Embelin Derivatives and Their Anticancer Activity through Microtubule Disassembly

Abstract

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 G₀/G₁ 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.

Abbreviations

DMSO:dimethyl sulfoxide

MTT:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide

Pet. ether:petroleum ether

SRB:sulphorhodamine B

Aegiceras corniculatum - Aegicerataceae - anticancer - cell cycle - microtubules - apoptosis

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