期刊
BIOORGANIC CHEMISTRY
卷 95, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.103530
关键词
Thioredoxin reductases (TrxRs); Xanthohumol (Xn); Hybrids; Fluorescence; Mitochondrial apoptosis; Cancer therapy
资金
- National Natural Science Foundation of China [81671682]
- Hospital fund of the First Affiliated Hospital of Zhengzhou University
The selenoprotein thioredoxin reductases (TrxRs) have been extensively studied as a potential target for the development of anticancer drugs. Herein, we designed, synthesized, and evaluated a series of coumarin-chalcone hybrids as TrxR inhibitors. Most of them exhibited enhancing anticancer activity than Xanthohumol (Xn). The representative Xn-2 (IC50 = 3.6 mu M) was a fluorescence agent, wherein drug uptake can be readily monitored in living cells by red fluorescence imaging. Xn-2 down-regulated the expression of TrxR, remarkedly induced ROS accumulation to activate mitochondrial apoptosis pathway. Furthermore, Xn-2 inhibited cancer cell metastasis and abolished the colony formation ability of cancer cells. Taken together, these results highlight that compound Xn-2 may be a promising theranostic TrxR inhibitor for human cancer therapy.
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