Abstract
The indole-substituted titanocene dichloride derivative Titanocene T, which is completely water-soluble and shows micromolar activity against the human renal cancer cells Caki-1, was tested in vivo an against xenografted human renal cell tumors in mice. Titanocene T was then given at 25 and 50 mg/kg, seven times every four days during three weeks to two groups (n=6) of Caki-1 tumor-bearing female NMRI:nu/nu mice, while the control group was treated with solvent only. At both doses Titanocene T induced a moderate to good tumor growth reduction with respect to the solventtreated control group, with an optimal T/C value of 51% and 32% and showed neither mortality nor toxicity. Immunohistochemical analysis revealed that the expression of the proliferation marker Ki-67 was reduced in the high-dosage group. Furthermore, anti-angiogenic activity was identified by CD31 staining; the number of micro vessels in a defined tumor area decreased by 27% and 29% due to Titanocene T treatment.
Keywords: Anticancer drug, anti-angiogenic drug, Titanocene, Renal cell cancer, Xenograft
Letters in Drug Design & Discovery
Title:The Activity of Titanocene T Against Xenografted Caki-1 Tumors
Volume: 10 Issue: 5
Author(s): Wolfgang Walther, Iduna Fichtner, Anthony Deally, Megan Hogan and Matthias Tacke
Affiliation:
Keywords: Anticancer drug, anti-angiogenic drug, Titanocene, Renal cell cancer, Xenograft
Abstract: The indole-substituted titanocene dichloride derivative Titanocene T, which is completely water-soluble and shows micromolar activity against the human renal cancer cells Caki-1, was tested in vivo an against xenografted human renal cell tumors in mice. Titanocene T was then given at 25 and 50 mg/kg, seven times every four days during three weeks to two groups (n=6) of Caki-1 tumor-bearing female NMRI:nu/nu mice, while the control group was treated with solvent only. At both doses Titanocene T induced a moderate to good tumor growth reduction with respect to the solventtreated control group, with an optimal T/C value of 51% and 32% and showed neither mortality nor toxicity. Immunohistochemical analysis revealed that the expression of the proliferation marker Ki-67 was reduced in the high-dosage group. Furthermore, anti-angiogenic activity was identified by CD31 staining; the number of micro vessels in a defined tumor area decreased by 27% and 29% due to Titanocene T treatment.
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Cite this article as:
Walther Wolfgang, Fichtner Iduna, Deally Anthony, Hogan Megan and Tacke Matthias, The Activity of Titanocene T Against Xenografted Caki-1 Tumors, Letters in Drug Design & Discovery 2013; 10 (5) . https://dx.doi.org/10.2174/1570180811310050002
DOI https://dx.doi.org/10.2174/1570180811310050002 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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