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  • Title: Bromocoumarinplatin, targeting simultaneously mitochondria and nuclei with p53 apoptosis pathway to overcome cisplatin resistance.
    Author: Ma J, Li L, Yue K, Li Y, Liu H, Wang PG, Wang C, Wang J, Luo W, Xie S.
    Journal: Bioorg Chem; 2020 Jun; 99():103768. PubMed ID: 32217375.
    Abstract:
    Mitochondria as one of potential anticancer target, alternatively damaging mtDNA other than nDNA is a potential method for platinum-based anticancer drugs to overcome cisplatin resistance. We herein report that bromocoumarinplatin 1, a coumarin-Pt(IV) prodrug, targeted simultaneously mitochondria and nuclei with the contents of Pt in nDNA and mtDNA were 25.75% and 65.91%, respectively, which demonstrated mtDNA apoptosis played a key role in overcoming cisplatin resistance. Moreover, 1 promoted the expression of p53 gene and protein more effectively than cisplatin, leading to the increased anticancer activity of 1 through p53 pathway. The property of preferential accumulation in cancer cells (Snu-368 and Snu-739) compared to the matched normal cells (HL-7702 cells) demonstrated that 1 was potentially safe for clinical therapeutic use. In addition, the higher therapeutic indices of 1 for HCT-116 cells in vivo indicated that bromocoumarinplatin behaved a vital function in the treatment of colon cancer.
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