[Zn(phen)(O,N,O)(H2O)] and [Zn(phen)(O,N)(H2O)] with O,N,O is 2,6-dipicolinate and N,O is L-threoninate: synthesis, characterization, and biomedical properties

作者：Chin Lee Fang; Kong Siew Ming; Seng Hoi Ling; Tiong Yee Lian; Neo Kian Eang; Maah Mohd Jamil; Khoo Alan Soo Beng; Ahmad Munirah; Hor Tzi Sum Andy; Lee Hong Boon; San Swee Lan; Chye Soi Moi; Ng Chew Hee^*

来源：Journal of Biological Inorganic Chemistry, 2012, 17(7): 1093-1105.

DOI：10.1007/s00775-012-0923-y

• Ternary zinc(II)-1,10-phenanthroline complex
• Nasopharyngeal carcinoma
• Dipicolinic acid
• L-Threonine
• Topoisomerase I

Two ternary Zn(II) complexes, with 1,10-phenanthroline (phen) as the main ligand and a carboxylate-containing ligand [dipicolinate (dipico) or l-threoninate (l-Thr)] as the subsidiary ligand, were prepared and characterized by elemental analysis, Fourier transform IR, UV, and fluorescence spectroscopy, X-ray diffraction, molar conductivity, and electrospray ionization mass spectrometry. X-ray structure analysis shows that both [Zn(phen)(dipico)(H2O)]center dot H2O (1) and [Zn(phen)(l-Thr)(H2O)Cl]center dot 2H(2)O (2) have octahedral geometry about the Zn(II) atom. Both complexes can inhibit topoisomerase I, and have better anticancer activity than cisplatin against nasopharyngeal cancer cell lines, HK1 and HONE-1, with concentrations causing 50 % inhibition of cell proliferation (IC50) in the low micromolar range. Complex 2 has the highest therapeutic index for HK1. Both Zn(II) complexes can induce cell death by apoptosis. Changing the subsidiary ligand in the Zn(II) complexes affects the UV-fluorescence spectral properties of the coordinated phen ligand, the binding affinity for some DNA sequences, nucleobase sequence-selective binding, the phase at which cell cycle progression was arrested for treated cancer cells, and their therapeutic index.

• 出版日期2012-10
• 单位河北医科大学