Anti-proliferative activity of nano-formulated phenolato titanium(IV) complexes against cancer cells

Sigalit Meker, Katrin Margulis-Goshen, Ester Weiss, Ori Braitbard, Jacob Hochman, Shlomo Magdassi, Edit Y. Tshuva

Research output: Contribution to journalArticlepeer-review


Nanoparticles of titanium(IV) complexes of phenolato ligands were formed and evaluated for cytotoxicity toward human HT-29 colon cancer, murine T-25 lymphoma, and murine HU-2 multidrug-resistant (MDR) cells. The nano-formulation, besides increasing the complexes' shelf lives, is particularly efficient in overcoming limitations in solubility and cell-penetration, thus enhancing biological accessibility; large complexes that were inactive when measured in a non-formulated form showed marked activity when nano-formulated. For active and accessible small complexes, the effect of the formulation was negligible. Most complexes showed similar activity toward MDR cells and their drug-sensitive analogues, further increasing their therapeutic potential. An exception is a particularly hydrophobic complex, which is presumably more accessible to interaction with the membrane ABCB1 (MDR1) transporter active in the multidrug resistance of HU-2 cells. The most efficient compound is a mononuclear complex of a single hexadentate ligand, combining particularly high activity and hydrolytic stability with accessibility aided by the nano-formulation. A nano-boost for the big: Titanium(IV) complexes of phenolato ligands were analyzed as synthesized and in nano-formulation and showed high cytotoxicity toward human and murine drug-sensitive and -resistant cells. The nano-formulation is highly efficient in improving the biological accessibility of particularly bulky complexes.

Original languageAmerican English
Pages (from-to)1294-1298
Number of pages5
Issue number6
StatePublished - Jun 2014


  • cytotoxicity
  • metallodrugs
  • multidrug resistance
  • nano-formulation
  • titanium(IV)

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • General Pharmacology, Toxicology and Pharmaceutics
  • Molecular Medicine
  • Biochemistry
  • Pharmacology
  • Organic Chemistry


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