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A fluorescence-based rapid screening assay for cytotoxic compounds.

Abstract：

:A simple fluorescence-based assay was developed for the rapid screening of potential cytotoxic compounds generated by combinatorial chemistry. The assay is based on detection of nuclear green fluorescent protein (GFP) staining of a human cervical cancer cell line (HeLa) carrying an integrated histone H2B-GFP fusion gene. Addition of a cytotoxic compound to the HeLa-GFP cells results in the eventual degradation of DNA and loss of the GFP nuclear fluorescence. Using this assay, we screened 11 distinct quinone derivatives and found that several of these compounds were cytotoxic. These compounds are structurally related to plumbagin an apoptosis-inducing naphthoquinone isolated from Black Walnut. In order to determine the mechanism by which cell death was induced, we performed additional experiments with the most cytotoxic quinones. These compounds were found to induce morphological changes (blebbing and nuclear condensation) consistent with induction of apoptosis. Additional tests revealed that the cytotoxic compounds induce both necrotic and apoptotic modes of death.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Montoya J,Varela-Ramirez A,Estrada A,Martinez LE,Garza K,Aguilera RJ

doi

10.1016/j.bbrc.2004.10.196

subject

Has Abstract

pub_date

2004-12-24 00:00:00

pages

1517-23

issue

4

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(04)02540-9

journal_volume

325

pub_type

杂志文章

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