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Syntheses of diacyltanshinol derivatives and their suppressive effects on macrophage foam cell formation by reducing oxidized LDL uptake.

Abstract：

:A series of diacyltanshinol derivatives were synthesized by esterifying the corresponding o-hydroquinones of tanshinones. The suppressive effects of the synthesized compounds on oxidized low-density lipoprotein (oxLDL) uptake and oxLDL-induced macrophage-derived foam cell formation were evaluated. Our results indicated that the nicotinate derivatives 1a and 2a, modified from tanshinone IIA and cryptotanshinone, showed stronger suppressive activity on oxLDL uptake and the resultant foam cell formation relative to tanshinone IIA. Western Blot analysis indicated that derivatives 1a and 2a could dose-dependently inhibit the expression of oxLDL-induced LOX-1, implying that the suppressive effects of 1a and 2a on oxLDL uptake and foam cell formation could be at least partially attributed to the inhibition of LOX-1 expression in macrophages.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Cheng X,Zhang DL,Li XB,Ye JT,Shi L,Huang ZS,Gu LQ,An LK

doi

10.1016/j.bioorg.2013.11.001

subject

Has Abstract

pub_date

2014-02-01 00:00:00

pages

24-30

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(13)00071-0

journal_volume

52

pub_type

杂志文章

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