Steroids
(Steroids) 《Steroids》
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目录导读
Published 2013年1月,Volume 78,Issue 1
最新一期
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Page ii
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Review
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It takes two to tango: Dimerisation of glucocorticoid receptor and its anti-inflammatory functionsReview ArticlePages 59-68 Mark Nixon, Ruth Andrew, Karen E. Chapman
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Regular papers
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Cytotoxic steroidal saponins from Ophiopogon japonicusOriginal Research ArticlePages 1-7 Ning Li, Liang Zhang, Ke-Wu Zeng, Yuan Zhou, Jia-Yu Zhang, Yan-Yun Che, Peng-Fei Tu
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Graphical abstract
Highlights
► Fifteen steroidal saponins (1–15) were isolated from Ophiopogon japonicus. ► Compounds 1–4 were new compounds. ► The cytotoxicity of compounds 2–15 were tested on five human tumor cell lines. ► The structure–activity relationship of these compounds was discussed.
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Estrogen receptor ESR1 regulates the phospholipase C-inositol phosphate signaling in the hippocampus from rats in proestrous and estrous phasesOriginal Research ArticlePages 8-14 Nadia O. Maruyama, Thaís F.G. Lucas, Catarina S. Porto, Fernando M.F. Abdalla
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Highlights
► 17β-Estradiol (E2) induce activation of the phosphoinositide hydrolysis in rat hippocampus. ► Classic ESR1, that underwent nuclear export, are involved in these actions. ► Regulation of ESR1 by estrous cycle does not play a role in the magnitude of the response to E2. ► The rapid actions might be a key step mediating cellular events important for learning and memory.
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DHEA metabolites activate estrogen receptors alpha and betaOriginal Research ArticlePages 15-25 Kristy K. Michael Miller, Numan Al-Rayyan, Margarita M. Ivanova, Kathleen A. Mattingly, Sharon L. Ripp, Carolyn M. Klinge, Russell A. Prough
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Highlights
► DHEA and its metabolites increased ERα and ERβ transcriptional activity. ► Androstenediol binds ERα with an IC50 ∼0.1 μM. ► Androstenedione binds ERβ with an IC50 ∼5 nM. ► DHEA metabolites stimulate MCF-7 cell proliferation. ► Miconazole inhibits ERα-coactivator interaction.
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In situ forming microparticle implants for delivery of sex steroids in fish: Modulation of the immune response of gilthead seabream by testosteroneOriginal Research ArticlePages 26-33 P. Castillo-Briceño, S. Águila-Martínez, S. Liarte, A. García Alcázar, J. Meseguer, V. Mulero, A. García-Ayala
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Highlights
► In situ forming microparticle implants are effective to deliver steroids in fish. ► Testosterone modifies serum sex steroid levels in fish. ► Testosterone promotes a pro- and/or anti-inflammatory response in fish.
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Synthesis of 6-azaprogesterone and 19-hydroxy-6-azasteroidsOriginal Research ArticlePages 34-37 Mario D. Martínez, Valeria C. Edelsztein, Fernando J. Durán, Pablo H. Di Chenna, Gerardo Burton
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Graphical abstract
Highlights
► The 6-azapregnane core may be obtained by a direct route via a Staudinger reaction. ► We synthesized 19-hydroxy-6-azaprogesterone (19 → 3 hemiketal) and 6-azaprogesterone. ► The 6-aza moiety causes the loss of affinity for the progesterone receptor.
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Cytotoxic cholestane-type and ergostane-type steroids from the aerial parts of Euphorbia altotibeticOriginal Research ArticlePages 38-43 Bei-Bei Zhang, Xue-Lian Han, Qian Jiang, Zhi-Xin Liao, Heng-Shan Wang
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Graphical abstract
Highlights
► Three new cholestane and three new ergostane-type steroids were isolated. ► The new steroids exhibited potent cytotoxic activity against HeLa and Hep-6 cell. ► It is the first report of in vitro cytotoxicity of steroids from Euphorbia altotibetic. ► The research deepens the understanding of chemical composition of Euphorbia plant.
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Alternative long-term markers for the detection of methyltestosterone misuseOriginal Research ArticlePages 44-52 C. Gómez, O.J. Pozo, J. Marcos, J. Segura, R. Ventura
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Graphical abstract
Highlights
► Three previously unreported methyltestosterone metabolites are detected in urine. ► These metabolites are excreted as conjugates with sulphate. ► The structure of these metabolites has been postulated based on GC–MS and LC–MS/MS. ► These metabolites are useful for the detection of methyltestosterone misuse. ► One of the metabolites improves the retrospectivity up to 2–3 times.
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Synthesis and antitumor activity of N-sulfonyl-3,7-dioxo-5β-cholan-24-amides, ursodeoxycholic acid derivativesOriginal Research ArticlePages 53-58 Jie Ren, Yongchao Wang, Junliang Wang, Jun Lin, Kun Wei, Rong Huang
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Graphical abstract
Highlights
► Ursodeoxycholic acid derivatives, N-sulfonyl-3,7-dioxo-5β-cholan-24-amides, were designed and synthesized. ► The in vitroantitumor activity was evaluated against four cancer cell lines. ► Three active compounds show high inhibitory activity on three human cancer cell lines.
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Synthesis and investigation of the anticancer effects of estrone-16-oxime ethers in vitroOriginal Research ArticlePages 69-78 Ágnes Berényi, Renáta Minorics, Zoltán Iványi, Imre Ocsovszki, Eszter Ducza, Hubert Thole, Josef Messinger, János Wölfling, Gergő Mótyán, Erzsébet Mernyák, Éva Frank, Gyula Schneider, István Zupkó
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Highlights
► Antiproliferative screen of 63 newly synthetized estrone-16-oxime ethers. ► Disturbance of cell cycle and apoptosis induction. ► Action mediated via proteins p16 and CDK4 governing the phosphorylation of Rb.
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Nine new steroidal glycosides from the roots of Cynanchum stauntoniiOriginal Research ArticlePages 79-90 Jin-Qian Yu, An-Jun Deng, Hai-Lin Qin
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Graphical abstract
Highlights
► More information about the chemical constituents of Cynanchum stauntonii were given. ►·Sixteen compounds were identified, including nine new steroidal glycosides. ►·Two new 14,15-secopregnane-type skeleton aglycones were reported for the first time. ► Several new oligosaccharide chains were found for the first time.
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Salivary testosterone in female-to-male transgender adolescents during treatment with intra-muscular injectable testosterone estersOriginal Research ArticlePages 91-95 Hong N. Bui, Sebastian E.E. Schagen, Daniel T. Klink, Henriette A. Delemarre-van de Waal, Marinus A. Blankenstein, Annemieke C. Heijboer
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Highlights
► An ID-LC–MS/MS method for measuring salivary testosterone (T) was developed. ► The ID-LC–MS/MS method has adequate accuracy and specificity. ► The reference range for salivary T by ID-LC–MS/MS was 135–400 pmol/L. ► Female to male-adolescents are treated with T-esters mixture injections. ► T profile after these injections was investigated by salivary T measurements.
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Dynamics of serum testosterone during the menstrual cycle evaluated by daily measurements with an ID-LC–MS/MS method and a 2nd generation automated immunoassayOriginal Research ArticlePages 96-101 Hong N. Bui, Patrick M. Sluss, Stuart Blincko, Dirk L. Knol, Marinus A. Blankenstein, Annemieke C. Heijboer
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Highlights
► Evaluation of testosterone across the menstrual cycle by an accurate LC–MS/MS assay. ► High intra-individual variation in testosterone levels were found. ► The elevation of mid-cycle testosterone levels is not clinically relevant. ► A single testosterone concentration might not be reflective of the overall status. ► The 2nd generation immunoassay gave comparable results across the menstrual cycle.
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A safe and practical method for the preparation of 7α-thioether and thioester derivatives of spironolactoneOriginal Research ArticlePages 102-107 Géraldine Agusti, Sandrine Bourgeois, Nathalie Cartiser, Hatem Fessi, Marc Le Borgne, Thierry Lomberget
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Graphical abstract
Highlights
► Efficient synthesis of the 7α-methylthioether metabolite of spironolactone. ► Green approach of 7α-thioether and thioester spironolactone derivatives. ► Small library of C19 steroids, having a spirannic γ-lactone at the C-17.
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3β,5α,6β-Oxygenated sterols from the South China Sea gorgonian Muriceopsis flavida and their tumor cell growth inhibitory activity and apoptosis-inducing functionOriginal Research ArticlePages 108-114 Tao-Fang Liu, Xin Lu, Hua Tang, Min-Min Zhang, Pan Wang, Peng Sun, Zhi-Yong Liu, Zeng-Lei Wang, Ling Li, Yao-Cheng Rui, Tie-Jun Li, Wen Zhang
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Graphical abstract
Highlights
► Nineteen 3β,5α,6β-oxygenated sterols were identified from Muriceopsis flavida. ► The structures were reported for the first time from the title gorgonian. ► The steroids exhibited growth inhibition activity against A549 and MG63 cells. ► Compounds 7 and 18 can significantly induce apoptosis in A549 cells. ► A preliminary attempt was made for the structure–activity relationship study.
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