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1.
Horiz. sanitario (en linea) ; 22(1): 181-190, Jan.-Apr. 2023. graf
Artigo em Espanhol | LILACS-Express | LILACS | ID: biblio-1528703

RESUMO

Resumen Objetivo: Crear la infografía de la guía de alimentación de Dieta Mediterránea Mexicanizada (DMM) y evaluar su comprensión. Material y Métodos: Estudio de tipo descriptivo, el cual constó de dos fases la 1ra. Se creó la infografía de la guía de alimentación de Dieta Mediterránea Mexicanizada. 2da. Se evaluó la apreciación y comprensión de la infografía de la guía de alimentación, en línea a población universitaria, incluidos familiares y conocidos. Resultados: 273 participantes de 42 años promedio, 74% mujeres y 26% varones, más del 94% de los participantes respondió comprender en su totalidad la infografía. DMM es práctica, aplicable, asequible, entendible, buena para el ser humano y ambiente. Conclusión: La Dieta Mediterránea puede prevenir parcial o totalmente el síndrome metabólico, la guía de alimentación de Dieta Mediterránea Mexicanizada promueve una vida sana y bienestar para todas las edades, respalda los objetivos de desarrollo sostenible, será una herramienta de salud pública, práctica, aplicable, asequible, entendible, apta para promoverse en la población mexicana.


Abstract Objective: To create the infographic of the Mexicanized Mediterranean Diet food guide and evaluate its understanding. Material and Methods: Descriptive type study, which consisted of two phases, the 1st. The infographic of the Mexicanized Mediterranean Diet food guide was created. 2nd Appreciation and comprehension of the food guide infographic was evaluated online for the university population, including relatives and acquaintances. Results: 273 participants with an average age of 42, 74% women and 26% men, more than 94% of the participants responded that they understood the infographic in its entirety. DMM is practical, applicable, affordable, understandable, good for humans and the environment. Conclusion: The Mediterranean Diet can partially or totally prevent metabolic syndrome, the Mexicanized Mediterranean Diet food guide promotes a healthy life and well-being for all ages, supports the objectives of sustainable development, will be a practical, applicable public health tool, affordable, understandable, suitable for promotion in the Mexican population.

2.
Curr Drug Targets ; 18(5): 605-616, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28017125

RESUMO

In nature, pathogenic parasite species with different susceptibility patterns of antiparasitic drugs abound. In this sense, natural products derived from plants are a potency for drugs with potential antiparasitic activity. Unfortunately, there are many metabolites and studying all of them would be costly in terms of money and resources. To this end, theoretical studies such as QSAR models could be useful. These, for the most part, predict the biological activity of the drugs against a single species of parasite. Consequently, foretell the probability with which a drug is active against many different species with a single QSAR model is an important achievement. This review consists of three parts: the first part is a review of metabolites found in nature that have antiparasitic activity, in particular the antiprotozoal (Leishmania and Trypanosoma); the second part includes a review of theoretical studies looking for a model that predicts the antiprotozoal activity of natural products; the third and final part concerns the study of theoretical models focused on the interaction between drug and receptor, analyzing new metabolites with antiprotozoal activity.


Assuntos
Antiprotozoários/química , Produtos Biológicos/química , Biologia Computacional/métodos , Antiprotozoários/farmacologia , Produtos Biológicos/farmacologia , Simulação por Computador , Humanos , Modelos Moleculares , Relação Quantitativa Estrutura-Atividade
3.
Mini Rev Med Chem ; 2015 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-25694070

RESUMO

Cecropia obtusifolia bertol is medicinal specie used in the treatment of diabetes mellitus and hypertension and it has scientific studies that support the traditional use. However, it is required to understand the influence of drying temperature on the yield and pharmacological activity. Drying rate, extraction efficiency, changes in the UV-Vis spectrum and estimating chlorophylls were stimulated with the increasing temperature. Finally, relaxant activity of vascular smooth muscle is increased by 70ºC and reducing ability by the method of CARF increases with temperature. Analytical studies are required to identify changes in the metabolic content and those that ensure the safety and efficacy for human consumption. In this sense, bioinformatic studies may be helpful. Studies such as QSAR can help us to study these metabolites derived from natural products. MIND-BETS model and NL MIND-BETS model to predict DPIs was introduced using MARCH-INSIDE (MI) software to calculate structural parameters for drugs and enzymes respectively. We firstly revised the state-of-art on the design with review of previous works with hypertension activity based on theoretical studies. A study, evaluating the effect of drying temperature of leaves of C. obtusifolia on the relaxing of vascular smooth muscle, antioxidant activity and the presence of chlorophylls, with a focus on Cecropia metabolites. Last, we carried out QSAR studies using MIND-BEST and NL MIND-BEST web servers in order to understand the essential metabolites structural requirement for binding with receptors for FDA proteins.

4.
Curr Drug Metab ; 15(5): 557-64, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24909421

RESUMO

Topological Indices (TIs) are numerical parameters useful to carry out Quantitative Structure-Property Relationships (QSPR) analysis and predict the effect of perturbations in many types of Complex Networks. This work, focuses on a very powerful class of TIs called Galvez charge transfer indices. First, we review the classic concept and some applications of these indices. Next, we review the Galvez-Markov TIs of order k (GMk), a recent generalization to these TIs introduced by us. We also reviewed some previous examples of calculation of GMk values for different classes of networks, including metabolic networks. Here, we also demonstrated that Galvez- Markov TIs are useful to predict perturbations and the transferability of biochemical patterns forms metabolic networks of species to others. We report a linear QSPR-Perturbation theory model that predicts more than 300,000 perturbations in metabolic networks with 85 - 99% of good classification in training and validation series.


Assuntos
Cadeias de Markov , Redes e Vias Metabólicas , Modelos Moleculares , Relação Quantitativa Estrutura-Atividade , Animais , Proteínas de Bactérias/metabolismo , Proteínas de Caenorhabditis elegans/metabolismo
5.
J Nat Prod ; 75(12): 2241-5, 2012 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-23234371

RESUMO

The phenanthrenes gymnopusin (1), fimbriol A (2), and erianthridin (3) from Maxillaria densa were found to induce significant relaxant effects in a concentration-dependent and endothelium-independent manner on aortic rings precontracted with norepinephrine (NE, 0.1 µM) and KCl (80 mM). Compound 1 was the most active and also inhibited the cumulative concentration-response contraction of NE or CaCl(2). Contractions induced by FPL 64176, an agonist of L-type voltage-dependent calcium channels, were blocked by 1. The potassium channel blockers glibenclamide and TEA (tetraethylammonium) reduced the relaxations induced by 1. Nevertheless, the effect of 1 was not modified by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, a specific soluble guanylate cyclase inhibitor. The functional results obtained suggest that 1 induces relaxation through an endothelium-independent pathway by the control of cationic channels (calcium channel blockade and potassium channel opening) in the myogenic response of rat aortic rings.


Assuntos
Fenantrenos/farmacologia , Bloqueadores dos Canais de Potássio/farmacologia , Vasodilatadores/farmacologia , Animais , Masculino , Norepinefrina/farmacologia , Fenantrenos/química , Fenantrenos/isolamento & purificação , Bloqueadores dos Canais de Potássio/química , Bloqueadores dos Canais de Potássio/isolamento & purificação , Ratos , Vasodilatação/efeitos dos fármacos , Vasodilatadores/química , Vasodilatadores/isolamento & purificação
6.
Bioorg Med Chem ; 18(11): 3985-91, 2010 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-20451399

RESUMO

A series of 1H-benzo[d]imidazole analogues of Pimobendan, substituted at position 5 with either -CF(3) or -NO(2), were synthesized using a short synthetic route. All the nitro derivatives were potent, and exhibited a concentration- and partial endothelium-dependent vasorelaxant effects, with EC(50)s <5microM. 2-Methoxy-4-[5-nitro-1H-benzo[d]imidazol-2-yl]phenol (compound 13) was the most potent derivative of the series, showing an EC(50) value of 1.81microM and E(max) of 91.7% for ex vivo relaxant response in intact aortic rings, resulting in a 2.5-fold higher activity compared to Pimobendan. The closely related 5-CF(3) analogue (compound 8), was 19 times less potent than 13. The antihypertensive activity of compound 13 was evaluated at doses of 25, 50 and 100mgkg(-1), using spontaneously hypertensive rats (SHR), showing a statistically significant dose-dependent effect.


Assuntos
Anti-Hipertensivos/síntese química , Imidazóis/síntese química , Vasodilatadores/síntese química , Animais , Anti-Hipertensivos/farmacologia , Aorta/efeitos dos fármacos , Relação Dose-Resposta a Droga , Imidazóis/farmacologia , Piridazinas , Ratos , Ratos Endogâmicos SHR , Relação Estrutura-Atividade , Vasodilatadores/farmacologia
7.
Nat Prod Res ; 24(2): 106-14, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-20077303

RESUMO

A simple and efficient protocol has been developed in order to obtain healthy seedlings by asymbiotic germination of seeds from Laelia autumnalis. Seeds from mature capsules were germinated asymbiotically after being cultured on full- or half-strength Murashige and Skoog's (MS) medium, without plant growth regulators and with 3.0% or 1.5% of sucrose. The percentage of germinated seeds (% GS) was recorded during 6 weeks using three different conditions of incubation: light (80% GS, p < 0.05), darkness (30% GS) and white light photoperiod (100% GS, p < 0.05). The best seed germination percentages were found on the light and white light photoperiod conditions. Moreover, we also investigated the vasorelaxant action of the methanolic extracts from wild L. autumnalis (roots, pseudobulbs and leaves) and plantlets generated in vitro. Results showed that the methanolic extract of roots and pseudobulbs produced a significant vasodilator effect, in a concentration-dependent and endothelium-independent manner on norepinephrine (NE) and potassium chloride (KCl)-induced contractions in rat aortic thoracic rings. Nevertheless, the methanolic extract of leaves and plantlets showed no relevant vasorelaxant activity. Therefore, the results suggest that pseudobulbs and roots were the main tissues of the plant where vasorelaxant compounds are stored.


Assuntos
Orchidaceae/química , Extratos Vegetais/farmacologia , Vasodilatadores/farmacologia , Germinação , Orchidaceae/embriologia , Orchidaceae/fisiologia , Sementes
8.
Fitoterapia ; 81(5): 350-7, 2010 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-19879929

RESUMO

RMELanc-induced relaxation in aortic rings precontracted with NE, 5-HT and KCl. It also reduced NE-induced transient contraction in Ca(2+)-free solution and inhibited contraction induced by increasing external calcium. Nevertheless, the vasorelaxant effect of RMELanc was not reduced by ODQ, 1-alprenolol, TEA, glibenclamide, and 2-AP. Oral administration of 100 mg/kg of RMELanc exhibited a significant decrease in systolic and diastolic blood pressures in SHR rats. HPLC analysis allowed us to detect the presence of 2,7-dihydroxy-3,4,9-trimethoxyphenantrene (1), which induced a significant relaxation effect. Therefore, our results suggest that RMELanc induces vasorelaxant and antihypertensive effects by blockade of Ca(2+) channels.


Assuntos
Anti-Hipertensivos/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Músculo Liso Vascular/efeitos dos fármacos , Orchidaceae/química , Fenantrenos/farmacologia , Vasodilatadores/farmacologia , Animais , Aorta , Pressão Sanguínea/efeitos dos fármacos , Cálcio , Cromatografia Líquida de Alta Pressão , Masculino , Contração Muscular/efeitos dos fármacos , Fenantrenos/análise , Raízes de Plantas , Ratos , Ratos Wistar
9.
Biochem Pharmacol ; 78(1): 54-61, 2009 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-19447223

RESUMO

Current investigation was undertaken to elucidate the mode of action of tilianin, isolated from Agastache mexicana, as a vasorelaxant agent on in vitro functional rat thoracic aorta test and to investigate the in vivo antihypertensive effect on spontaneously hypertensive rats (SHR). Tilianin (0.002-933 microM) induced significant relaxation in a concentration- and endothelium-dependent and -independent manners in aortic rings pre-contracted with noradrenaline (NA, 0.1 microM), and serotonin (5-HT, 100 microM). Effect was more significant (p < 0.05) in endothelium-intact (+E) aorta rings than when endothelium was removed(E). Pre-treatment with N-nitro-L-arginine methyl ester (L-NAME; 10 microM) or 1-H-[1,2,4]-oxadiazolo-[4,3a]-quinoxalin-1-one (ODQ, 1 microM) produced a significant change of the relaxant response and activity was markedly inhibited, but not by indomethacin (10 microM) or atropine (1 microM). Furthermore, tilianin (130 microM) provoked a significant displacement to the left in the relaxation curve induced by sodium nitroprusside (SNP; 0.32 nM to 0.1 microM). Moreover, tilianin induced significant in vitro NO overproduction (1.49 +/- 0.86 microM of nitrites/g of tissue) in rat aorta compared with vehicle (p < 0.05). In addition, pre-treatment with tetraethylammonium (TEA, 5 mM) and 2-aminopyridine (2-AP, 0.1 microM) shifted to the right the relaxant curve induced by tilianin (p < 0.05). Finally, a single oral administration of tilianin (50 mg/kg) exhibited a significant decrease in systolic and diastolic blood pressures (p < 0.05) in SHR model. Results indicate that tilianin mediates relaxation mainly by an endothelium-dependent manner,probably due to NO release, and also through an endothelium-independent pathway by opening K+ channels, both causing the antihypertensive effect.


Assuntos
Agastache/química , Anti-Hipertensivos/uso terapêutico , GMP Cíclico/fisiologia , Flavonoides/uso terapêutico , Glicosídeos/uso terapêutico , Ativação do Canal Iônico/efeitos dos fármacos , Óxido Nítrico/fisiologia , Canais de Potássio/fisiologia , Vasodilatadores/uso terapêutico , Relação Dose-Resposta a Droga , Flavonoides/isolamento & purificação , Glicosídeos/isolamento & purificação , Humanos , Medicina Tradicional , Metanol , México , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Plantas Medicinais , Canais de Potássio/efeitos dos fármacos
10.
Vascul Pharmacol ; 49(1): 26-31, 2008 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-18534917

RESUMO

The aim of the present study was to evaluate the possible mechanism of the vasorelaxant action of methanol extract from Laelia autumnalis (MELa) in isolated rat aortic rings, and to establish its antihypertensive activity in vivo. MELa (0.15-->50 microg/mL) induced relaxation in aortic rings pre-contracted with KCl (80 mM), showing an IC50 value of 34.61+/-1.41 microg/mL and E max value of 85.0+/-4.38% (in endothelium-intact rings) and an IC50 value of 45.11+/-4.17 microg/mL and E max value of 80.0+/-12.1% (in endothelium-denuded rings). Serotonin (5-HT, 1 x 10(-4) M) provoked sustained contraction, which was markedly inhibited by MELa (0.15-->50 microg/mL) in a concentration-dependent and endothelium-independent manner. Pretreatment with MELa (15, 46, 150, 300 and 1500 microg/mL) also inhibited contractile responses to norepinephrine (NE 1 x 10(-11) M to 1 x 10(-5.5) M). In endothelium-denuded rings, the vasorelaxant effect of MELa was reduced partially by ODQ (1 microM), but not by tetraethylammonium (5 microM), glibenclamide (10 microM), and 2-aminopyridine (100 microM). The extract also reduced NE-induced transient contraction in Ca2+-free solution, and inhibited contraction induced by increasing external calcium in Ca2+-free medium plus high KCl (80 mM). The antihypertensive effect of MELa was determined in spontaneously hypertensive rats (SHR). A single oral administration of the extract (100 mg/kg) exhibited a significant decrease in systolic and diastolic blood pressure and heart rate (p<0.05) in SHR rats. Our results suggest that MELa induces relaxation in rat aortic rings through an endothelium-independent pathway, involving blockade of Ca2+ channels and a possible cGMP enhanced concentrations and also causes an antihypertensive effect.


Assuntos
Anti-Hipertensivos/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Músculo Liso Vascular/efeitos dos fármacos , Orchidaceae/química , Animais , Aorta Torácica/efeitos dos fármacos , Pressão Sanguínea/efeitos dos fármacos , Cálcio/farmacologia , Técnicas In Vitro , Masculino , Contração Muscular/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Norepinefrina/farmacologia , Extratos Vegetais/farmacologia , Cloreto de Potássio/farmacologia , Ratos , Ratos Wistar , Retículo Sarcoplasmático/efeitos dos fármacos , Retículo Sarcoplasmático/metabolismo , Serotonina/farmacologia
11.
Life Sci ; 79(11): 1062-8, 2006 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-16630635

RESUMO

We have determined that the methanolic extract of L. caulescens (MELc) produced a significant vasodilator effect in a concentration-dependent and endothelium-dependent manner. This relaxation was blocked by N(omega)-nitro-L-arginine methylester (L-NAME), indicating that MELc vasodilator properties are endothelium mediated due to liberation of nitric oxide (NO). In this paper we aimed to corroborate its mode of action. MELc effects on noradrenaline (NA)-induced contraction in isolated rat aortic thoracic rings with endothelium (+E), in the presence of atropine (0.1 microM) and 1-H-[1,2,4]-oxadiazolo-[4,3a]-quinoxalin-1-one (ODQ, 1 microM) were conducted. MELc relaxation curve was significantly shifted to the right in the presence of ODQ and atropine, thus confirming that its mode of action is related with activation of nitric oxide synthase (NOS) and the consequent increment in NO formation. Bio-guided study of MELc allowed the isolation of ursolic acid (UA, 50 mg) and ursolic-oleanolic acids mixture [UA/OA (7:3), 450 mg]. The relaxant effect of UA (0.038-110 microM) was evaluated in functional experiments. UA induced a significant relaxation in a concentration- and endothelium-dependent manner (IC(50)=44.15 microM) and did not produce a vasorelaxant effect on contraction evoked by KCl (80 mM). In addition, NA-induced contraction was significantly displaced to the right by UA (30 microM). In order to determine its mode of action, UA-induced relaxant effect was evaluated in the presence of atropine (0.1 microM), indomethacin (10 microM), L-NAME (100 microM) and ODQ (1 microM). Relaxation was blocked by L-NAME and ODQ. On the other hand, UA (3 microM) provoked a significant displacement to the left in the relaxation curve induced by sodium nitroprusside (SNP, 0.32 nM to 0.1 microM), but it was not significant in the presence of Carbamoyl choline (carbachol, 1 nM to 10 microM). These results indicate that UA-mediated relaxation is endothelium dependent, probably due to NO release, and the consequent activation of vascular smooth muscle soluble guanylate cyclase (sGC), a signal transduction enzyme that forms the second messenger cGMP.


Assuntos
Endotélio Vascular/efeitos dos fármacos , Lamiaceae/química , Óxido Nítrico/metabolismo , Triterpenos/farmacologia , Vasodilatação , Vasodilatadores/farmacologia , Animais , Aorta Torácica/efeitos dos fármacos , Aorta Torácica/metabolismo , Atropina/farmacologia , Endotélio Vascular/metabolismo , Ativação Enzimática , Inibidores Enzimáticos/farmacologia , Técnicas In Vitro , Masculino , NG-Nitroarginina Metil Éster/farmacologia , Óxido Nítrico Sintase/antagonistas & inibidores , Óxido Nítrico Sintase/efeitos dos fármacos , Oxidiazóis/farmacologia , Extratos Vegetais/farmacologia , Quinoxalinas/farmacologia , Ratos , Ratos Wistar , Triterpenos/análise , Triterpenos/isolamento & purificação , Vasodilatação/efeitos dos fármacos , Ácido Ursólico
12.
Life Sci ; 79(5): 430-5, 2006 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-16487544

RESUMO

The relaxant activity of 2-(o, p-substituted phenyl)-1H-benzimidazole derivatives with various 5- and 6-position substituents (-H, -CH3, -NO2, -CF3), namely 1-7, was recorded using the in vitro rat aorta ring test. Compounds 3 and 6 [2-(5-nitro-1H-benzimidazol-2-yl)phenol and 2-(4-methoxyphenyl)-5-nitro-1H-benzimidazole] were prepared using a short route, and were the most potent compounds of the series, showing IC50 value of 0.95 and 1.41 (with endothelium) and 2.01 and 3.61 microM (without endothelium), respectively. Studying further structure-activity relationships through the use of bioisosteric substitution in these benzimidazole derivatives should provide novel vasorelaxant leads and possibly against hypertensive diseases.


Assuntos
Aorta/efeitos dos fármacos , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Fatores Relaxantes Dependentes do Endotélio/síntese química , Fatores Relaxantes Dependentes do Endotélio/farmacologia , Animais , Benzimidazóis/química , Relação Dose-Resposta a Droga , Fatores Relaxantes Dependentes do Endotélio/química , Técnicas In Vitro , Masculino , Ratos , Ratos Wistar
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