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Antiproliferative and apoptotic effects of the oxidative dimerization product of methyl caffeate on human breast cancer cells.

Abstract：

:Caffeic acid derivatives are increasingly regarded as potential oncoprotective that could inhibit both the initiation and progression of cancer. Here we have synthesized seven 1-arylnaphthalene lignans and related compounds and tested their impact on breast cancer cell growth in tissue culture. The product of the oxidative dimerization of methyl caffeate, 1-phenylnaphthalene lignan, was found to induce a strong decrease in breast cancer cell number (IC(50) ~1 μM) and was selected for further investigation. Flow cytometry analysis revealed a decrease in cell proliferation and an increase in apoptosis in both MCF-7 and MDA-MB-231 breast cancer cell lines that are representative of the two main categories of breast tumors. The 3,4-dihydroxyphenyl group probably induced the biological activity, as the control compounds lacking it had no effect on breast cancer cells. Together, our data indicate that the oxidative dimerization product of methyl caffeate can inhibit breast cancer cell growth at a concentration adequate for pharmacological use.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Bailly F,Toillon RA,Tomavo O,Jouy N,Hondermarck H,Cotelle P

doi

10.1016/j.bmcl.2012.11.009

subject

Has Abstract

pub_date

2013-01-15 00:00:00

pages

574-8

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01452-7

journal_volume

23

pub_type

杂志文章

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