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estradiol (E2III)

✓ Approved

Johnson & Johnson Services, Inc. · ESR1 · 小分子

什么是 estradiol？

estradiol 是一种小分子，由Johnson & Johnson Services, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Transdermal。

药物档案

商品名E2III
公司Johnson & Johnson Services, Inc.
药物类别小分子
分子靶点ESR1
给药途径Transdermal
状态Approved
来源： ClinicalTrials.gov, Johnson & Johnson Services, Inc.

作用机制

分子靶点

estradiol 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 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

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Prevalence and Reproductive Toxicity of Di-2-ethylhexyl Terephthalate (DEHTP) and Other Substituted Benzene Carboxylic Acid Derivatives Used as Phthalate Alternatives.

Potts Courtney C, Harbolic Allison A, Alahmadi Hanin H, Nadeem Maira M et al.

Phthalate alternatives have emerged worldwide recently in response to concerns that traditional ortho-substituted phthalates alter and inhibit endocrine and reproductive functions and behave as endocrine disrupting chemicals (EDC). As a result, legacy plasticizers are being phased out of use, giving rise to alternative plasticizers. Human biomonitoring studies indicate that people are increasingly exposed to alternative plasticizers. However, recent studies suggest that alternative plasticizers may disrupt endocrine and reproductive functions. Foremost among these emerging substitutes are di-2-ethylhexyl terephthalate (DEHTP), a ring substitution isomer of the most common plasticizer phthalate di-2-ethylhexyl phthalate (DEHP), and tri-2-ethylhexyl trimellitate (TOTM), which has three ester side chains compared to DEHP and DEHTP's two. In this literature review, we provide a comprehensive overview of environmental monitoring and biomonitoring of DEHTP and other substituted benzene carboxylic acid derivatives used as phthalate alternatives, which together illustrate the widespread use of these compounds leading to human and environmental exposures as ubiquitous as phthalates. We also review reproductive toxicity findings in animals, in vitro, and human epidemiology. Overall, the availability of studies regarding the health impacts of alternative plasticizers is limited. Published literature suggests that these chemicals can disrupt hormone levels in rodents and zebrafish. This review underscores the urgent need for further research to characterize the long-term health impacts of these emerging chemicals and to prevent the regrettable substitution of one hazard for another.

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Neurokinin pathway botanical antagonist for menopausal vasomotor symptoms: A randomized, double-blind, placebo-controlled study.

Lederman Samuel S, Minkin Mary Jane MJ, Doyle Audra Lisa AL, Rubio Jevaneeh J et al.

Vasomotor symptoms (VMS) are a prevalent and disruptive manifestation of menopause, and many women prefer nonhormonal, nonpharmacologic treatment options. This study evaluated the efficacy of a patented multi-ingredient botanical neurokinin inhibitor (BNI) on VMS and other patient-reported outcome measures. A randomized, double-blind, placebo-controlled trial was performed in menopausal women with 5 or more moderate to severe hot flashes daily. Participants were enrolled from community medical practices in the United States and randomized to BNI or placebo for 12 weeks. BNI is a novel formulation of plant extracts that attenuates neurokinin receptor signaling in vivo. Primary endpoints were changes in daily VMS frequency and score on the Hot Flash Related Daily Interference Scale (HFRDIS). Secondary endpoints included changes in Menopause-Specific Quality of Life (MENQOL) and Pittsburgh Sleep Quality Index (PSQI). Serum estrogen and liver function were assessed in a subgroup of patients. Of 74 randomized participants, 68 completed the trial (BNI, n = 32; placebo, n = 36). BNI supplementation reduced VMS frequency by 2.2 hot flashes per day more than placebo (p = 0.003), corresponding to a 47.7% relative decrease. HFRDIS was improved in the BNI group (p = 0.037), with significant reduction on all subscales. No significant differences were observed in global menopause symptoms (MENQOL) or sleep quality (PSQI). No changes in serum estradiol or liver function abnormalities were detected. BNI was well tolerated, with no difference in adverse events between groups. A combination of botanically derived neurokinin inhibitors produces significant and sustained relief of vasomotor symptoms in menopausal women. gov registration: NCT05813067.

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Estrogen receptor-positive (ER+) breast cancer is the most prevalent breast cancer subtype, and doxorubicin is a key systemic therapeutic drug. However, its use is limited by toxicity and mechanisms of drug resistance. Steryl glucosides are bioactive glycolipids with potential anticancer and immunomodulatory properties, but their role as chemotherapy-sensitizing agents remains undefined. Here, we investigated whether a soybean-derived steryl glucoside preparation (SG) enhances doxorubicin activity primarily in the MCF-7 ER+ breast cancer model. SG co-treatment increased doxorubicin-associated cytotoxicity and reduced cell viability of MCF-7. Dose-response matrix analysis and exploratory Bliss independence modeling identified concentration-dependent regions of greater-than-expected combined activity, supporting pharmacological potentiation but not definitive synergy. SG co-treatment also increased γ-H2AX-positive nuclei, consistent with enhanced doxorubicin-associated DNA damage signaling. Fluorescence-based extraction analysis showed increased doxorubicin-associated intracellular fluorescence in SG co-treated cells, while ABCB1 qRT-PCR revealed concentration-dependent transcriptional changes. These findings suggest altered intracellular drug exposure or transport-associated responses, although functional efflux activity was not directly assessed. In an ovariectomized, estradiol-supplemented MCF-7 xenograft model, the SG-doxorubicin group showed the lowest mean tumor-growth trajectory, reduced cumulative tumor burden, lower terminal tumor weight, reduced Ki-67 staining, and increased tumor necrosis. However, the longitudinal tumor-volume analysis did not establish unequivocal superiority over doxorubicin monotherapy. Exploratory T47D data indicated weaker responsiveness, suggesting that the effect may be model-dependent. This study provides proof-of-concept evidence that SG can enhance doxorubicin-associated antitumor activity mainly in the MCF-7 model. Further studies are required to define functional transport mechanisms, model generalizability, toxicity, and formal dose-sparing potential. This study provides proof-of-concept evidence that a soybean-derived steryl glucoside preparation can enhance doxorubicin-associated cytotoxicity, DNA damage signaling, and antitumor activity primarily in the MCF-7 estrogen receptor-positive breast cancer model. The findings support further investigation of SG as a candidate chemotherapy-sensitizing adjuvant, while highlighting the need for functional transport assays, broader model validation, comprehensive toxicity assessment, and formal dose-sparing studies before translational conclusions can be drawn.

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To investigate the impact of 1-hour plasma glucose (1 h-PG) on the metabolic characteristics and pregnancy outcomes in polycystic ovary syndrome (PCOS). This multicenter study analyzed 970 PCOS patients (2019-2025), including 289 undergoing assisted reproductive technology (198 successful deliveries). Participants were stratified by glucose tolerance: Group 1 (normal: fasting PG [FPG] ≤ 6.1, 1 h-PG < 8.6, 2-hour PG [2 h-PG] <7.8 mmol/L); Group 2 (isolated 1 h-prediabetes: 8.6 ≤ 1 h-PG < 11.6, FPG ≤ 6.1, 2 h-PG < 7.8 mmol/L); Group 3 (traditional 2 h-prediabetes: 7.8 ≤ 2 h-PG ≤ 11.1, FPG ≤ 6.1 mmol/L). Data included anthropometrics, metabolic biomarkers, sex hormones, and pregnancy outcomes were compared across three groups. PCOS with isolated 1 h-prediabetes (Group 2) had a more unfavorable metabolic profile with regard to metabolic traits, but were not significantly different from those of the traditional 2 h-prediabetes (Group 3). The adjusted odds ratios (ORs) for hypertension, hyperlipidemia, metabolic syndrome (MetS), and hyperuricemia in PCOS with Group 2 were 1.451 (1.013-2.079, P = 0.042), 1.706 (1.188-2.450, P = 0.004), 2.957 (1.755-4.981, P < 0.001), 1.890 (1.327-2.692, P < 0.001), respectively. For pregnancy outcomes, PCOS in Group 2 were more likely to progress to gestational diabetes mellitus (GDM) than those of Group 1, which was similarly observed in Group 3. The adjusted OR for GDM in the Group 2 was 4.065 (1.530-10.800, P = 0.005). Our study demonstrated that similar to 2 h-PG, elevated 1 h-PG was associated with different metabolic disorders and GDM. Therefore, 1 h-PG may serve as an additional marker of adverse metabolic status in women with PCOS.

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Inflammatory bowel disease (IBD) is a disorder characterized by defective intestinal barrier function, aberrant over-apoptosis of intestinal epithelial cells, and constitutive activation of pro-inflammatory signaling pathways. Glucagon-like peptide-2 (GLP-2), an endogenous gastrointestinal hormone, is known to exert protective effects against IBD by repairing the intestinal barrier and suppressing inflammatory responses. This study used molecular docking and molecular dynamics simulations to discover that [Gly2]-GLP-2(1-5) has a high binding affinity and strong binding stability with GLP-2R. In DSS-induced colitis mouse model, treatment with [Gly2]-GLP-2(1-5) can effectively reverse weight loss in mice, reduce disease activity index, increase colon length, and alleviate inflammatory damage in colon tissues; it also upregulates the expression of tight junction proteins, inhibits epithelial cell apoptosis and release of inflammatory factors, and enhances the regenerative ability of organoids. In LPS-stimulated intestinal epithelial cells, [Gly2]-GLP-2(1-5) can promote intestinal epithelial cell migration, maintain the integrity of tight junctions, and inhibit cell apoptosis. These findings suggest that [Gly2]-GLP-2(1-5) may be the shortest active short peptide of GLP-2 and is expected to be an effective peptide for the treatment of inflammatory bowel disease.

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