Sesquiterpenoids from the roots of Inula helenium inhibit acute myelogenous leukemia progenitor cells.

Abstract:

:One new eudesmane sesquiterpenoid, 11β-hydroxy-13-chloro-eudesm-5-en-12, 8-olide (1), was isolated from the roots of Inula helenium together with nine eudesmanolides (2-10) and one germacranolide (11). Their structures were elucidated on the basis of detailed spectroscopic analyses. All isolates were evaluated for their antiproliferative activities against human leukemia stem-like cell line KG1a. Compound 10 exhibited the most potent effect with the IC50 value of 3.36 ± 0.18 μM. A further investigation revealed that compound 10 could significantly induce apoptosis of KG1a cells. Additionally, compound 10 had an obvious effect on the levels of apoptosis-related proteins (Bcl-2, Bax, cytochrome c, caspase 9 and caspase 3), indicating that the antiproliferative effect of compound 10 on KG1a cells might be mediated through a mitochondria-dependent apoptotic pathway.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Ding Y,Pan W,Xu J,Wang T,Chen T,Liu Z,Xie C,Zhang Q

doi

10.1016/j.bioorg.2019.01.055

subject

Has Abstract

pub_date

2019-05-01 00:00:00

pages

363-367

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)31256-2

journal_volume

86

pub_type

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