Nogueira C W, Soares F A, Nascimento P C, Muller D, Rocha J B T
Departamento de Quimica, Centro de Ciencias Naturais e Exatas, Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.
Toxicology. 2003 Mar 3;184(2-3):85-95. doi: 10.1016/s0300-483x(02)00575-9.
Compounds derived from Dimercaprol, such as meso-2,3-dimercaptosuccinic acid (DMSA) and 2,3-dimercaptopropane-1-sulfonic acid (DMPS), are becoming common agents for treating humans exposed to heavy metals. Heavy metals such as Pb(2+), Hg(2+) and Cd(2+) can inhibit delta-aminolevulinate dehydratase (delta-ALA-D) activity. Delta-ALA-D catalyzes the condensation of two delta-aminolevulinic acid (delta-ALA) molecules with the formation of porphobilinogen, a heme precursor. The effects of DMSA and DMPS alone or in combination with Cd(2+), Hg(2+), or Pb(2+) on hepatic delta-ALA-D were examined. DMPS and DMSA caused a dose-dependent inhibition of hepatic delta-ALA-D. In the presence of Hg(2+) or Cd(2+) the inhibitory potency of DMPS increased. Similarly, the inhibitory effects of Hg(2+) and Cd(2+) were markedly increased in the presence of DMSA. In contrast, the inhibitory effect of DMPS was not changed by inclusion of Pb(2+). As observed with DMSA, Zn(2+) did not modified the inhibitory effect of DMPS. Data of the present report support the idea that the complexes formed (metals-DMSA or DMPS) were more inhibitory than the metal (Hg(2+) and Cd(2+)) or the chelating agent alone to the hepatic delta-ALA-D activity, in vitro. The mechanism of hepatic delta-ALA-D inhibition by Hg(2+)-DMPS/DMSA and Cd(2+)-DMPS/DMSA complexes involve the essential thiol groups of the enzyme.
源自二巯丙醇的化合物,如内消旋-2,3-二巯基丁二酸(DMSA)和2,3-二巯基丙烷-1-磺酸(DMPS),正成为治疗接触重金属的人类的常用药物。诸如Pb(2+)、Hg(2+)和Cd(2+)等重金属可抑制δ-氨基乙酰丙酸脱水酶(δ-ALA-D)的活性。δ-ALA-D催化两个δ-氨基乙酰丙酸(δ-ALA)分子缩合形成胆色素原,即血红素前体。研究了DMSA和DMPS单独或与Cd(2+)、Hg(2+)或Pb(2+)联合使用对肝脏δ-ALA-D的影响。DMPS和DMSA对肝脏δ-ALA-D产生剂量依赖性抑制。在存在Hg(2+)或Cd(2+)的情况下,DMPS的抑制效力增加。同样,在存在DMSA的情况下,Hg(2+)和Cd(2+)的抑制作用显著增强。相比之下,加入Pb(2+)后DMPS的抑制作用未改变。正如DMSA的情况一样,Zn(2+)并未改变DMPS的抑制作用。本报告的数据支持这样一种观点,即所形成的复合物(金属-DMSA或DMPS)在体外对肝脏δ-ALA-D活性的抑制作用比金属(Hg(2+)和Cd(2+))或单独的螯合剂更强。Hg(2+)-DMPS/DMSA和Cd(2+)-DMPS/DMSA复合物对肝脏δ-ALA-D的抑制机制涉及该酶的必需巯基。