The growth-supporting activity of a retinoidal benzoic acid derivative and 4,4-difluororetinoic acid.
The growth-supporting activity of a retinoidal benzoic acid derivative and 4,4-difluororetinoic acid.
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视黄醛苯甲酸衍生物和 4,4-二氟视黄酸的生长支持活性。
DOI：
10.1016/0003-9861(85)90248-6
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发表时间：
1985
影响因子：
3.9
通讯作者：
DeLuca,HF
中科院分区：
文献类型：
--
作者：
Stephens-Jarnagin,A;Miller,DA;DeLuca,HF
研究了两种合成类维生素A支持雄性维生素A缺乏大鼠生长的能力。发现其中一种化合物（E）-4-[2-（5，6，7，8-四氢-5，5，8，8-四甲基-2-萘基）-1-丙烯基]-苯甲酸（TTNPB）非常有效;其活性是全反式视黄酸的35倍。因此，体内结果与先前研究者发表的该化合物的体外活性一致，并支持该化合物可用于确定类维生素A作用的分子机制的观点。另一种类似物4，4-二氟维甲酸的有效性仅为维甲酸的12%。然而，该化合物可能的不稳定性和氟基团的电负性禁止了关于视黄酸4位代谢修饰的生物学功能的结论。
Two synthetic retinoids were examined for their ability to support growth in male vitamin A-deficient rats. One of the compounds, (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl]-benzoic acid (TTNPB), was found to be highly effective; it was 35-fold more active than all-trans-retinoic acid. Thus, thein vivoresults were in agreement with thein vitroactivity of this compound published by previous investigators, and support the view that this compound may be useful in determining the molecular mechanism of action of the retinoids. Another analog, 4,4-difluororetinoic acid, was only 12% as effective as retinoic acid. However, the possible instability of this compound and the electronegativity of the fluoro groups prohibited conclusions concerning the biological function of metabolic modification on the 4 position of retinoic acid.