基于γ-环糊精的抗癌药物 5,6,11,12,17,18,23,24-八氢环十二烷[1,2-b:4,5-b':7,8-b'':10,11-b''']四吲哚（CTet）制剂的合成及生物学评价。
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).
机构信息
Dipartimento di Scienze del Farmaco e della Salute, Università degli Studi di Urbino Carlo Bo I- 61029 Urbino, Piazza del Rinascimento 6, Italy.
出版信息
Molecules. 2010 Jun 4;15(6):4085-93. doi: 10.3390/molecules15064085.
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).
5,6,11,12,17,18,23,24-八氢环十二碳并[1,2-b:4,5-b':7,8-b'':10,11-b'']四吲哚（CTet）是一种吲哚-3-甲醇（I3C）代谢物，具有抗癌特性，但在生物测试中最常使用的溶剂中的溶解度较差。本研究表明，使用γ-环糊精（γ-CD）可避免此问题。用γ-CD 制成的 CTet 是雌激素受体阳性（MCF-7）和雌激素受体阴性（MDA-MB-231）人乳腺癌细胞系中 DNA 合成的有效抑制剂（IC50 分别为 1.20±0.04 μM 和 1.0±0.1 μM）。
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