Steroids最新文献

{"title":"α-Bromoketone derivatives from lithocholic acid: a comprehensive evaluation of their antibacterial activity","authors":"Mónica Díaz-Fernández ,&nbsp;Jesús Ramón-Sierra ,&nbsp;Elizabeth Ortiz-Vázquez ,&nbsp;María A. Fernández-Herrera","doi":"10.1016/j.steroids.2025.109658","DOIUrl":"10.1016/j.steroids.2025.109658","url":null,"abstract":"<div><div>A series of six α-bromoketones derived from lithocholic acid was synthesized through an oxidative bromination reaction, with four of these compounds being reported for the first time. All products were characterized using NMR, IR spectroscopy, and mass spectrometry. The structures and crystalline packing of two α-bromoketones were further confirmed through X-ray diffraction analysis. The antibacterial activity of the compounds was evaluated against both Gram-negative and Gram-positive bacterial strains of clinical relevance.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109658"},"PeriodicalIF":2.1,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144620718","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":"Exploring the urate lowering properties of Erigeron annuus Lin. and phytosterol contributions: In vitro assays and in silico approaches","authors":"Rupali Rana ,&nbsp;Anchal Sharma ,&nbsp;Nitish Kumar ,&nbsp;Pallvi Mohanna ,&nbsp;Jyoti ,&nbsp;Aanchal Khanna ,&nbsp;Jatinder Vir Singh ,&nbsp;Preet Mohinder Singh Bedi","doi":"10.1016/j.steroids.2025.109657","DOIUrl":"10.1016/j.steroids.2025.109657","url":null,"abstract":"<div><h3>Background</h3><div>Due to the severe hypersensitivity risks associated with some xanthine oxidase (XO) inhibitors, there is a pressing need to develop novel agents with improved safety and effective ADME profiles. This study evaluates the antihyperuricemic and antioxidant potential of <em>Erigeron annuus</em> Lin. (E. annuus) using in vitro and in silico models.</div></div><div><h3>Objective</h3><div>To assess the in vitro XO inhibitory and antioxidant activities of the hydroalcoholic crude extract, fractions, and isolated compounds from the aerial parts of E. annuus Lin.</div></div><div><h3>Methods</h3><div>A hydroalcoholic extract was prepared using a Soxhlet apparatus. Column chromatography and spectroscopic techniques were employed to isolate and identify two phytosterols: RR1 (<em>β</em>-sitosterol) and RR2 (stigmasterol). A further pharmacophore-based hypothesis was developed using DE Shaw Desmond software; an in-silico profile was also evaluated using LeadIT software and Swiss ADME, respectively. XO inhibitory activity was measured using a Biotek multi-mode plate reader, and antioxidant activity was assessed via the DPPH and FRAP assay. Additionally, potent compound RR2 was also evaluated for its cytotoxicity against HepG2 cell line.</div></div><div><h3>Results</h3><div>All tested extracts and fractions inhibited XO activity, with IC₅₀ values ranging from 0.086 µg/mL to 36.71 µg/mL. Allopurinol, used as a positive control, had an IC₅₀ of 0.027 µg/mL. The hexane fraction of E. annuus exhibited the most vigorous XO inhibitory activity (IC₅₀ = 0.086 µg/mL). RR2 (stigmasterol) showed notable inhibition from this fraction with an IC₅₀ of 0.331 µg/mL. Antioxidant assays and cytoxicity study also supported the bioactivity of these fractions.</div></div><div><h3>Conclusion</h3><div>The hexane fraction of E. annuus demonstrated potent XO inhibitory activity, highlighting its potential as a source for developing herbal treatments for hyperuricemia and gout. The study validates traditional use and supports the pharmacophore hypothesis, suggesting that structural optimization of the sterol nucleus could enhance therapeutic efficacy.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109657"},"PeriodicalIF":2.1,"publicationDate":"2025-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144596835","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":"Association of CYP27B1 promoter gene variants of vitamin D pathway with pulmonary tuberculosis and vitamin D levels","authors":"Harishankar Murugesan ,&nbsp;Pavithra Sampath ,&nbsp;Karthikeyan Ramamurthy ,&nbsp;Aarti Muralitharan ,&nbsp;Dhanyaa Muthukumaran ,&nbsp;Athikesavan Veerasamy ,&nbsp;Uma Devi Ranganathan ,&nbsp;Selvaraj Paramasivam ,&nbsp;Ramalingam Bethunaickan","doi":"10.1016/j.steroids.2025.109656","DOIUrl":"10.1016/j.steroids.2025.109656","url":null,"abstract":"<div><div><em>Cyp27b1</em> polymorphisms are stated to be associated with different diseases including tuberculosis (TB). Since the gene variants located in the promoter region may have a significant influence on gene transcription/translation and Cyp27b1 enzyme is involved in critical steps in vitamin D metabolism, we aim to study whether <em>Cyp27b1</em> gene promoter variants namely −1077 (C/G), −1260 (C/A) and the region immediately 5′ to the promoter −1918 (C/T) have any linkage with pulmonary tuberculosis risk/defence and to determine their influence on vitamin D level in normal healthy controls (HCs) and pulmonary tuberculosis (PTB) patients of the South Indian population. The polymerase chain reaction and restriction fragment length polymorphism (PCR-RFLP) method were used to genotype the genomic DNA after it was extracted using the salting-out approach. The Enzyme-Linked Immunosorbent Assay (ELISA) was used to measure the amount of vitamin D. In the co-dominant model, a significant association was detected with TB liability in the −1077 “GG” genotype [Odds ratio (OR): 2.10(1.18–3.73); p = 0.015]. In addition, a noteworthy linkage was detected with TB protection in the dominant model [GG vs CG + CC, OR: 0.40(0.21–0.75); p = 0.0035]. In the −1918 (C/T) variant, a substantial linkage was detected in the heterozygous −1918 “CT” genotype with TB risk [OR: 1.90 (1.05–3.44); p = 0.046] in co-dominant model, whereas a protective linkage was detected in less recurrent “TT” genotype [OR: 0.42 (0.19–0.94); p = 0.049] with TB. Furthermore, those risky genotypes are substantially linked with more TB risk in males than females. Strong links between −1077 and −1260 variations were revealed by haplotype analysis, and its haplotypes “GC” (−1077G, −1260C) were found to be significantly associated with increased TB risk. Vitamin D deficiency (&lt;20 ng/ml) was detected at a higher frequency in PTB patients than HCs in −1077 “GG”, −1260 “CA” and −1918 “CT” risky genotypes. This needs to be confirmed by bigger sample sizes in future research.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109656"},"PeriodicalIF":2.1,"publicationDate":"2025-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144605303","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":"The impact of serum estradiol levels on vaginal pH and Candida infections during infertility treatment","authors":"Çağın Çakırgöz ,&nbsp;Emine Çakırgöz ,&nbsp;Dilara Kirmiç ,&nbsp;Pınar Solmaz Hasdemir ,&nbsp;Kenan Değerli","doi":"10.1016/j.steroids.2025.109655","DOIUrl":"10.1016/j.steroids.2025.109655","url":null,"abstract":"<div><h3>Purpose</h3><div>This study aimed to evaluate the potential impact of serum E2 levels on vaginal pH regulation and Candida colonization in women undergoing infertility treatment, emphasizing mucosal barrier dynamics and epithelial immune modulation.</div></div><div><h3>Methods</h3><div>In this prospective observational study, 60 women aged 20–49 undergoing long-protocol ovulation induction were enrolled. Serum E2 levels, vaginal pH, and fungal cultures were assessed on cycle day 2 (baseline) and again at the time of estradiol peak, which was typically within 24 h before human chorionic gonadotropin (hCG) administration and after ultrasound-confirmed follicular maturation. Pre- and post-treatment paired samples were statistically compared, with significance set at p &lt; 0.05.</div></div><div><h3>Results</h3><div>Post-treatment analysis revealed a significant increase in serum E2 and vaginal pH levels (p &lt; 0.05). However, no significant correlation was observed between E2 and vaginal pH, Candida colonization, or vulvovaginal symptoms. Likewise, vaginal pH was not a significant predictor of fungal growth. Notably, a significant association between baseline symptoms and culture positivity was observed pre-treatment, which was not present post-treatment.</div></div><div><h3>Conclusion</h3><div>These findings indicate that the hormonal increase in E2 during infertility treatment, although associated with elevated vaginal pH, does not increase the risk of Candida infections. The preservation of epithelial barrier function despite hormonal shifts may explain this finding. These results support the microbiological safety of controlled ovarian stimulation protocols with regard to Candida susceptibility.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109655"},"PeriodicalIF":2.1,"publicationDate":"2025-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144476696","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":"Cortisol, testosterone and body composition changes during overwintering at Concordia in Antarctica","authors":"Katia Collomp ,&nbsp;Karine Paret ,&nbsp;Fabrice Prieur ,&nbsp;Nancy Vibarel-Rebot ,&nbsp;Sandrine Schiano-Lomoriello ,&nbsp;Nathalie Rieth ,&nbsp;Maud Miguet ,&nbsp;Aude Villemain","doi":"10.1016/j.steroids.2025.109654","DOIUrl":"10.1016/j.steroids.2025.109654","url":null,"abstract":"<div><div>Concordia in Antarctica is one of the most remote and inhospitable inhabited places on the planet. Overwintering at Concordia presents extreme environmental conditions combining both physiological stress [three-month-long period of polar night (early May to early August) and three-month period of polar day (early November to early February), severe cold, and high-altitude hypoxia] and conditions of isolation and confinement known to induce both physical and cognitive alterations. However, given the very small number of subjects experiencing such conditions, literature remains scarce on the real impact of an overwintering period on steroid hormone changes. Using monthly records, we therefore assessed the impact of an overwintering in 23 male participants on awakening and evening concentrations of cortisol and testosterone, body composition and physical aptitude assessed using a Chester submaximal test. Across overwintering, 10 of the 23 subjects (Group 1) lost more than 2 % of their muscle mass. Awakening and evening concentrations of cortisol and testosterone were preserved throughout wintering with no significant deterioration in physical aptitude. However, Group 1 vs. Group 2 participants had higher end-exercise heart rate and lower testosterone fluctuations between awakening and evening (p &lt; 0.05). These results highlighted the great adaptation of the hypothalamic–pituitary–adrenal and gonadal axis functions to long-term extreme polar exposure. Further studies are needed to determine the mechanisms underlying the alteration in muscle mass occurring in almost half of the winterers, taking into account the subjects’ energy intake and expenditure as well as their initial physical aptitude, in order to propose effective diet and physical activity countermeasures.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109654"},"PeriodicalIF":2.1,"publicationDate":"2025-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144470352","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":"Bidirectional effect of ecdysterone on thymocyte volume regulation and proliferation","authors":"Fariza A. Salimova ,&nbsp;Sarvinoz I. Rustamova ,&nbsp;Sirojbek A. Khojiboev ,&nbsp;Ozoda J. Khamidova ,&nbsp;Petr G. Merzlyak ,&nbsp;Diyor D. Fayziev ,&nbsp;Vladimir N. Syrov ,&nbsp;Feruza R. Egamova ,&nbsp;Ranokhon Sh. Kurbannazarova ,&nbsp;Ravshan Z. Sabirov","doi":"10.1016/j.steroids.2025.109653","DOIUrl":"10.1016/j.steroids.2025.109653","url":null,"abstract":"<div><div>The development and maturation of T cells requires an efficient cell volume regulation (CVR) system in which the volume-sensitive outwardly rectifying anion channel (VSOR/VRAC) plays a pivotal role. Ecdysterone (20-hydroxyecdysone, 20HE) is known to exert multiple effects in mammals, but the response of the thymus and thymocytes to this hormone remains virtually unexplored. In the present study, we observed a bidirectional effect of 20HE on the thymus and its cellular contents. In the short term, thymocytes responded by blockage of the VSOR/VRAC with a half-maximal effective concentration of ∼33–37 μM and a maximum observed inhibition by 57–62 % at 100 μM. Suppression of the thymocytic RVD occurred to a less degree of ∼31 % but more efficiently with a half-maximal concentration at ∼8 μM. In contrast to the short-term effects, prolonged exposure of thymocytes to 20HE increased their proliferative activity under primary culture conditions (by ∼67 % after 24 h) without detectable change in the VSOR/VRAC activity. Consistent with this result, at the whole organism level, administration of 20HE <em>per os</em> for 5 days strongly stimulated thymic growth (by ∼61 %) and up-regulated the CVR efficiency of the cells isolated from the 20HE-treated animals (parameter RVD increase by ∼12 %). The results obtained suggest that systemic effects of 20HE, which become apparent only after long-term exposure in primary culture conditions or in the whole organism, may counteract the acute blockade of thymocyte VSOR/VRAC and RVD induced by the steroid in the buffered saline.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109653"},"PeriodicalIF":2.1,"publicationDate":"2025-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144329901","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":"The Effect of Vitamin D3 supplementation on Flunitrazepam-Induced testicular dysfunction in Wistar rats","authors":"David Tolulope Oluwole ,&nbsp;Aliyah Ochuwa Yakubu ,&nbsp;Oladipupo Samuel Ebiwonjumi ,&nbsp;Lydia Oluwatoyin Ajayi ,&nbsp;Ayodeji Folorunsho Ajayi","doi":"10.1016/j.steroids.2025.109650","DOIUrl":"10.1016/j.steroids.2025.109650","url":null,"abstract":"<div><div>Prolonged flunitrazepam use has been reported to be increasing among young adolescents, and it has been reported to induce hyperprolactinemia, causing gross impairment of testicular function, ultimately resulting in male infertility. Hence, this current study seeks to examine the possible protective potential of the micronutrient Vitamin D3 in mitigating flunitrazepam-induced testicular dysfunction.</div><div>Adult male rats (Wistar strain), weighing 200–220 g, were categorized into four groups: Vehicle [0.3 ml of distilled water and 0.2 ml of olive oil, the respective solvents for flunitrazepam (Fluni) and Vitamin D3 (V.D3)], Fluni [0.35 mg/kg], V.D3 [0.01 mg/kg], and Fluni [0.35 mg/kg] + V.D3 [0.01 mg/kg]; these groups were treated orally for 56 days before the testes and epididymides were removed for biochemical and histological processing.</div><div>Vitamin D3 supplementation significantly prevented hyperprolactinemia and sperm cell damage, reduced testicular lipid peroxidation, and significantly increased serum concentrations of reproductive hormones, testicular steroidogenic enzymes, antioxidants, and improved inflammatory markers. It also improved sperm energy utilization, quality, and transmembrane pump activities, with a marked recovery of the epididymal smooth muscles and testicular interstitial and spermatogonial cells in the flunitrazepam-treated rats.</div><div>This present study shows that Vitamin D3 supplementation prevents impairment of testicular functions and ensures improved sperm function in flunitrazepam-exposed rats. Meanwhile, further molecular studies and clinical trials are encouraged to explore Vitamin D3′s possible intervention in drug-induced male infertility, given the limitations of animal studies.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109650"},"PeriodicalIF":2.1,"publicationDate":"2025-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144291238","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":"Mycochemical investigation, antioxidant, cytotoxic and enzyme inhibition activities of truffle Picoa lefebvrei","authors":"Çiğdem Kuş ,&nbsp;Meltem Taş Küçükaydın ,&nbsp;Selçuk Küçükaydın ,&nbsp;Mehmet Emin Duru ,&nbsp;Mehmet Öztürk","doi":"10.1016/j.steroids.2025.109651","DOIUrl":"10.1016/j.steroids.2025.109651","url":null,"abstract":"<div><div><em>Picoa lefebvrei</em> (Pat.) Maire is a truffle species that belongs to the Cistaceae family and grows mycorrhizally on the roots of <em>Helianthemum</em> species. <em>Picoa</em> species, which is indigenous to Western Anatolia and Tunisia, have been preferred as food and have economic potential. Recently, interest in bioactive compounds of mushrooms has increased and it is known that edible mushrooms and some truffles are used in the new generation of biotherapeutics. In this report, eight compounds were isolated from <em>P. lefebvrei</em> extracts namely, brassicasterol (<strong>1</strong>), brassicasteryl-<em>β-ᴅ</em>-glucopyranoside (<strong>2</strong>), uracil (<strong>3</strong>), <em><span>l</span></em>-uridine (<strong>4</strong>), erythritol (<strong>5</strong>), <em>α-ᴅ</em>-glucopyranosyl-<em>α-ᴅ</em>-glucopyranoside (<strong>6</strong>), brassicasteryl linoleate (<strong>7</strong>) and 5<em>α</em>-6<em>α</em>-epoxy ergosta-7,22-diene-3<em>β</em>-ol (<strong>8</strong>) via various chromatographic methods. Also, antioxidant, anticholinesterase, anti-urease, and cytotoxic (against MCF-7, H1299 and L929 cell lines) activities of extracts and compounds from <em>P. lefebvrei</em> were investigated. Compound <strong>4</strong> exhibited the highest antioxidant activity with IC₅₀ values of 92.61 ± 0.10, 70.55 ± 0.84 and 112.08 ± 0.15 µg/mL in the DPPH (2,2-Diphenyl-1-picrylhydrazyl), ABTS (2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and CUPRAC (Cupric Ion Reducing Antioxidant Capacity) assays, respectively. Compounds <strong>3</strong> and <strong>8</strong> exhibited the highest activities against acetylcholinesterase (AChE) (44.59 ± 0.37 % and 40.26 ± 0.53 %) and butyrylcholinesterase (BChE) (53.15 ± 1.07 % and 54.97 ± 0.41 %). Compound <strong>8</strong> had strongest cytotoxicity with IC₅₀ value of 33.94 ± 0.47 µg/mL against the H1299 lung cancer cells. Nevertheless, compound <strong>1</strong> (IC₅₀:24.72 ± 0.75 µg/mL), showed the greatest cytotoxicity against the MCF-7 breast cancer cells. These findings indicate that <em>P. lefebvrei</em>, is rich in steroidal compounds and is a possible source of ergostane-type steroids. Furthermore, this first detailed investigation highlights the potential of <em>P. lefebvrei</em> as a natural food and as a source of bioactive compounds.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109651"},"PeriodicalIF":2.1,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144279080","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":"Laetiporus sulphureus mushroom culture − source of secondary metabolites, and as a catalyst for biotransformation of breast cancer drug exemestane","authors":"Yagut Yusifova ,&nbsp;Atia-tul-Wahab ,&nbsp;M. Iqbal Choudhary ,&nbsp;Mahwish Siddiqui ,&nbsp;Nisha Khan ,&nbsp;Muhammad Atif ,&nbsp;Humaira Zafar ,&nbsp;Sayyara J. Ibadullayeva ,&nbsp;Dilzara N. Aghayeva","doi":"10.1016/j.steroids.2025.109647","DOIUrl":"10.1016/j.steroids.2025.109647","url":null,"abstract":"<div><div>Certain mushrooms are used as low-calorie food supplements due to their excellent taste, and presence of a variety of essential vitamins, minerals and secondary metabolites. Some of them have therapeutic significance, and used in traditional medicines. Mushrooms cells can also be used as biocatalysts for the derivatization of organic compounds. During the current study, 3<em>β</em>-hydroxy-24-methylenelanost-8-en-21-oic acid (<strong>1</strong>) was isolated from <em>Laetiporus sulphureus</em> (Bull.) Murrill. The cell culture of the same mushroom was used for the biotransformation of breast cancer drug, exemestane (<strong>2</strong>) into a new analogue, 18-hydroxy-6-methylene-androsta-1,4-diene-3,17-dione (<strong>3</strong>). Compounds <strong>1</strong>, and <strong>3</strong> were purified by using various chromatographic techniques, and their structures were determined with the help of 1D- and 2D-NMR, HREI-MS, and IR spectroscopic techniques. Since compound <strong>1</strong> also has a steroidal skeleton (like aromatase inhibiting drug exemestane (<strong>2</strong>)), the metabolite <strong>1</strong> was also evaluated for its aromatase inhibitory potential, along with a new transformed product <strong>3</strong>. Aromatase plays a crucial role in estrogen biosynthesis, and therefore its inhibition is a key approach for the treatment of estrogen receptor-positive (ER+) breast cancers. Compounds <strong>1</strong> and <strong>3</strong> demonstrated a significant aromatase inhibition, with IC₅₀ values of 590 ± 0.03 nM and 337.5 ± 0.01 nM, respectively, relative to exemestane’s IC₅₀ of 210.0 ± 0.16 nM. Furthermore, <em>in silico</em> studies predicted that these inhibitors <strong>1</strong>–<strong>3</strong> were able to occupy the active site and interacted with catalytically important residues of the enzyme. While molecular dynamic simulation predicted the stability of aromatase- ligand complexes. The studies identified that metabolites <strong>1</strong> and <strong>3</strong> can serve as drug candidate after further development.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109647"},"PeriodicalIF":2.1,"publicationDate":"2025-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144249668","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 of 25-hydroxycholesterol from bisnoralcohol","authors":"Bu-Luan Liang ,&nbsp;Yan-Xin Yue ,&nbsp;De-Jie Zhang ,&nbsp;Hao-Jie Ni ,&nbsp;Xiang-Zhong Gu ,&nbsp;Wen-Wei Qiu ,&nbsp;Chen-Chen Li","doi":"10.1016/j.steroids.2025.109640","DOIUrl":"10.1016/j.steroids.2025.109640","url":null,"abstract":"<div><div>25-Hydroxycholesterol not only exhibits various important biological activities but also plays a crucial role in the synthesis of 25-hydroxyvitamin D₃. To date, researchers have proposed multiple synthetic routes for 25-hydroxycholesterol. Herein, a novel synthetic method for 25-hydroxycholesterol is described, involving a seven-step reaction that starts from economical and commercially available plant-derived bisnoralcohol, with an overall yield of up to 43.4%. Key reaction conditions, including solvents, reaction temperatures, bases and catalysts, were thoroughly investigated and optimized. This novel synthetic route provides a cost-effective strategy for the potential large-scale production of plant-derived 25-hydroxycholesterol.</div></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"221 ","pages":"Article 109640"},"PeriodicalIF":2.1,"publicationDate":"2025-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144213488","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}