Synthesis and biological evaluation of a gamma-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).
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 gamma-cyclodextrin (gamma-CD) avoids this problem. Formulated with gamma-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 microM and 1.0 +/- 0.1 microM, respectively).
Lucarini
Simone
S
Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Urbino Carlo Bo I- 61029 Urbino, Piazza del Rinascimento 6, Italy. simone.lucarini@uniurb.it
De Santi
Mauro
M
Antonietti
Francesca
F
Brandi
Giorgio
G
Diamantini
Giuseppe
G
Fraternale
Alessandra
A
Paoletti
Maria Filomena
MF
Tontini
Andrea
A
Magnani
Mauro
M
Duranti
Andrea
A
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D047408:gamma-Cyclodextrins / Q000737:chemistry*
D000970:Antineoplastic Agents; D007211:Indoles; D047408:gamma-Cyclodextrins; C023792:gamma-cyclodextrin