, analgésico, purgante, anticonceptivo, antiespasmódico y diurético. Su composición química incluye triterpenos de tipo ciclo-artano e hidroxi-flavonoides, presentes en al menos 24 especies. Los extractos y compuestos del género Tillandsia se han reportado con propiedades antineoplásicas, hipolipidémicas, antifúngicas, anti-HSV-1, hipoglucemiantes y microbicidas. Esta revisión comunica la importancia económica, etnobotánica, composición química y las actividades biológicas del género Tillandsia, y analiza su perspectiva biológica y potencial económica. Tillandsia tiene importancia cultural, económica y farmacológica, con gran potencial en muchos aspectos esenciales de la sociedad moderna.

Assuntos

Plantas Medicinais/química , Extratos Vegetais/química , Etnobotânica , Tillandsia/química , Triterpenos/análise , Extratos Vegetais/farmacologia , Bromeliaceae/química

RESUMO

Catharanthus roseus (L.) G. (C. roseus) is a medicinal plant used traditionally for diabetes mellitus control. Several compounds of an alkaloidal nature have been proposed as hypoglycemic principles. However, little attention has been paid to other compounds in this plant that could also participate in this hypoglycemic activity. This study aimed to analyze the hypoglycemic effect of a polyphenolic fraction from C. roseus, as well as its action on insulin secretion and expression in RINm5F cells. Methods. An alkaloid-free aqueous extract was obtained from C. roseus stems. The hypoglycemic effect of different doses of this extract was evaluated in normal and streptozotocin-induced diabetic mice. This extract was fractionated by bipartition, and the resultant fractions were assessed by their hypoglycemic effects. Subsequently, the fraction with the greater hypoglycemic activity was added to the RINm5F cells, and the expression and secretion of insulin were analyzed. The antioxidant activity was determined by the DPPH method and through chromatographic analysis of the most active fraction by HPLC, using an Econosphere C18 column. Results. The aqueous alkaloid-free extract of C. roseus stems significantly reduced blood glucose in normal and diabetic mice. The fractionation of this extract provided three fractions, one of which (a precipitate) showed significant reductions in glycemia at 6 h (48.1 and 64.5% in normal and diabetic mice, respectively). This precipitate contained phenolic compounds and saponins. Its chromatographic analysis showed that it is formed by several phenolic compounds; gallic acid (0.053%) and chlorogenic acid (0.216%) were identified and quantified. Conclusion. The phenolic fraction of C. roseus containing gallic acid and chlorogenic acid had a hypoglycemic effect that may be explained by an increase in insulin secretion.

RESUMO

Glycine modulates inflammatory processes mediated by macrophages and adipocytes through decreasing the secretion of TNF-α, IL-6, and leptin, while increasing adiponectin. These effects have been associated with the inactivation of NF-κB in response to TNF-α, across an increase of its inhibitor IκB-α in adipocytes. However, glycine upstream mainly influences the IκB kinase (IKK) complex, a multi-protein kinase complex considered a critical point in regulation of the NF-κB pathway; whether that is responsible for the TNF-α-induced phosphorylation of IkB has not been explored. Additionally, although previous studies have described glycine interactions with specific receptors (GlyR) in different immune system cell types, it is currently unknown whether adipocytes present GlyR. In this research, participation of the IKK-α/ß complex in the inhibition of the TNF-α/NF-κB pathway by glycine was evaluated and associated with the synthesis and secretion of inflammatory cytokines in 3T3-L1 adipocytes. Furthermore, we also explored GlyR expression, its localization on the plasmatic membrane, intracellular calcium concentrations [Ca2+]i and strychnine antagonist action over the GlyR in these cells. Glycine decreased the IKK-α/ß complex and the phosphorylation of NF-κB, diminishing the expression and secretion of IL-6 and TNF-α, but increasing that of adiponectin. GlyR expression and its fluorescence in the plasma membrane were increased in the presence of glycine. In addition, glycine decreased [Ca2+]i; whereas strychnine + glycine treatment inhibited the activation of NF-κB observed with glycine. In conclusion, the reduction of TNF-α and IL-6 and suppression of the TNF-α/NF-κB pathway by glycine may be explained in part by inhibition of the IKK-α/ß complex, with a possible participation of GlyR in 3T3-L1 adipocytes.

Assuntos

Adipócitos/metabolismo , Glicina/metabolismo , Quinase I-kappa B/metabolismo , NF-kappa B/metabolismo , Células 3T3-L1 , Animais , Cálcio/metabolismo , Citocinas/biossíntese , Citocinas/metabolismo , Interleucina-6/metabolismo , Masculino , Camundongos , Fosforilação , Receptores de Glicina/metabolismo , Fator de Necrose Tumoral alfa/metabolismo

RESUMO

The chlorogenic acid (CGA) is a natural product isolated from Cecropia obtusifolia, which possesses several pharmacological properties, such as: anti-carcinogenic, neuroprotective, antioxidant, anti-inflammatory, hypoglycemic, and hypolipidemic. In relation to its effects on the hyperglycemia and hypertriglyceridemia, few is known about the mechanisms in which this compound may be acting, therefore, the aim of the present study was to determine if CGA acts as an insulin secretagogue increasing intracellular calcium concentrations ([Ca2+]i) in RINm5F cells; or as an insulin sensitizer and lipid-lowering agent stimulating the expression of PPARγ and PPARα, respectively, in 3T3-L1 adipocytes. As results, RINm5F cells treated with 200µM of CGA showed an increase in [Ca2+]i of 9-times versus control and 4-times as compared to positive control; in addition, an increase in insulin secretion was observed similarly to those of positive control. CGA also significantly increased the mRNA expression of PPARγ (150%) and GLUT4 (220%), as well PPARα (40%) and FATP (25%) as it was appreciated by RT-PCR. Additionally, a chemoinformatic analysis suggested that CGA has suitable physicochemical properties to be considered as leader bioactive molecule for the development of novel agents with similar properties. Together, our results indicate that CGA possesses multiple mechanisms of action for the development of highly effective therapeutics in the treatment of metabolic diseases such as type 2 diabetes.

Assuntos

Ácido Clorogênico/farmacologia , Insulina/metabolismo , PPAR alfa/agonistas , PPAR gama/agonistas , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Cálcio/metabolismo , Ácido Clorogênico/química , Biologia Computacional , Relação Dose-Resposta a Droga , Proteínas de Transporte de Ácido Graxo/metabolismo , Transportador de Glucose Tipo 4/metabolismo , Glibureto/farmacologia , Humanos , Secreção de Insulina , Camundongos , PPAR alfa/metabolismo , PPAR gama/metabolismo , Ratos

RESUMO

BACKGROUND: The aqueous extract of Cucurbita ficifolia (C. ficifolia) fruit has demonstrated hypoglycemic effect, which may be attributed to some components in the extract. However, the major secondary metabolites in this fruit have not yet been identified and little is known about its extra-pancreatic action, in particular, on liver carbohydrate metabolism. Therefore, in addition to the isolation and structural elucidation of the principal components in the aqueous extract of C. ficifolia, the aim of this study was to determine whether or not the hypoglycemic effect of the aqueous extract of Cucurbita ficifolia (C. ficifolia) fruit is due to accumulation of liver glycogen in diabetic mice. MATERIALS AND METHODS: The aqueous extract from fruit of C. ficifolia was fractionated and its main secondary metabolites were purified and chemically characterized (NMR and GC-MS). Alloxan-induced diabetic mice received daily by gavage the aqueous extract (30 days). The liver glycogen content was quantified by spectroscopic method and by PAS stain; ALT and AST by spectrometric method; glycogen synthase, glycogen phosphorylase and GLUT2 by Western blot; the mRNA expression of GLUT2 and glucagon-receptor by RT-PCR; while serum insulin was quantified by ELISA method. A liver histological analysis was also performed by H&E stain. RESULTS: Chemical fingerprint showed five majoritarian compounds in the aqueous extract of C. ficifolia: p-coumaric acid, p-hydroxybenzoic acid, salicin, stigmast-7,2,2-dien-3-ol and stigmast-7-en-3-ol. The histological analysis showed accumulation of liver glycogen. Also, increased glycogen synthase and decreased glycogen phosphorylase were observed. Interestingly, the histological architecture evidenced a liver-protective effect due the extract. CONCLUSION: Five compounds were identified in C. ficifolia aqueous extract. The hypoglycemic effect of this extract may be partially explained by liver glycogen accumulation. The bioactive compound responsible for the hypoglycemic effect of this extract will be elucidated in subsequent studies.

Assuntos

Cucurbita/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/química , Glicogênio Hepático/metabolismo , Compostos Fitoquímicos/análise , Fitoterapia/métodos , Extratos Vegetais/química , Aloxano , Animais , Álcoois Benzílicos/análise , Álcoois Benzílicos/farmacologia , Ácidos Cumáricos/análise , Ácidos Cumáricos/farmacologia , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Glucosídeos/análise , Glucosídeos/farmacologia , Hidroxibenzoatos/análise , Hidroxibenzoatos/farmacologia , Hipoglicemiantes/farmacologia , Insulina/sangue , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Propionatos , Sitosteroides/análise , Sitosteroides/farmacologia

RESUMO

Flavonoids from medicinal plants have been used in traditional medicine to treat a variety of prevalent diseases. Flavones activate the signaling pathways promoting fuel metabolism and insulin sensitizing in hepatocytes and adipocytes, which suggests that flavones may have the potential to exert in vivo antidiabetic and antihyperlipidemic effects. Thus, the aim of the current study was to determine the antidiabetic, antihyperlipidemic and anti-inflammatory effects of tilianin in diabetic rats. Also, to understand the mechanism involved using in vitro 3T3-L1 cells and tissues from experimental animals treated with test samples through molecular profile studies. Non insulin-dependent diabetic mellitus (NIDDM) rats were treated over a short period (for 10 days) with 60mg/Kg/day of tilianin. After treatment, a biochemical blood profile was determined. Also, adipose and thoracic aortic tissues were used to determine pro-inflammatory profile, adiponectin and adhesion molecules by real-time PCR. In 3T3-L1 cells pretreated with tilianin (10µM), PPARα, PPARγ, GLUT4, FATP-1 and ACSL-1 mRNA expression were measured. In order to explain the potential PPARα interaction with tilianin, a docking study with PPARα was carried out. Thus, intragastric administration of tilianin and metformin induced a decrease in plasma glucose (GLU) in diabetic rats on day 6, and remained significantly lower until the end of the treatment; also blood triacylglycerides (TAG) and cholesterol (CHOL) (p<0.05) were diminished. Moreover, IL-1ß and IL-18 expression was significantly decreased in adipose tissue (p<0.05); meanwhile adiponectin was significantly overexpressed (p<0.05). Besides, ICAM-1 expression was significantly reduced in aortic tissue (p<0.05). In 3T3-L1 cells it was found that tilianin increased PPARα and ACSL1 mRNA levels (p<0.05). Finally, tilianin docking studies with PPARα showed polar interactions with Glu269, Tyr314, His 440 and Tyr464 residues. In conclusion, short-term tilianin treatment might exert its antidiabetic and antihyperlipidemic effect by modulating a pro-inflammatory profile, and increasing adiponectin expression. In addition, our results suggest the possible interaction of tilianin with PPARα.

Assuntos

Anti-Inflamatórios/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Flavonoides/uso terapêutico , Glicosídeos/uso terapêutico , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/uso terapêutico , Células 3T3-L1 , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Animais , Aorta/efeitos dos fármacos , Aorta/metabolismo , Glicemia/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/genética , Ácidos Graxos/metabolismo , Perfilação da Expressão Gênica , Regulação da Expressão Gênica/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Lipogênese/genética , Masculino , Metformina/farmacologia , Metformina/uso terapêutico , Camundongos , Simulação de Acoplamento Molecular , Niacinamida , Oxirredução/efeitos dos fármacos , Ratos Wistar , Estreptozocina

RESUMO

Obesity, from children to the elderly, has increased in the world at an alarming rate over the past three decades, implying long-term detrimental consequences for individual's health. Obesity and aging are known to be risk factors for metabolic disorder development, insulin resistance and inflammation, but their relationship is not fully understood. Prevention and appropriate therapies for metabolic disorders and physical disabilities in older adults have become a major public health challenge. Hence, the aim of this study was to evaluate inflammation markers, biochemical parameters and glucose homeostasis during the obese-aging process, to understand the relationship between obesity and health span during the lifetime. In order to do this, the monosodium glutamate (MSG) obesity mice model was used, and data were evaluated at 4, 8, 12, 16 and 20 months in both female and male mice. Our results showed that obesity was a major factor contributing to premature alterations in MSG-treated mice metabolism; however, at older ages, obesity effects were attenuated and MSG-mice became more similar to normal mice. At a younger age (four months old), the Lee index, triglycerides, total cholesterol, TNF-α and transaminases levels increased; while adiponectin decreased and glucose tolerance and insulin sensitivity levels were remarkably altered. However, from 16 months old-on, the Lee index and TNF-α levels diminished significantly, while adiponectin increased, and glucose and insulin homeostasis was recovered. In summary, MSG-treated obese mice showed metabolic changes and differential susceptibility by gender throughout life and during the aging process. Understanding metabolic differences between genders during the lifespan will allow the discovery of specific preventive treatment strategies for chronic diseases and functional decline.

Assuntos

Obesidade/metabolismo , Glutamato de Sódio/toxicidade , Adiponectina/sangue , Fatores Etários , Animais , Colesterol/sangue , Feminino , Interleucina-6/sangue , Masculino , Camundongos , Obesidade/etiologia , Fatores Sexuais , Transaminases/sangue , Triglicerídeos/sangue , Fator de Necrose Tumoral alfa/sangue

RESUMO

Senna villosa (Miller) is a plant that grows in México. In traditional Mexican medicine, it is used topically to treat skin infections, pustules and eruptions and to heal wounds by scar formation. However, studies of its potential anti-inflammatory effects have not been performed. The aim of the present study was to determine the anti-inflammatory effect of extracts from the leaves of Senna villosa and to perform a bioassay-guided chemical study of the extract with major activity in a model of ear edema induced by 12-O-tetradecanoylphorbol 13-acetate (TPA). The results reveal that the chloroform extract from Senna villosa leaves has anti-inflammatory and anti-proliferative properties. Nine fractions were obtained from the bioassay-guided chemical study, including a white precipitate from fractions 2 and 3. Although none of the nine fractions presented anti-inflammatory activity, the white precipitate exhibited pharmacological activity. It was chemically characterized using mass spectrometry and infrared and nuclear magnetic resonance spectroscopy, resulting in a mixture of three aliphatic esters, which were identified as the principal constituents: hexyl tetradecanoate (C20H40O2), heptyl tetradecanoate (C21H42O2) and octyl tetradecanoate (C22H44O2). This research provides, for the first time, evidence of the anti-inflammatory and anti-proliferative properties of compounds isolated from Senna villosa.

Assuntos

Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Edema/tratamento farmacológico , Fabaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Fracionamento Químico , Citocinas/metabolismo , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/metabolismo , Mediadores da Inflamação/metabolismo , Contagem de Leucócitos , Masculino , Espectrometria de Massas , Medicina Tradicional , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Ratos , Acetato de Tetradecanoilforbol/efeitos adversos

RESUMO

Psacalium decompositum, commonly known as "Matarique," is a medicinal plant used in Mexico for diabetes mellitus empirical therapy. Previous studies have shown that the fructooligosaccharides (FOS) present in the roots of this plant exhibit a notable hypoglycemic effect in animal models; this effect might be associated with the attenuation of the inflammatory process and other metabolic disorders. In this study, we examined the effects of FOS fraction administration in a fructose-fed rat model for obesity. Phytochemical chromatographic studies (high performance thin layer chromatography and nuclear magnetic resonance) were performed to verify isolation of FOS. 24 male Wistar rats were maintained for 12 weeks on a diet of 20% HFCS in drinking water and chow. Glucose, cholesterol, triglycerides and liver transaminases levels were measured monthly, after administering FOS fraction intragastrically (150 mg/kg/day for 12 weeks), while the levels of inflammatory cytokines were only quantified at the end of the treatments. Rats treated with FOS fraction decreased body weight, cholesterol, triglycerides, and significantly reduced IL-6, IFN-γ, MCP-1, IL-1ß and VEGF levels (p < 0.05). These results suggest that P. decompositum has anti-inflammatory and hypolipidemic properties that might be used as an alternative treatment for the control of obesity.

Assuntos

Asteraceae/química , Dislipidemias/tratamento farmacológico , Frutose/efeitos adversos , Inflamação/tratamento farmacológico , Obesidade/tratamento farmacológico , Oligossacarídeos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Peso Corporal , Quimiocina CCL2/sangue , Colesterol/sangue , Modelos Animais de Doenças , Hipoglicemiantes/farmacologia , Interferon gama/sangue , Interleucina-1beta/sangue , Interleucina-6/sangue , Masculino , Obesidade/induzido quimicamente , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Plantas Medicinais/química , Ratos , Ratos Wistar , Triglicerídeos/sangue , Fator A de Crescimento do Endotélio Vascular/sangue

RESUMO

The antidiarrheal effects of chloroform, methanol, and aqueous extracts of Bidens odorata Cav. were investigated at doses of 200 mg/kg on castor-oil-induced diarrhea. The chloroform extract of B. odorata (CBO) reduced diarrhea by 72.72%. The effect of CBO was evaluated on mice with diarrhea induced by castor oil, MgSO4, arachidonic acid, or prostaglandin E2. CBO inhibited the contraction induced by carbachol chloride on ileum (100 µg/mL) and intestinal transit (200 mg/kg) in Wistar rats. The active fraction of CBO (F4) at doses of 100 mg/kg inhibited the diarrhea induced by castor oil (90.1%) or arachidonic acid (72.9%) but did not inhibit the diarrhea induced by PGE2. The active fraction of F4 (FR5) only was tested on diarrhea induced with castor oil and inhibited this diarrhea by 92.1%. The compositions of F4 and FR5 were determined by GC-MS, and oleic, palmitic, linoleic, and stearic acids were found. F4 and a mixture of the four fatty acids inhibited diarrhea at doses of 100 mg/kg (90.1% and 70.6%, resp.). The results of this study show that B. odorata has antidiarrheal effects, as is claimed by folk medicine, and could possibly be used for the production of a phytomedicine.

RESUMO

OBJECTIVES: Cucurbita ficifolia (characterised by its D chiro inositol (DCI) content) and of synthetic DCI on the redox state, mRNA expression and secretions of proinflammatory cytokines. Additionally, we evaluated the insulin-mimetic action of both treatments by assessing protein kinase B (PKB) activation in 3T3-L1 adipocytes. METHODS: Adipocytes were treated with C. ficifolia and synthetic DCI. The redox state was determined by spectrophotometry as changes in the reduced glutathione/oxidised glutathione (GSH/GSSG) ratio, glutathione peroxidase and glutathione reductase activities; H2 O2 levels were measured by flow cytometry. The mRNA expression and the protein level of cytokines were determinate by real-time reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. The activation of PKB activation was detected by Western blot. KEY FINDINGS: C. ficifolia extract and synthetic DCI reduced oxidative stress by decreased H2 O2 levels, increased glutathione peroxidase activity and changes in the GSH/GSSG ratio. Furthermore, DCI decreased the mRNA expression and secretion of tumour necrosis factor-α, interleukin 6 (IL-6) and resistin, while C. ficifolia reduced protein levels of resistin and increased IL-6 levels. Only DCI demonstrated insulin-mimetic action. CONCLUSIONS: The antioxidant and anti-inflammatory effects of C. ficifolia extract can be explained in part by its DCI content, which modulates the GSH/GSSG ratio and contributes to a reduced proinflammatory state. C. ficifolia and DCI treatments may reduce the disturbances caused by oxidative stress. Additionally, DCI may improve insulin sensitivity through its insulin-mimetic effects.

Assuntos

Adipócitos/efeitos dos fármacos , Antioxidantes/farmacologia , Cucurbita/química , Citocinas/imunologia , Inositol/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Células 3T3-L1 , Adipócitos/imunologia , Adipócitos/metabolismo , Adipocinas/metabolismo , Animais , Antioxidantes/isolamento & purificação , Técnicas de Cultura de Células , Sobrevivência Celular/efeitos dos fármacos , Peróxido de Hidrogênio/metabolismo , Inositol/isolamento & purificação , Camundongos , Oxirredução , Extratos Vegetais/isolamento & purificação , Proteínas Proto-Oncogênicas c-akt/metabolismo

RESUMO

In the present study, the production of a reduced-sugar pomegranate juice jelly supplemented with an aqueous extract of pomegranate peel (PE) is described. Influence of different carbohydrate polymers (guar (G), xanthan (X) and tragacanth (T) gums) on rheological properties was studied. Combination GXT presented the most similar rheological behaviour to commercial jelly. Jelly (J) and jelly with PE (JE) were stored at 4°C over an 8week period for physical, chemical, antioxidant, microbiological and sensory analysis. J and JE showed similar values for °Brix, colour and Aw, though the pH of JE was lower than J. Thiol and phenolic compounds were higher in JE than in J. Antioxidant activity (radical scavenging activity and autoxidation of linoleic acid) was higher in JE than in J at 0weeks, and were decreasing with time. Pomegranate juice with additives was generally less accepted than J and JE.

Assuntos

Antioxidantes/química , Bebidas/análise , Frutas/química , Lythraceae/química , Extratos Vegetais/análise , Adolescente , Bebidas/normas , Carboidratos/análise , Feminino , Humanos , Masculino , Paladar , Adulto Jovem

RESUMO

Cucurbita ficifolia Bouché fruit containing D-chiro-inositol and Ibervillea sonorae Greene root containing cucurbitane-type glycosides are used to control diabetes in Mexico. Although the hypoglycemic effect of both plants has been demonstrated and some active compounds proposed, their mechanisms are still unknown. The aim of this study was to determine if the incubation with both aqueous extracts avoids the inhibition of contraction induced by phenylephrine similarly to glibenclamide in rat aortic rings. The hypoglycemic aqueous extracts of C. ficifolia and I. sonorae were characterized for their content of either D-chiro inositol or cucurbitanes respectively, and then we assayed the characterized extracts in vitro on the diazoxide-induced relaxation of rat aortic rings precontracted with phenylephrine, using as positive control glibenclamide. I. sonorae extract blocked the KATP channels in a concentration-dependent manner (p < 0.05), whereas C. ficifolia extract had no effect on these channels. I. sonorae extract produces a hypoglycemic effect through a similar mechanism to sulphonylureas in this experimental model; however, hypoglycemic action of C. ficifolia extract should be explained by an independent KATP channels mechanism.

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Los frutos de Cucurbita ficifolia conteniendo D-quiro-inositol y las raíces de Ibervillea sonorae conteniendo glucósidos tipo cucurbitano son empleados en el control de la diabetes en México. Aunque el efecto hipoglucémico de ambas plantas ha sido demostrado y se han propuesto algunos de sus compuestos activos, aún se desconoce su mecanismo de acción. El objetivo de este estudio fue determinar si la incubación con ambos extractos acuosos evita la inhibición de la contracción inducida por fenilefrina de manera similar a la glibenclamida en anillos aórticos de rata. Los extractos acuosos hipoglucémicos de C. ficifolia e I. sonorae fueron caracterizados en su contenido de D-quiro inositol o cucurbitanos, respectivamente y entonces fueron estudiados en un modelo in vitro en la relajación inducida por diazóxido en anillos aórticos previamente contraídos con fenilefrina, usando como control positivo glibenclamida. El extracto de Ibervillea sonorae bloqueó los canales KATP de manera dosis-dependiente (p < 0.05), mientras que Cucurbita ficifolia no tuvo efecto en esos canales. El extracto de I. sonorae produce efecto hipoglucémico a través de un mecanismo similar al de las sulfonilureas en este modelo experimental; por su parte, la acción hipoglucemiante del extracto de C. ficifolia debe ser explicado mediante un mecanismo independiente de los canales KATP.

Assuntos

Animais , Ratos , Cucurbitaceae/química , Extratos Vegetais/farmacologia , Glicemia , Hipoglicemiantes/farmacologia , Aorta , Cromatografia Líquida de Alta Pressão , Diabetes Mellitus Experimental , Canais KATP , Ratos Wistar , Raízes de Plantas

RESUMO

Introduction. Catharanthus roseus (L.) is used in some countries to treat diabetes. The aim of this study was to evaluate the hypoglycemic activity of extracts from the flower, leaf, stem, and root in normal and alloxan-induced diabetic mice. Methods. Roots, leaves, flowers, and stems were separated to obtain organic and aqueous extracts. The blood glucose lowering activity of these extracts was determinate in healthy and alloxan-induced (75 mg/Kg) diabetic mice, after intraperitoneal administration (250 mg/Kg body weight). Blood samples were obtained and blood glucose levels were analyzed employing a glucometer. The data were statistically compared by ANOVA. The most active extract was fractioned. Phytochemical screen and chromatographic studies were also done. Results. The aqueous extracts from C. roseus reduced the blood glucose of both healthy and diabetic mice. The aqueous stem extract (250 mg/Kg) and its alkaloid-free fraction (300 mg/Kg) significantly (P < 0.05) reduced blood glucose in diabetic mice by 52.90 and 51.21%. Their hypoglycemic activity was comparable to tolbutamide (58.1%, P < 0.05). Conclusions. The best hypoglycemic activity was presented for the aqueous extracts and by alkaloid-free stem aqueous fraction. This fraction is formed by three polyphenols compounds.