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Synthesis and inhibitory effect of guaianolide Dehydrozaluzanin C on human bladder cancer T24 cells(PDF)

Chinese Journal of Applied & Environmental Biology[ISSN:1006-687X/CN:51-1482/Q]

2016 06
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Synthesis and inhibitory effect of guaianolide Dehydrozaluzanin C on human bladder cancer T24 cells
CHEN Yuwen1 2 MA Yuling2 ZENG Zhongqiu2 LI Wenhua2 LI Suiyan1** & TANG Yaxiong2**
1School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China 2Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China
Dehydrozaluzanin C synthesis bladder cancer T24 cells proliferation apoptosis PARP
Q949.329.810.6 : R965

Sesquiterpenoid lactones such as artemisinin from natural products have an important pharmaceutical potential. Dehydrozaluzanin C, a kind of guaianolide sesquiterpenoid lactone, is originally isolated from medicinal plants like A insliaea DC. However, the extremely low content in those plants limits its further development and utilization. So far the anti-cancer activity of Dehydrozaluzanin C remains largely unknown. In this study, Dehydrozaluzanin C was synthesized by a rapid and efficient method, and the anti-proliferative and apoptotic effects on human bladder cancer T24 cells were further investigated. Firstly, Dehydrozaluzanin C was synthesized beginning with dehydrocostuslactone in two steps including allylic and Dess-Martin oxidation, and the total yield was 73%. Furthermore, MTT assays showed that Dehydrozaluzanin C significantly inhibited the proliferation of bladder cancer T24 cells in a dose-dependent manner. Moreover, DAPI staining demonstrated that Dehydrozaluzanin C significantly induced the apoptosis of bladder cancer T24 cells. Mechanistically, western blot analysis further confirmed that the apoptotic effect of Dehydrozaluzanin C was associated with activation of the cleavage of PARP, leading to the apoptotic effect of T24 cells. Taken together, these findings suggest that guaianolide Dehydrozaluzanin C may be a promising lead compound for prevention and treatment of bladder cancer.


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Last Update: 2016-12-30