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)

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).