Embelin Derivatives and Their Anticancer Activity through Microtubule Disassembly

Biological activities of the 1,4-benzoquinone derivatives 5- O-ethylembelin ( 1) and 5- O-methylembelin ( 2) were investigated. Both of them showed antiproliferative activity against a panel of human tumor cell lines upon comparison to normal marsupial kidney cells (PtK2). They arrested HL-60 cells in the G 0/G 1 phase of the cell cycle in a dose- and time-dependent manner. In HeLa cells, exposure to 100 μM of 1 or 2 for 6 h induced a complete disassembly of the microtubule network and an increased number of cells blocked in mitotic stages. Treatment with 10 μM of 1 and 2 for 24 h induced apoptosis in HL-60 cells. This evidence suggests that both 1 and 2 are promising novel antimitotic and anticancer molecules targeting microtubular proteins. DMSO:dimethyl sulfoxide MTT:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide Pet. ether:petroleum ether SRB:sulphorhodamine B.

Medienart:

E-Artikel

Erscheinungsjahr:

2005

Erschienen:

Stuttgart: Georg Thieme Verlag ; 2005

Reproduktion:

Thieme Zeitschriftenarchive 1980-2007

Enthalten in:

Zur Gesamtaufnahme - volume:71

Enthalten in:

Planta medica - 71(2005), 10 vom: Okt., Seite 944-948

Sprache:

Deutsch

Beteiligte Personen:

Xu, Minjuan [VerfasserIn]
Cui, Jingrong [VerfasserIn]
Fu, Hongzheng [VerfasserIn]
Proksch, Peter [Sonstige Person]
Lin, Wenhan [Sonstige Person]
Li, Min [Sonstige Person]

Links:

dx.doi.org [Deutschlandweit zugänglich]

Themen:

Aegiceras corniculatum
Aegicerataceae
Anticancer
Apoptosis
Cell cycle
Microtubules

Umfang:

5

doi:

10.1055/s-2005-871250

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLEJ226233499