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Structure-activity Relationships for Unsaturated Dialdehydes. V. Estimation of the Lipophilicity of Nineteen Sesquiterpenoid Unsaturated Dialdehydes, and Determination of their Chemical Stability in Three In Vitro Assay Media
Alternatives to Laboratory Animals ( IF 2.7 ) Pub Date : 1991-04-01 , DOI: 10.1177/026119299101900203
Olov Sterner 1 , Marianne Andersson 2 , Anna Forsby 2 , Paloma Morales 1
Affiliation  

The lipophilicity, expressed as log P, has been estimated for 19 sesquiterpenoid unsaturated dialdehydes by the determination of the 1-octanol/water partition coefficient for 12 of the compounds, and the reversed-phase HPLC retention data for all the compounds. The log P values obtained varied between 0.5 and 3.02. The stability of 17 unsaturated dialdehydes in three common in vitro assay media at 37°C was investigated by HPLC analysis of samples dissolved in the media. All compounds investigated were essentially stable for up to 24 hours in a phosphate buffered saline, while several of them disappeared rapidly in media containing amino acids and fetal calf serum. This chemical instability must be considered when results from biological assays of unsaturated dialdehydes are compared.

中文翻译:

不饱和二醛的构效关系。V. 19 种倍半萜类不饱和二醛亲脂性的估计,以及它们在三种体外测定介质中的化学稳定性的测定

通过确定 12 种化合物的 1-辛醇/水分配系数和所有化合物的反相 HPLC 保留数据,已估计出 19 种倍半萜类不饱和二醛的亲脂性,以 log P 表示。获得的 log P 值在 0.5 和 3.02 之间变化。通过 HPLC 分析溶解在介质中的样品,研究了 17 种不饱和二醛在 37°C 下在三种常见体外测定介质中的稳定性。研究的所有化合物在磷酸盐缓冲盐水中基本上稳定长达 24 小时,而其中一些化合物在含有氨基酸和胎牛血清的培养基中迅速消失。当比较不饱和二醛的生物测定结果时,必须考虑这种化学不稳定性。
更新日期:1991-04-01
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