In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH₂Ph)]Br

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.

Cite this article as:

Garcia-Moreno Elena, Gascon Sonia, Garcia de Jalon A. Jose, Romanos Eduardo, Rodriguez-Yoldi Jesus M, Cerrada Elena and Laguna Mariano, In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH₂Ph)]Br, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (6) . https://dx.doi.org/10.2174/1871520615666150129211440