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Clomiphene citrate as a new modality in management of vaginal bleeding with depomedroxyprogesterone acetate (DMPA): A randomized controlled trial 枸橼酸氯米芬作为醋酸去甲地孕酮(DMPA)治疗阴道出血的新方法:随机对照试验
IF 2.7 4区 医学
Steroids Pub Date : 2024-04-16 DOI: 10.1016/j.steroids.2024.109425
Kareem Shaheen , Hany H. Kamel , Enas Mostafa Mohammed , Ahmed Hashim Mohammed , Sileem Ahmed Sileem , Mahmoud Fouad , Zainab Shehata Sayd , Mohamed E. ElHodiby
{"title":"Clomiphene citrate as a new modality in management of vaginal bleeding with depomedroxyprogesterone acetate (DMPA): A randomized controlled trial","authors":"Kareem Shaheen ,&nbsp;Hany H. Kamel ,&nbsp;Enas Mostafa Mohammed ,&nbsp;Ahmed Hashim Mohammed ,&nbsp;Sileem Ahmed Sileem ,&nbsp;Mahmoud Fouad ,&nbsp;Zainab Shehata Sayd ,&nbsp;Mohamed E. ElHodiby","doi":"10.1016/j.steroids.2024.109425","DOIUrl":"https://doi.org/10.1016/j.steroids.2024.109425","url":null,"abstract":"<div><h3>Background</h3><p>Depo-medroxyprogesterone acetate (DMPA) functions as a contraceptive method by inhibiting the secretion of gonadotropins, which prevents follicular maturation and ovulation, as well as thinning of the endometrium leading to unscheduled vaginal bleeding and subsequent discontinuation of DMPA. Our study aimed to evaluate the efficacy and safety of clomiphene citrate (CC) in stopping bleeding among DMPA users.</p></div><div><h3>Materials and Methods</h3><p>We randomly assigned 200 DMPA users using a computer-generated random numbers table in a 1:1 ratio to one of two groups; the study group, which received CC at a dose of 50 mg twice daily for five days (n = 100), and the control group, which received a placebo for five days (n = 100). Our primary outcome measure was the onset and duration of bleeding cessation. Secondary outcomes included endometrial thickness, recurrence of vaginal bleeding, and any reported side effects associated with CC use.</p></div><div><h3>Results</h3><p>Clomiphene citrate significantly resulted in early cessation of vaginal bleeding in 83 % of the patients, which continued for three months of follow-up. In addition, the recurrence of vaginal bleeding was significantly reduced in the CC group compared to the control group (11 % vs. 67 %; <em>p</em> &lt; 0.001). Endometrial thickness was significantly greater in the CC group than in the control group (<em>p</em> &lt; 0.001). Breast tenderness was more frequently reported in the study group, with no difference in dyspareunia between the two groups.</p></div><div><h3>Conclusions</h3><p>Clomiphene citrate is effective in controlling bleeding among DMPA users. Further studies are encouraged to confirm our findings.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"206 ","pages":"Article 109425"},"PeriodicalIF":2.7,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140645906","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
Sex and sex steroids as determinants of cardiovascular risk 性别和性类固醇是心血管风险的决定因素
IF 2.7 4区 医学
Steroids Pub Date : 2024-04-16 DOI: 10.1016/j.steroids.2024.109423
Andrea Cignarella , Chiara Bolego , Matthias Barton
{"title":"Sex and sex steroids as determinants of cardiovascular risk","authors":"Andrea Cignarella ,&nbsp;Chiara Bolego ,&nbsp;Matthias Barton","doi":"10.1016/j.steroids.2024.109423","DOIUrl":"https://doi.org/10.1016/j.steroids.2024.109423","url":null,"abstract":"<div><p>There are considerable sex differences regarding the risk of cardiovascular disease (CVD), including arterial hypertension, coronary artery disease (CAD) and stroke, as well as chronic renal disease. Women are largely protected from these conditions prior to menopause, and the risk increases following cessation of endogenous estrogen production or after surgical menopause. Cardiovascular diseases in women generally begin to occur at a later age than in men (on average with a delay of 10 years). Cessation of estrogen production also impacts metabolism, increasing the risk of developing obesity and diabetes. In middle-aged individuals, hypertension develops earlier and faster in women than in men, and smoking increases cardiovascular risk to a greater degree in women than it does in men. It is not only estrogen that affects female cardiovascular health and plays a protective role until menopause: other sex hormones such as progesterone and androgen hormones generate a complex balance that differentiates heart and blood vessel function in women compared to men. Estrogens improve vasodilation of epicardial coronary arteries and the coronary microvasculature by augmenting the release of vasodilating factors such as nitric oxide and prostacyclin, which are mechanisms of coronary vasodilatation that are more pronounced in women compared to men. Estrogens are also powerful inhibitors of inflammation, which in part explains their protective effects on CVD and chronic renal disease. Emerging evidence suggests that sex chromosomes also play a significant role in shaping cardiovascular risk. The cardiovascular protection conferred by endogenous estrogens may be extended by hormone therapy, especially using bioidentical hormones and starting treatment early after menopause.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"206 ","pages":"Article 109423"},"PeriodicalIF":2.7,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140645907","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
CBC-1 as a Cynanbungeigenin C derivative inhibits the growth of colorectal cancer through targeting Hedgehog pathway component GLI 1 CBC-1 作为赛南皂甙元 C 衍生物,通过靶向刺猬蛋白通路成分 GLI 1 抑制结直肠癌的生长
IF 2.7 4区 医学
Steroids Pub Date : 2024-04-11 DOI: 10.1016/j.steroids.2024.109421
Jinwen Chen , Wei Chen , Xiaoyu Li , Yiping Ye , Wenkang Huang , Lijuan Gao , Meng Zhang
{"title":"CBC-1 as a Cynanbungeigenin C derivative inhibits the growth of colorectal cancer through targeting Hedgehog pathway component GLI 1","authors":"Jinwen Chen ,&nbsp;Wei Chen ,&nbsp;Xiaoyu Li ,&nbsp;Yiping Ye ,&nbsp;Wenkang Huang ,&nbsp;Lijuan Gao ,&nbsp;Meng Zhang","doi":"10.1016/j.steroids.2024.109421","DOIUrl":"https://doi.org/10.1016/j.steroids.2024.109421","url":null,"abstract":"<div><p>Colorectal cancer (CRC) is one of the most common gastrointestinal cancers that results in death in worldwide. The Hedgehog (HH) signalling pathway regulates the initiation and progression of CRC. Inhibiting the HH pathway has been presented as a potential treatment strategy in recent years. Cynanbungeigenin C (CBC) is a new type of C<sub>21</sub> steroid that has been previously reported for the treatment of medulloblastoma. However, its further investigation was limited by its poor water solubility. In this study, six new CBC derivatives were synthesized through the structural modification of CBC, and four of them showed better water solubility than CBC. Moreover, their antiproliferative activities on CRC were evaluated. It was found that CBC-1 presented the best inhibitory effect on three types of CRC cell lines, and this effect was superior to that of CBC. Mechanistically, CBC-1 inhibited the proliferation of CRC cells through regulation of mRNA and proteins of the HH pathway according to qRT–PCR and Western blotting analysis. Furthermore, Cellular Thermal Shift Assay results indicated that CBC-1 regulated this signalling pathway by targeting glioma‑associated oncogene (GLI 1).In addition, cell apoptosis was induced increasingly by transfection with GLI 1 siRNA or treatment with CBC-1 to downregulate GLI 1. Last, the in vivo results demonstrated that CBC-1 significantly reduced tumour size and downregulated GLI 1 in CRC. Therefore, this study suggests that CBC-1, a new GLI 1 inhibitor derived from natural products, may be developed as a potential antitumour candidate for CRC treatment.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"206 ","pages":"Article 109421"},"PeriodicalIF":2.7,"publicationDate":"2024-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140633315","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
Association between sex hormones and gout: An analysis of the UK Biobank cohort 性激素与痛风之间的关系:英国生物库队列分析
IF 2.7 4区 医学
Steroids Pub Date : 2024-04-09 DOI: 10.1016/j.steroids.2024.109422
Yaoyao Jiang , Sen Liu , Gang Liu , An Pan , Miaomiao Peng , Yunfei Liao
{"title":"Association between sex hormones and gout: An analysis of the UK Biobank cohort","authors":"Yaoyao Jiang ,&nbsp;Sen Liu ,&nbsp;Gang Liu ,&nbsp;An Pan ,&nbsp;Miaomiao Peng ,&nbsp;Yunfei Liao","doi":"10.1016/j.steroids.2024.109422","DOIUrl":"10.1016/j.steroids.2024.109422","url":null,"abstract":"<div><h3>Objectives</h3><p>To investigate the associations between sex hormones and gout.</p></div><div><h3>Methods</h3><p>A total of 448,836 individuals free of gout at baseline were included from the UK Biobank. Cox regression models were used to estimate hazard ratios (HRs) for gout. Besides, we investigated the causal relationship between bioavailable testosterone (BAT) and gout using mendelian randomization (MR).</p></div><div><h3>Results</h3><p>There were differential effects in different testosterone active states in gout. One-unit higher log-transformed total testosterone (TT) was associated with a 52 % [95 % CI, 0.39–0.58] lower risk of gout in males. In contrast, free testosterone (FT) and BAT were associated with a 74 % [95 % CI, 1.38–2.20] and a 78 % [95 % CI, 1.41–2.25] higher risk of gout in males respectively. For MR, the weighted median [OR, 1.70; 95 % CI, 1.14–2.56;] and inverse variance-weighted [OR, 1.25; 95 % CI, 0.96–1.62; <em>P</em> = 0.09] method revealed significant and approximately significant positive effect of genetic liability to BAT levels on the risk of gout respectively.</p></div><div><h3>Conclusions</h3><p>Sex hormones were potentially associated with gout. Notably, we were the first to explore different testosterone states on gout and found that FT and BAT may increase the risk of gout in males, which is opposite to TT. And the former are active states of androgens, may be more accurately reflect the association between androgens and gout.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"207 ","pages":"Article 109422"},"PeriodicalIF":2.7,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140793311","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
Anabolic steroids in livestock production: Background and implications for chemical food safety 家畜生产中的合成代谢类固醇:化学食品安全的背景和影响
IF 2.7 4区 医学
Steroids Pub Date : 2024-04-03 DOI: 10.1016/j.steroids.2024.109420
Ting Chen, Bruno Le Bizec, Gaud Dervilly
{"title":"Anabolic steroids in livestock production: Background and implications for chemical food safety","authors":"Ting Chen,&nbsp;Bruno Le Bizec,&nbsp;Gaud Dervilly","doi":"10.1016/j.steroids.2024.109420","DOIUrl":"https://doi.org/10.1016/j.steroids.2024.109420","url":null,"abstract":"<div><p>The use of steroids in livestock animals is a source of concern for consumers because of the risks associated with the presence of their residues in foodstuffs of animal origin. Technological advances such as mass spectrometry have made it possible to play a fundamental role in controlling such practices, firstly for the discovery of marker metabolites but also for the monitoring of these compounds under the regulatory framework. Current control strategies rely on the monitoring of either the parent drug or its metabolites in various matrices of interest. As some of these steroids also have an endogenous status specific strategies have to be applied for control purposes. This review aims to provide a comprehensive and up-to-date knowledge of analytical strategies, whether targeted or non-targeted, and whether they focus on markers of exposure or effect in the specific context of chemical food safety regarding the use of anabolic steroids in livestock. The role of new approaches in data acquisition (e.g. ion mobility), processing and analysis, (e.g. molecular networking), is also discussed.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"206 ","pages":"Article 109420"},"PeriodicalIF":2.7,"publicationDate":"2024-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0039128X24000588/pdfft?md5=deaa396d05bdfaab30bf9193b1247750&pid=1-s2.0-S0039128X24000588-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140650216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Corrigendum to “Govanosides C-F, unprecedented steroidal saponins with rare sugars from rhizomes of Trillium govanianum and their antagonistic effects on acetylcholinesterase” [Steroids 199 (2023) 109293] 戈万甙 C-F,从戈万年三叶草根茎中提取的前所未有的含稀有糖类的甾体皂甙及其对乙酰胆碱酯酶的拮抗作用》[甾体 199 (2023) 109293]勘误表
IF 2.7 4区 医学
Steroids Pub Date : 2024-03-25 DOI: 10.1016/j.steroids.2024.109396
Prithvi Pal Singh , Patil Shivprasad Suresh , Anmol , Upendra Sharma
{"title":"Corrigendum to “Govanosides C-F, unprecedented steroidal saponins with rare sugars from rhizomes of Trillium govanianum and their antagonistic effects on acetylcholinesterase” [Steroids 199 (2023) 109293]","authors":"Prithvi Pal Singh ,&nbsp;Patil Shivprasad Suresh ,&nbsp;Anmol ,&nbsp;Upendra Sharma","doi":"10.1016/j.steroids.2024.109396","DOIUrl":"https://doi.org/10.1016/j.steroids.2024.109396","url":null,"abstract":"","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"204 ","pages":"Article 109396"},"PeriodicalIF":2.7,"publicationDate":"2024-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0039128X24000345/pdfft?md5=3b33c78ee1cb0339b7c90c53ad10dcaf&pid=1-s2.0-S0039128X24000345-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140209161","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Estrogen and testosterone secretion from the mouse brain 小鼠大脑分泌的雌激素和睾酮
IF 2.7 4区 医学
Steroids Pub Date : 2024-03-19 DOI: 10.1016/j.steroids.2024.109398
Ruby Vajaria , DeAsia Davis , Kongkidakorn Thaweepanyaporn , Janine Dovey , Slawomir Nasuto , Evangelos Delivopoulos , Francesco Tamagnini , Philip Knight , Nandini Vasudevan
{"title":"Estrogen and testosterone secretion from the mouse brain","authors":"Ruby Vajaria ,&nbsp;DeAsia Davis ,&nbsp;Kongkidakorn Thaweepanyaporn ,&nbsp;Janine Dovey ,&nbsp;Slawomir Nasuto ,&nbsp;Evangelos Delivopoulos ,&nbsp;Francesco Tamagnini ,&nbsp;Philip Knight ,&nbsp;Nandini Vasudevan","doi":"10.1016/j.steroids.2024.109398","DOIUrl":"10.1016/j.steroids.2024.109398","url":null,"abstract":"<div><p>Estrogen and testosterone are typically thought of as gonadal or adrenal derived steroids that cross the blood brain barrier to signal via both rapid nongenomic and slower genomic signalling pathways. Estrogen and testosterone signalling has been shown to drive interlinked behaviours such as social behaviours and cognition by binding to their cognate receptors in hypothalamic and forebrain nuclei. So far, acute brain slices have been used to study short-term actions of 17β-estradiol, typically using electrophysiological measures. For example, these techniques have been used to investigate, nongenomic signalling by estrogen such as the estrogen modulation of long-term potentiation (LTP) in the hippocampus. Using a modified method that preserves the slice architecture, we show, for the first time, that acute coronal slices from the prefrontal cortex and from the hypothalamus maintained in aCSF over longer periods i.e. 24 h can be steroidogenic, increasing their secretion of testosterone and estrogen. We also show that the hypothalamic nuclei produce more estrogen and testosterone than the prefrontal cortex. Therefore, this extended acute slice system can be used to study the regulation of steroid production and secretion by discrete nuclei in the brain.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"204 ","pages":"Article 109398"},"PeriodicalIF":2.7,"publicationDate":"2024-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0039128X24000369/pdfft?md5=141813e067e26d34ea251f9e3345318c&pid=1-s2.0-S0039128X24000369-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140185642","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Further evidence for blood-to-brain influx of unconjugated bile acids by passive diffusion: Determination of their brain-to-serum concentration ratios in rats by LC/MS/MS 非结合胆汁酸通过被动扩散从血液流入大脑的进一步证据:通过 LC/MS/MS 测定大鼠脑部与血清的胆汁酸浓度比。
IF 2.7 4区 医学
Steroids Pub Date : 2024-03-18 DOI: 10.1016/j.steroids.2024.109397
Toma Shibuya, Anri Sato, Shoich Nishimoto-Kusunose, Kazumi Yoshizawa, Tatsuya Higashi
{"title":"Further evidence for blood-to-brain influx of unconjugated bile acids by passive diffusion: Determination of their brain-to-serum concentration ratios in rats by LC/MS/MS","authors":"Toma Shibuya,&nbsp;Anri Sato,&nbsp;Shoich Nishimoto-Kusunose,&nbsp;Kazumi Yoshizawa,&nbsp;Tatsuya Higashi","doi":"10.1016/j.steroids.2024.109397","DOIUrl":"10.1016/j.steroids.2024.109397","url":null,"abstract":"<div><p>Bile acids (BAs) reside in the brain and are probably involved in some neurological disorders. The view that most of unconjugated BAs in the brain are derived across the blood–brain barrier from the periphery by passive diffusion depending on their hydrophobicity is currently dominant, but some studies have made conflicting claims. In this study, the correlation analysis between the rat brain and serum levels of unconjugated BAs with a wider range of hydrophobicity was conducted to obtain further evidence about the blood-to-brain influx of unconjugated BAs by passive diffusion. We first developed the precise, accurate and matrix effect-free LC/ESI-MS/MS methods for quantifying eight major unconjugated BAs in the rat brain and serum. Derivatization was employed for increasing the assay sensitivity and specificity. The analysis using these methods reproduced the strong positive correlations between the brain and serum levels, and significant higher concentrations in the serum than in the brain for all the unconjugated BAs. The BA with the higher log<em>P</em><sub>ow</sub> (hydrophobicity) had the higher brain-to-serum concentration ratio (mono- &gt; di- &gt; trihydroxy BAs). Furthermore, the hydrophobicity was considered as the stronger factor for the blood-to-brain influx of the BAs than the serum protein binding ratio. Thus, this study provided further evidence supporting that passive diffusion is the major mechanism for the blood-to-brain influx of the unconjugated BAs.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"204 ","pages":"Article 109397"},"PeriodicalIF":2.7,"publicationDate":"2024-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0039128X24000357/pdfft?md5=2377868a15c25a77dc9e8b7c78ac832e&pid=1-s2.0-S0039128X24000357-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140176563","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Prednisone and ibuprofen conjugate Janus dendrimers and their anticancer activity 泼尼松和布洛芬共轭 Janus 树枝状聚合物及其抗癌活性
IF 2.7 4区 医学
Steroids Pub Date : 2024-03-09 DOI: 10.1016/j.steroids.2024.109395
Israel Barajas-Mendoza , Irving Osiel Castillo-Rodríguez , Isabel Hernández-Rioja , Teresa Ramirez-Apan , Marcos Martínez-García
{"title":"Prednisone and ibuprofen conjugate Janus dendrimers and their anticancer activity","authors":"Israel Barajas-Mendoza ,&nbsp;Irving Osiel Castillo-Rodríguez ,&nbsp;Isabel Hernández-Rioja ,&nbsp;Teresa Ramirez-Apan ,&nbsp;Marcos Martínez-García","doi":"10.1016/j.steroids.2024.109395","DOIUrl":"10.1016/j.steroids.2024.109395","url":null,"abstract":"<div><p>Drug release from hyperbranched Janus dendrimer-drug conjugates and their subsequent activity are influenced by the different drugs in each dendron and the linker. To understand these effects, we synthetized new Janus-type dendrimers of first and second generation. One dendron with 2,2-Bis(hydroxymethyl)propionic acid functionalized with ibuprofen and the second dendron was obtained with 3-aminopropanol-amidoamine and prednisone. The dendrimers were obtained by copper(I)-catalyzed Click azide-alkyne cycloaddition for the formation of a triazole as a dendrimeric nucleus of Janus dendrimer conjugates are reported.</p><p>The influence of ibuprofen, prednisone, and spacer on cancer activity of Janus dendrimers conjugates is reported. The IC<sub>50</sub> values of the anticancer activity on cancer cell lines the Janus dendrimer of second generation was higher in comparison to the first generation dendrimer. Similarly, the anticancer activity was higher compared to the dendron conjugates. Also, no cytotoxic effects of dendrons and dendrimers on non-cancerous kidney COS-7 cell line was observed. The interesting anticancer activity of the prepared prednisone-ibuprofen Janus dendrimer conjugates suggest that the dendrimers could be of potential use as new anticancer drug.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"205 ","pages":"Article 109395"},"PeriodicalIF":2.7,"publicationDate":"2024-03-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140077029","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
Potential targets of diosgenin for the treatment of oral squamous cell carcinoma and their bioinformatics and transcriptional profiling analyses 地奥司明治疗口腔鳞状细胞癌的潜在靶点及其生物信息学和转录谱分析
IF 2.7 4区 医学
Steroids Pub Date : 2024-03-06 DOI: 10.1016/j.steroids.2024.109393
Yang Xiao , Bingbing Xu , Xiaolan Li , Tianhao Ding , Wenxin Zhao , Xiaoxue Nie , Junxia Mu , Zhiyou Xiao , Qian Wang , Qunli Ren , Enkui Zhang
{"title":"Potential targets of diosgenin for the treatment of oral squamous cell carcinoma and their bioinformatics and transcriptional profiling analyses","authors":"Yang Xiao ,&nbsp;Bingbing Xu ,&nbsp;Xiaolan Li ,&nbsp;Tianhao Ding ,&nbsp;Wenxin Zhao ,&nbsp;Xiaoxue Nie ,&nbsp;Junxia Mu ,&nbsp;Zhiyou Xiao ,&nbsp;Qian Wang ,&nbsp;Qunli Ren ,&nbsp;Enkui Zhang","doi":"10.1016/j.steroids.2024.109393","DOIUrl":"https://doi.org/10.1016/j.steroids.2024.109393","url":null,"abstract":"<div><p>Diosgenin can inhibit the proliferation and cause apoptosis of various tumor cells, and its inhibitory effect on oral squamous cell carcinoma (OSCC) and its mechanism are still unclear. In this study, we predicted the targets of diosgenin for the treatment of OSCC through the database, then performed bioinformatics analysis of the targets, and further verified the effect of diosgenin on the activity of OSCC cell line HSC-3, the transcriptional profile of the targets and the molecular docking of the targets with diosgenin. The results revealed that there were 146 potential targets of diosgenin for OSCC treatment, which involved signaling pathways such as Ras, TNF, PI3K-AKT, HIF, NF-κB, and could regulate cellular activity through apoptosis, autophagy, proliferation and differentiation, inflammatory response, DNA repair, etc. Diosgenin significantly inhibited HSC-3 cell activity. The genes such as <em>AKT1</em>, <em>MET1</em>, <em>SRC1</em>, <em>APP1</em>, <em>CCND1</em>, <em>MYC</em>, <em>PTGS2</em>, <em>AR</em>, <em>NFKB1</em>, <em>BIRC2</em>, <em>MDM2</em>, <em>BCL2L1</em>, <em>MMP2</em>, may be important targets of its action, not only their expression was regulated by diosgenin but also their proteins had a high binding energy with diosgenin. These results suggest that diosgenin may have a therapeutic effect on OSCC through AKT1, MMP2 and other targets and multiple signaling pathways, which is of potential clinical value.</p></div>","PeriodicalId":21997,"journal":{"name":"Steroids","volume":"205 ","pages":"Article 109393"},"PeriodicalIF":2.7,"publicationDate":"2024-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140063286","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
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