Anticancer and cytotoxic effects of a triorganotin compound with 2-mercapto-nicotinic acid in malignant cell lines and tumor bearing Wistar rats (Journal article)

Verginadis, II/ Karkabounas, S./ Simos, Y./ Kontargiris, E./ Hadjikakou, S. K./ Batistatou, A./ Evangelou, A./ Charalabopoulos, K.


Nowadays, investigation for possible therapeutic applications of various metal-based drugs attracts the scientific interest worldwide. The triorganotin compound bis[triphenyltin(IV)](3-carboxy-pyridine-2-thionato) (SnMNA), was tested for its anti-proliferative and antitumor activities. Cytotoxic activity was assessed by Trypan blue and 3-(4.5-dimethylthiazol-2-yl)-2.5-diphenyltetrazolium bromide assay (MTT). SnMNA exhibited potent cytotoxic effects against leiomyosarcoma cells (LMS) and human breast adenocarcinoma cells (MCF-7), which is 200 times stronger than that of cisplatin. Moreover, SnMNA induced significant apoptosis in LMS and MCF-7 cells characterized by flow cytometry analysis and DNA fragmentation. Acute and chronic toxicity studies on Wistar rats caused kidney and lung toxicity at a single dose of 80mg/kgBody Weight (BW) or four repeated doses of 8mg/kgBW once per week. Furthermore, antitumor activity studies on sarcoma bearing Wistar rats revealed that SnMNA complex at four repeated doses of 5.4mg/kgBW every three days prolonged mean survival time of the animal at 200% and decreased mean tumor growth rate (MTGR) compared to the control group (p<0.05). It is noteworthy to mention that the 30% (3 out of 10) of the bearing animals were totally cured. These findings indicate that SnMNA might be a promising new antitumor agent.
Institution and School/Department of submitter: Πανεπιστήμιο Ιωαννίνων. Σχολή Επιστημών Υγείας. Τμήμα Ιατρικής
Keywords: Animals,Antineoplastic Agents/chemistry/*pharmacology,Apoptosis/drug effects,Cell Line, Tumor,Drug Screening Assays, Antitumor,Female,Flow Cytometry,Humans,Neoplasms, Experimental/*pathology,Nicotinic Acids/chemistry/*pharmacology,Organotin Compounds/chemistry/*pharmacology,Platelet Aggregation/drug effects,Rats,Rats, Wistar,Sulfhydryl Compounds/chemistry/*pharmacology
URI: http://olympias.lib.uoi.gr/jspui/handle/123456789/23806
ISSN: 1879-0720
Link: http://www.ncbi.nlm.nih.gov/pubmed/21130873
http://www.sciencedirect.com/science/article/pii/S092809871000391X
Appears in Collections:Άρθρα σε επιστημονικά περιοδικά ( Ανοικτά)

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