Cytotoxic effect, antitumour activity and toxicity of organotin derivatives with ortho- or para-hydroxy-benzoic acids

AbstractThe cytotoxic and antitumour activities of five organotin complexes (1–5) witho-hydroxy-benzoic orp-hydroxy-benzoic acids were evaluated in a series of in vitro and in vivo experiments. All complexes exhibited strong cytotoxic activity against all cancer cells lines, whereas complexes1,2 and4 induced apoptosis at significantly lower doses than complexes3 and5. Human cancer cells treated with increasing concentrations of complexes1,2 and4 gradually lost their ability to form colonies. Only complexes1 and2 inhibited colony formation efficiency in rat leiomyosarcoma cells. Histopathology of liver and kidney showed mild damage and lung oedema after a single injection of 10  mg/kg body wt of complex1 to Wistar rats. At higher doses (100  mg/kg body wt) brain stem oedema was observed. Daily administration of tumour-bearing Wistar rats (leiomyosarcoma) with 1 mg/kg body wt of complex1 until death reduced the mean tumour growth rate by more than 3 × fold and prolonged mean survival time by 120%. These findings indicate that the organotin complexes with ortho- or para-hydroxy-benzoic acids possess potent cytotoxic and antitumour activity and they could be used as potential chemotherapeutic agents.

Source: Medicinal Chemistry Research - February 2, 2018 Category: Chemistry Source Type: research