In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH2Ph)]Br
In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH2Ph)]Br
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DOI：
10.2174/1871520615666150129211440
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发表时间：
2015-01-01
影响因子：
2.8
通讯作者：
Laguna, Mariano
中科院分区：
文献类型：
--
作者：
Garcia-Moreno, Elena;Gascon, Sonia;Laguna, Mariano
一种生理稳定的硫醇金（I）衍生物[Au（Spyrimidine）（PTA-CH 2 Ph）]Br通过细胞凋亡途径和细胞周期中的S期阻滞显示出对Caco-2/TC 7、Caco-2/PD 7和HTC-116-luc 2细胞系的结肠癌增殖的抑制。腹腔注射[Au（Spyrimidine）（PTA-CH 2 Ph）]Br可延长HTC-116-luc 2细胞接种裸鼠的存活时间，并能显著抑制肿瘤生长，甚至接近消失。在给予5 mg/kg体重（bw）的金络合物48 h后，在小鼠的尿液和血液中检测到低浓度的金，并且在金处理后检测到非器官（肾脏和肝脏）损伤。所获得的结果表明，此处所示的硫醇金（I）衍生物可被视为结肠癌治疗性治疗的候选物。
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.