Tretinoin 是维生素A的代谢产物，结合并激活视黄酸受体，从而诱导基因表达的变化，导致细胞分化、细胞增殖减少和肿瘤发生的抑制。它是RAR核受体的天然激动剂，对RARα/β/γ的IC50为14 nM，与PPARβ/δ结合的Kd值为17 nM。

Tretinoin binds to and activates retinoic acid receptors (RARs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of tumorigenesis. This agent also inhibits telomerase, resulting in telomere shortening and eventual apoptosis of some tumor cell types. Tretinoin is a naturally-occurring acid of retinol. The oral form of tretinoin has teratogenic and embryotoxic properties.

Tretinoin可以防止皮质类固醇诱导的无毛小鼠皮肤萎缩.在豚鼠体内,Tretinoin与咪喹莫特联用可使之出现组织病理学上的纹身褪色和中度的色素清除.在45 CD-1小鼠的皮肤切口上,Tretinoin使成纤维细胞分化增加,胶原蛋白产生量减少.与对照组老年大鼠相比,Tretinoin处理的老年雄性Fischer 344大鼠肾皮质中蛋白质含量低30%,这可能是因为其抑制了肿瘤坏死因子-β1和骨桥蛋白的表达.

在对谷胱甘肽含量和过氧化氢酶活性影响的研究中,Tretinoin以时间和剂量依赖的方式增加对应含量和活性,对人肾小球系膜细胞中的H2O2细胞毒性具有预防和降低作用。用Tretinoin培育系膜细胞,可使过氧化氢酶以及γ-谷酰基-半胱氨酸合成酶(催化亚基,还原型谷胱甘肽合成的限速步骤)mRNA水平的增加。此外,Tretinoin可使人瘢痕疙瘩衍生的成纤维细胞中基质金属蛋白酶-8/13上调。

Retinoic acid is dissolved in DMSO and stored, and then diluted with appropriate medium before use[3]. P19 cell are induced to undergo neuronal differentiation according to established procedures. Briefly, cells are cultured on 1% agarose-coated 10 cm dishes at 3×10 5 cells/mL in α-minimal essential medium supplemented with 10% FBS. Differentiation is induced by addition of Retinoic acid (1 μM) and medium containing Retinoic acid replaced 2 days later. On day 4, cell aggregates are collected by centrifugation, separated to single cells by trypsin/EDTA treatment, replated onto poly-L-lysine-coated plates, and cultured in α-minimal essential medium supplemented with 10% FBS. On day 6, medium is replaced with neurobasal medium containing B27 supplement and 2 mM GlutaMAX. Medium is replaced every 2 days for an additional week[3].

302-79-4

C20H28O2

300.442

维A酸;all-trans-Retinoic acid;ATRA;Vitamin A acid;维生素A酸;Tretinoin

Ethanol:6 mg/mL (19.97 mM)
H2O:<1 mgml
DMSO:56 mg/mL (186.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years