The compound (E)-2-cyano-N,3-diphenylacrylamide (JMPR-01) was structurally developed using bioisosteric modifications of a hybrid prototype as formed from fragments of indomethacin and paracetamol. Initially, in vitro assays were performed to determine cell viability (in macrophage cultures), and its ability to modulate the synthesis of nitrite and cytokines (IL-1β and TNFα) in non-cytotoxic concentrations. In vivo, anti-inflammatory activity was explored using the CFA-induced paw edema and zymosan-induced peritonitis models. To investigate possible molecular targets, molecular docking was performed with the following crystallographic structures: LT-A4-H, PDE4B, COX-2, 5-LOX, and iNOS. As results, we observed a significant reduction in the production of nitrite and IL-1β at all concentrations used, and also for TNFα with JMPR-01 at 50 and 25 μM. The anti-edematogenic activity of JMPR-01 (100 mg/kg) was significant, reducing edema at 2–6 h, similar to the dexamethasone control. In induced peritonitis, JMPR-01 reduced leukocyte migration by 61.8, 68.5, and 90.5% at respective doses of 5, 10, and 50 mg/kg. In silico, JMPR-01 presented satisfactory coupling; mainly with LT-A4-H, PDE4B, and iNOS. These preliminary results demonstrate the strong potential of JMPR-01 to become a drug for the treatment of inflammatory diseases.

Medicinal plants play an essential role in the health systems of many countries. Ulcerative colitis (UC) is a chronic inflammatory bowel disease with pharmacological therapy associated with adverse effects and relapses. Several experimental models are used to evaluate intestinal inflammation, including the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced ulcerative colitis model. Thus, the aim of the study was to identify plant extracts and phytoconstituents with promising activities in the experimental model of TNBS-induced ulcerative colitis and their respective mechanisms of action and, thus, aid in the treatment of UC. For this, a literature review was carried out using articles indexed in the Pubmed and Science Direct databases, with the descriptors: “Extracts”, “Ulcerative colitis” and “TNBS”. The inclusion criteria were articles in Portuguese, English and Spanish, published in the last 6 years (2019-2024) and the exclusion criteria were those that diverged from the chosen theme and outside the time range. Twenty articles were selected, indicating that extracts and phytoconstituents reduce the symptoms and severity of lesions caused by TNBS, through the inhibition of the expression of inflammatory pathways, enzymes, immune cells and cytokines involved in inflammation, in addition to the reduction of oxidative stress. Therefore, it is concluded that extracts and phytoconstituents are effective and safe options for the management of UC, acting as alternatives to conventional therapies.

Erythrina velutina, conhecida como mulungu, é uma espécie nativa da Caatinga, bioma brasileiro único e com características semiáridas. Essa espécie é utilizada popularmente na forma de decocto como sedativa, anticonvulsivante, neuroprotetora e ansiolítica. A ansiedade patológica é uma desordem psíquica que, atualmente, é a causa mais comum de incapacidade em todo o mundo, fato que intensificou a busca por novos tratamentos com menos efeitos adversos e melhor eficácia terapêutica. Dessa forma, o presente artigo teve como objetivo avaliar o efeito toxicológico agudo do decocto de Erythrina velutina (DEv) e investigar seu possível efeito ansiolítico. Foi avaliada a toxicidade aguda oral em camundongos durante 14 dias. A prospecção da atividade ansiolítica do DEv foi realizada por meio de testes comportamentais em camundongos, como Teste em Labirinto cruz elevada (TLCE) e medidas etológicas (espreitas, levantar-se, auto-limpeza e mergulho de cabeça), Teste da Movimentação Espontânea (TME) e teste de barra giratória (rota rod). A toxicidade aguda em camundongos não demostrou sinais de toxicidade do decocto na dose testada. No TLCE, o DEv apresentou efeito ansiolítico, houve redução dos fatores etológicos (espreita, mergulho de cabeça e auto-limpeza), no campo aberto o decocto aumentou no número de ambulação, reduziu a auto-limpeza e não modificou o levantar-se. No teste rota rod, pode-se presumir que o DEv apresentou alteração na atividade motora. Dessa forma, foi possível comprovar que o DEv apresenta promissora atividade ansiolítica, corroborando com seu uso popular. Palavras-chave: mulungu; labirinto em cruz elevado fitoterapia.

Background/Objectives: Inflammatory bowel diseases (IBD) are conditions of the gastrointestinal tract with treatments linked to side effects and relapses. Spondias mombin L. is a species with anti-inflammatory action, but there is little information in the literature about its application in the treatment of IBD. The aim of this study was to evaluate the intestinal anti-inflammatory activity of hydroalcoholic extract of Spondias mombin L. (HESm) in a rat model of ulcerative colitis (UC). Methods: Hydroalcoholic extract was obtained using the turboextraction technique, followed by identification of its major components using ultra-high performance liquid chromatography (UFLC). Intestinal anti-inflammatory activity was evaluated in an acute model of UC induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS). Groups received a vehicle, prednisolone (2 mg/kg), or HESm (125, 250 or 500 mg/kg) before and after UC induction. Ulcerated area, score, and intestinal weight/length ratio were analyzed. Histopathological analysis and the extract’s effect on the contractility of the intestinal segment were carried out. Results: UFLC identified the presence of quercetin, a flavonoid widely cited for the species. At doses of 125, 250, and 500 mg/kg, the extract reduced areas of injury by 86.82, 92.67, and 85.06%, respectively, compared to the control, in addition to reducing scores and weight/length ratio of the colons. Histopathological analysis confirmed the results. In contractility, the extract at the highest concentration tested reduced the response of the muscarinic agonist carbamylcholine to 53.7 ± 4.2% of control contraction. Conclusions: Results demonstrate the species’ ability to reduce injuries caused by colitis, suggesting its potential to contribute to the clinical management of IBD in the future.