A novel synthetic iminoquinone, BA-TPQ, as an anti-breast cancer agent: in vitro and in vivo activity and mechanisms of action.

Breast Cancer Research and Treatment
Wei WangRuiwen Zhang

Abstract

Herein, we report our examination of the anti-breast cancer activity of a novel synthetic compound, 7-(benzylamino)-1, 3, 4, 8-tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one (BA-TPQ). This agent is an analog of a naturally occurring marine compound, and was found to be the most active out of more than 40 related compounds. We investigated the in vitro activity of BA-TPQ on the survival, proliferation, and apoptosis of breast cancer cells using the MTT and BrdUrd assays, and Annexin/Annexin-PI staining and flow cytometry. The in vivo anti-cancer effects of BA-TPQ were evaluated in xenograft models of breast cancer. Finally, the mechanisms of action of the compound were also assessed by cDNA microarrays, RT-PCR and Western blotting. In a dose-dependent manner, BA-TPQ inhibited cell growth and induced apoptosis and cell cycle arrest in human MCF-7 and MDA-MB-468 breast cancer cells in vitro, and showed in vivo efficacy in mice bearing MCF-7 or MDA-MB-468 xenograft tumors. We demonstrated that BA-TPQ modifies the expression of numerous molecules involved in cell cycle progression and apoptosis. Similar changes in protein expression were observed in vitro and in vivo, as determined by examination of cells and excised xenograft tum...Continue Reading

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Citations

Feb 24, 2015·Marine Drugs·Christian Bailly
Jul 26, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Suzan Khayyat, Abd El-Galil Amr
Oct 14, 2011·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Marc SchumacherMarc Diederich
Apr 15, 2020·Organic & Biomolecular Chemistry·Matthew B MinusZachary T Ball
Jun 2, 2011·Organic & Biomolecular Chemistry·Panayiotis A KoutentisDaniele Lo Re
Oct 30, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Zviadi AburjaniaRenata Jaskula-Sztul

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