High in vitro and in vivo antitumor activities of luminecent platinum(II) complexes with jatrorrhizine derivatives.

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ID: 85614
2019
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Abstract
Two highly active anticancer Pt(II) complexes, [Pt(Jat1)Cl]Cl (Pt1) and [Pt(Jat2)Cl]Cl (Pt2), containing jatrorrhizine derivative ligands (Jat1 and Jat2) are described. Cell intake study showed high accumulation in cell nuclear fraction. Pt1 and Pt2 exhibited high selectivity for HeLa cancer cells (IC = 15.01 ± 1.05 nM and 1.00 ± 0.17 nM) comparing with HL-7702 normal cells (IC > 150 μM), by targeting p53 and telomerase. Pt2 containing Jat2 ligand was more potent and showed high selectivity for telomerase. It also caused mitochondria and DNA damage, sub-G1 phase arrest, and a high rate of cell apoptosis at the low dose of 1.00 nM. The HeLa tumor inhibition rate (TIR) of Pt2 was 48.8%, which was even higher than cisplatin (35.2%). In addition, Pt2 displayed green luminescent property and potent telomerase inhibition. Our findings demonstrated the promising development of platinum(II) complexes containing jatrorrhizine derivatives as novel Pt-based anti-cancer agents.
Reference Key
qin2019higheuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Qin, Qi-Pin;Zou, Bi-Qun;Wang, Zhen-Feng;Huang, Xiao-Ling;Zhang, Ye;Tan, Ming-Xiong;Wang, Shu-Long;Liang, Hong;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30879-7
URL
Keywords
apoptosis p53 telomerase antitcancer activity jatrorrhizine derivatives platinum(ii) complex

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