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estradiol acetate (Menoring / Femring / Estrace VR)

✓ Approved

Actavis · ESR1 · 小分子

什么是 estradiol acetate？

estradiol acetate 是一种小分子，由Actavis研发。该药已获批，用于治疗相关适应症，给药途径：Intravaginal、Surgical Implantation。

药物档案

商品名Menoring, Femring, Estrace VR
公司Actavis
药物类别小分子
分子靶点ESR1
给药途径Intravaginal, Surgical Implantation
状态Approved
来源： ClinicalTrials.gov, Actavis

作用机制

分子靶点

estradiol acetate 作用于 1 个分子靶点：

ESR1estrogen receptor 1 (ER, ESR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

estradiol acetate 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Surgical and medical proceduresHormone replacement therapy✓ Approved

相关研究文献

PubMedMolecular imaging and biology2026-09-11

Macrocycle Chelator Conjugation on the C3 Hydroxyl Group of 17β-Estradiol reduces Estrogen Receptor Binding.

Cheung Pierre P, Pandrala Mallesh M, Moses Abraham A, Landry Madeleine M et al.

Tumor heterogeneity in breast cancer complicates accurate molecular characterization when using standard-of-care imaging modalities. In this study, gallium-68 labeled estradiol-derivatives were synthesized and evaluated as candidate tracers to be used for multiplexed PET imaging with the goal of improving the molecular characterization of breast cancer. 17β-estradiol was conjugated to DOTA and NODAGA macrocycles and radiolabeled with gallium-68. The selectivity of the resulting radiotracers, [68 Ga]Ga-DOTA-estradiol and [68 Ga]Ga-NODAGA-estradiol, were assessed in vitro using recombinant human estrogen receptor (ER) protein and cell lines. In vivo PET/CT imaging was performed in mice bearing ER-positive and ER-negative tumors using [⁶⁸Ga]Ga-NODAGA-estradiol. Both radiotracers were obtained with high radiochemical purity. Neither [68 Ga]Ga-DOTA-estradiol nor [68 Ga]Ga-NODAGA-estradiol displayed selective binding to the recombinant human ER and no uptake difference could be identified between ER-positive and ER-negative cells. Competition blocking studies using non-radioactive [NatGa]Ga-DOTA-estradiol and [NatGa]Ga-NODAGA-estradiol significantly decreased the uptake of [18F]FES within ER-positive cells. In vivo imaging of [68 Ga]Ga-NODAGA-estradiol revealed negligible tumor uptake and predominant hepatobiliary clearance. Two estradiol-derived radiotracers were successfully synthesized and tested, however neither showed selective binding towards ER in vitro or in vivo. The conjugation site of the cyclic macrocycle on 17β-estradiol is likely a key parameter to retain strong binding towards ER. These findings identify an important limitation for chelator-based ER tracer design.

PMID 42722783
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PubMedBiotechnology journal2026-09-11

Metabolic Footprint of Drosophila S2 Cells: Findings During the Production of a Recombinant Rabies Virus Glycoprotein.

Decarli Monize Caiado MC, Dos Santos Diogo Peres DP, Correia Daniela Matilde DM, de Azevedo Amadeus Gomes AG et al.

Over the past 50 years, the Drosophila melanogaster S2 cells have been valued for their ability to synthesize therapeutic molecules at high yield. To further increase protein expression, it is imperative to improve cellular performance, which is intrinsically linked to cell metabolism. Nevertheless, information on S2 metabolism, including pathways, components, and cellular compartments, remains limited, hindering advances in S2 cellular performance. Herein, using a genetically modified S2 cell line expressing the recombinant rabies virus glycoprotein (RVGP), we investigated the stress caused by RVGP production on S2 cells. Batch cultures using wild- and rec-types were performed, and 27 compounds were quantified over 192 h. The extracellular metabolome affected the rec-S2 growth kinetics after RVGP expression was activated. Although RVGP was produced in high amounts, we identified a substrate limitation for rec-S2 cell growth (glutamine), changes in amino acid routes due to RVGP biosynthesis (leucine, serine, glycine, and valine), and metabolites that might be affecting rec-S2 cell growth (acetate, pyruvate, citrate, and malate). Organic acid analysis indicated that malate and acetate production are correlated with RVGP production. This work revealed metabolic correlations in S2 cells that may have direct implications for media optimization and yield maximization, thereby improving S2 performance for scale-up.

PMID 42723328
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PubMedSmall (Weinheim an der Bergstrasse, Germany)2026-09-11

Solvent-Chirality-Gated Recognition of Carbon Nanotubes by Polysaccharides.

Yoshida Kazuhiro K, Hatakeyama Yoshikiyo Y, Nonoguchi Yoshiyuki Y

Chiral molecular recognition is typically achieved through static complementarity between chiral hosts and molecular guests. Dynamic control of such recognition through external stimuli remains an important challenge, particularly for interactions involving extended solid surfaces. Here we show that solvent chirality can act as an external control parameter that modulates the conformation of polysaccharide dispersants and thereby creates a tunable chiral recognition field for one-dimensional nanomaterials. By continuously varying the enantiomeric excess of chiral solvents, the conformation of cellulose acetate can be modulated, resulting in switchable selectivity in the extraction of semiconducting single-walled carbon nanotubes (SWCNTs). Spectroscopic and structural analyses reveal that solvent chirality alters the balance between inter- and intramolecular interactions within the polysaccharide, leading to distinct conformational states that influence nanotube recognition. These findings demonstrate that chiral solvation can dynamically modulate macromolecular recognition fields and provide a strategy for controlling interactions between soft matter and extended solid nanostructures.

PMID 42723392
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PubMedRSC advances2026-09-11

Controlled aqueous nanoassembly-driven fully automated Fmoc solid-phase peptide synthesis (SPPS) with in-water coupling.

Hojo Keiko K, Kishimoto Mutsumi M, Nagai Ayana A, Rentier Cédric C et al.

Fmoc-based solid-phase peptide synthesis (SPPS) is a cornerstone of modern peptide manufacturing; however, its reliance on dimethylformamide (DMF)-a toxic and environmentally regulated solvent-poses significant sustainability challenges. Herein, we report a controlled aqueous nanoassembly-based strategy that enables fully automated Fmoc-SPPS under water-based coupling conditions. Aqueous nanoassemblies of Fmoc-protected amino acids, generated through a simple two-step preparation protocol, provide a stable and reactive coupling environment compatible with automated synthesis. The methodology was implemented on a commercially available peptide synthesizer and applied to peptides of varying lengths and sequence complexities, affording products of acceptable purity. Importantly, the platform was applied to the automated synthesis of long-chain peptides exceeding 30 residues, including GLP-1 (1-37), demonstrating its applicability to challenging sequences. At the time of writing, this represents, to the best of our knowledge, one of the earliest fully automated Fmoc-SPPS platforms employing water-based coupling cycles without the use of DMF. By eliminating DMF and employing environmentally benign solvents such as water and ethyl acetate, the present methodology provides a practical and sustainable alternative to conventional SPPS, advancing green practices in automated peptide synthesis.

PMID 42724454
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PubMedClinical and experimental hepatology2026-09-11

Estrogen receptor β activation attenuates portal hypertension and restores mesenteric vascular reactivity in cirrhotic rats via β-arrestin-2/RhoA/ROCK pathway modulation.

Sun Long-Ci LC, Ji Lin-Hua LH, Zhang Bin B, Wu Zhi-Yong ZY

This study investigated estrogen receptor (ER) subtype-specific effects on vascular hyporeactivity in cirrhotic portal hypertension (PHT), focusing on RhoA/ROCK signaling and β-arrestin-2. Cirrhosis and PHT were established by subcutaneous injection of CCl4. Cirrhotic rats were administered three ER subtype selective agonists (PPT [ERα], DPN [ERβ], G1 [GPER]) or β-estradiol (E2) alone or in combination with selective antagonists (MPP [ERα], PHTPP [ERβ], G15 [GPER]). Portal pressure and mesenteric arteriolar reactivity to norepinephrine were assessed. Protein expression was analyzed by immunoblotting. In cirrhotic rats, portal pressure was significantly elevated, and the dose-response curve of mesenteric arterioles to norepinephrine (NE) exhibited a rightward shift with reduced amplitude. Compared to cirrhotic rats, the CCl4 + E2 and CCl4 + DPN groups exhibited significantly reduced portal pressure and a leftward shift in the dose-response curve. The portal pressure was higher and the curve exhibited a rightward shift with reduced amplitude in group CCl4 + E2 + PHTPP, compare to group CCl4 + E2. Both portal pressure and the dose-response curve in the CCl4 + E2 + MPP and CCl4 + E2 + G15 groups remained comparable to the CCl4 + E2 group. Immunoblotting and densitometric analysis revealed that the intensity of β-arrestin-2 expression increased when cirrhosis and PHT developed. Compared with the CCl4 group, the intensity in the CCl4 + E2, CCl4 + DPN, CCl4 + E2 + MPP, and CCl4 + E2 + G15 groups decreased, while that in the CCl4 + PPT, CCl4 + G1, and CCl4 + E2 + PHTPP groups remained unchanged. No significant changes occurred in α1-AR, RhoA, ROCK-1, or moesin expression across groups. ERβ activation improves vascular hyporesponsiveness in cirrhosis by modulating β-arrestin-2, suggesting that ERβ may represent a novel therapeutic target for cirrhosis and PHT.

PMID 42724912
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PubMedPakistan journal of biological sciences : PJBS2026-09-11

Unveiling the Antioxidant Potential of Underutilized Moringa oleifera Parts: A DPPH and CUPRAC-Based Study.

Choirunnisa Atina Rizkiya AR, Asafiya Miladia Nur MN, Rizaldy Defri D, Hartati Rika R et al.

<b>Background and Objective:</b> <i>Moringa oleifera</i>, a plant rich in flavonoids and phenolic compounds, is widely recognized for its antioxidant potential. This study aimed to evaluate the antioxidant activity of underutilized parts of <i>M. oleifera</i> (twigs and stems) compared to leaves (well-utilized part), expressed as ascorbic acid equivalents. Additionally, the relationships between total phenolic content (TPC), total flavonoid content (TFC) and antioxidant activity were investigated. <b>Materials and Methods:</b> TPC and TFC were determined using UV-Visible spectrophotometry. Antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and Cupric Ion Reducing Antioxidant Capacity (CUPRAC) assays. Correlations among TPC, TFC and antioxidant activity were analyzed using Pearson's correlation, principal component analysis (PCA) and hierarchical cluster analysis (HCA). Flavonoid compounds were further characterized using TLC densitometry. Statistical significance among the data was analyzed using One-Way ANOVA in Minitab software at a significance level of p<0.05. <b>Results:</b> The ethanolic extract of <i>M. oleifera</i> leaves exhibited the highest antioxidant activity in both DPPH assays, while the ethyl acetate of <i>M. oleifera </i>twigs extract showed the highest activity using the CUPRAC assay. It is possible to develop twigs <i>M. oleifera </i>as a potential antioxidant agent resource. <b>Conclusion:</b> Among the tested plant parts, leaves demonstrated the highest antioxidant activity compared to twigs and stems. However, twigs also showed promising potential activity to be developed as source of antioxidant agent.

PMID 42723158
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