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Multifunctional Pt(IV) complexes containing a glutathione s-transferase inhibitor lead to enhancing anticancer activity and preventing metastasis of osteosarcoma cells

Abstract

Cisplatin has been clinically applied in the treatment of osteosarcoma (OS), but its efficacy is severely limited due to the drug resistance and metastasis. One of the chief culprits is the overexpression of glutathione s-transferase (GSTs) in cancer cells that can accelerate the interaction of glutathione (GSH) with cisplatin to reduce its biological effects. In this study, three Pt(IV) complexes derived from cisplatin conjugated with a GSTs inhibitor (NBDHEX) were designed and synthesized. The stability and releasing capability of these complexes as well as their ability to inhibit GSTs were investigated together with their in vitro anticancer activities toward osteosarcoma cells. Among them, complex 2 bearing one NBDHEX derivative and a hydroxyl group at the axial positions could markedly kill human OS cells due to its suitable stability and prominent ability to inhibit GSTs. Meanwhile, it can prevent the metastasis of OS via down-regulating Akt. Thus, complex 2 has the potential for further research in the treatment of OS.

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Publication details

The article was received on 18 Oct 2018, accepted on 06 Dec 2018 and first published on 06 Dec 2018


Article type: Paper
DOI: 10.1039/C8MT00296G
Citation: Metallomics, 2018, Accepted Manuscript
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    Multifunctional Pt(IV) complexes containing a glutathione s-transferase inhibitor lead to enhancing anticancer activity and preventing metastasis of osteosarcoma cells

    H. Chen, F. Chen, X. Wang and S. Gou, Metallomics, 2018, Accepted Manuscript , DOI: 10.1039/C8MT00296G

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