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Molecules 2016, 21(5), 620;

Synthesis and Biological Testing of Novel Glucosylated Epigallocatechin Gallate (EGCG) Derivatives

1,2,3,* , 1,2,3,5,* and 1,2,5,*
Key Laboratory of Pu-er Tea Science, Ministry of Education, Yunnan Agricultural University, Kunming 650201, China
Tea Research Center of Yunnan, Kunming 650201, China
Pu-er Tea Academy, Yunnan Agricultural University, Kunming 650201, China
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China
State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan, Kunming 650201, China
Authors to whom correspondence should be addressed.
Academic Editors: Jean Jacques Vanden Eynde, Annie Mayence and Tien L. Huang
Received: 10 March 2016 / Revised: 2 May 2016 / Accepted: 4 May 2016 / Published: 11 May 2016
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Epigallocatechin gallate (EGCG) is the most abundant component of green tea catechins and has strong physiological activities. In this study, two novel EGCG glycosides (EGCG-G1 and EGCG-G2) were chemoselectively synthesized by a chemical modification strategy. Each of these EGCG glycosides underwent structure identification, and the structures were assigned as follows: epigallocatechin gallate-4′′-O-β-d-glucopyranoside (EGCG-G1, 2) and epigallocatechin gallate-4′,4′′-O-β-d-gluco-pyranoside (EGCG-G2, 3). The EGCG glycosides were evaluated for their anticancer activity in vitro against two human breast cell lines (MCF-7 and MDA-MB-231) using MTT assays. The inhibition rate of EGCG glycosides (EGCG-G1 and EGCG-G2) is not obvious. The EGCG glycosides are more stable than EGCG in aqueous solutions, but exhibited decreasing antioxidant activity in the DPPH radical-scavenging assay (EGCG > EGCG-G2 > EGCG-G1). Additionally, the EGCG glycosides exhibited increased water solubility: EGCG-G2 and EGCG-G1 were 15 and 31 times as soluble EGCG, respectively. The EGCG glycosides appear to be useful, and further studies regarding their biological activity are in progress. View Full-Text
Keywords: epigallocatechin gallate (EGCG); glycosides; anticancer activity; DPPH; synthesis epigallocatechin gallate (EGCG); glycosides; anticancer activity; DPPH; synthesis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Zhang, X.; Wang, J.; Hu, J.-M.; Huang, Y.-W.; Wu, X.-Y.; Zi, C.-T.; Wang, X.-J.; Sheng, J. Synthesis and Biological Testing of Novel Glucosylated Epigallocatechin Gallate (EGCG) Derivatives. Molecules 2016, 21, 620.

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