Jiangsu Key Laboratory of Carcinogenesis and Intervention

Nanjing, China

Jiangsu Key Laboratory of Carcinogenesis and Intervention

Nanjing, China
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Gao Y.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Zhao Y.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Yao J.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Wang Y.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | And 2 more authors.
Journal of China Pharmaceutical University | Year: 2014

To investigate the anti-metastasis effect of wogonin on human alveolar adenocarcinoma cell A549 induced by IL-6 and its potential mechanism, the growth inhibition effect of wogonin by MTT assay and the anti- metastasis effect of wogonin by transwell invasion assay were investigated. The immunofluorescence and Real-time PCR assay were employed to observe wogonin regulating metastasis marker protein E-cadherin, N-cadherin, Vimentin protein and mRNA level expression. Snail and Twist mRNA level expression and transcription factors of metastasis were also detected. In order to explore the potential mechanism of wogonin, PcDNA3. 1 -Flag-STAT3 was transfected into A549 to detect metastasis marker protein mRNA level expression. Data showed that wogonin inhibited A549 cell invasion and metastasis, and regulated metastasis-related transcription factors and metastasis marker protein expression in a dose-dependent manner. In conclusion, all these results showed that wogonin can suppress A549 cells invasion andmetastasis induced by IL-6. It is possible that wogonin inhibits A549 cell inva sion and metastasis by regulating the activity of transcription factor Snail and Twist.


Jiang C.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Yang L.,China Pharmaceutical University | Wu W.-T.,China Pharmaceutical University | Guo Q.-L.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | You Q.-D.,Jiangsu Key Laboratory of Carcinogenesis and Intervention
Journal of Pharmacy and Pharmacology | Year: 2011

Objectives This study investigated the antiproliferative and apoptotic activities of CPUYJ039, a newly synthesized benzimidazole-based kinesin spindle protein (KSP) inhibitor, on HCT116 cell lines. Methods KSP-inhibitory activity was tested using the malachite-green method. The in-vitro cell proliferation inhibitory activity of the sample was measured using WST reagent. Flow-cytometric evaluation of cellular DNA content was performed. Apoptotic cells were quantified by annexin V-FITC-PI double staining. To confirm that the cytotoxic activity was a consequence of KSP inhibition, microtubule morphology and DNA segregation were observed by double staining of microtubules and DNA. The expression of Bcl-2 and Bax in CPUYJ039-treated HCT116 cells was detected by Western blotting. Key findings CPUYJ039 was evaluated and proved to have potent inhibitory activities in the KSP ATPase and HCT116 cell proliferation assays. CPUYJ039 inhibited the proliferation of HCT116 cells in a dose- and time-dependent manner and markedly induced G2/M phase cell-cycle arrest with characteristic monoastral spindles and subsequent cell death in HCT116 cells, which was associated with an increase of the Bax/Bcl-2 ratio. Conclusions These results suggest that CPUYJ039 may be a novel inducer of apoptosis in HCT116 cells with potent KSP inhibitory activity. © 2011 Royal Pharmaceutical Society.


Yang J.,Vanderbilt University | Feng F.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Guo Q.-L.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Guo Q.-L.,State Key Laboratory of Natural Medicines | And 3 more authors.
Zhongguo Zhongyao Zazhi | Year: 2013

Gamboge, the resin of Garcinia hanburyi has had a long history of use as the traditional dye as well as a complementary and alternative medicine. The antitumor activities of gamboge have been well demonstrated by inhibiting the growth and progression of cancer cells both in vitro and in vivo. In order to further clarify the mode of action of gamboge, there are three key questions needed to be answered, including what's in gamboge? How do the chemical components from gamboge work on cancer cells? How do biological systems work on the chemical components from gamboge after administration? In this review, we summarize the explorations of the answers toward these questions according to the recent progress in both of chemistry and biology research of gamboge. In addition, the implication in the future research and discovery of the caged G. xanthones as anticancer agents is also discussed.


Jiang C.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Jiang C.,China Pharmaceutical University | Zhang X.,Jiangsu Key Laboratory of Carcinogenesis and Intervention | Zhang X.,China Pharmaceutical University | And 4 more authors.
Progress in Chemistry | Year: 2010

Inhibition of kinesin spindle protein (KSP) represents a novel and specific mechanism to target the mitotic spindle that may be devoid of the neuropathy-associated side effects common to the agents that target microtubules. Since the discovery of monastrol, the first selective small molecular inhibitor of KSP, many types of KSP inhibitors have been reported. In this review we describe the development of different types of KSP inhibitors. The structures and functions of KSP and the use of which as a novel target in the research of anticancer agents are introduced. The structure-activity relationship of some KSP inhibitors and the perspective of the study on KSP inhibitors are also discussed.


PubMed | Jiangsu Key Laboratory of Carcinogenesis and Intervention
Type: Journal Article | Journal: The Journal of pharmacy and pharmacology | Year: 2011

This study investigated the antiproliferative and apoptotic activities of CPUYJ039, a newly synthesized benzimidazole-based kinesin spindle protein (KSP) inhibitor, on HCT116 cell lines.KSP-inhibitory activity was tested using the malachite-green method. The in-vitro cell proliferation inhibitory activity of the sample was measured using WST reagent. Flow-cytometric evaluation of cellular DNA content was performed. Apoptotic cells were quantified by annexin V-FITC-PI double staining. To confirm that the cytotoxic activity was a consequence of KSP inhibition, microtubule morphology and DNA segregation were observed by double staining of microtubules and DNA. The expression of Bcl-2 and Bax in CPUYJ039-treated HCT116 cells was detected by Western blotting.CPUYJ039 was evaluated and proved to have potent inhibitory activities in the KSP ATPase and HCT116 cell proliferation assays. CPUYJ039 inhibited the proliferation of HCT116 cells in a dose- and time-dependent manner and markedly induced G2/M phase cell-cycle arrest with characteristic monoastral spindles and subsequent cell death in HCT116 cells, which was associated with an increase of the Bax/Bcl-2 ratio.These results suggest that CPUYJ039 may be a novel inducer of apoptosis in HCT116 cells with potent KSP inhibitory activity.

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