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Dive into the research topics where Julio Rivera-Leyva is active.

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Featured researches published by Julio Rivera-Leyva.


Bioorganic & Medicinal Chemistry | 2010

Synthesis, vasorelaxant activity and antihypertensive effect of benzo[d]imidazole derivatives

Gabriel Navarrete-Vázquez; Sergio Hidalgo-Figueroa; Mariana Torres-Piedra; Jorge Vergara-Galicia; Julio Rivera-Leyva; Samuel Estrada-Soto; Ismael León-Rivera; Berenice Aguilar-Guardarrama; Yolanda Rios-Gómez; Rafael Villalobos-Molina; Maximiliano Ibarra-Barajas

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.


Fitoterapia | 2010

Vasorelaxant and antihypertensive effects of methanolic extract from roots of Laelia anceps are mediated by calcium-channel antagonism.

Jorge Vergara-Galicia; Rolffy Ortiz-Andrade; Julio Rivera-Leyva; Patricia Castillo-España; Rafael Villalobos-Molina; Maximiliano Ibarra-Barajas; Itzell Gallardo-Ortiz; Samuel Estrada-Soto

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.


Mutation Research-genetic Toxicology and Environmental Mutagenesis | 2012

Effect of melatonin administration on DNA damage and repair responses in lymphocytes of rats subchronically exposed to lead.

Minerva Martínez-Alfaro; Daniel Hernández-Cortés; Katarzyna Wrobel; Gustavo Cruz-Jiménez; Julio Rivera-Leyva; Rosa María Piña-Zentella; Alfonso Cárabez Trejo

Lead exposure induces DNA damage, oxidative stress, and apoptosis, and alters DNA repair. We investigated the effects of melatonin co-administered to rats during exposure to lead. Three doses of lead acetate (10, 50 and 100mg/kg/day) were administered to rats during a 6-week period. Lymphocytes were analyzed. Lead exposure decreased glutathione (GSH) levels in blood, and at doses of 100mg/kg/day and 50mg/kg/day without melatonin, caused high levels of DNA damage, induced apoptosis, and altered DNA repair. Melatonin co-treatment did not attenuate the effects of lead at 100mg/kg/day, indicating that the effect of melatonin on GSH reduction is not sufficient to reduce the genotoxic effects of lead at this high dose. After 6 weeks of treatment, decreased weight gain was observed in high lead-dose groups (100mg/kg/day), with or without melatonin, and in medium-dose groups (50mg/kg/day) with melatonin, compared with the control group. The protective action of melatonin against lead toxicity is dependent on the dose of lead. Further pharmacological studies are needed to determine whether melatonin acts via melatonin membrane receptors on lymphocytes.


Indian Journal of Pharmaceutical Sciences | 2012

Comparative Studies on the Dissolution Profiles of Oral Ibuprofen Suspension and Commercial Tablets using Biopharmaceutical Classification System Criteria

Julio Rivera-Leyva; M García-Flores; Adriana Valladares-Méndez; Luis Manuel Orozco-Castellanos; M Martínez-Alfaro

In vitro dissolution studies for solid oral dosage forms have recently widened the scope to a variety of special dosage forms such as suspensions. For class II drugs, like Ibuprofen, it is very important to have discriminative methods for different formulations in physiological conditions of the gastrointestinal tract, which will identify different problems that compromise the drug bioavailability. In the present work, two agitation speeds have been performed in order to study ibuprofen suspension dissolution. The suspensions have been characterised relatively to particle size, density and solubility. The dissolution study was conducted using the following media: buffer pH 7.2, pH 6.8, 4.5 and 0.1 M HCl. For quantitative analysis, the UV/Vis spectrophotometry was used because this methodology had been adequately validated. The results show that 50 rpm was the adequate condition to discriminate the dissolution profile. The suspension kinetic release was found to be dependent on pH and was different compared to tablet release profile at the same experimental conditions. The ibuprofen release at pH 1.0 was the slowest.


Journal of Ethnopharmacology | 2011

Validated liquid chromatographic method and analysis of content of tilianin on several extracts obtained from Agastache mexicana and its correlation with vasorelaxant effect.

Oswaldo Hernández-Abreu; Liliana Durán-Gómez; Roberto Best-Brown; Rafael Villalobos-Molina; Julio Rivera-Leyva; Samuel Estrada-Soto

ETHNOPHARMACOLOGICAL RELEVANCE To optimize the obtention of tilianin, an antihypertensive flavonoid isolated from Agastache mexicana (Lamiaceae), a medicinal plant used in Mexico for the treatment of hypertension. Also, a validated HPLC method to quantify tilianin from different extracts, obtained by several extraction methods, was developed. MATERIALS AND METHODS The aerial parts of Agastache mexicana were dried at different temperatures (22, 40, 50, 90, 100 and 180°C) and the dry material was extracted with methanol by maceration to compare the content of the active constituent tilianin in the samples. Furthermore, EtOH:H(2)O (7:3), infusion and decoction extracts were prepared from air-dried samples at room temperature to compare the content and composition of the different extraction methods. Moreover, an ex vivo vasorelaxant test on endothelium-intact aortic rat rings was conducted, in order to correlate the presence of tilianin with the activity of each extract. RESULTS Higher concentration and amounts of tilianin were determined from chromatograms in the obtained methanolic extracts from plant material dried at 90, 50, 40 and 22°C, followed by 100°C; however, lower concentrations were observed in dried at 180°C and EtOH:H(2)O (7:3). It is worth to notice that methanolic extracts with higher amount of tilianin were the most potent vasorelaxant extracts, even though these extracts were less potent than carbachol, a positive control used. Finally, decoction, infusion and EtOH:H(2)O (7:3) extracts did not show any vasorelaxant effect. CONCLUSION Results suggest that extracts with higher concentration of tilianin possess the best vasorelaxant activity, which allowed us to have a HPLC method for future quality control for this medicinal plant.


Journal of Pharmacy and Pharmacology | 2010

Vasorelaxant effect of Valeriana edulis ssp. procera (Valerianaceae) and its mode of action as calcium channel blocker

Samuel Estrada-Soto; Julio Rivera-Leyva; Juan José Ramírez-Espinosa; Patricia Castillo-España; Francisco Aguirre-Crespo; Oswaldo Hernández-Abreu

Objectives  The aim was to evaluate the relaxant effect of extracts from Valeriana edulis and determine the possible mechanism of action of the hexanic extract as vasorelaxant agent.


Bioorganic & Medicinal Chemistry Letters | 2014

Evaluation of the neuroprotective activity of stansin 6, a resin glycoside from Ipomoea stans.

Ismael León-Rivera; Juana Villeda-Hernández; Victoria Campos-Peña; Alma Aguirre-Moreno; Samuel Estrada-Soto; Gabriel Navarrete-Vázquez; María Yolanda Rios; Berenice Aguilar-Guadarrama; Patricia Castillo-España; Julio Rivera-Leyva

Stansin 6 a tetrasaccharide resin glycoside isolated from the root of Ipomoea stans was evaluated as anticonvulsant and neuroprotective in kainic acid-induced seizures of rats. Intraperitoneal injection of kainic acid (10 mg/kg) induced typical behavioral seizures such as wet dog shakes and limbic seizures, and histopathological changes in the hippocampus (degeneration and loss of pyramidal cells in CA1 to CA4 areas). Stansin 6 (10-80 mg/kg) had no effect on the behavior of rats and did not induce hippocampal damage. Pretreatment with stansin 6 inhibited convulsions in rats from kainic acid-induced seizures, reduced the degeneration pattern in the CA3 region, decreased astrocytic reactivity, and reduced the expression of IL-1β and TNF-α induced by kainic acid. These results suggest that stansin 6 possesses neuroprotective and anticonvulsant activities.


Journal of Chemistry | 2017

Synthesis and In Vitro AMPK Activation of Cycloalkyl/Alkarylbiguanides with Robust In Vivo Antihyperglycemic Action

Erika J. Gutiérrez-Lara; Carlos Martínez-Conde; Edgar Rosales-Ortega; Juan José Ramírez-Espinosa; Julio Rivera-Leyva; David Centurión; Karla Carvajal; Daniel Ortega-Cuellar; Samuel Estrada-Soto; Gabriel Navarrete-Vázquez

This work describes the design, synthesis in one step, and the in vitro, in vivo, and in silico antidiabetic evaluation of a series of ten alicyclic and aromatic (alkyl


Pharmacognosy Magazine | 2017

Methyl jasmonate and salicylic acid enhanced the production of ursolic and oleanolic acid in callus cultures of Lepechinia Caulescens

Víctor M Vergara Martínez; Samuel Estrada-Soto; José de Jesús Arellano-García; Julio Rivera-Leyva; Patricia Castillo-España; Angélica Flores Flores; Alexandre Cardoso-Taketa; Irene Perea-Arango

Background: The production of triterpenes from plants for pharmacological purposes varies in concentration, due to genetic and environmental factors. In vitro culture enables the control and increase of these bioactive molecules. Objective: To evaluate the effect of plant growth regulators and elicitors in the induction of calli and the production of ursolic acid (UA) and oleanolic acid (OA) in Lepechinia caulescens. Materials and Methods: Leaf explants were exposed for the induction of calli at different concentrations and combinations of 2,4-dichlorophenoxyacetic acid (2,4-D) and 6-benzylaminopurine (BAP). Methyl jasmonate (MJ) and salicylic acid were used as elicitors. High-performance liquid chromatography method was used to quantify UA and OA content in each treatment. Results: Treatment with 3.0 mg/L of 2,4-D and 0.1 mg/L of BAP produced the best results for calli induction and production of UA (1.57 mg/g dry weight [DW]) and OA (1.13 mg/g DW). Both elicitors facilitated the accumulation of triterpenes. Conclusion: The combination of auxins and cytokinins showed favorable results for the induction of calli. Variation concerning the accumulation of UA and OA was observed between treatments. MJ increased the production of triterpenes five times after 8 h of exposure, compared to control treatment. There is a greater accumulation of UA (16.58 mg/g DW) and OA (1.94 mg/g DW) in leaves of wild plants. Abbreviations used: 2,4-D: 2,4-dichlorophenoxyacetic acid, BAP: 6-benzylaminopurine, DW: Dry weight, MJ: Methyl jasmonate, OA: Oleanolic acid, PGRs: Plant growth regulators, UA: Ursolic acid, SA: Salicylic acid.


Molecules | 2017

Biopharmaceutical Characterization and Bioavailability Study of a Tetrazole Analog of Clofibric Acid in Rat

Nancy Vara-Gama; Adriana Valladares-Méndez; Gabriel Navarrete-Vázquez; Samuel Estrada-Soto; Luis Manuel Orozco-Castellanos; Julio Rivera-Leyva

In the current investigation, the physicochemical, biopharmaceutical and pharmacokinetic characterization of a new clofibric acid analog (Compound 1) was evaluated. Compound 1 showed affinity by lipophilic phase in 1 to 5 pH interval, indicating that this compound would be absorbed favorably in duodenum or jejunum. Also, Compound 1 possess two ionic species, first above of pH 4.43 and, the second one is present over pH 6.08. The apparent permeability in everted sac rat intestine model was 8.73 × 10−6 cm/s in duodenum and 1.62 × 10−5 cm/s in jejunum, suggesting that Compound 1 has low permeability. Elimination constant after an oral administration of 50 μg/kg in Wistar rat was 1.81 h−1, absorption constant was 3.05 h−1, Cmax was 3.57 μg/mL at 0.33 h, AUC0–α was 956.54 μ/mL·h and distribution volume was 419.4 mL. To IV administration at the same dose, ke was 1.21 h−1, Vd was 399.6 mL and AUC0–α was 747.81 μ/mL·h. No significant differences were observed between pharmacokinetic parameters at every administration route. Bioavailability evaluated was 10.4%. Compound 1 is metabolized to Compound 2 probably by enzymatic hydrolysis, and it showed a half-life of 9.24 h. With these properties, Compound 1 would be considered as a prodrug of Compound 2 with potential as an antidiabetic and anti dyslipidemic agent.

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Samuel Estrada-Soto

Universidad Autónoma del Estado de Morelos

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Gabriel Navarrete-Vázquez

Universidad Autónoma del Estado de Morelos

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Patricia Castillo-España

Universidad Autónoma del Estado de Morelos

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Adriana Valladares-Méndez

Universidad Autónoma del Estado de Morelos

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Juan José Ramírez-Espinosa

Universidad Autónoma del Estado de Morelos

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Oswaldo Hernández-Abreu

Universidad Autónoma del Estado de Morelos

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Rafael Villalobos-Molina

National Autonomous University of Mexico

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Emanuel Hernández-Núñez

Universidad Autónoma del Estado de Morelos

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Francisco Aguirre-Crespo

Universidad Autónoma del Estado de Morelos

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