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Synthesis and evaluations of pentahydroxylhexyl-L-cysteine and its dimer as chelating agents for cadmium or lead decorporation
Wang, C; Zhao, M; Yang, J; Li, XW; Peng, SQ
关键词cadmium lead antagonists
刊名TOXICOLOGY AND APPLIED PHARMACOLOGY
2004-11-01
DOI10.1016/j.taap.2004.04.009
200期:3页:229-236
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy ; Toxicology
研究领域[WOS]Pharmacology & Pharmacy ; Toxicology
关键词[WOS]MUTAGENICITY TEST ; CACO-2 CELLS ; MOBILIZATION ; PERMEABILITY ; ABSORPTION ; TRANSPORT ; MICE
英文摘要

N-(2,3,4,5,6-pentahydroxylhexyl)-L-cysteine (4) and NN′-di(2,3,4,5,6-pentahydroxylhexyl)-L-cystine (5) were synthesized. As antagonists of cadmium or lead intoxication, they were found to be effective by oral administration on repeated exposure. The bioassay in vivo indicated that their cadmium-mobilizing potencies are significantly superior to those of N-acetyl-L-cysteine and their lead-mobilizing properties are equivalent to those of DL-penicillamine (DL-PA). The stability constants of the Cd-4 and Cd-5 complexes or Pb-4 and Pb-5 complexes were determined by use of pH titration. The membrane permeability of compounds 4 and 5 was evaluated by transporting across the Caco-2 cell monolayer. The effect of compounds 4 and 5 on the concentrations of essential metal ions in the renal cortex is negligible in comparison with that of the group treated with lead only. The acute toxicity of compounds 4 was tested by oral gavage and the resulting LD50 value for both mice and rats is larger than 10 g kg(-1) bw. The cytogenetic effects of compound 4 were evaluated in the Ames assay, mouse bone marrow micronucleus test, and sperms shape abnormality assay, and all of them show the negative reactions. (C) 2004 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000224952000007
引用统计
被引频次:15[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/65283
专题北京大学药学院
作者单位1.Capital Univ Med Sci, Coll Pharmaceut Sci, Beijing 100054, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
3.Huamei Pharmaceut Co LTD, Chengdu 610000, Peoples R China
推荐引用方式
GB/T 7714
Wang, C,Zhao, M,Yang, J,et al. Synthesis and evaluations of pentahydroxylhexyl-L-cysteine and its dimer as chelating agents for cadmium or lead decorporation[J]. TOXICOLOGY AND APPLIED PHARMACOLOGY,2004,200(3):229-236.
APA Wang, C,Zhao, M,Yang, J,Li, XW,&Peng, SQ.(2004).Synthesis and evaluations of pentahydroxylhexyl-L-cysteine and its dimer as chelating agents for cadmium or lead decorporation.TOXICOLOGY AND APPLIED PHARMACOLOGY,200(3),229-236.
MLA Wang, C,et al."Synthesis and evaluations of pentahydroxylhexyl-L-cysteine and its dimer as chelating agents for cadmium or lead decorporation".TOXICOLOGY AND APPLIED PHARMACOLOGY 200.3(2004):229-236.
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