HPLC based activity profiling for 5-lipoxygenase inhibitory activity in Isatis tinctoria leaf extracts.
In the pursuit of the anti-inflammatory constituents in lipophilic woad extracts, the 5-lipoxygenase (5-LOX) inhibitory activity was investigated by HPLC-based activity profiling. In a low-resolution profiling, two time windows with peaks of activity were found. The first coincided with tryptanthrin, a known dual inhibitor of cyclooxygenase-2 (COX-2) and 5-LOX, whereas the major inhibitory fraction was towards the end of the HPLC run. The active fractions were profiled in a peak-resolved manner, and the compounds analyzed by LC-MS, GC and TLC. The activity in the lipophilic fractions of the Isatis extract could be linked to an unsaturated fatty acid, alpha-linolenic acid.
Oberthür
C
C
Institute of Pharmacy, Friedrich-Schiller-University Jena, Semmelweisstrasse 10, D-07741 Jena, Germany.
Jäggi
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R
Hamburger
M
M
D002851:Chromatography, High Pressure Liquid; D018922:HL-60 Cells; D006801:Humans; D031219:Isatis / Q000737:chemistry*; D016859:Lipoxygenase Inhibitors; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry*; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*; D017962:alpha-Linolenic Acid / Q000737:chemistry
D016859:Lipoxygenase Inhibitors; D010936:Plant Extracts; D011799:Quinazolines; D017962:alpha-Linolenic Acid; C046243:tryptanthrine