V. S. Slyusarenko, M. Korokin, S. Kovalenko, Aleksandr N. Stadnichenko, L. Korokina
{"title":"一种新的丙酸双药效团衍生物的抗炎活性研究","authors":"V. S. Slyusarenko, M. Korokin, S. Kovalenko, Aleksandr N. Stadnichenko, L. Korokina","doi":"10.26655/JMCHEMSCI.2021.4.10","DOIUrl":null,"url":null,"abstract":"This experimental laboratory animals research aimed at the anti-inflammatory activity of a new dipharmacophore derivative dexibuprofen and nebracetam when modeling an acute and chronic inflammatory reaction. The studied dipharmacophore compound based on dexibuprofen and nebracetam is indicated by the dexibuneb laboratory code and has the chemical formula (2S) -N - ((1-benzyl-5-hydroxypyrrolidin-3-yl) methyl) -2- (4-isobutylphenyl) propanamide. Dexibuneb was administered intragastrically at a dose of 80 mg/kg; dexibuprofen and nebracetam were administered intragastrically at a dose of 40 mg/kg. The minimum increase in paw edema was recorded in the group of animals treated with dexibuneb. It amounted to 33.61 ± 7.41 of the initial value, which is statistically significantly (p <0.05) less than the values both in the control group and in the groups treated with dexibuprofen nebracetam monotherapy. The use of dexibuneb reduced the increase in dry weight of the granuloma by 43.09% (p <0.05) relative to the increase in the control group. In this study, when studying the severity of the anti-inflammatory effect on acute and chronic inflammation models, we found a positive pharmacodynamic interaction of molecular fragments of various therapeutic orientations, combined in an innovative dipharmacophore compound with the laboratory name dexibuneb. Inhibition of paw edema after introducing carrageenan into the plantar aponeurosis and the increase in the mass of granulomas implanted in rat armpits was statistically significantly more pronounced in the groups of animals treated with dexibuneb than with dexibuprofen and nebracetam monotherapy.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"Anti-Inflammatory Activity of a New Dipharmacophore Derivative of Propionic Acid\",\"authors\":\"V. S. Slyusarenko, M. Korokin, S. Kovalenko, Aleksandr N. Stadnichenko, L. Korokina\",\"doi\":\"10.26655/JMCHEMSCI.2021.4.10\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"This experimental laboratory animals research aimed at the anti-inflammatory activity of a new dipharmacophore derivative dexibuprofen and nebracetam when modeling an acute and chronic inflammatory reaction. The studied dipharmacophore compound based on dexibuprofen and nebracetam is indicated by the dexibuneb laboratory code and has the chemical formula (2S) -N - ((1-benzyl-5-hydroxypyrrolidin-3-yl) methyl) -2- (4-isobutylphenyl) propanamide. Dexibuneb was administered intragastrically at a dose of 80 mg/kg; dexibuprofen and nebracetam were administered intragastrically at a dose of 40 mg/kg. The minimum increase in paw edema was recorded in the group of animals treated with dexibuneb. It amounted to 33.61 ± 7.41 of the initial value, which is statistically significantly (p <0.05) less than the values both in the control group and in the groups treated with dexibuprofen nebracetam monotherapy. The use of dexibuneb reduced the increase in dry weight of the granuloma by 43.09% (p <0.05) relative to the increase in the control group. In this study, when studying the severity of the anti-inflammatory effect on acute and chronic inflammation models, we found a positive pharmacodynamic interaction of molecular fragments of various therapeutic orientations, combined in an innovative dipharmacophore compound with the laboratory name dexibuneb. Inhibition of paw edema after introducing carrageenan into the plantar aponeurosis and the increase in the mass of granulomas implanted in rat armpits was statistically significantly more pronounced in the groups of animals treated with dexibuneb than with dexibuprofen and nebracetam monotherapy.\",\"PeriodicalId\":16365,\"journal\":{\"name\":\"Journal of Medicinal and Chemical Sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2021-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Medicinal and Chemical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.26655/JMCHEMSCI.2021.4.10\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicinal and Chemical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.26655/JMCHEMSCI.2021.4.10","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Anti-Inflammatory Activity of a New Dipharmacophore Derivative of Propionic Acid
This experimental laboratory animals research aimed at the anti-inflammatory activity of a new dipharmacophore derivative dexibuprofen and nebracetam when modeling an acute and chronic inflammatory reaction. The studied dipharmacophore compound based on dexibuprofen and nebracetam is indicated by the dexibuneb laboratory code and has the chemical formula (2S) -N - ((1-benzyl-5-hydroxypyrrolidin-3-yl) methyl) -2- (4-isobutylphenyl) propanamide. Dexibuneb was administered intragastrically at a dose of 80 mg/kg; dexibuprofen and nebracetam were administered intragastrically at a dose of 40 mg/kg. The minimum increase in paw edema was recorded in the group of animals treated with dexibuneb. It amounted to 33.61 ± 7.41 of the initial value, which is statistically significantly (p <0.05) less than the values both in the control group and in the groups treated with dexibuprofen nebracetam monotherapy. The use of dexibuneb reduced the increase in dry weight of the granuloma by 43.09% (p <0.05) relative to the increase in the control group. In this study, when studying the severity of the anti-inflammatory effect on acute and chronic inflammation models, we found a positive pharmacodynamic interaction of molecular fragments of various therapeutic orientations, combined in an innovative dipharmacophore compound with the laboratory name dexibuneb. Inhibition of paw edema after introducing carrageenan into the plantar aponeurosis and the increase in the mass of granulomas implanted in rat armpits was statistically significantly more pronounced in the groups of animals treated with dexibuneb than with dexibuprofen and nebracetam monotherapy.