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  • P-ISSN 1010-0695
  • E-ISSN 2288-3339

Inhibition of cyclooxygenase and prostaglandin E2 synthesis by crude methanolic extract from Euonymus alatus (Thunb.) Sieb in SKBR3 human breast cancer cell line

Journal of Korean Medicine / Journal of Korean Medicine, (P)1010-0695; (E)2288-3339
2005, v.26 no.1, pp.37-45





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Abstract

In the present study, we examined the effect of crude methanolic extract (CME) from Euonymus alatus(Thunb.) Sieb on arachidonic acid (AA) cascade in SKBR3 human breast cancer cell line. CME had a potent inhibitory activity of prostaglandin E2 (PGE2) release induced by A23187, a Ca2+ ionophore. The inhibition was concentration-dependent, with the 50 value of about 5 M. CME had no inhibitory effect on A23187-induced phosphorylation of p42/p44 extracellular signal regulated kinase/mitogen-activated protein kinase or on the liberation of [14C]-AA from the cells labeled with [14C]-AA. However, CME concentration-dependently inhibited the conversion of AA to PGE2 in microsomal preparations, showing its possible inhibition of cyclooxygenase (COX). In enzyme assay in vitro, CME inhibited the activities of both constitutive COX (COX-1) and inducible COX (COX-2) in a concentration-dependent manner, with the 50 values of about 0.8 and 2 M, respectively. Lineweaver-Burk plot analysis indicated that CME competitively inhibited the activities of both COX-1 and -2. This study is a first demonstration that CME directly inhibits COX activity.

keywords
CME Cyclooxygenase, PGE2, SKBR3 human breast cancer cell line., CME Cyclooxygenase, PGE2, SKBR3 human breast cancer cell line.


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