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In Vitro Cytotoxicity and In Vivo Antitumor Efficacy of Tetrazolato-Bridged Dinuclear Platinum ( II ) Complexes with a Bulky Substituent at Tetrazole C 5
| Content Provider | Semantic Scholar |
|---|---|
| Author | Komeda, Seiji Uemura, Masako Yoneyama, Hiroki Harusawa, Shinya Hiramoto, Keiichi |
| Copyright Year | 2019 |
| Abstract | Tetrazolato-bridged dinuclear platinum(II) complexes ([{cis-Pt(NH3)2}2(μ-OH)(μ-5-Rtetrazolato-N2,N3)]2+; tetrazolato-bridged complexes) are a promising source of next-generation platinum-based drugs. β-Cyclodextrin (β-CD) forms inclusion complexes with bulky organic compounds or substituents, changing their polarity and molecular dimensions. Here, we determined by 1H-NMR spectroscopy, the stability constants for inclusion complexes formed between β-CD and tetrazolato-bridged complexes with a bulky, lipophilic substituent at tetrazole C5 (complexes 1–3, phenyl, n-nonyl, and adamantyl substitution, respectively). We then determined the in vitro cytotoxicity and in vivo antitumor efficacy of complexes 1–3 against the Colon-26 colorectal cancer cell line in the absence or presence of equimolar β-CD. Compared with the platinum-based anticancer drug oxaliplatin (1R,2R-diaminocyclohexane)oxalatoplatinum(II)), complex 2 had similar cytotoxicity, complex 3 was moderately cytotoxic, and complex 1 was the least cytotoxic. The cytotoxicity of the complexes decreased in the presence of β-CD. When we examined the in vivo antitumor efficacy of complexes 1–3 (10 mg/kg) against homografted Colon-26 colorectal tumors in male BALB/c mice, they showed a relatively low tumor growth inhibition compared with oxaliplatin. However, in the presence of β-CD, complex 3 had higher in vivo antitumor efficacy than oxaliplatin, suggesting a new direction for future research into tetrazolato-bridged complexes with high in vivo antitumor activity. |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | https://res.mdpi.com/inorganics/inorganics-07-00005/article_deploy/inorganics-07-00005.pdf?attachment=1&filename= |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
