Title:In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH2Ph)]Br
Volume: 15
Issue: 6
Author(s): Elena Garcia-Moreno, Sonia Gascon, Jose A. Garcia de Jalon, Eduardo Romanos, M Jesus Rodriguez-Yoldi, Elena Cerrada and Mariano Laguna
Affiliation:
Keywords:
Apoptosis, colon cancer, gold(I), histopathology, in vivo, PTA, Thiolate.
Abstract: A physiologically stable thiolate gold(I) derivative [Au(Spyrimidine)(PTA-CH2Ph)]Br has shown
inhibition in colon cancer proliferation of Caco-2/TC7, Caco-2/PD7 and HTC-116-luc2 cell lines via apoptotic
pathway and S-phase arrest in the cell cycle. Intraperitoneal injection of [Au(Spyrimidine)(PTA-CH2Ph)]Br in
athymic nude mice inoculated with HTC-116-luc2 cells prolonged their survival and greatly inhibited tumour
growth, near to disappearance. Low concentration of gold in urine and blood were detected in mice after 48 h of
administration of 5 mg/kg body weight (bw) of the gold complex and non-organ (kidney and liver) damage has
been detected after gold treatment. The results obtained suggested that the thiolate gold(I) derivative shown here could be considered as a
candidate for therapeutic treatment in colon cancer.