Molecules (Jun 2010)

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)

  • Simone Lucarini,
  • Mauro De Santi,
  • Francesca Antonietti,
  • Giorgio Brandi,
  • Giuseppe Diamantini,
  • Alessandra Fraternale,
  • Maria Filomena Paoletti,
  • Andrea Tontini,
  • Mauro Magnani,
  • Andrea Duranti

DOI
https://doi.org/10.3390/molecules15064085
Journal volume & issue
Vol. 15, no. 6
pp. 4085 – 4093

Abstract

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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).

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