Department of Pharmacology, Faculty of Pharmacy, Erciyes University, Kayseri 38039, Turkey.
Nutrients. 2018 May 25;10(6):672. doi: 10.3390/nu10060672.
The aim of this study is to investigate the potential inhibitory effect of α-chaconine and α-solanine on RL95-2 estrogen receptor (ER) positive human endometrial cancer cell line and to identify the effect of these glycoalkaloids on the Akt signaling and ERα. The cell proliferation profiles and the cytotoxicity studies were performed by Real-Time Cell Analyzer (xCELLigence) and compared with Sulphorhodamine B (SRB) assay. The effects of α-chaconine (2.5, 5, 10 µM), α-solanine (20, 30, 50 µM), API-1 (25 µM) and MPP (20 µM) effects on Akt (Ser473) and ERα (Ser167) expressions evaluated by Western blot and qPCR method. Their IC values were as α-chaconine (4.72 µM) < MPP (20.01 µM) < α-solanine (26.27 µM) < API-1 (56.67 µM). 10 μM α-chaconine and 20, 30 and 50 μM α-solanine were effective in decreasing p-Akt(Ser473)/Akt ratio compared to positive control API-1. When the p-ERα/ERα ratios were evaluated, it was observed that α-chaconine (2.5, 5, 10 μM) and α-solanine (50 μM) were as effective as the specific ERα inhibitor MPP in reducing the ratio of p-ERα/ERα compared to the control group. In conclusion, it has been shown that the proliferation of α-chaconine and α-solanine in human endometrial carcinoma cells reduces the expression and activity of the Akt and ERα signaling pathway.
本研究旨在探讨α-茄碱和α-龙葵碱对 RL95-2 雌激素受体（ER）阳性人子宫内膜癌细胞系的潜在抑制作用，并确定这些糖苷生物碱对 Akt 信号和 ERα 的影响。通过实时细胞分析（xCELLigence）和磺酰罗丹明 B（SRB）测定法比较细胞增殖谱和细胞毒性研究。通过 Western blot 和 qPCR 方法评估α-茄碱（2.5、5、10 μM）、α-龙葵碱（20、30、50 μM）、API-1（25 μM）和 MPP（20 μM）对 Akt（Ser473）和 ERα（Ser167）表达的影响。它们的 IC 值分别为α-茄碱（4.72 μM）<MPP（20.01 μM）<α-龙葵碱（26.27 μM）<API-1（56.67 μM）。与阳性对照 API-1 相比，10 μMα-茄碱和 20、30 和 50 μMα-龙葵碱有效降低 p-Akt（Ser473）/Akt 比值。当评估 p-ERα/ERα 比值时，与对照组相比，观察到α-茄碱（2.5、5、10 μM）和α-龙葵碱（50 μM）与特异性 ERα 抑制剂 MPP 一样有效降低 p-ERα/ERα 的比值。总之，研究表明，α-茄碱和α-龙葵碱在人子宫内膜癌细胞中的增殖降低了 Akt 和 ERα 信号通路的表达和活性。
