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J Agric Food Chem. 2016 Sep 21;64(37):7002-13. doi: 10.1021/acs.jafc.6b02509. Epub 2016 Sep 9.

Repression of Human Hepatocellular Carcinoma Growth by Regulating Met/EGFR/VEGFR-Akt/NF-κB Pathways with Theanine and Its Derivative, (R)-2-(6,8-Dibromo-2-oxo-2H-chromene-3-carboxamido)-5-(ethylamino)-5-oxopentanoic Ethyl Ester (DTBrC).

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School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University , Yantai, 264005, People's Republic of China.
Key Laboratory of Tea Biochemistry & Biotechnology, Ministry of Agriculture, Anhui Agricultural University , Hefei, Anhui Province 230036, People's Republic of China.
Shandong Yingdong Yinghao Biotechnology Inc. , No. 101 Hangtianlu, Gaoxinqu, Yantai, Shandong Province 264670, People's Republic of China.


To explore the potential of theanine against cancer, we have studied the anticancer activities of theanine from tea and its semisynthesized derivative, (R)-2-(6,8-dibromo-2-oxo-2H-chromene-3-carboxamido)-5-(ethylamino)-5-oxopentanoic ethyl ester (DTBrC), in in vitro, ex vivo, and in vivo models of human hepatocellular carcinoma (HHC). Theanine and DTBrC displayed inhibitory effects on the growth and migration of HHC cells in vitro, ex vivo, and in vivo. Theanine and DTBrC significantly enhanced the repression of HHC cell growth in combination with anticancer drug pirarubicin. Theanine and DTBrC completely suppressed HGF- and EGF+HGF-induced migration with a reduction of p53 tumor suppressor level and enhanced the p53 protein expression in HHC cells. The Akt and NF-κB knockdown greatly reduced cancer cell migration with a decrease in CD44 expression. DTBrC and theanine significantly repressed the protein expressions in the Met/EGFR/VEGFR-Akt/NF-κB pathways, which might be the mechanism for their biologic effects.


DTBrC; human hepatocellular carcinoma; inhibition; signaling pathways; theanine

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