消旋-2,3-二巯基丁二酸对大鼠体内无机汞的动员作用

Racemic-2,3-dimercaptosuccinic acid for inorganic mercury mobilization in rats.

作者信息

Kostial K, Restek-Samarzija N, Blanusa M, Piasek M, Prester L, Jones M M, Singh P K

机构信息

Department of Mineral Metabolism, Institute for Medical Research and Occupational Health, Zagreb, Republic of Croatia.

出版信息

J Appl Toxicol. 1997 Jan-Feb;17(1):71-4. doi: 10.1002/(sici)1099-1263(199701)17:1<71::aid-jat395>3.0.co;2-u.

DOI:10.1002/(sici)1099-1263(199701)17:1<71::aid-jat395>3.0.co;2-u

PMID:9048230

Abstract

The efficiency of racemic-2,3-dimercaptosuccinic acid (rac-DMSA) compared with meso-2,3-dimercaptosuccinic acid (meso-DMSA) in mobilizing inorganic mercury was evaluated in female rats. Chelators were administered orally at a dose of 0.5, 1.0 or 2.0 mmol kg-1 on four consecutive days, 5 days after a single intraperitoneal 203Hg injection (with 0.5 mg HgCl2 kg-1). Both chelators reduced 203Hg retention in whole body and kidney and at higher doses also in the liver. Racemic-DMSA was more efficient at lower dose levels and equal to meso-DMSA at the highest dose level. Kidney retention decreased after rac-DMSA to 27, 10 and 10% of controls and after meso-DMSA to 68, 39 and 10% of control values at the 0.5, 1.0 and 2.0 mmol kg-1 dose level, respectively. Since meso-DMSA is already approved for human use, its stereoisomeric form, rac-DMSA, deserves further attention for treatment of mercury poisoning.

摘要

在雌性大鼠中评估了外消旋-2,3-二巯基丁二酸（rac-DMSA）与内消旋-2,3-二巯基丁二酸（meso-DMSA）在动员无机汞方面的效率。在单次腹腔注射203Hg（0.5 mg HgCl2 kg-1）5天后，连续4天以0.5、1.0或2.0 mmol kg-1的剂量口服螯合剂。两种螯合剂均降低了全身和肾脏中203Hg的滞留量，在较高剂量时肝脏中的203Hg滞留量也降低。外消旋-DMSA在较低剂量水平时更有效，在最高剂量水平时与内消旋-DMSA相当。在0.5、1.0和2.0 mmol kg-1剂量水平下，外消旋-DMSA处理后肾脏中汞的滞留量分别降至对照组的27%、10%和10%，内消旋-DMSA处理后分别降至对照组的68%、39%和10%。由于内消旋-DMSA已被批准用于人类，其立体异构体形式外消旋-DMSA在汞中毒治疗方面值得进一步关注。