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Exploring the urate lowering properties of Erigeron annuus Lin. and phytosterol contributions: In vitro assays and in silico approaches 探讨了灯盏花的降尿酸性能。和植物甾醇的贡献：体外分析和计算机方法
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-07-09 DOI: 10.1016/j.steroids.2025.109657
Rupali Rana , Anchal Sharma , Nitish Kumar , Pallvi Mohanna , Jyoti , Aanchal Khanna , Jatinder Vir Singh , Preet Mohinder Singh Bedi

Background

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 Erigeron annuus Lin. (E. annuus) using in vitro and in silico models.

Objective

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.

Methods

A hydroalcoholic extract was prepared using a Soxhlet apparatus. Column chromatography and spectroscopic techniques were employed to isolate and identify two phytosterols: RR1 (β-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.

Results

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.

Conclusion

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.
由于一些黄嘌呤氧化酶（XO）抑制剂存在严重的超敏风险，因此迫切需要开发具有更高安全性和有效ADME特性的新型药物。本研究评价了春花的抗高尿酸和抗氧化活性。（E. annuus）在体外和计算机模型中的应用。目的研究黄连地上部水醇粗提物、分离部位及分离化合物的体外XO抑制和抗氧化活性。方法采用索氏装置制备水乙醇提取物。采用柱层析和光谱技术分离鉴定了两种植物甾醇：RR1 （β-谷甾醇）和RR2（豆甾醇）。使用DE Shaw Desmond软件进一步提出了基于药效团的假设；还分别使用LeadIT软件和Swiss ADME对硅片进行了评估。使用Biotek多模式平板阅读器测量XO抑制活性，通过DPPH和FRAP测定抗氧化活性。此外，我们还评估了强效化合物RR2对HepG2细胞株的细胞毒性。结果各萃取部位对XO活性均有抑制作用，IC50值在0.086 ~ 36.71µg/mL之间。别嘌呤醇作为阳性对照，IC50为0.027µg/mL。正己烷部位对XO的抑制作用最强（IC50 = 0.086µg/mL）。RR2 （stigmastrol）对该部位有明显的抑制作用，IC50为0.331µg/mL。抗氧化试验和细胞毒性研究也证实了这些组分的生物活性。结论荆芥正己烷部分具有较强的XO抑制活性，为开发高尿酸血症和痛风的草药治疗提供了重要的研究价值。该研究验证了传统用法，支持药效团假说，提示甾醇核结构优化可提高治疗效果。
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引用次数: 0
The effect of various corticosteroids in the hospitalized patients with moderate and severe COVID-19: A tertiary hospital experience 各种糖皮质激素对中重度COVID-19住院患者的影响：三级医院经验
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-07-17 DOI: 10.1016/j.steroids.2025.109659
Hemasri Velmurugan , Pugazhenthan Thangaraju , Pankaj kumar kannauje , Muthathal Subramanian

Background

The pandemic of COVID-19 caused by the SARS-CoV-2 has irrevocably altered the lives of human beings and is challenging national health systems worldwide. Many treatment strategies have been put out to lessen the damage to the inflammatory organs in COVID-19 pneumonia cases, and corticosteroids are one of the most promising pharmaceutical treatments.

Aim

To assess the efficacy and safety of various corticosteroids (Dexamethasone, Methylprednisolone, Prednisolone, and Hydrocortisone) among patients with moderate and severe COVID-19 who received corticosteroids during their hospital stay.

Methods

It was a record-based retrospective cohort study conducted between April 1st, 2020, and June 30th, 2021, at the tertiary care teaching hospital, All India Institutes of Medical Sciences (AIIMS), Raipur. Only patients who received corticosteroids during their hospital stay were included in the study. COVID-19 severity was assessed using the WHO ordinal scale, where scores range from 0 (uninfected) to 8 (death).

Results

Out of 431 patients, 243 (56 %) patients survived and 188 (44 %) patients did not survive. Most patients were admitted with a WHO ordinal score of 4 (n = 239, 55.4 %), followed by score 5 (n = 4, 1 %), who were discharged with a score of 0 or 1 and more in group 1. More patients died in group 5 and group 2. 155 (35.9 %) patients did not survive in the severe group, followed by 33 (7.7 %) in the moderate group.

Conclusion

More research on the safety and effectiveness of corticosteroids is needed to improve the in-hospital care of COVID-19. The study found that using corticosteroids in combination and higher doses for longer durations will help policymakers recommend strict guidelines. We looked for dose and duration compliance and the relationship between adverse events and diabetes patients. However, the findings of this study support dexamethasone as a promising agent in the fight against SARS-CoV-2.
由SARS-CoV-2引起的COVID-19大流行已经不可逆转地改变了人类的生活，并对世界各国的国家卫生系统提出了挑战。为了减轻COVID-19肺炎患者炎症器官的损伤，已经提出了许多治疗策略，其中糖皮质激素是最有前途的药物治疗之一。目的评价住院期间接受糖皮质激素治疗的中重度COVID-19患者使用各种糖皮质激素（地塞米松、甲基强的松龙、泼尼松龙和氢化可的松）的疗效和安全性。方法本研究是一项基于记录的回顾性队列研究，于2020年4月1日至2021年6月30日在Raipur全印度医学科学研究所（AIIMS）三级护理教学医院进行。只有在住院期间接受皮质类固醇治疗的患者被纳入研究。COVID-19严重程度采用世卫组织序数量表进行评估，得分范围从0（未感染）到8（死亡）。结果431例患者中，243例（56%）患者存活，188例（44%）患者未存活。大多数患者入院时WHO评分为4分（n = 239, 55.4%），其次是5分（n = 4, 1%）， 1组患者出院时评分为0分或1分以上。第5组和第2组患者死亡较多。重度组155例（35.9%）死亡，中度组33例（7.7%）死亡。结论需进一步研究糖皮质激素的安全性和有效性，以改善COVID-19的住院护理。该研究发现，结合使用皮质类固醇，并在更长的时间内使用更高的剂量，将有助于政策制定者推荐严格的指导方针。我们寻找剂量和持续时间依从性以及不良事件与糖尿病患者之间的关系。然而，这项研究的结果支持地塞米松作为对抗SARS-CoV-2的有前途的药物。
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引用次数: 0
Association of CYP27B1 promoter gene variants of vitamin D pathway with pulmonary tuberculosis and vitamin D levels 维生素D通路CYP27B1启动子基因变异与肺结核和维生素D水平的关系
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-07-08 DOI: 10.1016/j.steroids.2025.109656
Harishankar Murugesan , Pavithra Sampath , Karthikeyan Ramamurthy , Aarti Muralitharan , Dhanyaa Muthukumaran , Athikesavan Veerasamy , Uma Devi Ranganathan , Selvaraj Paramasivam , Ramalingam Bethunaickan
Cyp27b1 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 Cyp27b1 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 (<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.
Cyp27b1多态性与包括结核病（TB）在内的不同疾病有关。由于位于启动子区域的基因变异可能对基因转录/翻译有重大影响，并且Cyp27b1酶参与维生素D代谢的关键步骤，我们的目的是研究Cyp27b1基因启动子变异- 1077 (C/G)，- 1260 （C/A）和距离启动子- 1918 (C/T) 5 '的区域与肺结核风险/防御有任何联系，并确定它们对正常健康对照（hc）和南印度人口肺结核（PTB）患者维生素D水平的影响。盐析法提取基因组DNA后，采用聚合酶链反应和限制性片段长度多态性（PCR-RFLP）法进行基因分型。采用酶联免疫吸附试验（ELISA）测定维生素d的含量。在共显性模型中，−1077“GG”基因型与结核病易感性显著相关[比值比（OR）： 2.10(1.18-3.73)；p = 0.015]。此外，在优势模型中检测到与TB保护显著的关联[GG vs CG + CC， OR: 0.40(0.21-0.75)；p = 0.0035]。在- 1918 （C/T）变异中，在杂合的- 1918“CT”基因型中发现了与结核病风险的实质性联系[OR: 1.90 (1.05-3.44)；p = 0.046]在共显性模型中，而在较少复发的“TT”基因型中检测到保护性连锁[OR: 0.42 (0.19-0.94)；p = 0.049]。此外，这些危险基因型与男性比女性更容易患结核病有实质性的联系。单倍型分析揭示了- 1077和- 1260变异之间的强联系，发现其单倍型“GC”（- 1077G, - 1260C）与结核病风险增加显著相关。在- 1077“GG”、- 1260“CA”和- 1918“CT”危险基因型中，PTB患者中维生素D缺乏症（<20 ng/ml）的检测频率高于hc。这需要在未来的研究中通过更大的样本量来证实。
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引用次数: 0
Corrigendum to "Advances in the understanding of androgen receptor structure and function and in the development of next-generation AR-targeted therapeutics". [Steroids 210 (2024) 109486]. “雄激素受体结构和功能的理解进展以及下一代ar靶向治疗的发展”的勘误表。[类固醇210(2024)109486]。
IF 2.3 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-07-24 DOI: 10.1016/j.steroids.2025.109661
Wendy Effah, Marjana Khalil, Dong-Jin Hwang, Duane D Miller, Ramesh Narayanan
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引用次数: 0
The impact of serum estradiol levels on vaginal pH and Candida infections during infertility treatment 血清雌二醇水平对不孕症治疗期间阴道pH和念珠菌感染的影响。
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-06-21 DOI: 10.1016/j.steroids.2025.109655
Çağın Çakırgöz , Emine Çakırgöz , Dilara Kirmiç , Pınar Solmaz Hasdemir , Kenan Değerli

Purpose

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.

Methods

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 < 0.05.

Results

Post-treatment analysis revealed a significant increase in serum E2 and vaginal pH levels (p < 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.

Conclusion

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.
目的：本研究旨在评估血清E2水平对不孕症妇女阴道pH调节和念珠菌定植的潜在影响，强调粘膜屏障动力学和上皮免疫调节。方法：在这项前瞻性观察研究中，纳入了60名年龄在20-49岁之间接受长期促排卵治疗的女性。在周期第2天（基线）评估血清E2水平、阴道pH值和真菌培养，并在雌二醇峰值时再次评估，雌二醇峰值通常在人绒毛膜促性腺激素（hCG）给药前和超声确认的卵泡成熟后24 h内。结果：治疗后分析显示，血清E2和阴道pH水平显著升高（p ）。结论：这些发现表明，在不孕症治疗期间，激素E2升高，尽管与阴道pH升高有关，但不会增加念珠菌感染的风险。尽管激素变化，上皮屏障功能的保存可以解释这一发现。这些结果支持关于念珠菌敏感性的控制卵巢刺激方案的微生物安全性。
{"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":"2025-09-01","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}
引用次数: 0
Synthesis of 25-hydroxycholesterol from bisnoralcohol 双诺醇合成25-羟基胆固醇
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-06-02 DOI: 10.1016/j.steroids.2025.109640
Bu-Luan Liang , Yan-Xin Yue , De-Jie Zhang , Hao-Jie Ni , Xiang-Zhong Gu , Wen-Wei Qiu , Chen-Chen Li
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.
25-羟基胆固醇不仅具有多种重要的生物活性，而且在25-羟基维生素D3的合成中起着至关重要的作用。迄今为止，研究人员已经提出了多种合成25-羟基胆固醇的途径。本文描述了一种新的合成25-羟基胆固醇的方法，包括从经济和商业上可用的植物衍生的双去甲醇开始的七步反应，总收率高达43.4%。对溶剂、反应温度、碱和催化剂等关键反应条件进行了研究和优化。这种新的合成路线为大规模生产植物源性25-羟基胆固醇提供了一种具有成本效益的策略。
{"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 D<sub>3</sub>. 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":"2025-09-01","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}
引用次数: 0
α-Bromoketone derivatives from lithocholic acid: a comprehensive evaluation of their antibacterial activity 石胆酸α-溴酮衍生物抗菌活性的综合评价。
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-07-10 DOI: 10.1016/j.steroids.2025.109658
Mónica Díaz-Fernández , Jesús Ramón-Sierra , Elizabeth Ortiz-Vázquez , María A. Fernández-Herrera
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.
以石胆酸为原料，经氧化溴化反应合成了6个α-溴酮，其中4个为首次报道。所有的产物都用核磁共振、红外光谱和质谱进行了表征。通过x射线衍射分析进一步证实了两种α-溴酮的结构和晶体排列。化合物的抗菌活性被评估对革兰氏阴性和革兰氏阳性菌株的临床相关性。
{"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":"2025-09-01","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}
引用次数: 0
Laetiporus sulphureus mushroom culture − source of secondary metabolites, and as a catalyst for biotransformation of breast cancer drug exemestane 乳腺癌药物依西美坦的次生代谢物来源及生物转化催化剂。
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-06-06 DOI: 10.1016/j.steroids.2025.109647
Yagut Yusifova , Atia-tul-Wahab , M. Iqbal Choudhary , Mahwish Siddiqui , Nisha Khan , Muhammad Atif , Humaira Zafar , Sayyara J. Ibadullayeva , Dilzara N. Aghayeva
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, 3β-hydroxy-24-methylenelanost-8-en-21-oic acid (1) was isolated from Laetiporus sulphureus (Bull.) Murrill. The cell culture of the same mushroom was used for the biotransformation of breast cancer drug, exemestane (2) into a new analogue, 18-hydroxy-6-methylene-androsta-1,4-diene-3,17-dione (3). Compounds 1, and 3 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 1 also has a steroidal skeleton (like aromatase inhibiting drug exemestane (2)), the metabolite 1 was also evaluated for its aromatase inhibitory potential, along with a new transformed product 3. 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 1 and 3 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, in silico studies predicted that these inhibitors 1–3 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 1 and 3 can serve as drug candidate after further development.
目前，某些蘑菇被用作低热量的食品补充剂，因为它们的味道很好，而且含有各种必需的维生素、矿物质和次级代谢物。其中许多具有治疗意义，被用于传统药物中。蘑菇细胞也可以用作有机化合物衍生化的生物催化剂。本研究从硫酸Laetiporus sulureus （Bull.）中分离得到3β-羟基-24-亚甲基烯酸-8-烯-21-酸(1)。Murrill。该菌的细胞培养用于将乳腺癌药物依西美坦(2)转化为新的代谢物18-羟基-6-亚甲基- androta -1,4-二烯-3,17-二酮(3)。化合物1和3通过各种色谱技术纯化，并通过1D和2d nmr、HREI-MS和IR光谱技术对其结构进行了测定。由于化合物1也具有甾体骨架（如芳香化酶抑制药物依西美坦(2)），因此也评估了代谢物1及其新的转化产物3的芳香化酶抑制潜力。芳香化酶在雌激素的生物合成中起着至关重要的作用，抑制其成为治疗雌激素受体阳性（ER+）乳腺癌的关键治疗策略。化合物1和3展示了重要的芳香化酶抑制,与590年的IC50值 ±0.03   nM和337.5±0.01  nM,分别相对于依西美坦的IC50 210.0±0.16  nM。此外，硅研究预测这些抑制剂1-3能够占据活性位点并与催化重要残基相互作用。分子动力学模拟预测了芳香化酶-配体配合物的稳定性。研究发现，代谢物1和3在进一步开发后可作为候选药物。
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引用次数: 0
Mycochemical investigation, antioxidant, cytotoxic and enzyme inhibition activities of truffle Picoa lefebvrei 松露Picoa lefebvrei的真菌化学、抗氧化、细胞毒和酶抑制活性研究
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-06-11 DOI: 10.1016/j.steroids.2025.109651
Çiğdem Kuş , Meltem Taş Küçükaydın , Selçuk Küçükaydın , Mehmet Emin Duru , Mehmet Öztürk
Picoa lefebvrei (Pat.) Maire is a truffle species that belongs to the Cistaceae family and grows mycorrhizally on the roots of Helianthemum species. Picoa 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 P. lefebvrei extracts namely, brassicasterol (1), brassicasteryl-β-ᴅ-glucopyranoside (2), uracil (3), l-uridine (4), erythritol (5), α-ᴅ-glucopyranosyl-α-ᴅ-glucopyranoside (6), brassicasteryl linoleate (7) and 5α-6α-epoxy ergosta-7,22-diene-3β-ol (8) 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 P. lefebvrei were investigated. Compound 4 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 3 and 8 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 8 had strongest cytotoxicity with IC50 value of 33.94 ± 0.47 µg/mL against the H1299 lung cancer cells. Nevertheless, compound 1 (IC50:24.72 ± 0.75 µg/mL), showed the greatest cytotoxicity against the MCF-7 breast cancer cells. These findings indicate that P. lefebvrei, is rich in steroidal compounds and is a possible source of ergostane-type steroids. Furthermore, this first detailed investigation highlights the potential of P. lefebvrei as a natural food and as a source of bioactive compounds.
Picoa lefebvrei（帕特）麦尔松露是一种松露，属于松露科，菌根生长在菊花的根部。Picoa原产于西安纳托利亚和突尼斯，是人们首选的食物，具有经济潜力。近年来，人们对蘑菇的生物活性成分越来越感兴趣，食用蘑菇和一些松露被用于新一代的生物治疗药物。本研究通过不同的色谱方法，从P. lefebvrei提取物中分离得到8个化合物，分别为：油菜甾醇(1)、油菜甾醇-β-酰-氨基葡萄糖苷(2)、尿嘧啶(3)、l-尿苷(4)、赤藓糖醇(5)、α-酰-氨基葡萄糖苷(6)、油菜甾醇亚油酸酯(7)和5α-6α- 6α-环氧麦角糖-7,22-二烯-3β-醇(8)。此外，还对其提取物和化合物的抗氧化活性、抗胆碱酯酶活性、抗脲酶活性和细胞毒活性（对MCF-7、H1299和L929细胞系）进行了研究。化合物4在DPPH（2,2-二苯基-1-picrylhydrazyl）、ABTS (2,2 ' - azno -bis（3-乙基苯并噻唑-6-磺酸）和CUPRAC （cu离子还原抗氧化能力）试验中的IC50值分别为92.61±0.10、70.55±0.84和112.08±0.15µg/mL，显示出最高的抗氧化活性。化合物3和8对乙酰胆碱酯酶（AChE）（44.59±0.37%）和丁基胆碱酯酶（BChE）（53.15±1.07%）和54.97±0.41%)的抑制活性最高。化合物8对H1299肺癌细胞的细胞毒性最强，IC50值为33.94±0.47µg/mL。然而，化合物1 （IC50:24.72±0.75µg/mL）对MCF-7乳腺癌细胞表现出最大的细胞毒性。这些发现表明，P. lefebvrei富含甾体化合物，可能是麦角甾类类固醇的来源。此外，这项首次详细的调查强调了P. lefebvrei作为天然食品和生物活性化合物来源的潜力。
{"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 IC<sub>50</sub> 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 IC<sub>50</sub> value of 33.94 ± 0.47 µg/mL against the H1299 lung cancer cells. Nevertheless, compound <strong>1</strong> (IC<sub>50</sub>: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":"2025-09-01","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}
引用次数: 0
Bidirectional effect of ecdysterone on thymocyte volume regulation and proliferation 外皮酮对胸腺细胞体积调节和增殖的双向作用
IF 2.1 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Steroids
Pub Date : 2025-09-01 Epub Date: 2025-06-19 DOI: 10.1016/j.steroids.2025.109653
Fariza A. Salimova , Sarvinoz I. Rustamova , Sirojbek A. Khojiboev , Ozoda J. Khamidova , Petr G. Merzlyak , Diyor D. Fayziev , Vladimir N. Syrov , Feruza R. Egamova , Ranokhon Sh. Kurbannazarova , Ravshan Z. Sabirov
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 per os 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.
T细胞的发育和成熟需要一个高效的细胞体积调节（CVR）系统，其中体积敏感的外向整流阴离子通道（VSOR/VRAC）起着关键作用。众所周知，蜕皮酮（20-羟基蜕皮酮，20HE）在哺乳动物中发挥多种作用，但胸腺和胸腺细胞对这种激素的反应实际上尚未被探索。在本研究中，我们观察到20HE对胸腺及其细胞内容物的双向作用。在短期内，胸腺细胞通过阻断VSOR/VRAC做出反应，阻断的一半有效浓度为~ 33-37 μM，在100 μM时观察到的最大抑制为57 - 62%。胸腺细胞RVD的抑制程度较低，约为31%，但在约8 μM的半最大浓度下更有效。与短期效应相反，在原代培养条件下，胸腺细胞长期暴露于20HE可增加其增殖活性（24小时后增加~ 67%），而VSOR/VRAC活性没有可检测到的变化。与此结果一致的是，在整个生物体水平上，连续5天给药20HE强烈刺激了胸腺生长（约61%），并上调了从20HE处理动物中分离的细胞的CVR效率（参数RVD增加约12%）。结果表明，20HE的全身效应可能会抵消缓冲盐水中类固醇引起的胸腺细胞VSOR/VRAC和RVD的急性阻断，这种效应只有在原代培养条件下或在整个机体中长期暴露后才会显现。
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