Su Bin, Mershon Serena M, Stonerock Laura A, Curley Robert W, Brueggemeier Robert W
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500W. 12th Avenue, Columbus, OH 43210, USA.
J Steroid Biochem Mol Biol. 2008 Mar;109(1-2):40-6. doi: 10.1016/j.jsbmb.2007.12.005. Epub 2007 Dec 7.
Recent studies exhibit that 4-hydroxyphenylretinamide (4HPR) decreases aromatase activity in breast and placental cells. The effect of synthetic 4HPR analogs on aromatase and expression was examined in three breast cancer cell lines. Most derivatives did not decrease cellular aromatase activity. Two of the analogs even stimulated aromatase activity at the transcriptional level. Only one derivative significantly decreased aromatase in all three breast cancer cell lines and also suppressed CYP19 gene expression in one of the cell line. Placental microsomal aromatase assay rule out the possibility that this compound directly inhibits the aromatase enzyme. A non-genomic mechanism in suppression of cellular aromatase activity of this compound is proposed.
最近的研究表明，4-羟基苯基视黄酸（4HPR）可降低乳腺和胎盘细胞中的芳香化酶活性。在三种乳腺癌细胞系中检测了合成的4HPR类似物对芳香化酶及其表达的影响。大多数衍生物并未降低细胞芳香化酶活性。其中两种类似物甚至在转录水平上刺激了芳香化酶活性。只有一种衍生物在所有三种乳腺癌细胞系中均显著降低了芳香化酶活性，并且在其中一种细胞系中还抑制了CYP19基因的表达。胎盘微粒体芳香化酶测定排除了该化合物直接抑制芳香化酶的可能性。提出了一种抑制该化合物细胞芳香化酶活性的非基因组机制。
