Mestranol - CAS 72-33-3
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Not Intended for Therapeutic Use. For research use only.
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Estrogen Receptor/ERR
Mestranol is the 3-methyl ether of ethinylestradiol. It was the estrogen used in many of the first oral contraceptives.
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1.Parent and conjugated estrogens and progestagens in surface water of the Santa Ana River: Determination, occurrence and risk assessment.
Ma L1,2, Yates SR2, Ashworth D1,2. Environ Toxicol Chem. 2016 Apr 6. doi: 10.1002/etc.3447. [Epub ahead of print]
This present study investigated the occurrence of 13 parent and conjugated estrogens and progestagens in surface water of the Santa Ana River. With the exception of the synthetic hormones 17 α-ethynylestradiol and mestranol, other compounds were detected at least twice at 10 representative sites, with the ubiquitous estrone (E1) and 17β-estradiol-3-sulfate as the dominant compounds quantified (0.24-6.37 ng/L and 0.49-9.25 ng/L, respectively). Sites near dairy farms exhibited high levels of conjugates while those close to a sewage treatment plant (STP) effluent outlet displayed relatively high concentrations of E1. Principle component analysis coupled with multiple linear regression revealed dairy farms and the STP as the 2 significant contamination sources, accounting for 69.9 and 31.1% of the total hormone burden, respectively. Risk assessment results suggested E1 and 17β-estradiol (E2) as the 2 hormones with largest risks to aquatic organisms, and which combined, contributed >90% of the total estrogenicity.
2.Effect of CYP2C9 Genetic Polymorphism in a Chinese Population on the Metabolism of Mestranol in vitro.
Hu JH1, Wang L, Li WS, Dai DP, Cai JP, Hu GX. Pharmacology. 2015;95(5-6):218-23. doi: 10.1159/000381189. Epub 2015 Apr 25.
BACKGROUND: Mestranol is a widely used estrogen, which is converted into its active metabolite ethinyl estradiol by cytochrome P450 (CYP) 2C9. To comprehensively examine the enzymatic activity of reported CYP2C9 variants in Chinese individuals in response to mestranol, wild-type CYP2C9*1 and 35 allelic variants were highly expressed in Sf21 insect cell microsomes and used for the detection of their enzymatic values in vitro. These results showed that the majority of tested variants exhibited decreased clearance values compared to wild type, except for CYP2C9*40 and *36.
3.Trace analysis of selected hormones and sterols in river sediments by liquid chromatography-atmospheric pressure chemical ionization-tandem mass spectrometry.
Matić I1, Grujić S2, Jauković Z2, Laušević M2. J Chromatogr A. 2014 Oct 17;1364:117-27. doi: 10.1016/j.chroma.2014.08.061. Epub 2014 Aug 26.
In this paper, development and optimization of new LC-MS method for determination of twenty selected hormones, human/animal and plant sterols in river sediments were described. Sediment samples were prepared using ultrasonic extraction and clean up with silica gel/anhydrous sodium sulphate cartridge. Extracts were analyzed by liquid chromatography-linear ion trap-tandem mass spectrometry, with atmospheric pressure chemical ionization. The optimized extraction parameters were extraction solvent (methanol), weight of the sediment (2 g) and time of ultrasonic extraction (3× 10 min). Successful chromatographic separation of hormones (estriol and estrone, 17α- and 17β-estradiol) and four human/animal sterols (epicoprostanol, coprostanol, α-cholestanol and β-cholestanol) that have identical fragmentation reactions was achieved. The developed and optimized method provided high recoveries (73-118%), low limits of detection (0.8-18 ng g(-1)) and quantification (2.
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