Synthesis and Evaluation of Curcumin-Related Compounds Containing Benzyl Piperidone for Their Effects on Human Cancer Cells
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- Zhou Dai-Ying
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology Guangdong Food and Drug Vocational College
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- Zhang Kun
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology
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- Conney Allan H.
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey
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- Ding Ning
- Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey
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- Cui Xiao-Xing
- Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey
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- Wang Hui
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology
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- Verano Michael
- Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey
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- Zhao Su-qing
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology
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- Fan Yan-Xiong
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology
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- Zheng Xi
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey
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- Du Zhi-Yun
- Allan H Conney Laboratory for Research, Institute of Natural Medicinal Chemistry & Green Chemistry, Guangdong University of Technology
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抄録
Eleven curcumin-related compounds containing a benzyl piperidone moiety were synthesized and evaluated for their effects on cultured prostate cancer PC-3 cells, pancreas cancer BxPC-3 cells, colon cancer HT-29 cells and lung cancer H1299 cells. Inhibitory effects of these compounds on the growth of PC-3, BxPC-3, HT-29 and H1299 cells were determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and trypan blue exclusion assay. Compounds benzyl piperidone 2 (P2), P4, P7, 4-bromo-2-fluoro-benzyl piperidone 2 (PFBr2), PFBr3 and PFBr4 (see syntheses and structures in Figs. 1, 2) exhibited potent inhibitory effects on the growth of cultured PC-3, BxPC-3, HT-29 and H1299 cells. The IC50 for these compounds was lower than 2 µM in all four cell lines. PFBr4 was 41-, 36-, 40- and 46-fold more active than curcumin for inhibiting the growth of PC-3, BxPC-3, HT-29 and H1299 cells, respectively. The benzyl piperidone-containing compounds studied also stimulated apoptosis in PC-3 cells. Mechanistic studies indicate that the effects of both curcumin and PFBr4 on PC-3 cells were associated with a decrease in phospho-Akt and phospho-extracellular signal-regulated kinase (Erk)1/2. The present study indicates that P2, P4, P7, PFBr2, PFBr3 and PFBr4 may have useful effects on human cancer cells.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 61 (11), 1149-1155, 2013
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679154635136
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- NII論文ID
- 130003360913
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- NII書誌ID
- AA00602100
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- COI
- 1:STN:280:DC%2BC3sbjtFOltA%3D%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 024957181
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- PubMed
- 23985704
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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- PubMed
- CiNii Articles
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- 使用不可