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Design and synthesis of pentahydroxylhexylamino acids and their effect on lead decorporation
Wang, Yuji1; Bi, Lanrong1; Hou, Baoguang1; Chen, Yu1; Zhao, Ming1; Wang, Chao1; Wang, Wei1; Ju, Jingfang1; Peng, Shiqi1
刊名CHEMICAL RESEARCH IN TOXICOLOGY
2007-04-01
DOI10.1021/tx6003437
20期:4页:609-615
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Toxicology
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry ; Toxicology
关键词[WOS]CHELATING-AGENTS ; MESO-2,3-DIMERCAPTOSUCCINIC ACID ; CACO-2 CELLS ; CADMIUM ; MOBILIZATION ; PERMEABILITY ; INTOXICATION ; ABSORPTION ; RATS ; MICE
英文摘要

A series of enantiopure pentahydroxylhexylamino acids 4a-t were synthesized via an improved one-pot-three-step procedure. Their potential as antagonists for lead intoxication was investigated both in vitro and in vivo. Lead decorporation assays in vivo confirmed that after treatment with 4a-t, the levels of lead in treated mice were significantly reduced in the liver, kidney, bone, and brain compared to those in the control group. In addition, the lead levels in feces and urine were significantly higher after treatment with 4a-t than those of the control group. In particular, the lead decorporation potency of compounds 4b, 4i, 4j, and 4s were comparable or better than that of DL-penicillamine. Furthermore, new chelating agents did not affect the levels of endogenous essential metals. The stability constants of the formed lead complexes of 4a-t were determined by potentiometric titration. It seems that the therapeutic efficiency of the lead chelating agents depends on factors that affect the stability constants of the formed lead complexes. The membrane permeability of representative compounds was evaluated in a Caco-2 cell monolayer. A good correlation between in vitro results and in vivo lead decorporation capacity of the chelating agents was observed. Some of these new pentahydroxylhexylamino acids (4, 4i, 4j, and 4s) may be developed as effective lead chelating agents.

语种英语
WOS记录号WOS:000245690100008
引用统计
被引频次:7[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/400002259/53179
专题北京大学药学院
作者单位1.Mitchell Canc Inst, Mobile, AL 36688 USA
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
3.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
4.Capital Med Univ, Sch Publ Hlth & Family Med, Beijing 100069, Peoples R China
推荐引用方式
GB/T 7714
Wang, Yuji,Bi, Lanrong,Hou, Baoguang,et al. Design and synthesis of pentahydroxylhexylamino acids and their effect on lead decorporation[J]. CHEMICAL RESEARCH IN TOXICOLOGY,2007,20(4):609-615.
APA Wang, Yuji.,Bi, Lanrong.,Hou, Baoguang.,Chen, Yu.,Zhao, Ming.,...&Peng, Shiqi.(2007).Design and synthesis of pentahydroxylhexylamino acids and their effect on lead decorporation.CHEMICAL RESEARCH IN TOXICOLOGY,20(4),609-615.
MLA Wang, Yuji,et al."Design and synthesis of pentahydroxylhexylamino acids and their effect on lead decorporation".CHEMICAL RESEARCH IN TOXICOLOGY 20.4(2007):609-615.
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