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Cytotoxicity of oleanolic and ursolic acid derivatives toward hepatocellular carcinoma and evaluation of NF-κB involvement.

Abstract：

:Oleanolic and ursolic acids are two ubiquitous isomeric triterpene phytochemicals known for their anticancer activity. A set of derivatives of the two compounds with a modified oxidation state and lipophylicity at C-3 and C-28 positions, were prepared and tested as anticancer agents versus the lines HepG2, Hep3B and HA22T/VGH of hepatocarcinoma, a strongly aggressive tumor that is not responsive toward the standard therapies. New derivatives containing a three carbons side chain on the C-3 position were synthetized in both stereoisomeric forms by the Barbier-Grignard procedure and three of them were found to be active toward all of the three targets. The implication of the transcriptional nuclear factor NF-κB in the mechanism of action was assessed for the more active compounds in the set, as hepatocellular carcinoma (HCC) cyto-types are known to overexpress NF-κB.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Fontana G,Bruno M,Notarbartolo M,Labbozzetta M,Poma P,Spinella A,Rosselli S

doi

10.1016/j.bioorg.2019.103054

subject

Has Abstract

pub_date

2019-09-01 00:00:00

pages

103054

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30275-5

journal_volume

90

pub_type

杂志文章

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