Anticancer siRNA delivery by new anticancer molecule: A novel combination strategy for cancer cell killing

作者:Muktapuram Prathap Reddy; Gara Rishi Kumar; Sharma Komal; Rohit Chilappa; Srinivas Kolupula; Mishra Durga Prasad; Bathula Surendar Reddy*
来源:European Journal of Medicinal Chemistry, 2012, 56: 400-408.
DOI:10.1016/j.ejmech.2012.07.035

摘要

The present report describes development of a novel, bifunctional molecule possessing both selective antiproliferative activity and siRNA transfection ability. We synthesized a series of cationic lipobenzamides and screened for in vitro anticancer activities against a panel of cancer and non-cancer cells. The molecule with a ten carbon chain-length (C10M) significantly inhibited proliferation of cancer cells via arresting the cell cycle predominantly in the G1 phase; but did not affect non-cancerous cells. C10M effectively mediated siRNA delivery in vitro. The combined anticancer effect of the delivery of C10M together with its survivin-targeting siRNA cargo was significantly (p < 0.05) superior to that of agent alone. To our knowledge, this is the first report of a dual-purpose molecule with intrinsic anticancer activity and suitability for use in siRNA delivery.

  • 出版日期2012-10