Dual inhibition of cyclooxygenase-1 and 5-lipoxygenase by aerial part of Bupleurum fruticescens methanol extract.
The effect of the methanol extract from aerial parts of Bupleurum fruticescens on the release of eicosanoids and hydrolytic enzymes was determined on in vitro cell systems. The extract had a significant effect on 5-lipoxygenase (5-LOX) activity, inhibiting both LTB4 and 5(S)-HETE production with IC50 values of 112 microg/ml and 95 microg/ml, respectively. At concentrations of 200 microg/ml, the extract also inhibited cyclooxygenase-1 (90%) and elastase activities (54%). The 12-LOX activity in intact platelets was not affected; a fact, which suggests that phospholipase A2 (PLA2) activity, is not modified by the extract.
Prieto
J M
JM
Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Avenida Vicent Andrés Estellés, s/n. 46100 Burjassot, Valencia, Spain.
Giner
R M
RM
Recio
M C
MC
Máñez
S
S
Ríos
J L
JL
D000818:Animals; D029972:Bupleurum; D051545:Cyclooxygenase 1; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D035264:Flowers; D006801:Humans; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D008084:Lipoxygenase / Q000187:drug effects*; D008565:Membrane Proteins; D008517:Phytotherapy; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018517:Plant Roots; D011451:Prostaglandin-Endoperoxide Synthases; D051381:Rats; D017208:Rats, Wistar
C051274:Bupleurum root extract; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D010936:Plant Extracts; D008084:Lipoxygenase; D051545:Cyclooxygenase 1; C496511:PTGS1 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; C496513:Ptgs1 protein, rat; D019272:Leukocyte Elastase