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Cellular uptake and toxicity study of cis-bis(6-aminoquinoline) dichloroplatinum (II).
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 1991-06-01 , DOI: 10.1016/0162-0134(91)84037-a
M Q Lu 1 , J C Chang , B L Bergquist
Affiliation  

A fluorescent analog of cis-diamminedichloroplatinum(II), cis-bis(6-aminoquinoline)dichloroplatinum(II), was prepared from K2[PtCl4] and 6-aminoquinoline (AQL). HPLC of the thiourea derivative of the new complex showed that it has the cis-configuration. The Pt-AQL complex and the parent ligand AQL were evaluated for biological activity and cellular uptake, using the ciliate Tetrahymena pigmentosa. The complex was relatively nontoxic at the tested levels below 5 x 10(-4) M, but did exhibit inhibition of culture growth at 5 x 10(-4) M. Measurement of cellular uptake of the Pt-AQL complex demonstrated incorporation into the cell, with localization primarily within the vacuoles of the cells. Comparable measurement of the parent ligand AQL showed little measurable cellular uptake.

中文翻译:

顺式双(6-氨基喹啉)二氯铂(II)的细胞吸收和毒性研究。

从K2 [PtCl4]和6-氨基喹啉(AQL)制备了顺式二甲基二氯铂(II)的荧光类似物,即顺式双(6-氨基喹啉)二氯铂(II)。新的配合物的硫脲衍生物的HPLC显示其具有顺式构型。使用纤毛四膜虫评估了Pt-AQL复合物和母体配体AQL的生物活性和细胞摄取。在低于5 x 10(-4)M的测试水平下,该复合物相对无毒,但在5 x 10(-4)M时却显示出对培养物生长的抑制作用。对Pt-AQL复合物细胞摄取的测量表明,该复合物可掺入细胞,主要定位在细胞的液泡内。母体配体AQL的可比测量显示几乎没有可测量的细胞摄取。
更新日期:2019-11-01
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