2. Academic Validation
  3. New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo

New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo

  • Eur J Med Chem. 2017 May 5:131:141-151. doi: 10.1016/j.ejmech.2017.03.006.
Min-Tsang Hsieh 1,  Ling-Chu Chang 2,  Hsin-Yi Hung 3,  Hui-Yi Lin 4,  Mei-Hui Shih 4,  Chang-Hai Tsai 5,  Sheng-Chu Kuo 6,  Kuo-Hsiung Lee 7
Affiliations

Affiliations

  • 1 Chinese Medicinal Research and Development Center, China Medical University and Hospital, Taichung 404, Taiwan; School of Pharmacy, China Medical University, Taichung 404, Taiwan.
  • 2 Chinese Medicinal Research and Development Center, China Medical University and Hospital, Taichung 404, Taiwan.
  • 3 School of Pharmacy, National Cheng Kung Hospital, College of Medicine, National Cheng Kung University, Tainan 701, Taiwan.
  • 4 School of Pharmacy, China Medical University, Taichung 404, Taiwan.
  • 5 China Medical University and Hospital, Taichung 404, Taiwan.
  • 6 Chinese Medicinal Research and Development Center, China Medical University and Hospital, Taichung 404, Taiwan; School of Pharmacy, China Medical University, Taichung 404, Taiwan. Electronic address: sckuo@mail.cmu.edu.tw.
  • 7 Chinese Medicinal Research and Development Center, China Medical University and Hospital, Taichung 404, Taiwan; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, United States. Electronic address: khlee@unc.edu.
PMID: 28319780 DOI: 10.1016/j.ejmech.2017.03.006
Abstract

Novel bis(hydroxymethyl) alkanoate curcuminoid derivatives were designed, synthesized and screened for in vitro antiproliferative and in vivo antitumor activity. Selected new compound 9a and curcumin were further evaluated for inhibitory activity against ER+/PR+ breast Cancer (MCF-7, T47D), HER 2+ breast Cancer (SKBR3, BT474, and MDA-MB-457) and triple negative breast Cancer (TNBC) (HS-578T, MDA-MB-157, and MDA-MB-468) cell lines. In addition, compound 9a was evaluated in the MDA-MB-231 xenograft nude mice model. Compound 9a exhibited greater inhibitory activity than curcumin against TNBC cells and also demonstrated significant inhibitory activity against doxorubicin-resistant MDA-MB-231 cells, with ten-fold higher potency than curcumin. Furthermore, when evaluated against the MDA-MB-231 xenograft nude mice model, compound 9a alone was ten-fold more potent than curcumin. Moreover, synergistic activity was observed when 9a was used in combination with doxorubicin against MDA-MB-231 breast Cancer cells.

Keywords

Antiproliferative agents; Antitumor agents; Bis(hydroxymethyl) alkanoate curcuminoids; Curcumin; Triple-negative breast cancer.

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