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

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
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摘要

本研究评估了合成化合物2-苄基-1,3-二苯基-1,3-丙二酮(DPBP)在足跖水肿和炎症性肠病模型中的抗炎、抗炎和抗氧化活性。此外,在腹腔和透皮给药后,对化合物的药代动力学进行了评估。通过测量抗炎细胞因子(IL-4、IL-10)和促炎细胞因子(IFN-γ)的水平,通过福尔马林诱导的足跖水肿来评估抗炎活性。通过评估动物舔、摇或咬注射的爪子的时间减少,以及通过腹腔注射乙酸引起的腹部扭动减少,来确定抗伤性活性。通过测定抗氧化酶如超氧化物歧化酶(SOD)、过氧化氢酶(CAT)和谷胱甘肽s -转移酶(GST)的活性,以及丙二醛(MDA)和一氧化氮(NO)的组织浓度来评估抗氧化活性。经皮和腹腔给药后,血清中检测到DPBP长达12 h。经皮给药DPBP显示出显著的抗氧化活性,降低炎症性肠病动物结肠和小肠中的一氧化氮水平。这些结果表明,透皮途径是这种疾病的一种可行的替代方法,特别是考虑到对炎症性肠病的替代和创新疗法的兴趣日益增长,透皮给药成为一种有希望的方法。腹腔注射减少足部水肿,减少福尔马林引起的疼痛后的伤害行为,减少醋酸引起的腹部扭动。此外,腹腔内给药增加了抗炎细胞因子如IL-4和IL-10的产生,增强了抗氧化酶(SOD和GST)的活性。这些发现表明,DPBP具有很强的抗炎、抗伤和抗氧化活性,使其成为治疗炎症及其相关症状的有希望的候选物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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.
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