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2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa.
Sci Rep. 2016 Jul 1;6:28612.
Inhibition of hypoxia inducible factor-1α attenuates abdominal aortic aneurysm progression through the down-regulation of matrix metalloproteinases.
2-Methoxyestradiol purchased from AbMole
_figure5_2-methoxyestradiol(2-me).jpg) |
Source | Sci Rep (2016). Figure 5. 2-methoxyestradiol (2-ME) was purchased from Abmole |
| Method | CHIP assay and Immunohistochemistry staining | |
| Cell Lines | in vivo experiment | |
| Concentrations | 25mg/kg daily | |
| Incubation Time | 30 days | |
| Results | Administration of 2-ME and digoxin significantly decreased AngII- mediated HIF-1α, VEGF, MMP-2 and MMP-9 overexpression in the homogenates of the whole aortas, as shown in Fig. 5A. 2-ME and digoxin decreased the AngII induced HIF-1α levels accumulation and elastin degradation in the aorta (Fig. 5B). |
_figure4_2-methoxyestradiol(2-me).jpg) |
Source | Sci Rep (2016). Figure 4. 2-methoxyestradiol (2-ME) was purchased from Abmole |
| Method | in vivo experiment | |
| Cell Lines | ||
| Concentrations | 25mg/kg daily | |
| Incubation Time | 30 days | |
| Results | Both non-selective HIF-1α inhibitors 2-ME (25 mg/kg/day, s.c.) and digoxin (1.25 mg/kg/day, i.p.) significantly improved the survival rates (log rank test, n= 20 in each group, p < 0.05, Fig. 4B); decreased the incidences of AAA (0% vs. 84% vs. 35%, vs. 40%, p < 0.01, Fig. 4C), the severities of AAA, in terms of less type III and type IV lesions (43% vs. 15%, vs. 15%, p < 0.05, Fig. 4D) and the external diameters of the aorta (0.67 ± 0.11 mm vs. 1.68.± 0.77 vs. 0.96± 0.30 vs. 1.10± 0.53 mm, p< 0.05, Fig. 4E). |
_figure3_2-methoxyestradiol(2-me).jpg) |
Source | Sci Rep (2016). Figure 3. 2-methoxyestradiol (2-ME) was purchased from Abmole |
| Method | CHIP assay | |
| Cell Lines | HAECs | |
| Concentrations | 6 μM | |
| Incubation Time | 30 min | |
| Results | We found that both 2-ME and digoxin attenuated AngII and oxPAPC induced up-regulation of MMP-2 and MMP-9 (n = 5, Fig. 3) |
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 and MDA-MB-231 cells |
| Preparation method | Cell culture and cell treatment. MCF-7 estrogen receptor-positive (ER+ve) human breast cancer cells, MDA-MB-231 ER-negative (ER−ve) human breast cancer cells were obtained from the American Type Culture Collection. Cells were routinely cultured in RPMI-1640 medium supplemented with 10% (v/v) fetal calf serum, 1% L-glutamine (200 mM), 1% non-essential amino acids (100 ×) and 1% bicarbonate (7.5%) and maintained in a humidified incubator under 5% CO2 atmosphere at 37°C. For experiments using hypoxic conditions, cells were incubated under 1% O2 and 5% CO2 atmosphere at 37°C. |
| Concentrations | 0.5 μM |
| Incubation time | 18 h |
| Animal Experiment | |
|---|---|
| Animal models | mice bearing MCF-7 and MDA-MB-231 xenografts model |
| Formulation | 10% tetrahydrofuran: 90% propylene glycol |
| Dosages | 40 or 75 mg/kg |
| Administration | orally daily for 28 days |
| Molecular Weight | 302.41 |
| Formula | C19H26O3 |
| CAS Number | 362-07-2 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Lakhani NJ, et al. Pharmacotherapy. 2-Methoxyestradiol, a promising anticancer agent.
| Related HIF Products |
|---|
| FG-4592 (Roxadustat)
FG-4592 (Roxadustat; ASP1517) is a novel Hypoxia Inducible Factor Prolyl Hydroxylase inhibitor. |
| DMOG
DMOG (Dimethyloxaloyl glycine) is an antagonist of α-ketoglutarate cofactor and a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy. |
| IOX2
IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. |
| Hydralazine hydrochloride
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM. |
| Paeoniflorin
Paeoniflorin is a glycoside isolated from the root of Paeonia lactiflora. Paeoniflorin has been used as an anticonvulsant and has hypoglycemic effect. |
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