Issue 10, 2003

A novel bioassay for screening and quantification of taxanes

Abstract

We report a novel method for screening and quantifying tubulin-binding antimitotic agents that promote microtubule formation. The method is based on the shift in the peak of the fluorescence emission difference spectrum of tubulin complexed to metal free tetrakis(4-carboxyphenyl)porphyrin (TCPP) in the presence of antimitotic agents. Taxol® (paclitaxel), an anti-tumor drug approved for the treatment of a variety of cancers, caused the appearance of a new fluorescence peak at 645 nm at concentrations as low as 125 nM, the intensity of which was a function of the paclitaxel concentration. Cephalomannine caused the induction of a new fluorescence peak at 651 nm only above 1 µM. Baccatin did not induce the appearance of any new peak within detectable operating measurement conditions. These observations are in accordance with the biological activities/cytotoxicities of these compounds. Accordingly, it is proposed that the new method can be used for high throughput screening of antimitotic compounds.

Graphical abstract: A novel bioassay for screening and quantification of taxanes

Article information

Article type
Communication
Submitted
24 Feb 2003
Accepted
27 Mar 2003
First published
17 Apr 2003

Chem. Commun., 2003, 1188-1189

A novel bioassay for screening and quantification of taxanes

S. Morais, P. C. Pandey, W. Chen and A. Mulchandani, Chem. Commun., 2003, 1188 DOI: 10.1039/B302112B

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