Journal
JOURNAL OF CHEMICAL RESEARCH
Volume 44, Issue 9-10, Pages 586-591Publisher
SAGE PUBLICATIONS LTD
DOI: 10.1177/1747519820910390
Keywords
combination; (-)-epigallocatechin-3-gallate derivative; wild type of epidermal growth factor receptor; non-small-cell lung cancer; synthesis
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Funding
- National Nature Science Foundation of China [21602196, 31760226]
- Yunnan Provincial Science and Technology Department [2017ZF003, 2017FD084, 2017FG001046]
- National Key R&D Program of China [2016YFE0117700]
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Non-small-cell lung cancer is one of the principal causes of cancer-related death around the world. Chemotherapy is commonly used to treat wild type of epidermal growth factor receptor non-small-cell lung cancer. (-)-Epigallocatechin-3-gallate is the most abundant and active catechin. However, (-)-epigallocatechin-3-gallate has limited clinical application due to its poor stability and absorption. Herein, we report that a glycosylated azide undergoes a click reaction with the terminal alkyne of (-)-epigallocatechin-3-gallate to yield a triazole-linked glucose-(-)-epigallocatechin-3-gallate derivative and have evaluated its in vitro anticancer activity against human non-small-cell lung cancer cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The product inhibits human non-small-cell lung cancer cell lines with wild type of epidermal growth factor receptor and in combination with cisplatin/paclitaxel results in more pronounced proliferation inhibition than when used alone. Stability investigations indicates that the conjugated glucose residue can improve the stability of the (-)-epigallocatechin-3-gallate scaffold. Our studies suggest that the combination of the glucose-(-)-epigallocatechin-3-gallate derivative and chemotherapeutic drugs may provide a novel strategy for the treatment of non-small-cell lung cancer.
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