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

Author(s): Elena Garcia-Moreno, Sonia Gascon, Jose A. Garcia de Jalon, Eduardo Romanos, M Jesus Rodriguez-Yoldi, Elena Cerrada, Mariano Laguna.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 15 , Issue 6 , 2015

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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.

Keywords: Apoptosis, colon cancer, gold(I), histopathology, in vivo, PTA, Thiolate.

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Article Details

VOLUME: 15
ISSUE: 6
Year: 2015
Page: [773 - 782]
Pages: 10
DOI: 10.2174/1871520615666150129211440
Price: $58

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