3,5-Dicaffeoylquinic acid isolated from Artemisia argyi and its ester derivatives exert anti-leucyl-tRNA synthetase of Giardia lamblia (GlLeuRS) and potential anti-giardial effects.
An aqueous ethanol extract of Artemisia argyi inhibited the aminoacylation activity of LeuRS from Giardia lamblia (GlLeuRS). The bioassay-guided fractionation of the extract led to the isolation of 3,5-dicaffeoylquinic acid (1), with an IC₅₀ of 5.82 μg/mL. The ester derivatives of 1 were also found to possess strong anti-GlLeuRS effects, with IC₅₀ values of 1.79, 5.51 and 2.56 μg/mL respectively. Anti-giardial assay showed that the derivatives, especially 3,5-dicaffeoylquinic acid propyl ester (4) (IC₅₀=4.62 μg/mL), were effective at killing G. lamblia.
Shanghai Key Laboratory of Functional Materials Chemistry, and Research Center of Analysis and Test, East China University of Science and Technology, Shanghai 200237, PR China.
Yan-Hong
YH
Zhang
Mei-Qin
MQ
Xue
Yuan-Chao
YC
Bai
Hui-Hui
HH
Yuan
Hong-Li
HL
Zhao
Min-Bo
MB
Lan
D049148:Aminoacylation; D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D019306:Artemisia / Q000737:chemistry*; D002726:Chlorogenic Acid / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology; D016829:Giardia lamblia / Q000187:drug effects* / Q000235:genetics; D007935:Leucine-tRNA Ligase / Q000037:antagonists & inhibitors*; D021261:Parasitic Sensitivity Tests; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*
C577185:3,5-dicaffeoylquinic acid propyl ester; D000981:Antiprotozoal Agents; D010936:Plant Extracts; D002726:Chlorogenic Acid; D007935:Leucine-tRNA Ligase; C100434:3,5-dicaffeoylquinic acid