title: 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.affiliation: Department of Pharmacology and Pharmaceutical Chemistry, S.R. College of Pharmacy, Ananthasagar, Warangal, India. shyamar9@gmail.com
authors.forename: Shyam Sunder
authors.initials: SS
authors.lastname: Anchuri
authors.forename: Sreekanth
authors.initials: S
authors.lastname: Thota
authors.forename: Rajeshwar
authors.initials: R
authors.lastname: Yerra
authors.forename: Krishna Prasad
authors.initials: KP
authors.lastname: Devarakonda
authors.forename: Satyavathi
authors.initials: S
authors.lastname: Dhulipala
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology*; D001835:Body Weight / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy* / Q000401:mortality; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D008297:Male; D051379:Mice; D010618:Phenanthrolines / Q000737:chemistry / Q000494:pharmacology; D017975:Ruthenium Compounds / Q000009:adverse effects / Q000494:pharmacology*; D013882:Thiosemicarbazones / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D010618:Phenanthrolines; D017975:Ruthenium Compounds; D013882:Thiosemicarbazones