ABSTRACT
The mandible condylar process cartilage (CP) of Wistar rats is a secondary cartilage and acts as a mandibular growth site. This phenomenon depends on adequate proteins intake and hormone actions, including insulin. Objectives The present study evaluated the morphological aspects and the expression of the insulin receptor (IR) in the cartilage of the condylar process (CP) of rats subjected to protein undernourishment. Material and Methods The nourished group received a 20% casein diet, while the undernourished group (U) received a 5% casein diet. The re-nourished groups, R and RR, were used to assess the effects of re-nutrition during puberty and adulthood, respectively. CPs were processed and stained with picro-sirius red, safranin-O and azocarmine. Scanning electron microscopy and immunohistochemistry were also performed. Results The area of the CP cartilage and the number of cells in the chondroblastic layer decreased in the U group, as did the thickness of the CP layer in the joint and hypertrophic layer. Renourishment during the pubertal stage, but not during the adult phase, restored these parameters. The cell number was restored when re-nutrition occurred in the pubertal stage, but not in the adult phase. The extracellular matrix also decreased in the U group, but was restored by re-nutrition during the pubertal stage and further increased in the adult phase. IR expression was observed in all CPs, being higher in the chondroblastic and hypertrophic cartilage layers. The lowest expression was found in the U and RR groups. Conclusions Protein malnutrition altered the cellularity, the area, and the fibrous cartilage complex, as well as the expression of the IRs. .
Subject(s)
Animals , Mice , Anti-Inflammatory Agents, Non-Steroidal/metabolism , Cyclooxygenase 1/metabolism , /metabolism , Cyclooxygenase Inhibitors/metabolism , Piroxicam/analogs & derivatives , Thiazines/metabolism , Thiazoles/metabolism , Amino Acid Substitution , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Arginine/chemistry , Arginine/genetics , Arginine/metabolism , Binding Sites , Catalytic Domain , Cyclooxygenase 1/chemistry , Cyclooxygenase 1/genetics , /chemistry , /genetics , Cyclooxygenase Inhibitors/chemistry , Hydrogen Bonding , Leucine/chemistry , Leucine/genetics , Leucine/metabolism , Mutation , Piroxicam/chemistry , Piroxicam/metabolism , Protein Structure, Secondary , Serine/chemistry , Serine/genetics , Serine/metabolism , Thiazines/chemistry , Thiazoles/chemistry , Tyrosine/chemistry , Tyrosine/genetics , Tyrosine/metabolism , WaterABSTRACT
The value of meloxicam as a non-steroidal anti-inflammatory drug is well established. This study was carried out to formulate a stable and effective meloxicam topical preparation. The in vitro release of meloxicam from different semisolid bases, which are: o/w, w/o emulsions, sodium carboxy methylcellulose gel and carbomer gel base was established. The study also involved the diffusion of meloxicam through excised mouse skin with different concentrations using carbomer gel in addition to the effect of different enhancing agents such as PG [Propylene Glycol], methyl salicylate, urea, oleic acid, DMSO [Dimethyl Sulfoxide], xanthan gum and PEG 1000 [Poly Ethylene Glycol] and the last one gave the highest diffusion. The results showed that the selected formula of meloxicam was not irritant and this result was supported by histological examination. In addition, the results showed that the use of disodium EDTA [stabilizer] gave more stable formula where the expiration date was 2 years compared to 0.8 year when using both dl- alpha tocopherol and blank formula. The results showed that the temperature and the storage period led to decrease both the diffusion rate and viscosity of meloxicam 1% gel but with little change in pH. On the other hand preliminary clinical study was carried out for 26 patients and the results indicated that 84.6% of patients got positive responses
Subject(s)
Thiazines/chemistry , Thiazines/pharmacology , Thiazines/pharmacokinetics , Diffusion , Anti-Inflammatory Agents, Non-Steroidal , Carboxymethylcellulose Sodium , Propylene Glycol , Dimethyl Sulfoxide , Polyethylene GlycolsABSTRACT
4-aryl-1,2,3,4-tetrahydro-5-oxoindeno [1,2-d] pyrimidine-2-thiols [I] were synthesized in the laboratories and their corresponding hydrazono derivatives [II] were submitted to react with chloroacetic acid, 2-bromopropionic acid or 3-bromopropionic acid in the presence of fused sodium acetate and acetic anhydride to give 5-aryl-2,3- dihydro-5H, 6-arylhydrazonoindeno [1,2-d] thiazolo [3,2-a] pyrimidin-3-ones [III], its methyl derivatives [IV] and 6-aryl-6H, 7-arylhydrazonoindeno [1,2-d]-pyrimidino-[2,1-b]-1,3-thiazin-4-ones [V], respectively. The indenothiazolopyrimidones [III] condensed with aromatic aldehydes in the presence of acetic anhydride to yield 2-arylmethylene-5 aryl-2,3-dihydro-5H-6-arylhydrazonoimdeno [1,2-d] thiazolo [3,2-a] pyrimidin-3-ones [VI], which was obtained directly from their arylhydrazono derivatives [II] by the reaction of chloroacetic acid in the presence of the corresponding aromatic aldehyde and in refluxing acetic acid/acetic anhydride mixture