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
|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|
|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).|
|Source||Sci Rep (2016). Figure 4. 2-methoxyestradiol (2-ME) was purchased from Abmole|
|Method||in vivo experiment|
|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).|
|Source||Sci Rep (2016). Figure 3. 2-methoxyestradiol (2-ME) was purchased from Abmole|
|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 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 (LGC Promochem, Teddington, UK). 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%) from Sigma 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.
|Incubation time||18 h|
|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|
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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