Ursolic acid derivative FZU-03,010 inhibits STAT3 and induces cell cycle arrest and apoptosis in renal and breast cancer cells | Zendy

Wei Li | Zendy; Hongxiu Zhang | Zendy; Mingxiu Nie | Zendy; Yanlei Tian | Zendy; Xu Chen | Zendy; Ceshi Chen | Zendy; Haijun Chen | Zendy; Rong Liu | Zendy

Open Access

Ursolic acid derivative FZU-03,010 inhibits STAT3 and induces cell cycle arrest and apoptosis in renal and breast cancer cells

Author(s) -

Wei Li,

Hongxiu Zhang,

Mingxiu Nie,

Yanlei Tian,

Xu Chen,

Ceshi Chen,

Haijun Chen,

Rong Liu

Publication year - 2017

Publication title -

acta biochimica et biophysica sinica

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.771

H-Index - 57

eISSN - 1745-7270

pISSN - 1672-9145

DOI - 10.1093/abbs/gmx012

Subject(s) - cancer research , ursolic acid , apoptosis , cell cycle , cell cycle checkpoint , cell , stat protein , cancer , g1 phase , clear cell renal cell carcinoma , breast cancer , chemistry , viability assay , cancer cell , renal cell carcinoma , medicine , stat3 , biochemistry , chromatography

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.

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