School of Pharmacy, Anhui Medical University, Mei Shan Road, Anhui Province, 230032 Hefei, PR China.
Biomed Pharmacother. 2013 Oct;67(8):687-92. doi: 10.1016/j.biopha.2013.05.001. Epub 2013 Jun 11.
4-Amino-2-Trifluoromethyl-Phenyl Retinate (ATPR) is one of the retinoid derivatives designed and synthesized in our team. In this paper, we explored the potential anti-tumor effects of ATPR in breast cancer. Here we found that ATPR showed remarkable anti-proliferative effects in a dose- and time-dependent manner, caused cell cycle arrest in the G0/G1 phase and significantly increased the expression of retinoid receptor-induced gene-1 (RRIG1). ATPR decreased the expression of phosphorylation-ERK (p-ERK) and increased the expression of estrogen receptor β (ERβ) and phosphorylation-p38 (p-p38). Following RRIG1 knockdown by RNAi interference, we found that the changes of ERβ, p-ERK and p-p38 induced by ATPR were both depressed. Our data suggest that ATPR could inhibit the proliferation and induce differentiation of MCF-7 cells via mediating the expression of RRIG1.
4-氨基-2-三氟甲基-苯维甲酸酯（ATPR）是本团队设计和合成的一种类视黄醇衍生物。在本文中，我们探讨了 ATPR 在乳腺癌中的潜在抗肿瘤作用。结果发现，ATPR 呈剂量和时间依赖性显著抑制增殖，使细胞周期阻滞于 G0/G1 期，并显著增加视黄醇受体诱导基因-1（RRIG1）的表达。ATPR 降低磷酸化 ERK（p-ERK）的表达，增加雌激素受体β（ERβ）和磷酸化 p38（p-p38）的表达。用 RNAi 干扰敲低 RRIG1 后，我们发现 ATPR 诱导的 ERβ、p-ERK 和 p-p38 的变化均受到抑制。我们的数据表明，ATPR 可能通过调节 RRIG1 的表达来抑制 MCF-7 细胞的增殖并诱导其分化。
