Novel mononuclear ruthenium(II) compounds in cancer therapy.

Abstract

The present study was conducted to evaluate in vivo anticancer activity of two novel mononuclear ruthenium(II) compounds, namely Ru(1,10-phenanthroline)2(2-nitro phenyl thiosemicarbazone)Cl2 (Compound R1) and Ru (1,10-phenanthroline)2(2-hydroxy phenyl thiosemicarbazone)Cl2 (Compound R2) against Ehrlich ascites carcinoma (EAC) mice and in vitro cytotoxic activity against IEC-6 (small intestine) cell lines and Artemia salina nauplii using MTT [(3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide)] and BLT [brine shrimp lethality] assays respectively. The test ruthenium compounds at the doses 2 and 4 mg/kg body weight showed promising biological activity, especially in decreasing tumor volume, viable ascites cell counts and body weights. These compounds prolonged the life span (% ILS), mean survival time (MST) of mice bearing-EAC tumor. The results for in vitro cytotoxicity against IEC-6 cells showed the ruthenium compound R2 to have significant cytotoxic activity with a IC50 value of 20.0 μg/mL than R1 (IC50=78.8 μg/mL) in the MTT assay and the LC50 values of R1 and R2 compounds were found to be 38.3 and 43.8 μg/mL respectively in the BLT assay. The biochemical and histopathological results revealed that there was no significant hepatotoxicity and nephrotoxicity associated with the ruthenium administration to mice.

• Authors: Shyam Sunder Anchuri, Sreekanth Thota, Rajeshwar Yerra, Krishna Prasad Devarakonda, Satyavathi Dhulipala
• Journal: Asian Pacific journal of cancer prevention : APJCP (Asian Pac J Cancer Prev) Vol. 13 Issue 7 Pg. 3293-8 ( 2012) ISSN: 2476-762X [Electronic] Thailand
• PMID: 22994750 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Phenanthrolines
• Ruthenium Compounds
• Thiosemicarbazones

Topics

• Animals
• Antineoplastic Agents (adverse effects, pharmacology)
• Body Weight (drug effects)
• Carcinoma, Ehrlich Tumor (drug therapy, mortality)
• Cell Line, Tumor
• Drug Screening Assays, Antitumor
• Male
• Mice
• Phenanthrolines (chemistry, pharmacology)
• Ruthenium Compounds (adverse effects, pharmacology)
• Thiosemicarbazones (chemistry, pharmacology)