Introduction: Rheumatoid arthritis (RА) is an immune-inflammatory disease intrinsic to up to 1.0% of the world’s population. Standard drugs for RA therapy are basic medications, glucocorticoids and non-steroid anti-inflammatory drugs, which often only ease or hinder the course of disease, not curing the patient completely. Also, on the average 20-50 % of patients are unresponsive to treatment, allergic to the prescribed drugs or find them ineffective. That is why medications with a different mechanism of action are being widely researched, some of them being antagonists of proteinase-activated receptors (PAR-2). Materials and Methods: The inflammatory process was reproduced by injecting a 2% solution of neutral formalin in a volume of 0.1 mL under the aponeurosis of the posterior left foot. A total of 84 white rats were used in the experiment. Diclofenac sodium was administered as a reference drug. Results and Discussion: An experiment on researching the impact of 5 samples of derivatives of 4.5-dihydroisoxazol-5-carboxamide on formalin oedema development among rats showed that the compound R001, compared with other substances studied, differs in the late onset of the therapeutic effect when ingested; the restoration of the foot volume to the initial level occurs only after the introduction of R005, R004 and R002. R005 to a greater extent than other compounds prevents the development of edema and has greater therapeutic efficacy than diclofenac sodium both with intragastric administration and subcutaneous injection. Conclusion: All five compounds in question showed anti-inflammatory activity, with the spectrum not so unequivocal both in qualitative and quantitative values.
This article was designed to discuss the issues related to ensuring the methodological uniformity of investigations of the novel psychoactive substances based on the system of the newly established specialized laboratories. The authors propose the methodological approaches to the implementation of comprehensive chemical and pharmacological research including chemical, biological, and sociological studies. The main specific features of these approaches are the use of laboratory animals and the automation of in vivo experiments. Also, we discuss the use of the concrete results of the computational experiments designed to elucidate the parameters responsible for the chemical similarity of psychoactive substances. The mechanisms of their action are considered. The special emphasis is placed on the necessity of close cooperation between scientific and expert communities with a view to accumulation of the data on the newly developed and potentially harmful psychoactive substances as a basis for the efficacious prevention of their illegal trafficking.
31 October 2022 in "Medical & Pharmaceutical Journal "Pulse"
The biological activity of extracts from Cirsium heterophyllum leaves is of interest. Traditional medicine and preliminary studies indicate that this raw material may have the potential for anti-inflammatory activity. The aim of this study was to evaluate the anti-inflammatory activity of an aqueous extract of Cirsium heterophyllum leaves. We studied the anti-inflammatory activity of aqueous extracts of Cirsium heterophyllum leaves harvested in Vasilyevka village, Perm district, Perm territory (kray), Russia. The extracts were standardized for the content of flavonoids in terms of cynaroside. To study the anti-inflammatory activity, we used carrageenan-induced paw edema model in outbred ICR (CD-1) mice and outbred Wistar rats. Diclofenac was used as a reference drug. The test substances were dissolved in a 2% starch solution and injected intraperitoneally to the animals. The paw volume was measured hydrometrically and photometrically. The study has shown that the aqueous extracts of Cirsium heterophyllum have a mild effect compared to diclofenac. In mice, the percentage of inhibition of edema at the 4th hour was 19% (p-value = 0.0310) and 20% (p-value = 0.0130) for photometry and hydrometry, respectively. In rats, the percentage of edema inhibition was 47% (p-value = 0.0300) at the 1st hour and 28.7% (p-value = 0.0170) at 3 hours for hydrometry; photometry did not confirm these results. The results suggest that the aqueous extract of Cirsium heterophyllum has a mild activity in comparison with diclofenac, which may be due to the mutual action of the extract substances when applied intraperitoneally, as well as the presence of polysaccharides in the aqueous extract. Further research is required to determine whether the anti-inflammatory activity of its aqueous extract might be better combined with wound healing effects when applied topically.
26 December 2023 in Drug development & registration
Introduction. Studying the psychoactive properties of substances is an important task for regulating their circulation. It is relevant both for new psychoactive substances (NPS) that are in illegal circulation and for drugs entering the pharmaceutical market. In this regard, the issue of creating specialized analytical centers for conducting complex chemical and pharmacological studies does not lose its relevance.Aim. The purpose of the work is to develop scientific, methodological and organizational approaches to conducting comprehensive studies of psychoactive substances based on generalizing the work experience of employees of the Regional Test Center (RTC) "Pharmatest" of the Perm State Pharmaceutical Academy, both in the study of new psychoactive substances, withdrawn from illegal circulation, as part of expert studies on behalf of law enforcement agencies, and as part of preclinical studies of new medicines.Materials and methods. When performing the work, experimental and statistical data for 2010–2023 were used. on the study of NPS on the basis of the RTC "Pharmatest" in order to determine the possibility of classifying them as analogues of drugs of abuse, materials on the study of new drugs for the possible presence of psychoactive properties and affinity for certain receptors, approaches to conducting individual stages of expert examinations were assessed and described research, chemical and biological methods used.Results and discussion. The stages of research into new psychoactive substances and the methodology for conducting tests on each of them, as well as the necessary equipment and approaches to interpreting the results obtained, have been determined and scientifically substantiated. The need to create analytical centers to conduct comprehensive expert studies of narcotic substances and preclinical studies of drugs is shown.Conclusion. The developed methodological principles and organizational measures for conducting a comprehensive study of new psychoactive substances are important both for suppressing illegal drug trafficking in order to implement the State anti-drug policy, and for the development of domestic pharmaceuticals, designed to ensure the use of effective and safe medicines in medical practice.