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Obesity is characterized by an excessive and abnormal accumulation of fat. According to the 2022 National Health and Nutrition Survey, in Mexico, the prevalence of overweight and obesity-diagnosed if one's body mass index (BMI) was ≥25 kg/m2-in adults was 75.2%. A strong association between the amount of visceral fat and diseases such as diabetes mellitus type II has been recognized. Species of the Bauhinia genus have lipid-lowering and antidiabetic properties. The aim of this work was to evaluate the lipolytic and antiadipogenic activity of Bauhinia divaricata L. in 3T3-L1 cells and to identify the major compounds in the bioactive treatments. The extraction of aerial parts allowed us to obtain hexanic (BdHex), ethyl acetate (BdEAc), and hydroalcoholic (BdHA) extracts. Lipid levels were measured in 3T3-L1 cells differentiated into adipocytes. Our evaluation of cell viability identified an IC50 > 1000 µg/mL in all the extracts, and our evaluation of the antiadipogenic activity indicated that there was a significant reduction (p < 0.001) in the accumulation of lipids with hydroalcoholic (60%) and ethyl acetate (75%) extracts of B. divaricate compared with metformin at 30 mM (65%). The major compounds identified in these extracts were as follows: triacetin (1), 2,3-dihydroxypropyl acetate (2), (3E)-2-methyl-4-(1,3,3-trimethyl-7-oxabicyclo[4.1.0]hept-2-yl)-3-buten-2-ol (3), 2,5-dihydroxyphenylacetic acid (4), (3R)-3-hydroxydodecanoic acid (5), kaempferol-3-O-rhamnoside (6), and quercetin 3-O-rhamnoside (7). Some of these naturally occurring compounds have been related to the anti-obesity effects of other medicinal plants; therefore, these compounds isolated from B. divaricata could be responsible for inhibiting the differentiation process from preadipocytes to mature adipocytes.
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Coffee is one of the most consumed beverages in the world; its production is based mainly on varieties of the Coffea arabica species. Mexico stands out for its specialty and organic coffee. In Guerrero, the production is done by small indigenous community cooperatives that market their product as raw material. Official Mexico Standards stipulate the requirements for its commercialization within the national territory. In this work, the physical, chemical, and biological characterizations of green, medium, and dark roasted beans from C. arabica varieties were carried out. Analysis by HPLC showed higher chlorogenic acid (55 mg/g) and caffeine (1.8 mg/g) contents in the green beans of the Bourbon and Oro Azteca varieties. The caffeine (3.88 mg/g) and melanoidin (97 and 29 mg/g) contents increased according to the level of roasting; a dissimilar effect was found in the chlorogenic acid content (14.5 mg/g). The adequate nutritional content and the sensory evaluation allowed the classification of dark-roasted coffee as premium coffee (84.25 points) and medium-roasted coffee as specialty coffee (86.25 points). The roasted coffees presented antioxidant activity without cytotoxic effects; the presence of CGA and caffeine supports the beneficial effects of drinking coffee. The results obtained will serve as a basis for making decisions on improvements to the coffees analyzed.
Assuntos
Cafeína , Coffea , Cafeína/farmacologia , Cafeína/análise , Ácido Clorogênico/farmacologia , Ácido Clorogênico/análise , Coffea/química , Sementes/química , Extratos Vegetais/químicaRESUMO
In Mexico, Cactaceae plants are widely used in folk medicine for the treatment of diabetes. The genus Opuntia spp. Opuntia matudae Sheinvar prickly pears are known as xoconostle and are used in Mexican cuisine for their acidic flavor. Currently there are few reports of pharmacological properties of this plant, which include antioxidant and antimicrobial activities. This study focuses on the chemical characterization of the methanolic (OmMe) and aqueous (OmAq) extracts and the evaluation of the antidiabetic activity of O. matudae fruits in two biological models. For the in vivo model, streptozotocin (STZ)-induced diabetic mice were used, and for the in vitro model, liver sections isolated from healthy mice were used. The OmAq (100 mg/kg, oral pathway [p.o.]) extract decreased postprandial glucose peak at 0.5 h after glucose uptake by 43.1%, similarly, OmMe (100 mg/kg, p.o.) extract reduced postprandial glucose peak at 0.5 h by 34.1% in healthy mice. The effect of the two extracts and the fraction of the mixture of unidentified betalains (OmB) of O. matudae evaluated in the isolated mouse liver slice model showed a concentration-dependent decrease in hepatic glucose output (HGO) with and without insulin administration with the OmMe extract. The OmAq extract, however, showed concentration-dependent increases of HGO with and without insulin, and the OmB fraction generally exhibited an insulin mimetic effect. Moreover, both OmAq and OmMe extracts were tested in mice with STZ-induced diabetes (160 mg/kg, intraperitoneal route), using a semichronic daily administration (2-28 days after diabetes onset) of OmAq extract was able to reduce blood glucose by 34.3%, meanwhile OmMe extract reduced blood glucose by 22.9%, 28 days after diabetes onset. We identified five compounds (1-5) in the two extracts, consisting of two phenolic acids (1, 2), three flavanols (3-5), as well as two unidentified betalains. Therefore, we conclude that the aqueous extract of the xoconostle fruit where betalains are present may be useful for the treatment of diabetes mellitus.
Assuntos
Diabetes Mellitus Experimental , Opuntia , Animais , Glicemia , Diabetes Mellitus Experimental/tratamento farmacológico , Frutas , Hipoglicemiantes , Camundongos , Extratos VegetaisRESUMO
Aristolochia odoratissima L. is employed for the treatment of pain and as an antidote against the poison of venomous animals in traditional medicine. However, reports have not been found, to our knowledge, about the evaluation of the antinociceptive activity of extracts nor about the presence of compounds associated with this activity. Thus, the purpose of this work was to evaluate the antinociceptive activity of extracts and compounds isolated from the stems of Artistolochia odoratissima L. The extracts were obtained with solvents of increasing polarity and the compounds were isolated and characterized by column chromatography, HPLC, and NMR. The antinociceptive activity was carried out by the formalin test in mice. Ethyl acetate (AoEA) and methanolic (AoM) extracts decreased the paw licking in both phases of the formalin test. The isolated compounds (kaurenoic acid and hinokinin) from AoEA showed the highest antinociceptive activity in both phases of the formalin test. These results confirmed the analgesic effect of this specie described in traditional medicine and provided a base for a novel analgesic agent. They also allowed an approach for the development of standardized plant extracts with isolated metabolites.
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4-Butirolactona/análogos & derivados , Aristolochia/química , Benzodioxóis/uso terapêutico , Diterpenos/uso terapêutico , Lignanas/uso terapêutico , Dor/tratamento farmacológico , 4-Butirolactona/química , 4-Butirolactona/uso terapêutico , Analgésicos/química , Analgésicos/uso terapêutico , Animais , Benzodioxóis/química , Cromatografia Líquida de Alta Pressão , Diterpenos/química , Lignanas/química , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Medição da Dor , Extratos Vegetais/química , Extratos Vegetais/uso terapêuticoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Oenothera rosea (Onagraceae), commonly known as "hierba del golpe" in Mexico, is an herbaceous plant widely used in Mexican traditional medicine for the treatment of pain and inflammation. AIM OF THE STUDY: The aim of this study was to assess the effect of extracts and compounds isolated from O. rosea in kaolin-carrageenan induced arthritis. MATERIALS AND METHODS: Hydroalcoholic extract from aerial parts of O. rosea was obtained and chemically separated in order to obtain OrEA and isolated compounds using column chromatography, HPLC, UPLC and NMR analysis. O. rosea extract and derivatives were tested on the kaolin/carrageenan (K/C) induced arthritis model on ICR mice. Knee inflammation and paw withdrawal threshold were assessed following intraarticular administration of kaolin and carrageenan (4% and 2%, respectively) and subsequent oral administration of O. rosea. TNF-α, IL-1ß, IL-6 and IL-10 levels from synovial capsule were measured using ELISA kits. NF-κB activity was also measured using the RAWBlue™ cell line. Finally, spleen and lungs were dissected to investigate body index. RESULTS: Oral administration of the O. rosea ethyl acetate fraction (25, 50 and 100 mg/kg) and isolated compounds (2 mg/kg) reduced the edema induced by kaolin/carrageenan, similar to the effect of methotrexate (1 mg/kg). Hyperalgesia but not allodynia was observed during this experiment. O. rosea derivatives reduced this behavior. The quantification of cytokines showed a reduction in TNF-α, IL-1ß and IL-6, as well as an increase of IL-10. NF-κB production was also reduced by administering O. rosea derivatives. Chemical analysis of O. rosea derivatives showed that the major compounds present in the ethyl acetate fraction were phenolic compounds. Gallic acid, quercetin glucoside and quercetin rhamnoside were separated and identified by UPLC-UV-MS, and myricetin glycoside and tamarixetin glucoside using 1H and 13C NMR. CONCLUSIONS: O. rosea produces different phenolic compounds capable of reducing the inflammation and secondary mechanical hyperalgesia produced by K/C administration. They also reduced proinflammatory cytokines and increased anti-inflammatory cytokines. Finally, NF-κB modulation was reduced by the administration of O. rosea. Therefore, O. rosea could be considered of interest in inflammatory and painful diseases.
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Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Artrite/tratamento farmacológico , Hiperalgesia/tratamento farmacológico , Oenothera , Fenóis/uso terapêutico , Extratos Vegetais/uso terapêutico , Analgésicos/química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Artrite/induzido quimicamente , Artrite/imunologia , Carragenina , Linhagem Celular , Citocinas/imunologia , Modelos Animais de Doenças , Feminino , Hiperalgesia/imunologia , Caulim , Camundongos Endogâmicos ICR , NF-kappa B/imunologia , Fenóis/análise , Fenóis/farmacologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Membrana Sinovial/efeitos dos fármacos , Membrana Sinovial/imunologiaRESUMO
BACKGROUND: Physical activity and sports have acquired great importance in contemporary society, given that they have created trends to improve performance, strength and muscle mass through the consumption of nutritional supplements. OBJECTIVE: To determine the profile of the consumer and the type of nutritional supplements in people attending the gyms of the northern border of Tamaulipas. METHOD: It was carried out a cross-sectional and descriptive study in a sample of 800 people attending gyms in 4 cities in the border area between the United States and Mexico, in the state of Tamaulipas (Reynosa, Rio Bravo, Nuevo Laredo and Matamoros). A survey was applied to determine the profile of the consumer and the type of supplements they consumed. RESULTS: 81% of people who went to a gym consumed nutritional supplements, and both genders used them, regardless of their body mass index. CONCLUSIONS: The most used supplements were proteins, essential amino acids and nitric oxide. Improving sports performance, beauty or aesthetics, health care and finally compensating losses were the reasons selected to justify the consumption of nutritional supplements.
INTRODUCCIÓN: La actividad física y el deporte han adquirido gran importancia en la sociedad actual, pues han generado tendencias para mejorar el rendimiento, la fuerza y la masa muscular mediante el consumo de suplementos alimenticios. OBJETIVO: Determinar el perfil del consumidor y el tipo de suplementos nutricionales en personas que asisten a gimnasios de la frontera norte de Tamaulipas. MÉTODO: Estudio transversal y descriptivo en una muestra de 800 personas que se ejercitaban en gimnasios en cuatro ciudades (Reynosa, Río Bravo, Nuevo Laredo y Matamoros) de la zona fronteriza entre los Estados Unidos de Norteamérica y México, en el estado de Tamaulipas. Se aplicó una encuesta para determinar el perfil del consumidor y el tipo de suplementos que empleaba. RESULTADOS: El 81% de las personas que acudieron a un gimnasio consumían suplementos nutricionales y ambos sexos los utilizaron, independientemente de su índice de masa corporal. CONCLUSIONES: Los suplementos más utilizados fueron proteínas, aminoácidos esenciales y óxido nítrico. Mejorar el rendimiento deportivo, la belleza física o el aspecto estético, el cuidado de salud y, por último, compensar pérdidas, fueron las razones seleccionadas para justificar el consumo de suplementos nutricionales.
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AIM: In this study, the pharmacological interactions between a Rhodiola rosea ethanol extract and B-vitamins such as thiamine (B1), riboflavine (B2), pyridoxine (B6), cyanocobalamin (B12) and a mixture of vitamins B1+B6+B12 was investigated in the mouse formalin test. METHODS: Individual dose response curves of the Rhodiola rosea ethanol extract, as well as B-vitamins alone or in a mixture were evaluated in mice in which nociception was induced with 2% formalin intraplantarly. The antinociceptive mechanisms of the Rhodiola rosea were investigated by exploring the role of the opioid and serotonin receptors and the nitric oxide pathway. Isobolographic analysis was used to evaluate the pharmacological interactions between the Rhodiola rosea ethanol extract and each B-vitamin individually or the mixture of vitamins B1+B6+B12 by using the ED30 and a fixed 1:1 ratio combination. RESULTS: Administration of the Rhodiola rosea extract alone or in combination with all of the vitamins produced a significant and dose-dependent antinociceptive response. The antinociceptive effect of the Rhodiola rosea extract (ED50=81 mg/kg, p.o.) was significant and reverted in the presence of antagonists of the 5-HT1A, GABA/BDZs and opioid receptors and by blocking mediators of the nitric oxide/cGMP/K(+) channels pathway. Isobolograms demonstrate that all of the combinations investigated in this study produced a synergistic interaction experimental ED30 values were significantly smaller than those calculated theoretically. CONCLUSIONS: These results provide evidence that a Rhodiola rosea ethanol extract in combination with B-vitamins produces a significant diminution in the nociceptive response in a synergistic manner, which is controlled by various mechanisms. These findings could aid in the design of clinical studies and suggest that these combinations could be applied for pain therapy.
Assuntos
Analgésicos/uso terapêutico , Interações Medicamentosas , Dor/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Rhodiola , Complexo Vitamínico B/uso terapêutico , Analgésicos/farmacologia , Animais , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Feminino , Formaldeído , Camundongos , Camundongos Endogâmicos ICR , Dor/induzido quimicamente , Extratos Vegetais/farmacologia , Complexo Vitamínico B/farmacologiaRESUMO
Worldwide over 12 million people were diagnosed with cancer (excluding non-melanoma skin cancer) and 8 million individuals died from cancer in 2008. Recent data indicate that 75-90% of patients with advanced stage diseases or metastatic cancer will experience significant cancer pain. Bone cancer pain is common in patients with advanced breast, prostate, and lung cancer as these tumors have a marked affinity to metastasize to bone. Once tumors metastasize to bone, they are a major cause of morbidity and mortality as the tumor induces significant skeletal remodeling, fractures, pain and anemia; all of which reduce the functional status, quality of life and survival of the patient. Currently, the factors that drive cancer pain are poorly understood, however, several recently introduced models of bone cancer pain that mirror the human condition, are providing insight into the mechanisms that drive bone cancer pain and guiding the development of novel therapies to treat the cancer pain. Several of these therapies have recently been approved by the FDA to treat bone cancer pain (bisphosphonates, denosumab) and others are currently being evaluated in human clinical trials (tanezumab). These new mechanism-based therapies are enlarging the repertoire of modalities available to treat bone cancer pain and improving the quality of life and functional status of patients with bone cancer.