RESUMO
Phytochemical investigation on the fruits of Cydonia oblonga Mill., a traditional Uighur medicine, led to the isolation of seven undescribed and nine known megastigmane glycosides. Their structures including absolute configurations were characterized by an extensive analysis of spectroscopic data including HRESIMS and NMR, combined with ECD calculations. Additionally, compounds 1, 2, 4, and 6-16 exhibited anti-inflammatory activity by inhibiting the secretion of cytokines TNF-α and IL-6 in RAW264.7 cells induced by lipopolysaccharides (LPS) with inhibitory rates of 10.79%-44.58% at 20 µM.
Assuntos
Cicloexanonas , Glicosídeos , Lipopolissacarídeos , Norisoprenoides , Norisoprenoides/química , Norisoprenoides/farmacologia , Norisoprenoides/isolamento & purificação , Camundongos , Glicosídeos/química , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Células RAW 264.7 , Animais , Cicloexanonas/química , Cicloexanonas/farmacologia , Cicloexanonas/isolamento & purificação , Lipopolissacarídeos/farmacologia , Lipopolissacarídeos/antagonistas & inibidores , Estrutura Molecular , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Interleucina-6/antagonistas & inibidores , Interleucina-6/metabolismo , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Relação Estrutura-Atividade , Relação Dose-Resposta a Droga , GlucosídeosRESUMO
OBJECTIVE: To study the preventive effects of jinghua weikang capsule (JWC) on nonsteroidal anti-inflammatory drugs (NSAIDs) induced injury to the mucosa of the small intestine. METHODS: Thirty-two Wistar rats were randomly divided into four groups, i.e., the blank control group, the model group, the JWC group, and the esomeprazole group. Diclofenac was administered to rats in the model group, the JWC group, and the esomeprazole group at the daily dose of 15 mg/kg. JWC and esomeprazole was respectively given to those in the JWC group, and the esomeprazole group one day ahead. Normal saline was given to rats in the blank control group. Rats were killed 3 days later. The pathological changes of the small intestine were observed by hematoxylin and eosin stain. RESULTS: Compared with the blank control group, the general score for the small intestine (4.63 +/-0.52 vs 0.00 +/-0. 00) and the pathological score (4.00 +/-0.90 vs 0.00 +/-0. 00) obviously increased in the model group, showing statistical difference (P <0.05). Compared with the model group, the general score for the small intestine (1.88 +/-0.99) and the pathological score (2.11 +/-1.11) obviously decreased in the JWG group, showing statistical difference (P <0.05). Compared with the model group, the general score for the small intestine (2.75 +/-1.28) and the pathological score (2. 30 +/-0.94) obviously decreased in the esomeprazole group, showing statistical difference (P <0.05). CONCLUSION: JWC could prevent NSAIDs induced injury to the mucosa of the small intestine.