title: Lead detoxification activities of a class of novel DMSA--amino acid conjugates.
abstract: The coupling of the 1-carboxyl of DMSA with l-amino acids led to a class of novel 1-(carbonyl-l-amino-acid)-2,3-dimercaptosuccinic acids (DMSA--amino acid conjugates, DMSA-Gly, -Ser, -Val, -Leu, -Ile, -Asn, -Asp, -Gln, -Glu, -Met, -Phe, and -Trp). In the in vivo evaluation of Pb-loaded mice, 0.4 mmol/kg of the conjugates effectively decreased the Pb levels of the femur, brain, kidney, liver, and blood, greatly enhanced urination, and increased the Pb levels of both urine and feces, while causing no redistributions of Pb to the other organs, especially to the brain. With respect to lowering the bone and brain Pb, DMSA-Ile, -Asn, -Gln, and -Met were more effective than DMSA. This benefit was attributed to their high transmembrane ability. In contrast to Pb, the essential metals such as Fe, Cu, Zn, and Ca of the treated mice were not affected by the administration of the conjugates. Silico molecular modeling predicted that the conjugates had little hepatotoxicity, except possibly for DMSA-Phe.
authors: College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
authors: Yanxia
authors: Y
authors: Xu
authors: Yuji
authors: Y
authors: Wang
authors: Ling
authors: L
authors: Wang
authors: Ming
authors: M
authors: Zhao
authors: Xiaoyi
authors: X
authors: Zhang
authors: Xiaomin
authors: X
authors: Hu
authors: Baoguang
authors: B
authors: Hou
authors: Li
authors: L
authors: Peng
authors: Meiqing
authors: M
authors: Zheng
authors: Jianhui
authors: J
authors: Wu
authors: Shiqi
authors: S
authors: Peng