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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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