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2,2'-5,5'-四氯联苯的4-位和4,4'-位含硫取代衍生物在小鼠体内的支气管黏膜和肾皮质亲和力

Bronchial mucosal and kidney cortex affinity of 4- and 4,4'-substituted sulphur-containing derivatives of 2,2'-5,5'-tetrachlorobiphenyl in mice.

作者信息

Brandt I, Bergman A

出版信息

Chem Biol Interact. 1981 Feb;34(1):47-55. doi: 10.1016/0009-2797(81)90089-2.

Abstract

In order to evaluate further the structural requirements previously proposed for accumulation of polychlorinated biphenyls (PCB) and their sulphur-containing metabolites in the respiratory tract of mice, 4-methylthio-, 4-methylsulphonyl and 4,4'-bis(methylthio)-2,2',5,5'-[14C] tetrachlorobiphenyl were studied by whole body autoradiography. All the compounds gave rise to a strong accumulation of radioactivity in the mucosa of the bronchi, trachea and larynx. The first two substances were also concentrated in the mucosa of the nasal cavities. At the longer post-injection times all the compounds studied were localized in distinct sites of the kidney cortex. However, while the uptake of the monosubstituted sulphur-containing tetrachlorobiphenyl metabolites there was comparatively weak, the bis(methylthio) derivative showed a remarkable accumulation and retention in the kidney cortex. The study makes it possible to formulate the structural requirements for bronchial accumulation on the basis of the structure of the compounds that are accumulated rather than on the structure of the unmetabolized polychlorobiphenyls. Also with regard to the uptake in the kidney cortex a specific structure-dependency seems to exist.

摘要

为了进一步评估先前提出的多氯联苯(PCB)及其含硫代谢物在小鼠呼吸道蓄积的结构要求,通过全身放射自显影术对4-甲硫基-、4-甲磺酰基和4,4'-双(甲硫基)-2,2',5,5'-[¹⁴C]四氯联苯进行了研究。所有这些化合物在支气管、气管和喉的黏膜中都引起了强烈的放射性蓄积。前两种物质也在鼻腔黏膜中富集。在注射后较长时间,所有研究的化合物都定位于肾皮质的不同部位。然而,虽然含硫单取代四氯联苯代谢物在那里的摄取相对较弱,但双(甲硫基)衍生物在肾皮质中显示出显著的蓄积和滞留。该研究使得能够根据蓄积化合物的结构而非未代谢多氯联苯的结构来制定支气管蓄积的结构要求。关于在肾皮质中的摄取,似乎也存在特定的结构依赖性。

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