41164-35-6Relevant academic research and scientific papers
Immunosensors for estradiol and ethinylestradiol based on new synthetic estrogen derivatives: Application to wastewater analysis
Kanso, Hussein,Barthelmebs, Lise,Inguimbert, Nicolas,Noguer, Thierry
, p. 2397 - 2404 (2013)
Novel electrochemical immunosensors for sensitive detection of 17-β estradiol (E2) and ethinylestradiol (EE2) are described on the basis of the use of magnetic beads (MBs) as solid support and screen-printed electrodes as sensing platforms. Four synthetic estrogen derivatives containing either a carboxylic group or an amine group at the C-3 position were synthesized and covalently bound to MBs functionalized with amine or carboxyl groups, respectively. The assay was based on competition between the free and immobilized estrogen for the binding sites of the primary antibody, with subsequent revelation using alkaline phosphatase-labeled secondary antibody. Preliminary colorimetric tests were performed in order to validate the applicability of the synthetic estrogens to immuno-recognition and to optimize different experimental parameters. In a second step, electrochemical detection was carried out by square wave voltammetry (SWV). Under the optimized working conditions, the electrochemical immunosensors showed a highly sensitive response to E2 and EE2, with respective detection limits of 1 and 10 ng/L. Cross-reactivity evaluated against other hormones demonstrated an excellent selectivity. The developed devices were successfully applied to analysis of spiked and natural water samples. These new immunosensors offer the advantages of being highly sensitive, easy, and rapid to prepare, with a short assay time.
N omega-Asp-N alpha-(17 beta-estradiol-3-acetyl)-Lys, as well as preparation, activity and application thereof
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Paragraph 0019; 0020, (2019/07/08)
The invention discloses N omega-Asp-N alpha-(17 beta-estradiol-3-acetyl)-Lys having the formula in the specification, a preparation method thereof, a stepwise stability constant of the N omega-Asp-N alpha-(17 beta-estradiol-3-acetyl)-Lys complexed with Ca
1-asparaginic acid conjugate-3-estrone and preparation, nano structure, anti-osteoporosis activity and application thereof
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Paragraph 0019; 0020, (2018/04/03)
The invention discloses 1-molecule asparaginic acid conjugate 3-molecule estradiol compound (called 1-asparaginic acid conjugate-3-estrone for short) which is shown in a following formula, discloses apreparation thereof, discloses a nano structure thereof and further discloses an anti-osteoporosis effect thereof on a chemical-castration female mouse osteoporosis model. Therefore, the invention discloses an application prospect thereof in preparing anti-osteoporosis medicine. The formula is shown in the description.
3D QSAR of novel estrogen-RGD peptide conjugates: Getting insight into structural dependence of anti-osteoporosis activity and side effect of estrogen in ERT
Zhao, Ming,Liu, Jiangyuan,Zhang, Xiaoyi,Peng, Li,Li, Chunyu,Peng, Shiqi
supporting information; experimental part, p. 3680 - 3689 (2009/10/17)
To explore the structural dependence of the oral potency and side effect of estrogen-RGD peptide conjugates, here six novel conjugates were prepared via introducing RGD-tetrapeptides into both 3- and 17-positions of estradiol, and introducing RGD-octapept
Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity
Liu, Jiangyuan,Zhang, Xiaoyi,Zhao, Ming,Peng, Shiqi
experimental part, p. 1689 - 1704 (2009/05/26)
To enhance the potency, reduce the side effects and improve oral property of estradiol in estrogen replacement therapy (ERT), 6 novel estradiol-RGD octapeptide conjugates have been prepared. In an ovariectomized mouse osteoporotic model, at an oral dosage
Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates
Xiong, Yu,Zhao, Ming,Wang, Chao,Heng, Wei Chang,Peng, Shiqi
, p. 3340 - 3353 (2008/02/12)
To improve the specificity and potency of estrogen replacement therapy therapeutics while also minimizing the side effects such as bone resorption and thickening of the uterine wall, a series of novel estrogen-derived conjugates estradiol-3-RGD, estradiol
