Pub Date : 2021-10-25DOI: 10.19163/2307-9266-2021-9-5-400-409
V. V. Prokopenko, T. I. Kabakova, M. Chernikov, A. Goryachev, S. Mikhailova, O. Knysh
the aim. Focused on optimizing the assortment portfolio of pharmacy organizations and improving the process of drug supply to end-consumers, the aim of the study was to analyze the regional pharmaceutical market for antihistamines.Materials and methods. In the study, the following methods were used: a content analysis of regulatory documents; a documentary observation method of the volume of antihistamines sales; a sociological survey method. The objects of the study were accounting registers in 32 pharmacy organizations for 2020, as well as the sociological survey results of 174 respondents – consumers of antihistamines.Results. The classification analysis of 38 international non-proprietary trade names of antihistamines, represented by 187 names of drugs, revealed the prevalence of the first-generation drugs (63%). On the Russian pharmaceutical market, there were also 55% of foreign production drugs. At the regional level, there are 66 types of drugs in circulation, 50% of which are second-generation ones. The cost analysis showed rather a wide rage of the pricing proposal and the economic availability of antihistamines for patients. The sociological survey revealed the fact that 46% of the consumers were ready to pay for the necessary drugs in the price range “over 100 and up to 500 rubles” (over $ 1.38 and up to $ 6.88) for one conventional package. A medical-demographic profile of the antihistamines consumer at the regional level has been made up, and guidelines for pharmaceutical specialists on managing the assortment portfolio of pharmaceutical organizations have been developed.Conclusion. As a result of the study, the following facts have been established: the seasonal peaks in the antihistamines consumption; a gradual renewal of the pharmacies assortment portfolio due to the increased consumption of the second and third generation antihistamines. The medical and demographic profile of the consumer should be taken into consideration when planning a drug provision for the patients with allergic pathologies, and it is connected with the growth in pharmacies profits due to the sale of drugs in the range from 100 to 500 rubles (from $ 1.38 to $ 6.88). The methodical recommendations have been brought to the attention of the management of regional pharmacy organizations.
{"title":"ANTIHISTAMINES: RESEARCH AND ANALYSIS OF THE REGIONAL RETAIL MARKET","authors":"V. V. Prokopenko, T. I. Kabakova, M. Chernikov, A. Goryachev, S. Mikhailova, O. Knysh","doi":"10.19163/2307-9266-2021-9-5-400-409","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-5-400-409","url":null,"abstract":"the aim. Focused on optimizing the assortment portfolio of pharmacy organizations and improving the process of drug supply to end-consumers, the aim of the study was to analyze the regional pharmaceutical market for antihistamines.Materials and methods. In the study, the following methods were used: a content analysis of regulatory documents; a documentary observation method of the volume of antihistamines sales; a sociological survey method. The objects of the study were accounting registers in 32 pharmacy organizations for 2020, as well as the sociological survey results of 174 respondents – consumers of antihistamines.Results. The classification analysis of 38 international non-proprietary trade names of antihistamines, represented by 187 names of drugs, revealed the prevalence of the first-generation drugs (63%). On the Russian pharmaceutical market, there were also 55% of foreign production drugs. At the regional level, there are 66 types of drugs in circulation, 50% of which are second-generation ones. The cost analysis showed rather a wide rage of the pricing proposal and the economic availability of antihistamines for patients. The sociological survey revealed the fact that 46% of the consumers were ready to pay for the necessary drugs in the price range “over 100 and up to 500 rubles” (over $ 1.38 and up to $ 6.88) for one conventional package. A medical-demographic profile of the antihistamines consumer at the regional level has been made up, and guidelines for pharmaceutical specialists on managing the assortment portfolio of pharmaceutical organizations have been developed.Conclusion. As a result of the study, the following facts have been established: the seasonal peaks in the antihistamines consumption; a gradual renewal of the pharmacies assortment portfolio due to the increased consumption of the second and third generation antihistamines. The medical and demographic profile of the consumer should be taken into consideration when planning a drug provision for the patients with allergic pathologies, and it is connected with the growth in pharmacies profits due to the sale of drugs in the range from 100 to 500 rubles (from $ 1.38 to $ 6.88). The methodical recommendations have been brought to the attention of the management of regional pharmacy organizations.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"105 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84883768","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-10-25DOI: 10.19163/2307-9266-2021-9-5-410-422
Z. Aladysheva, N. Pyatigorskaya, V. Belyaev, N. Nikolenko, E. I. Nesterkina, S. A. Loseva
The aim of the study is to investigate topical problems of the professional and personal development of qualified persons responsible for quality of medicinal products for human use.Materials and methods. In the period from April 6 to May 10, 2020, an online survey of leading employees in the field of quality assurance of Russian manufacturers was conducted. 176 people took part in the survey; the return of questionnaires was about 17.9%.Results. From the standpoint of D. Super’s theory of professional development, the largest number of respondents was at the maintenance stage, holding their achieved positions (53.2%). All respondents, regardless of age, were motivated for professional development. Most often qualified persons had chemical engineering (27.3%) and pharmaceutical education (22.2%). Most of them had a working experience in 1–2 divisions of the enterprise, and combined the functions of qualified persons with managerial positions (74.5% and 71.9%, respectively). The majority of the qualified persons (86.4%) indicated the sufficiency of the available knowledge and the lack of knowledge on certain issues. Knowledge and skills in the quality risk management, specific GMP issues and statistical methods (59.0%, 49.2 and 44.2%, respectively); communication and interpersonal skills and, in particular, stress management, emotion management and the art of negotiation (49.4%, 41.3% and 40.9%, respectively), were most popular. About 36% of respondents notified the need for the digital economy competencies, while only 5.1% notified the presence of an electronic batch production record at the enterprise. Finally, only half of the respondents (50.5%) had a formal training plan for qualified persons.Conclusion. This pilot study revealed the need for the revision of the Exemplary Additional Professional Training Program for Qualified Persons and the professional standard, the urgent need for the regulatory body to develop a scheme and principles for the continuous professional development of qualified persons, and showed the direction of further research in this area.
{"title":"ACTUAL PROBLEMS OF PROFESSIONAL AND PERSONAL DEVELOPMENT QUALIFIED PERSONS RESPONSIBLE FOR QUALITY OF MEDICINAL PRODUCTS FOR HUMAN USE","authors":"Z. Aladysheva, N. Pyatigorskaya, V. Belyaev, N. Nikolenko, E. I. Nesterkina, S. A. Loseva","doi":"10.19163/2307-9266-2021-9-5-410-422","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-5-410-422","url":null,"abstract":"The aim of the study is to investigate topical problems of the professional and personal development of qualified persons responsible for quality of medicinal products for human use.Materials and methods. In the period from April 6 to May 10, 2020, an online survey of leading employees in the field of quality assurance of Russian manufacturers was conducted. 176 people took part in the survey; the return of questionnaires was about 17.9%.Results. From the standpoint of D. Super’s theory of professional development, the largest number of respondents was at the maintenance stage, holding their achieved positions (53.2%). All respondents, regardless of age, were motivated for professional development. Most often qualified persons had chemical engineering (27.3%) and pharmaceutical education (22.2%). Most of them had a working experience in 1–2 divisions of the enterprise, and combined the functions of qualified persons with managerial positions (74.5% and 71.9%, respectively). The majority of the qualified persons (86.4%) indicated the sufficiency of the available knowledge and the lack of knowledge on certain issues. Knowledge and skills in the quality risk management, specific GMP issues and statistical methods (59.0%, 49.2 and 44.2%, respectively); communication and interpersonal skills and, in particular, stress management, emotion management and the art of negotiation (49.4%, 41.3% and 40.9%, respectively), were most popular. About 36% of respondents notified the need for the digital economy competencies, while only 5.1% notified the presence of an electronic batch production record at the enterprise. Finally, only half of the respondents (50.5%) had a formal training plan for qualified persons.Conclusion. This pilot study revealed the need for the revision of the Exemplary Additional Professional Training Program for Qualified Persons and the professional standard, the urgent need for the regulatory body to develop a scheme and principles for the continuous professional development of qualified persons, and showed the direction of further research in this area.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88790961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-10-25DOI: 10.19163/2307-9266-2021-9-5-356-366
N. A. Ryabov, V. M. Ryzhov, V. Kurkin
Currently, the actual task of modern pharmacy is to study the chemical composition and pharmacological properties of plant objects. Within the framework of this concept, it seems interesting to study Quercus robur L. buds. One of the promising groups of biologically active compounds of Quercus robur L. buds are flavonoids. This group of substances has a wide range of a pharmacological activity, which is significant in the creation of new medicines based on medicinal plant raw materials.The aim of the article was to work out methods for quantitative determination of total flavonoids in Quercus robur l. buds.Materials and methods. The research materials were aqueous-alcoholic extracts from Quercus robur L. buds with 70% ethyl alcohol which were analyzed by differential UV spectrophotometry on spectrophotometer “SF 2000” (Russia).Results. The methods for quantitative determination of total flavonoids in Quercus robur L. buds by differential UV spectrophotometry, has been developed using a standard sample of cynaroside at the analytical wavelength of 400 nm. The optimum parameters for the extraction of total flavonoids from Quercus robur L. buds have been determined. They are: the optimum extractant is 70% ethyl alcohol; the “raw material-extractant” ratio is 1:50; the extraction time is 120 min, the degree of atomization is 2 mm.The content of total flavonoids for Quercus robur L. buds has been determined; it varies from 0.27%±0.01 to 0.44%±0.02. These results make possible to recommend the content of total flavonoids for this type of raw materials not less than 0.25% as a lower limit.Conclusion. The data obtained in the course of the experiment, makes it possible to conclude that a further study of Quercus robur L. buds is promising, and it also contributes to the implementation of medicinal plant raw materials “Quercus robur L. buds” in the State Pharmacopoeia (Russia).
{"title":"METHODS FOR QUANTITATIVE DETERMINATION OF TOTAL FLAVONOIDS IN QUERCUS ROBUR L. BUDS","authors":"N. A. Ryabov, V. M. Ryzhov, V. Kurkin","doi":"10.19163/2307-9266-2021-9-5-356-366","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-5-356-366","url":null,"abstract":"Currently, the actual task of modern pharmacy is to study the chemical composition and pharmacological properties of plant objects. Within the framework of this concept, it seems interesting to study Quercus robur L. buds. One of the promising groups of biologically active compounds of Quercus robur L. buds are flavonoids. This group of substances has a wide range of a pharmacological activity, which is significant in the creation of new medicines based on medicinal plant raw materials.The aim of the article was to work out methods for quantitative determination of total flavonoids in Quercus robur l. buds.Materials and methods. The research materials were aqueous-alcoholic extracts from Quercus robur L. buds with 70% ethyl alcohol which were analyzed by differential UV spectrophotometry on spectrophotometer “SF 2000” (Russia).Results. The methods for quantitative determination of total flavonoids in Quercus robur L. buds by differential UV spectrophotometry, has been developed using a standard sample of cynaroside at the analytical wavelength of 400 nm. The optimum parameters for the extraction of total flavonoids from Quercus robur L. buds have been determined. They are: the optimum extractant is 70% ethyl alcohol; the “raw material-extractant” ratio is 1:50; the extraction time is 120 min, the degree of atomization is 2 mm.The content of total flavonoids for Quercus robur L. buds has been determined; it varies from 0.27%±0.01 to 0.44%±0.02. These results make possible to recommend the content of total flavonoids for this type of raw materials not less than 0.25% as a lower limit.Conclusion. The data obtained in the course of the experiment, makes it possible to conclude that a further study of Quercus robur L. buds is promising, and it also contributes to the implementation of medicinal plant raw materials “Quercus robur L. buds” in the State Pharmacopoeia (Russia).","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87353150","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-10-25DOI: 10.19163/2307-9266-2021-9-5-387-399
I. Krysanov, E. Y. Ermakova, L. Vaskova, M. Tiapkina
Clinical trials conducted in various countries indicate that the use of epoetin alfa in patients with nephrogenic anemia in chronic kidney disease can increase the effectiveness of treatment, reduce the incidence of cardiovascular and infectious complications, and reduce mortality in patients with chronic kidney disease.The aim of the article was to conduct a comparative clinical and economic assessment of the treatment costs of nephrogenic anemia in adult dialysis patients with recombinant human erythropoietins: epoetin alfa, darbepoetin and long-acting methoxy polyethylene glycol – epoetin beta.Materials and methods. The study took into account direct medical costs of nephrogenic anemia pharmacotherapy on the basis of 1 year maintenance therapy according to the following scheme: epoetin alfa – 3 times per week, darbepoetin alfa – once per week, methoxy polyethylene glycol – epoetin beta – once per 2 or 4 weeks. A “costs minimization” analysis was performed for equivalent maintenance epoetins doses for intravenous and subcutaneous administrations. Epoetin alpha equivalents were calculated for an average patient weighing 75 kg by converting a weekly dose of short-acting epoetin (7500 IU) into equivalent doses using dose conversion factors.Results. In the hypothetical cohort of patients under study, epoetin alfa, darbepoetin alfa, and methoxy polyethylene glycol – epoetin beta not differ in effectiveness in achieving target Hb values and in safety. With the equal effectiveness of the investigated drugs, in the studied patients, intravenous epoetin alfa can be less expensive drug therapy relative to the equivalent doses obtained by the calculation: darbepoetin by 14–24% and methoxy polyethylene glycol – epoetin beta by 4–30%. The change-over of patients to the subcutaneous administration makes it possible to decline a weekly dose of epoetin alfa by 20–30% by reducing the frequency of taking the drug to twice a week, and to reduce the cost of drug therapy by a third.Conclusion. Intravenous and subcutaneous administrations of epoetin alfa 2500 IU may be a more economical drug therapy in comparison with the equivalent doses of darbepoetin and methoxy polyethylene glycol – epoetin beta.
{"title":"COST-MINIMIZATION ANALYSIS OF USING SHORT AND LONG-ACTING ERYTHROPOESIS-STIMULATING AGENTS FOR CORRECTION OF NEPHROGENIC ANEMIA AGAINST THE BACKGROUND OF SUBSTITUTION THERAPY","authors":"I. Krysanov, E. Y. Ermakova, L. Vaskova, M. Tiapkina","doi":"10.19163/2307-9266-2021-9-5-387-399","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-5-387-399","url":null,"abstract":"Clinical trials conducted in various countries indicate that the use of epoetin alfa in patients with nephrogenic anemia in chronic kidney disease can increase the effectiveness of treatment, reduce the incidence of cardiovascular and infectious complications, and reduce mortality in patients with chronic kidney disease.The aim of the article was to conduct a comparative clinical and economic assessment of the treatment costs of nephrogenic anemia in adult dialysis patients with recombinant human erythropoietins: epoetin alfa, darbepoetin and long-acting methoxy polyethylene glycol – epoetin beta.Materials and methods. The study took into account direct medical costs of nephrogenic anemia pharmacotherapy on the basis of 1 year maintenance therapy according to the following scheme: epoetin alfa – 3 times per week, darbepoetin alfa – once per week, methoxy polyethylene glycol – epoetin beta – once per 2 or 4 weeks. A “costs minimization” analysis was performed for equivalent maintenance epoetins doses for intravenous and subcutaneous administrations. Epoetin alpha equivalents were calculated for an average patient weighing 75 kg by converting a weekly dose of short-acting epoetin (7500 IU) into equivalent doses using dose conversion factors.Results. In the hypothetical cohort of patients under study, epoetin alfa, darbepoetin alfa, and methoxy polyethylene glycol – epoetin beta not differ in effectiveness in achieving target Hb values and in safety. With the equal effectiveness of the investigated drugs, in the studied patients, intravenous epoetin alfa can be less expensive drug therapy relative to the equivalent doses obtained by the calculation: darbepoetin by 14–24% and methoxy polyethylene glycol – epoetin beta by 4–30%. The change-over of patients to the subcutaneous administration makes it possible to decline a weekly dose of epoetin alfa by 20–30% by reducing the frequency of taking the drug to twice a week, and to reduce the cost of drug therapy by a third.Conclusion. Intravenous and subcutaneous administrations of epoetin alfa 2500 IU may be a more economical drug therapy in comparison with the equivalent doses of darbepoetin and methoxy polyethylene glycol – epoetin beta.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"30 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85582974","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-10-25DOI: 10.19163/2307-9266-2021-9-5-377-386
A. Safronenko, E. Gantsgorn, E. A. Sanina, M. A. Khachumova, S. Panenko, I. Kuznetsov, A. A. Kivva, V. Polyakova
The aim of this retrospective study was to analyze the pharmacotherapy regimens of the decompensated form of type 2 diabetes mellitus (DM2) and to evaluate its effectiveness, its compliance with clinical recommendations.Materials and methods: A retrospective analysis of 54 medical cards of patients with decompensated DM2 was conducted. The 1st group (n=24; 44%) included the patients who had a decrease in glycated hemoglobin (HbA1c) by 50% or more in 3 months after hypoglycemic therapy; and the 2nd group (n=30; 56%) – the patients whose HbA1c level decreased by less than 50%.Results. A HbA1c level was 10.4% in the 1st group and 13.2% in the 2nd group (р<0.001). However, the target levels of venous blood plasma glucose and HbA1c were not achieved in any of the patient groups. The total number of the drugs prescribed to the patients ranged from 4 (in 25% (n=6) and 10% (n=3) cases in the 1st and the 2nd groups, respectively) to 8 (in 12.5% (n=3) and 20% (n=6) cases in the 1st and the 2nd, groups, respectively). However, in a number of cases some violations of clinical recommendations were recorded: the prescription to the obese patients of insulin drugs, the administration of sulfonylureas derivatives to patients with a history of cardiovascular diseases of the atherosclerotic origin, but modern hypoglycemic drugs with proven benefits in reducing cardiovascular risks were rarely prescribed.Conclusion. The tactics of pharmacotherapy in the patients with a decompensated form of DM2 does not fully comply with the approved clinical guidelines, which requires the effectiveness of treatment optimization of this medically and socially significant pathology.
{"title":"TYPE 2 DIABETES MELLITUS’S DECOMPENSATED FORM: ON THE PROBLEM OF EFFECTIVE PHARMACOTHERAPY IN REAL CLINICAL PRACTICE","authors":"A. Safronenko, E. Gantsgorn, E. A. Sanina, M. A. Khachumova, S. Panenko, I. Kuznetsov, A. A. Kivva, V. Polyakova","doi":"10.19163/2307-9266-2021-9-5-377-386","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-5-377-386","url":null,"abstract":"The aim of this retrospective study was to analyze the pharmacotherapy regimens of the decompensated form of type 2 diabetes mellitus (DM2) and to evaluate its effectiveness, its compliance with clinical recommendations.Materials and methods: A retrospective analysis of 54 medical cards of patients with decompensated DM2 was conducted. The 1st group (n=24; 44%) included the patients who had a decrease in glycated hemoglobin (HbA1c) by 50% or more in 3 months after hypoglycemic therapy; and the 2nd group (n=30; 56%) – the patients whose HbA1c level decreased by less than 50%.Results. A HbA1c level was 10.4% in the 1st group and 13.2% in the 2nd group (р<0.001). However, the target levels of venous blood plasma glucose and HbA1c were not achieved in any of the patient groups. The total number of the drugs prescribed to the patients ranged from 4 (in 25% (n=6) and 10% (n=3) cases in the 1st and the 2nd groups, respectively) to 8 (in 12.5% (n=3) and 20% (n=6) cases in the 1st and the 2nd, groups, respectively). However, in a number of cases some violations of clinical recommendations were recorded: the prescription to the obese patients of insulin drugs, the administration of sulfonylureas derivatives to patients with a history of cardiovascular diseases of the atherosclerotic origin, but modern hypoglycemic drugs with proven benefits in reducing cardiovascular risks were rarely prescribed.Conclusion. The tactics of pharmacotherapy in the patients with a decompensated form of DM2 does not fully comply with the approved clinical guidelines, which requires the effectiveness of treatment optimization of this medically and socially significant pathology.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87376817","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-10-25DOI: 10.19163/2307-9266-2021-9-5-367-376
S. S. Shatokhin, V. Tuskaev, S. Gagieva, D. Pozdnyakov, E. Oganesyan
The aim is based on the results of the in silico prediction, to obtain and characterize a number of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one derivatives, and also to study their antioxidant activity.Materials and methods. The synthesis of the target compounds was carried out by condensation of substituted 3-formylchromones and 3-acetylcoumarins under the acid catalysis conditions. 1H NMR spectra were recorded on the instruments of Bruker Avance-400 (400 MHz) and Bruker Avance-300 (300 MHz) in the solutions of CDCl3 or DMSO-d6. Mass spectra (ESI) were obtained on a Finnigan LCQ Advantage mass spectrometer (USA). The melting points of the compounds were determined on a PTP (M) instrument. Quantum-chemical calculations were carried out on the basis of a density functional theory using the Gaussian 09 program using the B3LYP/6-311G (d, p) method, as well as using the Way2Drug (PASS Online) online service. The antiradical activity of the compounds was studied by the DPPH test, and the chelating properties were assessed by the o-phenanthroline method.Results. 15 derivatives of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one have been obtained and characterized. The calculations based on the density functional theory showed that the highest occupied molecular orbital exhibiting electron-donating properties is localized on the propenone fragment, which confirms the likelihood of the manifestation of antiradical properties. According to the prediction of the probable spectrum of the biological activity, the obtained compounds are more likely to exhibit their direct antioxidant activity. According to the results of the in vitro study of the antioxidant activity, it was found out that compounds 1-15 are the most active in relation to the DPPH radical, which confirms the obtained prognostic data.Conclusion. Thus, based on the in silico prediction data, 15 derivatives of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one have been obtained and characterized, for which the method antioxidant activity has been studied in vitro. It was found out that compounds 1-15 exhibit the antiradical activity to a large extent.
{"title":"SYNTHESIS AND ANTIOXIDANT ACTIVITY OF (E)-3-(3-(4-OXO-4H-CHROMEN-3-YL)ACRYLOYL) 2H-CHROMEN-2-ONE DERIVATIVES","authors":"S. S. Shatokhin, V. Tuskaev, S. Gagieva, D. Pozdnyakov, E. Oganesyan","doi":"10.19163/2307-9266-2021-9-5-367-376","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-5-367-376","url":null,"abstract":"The aim is based on the results of the in silico prediction, to obtain and characterize a number of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one derivatives, and also to study their antioxidant activity.Materials and methods. The synthesis of the target compounds was carried out by condensation of substituted 3-formylchromones and 3-acetylcoumarins under the acid catalysis conditions. 1H NMR spectra were recorded on the instruments of Bruker Avance-400 (400 MHz) and Bruker Avance-300 (300 MHz) in the solutions of CDCl3 or DMSO-d6. Mass spectra (ESI) were obtained on a Finnigan LCQ Advantage mass spectrometer (USA). The melting points of the compounds were determined on a PTP (M) instrument. Quantum-chemical calculations were carried out on the basis of a density functional theory using the Gaussian 09 program using the B3LYP/6-311G (d, p) method, as well as using the Way2Drug (PASS Online) online service. The antiradical activity of the compounds was studied by the DPPH test, and the chelating properties were assessed by the o-phenanthroline method.Results. 15 derivatives of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one have been obtained and characterized. The calculations based on the density functional theory showed that the highest occupied molecular orbital exhibiting electron-donating properties is localized on the propenone fragment, which confirms the likelihood of the manifestation of antiradical properties. According to the prediction of the probable spectrum of the biological activity, the obtained compounds are more likely to exhibit their direct antioxidant activity. According to the results of the in vitro study of the antioxidant activity, it was found out that compounds 1-15 are the most active in relation to the DPPH radical, which confirms the obtained prognostic data.Conclusion. Thus, based on the in silico prediction data, 15 derivatives of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one have been obtained and characterized, for which the method antioxidant activity has been studied in vitro. It was found out that compounds 1-15 exhibit the antiradical activity to a large extent.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87772783","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-09-08DOI: 10.19163/2307-9266-2021-9-4-294-305
М. В. Korokin, M. Kubekina, A. Deykin, O. V. Antsiferov, V. Pokrovskii, L. Korokina, N. Kartashkina, V. Soldatova, E. Kuzubova, A. Radchenko, M. Pokrovskii
The aim of the research was to study antiatherosclerotic and endothelial kinds of a protective activity of peptides mimicking an erythropoietin a-helix B tertiary structure with laboratory codes EP-11-1 (UEHLERALNSS), EP-11-2. (UEQLERALNCS), EP-11-3 (UEQLERALNTS).Materials and methods. The study was conducted on 96 C57Bl/6J male double transgenic Polgmut/mut/Cdh5-CRE mice. Atherosclerosis was induced by a balloon injury accompanied by Western diet. Then, for 27 days, the drugs under study were administered once per 3 days at the dose of 20 μg/kg. On the 28th day, the animals were euthanized and the area of atherosclerotic plaques was collected for an assessment. The expression of genes associated with the processes of inflammation, apoptosis, and angiogenesis was determined in the tissues of the aorta. In addition, the endothelial protective effect of peptides in isolated segments of the thoracic aorta of wild and transgenic ransgenic Polgmut/mut mice was studied.Results. The assessment of the plaque size in the animals with the Polgmut/mut/Cdh5-CRE genotype against the background of the peptides under study did not reveal statistically significant differences in comparison to control. However, a quantitative PCR showed a statistically significant decreased expression of pro-apoptotic factors p-53 and Bax, and also increase the expression of anti-apoptotic factor Bcl-2 against the background of the peptides EP-11-1 and EP-11-2 administration. The administration of EP-11-1 and the original peptide pHBSP resulted in a statistically significant decrease in the Bax/Bcl-2 ratio. Compounds EP-11-1, EP-11-2, and EP-11-3 were more effective than the original peptide pHBSP, in reducing the increased expression of genes for inflammatory markers iNos, intercellular adhesion molecules Icam-1, Vcam-1 and E-selectin. The use of EP-11-1 led to a more efficient, in comparison with pHBSP, restoration of endothelial-dependent vasodilation of the aortic segments in mice with endothelial-specific overexpression of the mutant Polg gene.Conclusion. The study carried out on a murine model of the endothelial-specific expression of mutant gamma polymerase has shown that derivatives of the pHBSP peptide with laboratory codes EP-11-1, EP-11-2, EP-11-3, obtained by BLAST-searching for groups of pHBSP related peptides, have atheroprotective and endothelial protective kinds of a protective activity, which is more pronounced in comparison with the original peptide pHBSP.
{"title":"STUDY OF THE PHARMACOLOGICAL ACTIVITY OF NOVEL EPOR/CD131 HETERORECEPTOR AGONISTS IN MICE WITH ENDOTHELIAL-SPECIFIC EXPRESSION OF MUTANT POLG GENE","authors":"М. В. Korokin, M. Kubekina, A. Deykin, O. V. Antsiferov, V. Pokrovskii, L. Korokina, N. Kartashkina, V. Soldatova, E. Kuzubova, A. Radchenko, M. Pokrovskii","doi":"10.19163/2307-9266-2021-9-4-294-305","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-4-294-305","url":null,"abstract":"The aim of the research was to study antiatherosclerotic and endothelial kinds of a protective activity of peptides mimicking an erythropoietin a-helix B tertiary structure with laboratory codes EP-11-1 (UEHLERALNSS), EP-11-2. (UEQLERALNCS), EP-11-3 (UEQLERALNTS).Materials and methods. The study was conducted on 96 C57Bl/6J male double transgenic Polgmut/mut/Cdh5-CRE mice. Atherosclerosis was induced by a balloon injury accompanied by Western diet. Then, for 27 days, the drugs under study were administered once per 3 days at the dose of 20 μg/kg. On the 28th day, the animals were euthanized and the area of atherosclerotic plaques was collected for an assessment. The expression of genes associated with the processes of inflammation, apoptosis, and angiogenesis was determined in the tissues of the aorta. In addition, the endothelial protective effect of peptides in isolated segments of the thoracic aorta of wild and transgenic ransgenic Polgmut/mut mice was studied.Results. The assessment of the plaque size in the animals with the Polgmut/mut/Cdh5-CRE genotype against the background of the peptides under study did not reveal statistically significant differences in comparison to control. However, a quantitative PCR showed a statistically significant decreased expression of pro-apoptotic factors p-53 and Bax, and also increase the expression of anti-apoptotic factor Bcl-2 against the background of the peptides EP-11-1 and EP-11-2 administration. The administration of EP-11-1 and the original peptide pHBSP resulted in a statistically significant decrease in the Bax/Bcl-2 ratio. Compounds EP-11-1, EP-11-2, and EP-11-3 were more effective than the original peptide pHBSP, in reducing the increased expression of genes for inflammatory markers iNos, intercellular adhesion molecules Icam-1, Vcam-1 and E-selectin. The use of EP-11-1 led to a more efficient, in comparison with pHBSP, restoration of endothelial-dependent vasodilation of the aortic segments in mice with endothelial-specific overexpression of the mutant Polg gene.Conclusion. The study carried out on a murine model of the endothelial-specific expression of mutant gamma polymerase has shown that derivatives of the pHBSP peptide with laboratory codes EP-11-1, EP-11-2, EP-11-3, obtained by BLAST-searching for groups of pHBSP related peptides, have atheroprotective and endothelial protective kinds of a protective activity, which is more pronounced in comparison with the original peptide pHBSP.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89848881","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-09-08DOI: 10.19163/2307-9266-2021-9-4-306-317
R. Litvinov, A. Gontareva, L. E. Usmiyanova, D. Klimenko
The aim of the research is to investigate the influence of the factor of the glycation behavior of bovine serum albumin (BSA) by glucose, and the factor of d-metal cations (nickel (II), cobalt (II), iron (II), iron (III), copper (II) or zinc (II)) presence, on the process of aggregation and the amyloid transformation of BSA and, therefore, to establish the effect of these cations on the rate of the formation of advanced glycation end products (AGEs), and the intensity of fluorescence of the amino acids tyrosine and tryptophan.Materials and methods. Reagents in the glycation are: glucose (at the final concentration of 0.36 M), BSA (at the final concentration of 1 mg/ml), deionized water, one of the d-metal cations, i. e. nickel (II), cobalt (II), iron (II), iron (III), copper (II) or zinc (II) (in the form of chloride, sulfate or nitrate salts, at the final concentration of 40 μM). The conditions for the glycation reaction are the incubation for 24 hours at the temperature of 60°C. The influence of two factors (the factor of the glycation reaction and the factor of a d-metal ion presence in the reaction medium) on the concentration of glycation end products (AGEs) formed during the glycation reaction, on the fluorescence intensity of the amino acids tryptophan and tyrosine, on the aggregation of BSA, and on the ability of BSA to the amyloid transformation under the described conditions, have been studied.Results. It was found out that the studied factors have a statistically significant effect on the considered parameters. The highest activity was found for the copper ion (II), which intensifies the formation of the AGEs in the samples where glycation occurs, reduces the fluorescence intensity of the amino acids’ tryptophan and tyrosine (independently and increasing the effect against the background of glycation). Besides, it independently causes the aggregation of BSA hereby intensifying the effect against the background of glycation, it independently causes the amyloid transformation of BSA enhancing the effect against the background of glycation. The above-listed effects were the least pronounced in the reaction media with the addition of nickel (II) or cobalt (II). These cations reduce the rate of the AGEs formation, do not cause the formation of protein aggregates. In the presence of glucose, nickel (II) weakly suppresses the fluorescence intensity of tryptophan and tyrosine, and slightly enhances the amyloid transformation of BSA. Cobalt (II) slightly inhibits the amyloid transformation of BSA. In terms of the severity and nature of the effects, the iron (II), iron (III) and zinc (II) cations occupy an intermediate position between copper (II), on the one hand, and nickel (II) and cobalt (II), on the other hand, combining the influence on the AGEs formation, the intensity of fluorescence of tryptophan and tyrosine, the aggregation and amyloid transformation of BSA. In the absence of glucose, the ability of zinc (II) to induce the formation o
{"title":"INFLUENCE OF CERTAIN D-METALS ON FORMATION OF ADVANCED GLYCATION END PRODUCTS, AGGREGATION AND AMYLOID TRANSFORMATION OF ALBUMIN IN GLYCATION REACTION","authors":"R. Litvinov, A. Gontareva, L. E. Usmiyanova, D. Klimenko","doi":"10.19163/2307-9266-2021-9-4-306-317","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-4-306-317","url":null,"abstract":"The aim of the research is to investigate the influence of the factor of the glycation behavior of bovine serum albumin (BSA) by glucose, and the factor of d-metal cations (nickel (II), cobalt (II), iron (II), iron (III), copper (II) or zinc (II)) presence, on the process of aggregation and the amyloid transformation of BSA and, therefore, to establish the effect of these cations on the rate of the formation of advanced glycation end products (AGEs), and the intensity of fluorescence of the amino acids tyrosine and tryptophan.Materials and methods. Reagents in the glycation are: glucose (at the final concentration of 0.36 M), BSA (at the final concentration of 1 mg/ml), deionized water, one of the d-metal cations, i. e. nickel (II), cobalt (II), iron (II), iron (III), copper (II) or zinc (II) (in the form of chloride, sulfate or nitrate salts, at the final concentration of 40 μM). The conditions for the glycation reaction are the incubation for 24 hours at the temperature of 60°C. The influence of two factors (the factor of the glycation reaction and the factor of a d-metal ion presence in the reaction medium) on the concentration of glycation end products (AGEs) formed during the glycation reaction, on the fluorescence intensity of the amino acids tryptophan and tyrosine, on the aggregation of BSA, and on the ability of BSA to the amyloid transformation under the described conditions, have been studied.Results. It was found out that the studied factors have a statistically significant effect on the considered parameters. The highest activity was found for the copper ion (II), which intensifies the formation of the AGEs in the samples where glycation occurs, reduces the fluorescence intensity of the amino acids’ tryptophan and tyrosine (independently and increasing the effect against the background of glycation). Besides, it independently causes the aggregation of BSA hereby intensifying the effect against the background of glycation, it independently causes the amyloid transformation of BSA enhancing the effect against the background of glycation. The above-listed effects were the least pronounced in the reaction media with the addition of nickel (II) or cobalt (II). These cations reduce the rate of the AGEs formation, do not cause the formation of protein aggregates. In the presence of glucose, nickel (II) weakly suppresses the fluorescence intensity of tryptophan and tyrosine, and slightly enhances the amyloid transformation of BSA. Cobalt (II) slightly inhibits the amyloid transformation of BSA. In terms of the severity and nature of the effects, the iron (II), iron (III) and zinc (II) cations occupy an intermediate position between copper (II), on the one hand, and nickel (II) and cobalt (II), on the other hand, combining the influence on the AGEs formation, the intensity of fluorescence of tryptophan and tyrosine, the aggregation and amyloid transformation of BSA. In the absence of glucose, the ability of zinc (II) to induce the formation o","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"301 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79724353","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-09-08DOI: 10.19163/2307-9266-2021-9-4-266-277
M. V. Larskiy, A. E. Pozdnyakova, Z. D. Khadzhieva, D. I. Pozdnyakov
Intranasal administration of H1-histamine receptor blockers may be a promising approach to the treatment of allergic rhinitis. Earlier, an original composition of a nasal spray containing fexofenadine hydrochloride and ammonium glycyrrhizinate and demonstrating a high level of therapeutic efficacy, was developed.The aim of the study was to develop and validate a method of the quantitative determination of active pharmaceutical ingredients fexofenadine hydrochloride and ammonium glycyrrhizinate in a spray for intranasal administration.Materials and methods. During the development and validation of the method of the fexofenadine hydrochloride and ammonium glycyrrhizinate quantitative determination in a nasal spray, the method of high performance liquid chromatography was used: a Dionex Ultimate 3000 UV chromatograph with a Luna C18 column (2) containing octadecylsilicagel with a 5 μm grain size as a sorbent. The analysis and validation procedures were performed in accordance with the requirements of the State Pharmacopoeia of the Russian Federation, the XIVth edition.Results. The study showed that for the simultaneous quantitative determination of fexofenadine hydrochloride and ammonium glycyrrhizinate, the optimal elution regime is a gradient mode with a mobile phase containing 50 mmol/L potassium dihydrogen phosphate solution with methanol (45:55), which ensured the separation of the components in the 20 minutes interval. The validation procedures showed that the developed methodology correspond to all the criteria of validity in terms of the following indicators: correctness, precision, specificity and linearity in the analytical area.Conclusion. The obtained results indicate the possibility of using the method of high-performance liquid chromatography in a gradient elution mode with a mobile phase of the composition of a 50 mmol/L solution of potassium dihydrogen phosphate with methanol (45:55) for the simultaneous quantitative determination of active pharmaceutical ingredients – fexofenadine hydrochloride and ammonium glycyrrhizinate as parts of a promising nasal spray for the allergic rhinitis treatment.
{"title":"DEVELOPMENT AND VALIDATION OF METHODS FOR QUANTITATIVE DETERMINATION OF ACTIVE PHARMACEUTICAL SUBSTANCES IN NASAL SPRAY","authors":"M. V. Larskiy, A. E. Pozdnyakova, Z. D. Khadzhieva, D. I. Pozdnyakov","doi":"10.19163/2307-9266-2021-9-4-266-277","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-4-266-277","url":null,"abstract":"Intranasal administration of H1-histamine receptor blockers may be a promising approach to the treatment of allergic rhinitis. Earlier, an original composition of a nasal spray containing fexofenadine hydrochloride and ammonium glycyrrhizinate and demonstrating a high level of therapeutic efficacy, was developed.The aim of the study was to develop and validate a method of the quantitative determination of active pharmaceutical ingredients fexofenadine hydrochloride and ammonium glycyrrhizinate in a spray for intranasal administration.Materials and methods. During the development and validation of the method of the fexofenadine hydrochloride and ammonium glycyrrhizinate quantitative determination in a nasal spray, the method of high performance liquid chromatography was used: a Dionex Ultimate 3000 UV chromatograph with a Luna C18 column (2) containing octadecylsilicagel with a 5 μm grain size as a sorbent. The analysis and validation procedures were performed in accordance with the requirements of the State Pharmacopoeia of the Russian Federation, the XIVth edition.Results. The study showed that for the simultaneous quantitative determination of fexofenadine hydrochloride and ammonium glycyrrhizinate, the optimal elution regime is a gradient mode with a mobile phase containing 50 mmol/L potassium dihydrogen phosphate solution with methanol (45:55), which ensured the separation of the components in the 20 minutes interval. The validation procedures showed that the developed methodology correspond to all the criteria of validity in terms of the following indicators: correctness, precision, specificity and linearity in the analytical area.Conclusion. The obtained results indicate the possibility of using the method of high-performance liquid chromatography in a gradient elution mode with a mobile phase of the composition of a 50 mmol/L solution of potassium dihydrogen phosphate with methanol (45:55) for the simultaneous quantitative determination of active pharmaceutical ingredients – fexofenadine hydrochloride and ammonium glycyrrhizinate as parts of a promising nasal spray for the allergic rhinitis treatment.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80406930","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-09-08DOI: 10.19163/2307-9266-2021-9-4-252-265
I. P. Kolpaksidi, M. Dmitrieva, I. V. Yarosh, I. Krasnyuk
The aim of the work is to generalize the literature data on indolocarbazole derivatives with an antitumor activity.Materials and methods. The objects of the study were the preparations based on indolocarbazole derivatives with the antitumor activity. To search for materials on the problem under study, the following search and information as well as library databases were used: ebibrary, PubMed, CyberLeninka, ResearchGate, the State Register of Medicines, clinical trials registries clinline.ru and clinicaltrials.gov. The search for the following words / phrases was performed: indolocarbazoles, indolocarbazole derivatives, staurosporine, rebeccamycin, staurosporine derivatives. The search was conducted from January 11 until March 1, 2021. The compounds with a biological activity which were undergoing or had undergone preclinical and clinical trials, were taken into account. All the materials from 1977 to January 1, 2021, were taken into account.Results. The materials obtained indicate that indolocarbazole derivatives are promising compounds for the creation of anticancer medicinal preparations due to their properties and peculiarities of the action mechanism. These drugs have a selective action due to the targeted interaction with specific molecular targets: kinases (especially protein kinase C and its isozymes), DNA and DNA topoisomerase. To date, many compounds from the class of indolocarbazoles have been synthesized and investigated. They have shown a high antitumor activity in the treatment of systemic and solid tumors. However, despite this, only one MP based on a staurosporine derivative, registered by the TN of Rydapt® (in the USA and EU countries) and Miticaid® (in the Russian Federation), is approved for use in the clinical practice.Conclusion. Thus, the basic data from scientific publications on promising anticancer medicinal preparations based on compounds from the class of indolocarbazoles, have been summarized. The information is provided, in particular, on their molecular structure, the origin, classification, the main representatives of the class, which are at various stages of the research and are approved for use in the clinic.
{"title":"ANTITUMOR DRUGS BASED ON INDOLOCARBAZOL DERIVATIVES","authors":"I. P. Kolpaksidi, M. Dmitrieva, I. V. Yarosh, I. Krasnyuk","doi":"10.19163/2307-9266-2021-9-4-252-265","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-4-252-265","url":null,"abstract":"The aim of the work is to generalize the literature data on indolocarbazole derivatives with an antitumor activity.Materials and methods. The objects of the study were the preparations based on indolocarbazole derivatives with the antitumor activity. To search for materials on the problem under study, the following search and information as well as library databases were used: ebibrary, PubMed, CyberLeninka, ResearchGate, the State Register of Medicines, clinical trials registries clinline.ru and clinicaltrials.gov. The search for the following words / phrases was performed: indolocarbazoles, indolocarbazole derivatives, staurosporine, rebeccamycin, staurosporine derivatives. The search was conducted from January 11 until March 1, 2021. The compounds with a biological activity which were undergoing or had undergone preclinical and clinical trials, were taken into account. All the materials from 1977 to January 1, 2021, were taken into account.Results. The materials obtained indicate that indolocarbazole derivatives are promising compounds for the creation of anticancer medicinal preparations due to their properties and peculiarities of the action mechanism. These drugs have a selective action due to the targeted interaction with specific molecular targets: kinases (especially protein kinase C and its isozymes), DNA and DNA topoisomerase. To date, many compounds from the class of indolocarbazoles have been synthesized and investigated. They have shown a high antitumor activity in the treatment of systemic and solid tumors. However, despite this, only one MP based on a staurosporine derivative, registered by the TN of Rydapt® (in the USA and EU countries) and Miticaid® (in the Russian Federation), is approved for use in the clinical practice.Conclusion. Thus, the basic data from scientific publications on promising anticancer medicinal preparations based on compounds from the class of indolocarbazoles, have been summarized. The information is provided, in particular, on their molecular structure, the origin, classification, the main representatives of the class, which are at various stages of the research and are approved for use in the clinic.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87086751","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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