RESUMO
Two previously undescribed coumarins (1-2) were isolated from the root of Notopterygium incisum. The structures of new findings were elucidated by analyses of spectral evidences in HRESIMS, NMR, as well as ICD. The absolute configurations were further confirmed by chemical calculations. 1-2 exhibits obviously anti-inflammatory activity by inhibiting the expression of inflammatory mediators (COX-2, iNOS), as well as reducing the release of NO and the accumulation of ROS in cells. Western blotting analysis revealed that 2 could inhibit the PI3K/AKT pathway by reducing the expression of p-PI3K and p-AKT.
Assuntos
Apiaceae , Cumarínicos , Óxido Nítrico Sintase Tipo II , Óxido Nítrico , Animais , Camundongos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Apiaceae/química , Cumarínicos/química , Cumarínicos/farmacologia , Cumarínicos/isolamento & purificação , Ciclo-Oxigenase 2/metabolismo , Relação Dose-Resposta a Droga , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Fosfatidilinositol 3-Quinases/metabolismo , Raízes de Plantas/química , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores , Células RAW 264.7 , Espécies Reativas de Oxigênio/metabolismo , Espécies Reativas de Oxigênio/antagonistas & inibidores , Relação Estrutura-Atividade , Nitrilas/químicaRESUMO
OBJECTIVE: To observe the clinical therapeutic effect of the combination of electroacupuncture (EA) at Baliao points (bilateral Shangliao [BL 31], Ciliao [BL 32], Zhongliao [BL 33] and Xialiao [BL 34]) and oral administration of mifepristone tablets and its influence on uterine volume restoration after uterine curettage of incomplete abortion as compared with simple oral administration of mifeprstone tablets. METHODS: A total of 58 patients after uterine curettage of incomplete abortion were randomized into an EA group and a western medication group, 29 cases in each one. In the western medication group, mifepristone tablets were administered orally, 2 tablets each time, once daily. In the EA group, on the base of the treatment as the western medication group, EA was applied to Baliao points, with disperse-dense wave, once daily, 50 min each time. The treatment for 3 days was as one course and 2 courses of treatment were required, at the interval of 1 day in the two courses. Before and after treatment, the area of intrauterine residue and blood flow signal positive rate of color Doppler flow imaging (CDFI) were recorded in patients of the two groups respectively. The days of vaginal bleeding and the rate of second operation were recorded after treatment in patients of the two groups. Using the three-dimensional ultrasound B reconstruction, the uterine endometrial volume after menstruation resumption was measured in patients of the two groups, and the clinical therapeutic effect was evaluated. RESULTS: After treatment, the intrauterine residue area and CDFI blood flow signal positive rate were all reduced as compared with the values before treatment in patients of the two groups (P<0.05). After treatment, the intrauterine residue area and CDFI blood flow signal positive rate in the EA group were less than those in the western medication group (P<0.05). After treatment, the days of vaginal bleeding in patients of the EA group were less than that in the western medication group and the rate of second operation was lower than the western medication group (P<0.05). The uterine endomentrial volume after menstruation resumption in the EA group was larger than that in the western medication group after treatment (P<0.05). The total effective rate was 55.2% (16/29) in the EA group, higher than 37.9% (11/29) in the western medication group (P<0.05). CONCLUSION: The combined treatment of electroacupuncture at Baliao points and oral administration of mifepristone tablets effectively promotes uterine contraction, softens and discharges intrauterine residue and contributes to uterine volume restoration in the patients after uterine curettage of incomplete abortion. The therapeutic effect of this combined therapy is better than simple oral administration of mifepristone tablets.
Assuntos
Aborto Incompleto , Aborto Induzido , Eletroacupuntura , Aborto Incompleto/terapia , Pontos de Acupuntura , Curetagem , Feminino , Humanos , GravidezRESUMO
The aim of this study was to evaluate the role of endoplasmic reticulum (ER) stress in diabetic retinopathy (DR) using in vitro and in vivo models. For the in vivo studies, diabetes was induced in rats, and retinal expression of glucose-regulated protein 78 (GRP78), activating transcription factor 4 (ATF4), C/EBP homologous protein (CHOP), and vascular endothelial growth factor (VEGF) in groups of rats at 1, 3, and 6 months was assessed. For the in vitro studies, human retinal capillary endothelial cells (HRCECs) were cultured in the presence of varying glucose concentrations, and the expression of mRNA and protein for GRP78, ATF4, CHOP, and VEGF was assessed. The chosen glucose concentrations were reflective of those apparent in diabetic patients. Expression of VEGF and CHOP mRNA levels were significantly increased in diabetic rats compared to control rats at 1, 3, and 6 months (P < 0.05). In HRCECs cultured in the presence of high as well as variable glucose concentrations, CHOP expression and apoptosis were significantly increased (P < 0.05). However, GRP78 and ATF4 expression levels were unchanged. Our findings suggest that early progression of DR may be mediated by ER stress, but probably does not involve changes in ATF4 or GRP78.