Issue 9, 2013

Delivery and release of curcumin by a hypoxia-activated cobalt chaperone: a XANES and FLIM study

Abstract

We present a bioreductively activated cobalt(III) carrier system for the delivery of curcumin with enhanced drug stability, tumour penetration and efficacy in hypoxic tumour regions. Curcumin is a natural product with potent anticancer activity but low bioavailability and serum stability. With the aim of overcoming these limitations, we prepared a cobalt(III) prodrug of curcumin and compared the stability, cytotoxicity and cellular uptake with those of the free drug. Using a combination of fluorescence lifetime imaging and X-ray absorption spectroscopy, we demonstrated that curcumin is released from the cobalt carrier complex in tumour cells, with strong evidence to suggest that the process occurs via reduction of the cobalt centre. Furthermore, fluorescence lifetime imaging in solid tumour models showed that the cobalt complex delivered curcumin uniformly throughout the tumour model, while free curcumin only accumulated on the outer edges. For comparison, we also investigated the isoelectronic ruthenium(II) complex and found its properties and biological activity to be very different to those of the cobalt analogue.

Graphical abstract: Delivery and release of curcumin by a hypoxia-activated cobalt chaperone: a XANES and FLIM study

Supplementary files

Article information

Article type
Edge Article
Submitted
31 May 2013
Accepted
10 Jul 2013
First published
10 Jul 2013
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2013,4, 3731-3739

Delivery and release of curcumin by a hypoxia-activated cobalt chaperone: a XANES and FLIM study

A. K. Renfrew, N. S. Bryce and T. W. Hambley, Chem. Sci., 2013, 4, 3731 DOI: 10.1039/C3SC51530C

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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