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Discovery of 3-Peptide Substituted Arenobufagin Derivatives as Potent Antitumor Agents with Low Cardiotoxicity.

Baobao Chen, Chuanhao Wang, Jianjiang Ma, Haijun Ma, Yuan Wang, Hui Zhang, Yazhao Zhu, Jianzhong Yao, Chuan Luo, Zhenyuan Miao, Yuelin Wu,

Active natural productscan be valuable lead compounds and numerous drugs derived from natural products have successfully entered the clinic. Arenobufagin, one of the important active components of toad venom, indicates significant antitumor activities with limited preclinical development for its strong cardiotoxicity. Ten 3-monopeptide substituted arenobufagin derivatives have been designed and ... Read more >>

Steroids (Steroids)
[2020, :108772]

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Transformations, NMR Studies and Biological Testing of Some 17β-Isoxazolyl steroids and Their Heterocyclic Ring Cleavage Derivatives.

Alexander Baranovsky, Alesya Ladyko, Tatsiana Shkel, Sergey Sokolov, Natallia Strushkevich, Andrey Gilep,

The synthesis and NMR structure analysis of a group of oxygenated steroids containing isoxazole, dihydrofuran, tetrahydrofuran rings or enamino carbonyl fragment in the side chain have been fulfilled. The prepared compounds were tested toward several enzymes (human cytochrome P450s CYP17, CYP19, CYP51 and CYP51 of pathogenic fungus Candida glabrata) as ... Read more >>

Steroids (Steroids)
[2020, :108768]

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Anti-atherogenic effect of Nepitrin-7-O-glucoside: a flavonoid isolated from Nepeta Hindostana via acting on PPAR - α receptor.

Sushma Devi, Naresh Kumar Rangra, Ravi Rawat, Majed M Alrobaian, Aftab Alam, Randhir Singh, Akanksha Singh,

Atherogenic dyslipidemia is a condition and responsible for the induction of major cardiovascular diseases. Traditionally, Nepeta hindostana a medicinal plant commonly used as cardioprotective in Indo-Pak regions has gained importance because of its therapeutic active flavonoid Nepitrin-7-O-glucoside. Flavonoid-glycosides are steroids having the ability to exert specific, decisive action on the ... Read more >>

Steroids (Steroids)
[2020, :108770]

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Deoxycholic acid as a molecular scaffold for tyrosyl-DNA phosphodiesterase 1 inhibition: a synthesis, structure-activity relationship and molecular modeling study.

Oksana V Salomatina, Irina I Popadyuk, Alexandra L Zakharenko, Olga D Zakharova, Arina A Chepanova, Nadezhda S Dyrkheeva, Nina I Komarova, Jóhannes Reynisson, Rashid O Anarbaev, Nariman F Salakhutdinov, Olga I Lavrik, Konstantin P Volcho,

Para-Bromoanilides of deoxycholic acid with various functional groups on the steroid scaffold were designed as promising tyrosyl-DNA phosphodiesterase 1 (Tdp1) inhibitors. Tdp1 is a DNA repair enzyme, involved in removing DNA damage caused by topoisomerase I poisons; an important class of anticancer drugs. Thus, reducing the activity of Tdp1 can ... Read more >>

Steroids (Steroids)
[2020, :108771]

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Recent advances in the bile acid based conjugates/derivatives towards their gelation applications.

Dipakkumar Bariya, Vivek Anand, Satyendra Mishra,

Bile acids have contributed immensely to hydrogel research due to their peculiar physicochemical properties and biocompatibility. The wide accessibility of bile acids and their straightforward derivatization methods make them attractive building blocks for the design of novel hydrogels systems to deliver biomolecules, drugs, and vaccines. This review conceptualizes recent developments ... Read more >>

Steroids (Steroids)
[2020, 165:108769]

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Cytotoxic ergostane-type steroids from Ganoderma lingzhi.

Jin-Hai Yu, Shu-Juan Yu, Kai-Lu Liu, Chao Wang, Chao Liu, Jin-Yue Sun, Hua Zhang,

Two new ergostane-type steroids (1 and 2) have been isolated from the fruiting body of a medicinal macro fungus Ganoderma lingzhi. The structures including the absolute configurations of them were elucidated by a combination of different spectroscopic analyses especially <sup>13</sup>C NMR and ECD calculations. Compound 2 features an unusual 1,2-dioxolane ... Read more >>

Steroids (Steroids)
[2020, 165:108767]

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Russelioside B; A pregnane glycoside for treatment of gastric ulcer via modulation of heat shock protein-70 and vascular endothelial growth factor.

Riham A El-Shiekh, Abeer Salama, Asmaa K Al-Mokaddem, Ammar Bader, Essam A Abdel-Sattar,

Gastric ulcers are a very common public health problem affecting up to 10% worldwide. Russelioside B is a steroidal glycoside isolated from several Caralluma species. No study tested the ulcer healing potential of the compound. The current study aimed to assess the protective effect of russelioside B against ethanol-induced gastric ... Read more >>

Steroids (Steroids)
[2020, 165:108759]

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Acute kidney injury induced by glycerol is worsened by orchiectomy and attenuated by testosterone replacement.

Samira Itana de Souza, Edilene Cândido Rocha, Halanna Rocha Ferraz, Jéssica Afonso Dias, Antonio Carlos Seguro, Rildo Aparecido Volpini, Daniele Canale, Ana Carolina de Bragança, Maria Heloisa Massola Shimizu, Lucas Miranda Marques, Amélia Cristina Mendes de Magalhães, Terezila Machado Coimbra, Telma de Jesus Soares,

Although several studies have demonstrated that the male gender represents an independent risk factor for renal disease, evidence shows that androgens exert renal protective actions. The findings are controversial and no studies have evaluated the effects of orchiectomy and testosterone replacement on glycerol-induced renal injury. Male Wistar rats were submitted ... Read more >>

Steroids (Steroids)
[2020, 165:108755]

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Enterohepatic circulation of bile acids and their emerging roles on glucolipid metabolism.

Meng-Jun Chen, Chen Liu, Yue Wan, Lei Yang, Shu Jiang, Da-Wei Qian, Jin-Ao Duan,

Bile acids (BAs) are amphiphilic molecules with a nonpolar steroid carbon skeleton and a polar carboxylate side chain. Recently, BAs have aroused the attention of scholars due to their potential roles on metabolic diseases. As important endogenous ligands, BAs are wildly active in the enterohepatic circulation, during which microbiota play ... Read more >>

Steroids (Steroids)
[2020, 165:108757]

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Survey of protein-based sport supplements for illegally added anabolic steroids methyltestosterone and 4-androstenedione by UPLC-MS/MS.

Somaye Alaedini, Maryam Amirahmadi, Farzad Kobarfard, Hossein Rastegar, Sasan Nasirahmadi, Shahram Shoeibi,

There is some evidence that marketable supplements contain hormones not declared on the product label. The presence of these androgenic anabolic steroids (AAS) in sports supplements can be considered an adulteration and affect the health of consumers, who are predominantly athletes. This study aimed to measure anabolic hormones (methyltestosterone and ... Read more >>

Steroids (Steroids)
[2020, 165:108758]

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Phytosteroid 28-homobrassinolide targets cholesterol and glucose homeostasis implicating ABCA1 and SREBP role in regulation.

Victor Mukherjee, Premalatha Ramakrishna, Sushmita Bora, Srikumar Kotteazeth,

Oxysterols are natural ligands of certain nuclear receptors known as liver X receptors (LXR). LXRs are regulators of fatty acid, cholesterol, and glucose homeostasis. Dietary phyto-oxysterol 28-homobrassinolide (28-HB) has been demonstrated to transactivate rat LXR α and β. In this study we assessed the potential of 28-HB to effect such ... Read more >>

Steroids (Steroids)
[2020, 165:108756]

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Effects of Cangfu Daotan Decoction on obese polycystic ovary syndrome and its mechanism.

Weimin Yi, Xue Li, Ke Chen, Min Zhu, Xuehua Cai, Aizhen Pan,

BACKGROUND:Polycystic ovary syndrome (PCOS) is one of the most common endocrine disorders affecting women of reproductive age. Cangfu Daotan Decoction (CFDTT) is one of the prescriptions in the stagnation of obesity-type PCOS. Our previous study showed that CFDTT treatment of obese PCOS was correlated with organic anion transporting polypeptides (OATPs). ... Read more >>

Steroids (Steroids)
[2020, 165:108740]

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High, not low-dose of stanozolol (Anabolic - androgenic steroid) impedes embryo implantation by attenuating endometrial receptivity in the mouse, Mus musculus.

Chaitra R Sharma, Nafisa H Balasinor, Laxmi S Inamdar Doddamani,

The present investigation is aimed at evaluating the efficacy of one of the anabolic -androgenic steroids, stanozolol (ST), on establishment and maintenance of pregnancy in mice. A total of 40 female mice were assigned to three experimental groups. Stanozolol was dosed subcutaneously (low-dose, 0.5 mg/kg bwt; high-dose, 5.0 mg/kg bwt or 1% ... Read more >>

Steroids (Steroids)
[2020, 165:108752]

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Gender roles and behavioral problems in children with 21-hydroxylase deficiency in Southern China.

Lina Zhang, Pinggan Li, Hui Ou, Zulin Liu, Yi Sun, Qingfang Song, Lele Hou, Siqi Huang, Zhe Meng, Liyang Liang,

PURPOSE:To assess the gender roles and behavioral outcomes in children with 21-hydroxylase deficiency (21-OHD) in Southern China. METHODS:A total of 50 individuals with 21-OHD participated in our study, (30 boys and 20 girls), as well as another 19 age-matched non-affected relatives of patients (12 boys and 7 girls). Psychological adjustment ... Read more >>

Steroids (Steroids)
[2020, 165:108754]

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Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review.

Steven B Machek, Thomas D Cardaci, Dylan T Wilburn, Darryn S Willoughby,

Anabolic androgenic steroids (AAS) are testosterone and testosterone-derivative compounds sporadically employed by athletes and increasingly used recreationally to acquire a competitive edge or improve body composition. Nevertheless, users are subject to undesired side effects majorly associated with tissue-specific androgen receptor (AR) binding-mediated actions. More recently, selective AR modulators (SARMs) have ... Read more >>

Steroids (Steroids)
[2020, 164:108753]

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Circulating steroids and mood disorders in patients with polycystic ovary syndrome.

Tomoko Yoshida, Kazuki Saito, Toshihiro Kawamura, Tomonori Ishikawa, Tsuguhiko Kato, Keiko Matsubara, Naoyuki Miyasaka, Mami Miyado, Maki Fukami,

Aberrant androgen metabolism is a characteristic feature of polycystic ovary syndrome (PCOS). Various androgens as well as their precursors and metabolites can accumulate in the blood of PCOS patients. Although these steroids include neuroactive steroids, such as allopregnanolone and androstenedione (Δ4A), it remains unknown whether altered blood steroid levels contribute ... Read more >>

Steroids (Steroids)
[2020, 165:108748]

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A sensitive, precise and rapid LC-MS/MS method for determination of ergosterol peroxide in Paecilomyces cicadae mycelium.

Linfu He, Xiaoyan He, Xiaocui Liu, Wenjing Shi, Xiaofeng Xu, Zhicai Zhang,

Ergosterol peroxide (EP) has considerable potential effect against the proliferation of tumor cells. Here, we established a new approach for EP content detection through liquid chromatography-tandem mass spectrometry. The specificity, limit of detection (LOD)/quantitative (LOQ), linearity and range, accuracy, repeatability, and intermediate precision were tested. The EP retention time was ... Read more >>

Steroids (Steroids)
[2020, 164:108751]

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Stochastic dynamic mass spectrometric quantification of steroids in mixture - Part II.

Bojidarka Ivanova, Michael Spiteller,

This paper deals with quantification of the following steroids in mixture: hydrocortisone (1), deoxycorticosterone (2), progesterone (3) and methyltestosterone (4) by means of mass spectrometry and implementing our innovative stochatic dynamic functional relationship between the analyte concentration in solution and the experimental variable intensity. The mass spectrometric data are correlated ... Read more >>

Steroids (Steroids)
[2020, 164:108750]

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Effects of synthetic glucocorticoids on breast cancer progression.

Jia Meng Pang, Yi-Chen Huang, Shu-Pin Sun, Yan-Ru Pan, Chia-Yi Shen, Ming-Chien Kao, Rong-Hsuan Wang, Lu-Hai Wang, Kai-Ti Lin,

Glucocorticoids (GCs) are widely prescribed as adjuvant therapy for breast cancer patients. Unlike other steroid hormone receptors, the GC receptor is not considered an oncogene. Research in the past few years has revealed the complexity of GC-mediated signaling, but it remains puzzling whether GCs promote or inhibit tumor progression in ... Read more >>

Steroids (Steroids)
[2020, 164:108738]

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Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin.

Yang Zhou, Jinjun Hou, Huali Long, Zijia Zhang, Min Lei, Wanying Wu,

A series of cinobufagin-3-yl nitrogen-containing-carbamate derivatives were designed, synthesized, and evaluated for their proliferation inhibition activities. The structure-activity relationships suggested that the substituents at C-16 was a crucial factor for the potency and that follows this trends: acetic ester ≫ benzoic ester ≈ hydroxy > carbamate. Compounds 3f, 3g, 3h, and 3i exhibited significant in vitro ... Read more >>

Steroids (Steroids)
[2020, 164:108749]

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A spirostanol saponin isolated from Tupistra chinensis Baker simultaneously induces apoptosis and autophagy by regulating the JNK pathway in human gastric cancer cells.

Jingwen Xu, Zhe Wang, Yuying Huang, Yihai Wang, Limin Xiang, Xiangjiu He,

T-17, a bioactive spirostanol saponin extracted from Tupistra chinensis Baker, was previously reported with anti-inflammatory and cytotoxic activities. However, the mechanism underlying of its anti-proliferation activity remains to be elucidated. In this study, we investigated the anti-gastric cancer cell growth activity of T-17 in terms of cell viability, colony formation, ... Read more >>

Steroids (Steroids)
[2020, 164:108737]

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Separation and identification of tubocapsanolide MAP and tubocapsunolide A, and the structure-activity relationship of their anti-TNBC activity.

PanTing Shou, Jiao Li, YingYing Wei, GuoYin Kai, FuQian Wang, HuaJun Zhao, Bo Yang,

A new withanolide, tubocaapsanolide MAP (MeOH addition product) (1), as well as its known precursor tubocaapsanolide A (2) were obtained from Tubocapsicum anomalum (Solanaceae). Compound 1 was a MeOH addition product transformed from compound 2 during the process of separation using MeOH as solvent. The structures of the two withanolides ... Read more >>

Steroids (Steroids)
[2020, 164:108734]

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Dutasteride combined with androgen receptor antagonists inhibit glioblastoma U87 cell metabolism, proliferation, and invasion capacity: Androgen regulation.

M Orozco, R A Valdez, L Ramos, M Cabeza, J Segovia, M C Romano,

Glioblastoma (GB) is the most common and aggressive primary brain tumor in adult humans. Therapeutic resistance and tumor recurrence after surgical resection contributes to a poor prognosis for glioblastoma patients. Men are known to be more likely than women to develop an aggressive form of GB. Although the reasons for ... Read more >>

Steroids (Steroids)
[2020, 164:108733]

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A review on steroid dimers: 2011-2019.

Lutfun Nahar, Satyajit D Sarker,

The first review article on steroid dimers by Li and Dias in 1997, followed by the second review and a book on steroid dimers by Nahar and Sarker in 2007 and 2012, respectively, covered steroid dimers reported until the end of 2010. Since then, there have been considerable amounts of ... Read more >>

Steroids (Steroids)
[2020, 164:108736]

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Medroxyprogesterone derivatives from microbial transformation as anti-proliferative agents and acetylcholineterase inhibitors (combined in vitro and in silico approaches).

Sharifah Nurfazilah Wan Yusop, Syahrul Imran, Mohd Ilham Adenan, Sadia Sultan,

The fungal transformations of medroxyrogesterone (1) were investigated for the first time using Cunninghamella elegans, Trichothecium roseum, and Mucor plumbeus. The metabolites obtained are as following: 6β, 20-dihydroxymedroxyprogesterone (2), 12β-hydroxymedroxyprogesterone (3), 6β, 11β-dihydroxymedroxyprogesterone (4), 16β-hydroxymedroxyprogesterone (5), 11α, 17-dihydroxy-6α-methylpregn-4-ene-3, 20-dione (6), 11-oxo-medroxyprogesterone (7), 6α-methyl-17α-hydroxypregn-1,4-diene-3,20-dione (8), and 6β-hydroxymedroxyprogesterone (9), 15β-hydroxymedroxyprogesterone (10), 6α-methyl-17α, ... Read more >>

Steroids (Steroids)
[2020, 164:108735]

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