Treatment of refractory sclerodermatous chronic graft-versus-host disease with intravenous lidocaine infusions

Three new platinum(II) complexes of lidocaine and phenylcyanamide derivative ligands of formula K[Pt(3,5-(NO)pcyd)(LC)], 1, K[Pt(3,5-(CF)pcyd)(LC)], 2, K[Pt(3,5-Clpcyd)(LC)], 3 (LC: lidocaine, 3,5-(NO)pcyd: 3,5-dinitro phenylcyanamide, 3,5-(CF)pcyd: 3,5-bis(trifluoromethyl) phenylcyanamide, 3,5-Clpcyd: 3,5-dichloro phenylcyanamide) have been synthesized and fully characterized. Cellular uptake, DNA platination and cytotoxicity against a panel of human tumor cell lines were evaluated. The complexes 1-3 revealed a significant in vitro antiproliferative activity against human ovarian carcinoma (A2780), colorectal adenocarcinoma (HT29), breast (MCF-7), liver hepatocellular carcinoma (HepG-2) and lung adenocarcinoma (A549) cancer cell lines. All the complexes are more active than cisplatin and follow the trend 1 > 2 > 3. Mechanistic studies showed that the trend in cytotoxicity of the Pt(II) complexes is mainly consistent with their ability to accumulate into cancer cells and to increase intracellular basal reactive oxygen species levels, which consequently results in the loss of mitochondrial membrane potential and apoptosis induction. The complex 1 caused to approximately 80-fold higher DNA platination level with respect to cisplatin. The complexes 1-3 can considerably stimulate the production of hydrogen peroxide in a time-dependent manner. Also, the complexes 1-3 induced an increase in reactive oxygen species (ROS) production that was superior to that induced by antimycin. The complex 1 had the most effect on ROS production in comparison with other complexes.

show abstract

Cytotoxicity and cellular response mechanisms of water-soluble platinum(II) complexes of lidocaine and phenylcyanamide derivatives

Tabrizi

Chiniforoshan

2016

Biometals

View full text Add to dashboard Cite

show abstract

New water-soluble palladium(II) complexes of lidocaine and phenylcyanamide derivative ligands: cytotoxicity and cellular response mechanisms

Tabrizi

Chiniforoshan

2016

Invest New Drugs

View full text Add to dashboard Cite

Three new palladium(II) complexes of lidocaine and phenylcyanamide derivative ligands of formula K[Pd(2,6-Mepcyd)(LC)], 1, K[Pd(2,6-Etpcyd)(LC)], 2, K[Pd(2,6-Clpcyd)(LC)], 3 (LC: lidocaine, 2,6-Mepcyd: 2,6-dimethyl phenylcyanamide, 2,6-Etpcyd: 2,6-diethyl phenylcyanamide, 2,6-Clpcyd: 2,6-dichloro phenylcyanamide) have been synthesized and fully characterized. The complexes 1-3 revealed a significant in vitro antiproliferative activity against human ovarian carcinoma (A2780), colorectal adenocarcinoma (HT29), breast (MCF-7), liver hepatocellular carcinoma (HepG-2) and lung adenocarcinoma (A549) cancer cell lines. All the complexes are more active than cisplatin and follow the trend 2 > 1 > 3. Mechanistic studies showed that the trend in cytotoxicity of the Pd(II) complexes is mainly consistent with their ability to accumulate into cancer cells and to increase intracellular basal reactive oxygen species levels, which consequently results in the loss of mitochondrial membrane potential and apoptosis induction.

show abstract

Nickel(II) and cobalt(II) complexes of lidocaine: Synthesis, structure and comparative in vitro evaluations of biological perspectives

Tabrizi

McArdle

Erxleben

et al. 2015

European Journal of Medicinal Chemistry

View full text Add to dashboard Cite

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

hi@scite.ai

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Treatment of refractory sclerodermatous chronic graft-versus-host disease with intravenous lidocaine infusions

Cited by 5 publications

References 8 publications

Cytotoxicity and cellular response mechanisms of water-soluble platinum(II) complexes of lidocaine and phenylcyanamide derivatives

Cytotoxicity and cellular response mechanisms of water-soluble platinum(II) complexes of lidocaine and phenylcyanamide derivatives

New water-soluble palladium(II) complexes of lidocaine and phenylcyanamide derivative ligands: cytotoxicity and cellular response mechanisms

Nickel(II) and cobalt(II) complexes of lidocaine: Synthesis, structure and comparative in vitro evaluations of biological perspectives

Contact Info

Product

Resources

About