A novel synthetic ursolic acid derivative inhibits growth and induces apoptosis in breast cancer cell lines

Li,Wei; Zhang,Hongxiu; Nie,Mingxiu; Wang,Wei; Liu,Zongtao; Chen,Ceshi; Chen,Haijun; Liu,Rong; Baloch,Zulqarnain; Ma,Ke

doi:10.3892/ol.2017.7578

A novel synthetic ursolic acid derivative inhibits growth and induces apoptosis in breast cancer cell lines

Authors:
- Wei Li
- Hongxiu Zhang
- Mingxiu Nie
- Wei Wang
- Zongtao Liu
- Ceshi Chen
- Haijun Chen
- Rong Liu
- Zulqarnain Baloch
- Ke Ma
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Affiliations: Department of Urology, The First People's Hospital of Yunnan Province, Kunming, Yunnan 650032, P.R. China, College of Pharmacy, Qingdao University, Qingdao, Shandong 266021, P.R. China, Key Laboratory of Animal Models and Human Disease Mechanisms of Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, P.R. China, College of Chemistry, Fuzhou University, Fuzhou, Fujian 350116, P.R. China, Medical College of Kunming University of Science and Technology, Kunming, Yunnan 650500, P.R. China, College of Traditional Chinese Medicine, Shandong University of Traditional Chinese Medicine, Jinan, Shandong 250355, P.R. China
Published online on: December 11, 2017 https://doi.org/10.3892/ol.2017.7578
Pages: 2323-2329
Copyright: © Li et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

The present study investigated the anticancer functions of ursolic acid (UA) and its novel derivatives, with a nitrogen‑containing heterocyclic scaffold and the privileged fragment at the C‑28 position on apoptosis induction, cell proliferation and cell cycle in human BC lines. UA was chemically modified in the present study to increase its antitumor activity and bioavailability. A novel UA derivative, FZU3010, was synthesized using a nitrogen‑containing heterocyclic scaffold and a privileged fragment at the C‑28 position. Sulforhodimine B assays were used to measure the effect of UA and different concentrations of FZU3010 on the viability of breast cancer (BC) SUM149PT and HCC1937 cells. FZU3010 significantly repressed the proliferation of the two cancer cell lines in a dose‑dependent manner, with a half‑maximal inhibitory concentration of 4‑6 µM, and exhibited decreased cytotoxicity compared with vehicle‑treated cell lines. The effect of FZU3010 on cell cycle distribution and cellular apoptosis was also investigated. The results of this investigation indicated that FZU3010 significantly increased the number of SUM149PT and breast cancer HCC1937 cells in the G0/G1 phase in a dose‑dependent manner. Additionally, at a concentration of 5 µM, the capability of FZU3010 to induce BC apoptosis was significantly higher than the capability of UA. Thus, the results of the current study indicated that FZU3010 induced apoptosis in BC cells, together with induction of cell cycle arrest at the S and G0/G1 phase. FZU3010 may therefore be considered as a potential therapeutic agent for the treatment of BC.

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