MPP dihydrochloride is a selective estrogen receptor α (ERα) antagonist [1]. MPP dihydrochloride blocks estrogen signaling, thereby inducing cell apoptosis [2]. MPP dihydrochloride is used to treat cancer [3].
In MCF-7 cells, MPP dihydrochloride (5μM, 15μM, 20μM; 1h) treatment dose-dependently enhanced silibinin-induced growth inhibition of cells [4]. In SKOV3 cells, MPP dihydrochloride (20μM; 24h) treatment significantly increased the number of cells [5]. In SKOV3 and OV2008 Cells, MPP dihydrochloride (10pM, 100pM, 1000pM; 24h) treatment significantly inhibited cell growth in both cell lines [6]. In ectopic endometrial stromal cells (eESCs), MPP dihydrochloride (2.7nM; 48h) treatment increases the autophagy level in eESCs [7].
In SKOV3 cell subcutaneous tumor mice model, MPP dihydrochloride (1mg/kg; ip; 35d) treatments reduce in vivo tumor cell growth in mice [6]. In SERT+ mice, MPP dihydrochloride (2mg/kg; sc; 14d) attenuates the development of pulmonary hypertension (PH) in normoxic and hypoxic female SERT+ mice [8]. In C57/BL6 mice, MPP dihydrochloride (200μg/kg; ip; 7d) treatment significantly reduced the expression of rictor, p-AKT(Ser473)/AKT, p-cofilin (Ser3), and profilin-1 [9].
References:
[1]. Tskitishvili E, Pequeux C, Munaut C, et al. Estrogen receptors and estetrol-dependent neuroprotective actions: a pilot study. The Journal of Endocrinology. 2016 Nov 17; 232(1): 85.
[2]. Liu X, Fan XL, Zhao Y, et al. Estrogen provides neuroprotection against activated microglia‐induced dopaminergic neuronal injury through both estrogen receptor‐α and estrogen receptor‐β in microglia. Journal of neuroscience research. 2005 Sep 1; 81(5): 653-665.
[3]. Karaboğa Arslan AK, Yerer MB. α-Chaconine and α-Solanine inhibit RL95-2 endometrium cancer cell proliferation by reducing expression of Akt (Ser473) and ERα (Ser167). Nutrients. 2018 May 25; 10(6): 672.
[4]. Zheng N, Zhang P, Huang H, et al. ERα down-regulation plays a key role in silibinin-induced autophagy and apoptosis in human breast cancer MCF-7 cells. Journal of pharmacological sciences. 2015 Jul 1; 128(3): 97-107.
[5]. Yan Y, Jiang X, Zhao Y, et al. Role of GPER on proliferation, migration and invasion in ligand‐independent manner in human ovarian cancer cell line SKOV3. Cell biochemistry and function. 2015 Dec; 33(8): 552-559.
[6]. Chan KK, Leung TH, Chan DW, et al. Targeting estrogen receptor subtypes (ERa and ERb) with selective ER modulators in ovarian cancer. J. Endocrinol. 2014; 221: 325-336.
[7]. Zhang B, Zhou WJ, Gu CJ, et al. The ginsenoside PPD exerts anti-endometriosis effects by suppressing estrogen receptor-mediated inhibition of endometrial stromal cell autophagy and NK cell cytotoxicity. Cell death & disease. 2018 May 14; 9(5): 574.
[8]. Wright AF, Ewart MA, Mair K, et al. Oestrogen receptor alpha in pulmonary hypertension. Cardiovascular research. 2015 May 1; 106(2): 206-216.
[9]. Xing FZ, Zhao YG, Zhang YY, et al. Nuclear and membrane estrogen receptor antagonists induce similar mTORC 2 activation‐reversible changes in synaptic protein expression and actin polymerization in the mouse hippocampus. CNS neuroscience & therapeutics. 2018 Jun; 24(6): 495-507.
MPP dihydrochloride是一种选择性雌激素受体α（ERα）拮抗剂 [1]。MPP dihydrochloride可阻断雌激素信号传导，从而诱导细胞凋亡 [2]。MPP dihydrochloride用于治疗癌症 [3]。
在MCF-7细胞中，MPP dihydrochloride（5μM、15μM、20μM；1h）处理剂量依赖性地增强了水飞蓟宾诱导的细胞生长抑制作用 [4]。在SKOV3细胞中，MPP dihydrochloride（20μM；24h）处理显著增加了细胞数量 [5]。在SKOV3和OV2008细胞中，MPP dihydrochloride（10pM、100pM、1000pM；24h）处理显著抑制了这两种细胞系的细胞生长 [6]。在异位子宫内膜基质细胞（eESC）中，MPP dihydrochloride （2.7nM；48和）治疗可提高eESC的自噬水平 [7]。
在SKOV3细胞皮下肿瘤小鼠模型中，MPP dihydrochloride（1mg/kg；ip；35d）治疗可降低小鼠体内肿瘤细胞的生长 [6]。在SERT+小鼠中，MPP dihydrochloride（2mg/kg；sc；14d）可减轻常氧和缺氧雌性SERT+小鼠的肺动脉高压（PH）发展 [8]。在C57/BL6小鼠中，MPP dihydrochloride（200μg/kg；ip；7d）治疗可显著降低rictor、p-AKT（Ser473）/AKT、p-cofilin（Ser3）和profilin-1的表达 [9]。