Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (9): 600-607.DOI: 10.5246/jcps.2018.09.061

• Original articles • Previous Articles     Next Articles

A novel aza-naphthoquinone inhibits tumor growth by inducing apoptosis

Li Lei, Yu Chen, Simin Yang, Xiangbao Meng, Siwang Yu*   

  1. State Key Laboratory of Natural and Biomimetic Drugs; Department of Molecular and Cellular Pharmacology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2018-06-05 Revised:2018-07-11 Online:2018-09-29 Published:2018-08-12
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  • Supported by:

    National Natural Science Foundation of China (Grant No. 81472657 and 81273370).


Natural product menaquinone has been reported to exhibit antitumor activity mediated by inhibiting IDO-1 enzyme, and naphthoquinone compounds like pyranaphthoquinone have attracted extensive research interests since they share the naphthoquinone pharmacophores. In the present study, a novel series of aza-naphthoquinones was synthesized based on 6,7-dichloroquinoline-5,8-dione structure, and their cytotoxicities were screened using lung cancer cells. Among them CY-26-11was identified as the most potent one. CY-26-11 concentration-dependently induced apoptosis in A549 human lung adenocarcinomacells, as indicated by annexin-V staining. Further experimental data show that CY-26-11 down-regulated Bcl-2 while up-regulatedBax and Puma protein levels, and activated caspase-3. Finally, CY-26-11 significantly inhibited the growth of Lewis lung carcinomaxenografts in vivo without significant major toxicities. Taken together, our results demonstrate that CY-26-11 exhibited IDO-1-independent anti-tumor effects both in vitro and in vivo, providing a new anti-tumor mechanism for naphthoquinonecompounds.

Key words: Naphthoquinone, CY-26-11, Apoptosis, Anti-tumor activity

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