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Molecules 2010, 15(6), 4085-4093; doi:10.3390/molecules15064085

Synthesis and Biological Evaluation of a γ-Cyclodextrin-based Formulation of the Anticancer Agent 5,6,11,12,17,18,23,24- Octahydrocyclododeca[1,2-b:4,5-b’:7,8-b’’:10,11-b’’’]tetraindole (CTet)

1
Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Urbino “Carlo Bo” I- 61029 Urbino, Piazza del Rinascimento 6, Italy
2
Dipartimento di Scienze Biomolecolari, Università degli Studi di Urbino “Carlo Bo” I-61029 Urbino, Via Aurelio Saffi 2, Italy
*
Author to whom correspondence should be addressed.
Received: 21 April 2010 / Revised: 27 May 2010 / Accepted: 1 June 2010 / Published: 4 June 2010
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Abstract

5,6,11,12,17,18,23,24-octahydrocyclododeca[1,2-b:4,5-b’:7,8-b’’:10,11- b’’’]tetrai ndole (CTet), an indole-3-carbinol (I3C) metabolite endowed with anticancer properties, is poorly soluble in the solvents most frequently used in biological tests. This study indicates that the use of γ-cyclodextrin (γ-CD) avoids this problem. Formulated with γ-CD CTet is a potent inhibitor of DNA synthesis in both estrogen receptor positive (MCF-7) and estrogen receptor negative (MDA-MB-231) human breast cell lines (IC50 = 1.20 ± 0.04 μM and 1.0 ± 0.1 μM, respectively).
Keywords: indole-3-carbinol; indole cyclic tetramer; γ-cyclodextrin; breast cancer indole-3-carbinol; indole cyclic tetramer; γ-cyclodextrin; breast cancer
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Lucarini, S.; De Santi, M.; Antonietti, F.; Brandi, G.; Diamantini, G.; Fraternale, A.; Paoletti, M.F.; Tontini, A.; Magnani, M.; Duranti, A. Synthesis and Biological Evaluation of a γ-Cyclodextrin-based Formulation of the Anticancer Agent 5,6,11,12,17,18,23,24- Octahydrocyclododeca[1,2-b:4,5-b’:7,8-b’’:10,11-b’’’]tetraindole (CTet). Molecules 2010, 15, 4085-4093.

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