Experimental study of state of gastric mucosa in rats under introduction of new derivate of 4-[4-oxo-4h-quinazoline-3-yl] benzoic acid (PC-66)
Journal Title: ScienceRise: Pharmaceutical Science - Year 2017, Vol 0, Issue 2
Abstract
<p>Screening studies have revealed that the new derivate of 4-[4-oxo-4H-quinazoline-3-yl] benzoic acid (compound PC-66) possess significant antinociceptive and weakly expressed anti-inflammatory and antipyretic activity on different models of pain and inflammation. The cоndition of gastric defense under influence of PC-66 is unknown.</p><p>The aim of this study was to explore the ability of PC-66 in comparison with diclophenac sodium produce gastric lesions on intact and rats with adjuvant arthritis, and to determine the role of influence on prostaglandin–H-synthase and stable metabolits of nitric oxide in the pathogenesis of these damages.</p><p>Materials and methods: The impact of PC-66 compound and a diclofenac sodium was explored on macroscopic changes in gastric mucosa under conditions of long-term administration and of experimental inflammation.</p><p>The spectrophotometric method revealed active prostaglandin-endoperoxide synthase in the rats` GM homogenates against accumulation of oxidized form of adrenaline electron donor. The total content of nitrites and nitrates was determined by reaction with Griess reagent after preliminary restoration of nitrates with a suspension of zinc dust in ammonia solution.</p><p>Results and Discussion. PC-66 compound, unlike the reference medicine, did not cause significant gastric lesions under conditions of its long-term administration to intact rats. We found that during diclofenac administration, the activity of PGH-synthetase in GM significantly decreased compared to the control, whilst under the influence of PC-66, the activity of this enzyme remained practically unchanged. Administration of PC-66 compound to rats, unlike diclofenac, was associated with a significant increase of stable NO metabolites in GM, whilst this index decreased compared to control under the influence of investigational NSAID.</p><p>Conclusions: 4- [4-oxo-4H-quinazoline-3-yl] benzoic acid has no damaging effect on the gastric mucosa both in intact animals and in rats with experimental inflammation. The basis of its GM safety rests on lacking inhibitory effect on production of vasodilator molecules in GM of PC-66 compound, unlike diclofenac sodium</p>
Authors and Affiliations
Hanna Kramar
Keywords
Related Articles
- EP ID EP647136
- DOI 10.15587/2519-4852.2017.100549
- Views 131
- Downloads 0
Β-lactam antibiotics in Ukraine: market and consumption analysis in 2013–2018
<p>The strategy of combating the development of antibiotic resistance is a global challenge for the scientific community for the sake of life and health of the population. An analysis of the relationship between the leve...
Verification of dissolution test for doxycycline hyclate in capsules to implement into the pharmacopoeial monograph
<p>The study of dissolution profiles is important as a cheap and easy supplement to bioequivalence research, and as a variation to such studies. This method is not outlined in the State Pharmacopoeia of Ukraine for the d...
Первинний аналіз та пріоритезація ризиків процедури біовейвер
<p><strong>Мета</strong><strong>:</strong> Проведення причинно-наслідкового аналізу ідентифікованих ризиків, ранжування та визначення пріоритетів згідно методології загального оцінювання ризиків для забезпечення належног...
New possibilities of use of oat raw materials for investigation of biologically active components in therapy of experimental diabetes
<p>Aim of the work is to suggest the technology of aqua dynamic extraction of bioactive substances from oat straw. The amount of the extract and the concentration of extracted substances depend on the duration of extract...
Algorithm for carrying out a procedure for verification of a spectrophotometric method for analysis of solid-dosed dosage forms according to the requirements of SPHU 2.0
<p><strong>Aim</strong><strong>. </strong>The increase in the pharmaceutical market of Ukraine of the range of medicines leads to stricter requirements for their quality. According to the requirements of international st...