DISCOVERY AND UTILIZATION OF BIOACTIVE COMPONENTS FROM NEW CROPS AND AGRICULTURAL CO-PRODUCTS
Location: Functional Foods Research Unit
Title: Dicaffeoylquinic acids in Yerba mate (Ilex paraguariensis St. Hilaire) inhibit NF-kB nucleus translocation in macrophages and induce apoptosis by activating caspases-8 and -3 in human colon cancer cells
Submitted to: Molecular Nutrition and Food Research
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: April 12, 2011
Publication Date: June 8, 2011
Citation: Puangpraphant, S., Berhow, M.A., Vermillion, K., Potts, G., Gonzalez De Mejia, E. 2011. Dicaffeoylquinic acids in Yerba mate (Ilex paraguariensis St. Hilaire) inhibit NF-kB nucleus translocation in macrophages and induce apoptosis by activating caspases-8 and -3 in human colon cancer cells. Molecular Nutrition and Food Research. 55:1509-1522.
Interpretive Summary: Yerba mate is a popular South American tea drink prepared from mate leaves. The extracts contain several natural products which have yet to be characterized for their health benefits. One group of compounds are the various caffoylquinic acid esters which are commonly found in many plants. As part of an ongoing assessment of the compounds in mate, these compounds were isolated and characterized and assessed for their biological activities. The dicaffeoylquinic acid esters from Yerba mate were shown to process anti-inflammatory activity and activity against colon cancer cell growth. These compounds could be potential anti-cancer agents in colon cancertherapy.
Caffeoylquinic acid derivatives (CQAs) are widely distributed in plants including Yerba mate (Ilex paraguariensis). However, isolation of these isomers in Yerba mate and their anti-inflammatory and anti-colon cancer effects has not been studied. The objectives of this study were to isolate and purify di-CQAs from Yerba mate leaves and assess their anti-inflammatory and anti-cancer capabilities. Methanol extracts of dried mate leaves were resolved by flash chromatography and further purified using preparative HPLC, resulting in the isolation of a fraction containing 3,4- and 3,5-diCQAs and a fraction containing 4,5-diCQA. Two purified fractions were assessed for their anti-inflammatory effects on RAW 264.7 macrophages and anti-cancer on HT-29 and RKO colon cancer cell lines. Both fractions (1-200 µM) inhibited LPS-induced inflammation by suppressing NO/iNOS and PGE2/COX-2 pathways through inhibiting nucleus translocation of NF-'B subunits, p50 and p65. The diCQA fractions inhibited HT-29 and RKO cells proliferation by inducing apoptosis in time- and concentration-dependent manner, but did not affect the protein levels of p21, p27, p53, and Bax:Bcl-2 ratio in RKO cells. In HT-29 cells, however, the diCQA fractions increased Bax:Bcl-2 ratio. Western-blot analyses of total cell lysates revealed the diCQA fractions increased the activation of caspase-8 leading to cleavage of caspase-3 in both RKO and HT-29 colon cancer cells. DiCQAs from Yerba mate process anti-inflammatory activity and activity against colon cancer cell growth. These diCQAs could be potential anti-cancer agents in colon cancer therapy.