Abstract This study aimed to investigate the therapeutic effect of koumine on collagen-induced arthritis (CIA) in mice. Koumine was extracted from Gelsemium Elegans Benth. The CIA model was established in Balb/c mice. Forty successfully modeled mice were randomly divided into model group and 2, 4 and 8 mg/kg koumine groups, 10 mice in each group. Another 10 normal mice were selected as control group. The 2, 4 and 8 mg/kg koumine groups were treated with 2, 4 and 8 mg/kg koumine, respectively, for three successive weeks. At the end of treatment, compared with model group, in 4 and 8 mg/kg koumine groups the arthritis index was significantly decreased (P < 0.05), the peripheral blood interleukin-17 level and T helper 17 (Th17) cell percentage were significantly decreased (P < 0.05), the peripheral blood interleukin-10 level and regulatory T (Treg) cell percentage were significantly increased (P < 0.05), the spleen tissue RORγt protein expression level was significantly decreased (P < 0.05), and the spleen tissue Foxp3 protein expression level was significantly increased (P < 0.05). In conclusion, koumine has therapeutic effect on CIA in mice. The mechanism may be related to its regulating the RORγt/Foxp3 expressions, thus correcting the Th17/Treg immune imbalance.

Hepatocellular carcinoma is one of the most prevalent malignancies and a leading cause of cancer-related mortality worldwide. However, the therapies to prevent hepatocellular carcinoma are still limited and the emergence of drug resistance leads to the development of new anti-cancer drugs and combinational chemotherapy regimens. Our study was aimed to explore the anticancer effects of the essential oil extract (EEEO) from Euphorbia esula which has been widely used in traditional Chinese folk medicine and possessed potential cytotoxic effects in several human tumor cells. However, the mechanisms of EEEO-induced anti-proliferation and apoptosis have not been completely elucidated. In this study, EEEO was prepared by hydro-distillation and the main chemical component of EEEO was identified by GC-MS. HepG2 cells were treated with EEEO in vitro and then evaluated with respect to proliferation, apoptosis, and levels of reactive oxygen species (ROS) and apoptotic proteins. Our studies showed that EEEO decreased cell viability, elevated ROS levels, and induced apoptosis of HepG2 cells in a concentration- and time-dependent manner. Furthermore, Bcl-2 was down-regulated, while Bax was up-regulated in HepG2 after EEEO treatment. These results suggest that EEEO induced apoptosis of HepG2 cells and indicate that this apoptosis might be mediated by the mitochondrial pathway.

Resumo Justificativa e objetivos: O cloridrato de tramadol é um analgésico opioide de ação central que se liga a receptores opioides específicos. É usado no tratamento de dor crônica e recomendado como fármaco de primeira linha para o tratamento no pós-operatório ou em dor aguda induzida por lesão ortopédica. O presente estudo visa a preparar e avaliar o filme bucal mucoadesivo de cloridrato de tramadol como uma nova forma de analgesia prolongada para pacientes com lesões ortopédicas. Método: Filmes bucais de cloridrato de tramadol foram preparados pelo método de evaporação de solvente. Os filmes preparados foram avaliados para os vários parâmetros de avaliação, como espessura, pH da superfície, uniformidade do peso, uniformidade do conteúdo, resistência a dobras, índice de intumescimento, estudo de liberação da droga in vitro, teste in vitro para mucoadesão e estudos in vivo (teste de irritação da mucosa primária e atividade analgésica). Resultados: Todas as formulações apresentaram bons resultados para caracterizações físico-químicas. Em estudo de libertação de droga in vitro, os filmes exibiram liberação controlada por mais de 12 horas. A formulação de BFT2 (com quitosana e PVP K-90) não mostrou efeito irritante sobre a mucosa bucal e provocou uma atividade analgésica significativa in vivo com 57,14% de analgesia versus a do padrão (61,04%). Concluiu-se que os filmes mucoadesivos de cloridrato de tramadol podem ser usados eficazmente para aliviar a dor intensa de lesões ortopédicas com início rápido e ação prolongada.

Abstract Background and objectives: Tramadol hydrochloride is a centrally-acting synthetic opioid analgesic binding to specific opioid receptors. It is used in the management of chronic pain and is recommended as first line drug in the treatment of postoperative or orthopedic injury induced acute pain. The present work is designed to prepare and evaluate mucoadhesive buccal film of tramadol hydrochloride as a novel form of prolonged analgesia for patients with orthopedic injuries. Methods: Buccal films of tramadol hydrochloride were prepared by solvent casting method. The prepared films were evaluated for the various evaluation parameters like thickness, surface pH, weight uniformity, content uniformity, folding endurance, swelling index, in vitro drug release study, in vitro test for mucoadhesion and in vivo studies (primary mucosal irritancy test and analgesic activity). Results: All the formulations exhibited good results for physicochemical characterizations. In in vitro drug release study the films exhibited controlled release more than 12 hours. The formulation BFT2 (containing chitosan and PVP K-90) showed no irritant effect on buccal mucosa and elicit the significant in vivo analgesic activity with 57.14% analgesia against that of standard (61.04%). It was concluded that the mucoadhesive films of tramadol hydrochloride can be effectively used to alleviate the severe pain of orthopedic injuries with prompt onset and prolonged action.

The enantioselective synthesis of highly functionalized cyclohexa-1,3-dienes was achieved via an organocatalytic one-pot three-component domino reaction. In addition, a possible mechanism accounting for the reaction was proposed.

Cinco derivados naturais [ácido ferúlico (FA), polifenol de chá lipidio-solúvel (LTP), polifenol de chá solúvel em água (WTP), sesamol (SE) e ácido cafeico (CA)] foram avaliados como aditivos antioxidantes para melhorar a estabilidade da oxidação de biodiesel de óleo de soja (SBO-BD). Verificou-se que WTP, LTP, SE e CA podem melhorar significativamente a estabilidade de SBO-BD. CA apresentou o melhor desempenho no intervalo de concentração de 500 a 1500 ppm, enquanto que WTP mostrou atividade mais elevada a uma concentração de 200 ppm. Para comparação, o efeito estabilizador de três antioxidantes sintéticos [α-tocoferol (α-T), butilhidroxitolueno (BHT) e butilhidroxianisol (BHA)] foi avaliado simultaneamente. Os resultados mostraram que o efeito de alguns aditivos naturais (WTP, LTP, SE e CA) foi melhor que de aditivos sintéticos (α-T, BHT e BHA) na estabilidade da oxidação de SOB-BD. Uma explicação possível para os efeitos diferentes entre os antioxidantes testados foi elaborada levando em conta sua estrutura molecular.

Five natural derivatives [ferulic acid (FA), lipid-soluble tea polyphenol (LTP), water-soluble tea polyphenol (WTP), sesamol (SE) and caffeic acid (CA)] were evaluated as antioxidative additives for enhancing the oxidation stability of soybean oil based biodiesel (SBO-BD). It was found that WTP, LTP, SE and CA could significantly improve the oxidation stability of SBO-BD. CA displayed the best performance in the concentration range from 500 to 1500 ppm, whereas WTP displayed the highest activeness at a concentration of 2000 ppm. For comparison, the stabilizing effect of three synthetic anti-oxidants [α-tocopherol (α-T), butylhydroxytoluene (BHT) and butylhydroxyanisol (BHA)] was simultaneously evaluated. The results showed that the effect of some natural additives (WTP, LTP, SE and CA) was better than that of synthetic additives (α-T, BHT and BHA) on the oxidation stability of SBO-BD. A possible explanation for the different effects among the tested antioxidants was given based on their molecular structures.