4.7 Article

Two telomerase-targeting Pt(II) complexes of jatrorrhizine and berberine derivatives induce apoptosis in human bladder tumor cells

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DALTON TRANSACTIONS
卷 48, 期 40, 页码 15255-15262

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c9dt02381j

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资金

  1. National Natural Science Foundation of China [21867017, 21761033, 21565028]
  2. Natural Science Foundation of Guangxi [2018GXNSFBA138021, 2018GXNSFBA281188]
  3. Innovative Team & Outstanding Talent Program of Colleges and Universities in Guangxi [2014-49, 2017-38]

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Two novel Pt(II) complexes, [Pt(B-TFA)Cl]Cl (Pt1) and [Pt(J-TFA)Cl]Cl (Pt2) with jatrorrhizine and berberine derivatives (B-TFA and J-TFA) were first prepared as desirable luminescent agents for cellular applications and potent telomerase inhibitors, which can induce bladder T-24 tumor cell apoptosis by targeting telomerase, together with induction of mitochondrial dysfunction, telomere DNA damage and cell-cycle arrest. Importantly, T-24 tumor inhibition rate (TIR) was 50.4% for Pt2, which was higher than that of Pt1 (26.4%) and cisplatin (37.1%). Taken together, all the results indicated that jatrorrhizine and berberine derivatives Pt1 and Pt2 show low toxicity and could be novel Pt-based anti-cancer drug candidates.

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