Tang Xiaojiang, Zhu Jinqiu, Zhong Zhiyong, Luo Minhui, Li Guangxian, Gong Zhihong, Zhang Chenzi, Fei Fan, Ruan Xiaolin, Zhou Jinlin, Liu Gaofeng, Li Guoding, Olson James, Ren Xuefeng
Guangdong Medical Laboratory Animal Center, China.
Department of Epidemiology and Environmental Health, The State University of New York, Buffalo, NY, USA.
Toxicol Appl Pharmacol. 2016 Aug 15;305:143-152. doi: 10.1016/j.taap.2016.06.001. Epub 2016 Jun 6.
Chronic exposure to cadmium compounds (Cd(2+)) is one of the major public health problems facing humans in the 21st century. Cd(2+) in the human body accumulates primarily in the kidneys which leads to renal dysfunction and other adverse health effects. Efforts to find a safe and effective drug for removing Cd(2+) from the kidneys have largely failed. We developed and synthesized a new chemical, sodium (S)-2-(dithiocarboxylato((2S,3R,4R,5R)-2,3,4,5,6 pentahydroxyhexyl)amino)-4-(methylthio) butanoate (GMDTC). Here we report that GMDTC has a very low toxicity with an acute lethal dose (LD50) of more than 10,000mg/kg or 5000mg/kg body weight, respectively, via oral or intraperitoneal injection in mice and rats. In in vivo settings, up to 94% of Cd(2+) deposited in the kidneys of Cd(2+)-laden rabbits was removed and excreted via urine following a safe dose of GMDTC treatment for four weeks, and renal Cd(2+) level was reduced from 12.9μg/g to 1.3μg/g kidney weight. We observed similar results in the mouse and rat studies. Further, we demonstrated both in in vitro and in animal studies that the mechanism of transporting GMDTC and GMDTC-Cd complex into and out of renal tubular cells is likely assisted by two glucose transporters, sodium glucose cotransporter 2 (SGLT2) and glucose transporter 2 (GLUT2). Collectively, our study reports that GMDTC is safe and highly efficient in removing deposited Cd(2+) from kidneys assisted by renal glucose reabsorption system, suggesting that GMDTC may be the long-pursued agent used for preventive and therapeutic purposes for both acute and chronic Cd(2+) exposure.
长期接触镉化合物(Cd(2+))是21世纪人类面临的主要公共卫生问题之一。人体中的Cd(2+)主要在肾脏中蓄积,这会导致肾功能障碍及其他不良健康影响。寻找一种安全有效的药物来清除肾脏中Cd(2+)的努力大多以失败告终。我们研发并合成了一种新化学物质,(S)-2-(二硫代羧基((2S,3R,4R,5R)-2,3,4,5,6-五羟基己基)氨基)-4-(甲硫基)丁酸钠(GMDTC)。在此我们报告,GMDTC毒性极低,通过对小鼠和大鼠口服或腹腔注射,其急性致死剂量(LD50)分别超过10000mg/kg或5000mg/kg体重。在体内实验中,给镉负荷兔安全剂量的GMDTC治疗四周后,肾脏中沉积的Cd(2+)高达94%被清除并通过尿液排出,肾脏Cd(2+)水平从12.9μg/g肾脏重量降至1.3μg/g。我们在小鼠和大鼠研究中也观察到了类似结果。此外,我们在体外和动物研究中均证明,GMDTC和GMDTC-Cd复合物进出肾小管细胞的转运机制可能由两种葡萄糖转运体协助,即钠葡萄糖协同转运蛋白2(SGLT2)和葡萄糖转运蛋白2(GLUT2)。总体而言,我们的研究报告表明,在肾脏葡萄糖重吸收系统的协助下,GMDTC在清除肾脏中沉积的Cd(2+)方面安全且高效,这表明GMDTC可能是长期以来寻求的用于急性和慢性Cd(2+)暴露预防和治疗的药物。