Antitumor activity of nanoliposomes encapsulating the novobiocin analog 6BrCaQ in a triple-negative breast cancer model in mice

Abstract : In this study, we investigated the anticancer efficacy of pegylated liposomes containing 6BrCaQ, an hsp90 inhibitor derived from novobiocin. 6BrCaQ has been previously identified as the most potent compound in a series of quinoleic novobiocin analogs but is poorly water-soluble. We investigated, for the first time, the anti-proliferative effects of this drug in vivo in an orthotopic breast cancer model (MDA-MB-231 luc) using pegylated liposomes to allow its administration. Hsp90, hsp70 and hsp27 protein and mRNA expressions were not strongly affected after treatment meaning it did not induce a heat shock response often associated with resistance and poor prognosis. Liposomal delivery of 6BrCaQ retarded tumor growth at a low dose (1 mg/kg, injected once a week for 4 weeks). Histological analysis of tumors revealed necrosis and a lower proportion of proliferative cells in treated mice indicating that this drug has potential for breast cancer therapy when encapsulated in liposomes.
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https://www.hal.inserm.fr/inserm-02096216
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Submitted on : Thursday, April 11, 2019 - 10:56:46 AM
Last modification on : Thursday, July 25, 2019 - 2:24:04 PM

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Félix Sauvage, Elias Fattal, Walhan Al-Shaer, Stéphanie Denis, Emilie Brotin, et al.. Antitumor activity of nanoliposomes encapsulating the novobiocin analog 6BrCaQ in a triple-negative breast cancer model in mice. Cancer Letters, Elsevier, 2018, 432, pp.103-111. ⟨10.1016/j.canlet.2018.06.001⟩. ⟨inserm-02096216⟩

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