ScienceRise: Biological Science

Study of analgesic and myotropic spasmolytic activity of alkylcarb

Fri, 30 Jun 2023 00:00:00 +0300

The work is devoted to the search for new biologically active substances in a series of alkylamides of dihydroquinoline-3-carboxylic acid. Analgesic properties of 30 newly synthesized substances were studied, which made it possible to identify the leader compound (provisional name alkylcarb) and recommend its effectiveness for further research as an antispasmodic agent for pain relief. It has been established experimentally, that the substance alkylcarb exhibits concentration-dependent vasodilatory properties in vitro on segments of the thoracic aorta of rats. The data, obtained in the work, justify the prospect of using the leader substance as a new analgesic and antispasmodic drug. The research expands and deepens knowledge about the pharmacological properties of alkylamide derivatives of dihydroquinoline-3-carboxylic acid.

The aim of the work was to conduct screening studies to establish the analgesic activity of a newly synthesized series of chemical compounds among alkylamides of dihydroquinoline-3-carboxylic acid and to study the myotropic spasmolytic activity of the leader substance.

Materials and methods. Analgesic properties of alkylamides of dihydroquinoline-3-carboxylic acid were studied on outbred white mice in the "acetic acid convulsions" test. During the experiment, the animals were treated in accordance with the International Principles of the European Convention for the Protection of Vertebrate Animals Used for Experiments and Other Scientific Purposes (Strasbourg, March 18, 1986). The studied substances were administered intragastrically to experimental animals at a dose of 10 mg/kg in the form of a finely dispersed aqueous suspension, stabilized with Tween-80. Voltaren at a dose of 8 mg/kg, recommended for preclinical studies, and analgin at a dose of 50 mg/kg were chosen as reference drugs.

The studies of the contractile activity of smooth muscle vessels were carried out on segments of the thoracic aorta of rats of both sexes weighing 180-200 g. The studies of dilator reactions were carried out against the background of preliminary contraction with phenylephrine at a concentration of 10^-6 mol/l. The antispasmodic efficiency of the new compound was determined in comparison with the classic antispasmodic drotaverine.

The statistical processing of the results was carried out using the package of statistical analysis of electronic spreadsheets Exel, with the help of the program "Statgraphics Plus v. 3.0.” and the standard package of statistical programs "Statistica, V. 6.0". We used the Student's test, a non-parametric analog of univariate variance analysis - the Kruskal-Wallis test, and the Mann-Whitney test. Differences were considered statistically significant at p<0.05.

Results. The study of the analgesic activity of substances АO₁-АO₃₀ in the "acetic acid convulsion" test in mice showed that a compound АO₂₆ (provisional name alkylcarb) has the most pronounced analgesic activity when administered intragastrically. In the "acetic acid convulsion" test, alkylcarb (10 mg/kg, per os) probably reduces the number of convulsions, caused by acetic acid. The level of activity of this compound is comparable to the activity of diclofenac (8 mg/kg, per os) and exceeds analgin (50 mg/kg, per os). The substance alkylcarb relieved vasospasm at the level of the comparison drug drotaverine in in vitro experiments on a model of an isolated fragment of the thoracic aorta of rats against the background of previous constriction with phenylephrine.

Conclusion. Today, the search for new highly effective non-opioid analgesics is an urgent problem of modern pharmacology, since painkillers used in clinical practice do not meet the requirements of efficiency and safety. In this regard, in recent years, scientists of the National Pharmaceutical University have been intensively searching for new, highly effective substances with antinociceptive, anti-inflammatory and antipyretic effects among alkylamides of dihydroquinoline-3-carboxylic acid.

Study of the antiulcer activity of garden cabbage extract on the chronic acetic ulcer model in rats

Fri, 30 Jun 2023 00:00:00 +0300

The aim of the study was to study the gastroprotective properties of the dry extract of garden cabbage in the model of chronic acetic ulcer in rats.

Materials and methods. Chronic ulcerative lesions of the gastric mucosa of rats were modeled by introducing 0.05 ml of a 30 % solution of acetic acid into the subserous layer of the stomach wall. The dry extract of garden cabbage in a conditionally therapeutic dose of 50 mg/kg and reference drugs omeprazole and altan were administered intragastrically for 10 days, starting from the second day of the experiment. When choosing the duration of the course of treatment, we proceeded from the data that the effectiveness of the antiulcer action in the clinic is assessed after 10-12 days of treatment. The percentage of animals with ulcers in the group, the state of the gastric mucosa were evaluated, the ulcer index and antiulcer activity were calculated. To elucidate the possible mechanism of action of the extract, we studied its effect on synthetic processes in terms of the content of RNA and DNA in homogenates of the gastric mucosa by the spectrophotometric method by reaction with perchloric acid.

Results. On the model of stomach damage, caused by acetic acid, a pronounced antiulcer activity of the extract (54.26) was established at the level of omeprazole (54.62). The maximum antiulcer activity (72.75) was revealed when using the combination of the extract with omeprazole, which, in terms of ulcerative effect, is superior to monotherapy with the extract, omeprazole and altan (35.08).

Reparative regeneration is a component of an adaptive tissue reaction; under conditions of violation of the reparative potencies of the mucosa, chronic diseases of the gastrointestinal tract develop. Since the final goal of antiulcer therapy is the healing of the ulcer, and the basis of this process is reparative regeneration, the reparative properties of the extract have been studied. Under the influence of cabbage extract, the content of RNA and DNA in the mucosa probably increased by 2.8 and 2.4 times, respectively, at the same level with omeprazole. If possible, to activate the synthetic processes of DEGC and omeprazole, altan significantly prevailed.

The most pronounced effect of enhancing reparative processes was established with the combined use of the extract and omeprazole, which turned out to be a significant increase in the content of RNA and DNA in the gastric mucosa by 3.2 and 2.9 times compared with the control.

Conclusions. On the model of chronic damage to the stomach of rats, cabbage extract showed an antiulcer effect, the severity of which was not inferior to the comparison drug, the proton pump inhibitor omeprazole, and significantly exceeded the phytopreparation - altan. The combined use of the extract and omeprazole showed the highest preventive effect of preventing the negative effects of acetic acid on the gastric mucosa. One of the mechanisms of the gastroprotective action of the extract is its ability to enhance reparative processes in the gastric mucosa. The results obtained indicate the prospects for further research on the antiulcer properties of cabbage extract with a view to its use in the complex therapy of peptic ulcer

Effectiveness of a new means of etiotropic therapy of mastits in cows during the lactation period

Fri, 30 Jun 2023 00:00:00 +0300

The aim: is to study the therapeutic effectiveness of the new veterinary medicinal product Revozyn RTU 400 mg/ml (suspension for injections), manufactured by Eurovet Animal Health B.V. (Netherlands), in the treatment of acute (clinical) and hidden (subclinical) mastitis in cows during lactation.

Materials and methods. The research was conducted on dairy cows of the Simmental breed with a milk productivity of 6000-6500 kg of milk per lactation (F "Pchany-Denkovich", Pchany village, Stryi district, Lviv region). To confirm the diagnosis of "acute mastitis" and to identify cows with hidden (subclinical) mastitis, as well as to establish the effectiveness of the researched drug after treatment, a sample was taken with the California Mastitis Test (CMT), manufactured by Bayer Animal Health GmbH, Germany. For bacteriological research, milk samples were taken from the affected quarters of the mammary gland (1 sample from each cow) in compliance with generally accepted sanitary rules. The sensitivity of bacterial isolates to the drug was determined by diffusion in agar using standard discs with benzylpenicillin.

Results. A clinical examination of 127 Simmental dairy cows of different periods of lactation was carried out. During the clinical-diagnostic examination of animals, 8 cows with clinically pronounced, acute course of mastitis were found. According to the nature of the exudate in 3 cows, mastitis was serous, in 5 cows it was purulent-catarrhal. For serous mastitis, the CM test gave a positive result – thickening, the milk solution looks like a gel. In case of purulent catarrh, a sample with the CMT gave a strongly positive result – the mixture thickened, the gel took on a certain shape and became very viscous. The CMT revealed 12 cows with suspected latent mastitis. Representatives of opportunistic microflora – Streptococcus agalactiae, Staphylococcus aureus, and Escherichia coli bacteria were isolated and identified from mastitis milk. The summarized results of the clinical trial of the drugs Revozyn RTU 400 mg/ml and Procillin® 30 % on cows suffering from the clinical form of mastitis were as follows. On the 10th day of the experiment, a milk sample with the California mastitis test showed that all milk samples from cows of both groups (with the exception of one milk sample from a cow from the control group) gave a negative result (the solution remained liquid, blue or gray and homogeneous, without clots). Taking into account the results of the CMT and the number of somatic cells in the milk after the therapy, the therapeutic effectiveness of the veterinary medicinal product Revozyn RTU 400 mg/ml in the treatment of various forms of mastitis in lactating cows was 100 %, and the one of the comparative drug Procillin® 30 % was 83.3 % .

Conclusions. A clinical study of the veterinary medicinal product Revozyn RTU 400 mg/ml, suspension for injections, manufactured by Eurovet Animal Health B.V. (Netherlands) established its effectiveness in the dosage, recommended by the manufacturer, in the treatment of clinical and subclinical mastitis in lactating cows, caused by microorganisms sensitive to benzylpenicillin. In terms of therapeutic effectiveness, the drug Revozyn RTU 400 mg/ml was not inferior to the comparative drug Procillin® 30 % in its dosage form and active substance when used in the treatment of various forms of mastitis in lactating cows

Ultrasound and x-ray examination at lung edema of domestic cat

Fri, 30 Jun 2023 00:00:00 +0300

The aim: This study aims to determine the diagnostic value of lung ultrasound compared with radiography for respiratory distress in cats.

Materials and methods: The database of the veterinary center was analyzed. 130 animals diagnosed with pulmonary edema were selected. The lungs of sick cats were examined ultrasonographically; The line was counted in 4 anatomical sections on each hemithorax. A site was evaluated as positive when > 3 "B-lines" were detected. Animal treatment protocols were studied to clarify the final diagnosis (reference standard), and the sensitivity and specificity of lung ultrasound and chest X-ray for the diagnosis of pulmonary edema were calculated.

Result: Cats with a final diagnosis of cardiogenic pulmonary edema had a greater number of positive areas on ultrasound than those, in which respiratory distress was caused by non-cardiogenic pulmonary edema. The overall sensitivity and specificity of US for the diagnosis of pulmonary edema were 87 % and 89 %, respectively, and these values were similar to those of chest radiography (85 % and 86 %, respectively). The use of ultrasound led to a false diagnosis of cardiogenic pulmonary edema (ie, a false-positive result) in animals with diffuse interstitial or alveolar changes.

Conclusions: Ultrasound examination of the lungs in cats with respiratory distress syndrome is a promising diagnostic method. Emergency diagnosis of pulmonary edema in cats is difficult, especially in patients with severe shortness of breath, and limits the diagnostic evaluation. Chest x-rays are considered the standard diagnostic test, but the results are sometimes ambiguous and the process of obtaining the x-rays can increase respiratory distress in the animal.

According to the results of the study, it was established, that ultrasound examination of the lungs can be used to differentiate the causes of shortness of breath (cardiogenic and non-cardiogenic) with sufficiently high sensitivity and specificity and less influence of the iatrogenic factor on the development of respiratory distress in cats, compared to chest radiography

Bacterial risks and determination of critical control points at the industrial production of chicken edible egg

Denys Demianenko — Fri, 30 Jun 2023 00:00:00 +0300

The aim: study the bacterial risks and to determine the control critical points at the industrial production of chicken edible egg.

Materials and methods. The first stage of our research was to study the degree of risk of contamination by opportunistic and pathogenic microflora at all stages of production of chicken edible eggs according to ISO 22000:2007. In order to achieve the goal, bacteriological research was conducted on pathological material from day-old chickens and adult birds, the content of marketable eggs from birds of different age groups; as well as washed from the equipment of poultry farms, the repair young poultry department, the industrial herd department, egg sorting and certification workshops, from the surface of the egg, from the working surfaces of special vehicles. Bacterial contamination of air, droppings, bedding, complete feed was studied. Bacteriological studies were carried out according to generally accepted schemes, using accumulative, selective and differential diagnostic media (heptadecyl sulfate agar, endo, xylose-lysine agar, differentiated agar with diamond green, Muller-Hinton). The sampling was carried out using universal sterile applicators "Voles".

The next stage was to analyze the results of bacteriological studies and determine the basic list of criteria for creating critical control points (CCPs) for the further development of a risk management scheme for the bacterial biosafety of edible eggs according to HACCP principles.

Results. Isolation of S. aureus from the heart and lungs, E. coli, P. aeruginosa, Enterobacter spp, Enterococcus spp - from the intestines of day-old chickens and litter - indicate violations of veterinary and sanitary standards in the hatchery and the low quality of disinfection before the placement of day-old young birds, as well as non-observance of veterinary and sanitary norms for the transportation regime of day-old young birds. Isolation of E. coli, Enterobacter spp, Klebsiella spp.Str. zymogenes from compound feed, and E. coli, Enterobacter spp, Shigella spp. in washings from the equipment of the feed mill is evidence of insufficient veterinary and sanitary control of incoming raw materials, compound feed, as well as poorly carried out disinfection of equipment and specialized vehicles.When examining objects from the production line, E. coli, Enterobacter spp., P. aeruginosa, and S. epiderrmidis were most often isolated. From the pathological material during the bacteriological examination, microflora of the genus E. coli, Streptococcus spp., S. aureus (most often pathogenic serotypes) prevailed. As a result of the analysis of the conducted studies, we determined a basic list of criteria for creating a CCP and developing a risk management scheme for the bacterial biosafety of edible eggs according to the principles of HACCP.

Conclusions. As a result of the bacteriological monitoring of objects of the technological cycle of chicken edible egg production, we established a list of bacteriological risks at all stages of production. As a result of the conducted research, it was determined, that the spectrum of bacterial contamination was mainly represented by opportunistic microflora. In the majority, the following types of microorganisms were detected: E. coli, P. aeruginosa, Enterobacter spp, Enterococcus spp. But C. jejuni, Streptococcus spp., S. aureus. Salmonella spp, which are the most dangerous for the consumer and poultry, were not isolated. We studied the bacterial risks at all the main stages of the industrial production of chicken edible eggs and identified the main critical control points of production according to the principles of the HACCP system