Matheus Brum Felício , Caio de Castro Mello , Marcela de Sá Hauck , Tiago Antônio de Oliveira Mendes , Virginia Ramos Pizziolo , Maria do Carmo Pelusio , Gaspar Diaz-Muñoz , Leandro Licursi de Oliveira , Marisa Alves Nogueira Diaz
{"title":"二苯甲酰甲烷衍生物在炎症和疼痛实验模型中的抗炎和抗氧化活性","authors":"Matheus Brum Felício , Caio de Castro Mello , Marcela de Sá Hauck , Tiago Antônio de Oliveira Mendes , Virginia Ramos Pizziolo , Maria do Carmo Pelusio , Gaspar Diaz-Muñoz , Leandro Licursi de Oliveira , Marisa Alves Nogueira Diaz","doi":"10.1016/j.prerep.2025.100052","DOIUrl":null,"url":null,"abstract":"<div><div>This study evaluated the anti-inflammatory, antinociceptive, and antioxidant activities of the synthetic compound 2-benzyl-1,3-diphenyl-1,3-propanedione (DPBP) in paw edema and inflammatory bowel disease models. Additionally, the pharmacokinetics of the compound were assessed following intraperitoneal and transdermal administration. The anti-inflammatory activity was evaluated through formalin-induced paw edema and by measuring levels of anti-inflammatory cytokines (IL-4, IL-10) and pro-inflammatory cytokines (IFN-γ). Antinociceptive activity was determined by assessing the reduction in time animals spent licking, shaking, or biting the injected paw, as well as by the reduction in abdominal writhing induced by intraperitoneal injection of acetic acid. Antioxidant activity was assessed by measuring the activities of antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), and glutathione S-transferase (GST), along with tissue concentrations of malondialdehyde (MDA) and nitric oxide (NO). DPBP was detected in serum for up to 12 h following both transdermal and intraperitoneal administration. Transdermal administration of DPBP demonstrated significant antioxidant activity, reducing nitric oxide levels in the colon and small intestine of animals with inflammatory bowel disease. These results show that the transdermal route is a viable alternative for this disease, especially considering the growing interest in alternative and innovative therapies for inflammatory bowel disease, with transdermal delivery emerging as a promising approach. Intraperitoneal administration reduced paw edema, decreased nociceptive behavior following formalin-induced pain, and reduced abdominal writhing caused by acetic acid. Furthermore, intraperitoneal administration increased the production of anti-inflammatory cytokines such as IL-4 and IL-10 and enhanced the activity of antioxidant enzymes (SOD and GST). These findings suggest that DPBP exhibits strong anti-inflammatory, antinociceptive, and antioxidant activities, making it a promising candidate for the treatment of inflammation and its associated symptoms.</div></div>","PeriodicalId":101015,"journal":{"name":"Pharmacological Research - Reports","volume":"4 ","pages":"Article 100052"},"PeriodicalIF":0.0000,"publicationDate":"2025-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Anti-inflammatory and antioxidant activities of a dibenzoylmethane derivative in experimental models of inflammation and pain\",\"authors\":\"Matheus Brum Felício , Caio de Castro Mello , Marcela de Sá Hauck , Tiago Antônio de Oliveira Mendes , Virginia Ramos Pizziolo , Maria do Carmo Pelusio , Gaspar Diaz-Muñoz , Leandro Licursi de Oliveira , Marisa Alves Nogueira Diaz\",\"doi\":\"10.1016/j.prerep.2025.100052\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>This study evaluated the anti-inflammatory, antinociceptive, and antioxidant activities of the synthetic compound 2-benzyl-1,3-diphenyl-1,3-propanedione (DPBP) in paw edema and inflammatory bowel disease models. Additionally, the pharmacokinetics of the compound were assessed following intraperitoneal and transdermal administration. The anti-inflammatory activity was evaluated through formalin-induced paw edema and by measuring levels of anti-inflammatory cytokines (IL-4, IL-10) and pro-inflammatory cytokines (IFN-γ). Antinociceptive activity was determined by assessing the reduction in time animals spent licking, shaking, or biting the injected paw, as well as by the reduction in abdominal writhing induced by intraperitoneal injection of acetic acid. Antioxidant activity was assessed by measuring the activities of antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), and glutathione S-transferase (GST), along with tissue concentrations of malondialdehyde (MDA) and nitric oxide (NO). DPBP was detected in serum for up to 12 h following both transdermal and intraperitoneal administration. Transdermal administration of DPBP demonstrated significant antioxidant activity, reducing nitric oxide levels in the colon and small intestine of animals with inflammatory bowel disease. These results show that the transdermal route is a viable alternative for this disease, especially considering the growing interest in alternative and innovative therapies for inflammatory bowel disease, with transdermal delivery emerging as a promising approach. Intraperitoneal administration reduced paw edema, decreased nociceptive behavior following formalin-induced pain, and reduced abdominal writhing caused by acetic acid. Furthermore, intraperitoneal administration increased the production of anti-inflammatory cytokines such as IL-4 and IL-10 and enhanced the activity of antioxidant enzymes (SOD and GST). These findings suggest that DPBP exhibits strong anti-inflammatory, antinociceptive, and antioxidant activities, making it a promising candidate for the treatment of inflammation and its associated symptoms.</div></div>\",\"PeriodicalId\":101015,\"journal\":{\"name\":\"Pharmacological Research - Reports\",\"volume\":\"4 \",\"pages\":\"Article 100052\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2025-06-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmacological Research - Reports\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2950200425000266\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmacological Research - Reports","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2950200425000266","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Anti-inflammatory and antioxidant activities of a dibenzoylmethane derivative in experimental models of inflammation and pain
This study evaluated the anti-inflammatory, antinociceptive, and antioxidant activities of the synthetic compound 2-benzyl-1,3-diphenyl-1,3-propanedione (DPBP) in paw edema and inflammatory bowel disease models. Additionally, the pharmacokinetics of the compound were assessed following intraperitoneal and transdermal administration. The anti-inflammatory activity was evaluated through formalin-induced paw edema and by measuring levels of anti-inflammatory cytokines (IL-4, IL-10) and pro-inflammatory cytokines (IFN-γ). Antinociceptive activity was determined by assessing the reduction in time animals spent licking, shaking, or biting the injected paw, as well as by the reduction in abdominal writhing induced by intraperitoneal injection of acetic acid. Antioxidant activity was assessed by measuring the activities of antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), and glutathione S-transferase (GST), along with tissue concentrations of malondialdehyde (MDA) and nitric oxide (NO). DPBP was detected in serum for up to 12 h following both transdermal and intraperitoneal administration. Transdermal administration of DPBP demonstrated significant antioxidant activity, reducing nitric oxide levels in the colon and small intestine of animals with inflammatory bowel disease. These results show that the transdermal route is a viable alternative for this disease, especially considering the growing interest in alternative and innovative therapies for inflammatory bowel disease, with transdermal delivery emerging as a promising approach. Intraperitoneal administration reduced paw edema, decreased nociceptive behavior following formalin-induced pain, and reduced abdominal writhing caused by acetic acid. Furthermore, intraperitoneal administration increased the production of anti-inflammatory cytokines such as IL-4 and IL-10 and enhanced the activity of antioxidant enzymes (SOD and GST). These findings suggest that DPBP exhibits strong anti-inflammatory, antinociceptive, and antioxidant activities, making it a promising candidate for the treatment of inflammation and its associated symptoms.