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chlormadinone acetate + ethinyl estradiol (Balianca / Belara / CG5025)

✓ Approved

Faes · AR · 小分子

什么是 chlormadinone acetate + ethinyl estradiol?

chlormadinone acetate + ethinyl estradiol 是一种小分子,由Faes研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名Balianca, Belara, CG5025
公司Faes
药物类别小分子
分子靶点AR, ESR1
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

chlormadinone acetate + ethinyl estradiol 作用于 2 个分子靶点:

ARandrogen receptor (TFM, NR3C4)
ESR1estrogen receptor 1 (ESR, ESTRR)
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

chlormadinone acetate + ethinyl estradiol 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Reproductive system and breast disordersPolycystic ovaries✓ Approved
Endocrine disordersPolycystic ovarian syndrome✓ Approved

相关研究文献

PubMedInternational journal of fertility & sterility2026-10-26

Treatment Approach to Disseminated Peritoneal Leiomyomatosis in A Patient Desiring Future Fertility: A Case Report.

Neal Samantha E SE, Ryles Hannah T HT, Koomson Christabel C, Madueke-Laveaux Obianuju Sandra OS et al.

Disseminated peritoneal leiomyomatosis (DPL) is a rare condition in which fibroids diffusely grow in extrauterine locations. Given its low prevalence, the literature is limited, making evidence-based treatment particularly challenging, especially in premenopausal patients. This case report describes a 34-year-old nulligravid woman with a history of two prior myomectomies who presented with upper abdominal bulk symptoms. Abdominal and pelvic magnetic resonance imaging (MRI) revealed multiple mesenteric and omental masses concerning for recurrent DPL. She underwent exploratory laparotomy with removal of 13 abdominal fibroids ranging from 2 to 12 cm. Postoperatively, her symptoms improved, and she was treated with a gonadotropin-releasing hormone (GnRH) analog (relugolix/estradiol/ norethindrone acetate) with a favorable response and sustained remission on follow up. Our case report demonstrates the efficacy of a novel medical therapy and our scoping review highlights the importance of aggressive surgical management followed by medical therapy for the treatment of DPL in patients with future fertility desires.

PMID 42929007
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PubMedMicrobial biotechnology2026-10-26

Adaptive Laboratory Evolution Rewires Pseudomonas putida for Resource-Efficient Acetate Assimilation.

Gurdo Nicolás N, Srinivasan Aparajitha A, Tagliani Tommaso T, Filbig Melanie M et al.

Acetate is an attractive renewable two-carbon substrate for microbial biotechnology, but toxicity limits growth and carbon-use efficiency at process-relevant concentrations. Here, we used adaptive laboratory evolution to improve acetate tolerance in a genome-reduced strain of Pseudomonas putida and combined whole-genome sequencing, quantitative physiology, reverse engineering, transcriptomics, proteomics and 13C-acetate fluxomics to resolve the underlying adaptation mechanisms. Evolution under increasing acetate concentrations selected recurrent mutations in gacA and fabB, which encode a global response regulator and a fatty acid biosynthesis enzyme, respectively. Reverse engineering of these mutations recapitulated most of the evolved phenotype, including shorter lag phase and substantially higher biomass yield from acetate. Multi-omic analyses showed repression of type VI secretion systems, carbohydrate storage functions, fatty acid metabolism and oxidative stress-associated proteins, indicating resource reallocation away from costly stress and non-essential programs. Fluxomics further revealed reduced carbon cycling and increased glyoxylate shunt flux, consistent with improved acetate-carbon retention in biomass. These results establish acetate tolerance in P. putida as a resource-efficiency phenotype and identify gacA and fabB as actionable targets for acetate-based bioproduction.

PMID 42929247
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PubMedCells2026-10-26

Selective Estradiol Sensitivity in 12Z Human Endometriotic Epithelial Cell Line.

Banerjee Shohini S, Chopra Esha E, Smith Ian M IM, Stroka Kimberly M KM

Estradiol (E2) is a potent estrogen molecule that plays a crucial role in regulating numerous healthy and pathophysiological processes. To model estrogen-dependent cellular activities in vitro in a physiologically meaningful way, cells chosen for experimentation should exhibit sensitivity to E2. The 12Z human endometriotic epithelial cell line is gaining attention as a model for estrogen-dependent conditions, but its functional responsiveness to E2 has not been well characterized. For the passage range in the following study, we found that E2 does not statistically significantly influence 12Z proliferation, wound closure, or single-cell migration. However, 12Zs were selectively responsive to E2 in 3D migration models where the cells were physically confined. Upregulating ESR1, the primary mediator of estrogenic action, in the 12Zs did not enhance their functional E2 sensitivity. These results highlight the importance of verifying hormone responsiveness when using 12Z cells to model estrogen-dependent processes and conditions.

PMID 42929847
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PubMedProtoplasma2026-10-26

Morphological, anatomical, and phytochemical characterization of Sisymbrium altissimum L.: chemical composition, biological activities, and isolation of major constituents.

Tekman Enes E, Aydın Bilge B, Yuca Hafize H, Özbek Hilal H et al.

This study comprehensively evaluated the phytochemical composition and multidimensional biological activities of Sisymbrium altissimum L., a wild edible species belonging to the Brassicaceae family. Methanolic extracts obtained from aerial parts, flowers, fruits, and roots were successively fractionated using solvents of increasing polarity, and essential and fatty oils were characterized by GC-MS and GC-FID analyses. The essential oil composition showed marked organ-dependent variation, with methallyl cyanide dominating fruit (91.9%) and flower (75.9%) oils, while phenylethyl isothiocyanate (48.7%) was the major constituent in roots. Further phytochemical investigation of the biologically active root hexane extract led to the isolation of β-sitosterol, lauric acid, and β-sitosterol-3-O-glucoside. Biological activity assays revealed strong α-glucosidase inhibition, particularly in the root hexane extract (87.92%), exceeding the reference drug acarbose (68.49%), whereas α-amylase inhibition was moderate, with the root ethyl acetate fraction exhibiting the highest activity (40.84%). Cholinesterase inhibition assays demonstrated low to moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities depending on the plant part and extract fraction. Hyaluronidase inhibition was notably high, reaching up to 98.70%, whereas moderate collagenase (27.56%) and elastase (23.98%) inhibition and low tyrosinase activity were observed. Antioxidant activity was prominent in ethyl acetate and n-butanol fractions, with ABTS radical scavenging values approaching those of standard antioxidants. Total phenolic and flavonoid contents correlated with antioxidant capacity, although structural factors also influenced activity. Importantly, all tested extracts and cold-pressed oil exhibited no mutagenic or genotoxic effects in the Ames/Salmonella assay. Overall, these findings provide a comprehensive characterization of S. altissimum and highlight its potential as a source of biologically active natural products.

PMID 42928286
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PubMedAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2026-10-26

Plasma Membrane Lipid Asymmetry Dynamically Regulates Passive Diffusion.

Ping Jieming J, Wang Wenliang W, Xu Jinnuo J, Yang Mengyun M et al.

Plasma membrane (PM) phospholipid asymmetry is a fundamental feature of eukaryotic cells that regulates signaling, trafficking, and cell fate. Whether it also controls passive diffusion across the PM remains unknown. Here, we show that phospholipid asymmetry is a critical determinant of PM permeability to hydrophobic molecules. Using genetic and biochemical approaches, we demonstrate that disruption of lipid asymmetry by the Ca2 +-activated scramblase TMEM16F or apoptotic scramblase XKR8 profoundly alters the permeation and intracellular accumulation of diverse hydrophobic compounds, including widely used fluorescent probes, while preserving the barrier to membrane-impermeable molecules. Lipid scrambling is sufficient to remodel membrane permeability to lipophilic molecules, alter membrane biophysical properties, and differentially affect their intracellular accumulation, suggesting selective regulation of passive diffusion rather than nonspecific membrane leakage. Physiological lipid scrambling during T cell activation was also accompanied by altered membrane permeability. Moreover, lipid asymmetry regulates the cellular entry of doxorubicin, 17β-estradiol, and all-trans retinoic acid. Together, our findings identify PM lipid asymmetry as a previously unrecognized regulator of membrane permeability and establish a link between membrane organization and molecular transport.

PMID 42928505
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PubMedApplied and environmental microbiology2026-10-26

Mechanistic insights into atmospheric and room-temperature plasma (ARTP)-induced genomic alterations and phenotypic evolution in Saccharomyces cerevisiae.

Sheng Huan H, Yao Jun J, Liu Yue Y, Li Ke-Jing K-J et al.

Atmospheric and room-temperature plasma (ARTP) is a potent tool for microbial strain engineering; however, the mechanistic basis of its genome-wide mutagenic effects remains poorly understood. Utilizing Saccharomyces cerevisiae as a model, we performed a comprehensive characterization of the mutational landscape and DNA repair pathways elicited by ARTP. Under high-lethality conditions (~99% mortality), ARTP treatment induced a substantial mutational burden, with SNVs and InDels rates increasing 25.2- and 36.7-fold relative to untreated controls, respectively. These mutations exhibited a pronounced bias toward C-T/G-A and A-T/T-A substitutions and InDels within AT-rich regions. Remarkably, the frequency of loss of heterozygosity (LOH) surged 57.4-fold, suggesting a potent capacity for inducing DNA breaks. Through sectored colony assays, we demonstrate that ARTP primarily inflicts pre-replicative double-strand breaks (DSBs), with reciprocal crossovers serving as the predominant driver of terminal LOH. The distribution and pattern of LOH were also altered in ARTP-treated cells. Mechanistically, our study establishes that the translesion synthesis polymerases Rev1 and Pol ζ are indispensable for converting ARTP-induced lesions-likely pyrimidine dimers-into fixed point mutations. In contrast, Rad30 facilitates high-fidelity bypass across these dimers. The base excision repair pathway appears largely dispensable for the processing of these lesions. In contrast, the nucleotide excision repair pathway plays a predominant role in mitigating ARTP-induced mutations. Finally, the strategic application of iterative ARTP mutagenesis facilitated the rapid evolution of acetate-tolerant strains. Our findings provide fundamental insights into the molecular signatures of ARTP mutagenesis, offering a framework for its optimized application in directed evolution. While ARTP is a cornerstone of non-thermal mutagenesis in industrial biotechnology, its genetic impact has long been treated as a "black box." This study provides a high-resolution molecular dissection of ARTP-induced genomic alterations using a diploid yeast model. We demonstrate that ARTP is not merely a source of point mutations but a potent catalyst for pre-replicative double-strand breaks and extensive mitotic recombination. By elucidating the pivotal roles of specific DNA repair pathways in mutation fixation, we transition ARTP from a purely empirical screening tool to a mechanistically grounded platform for directed evolution. Furthermore, we demonstrate the practical utility of this platform by evolving acetate-tolerant strains and identifying the underlying genetic drivers of their resilience.

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