Protective effects of epigallocatechin gallate (EGCG) derivatives on azoxymethane-induced colonic carcinogenesis in mice

TY - JOUR

T1 - Protective effects of epigallocatechin gallate (EGCG) derivatives on azoxymethane-induced colonic carcinogenesis in mice

AU - Zhong, Ying

AU - Chiou, Yi Siou

AU - Pan, Min Hsiung

AU - Ho, Chi Tang

AU - Shahidi, Fereidoon

N1 - Funding Information: One of us (F.S.) thanks the Natural Science and Engineering Research Council (NSERC) of Canada for financial support. Support from AFMNet (Advanced Foods and Materials Network) is also acknowledged.

PY - 2012/1

Y1 - 2012/1

N2 - Epigallocatechin gallate (EGCG), the major polyphenol in green tea and a functional food ingredient/nutraceutical with health-promoting properties, was structurally modified by esterification with butyric and docosahexaenoic (DHA) acid in order to improve its lipophilicity and hence bioefficacy in vivo. The lipophilic derivatives of EGCG so-prepared were evaluated for their anticancer activity against azoxymethane (AOM)-induced colon carcinogenesis in mice. Formation of colonic aberrant crypt foci (ACF) was monitored as the biomarker of colorectal cancer (CRC). It was found that oral administration of EGCG derivatives led to reduced size of ACF in the mouse colon. EGCG-DHA esters were more effective than EGCG-butyrate in inhibiting the formation of ACF. The total number of large colonic ACF was remarkably decreased by treatment with EGCG derivatives, especially by the EGCG-DHA esters, which showed a 100% inhibition of large ACF formation. Two tumor-promoting enzymes, iNOS and COX-2 were also inhibited by EGCG derivatives to various extents at the expression level. The results suggest that the lipophilic ester derivatives of EGCG are effective in inhibiting colon carcinogenesis and may be good candidates for colon cancer prevention/treatment.

AB - Epigallocatechin gallate (EGCG), the major polyphenol in green tea and a functional food ingredient/nutraceutical with health-promoting properties, was structurally modified by esterification with butyric and docosahexaenoic (DHA) acid in order to improve its lipophilicity and hence bioefficacy in vivo. The lipophilic derivatives of EGCG so-prepared were evaluated for their anticancer activity against azoxymethane (AOM)-induced colon carcinogenesis in mice. Formation of colonic aberrant crypt foci (ACF) was monitored as the biomarker of colorectal cancer (CRC). It was found that oral administration of EGCG derivatives led to reduced size of ACF in the mouse colon. EGCG-DHA esters were more effective than EGCG-butyrate in inhibiting the formation of ACF. The total number of large colonic ACF was remarkably decreased by treatment with EGCG derivatives, especially by the EGCG-DHA esters, which showed a 100% inhibition of large ACF formation. Two tumor-promoting enzymes, iNOS and COX-2 were also inhibited by EGCG derivatives to various extents at the expression level. The results suggest that the lipophilic ester derivatives of EGCG are effective in inhibiting colon carcinogenesis and may be good candidates for colon cancer prevention/treatment.

KW - Aberrant crypt foci (ACF)

KW - COX-2

KW - Colon cancer

KW - EGCG ester

KW - INOS

UR - http://www.scopus.com/inward/record.url?scp=84857690392&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84857690392&partnerID=8YFLogxK

U2 - 10.1016/j.jff.2011.12.011

DO - 10.1016/j.jff.2011.12.011

M3 - Article

SN - 1756-4646

VL - 4

SP - 323

EP - 330

JO - Journal of Functional Foods

JF - Journal of Functional Foods

IS - 1

ER -