Steroids最新文献

{"title":"Selectivity, stability, and pharmacokinetic profiling of Spongia-derived steroids targeting AChE and BuChE for Alzheimer’s therapy","authors":"Damião Sampaio de Sousa ,&nbsp;Marcus Vinicius Ferreira da Silva ,&nbsp;Aluísio Marques da Fonseca ,&nbsp;Maria Mabelle Pereira Costa Paiva ,&nbsp;Carminda Sandra Brito Salmito Vanderley ,&nbsp;Gabrielle Silva Marinho","doi":"10.1016/j.steroids.2025.109705","DOIUrl":"10.1016/j.steroids.2025.109705","url":null,"abstract":"<div><div>Alzheimer’s disease (AD) is the leading form of dementia in the world. It presents significant therapeutic challenges, especially in terms of the efficacy and safety of current cholinesterase inhibitors, such as AChE. To explore more effective therapeutic alternatives, this study investigated the potential of steroids derived from <em>Spongia</em> sp. as inhibitors of AChE and BuChE, utilizing in silico approaches. Six compounds (SP1-SP6) were subjected to pharmacokinetic property predictions (ADMET), metabolic stability evaluation, and molecular docking and molecular dynamics studies. The analyses indicated that compounds SP4-SP6 show greater polarity and metabolic stability in the hepatic microsomal system, while SP1-SP3 exhibit greater cell permeability and bioaccumulation potential. Among them, compound SP6 stood out for showing relevant interactions with active residues of BuChE, suggesting selectivity and structural compatibility with this enzyme. The results were reinforced by molecular dynamics simulations, which confirmed the stability of the SP6-BuChE complex, characterized by low structural deviations (RMSD), minimal residual fluctuations (RMSF), maintenance of hydrogen bonds, and a favorable binding free energy (MMGBSA). Thus, the steroids evaluated, especially SP6, have promising characteristics for modulating BuChE, with potential therapeutic application in AD. Additional experimental studies are needed to validate the efficacy and selectivity of these drugs. Additional experimental studies are needed to validate the efficacy and selectivity of these compounds in biological models.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"224 ","pages":"Article 109705"},"PeriodicalIF":2.3,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145418131","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"α-Silyl substituted vinyl carbanions in the synthesis of brassinolide and castasterone","authors":"Maryia V. Barysevich ,&nbsp;Volha V. Kazlova ,&nbsp;Natalia M. Chaschina ,&nbsp;Maxim D. Akalovich ,&nbsp;Vitaly E. Syakhovich ,&nbsp;Vladimir N. Zhabinskii ,&nbsp;Vladimir A. Khripach","doi":"10.1016/j.steroids.2025.109706","DOIUrl":"10.1016/j.steroids.2025.109706","url":null,"abstract":"<div><div>A concise synthesis of brassinolide and castasterone has been accomplished herein. The strategy relies on the addition of α−silyl substituted vinyl carbanions to steroidal C-22 aldehydes with pre-formed functionalities in the cyclic part. Commercially available brassinosteroids were used as a starting material. The key step of the present synthesis was the opening of the 23,24-epoxide with Me₃Al in the presence of Ph₃P as a Lewis base, which enhances the formation of a more nucleophilic alkylating agent. It was shown why the use of Me₃Al is incompatible with the 3α,5-cyclo steroids, which are often employed as intermediates in the synthesis of brassinosteroids.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"224 ","pages":"Article 109706"},"PeriodicalIF":2.3,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145410151","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Potential of betulinic acid in the Antiformation and eradication of bacterial biofilms and pharmacokinetic and toxicological analysis","authors":"Camila Aparecida Pereira da Silva ,&nbsp;Nara Juliana Santos Araújo ,&nbsp;Maria do Socorro Costa ,&nbsp;Ana Raquel Pereira da Silva ,&nbsp;Cícera Laura Roque Paulo ,&nbsp;José Bezerra de Araújo Neto ,&nbsp;José Maria Barbosa Filho ,&nbsp;Thiago Sampaio de Freitas ,&nbsp;Juliete Bezerra Soares ,&nbsp;Josefa Sayonara dos Santos ,&nbsp;Maria Flaviana Bezerra Morais Braga ,&nbsp;Henrique Douglas Melo Coutinho ,&nbsp;Jacqueline Cosmo Andrade-Pinheiro","doi":"10.1016/j.steroids.2025.109702","DOIUrl":"10.1016/j.steroids.2025.109702","url":null,"abstract":"<div><div>Bacterial biofilms are complex, organized structures that adhere to surfaces, protected by a self-produced extracellular matrix. This conformation makes it difficult to eradicate infections with conventional treatments. In view of this, natural compounds have emerged as promising therapeutic alternatives. This study evaluated the potential of betulinic acid, a pentacyclic triterpene, in inhibiting the formation and eradication of bacterial biofilms, as well as predicting its pharmacokinetic properties and toxicity by means of in silico analyses. Six bacterial strains were tested. The crystal violet test was used to evaluate the antibiofilm activity, with chlorhexidine and the antibiotics norfloxacin, ampicillin and gentamicin as controls. The results showed that betulinic acid had moderate to good activity in inhibiting biofilm formation and a variable response in eradication, depending on the strain. In silico analyses indicated favorable physicochemical and pharmacokinetic properties, with emphasis on good intestinal absorption, oral bioavailability and absence of inhibition of cytochrome P450 enzymes, although potential toxicity risks were identified. These findings suggest that betulinic acid is a promising candidate for the development of new therapeutic strategies to combat infections associated with biofilms.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"224 ","pages":"Article 109702"},"PeriodicalIF":2.3,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145329857","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Steroidal scaffold dichotomy: pathogenic role of 7-ketocholesterol versus protective FXR-antagonistic actions of guggulsterone in metabolic regulation","authors":"Sarvesh Sabarathinam ,&nbsp;Nila Ganamurali","doi":"10.1016/j.steroids.2025.109691","DOIUrl":"10.1016/j.steroids.2025.109691","url":null,"abstract":"<div><div>Obesity-associated Dyslipidemia and inflammation are aggravated by the accumulation of toxic oxysterols, particularly 7-ketocholesterol (7-KC), which amplifies oxidative stress and metabolic dysfunction. The steroidal scaffold is a central determinant of whether such molecules exert protective or pathogenic effects. This review highlights the dichotomy between 7-KC, a cytotoxic oxysterol, and Guggulsterone, a Phytosteroids with therapeutic potential. Guggulsterone retains the tetracyclic steroid backbone, enabling it to mimic endogenous sterols while functioning as a farnesoid X receptor (FXR) antagonist. By relieving FXR-mediated suppression of CYP7A1, Guggulsterone enhances bile acid synthesis, promotes cholesterol clearance, and improves lipid profiles. Additionally, its structural features confer anti-inflammatory activity via NF-κB inhibition, contrasting with the pro-oxidant nature of 7-KC. The concept of steroid scaffold mimicry underscores the potential of Phytosteroids as blueprints for drug design, offering a path toward innovative therapies for obesity-linked metabolic disorders.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109691"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145157805","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Duration of vitamin D supplementation modulates the association between cardiovascular disease and high-sensitivity C-reactive protein across body mass index strata","authors":"Theocharis Koufakis ,&nbsp;Theofylaktos Georgiadis ,&nbsp;Areti Kourti ,&nbsp;Katerina Thisiadou ,&nbsp;Paraskevi Karalazou ,&nbsp;Alexander Kokkinos ,&nbsp;Michael Doumas ,&nbsp;Kalliopi Kotsa ,&nbsp;Kali Makedou","doi":"10.1016/j.steroids.2025.109690","DOIUrl":"10.1016/j.steroids.2025.109690","url":null,"abstract":"<div><h3>Background</h3><div>Cardiovascular disease (CVD) and higher body mass index (BMI) are linked to chronic low-grade inflammation. It is unclear whether vitamin D modifies the association between CVD and inflammatory biomarkers uniformly across BMI strata. We therefore tested whether vitamin D status and supplementation modify the CVD–biomarker association and whether any modification differs by BMI category.</div></div><div><h3>Methods</h3><div>In a cross-sectional cohort of adults free of acute infection (N = 88; 20 with normal BMI, 34 with overweight, and 34 with obesity), four inflammatory biomarkers were assessed: high-sensitivity C-reactive protein (hs-CRP), presepsin, ferritin, and β-defensin-2. Outcomes were modeled on the natural-log scale with age and sex as covariates. We tested the interaction between BMI and CVD and evaluated whether vitamin D variables [25(OH)D concentrations, supplementation status, supplementation duration, sufficiency category] modified the CVD–biomarker relationship, including prespecified three-way interactions among CVD, vitamin D, and BMI.</div></div><div><h3>Results</h3><div>No interaction between BMI and CVD was detected for any biomarker. For hs-CRP, a significant three-way interaction among CVD, vitamin D supplementation duration, and BMI was observed (p = 0.008) and was robust to sensitivity analyses [duration capped at three or six months; additional adjustment for 25(OH)D and supplementation status]. With longer supplementation, the CVD–hs-CRP difference widened in the moderate-BMI category and attenuated in the higher-BMI category. Other biomarkers showed no comparable interactions.</div></div><div><h3>Conclusion</h3><div>Vitamin D exposure—particularly supplementation duration—may modulate CVD-related inflammation in a BMI-dependent manner. Replication in larger studies is warranted.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109690"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145150876","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Are dexamethasone implants a safe and effective breakthrough in uveitis treatment? A systematic review and meta-analysis","authors":"Kai-Yang Chen ,&nbsp;Hoi-Chun Chan ,&nbsp;Chi-Ming Chan","doi":"10.1016/j.steroids.2025.109675","DOIUrl":"10.1016/j.steroids.2025.109675","url":null,"abstract":"<div><h3>Background</h3><div>Uveitis encompasses inflammatory conditions affecting the iris, ciliary body, and choroid. Its management relied on corticosteroids, immunosuppressive agents, and, more recently, biologic therapies. The development of sustained-release intravitreal corticosteroid delivery systems, like dexamethasone intravitreal implants, has revolutionized the treatment of posterior uveitis.</div></div><div><h3>Objectives</h3><div>To critically appraise the evidence of the safety and efficacy of dexamethasone implants in managing Uveitis.</div></div><div><h3>Methods</h3><div>A systematic review of the safety and efficacy of dexamethasone implants in managing Uveitis was conducted. A comprehensive and systematic electronic database search was conducted in Scopus, PubMed, Cochrane Library, ScienceDirect, Google Scholar, and Wiley Online Library for studies published from their inception to the present date. Modified PICOS criteria were used to screen and select the eligible studies from the potential articles retrieved from the database search. Studies were considered if they included patients with uveitis. A comprehensive risk of bias assessment was conducted using the Newcastle Ottawa Scale (NOS) for cohort studies, the Risk of Bias in Non-Randomized Studies (ROBINS-I) tool for non-randomized trials, the risk of bias visualization tool (ROB 2.0) tool for RCTs, and the National Institutes of Health (NIH) quality assessment tool for Interventional case-series. Data were then procedurally extracted and analyzed.</div></div><div><h3>Results</h3><div>The study selection process identified 29 studies, including 1,086 eyes. Dexamethasone implant significantly reduced central retinal/macular thickness at all time points: 150.4 μm at 1 month (p &lt; 0.001), 200.8 μm at 3 months (p &lt; 0.001), and 225.5 μm at 6–24 months (p &lt; 0.001). Inflammation control was achieved in 80.8 % of cases (p &lt; 0.001). Visual acuity improvements were modest at 6 months (p = 0.078) but significant long-term (p &lt; 0.001). However, the dexamethasone implant resulted in cataract formation (p = 0.010), with a recurrence rate of 0.501 (p = 0.968).</div></div><div><h3>Conclusion</h3><div>Dexamethasone implants offer clinically significant benefits, resulting in substantial reductions in central retinal thickness, improvements in visual acuity, and effective control of inflammation in patients with uveitis.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109675"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144883756","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Vitamin D potentiation of metformin hepatoprotective activities: Concurrent targeting of carbohydrate enzymatic pathways and PCSK9/AGEs-regulated oxidative stress mechanisms in type 2 diabetic male Wistar rats","authors":"Halimat Amin Abdulrahim ,&nbsp;Adeyemi Fatai Odetayo ,&nbsp;Muhammad Bashir Amosa ,&nbsp;John Oluwapelumi Olumoye ,&nbsp;Wasiu Abiodun Hassan ,&nbsp;Ivan Ayomide Ebadan ,&nbsp;Kehinde Yusuf Yusuf ,&nbsp;Gloria Toluwase Abodunrin ,&nbsp;Samuel Oluwaseyi Adefolarin ,&nbsp;Ayodeji Johnson Ajibare ,&nbsp;Temilade Olatunji ,&nbsp;Tahir Abdussalam ,&nbsp;Kazeem Bidemi Okesina ,&nbsp;Luqman Aribidesi Olayaki","doi":"10.1016/j.steroids.2025.109685","DOIUrl":"10.1016/j.steroids.2025.109685","url":null,"abstract":"<div><h3>Background</h3><div>Emerging evidence indicates that metformin-based combination therapy may offer better glycemic control and improved tolerability compared to diabetes monotherapy. Building on this, vitamin D was considered a potential adjunct to metformin for managing type 2 diabetes. Although vitamin D is primarily recognized for its role in calcium regulation, it also appears to influence glucose metabolism and other non-skeletal functions. Therefore, this study was designed to evaluate the hepatoprotective effects of vitamin D and metformin in diabetic rats.</div></div><div><h3>Methodology</h3><div>Thirty (30) male Wistar rats were randomized into five treatment groups as follows: control, diabetes (DM) untreated, DM treated with vitamin D (25 µg/kg), DM treated with metformin (180 mg/kg), and DM treated with both vitamin D (25 µg/kg) and metformin (180 mg/kg). All treatments were via the oral route and lasted for 28 days.</div></div><div><h3>Results</h3><div>Vitamin D and/or metformin improved glucose and lipid imbalances caused by diabetes. These benefits were linked to enhanced activity of key liver enzymes involved in glucose metabolism, including hexokinase, phosphofructokinase, pyruvate kinase, glucose-6-phosphate dehydrogenase, G-6-phosphatase, and lactate dehydrogenase. Additionally, treatment with vitamin D and/or metformin counteracted diabetes-induced increases in pro-oxidant levels, restored both enzymatic and non-enzymatic antioxidant defenses, and reduced inflammation. This oxido-inflammatory response appeared to be connected to oxidative signaling mediated by proprotein convertase subtilisin/kexin type 9 (PCSK9), highlighting a potential mechanism underlying the protective effects of these therapies.</div></div><div><h3>Conclusion</h3><div>Vitamin D enhanced the antidiabetic effects of metformin by further improving the activity of carbohydrate-metabolizing enzymes and modulating PCSK9-mediated oxidative signaling. This suggests that vitamin D can boost metformin’s efficacy in regulating glucose-lipid metabolism and reducing oxidative stress in diabetes.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109685"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145024148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Quercetin-cyclodextrin combination effects on cytochrome P450 genes, oxidative stress and ovarian function in PCOS rats","authors":"Fatemeh Taghipour ,&nbsp;Hadi Samadian ,&nbsp;Razieh Dalirfardouei ,&nbsp;Sara Soleimani Asl ,&nbsp;Nastaran Barati ,&nbsp;Tayebe Artimani","doi":"10.1016/j.steroids.2025.109688","DOIUrl":"10.1016/j.steroids.2025.109688","url":null,"abstract":"<div><div>This study investigates the effect of the quercetin/cyclodextrin (Que/β-CD) complex on oxidative stress, cytochrome P450 gene expression, and ovarian tissue structure in a rat polycystic ovary syndrome (PCOS) model. The Que/β-CD complexes were synthesized using the solvent evaporation method and characterized via scanning electron microscope (SEM) imaging and fourier transform infrared (FTIR) spectroscopy. Thirty female Wistar rats (6 weeks old, 160–180 g) with regular estrous cycles were randomly divided into six experimental groups: control, PCOS, PCOS treated with Que, PCOS adminstrated the β-CD, PCOS recivied metformin, and PCOS given Que/β-CD complex. Following model induction and treatments, tissue and gene expression analyses were performed. Characterization confirmed the successful synthesis of Que/β-CD complex. PCOS rats showed increased weight and higher number of atretic follicles compared to the controls (p &lt; 0.01), which were effectively decreased after Que/β-CD treatment. Additionally, PCOS rats had reduced corpora lutea and CYP19A expression levels (p &lt; 0.01), which were enhanced after Que/β-CD administration. Elevated CYP11A and CYP17A gene expression in PCOS rats markedly diminished with Que/β-CD treatment, indicating an improvement in disease symptoms. Oxidant levels, higher in PCOS rats (p &lt; 0.01), meaningfully decreased after treatment with metformin, Que, or Que/β-CD (p &lt; 0.0001, p &lt; 0.001, and p &lt; 0.001, respectively).</div><div>Overall, Que/β-CD treatment in the PCOS model resulted in to a significant decrease in body and ovary weights, number of cysts, atretic follicles, and oxidative stress markers, accompanied by a notable increase in corpora lutea, CYP19A expression, and antioxidant activity. These findings highlight Que/β-CD’s therapeutic potential in managing PCOS symptoms.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109688"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145058664","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, synthesis and characterization of novel cholesterol derivatives: Anti-cancer activity, ADMET profiling and DFT insights","authors":"Anmol Verma ,&nbsp;Poonam Rawat ,&nbsp;Sanyukta Shukla ,&nbsp;Ranvijay Pratap Singh ,&nbsp;Pratishtha Gupta ,&nbsp;Shama Parveen ,&nbsp;Monisha Banerjee ,&nbsp;Arun Sethi ,&nbsp;Saurabh Kumar Singh","doi":"10.1016/j.steroids.2025.109687","DOIUrl":"10.1016/j.steroids.2025.109687","url":null,"abstract":"<div><div>In the present work, Steglich esterification and Mizoroki-Heck reaction have been carried out for the synthesis of novel cholesterol derivatives. The synthesized derivatives <strong>2, 3, 4, 5</strong> and <strong>6</strong> were purified through column chromatography and characterized by ¹H, ¹³C NMR, FT-IR spectroscopy, and mass spectrometry. The geometries of all the compounds were optimized in the ground state by the density function theory at the B3LYP/6-31G(d,p) level. The <em>in vitro</em> evaluation of compounds <strong>2 (IC₅₀ 17), 3 (IC₅₀ 11), 4 (IC₅₀ 14)</strong> and <strong>6 (IC₅₀ 20)</strong> for their anti-cancer activity against SiHa cells demonstrated an increased apoptotic activity in comparison to the parent compound <strong>1 (IC₅₀ 24)</strong> i.e. cholesterol. The Molecular docking studies were carried out against two proteins bearing the protein data bank (PDB) ID 2B9D and 1R9W to investigate the inhibitory action of the derivatives. The result of molecular docking showed appreciable interactions of <strong>2, 3, 4, 5</strong> and <strong>6</strong> with the selected proteins as compared to <strong>1</strong>. The <em>in vitro</em> and molecular docking studies show that the synthesized molecules can prove to be better anti-cancer agents on other cancer cells also. The computational analysis data and the experimental data were in conformation with each other. ADMET analysis was carried out using the admetSAR database and Swiss ADME.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109687"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145081393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and preliminary biological evaluation of novel steroidal compounds as antibacterial agents","authors":"Anna Esposito ,&nbsp;Maria Stabile ,&nbsp;Antonella Migliaccio ,&nbsp;Eliana De Gregorio ,&nbsp;Stefano D’Errico ,&nbsp;Annalisa Guaragna","doi":"10.1016/j.steroids.2025.109686","DOIUrl":"10.1016/j.steroids.2025.109686","url":null,"abstract":"<div><div>Antimicrobial resistance is currently one of the most serious and alarming threats to human health; therefore, the identification of novel antimicrobial agents is a compelling need. Recently, we identified the heterocyclic steroid PYED-1 as a novel promising antibacterial and antibiofilm agent. In an effort to broaden the repertoire of active compounds and elucidate the structural features responsible for their antibacterial activity, two novel derivatives of PYED-1 have been conceived herein. The target compounds have been readily obtained in few steps and with very good yields. The antibacterial activity has been evaluated against <em>S. aureus</em> and <em>A. baumannii</em> strains, as examples of Gram-positive and -negative bacteria, by the broth microdilution method, while hemolysis assay has been used for the assessment of cytotoxicity. One of the two derivatives was able to inhibit the growth of <em>S. aureus</em> strains with lower MIC values (8 µg/mL) compared with those of PYED-1 (16 µg/mL) without showing hemolytic effect suggesting therefore a favorable safety profile. Overall, this study provides further indications on the functional groups required for the antibacterial activity of these novel steroidal derivatives.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"223 ","pages":"Article 109686"},"PeriodicalIF":2.3,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145030601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}