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Mol Nutr Food Res ; 50(4-5): 396-400, 2006 Apr.
Article in English | MEDLINE | ID: mdl-16598806

ABSTRACT

3,4,5-Tricaffeoylquinic acid (TCQA) that is not found in intact plant of lettuce leaves was isolated from the cultured cells. The intact plant produced chicoric acid (dicaffeoyl tartaric acid: L-CCA) as well as chlorogenic acid (3-caffeoylquinic acid: 3-CQA) as the major metabolites. After subculturing of the cells for 40 days, the amount of 3,4,5-TCQA reached to 0.14 mg/g fresh weight. The inhibitory effect of 3,4,5-TCQA for human immunodeficiency virus (HIV) Type 1 integrase was assayed. Anti-HIV activity using HIV and MT-2 cells was 1.15 microM and IC(50) against HIV integrase was 0.063 microM whereas cell toxicity of this chemical was expressed as 5% death of all living cells to be 18.4 microM. The HIV inhibitory effect of 3,4,5-TCQA was the highest in values among L-CCA, and other dicaffeoylquinic acids. This data will provide a new possibility for creating a new drug design for HIV.


Subject(s)
Anti-HIV Agents/pharmacology , Chlorogenic Acid/analogs & derivatives , HIV-1/drug effects , Lactuca/chemistry , Plant Leaves/chemistry , Plant Leaves/cytology , Caffeic Acids/metabolism , Cells, Cultured , Chlorogenic Acid/isolation & purification , Chlorogenic Acid/metabolism , Chlorogenic Acid/pharmacology , HIV Integrase/pharmacology , HIV-1/enzymology , Lactuca/metabolism , Quinic Acid/analogs & derivatives , Succinates/metabolism
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