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Zhu W.,Chinese Academy of Sciences | Liu X.,Chinese Academy of Sciences | He J.,Chinese Academy of Sciences | Chen D.,Chinese Academy of Sciences | And 2 more authors.
BMC Cancer | Year: 2011

Background: Lung cancer is the leading cause of cancer-related deaths worldwide. Early detection is considered critical for lung cancer treatment. MicroRNAs (miRNAs) have shown promise as diagnostic and prognostic indicators. This study was to identify specific miRNAs with diagnostic and prognostic value for patients with lung cancer, and to explore the correlation between expression profiles of miRNAs and patient survival.Methods: Gene expression of members of the miR-183 family (miR-96, miR-182, and miR-183) were examined in 70 paired samples from lung cancer patients (primary cancer and non-cancerous tissues and sera), as well as 44 serum samples from normal volunteers and lung cancer cell lines by quantitative real-time reverse transcription polymerase chain reaction (RT-qPCR). The correlation between the expression of miRNAs in tissues, sera, and patient overall survival were also examined by log-rank and Cox regression analysis.Results: Expression levels of members of the miR-183 family in lung cancer tumor and sera were higher than that of their normal counterparts. The miR-96 expression in tumors was positively associated with its expression in sera. Log-rank and Cox regression analyses demonstrated that high expression of tumor and serum miRNAs of the miR-183 family were associated with overall poor survival in patients with lung cancer.Conclusions: Our results suggest that the expressions of miR-96, miR-182, and miR-183 in tumor and sera may be considered potential novel biomarkers for the diagnosis and prognosis of lung cancer. © 2011 Zhu et al; licensee BioMed Central Ltd.

Zhao S.-L.,Zhejiang Ocean University | Peng Z.,Zhejiang Ocean University | Zhen X.-H.,Zhejiang Ocean University | Jin H.-G.,Zhoushan Hospital of Zhejiang Province | And 3 more authors.
Medicinal Chemistry Research | Year: 2015

In this study, we examined a series of 2′,4′,6′-trihydroxychalcone derivatives for their inhibitory activity as inhibitors of CDC25B and PTP1B. The pharmacological results showed that all of the tested compounds significantly inhibited CDC25B and PTP1B phosphatase in vitro. Among them, three compounds 2, 6, and 7 had the best inhibition activity, with inhibition rates against CDC25B were 99.56, 99.68, and 99.63 %, respectively, and with inhibition rates against PTP1B were 98.99, 99.37, and 98.08 %, respectively, which is similar to reference drugs Na3VO4 and Oleanolic acid, respectively. Cytotoxic activity assays showed compounds 2, 6, and 7 are potent against HeLa and HCT116. Moreover, compound 6 delayed the potent antitumor inhibitory activity in a colo205 xenograft model in vivo. © 2014 Springer Science+Business Media.

Ma J.-Y.,Zhejiang Ocean University | Quan Y.-C.,Yanbian University | Jin H.-G.,Zhoushan Hospital of Zhejiang Province | Zhen X.-H.,Zhejiang Ocean University | And 2 more authors.
Chemical Biology and Drug Design | Year: 2016

Herein, a series of 3-phenyliminoindolin-2-one derivatives were designed, synthesized, and screened for their antidepressant and anticonvulsant activities. The IR spectra of the compounds afforded NH stretching (3340-3346 cm-1) bands and C=O stretching (1731-1746 cm-1). In the 1H-NMR spectra of the compounds, N-H protons of indoline ring were observed at 10.65-10.89 ppm generally as broad bands, and 13C-NMR spectra of the compounds C=O were seen at 161.72-169.27 ppm. Interestingly, compounds 3o, 3p and 3r significantly shortened immobility time in the The forced swimming test (FST) and The tail suspension test (TST) at 50 mg/kg dose levels. In addition, compound 3r exhibited higher levels of efficacy than the reference standard fluoxetine but had no effect on locomotor activity in the open-field test. Compound 3r significantly increased serotonin and norepinephrine and the metabolite 5-hydroxyindoleacetic acid in mouse brain, suggesting that the effects of compound 3r may be mediated through these neurotransmitters. In the seizure screen, 15 compounds showed some degree against PTZ-induced seizure at a dose of 100 mg/kg, and the tested compounds did not show any neurotoxicity at a dose of 300 mg/kg in the rotarod test. © 2015 John Wiley & Sons A/S.

Wang Z.,Zhoushan Hospital of Zhejiang Province | Sun H.,Tongji University | Yakisich J.S.,Karolinska University Hospital
Anti-Cancer Agents in Medicinal Chemistry | Year: 2014

Treatment of brain tumors with chemotherapy is limited mostly because of delivery impediments related to the blood-brain barrier (BBB). For gliomas, the most common and aggressive primary brain tumor, treatment includes surgery, radiotherapy, and chemotherapy usually administered orally or intravenously. These routes do not deliver effective concentrations. To complicate matters, chemotherapy is usually a long treatment. Therefore, transient disruption of the BBB is likely insufficient to deliver effective intratumoral concentrations of anticancer drugs. This review briefly updates current strategies for overcoming the BBB with emphasis on their limitations and challenges intrinsic to the biology of cancer cells. © 2014 Bentham Science Publishers.

Le H.,Zhoushan Hospital of Zhejiang Province | Zeng F.,Chinese Academy of Sciences | Xu L.,Chinese Academy of Sciences | Liu X.,Chinese Academy of Sciences | Huang Y.,Chinese Academy of Sciences
Molecular Medicine Reports | Year: 2013

Cancer stem cells (CSCs) are a small population of undifferentiated cancer cells within tumors, which contribute to tumorigenicity and relapse. In the current study, CD133 (also termed prominin-1), a CSC marker, was investigated to determine its involvement in predicting carcinogenesis and prognosis in patients with non-small cell lung carcinoma (NSCLC). CD133-positive lung cancer cells were isolated to analyze self-renewal, differentiation and tumorigenic abilities in vitro and in vivo. Quantitative polymerase chain reaction was used to detect the expression of CD133 and three other CSC-associated markers, octamer-binding transcription factor 4 (OCT4A), Nanog homeobox (NANOG) and multidrug resistance protein 1 (MDR1), in primary NSCLC and adjacent non-cancer tissues. A series of statistical methods were used to analyze the correlation between mRNA expression levels, clinicopathological features and patient survival. The results showed that CD133-positive NSCLC cells demonstrated clonogenic, tumorigenic and drug-resistance properties compared with their CD133-negative counterparts or parental cells. In addition, compared with the adjacent normal lung tissue, the levels of CSC-associated biomarkers CD133, OCT4A, NANOG and MDR1 were significantly increased in NSCLC tissue. Elevated expression of CD133 was associated with stage, tumor size and differentiation of NSCLC; however, the cox hazard regression analysis showed no significant association between CD133 expression and overall patient survival. The present study supports the hypothesis that the stem cell population can be enriched in cells expressing the CD133 cell surface marker and that highly expressed CD133 is involved in the occurrence of NSCLC. However, CD133 may not be considered as an independent factor in predicting the prognosis of patients with NSCLC. Further studies are required to investigate the association between CD133 expression and overall patient survival.

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