Synthesis and antitumor activity of emodin quaternary ammonium salt derivatives - Details

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Abstract：

A　series　of　new　emodin　derivatives　modified　at　the　C-3　and　the　C-6　positions　were　synthesized,　and　evaluated　for　their　anticancer　activities　in　vitro　and　in　vivo.　Among　them,　Compounds　5g　and　5h　had　more　significant　antiproliferative　ability　against　HepG2,　BGC-823,　AGS　cancer　cell　lines　and　low　cytotoxicity　to　HELF　normal　cell　line,　respectively.　Compounds　5g　and　5h　induced　AGS　cell　cycle　arrest　at　G0/G1　phase　and　induce　apoptosis　via　activation　of　caspase-3　and　caspase-9　enzyme.　In　vivo　studies　using　H22　xenografts　in　Kunming　mice　were　conducted　with　5g　and　5h.　The　results　revealed　that　the　medium　dosage　group　(10　mg/kg)　of　5g　and　the　high　dosage　group　(25　mg/kg)　of　5h　showed　significant　antitumor　activity　compared　to　the　control　group.　©　2012　Elsevier　Masson　SAS.　All　rights　reserved.

Keyword：

Anticancer activity; Apoptosis; Emodin; Long carbon chain; Quaternary ammonium salt

Community：

[ 1 ] [Shao, J.]Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 2 ] [Zhang, F.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 3 ] [Bai, Z.]Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 4 ] [Wang, C.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 5 ] [Yuan, Y.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China
[ 6 ] [Wang, W.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China

Reprint 's Address：

[Wang, W.]Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, China

Email：

wangwf@fzu.edu.cn

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Source ：

European Journal of Medicinal Chemistry

ISSN： 0223-5234

Year： 2012

Volume： 56

Page： 308-319

3 . 4 9 9

JCR@2012

6 . 0 0 0

JCR@2023

JCR Journal Grade：1

CAS Journal Grade：2

Cited Count：

WoS CC Cited Count： 0

SCOPUS Cited Count： 24

ESI Highly Cited Papers on the List： 0 Unfold All

WanFang Cited Count：

Chinese Cited Count：

30 Days PV： 3

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