Vol 49 No. 4: 367-373 [PDF] [Full Text]
Ursolic acid derivative FZU-03,010 inhibits STAT3 and induces cell cycle arrest and apoptosis in renal and breast cancer cells
Wei Li1,2,†, Hongxiu Zhang1,2,†, Mingxiu Nie1,2, Yanlei Tian1,3, Xu Chen1,2, Ceshi Chen4, Haijun Chen5,*, and Rong Liu4,*

1Department of Urology of the First People’s Hospital of Yunnan Province, Kunming 650032, China,
2Medical College of Kunming University of Science and Technology, Kunming 650032, China,
3Yunnan University of Traditional Chinese Medicine, Kunming 650032, China,
4Key Laboratory of Animal Models and Human Disease Mechanisms of Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China, and
5College of Chemistry, Fuzhou University, Fuzhou 350116, China
These authors contributed equally to this work.

Abstract  Advanced renal cell carcinoma and triple negative breast cancer (TNBC) are malignancies without effective therapeutics currently. Ursolic acid (UA) has been previously reported to have anti-cancer effects in multiple solid tumors. In order to develop more potent anti-cancer reagents, FZU-03,010 based on the chemical structure of UA were synthesized. The results demonstrated that, compared with UA, FZU-03,010 could suppress renal cancer cell 786-0 and TNBC cell HCC1806 cell viability more potently. Furthermore, FZU-03,010 could induce G1 cell cycle arrest and cell apoptosis more efficiently than UA. FZU-03,010 could also inhibit signal transducer and activator of transcription 3 activation, induce the expression of cell cycle-dependent kinase inhibitors (p21 and p27) and promote cell apoptosis. In conclusion, our results suggest that the UA derivative FZU-03,010 is more potent in inhibiting cancer cell survival, and FZU-03,010 has the potential to be developed as a therapeutic for renal cell cancers and TNBCs.


Keywords   renal cell carcinoma, triple negative breast cancer, ursolic acid, FZU-03,010, STAT3


Received   2016-11-14  


Funding  This work was supported by the grants from the National Natural Science Foundation of China (Nos. 81272930 and 81322038 to R.L.), West Light Foundation of the Chinese Academy of Sciences (to R.L.), Youth Innovation Promotion Association, Chinese Academy of Sciences (to R.L.), the Yunnan Applied Basic Research Key Projects (No. 2015FA027 to R.L.), and Diagnosis, Treatment and Transformation Engineering Technology Research Center for Renal Cell Carcinoma of Yunnan Province (to W.L.) .


* Correspondence address  Tel/Fax: +86-871-65181945; E-mail: liurong@mail.kiz.ac.cn (R.L.)/Tel/Fax: +86-591-83779326; E-mail: chenhaij@gmail.com (H.C.)

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