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1.
Front Pharmacol ; 9: 975, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30283333

RESUMEN

Introduction: Strontium ranelate (SrRan) has the potential to interfere in the progression of osteoarthritis (OA), multifactorial disease associated with mechanical problems and articular inflammatory changes. Objectives: This study aimed to test the effects of prophylactic and therapeutic use of SrRan on clinical parameters of pain, the inflammatory process, and degradation of the articular cartilage. Methods: This was an experimental study, using a model of knee OA induced by intra-articular injection of monoiodoacetate. Thirty Wistar rats were divided into five groups and treated as indicated: control, without intervention; prophylactic, received SrRan at a daily oral dose of 250 mg/kg for 28 days before OA induction; SrRan treatments, administered 250 or 500 mg/kg/day for 28 days after the induction; and model control, received saline solution after the induction. Behavioral tests (joint incapacity, mechanical hyperalgesia, tactile sensitivity, and forced ambulation), histological evaluation of articular cartilage, and determination of inflammatory cytokines in the synovial fluid (interleukin [IL]-6, IL-10, tumor necrosis factor [TNF]-α, and interferon [INF]-γ) were performed. Results: Both prophylactic and therapeutic treatments improved the articular discomfort. A prophylactic dose of 500 mg/kg/day also improved mechanical hyperalgesia and the same dose was beneficial on tactile sensitivity. SrRan did not improve ambulation. Levels of IL-6, IL-10, TNF-α, and IFN-γ in SrRan-treated groups with OA were not significantly different compared with those in the normal control animals. The histopathological evaluation showed less articular damage in the SrRan-treated and control groups compared to the saline-treated group. Conclusion: The prophylactic and therapeutic administration of SrRan was associated with improved behavioral patterns of pain, especially joint discomfort. SrRan administration mitigated histological changes in the articular cartilage and reduced the inflammatory process, which beneficially reduced the progression of OA in the experimental model studied.

2.
An Acad Bras Cienc ; 89(3 Suppl): 2273-2280, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28746551

RESUMEN

Control strategies using insecticides are sometimes ineffective due to the resistance of the insect vectors.In this scenario new products must be proposed for the control of insect vectors.The complexes L-aspartate Cu (II) and L-glutamate-Cu (II) complexes were synthesized and characterized by elemental analysis, visible ultraviolet, infrared spectroscopy and potentiometric titration. The toxicity of these complexes was analyzed in Aedes aegypti (Diptera: Culicidae) larvae and Gram-negative and Gram-positive bacteria. The interaction between the ligands and the amino acid balance and the distribution of the species as a function of pH were discussed. The lethal concentration median (LC50) for Ae. aegypti larvae were: L-glutamic acid-Cu (II) - 53.401 mg L-1 and L-aspartate-Cu (II) - 108.647 mg L-1. The minimum inhibitory concentration (MIC) required for Staphylococcus aureus and Escherichia coli was: L-glutamate-Cu (II) 500-2000 mg L-1 and L-aspartate-Cu (II) 1000-2000 mg L-1. The concentrations demonstrated toxicity that evidence the potential of the complexes as bactericide and insecticide. Metal complexes formed by amino acids and transition metals are advantageous because of low environmental toxicity, biodegradability and low production cost.


Asunto(s)
Aedes/efectos de los fármacos , Ácido Aspártico , Cobre , Escherichia coli/efectos de los fármacos , Ácido Glutámico , Staphylococcus aureus/efectos de los fármacos , Animales , Ácido Aspártico/química , Cobre/química , Ácido Glutámico/química , Larva/efectos de los fármacos , Dosificación Letal Mediana , Pruebas de Toxicidad
3.
An. acad. bras. ciênc ; 89(3,supl): 2273-2280, 2017. tab, graf
Artículo en Inglés | LILACS | ID: biblio-886818

RESUMEN

ABSTRACT Control strategies using insecticides are sometimes ineffective due to the resistance of the insect vectors.In this scenario new products must be proposed for the control of insect vectors.The complexes L-aspartate Cu (II) and L-glutamate-Cu (II) complexes were synthesized and characterized by elemental analysis, visible ultraviolet, infrared spectroscopy and potentiometric titration. The toxicity of these complexes was analyzed in Aedes aegypti (Diptera: Culicidae) larvae and Gram-negative and Gram-positive bacteria. The interaction between the ligands and the amino acid balance and the distribution of the species as a function of pH were discussed. The lethal concentration median (LC50) for Ae. aegypti larvae were: L-glutamic acid-Cu (II) - 53.401 mg L-1 and L-aspartate-Cu (II) - 108.647 mg L-1. The minimum inhibitory concentration (MIC) required for Staphylococcus aureus and Escherichia coli was: L-glutamate-Cu (II) 500-2000 mg L-1 and L-aspartate-Cu (II) 1000-2000 mg L-1. The concentrations demonstrated toxicity that evidence the potential of the complexes as bactericide and insecticide. Metal complexes formed by amino acids and transition metals are advantageous because of low environmental toxicity, biodegradability and low production cost.


Asunto(s)
Animales , Staphylococcus aureus/efectos de los fármacos , Ácido Aspártico/química , Ácido Glutámico/química , Cobre/química , Aedes/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Pruebas de Toxicidad , Larva/efectos de los fármacos , Dosificación Letal Mediana
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