Haixia Wang

Luteolin, a polyphenolic flavone, has been demonstrated to exert anti-tumor activity in various cancer types. Cisplatin drug resistance is a major obstacle in the management of ovarian cancer. In the present study, we investigated the chemo-sensitizing effect of luteolin in both cisplatin-resistant ovarian cancer cell line and a mice xenotransplant model. In vitro, CCK-8 assay showed that luteolin inhibited cell proliferation in a dose-dependent manner, and luteolin enhanced anti-proliferation effect of cisplatin on cisplatin-resistant ovarian cancer CAOV3/DDP cells. Flow cytometry revealed that luteolin enhanced cell apoptosis in combination with cisplatin. Western blotting and qRT-PCR assay revealed that luteolin increased cisplatin-induced downregulation of Bcl-2 expression. In addition, wound-healing assay and Matrigel invasion assay showed that luteolin and cisplatin synergistically inhibited migration and invasion of CAOV3/DDP cells. Moreover, in vivo, luteolin enhanced cisplatin-induced reduction of tumor growth as well as induction of apoptosis. We suggest that luteolin in combination with cisplatin could potentially be used as a new regimen for the treatment of ovarian cancer.

BMS-816336 (6n-2), a hydroxy-substituted adamantyl acetamide, has been identified as a novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC₅₀ 3.0 nM) with >10000-fold selectivity over human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2). 6n-2 exhibits a robust acute pharmacodynamic effect in cynomolgus monkeys (ED₅₀ 0.12 mg/kg) and in DIO mice. It is orally bioavailable (%F ranges from 20 to 72% in preclinical species) and has a predicted pharmacokinetic profile of a high peak to trough ratio and short half-life in humans. This ADME profile met our selection criteria for once daily administration, targeting robust inhibition of 11β-HSD1 enzyme for the first 12 h period after dosing followed by an “inhibition holiday” so that the potential for hypothalamic–pituitary–adrenal (HPA) axis activation might be mitigated. 6n-2 was found to be well-tolerated in phase 1 clinical studies and represents a potential new treatment for type 2 diabetes, metabolic syndrome, and other human diseases modulated by glucocorticoid control.

The aim of the present study was to determine the prevalence and risk factors for vaginitis, the proportion of pathogens, and cognition of reproductive age patients on the harmful effects of vaginitis, its risk factors, and treatment. This retrospective study enrolled 6,150 patients admitted to the Shanghai Jinshan Central Hospital from 2011 to 2015 with a chief complaint of abnormal vaginal discharge. A questionnaire was designed to survey the cognition of patients on the harmful effects of vaginitis. Routine gynecological examinations and laboratory tests were performed and the risk factors for contracting vaginitis were analyzed by multifactor logistic regression analysis. The positive pathogen rate was 65.63% (4,036/6,150). Trichomonas infections were diagnosed in 1,416 (35.08%) cases including 761 (18.86%) cases of single trichomonas infections, which was significantly higher than the proportion of any other single pathogen infection (P<0.05). From 2011 to 2015, trichomoniasis and chlamydia infections decreased, but bacteria, candida and mycoplasma infections increased. The questionnaire survey showed a low cognition level on iatrogenic and mother-to-child transmission of vaginal infections as well as the risk of ectopic pregnancy and infertility, and on how to prevent vaginal infections. Logistic multifactor regression analysis revealed that advanced age, a low educational level, farmers, childbearing history and a low income were the risk factors for vaginitis. Women of reproductive age showed a high rate of vaginal infections and more attention should be paid to women with a low education level and income to reduce the incidence of vaginal infections in this population.