Estriol is a G-protein coupled estrogen receptor antagonist. It is one of the three main estrogens produced by the human body. It can be a weak or strong estrogen depending on if it is given acutely or chronically when given to immature animals, but is an antagonist when given in combination with estradiol. It may play a role in the development of breast cancer, but based on in vitro research does appear to act as an antagonist to the G-protein coupled estrogen receptor
Expert Opin Ther Targets. 2020 Apr;24(4):389-402.
Cepharanthine hydrochloride induces mitophagy targeting GPR30 in hepatocellular carcinoma (HCC)
Estriol purchased from AbMole
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Source | Expert Opinion on Therapeutic Targets 2020 Apr. Figure 4. Estriol (Abmole Bioscience, USA) |
| Method | Western blotting | |
| Cell Lines | Huh7 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 12 h | |
| Results | Furthermore, in Huh7 and HepG2 cells, increased p-DRP1 induced by CH can be reduced by Estriol (E3), which is an inhibitor of GPR30, thus suggesting that CH may play an estrogen-like role in activating the GPR30 signaling cascade in HCC cells. |
| Cell Experiment | |
|---|---|
| Cell lines | SkBr3 cells |
| Preparation method | For the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, culturing cells in 96-well plates under 200 μL of growth medium and at an initial density of 10,000 cells per well. Washing cells once they have attached and further incubated in medium which contains 2.5% charcoal-stripped FBS with the indicated treatment. Changing the medium every 2 days (with treatment). Where applicable,transfecting 200 ng of the indicated plasmids every 2 days before treatments using Fugene6 Reagent, as recommended by the manufacturer. Following 6 days of incubation, adding the assay mixture (10µL per well) which contains 1mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to each well and incubated at 37 ◦C for 4 h in a 5% CO2 atmosphere. The yellow tetrazolium MTT, reduced by metabolically active cells, results in intracellular purple formazan, which is released after overnight incubation with 200 µL 1% sodium dodecyl sulfate in 0.01N HCL and quantified spectrophotometrically by reading absorbance at 570nm using an enzyme-linked immunosorbent assay plate reader. |
| Concentrations | ~100 nM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | mPTEN+/- and wild-type mice |
| Formulation | Estriol is dissolved in ethanol and corn oil. |
| Dosages | 4 μg/g/day |
| Administration | Administrated via s.c.SkBr3 细胞 |
| Molecular Weight | 288.39 |
| Formula | C18H24O3 |
| CAS Number | 50-27-1 |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
[1] Emad S Ali, et al. Estriol: emerging clinical benefits
[2] M Taylor. Unconventional estrogens: estriol, biest, and triest
[3] G P Vooijs, et al. Review of the endometrial safety during intravaginal treatment with estriol
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