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Shan Huang, Yu Liang, Jianguo Cui, Jiangning Xie, Yi Liu, Baoqing Hu, Qi Xiao
Steroidal derivatives have attracted tremendous attentions in biological and biomedical areas, due to their variety biological activities. The investigation of structural influences helps in understanding their biological activities. The interactions of steroidal derivatives with DNA may play important roles in biological activities, however only a few investigations were reported on this issue. Herein, the structural influences of three steroidal derivatives were investigated based on their binding interactions with d(GGGT)4 G-quadruplex aptamer by spectroscopic approaches, nuclear magnetic resonance (NMR), electrochemical methods, and molecular modeling techniques...
February 16, 2018: Steroids
Vasiliki Pelekanou, Eleftheria Anastasiou, Efstathia Bakogeorgou, George Notas, Marilena Kampa, Rolando Garcia-Milian, Katerina Lavredaki, Eleni Moustou, Georgia Chinari, Petroula Arapantoni, Anthony O'Grady, Vassilios Georgoulias, Andreas Tsapis, Efstathios N Stathopoulos, Elias Castanas
The expression profile of estrogen receptors (ER) in Non-Small Cell Lung Carcinoma (NSCLC) remains contradictory. Here we investigated protein and transcriptome expression of ERα wild type and variants. Tissue Micro-Arrays of 200 cases of NSCLC (paired tumor/non-tumor) were assayed by immunohistochemistry using a panel of ERα antibodies targeting different epitopes (HC20, 6F11, 1D5, ERα36 and ERα17p). ERβ epitopes were also examined for comparison. In parallel we conducted a probe-set mapping (Affymetrix HGU133 plus 2 chip) meta-analysis of 12 NSCLC tumor public transcriptomic studies (1418 cases) and 39 NSCLC cell lines...
February 15, 2018: Steroids
Xuemei Li, Xi Chen, Yu Wang, Peiyuan Yao, Rui Zhang, Jinhui Feng, Qiaqing Wu, Dunming Zhu, Yanhe Ma
Mycobacterium neoaurum NRRL B-3805 metabolizes sterols to produce androst-4-en-3,17-dione (AD) as the main product, and androsta-1,4-dien-3,17-dione, 9α-hydroxyandrost-4-en-3,17-dione and 22-hydroxy-23,24-bisnorchol-4-en-3-one have been identified as by-products. In this study, a new by-product was isolated from the metabolites of sterols and identified as methyl 3-oxo-23,24-bisnorchol-4-en-22-oate (BNC methyl ester), which was proposed to be produced via the esterification of BNC catalyzed by an O-methyltransferase using S-adenosyl-l-methionine as the methyl group donor...
February 7, 2018: Steroids
Qiqi Zhu, Fei Ge, Yaoyao Dong, Wei Sun, Zhe Wang, Yuanyuan Shan, Ruijie Chen, Jianliang Sun, Ren-Shan Ge
Many flavonoids and isoflavonoids have anti-diabetic effects in animal models. However, the mechanisms that are involved are generally unclear. Since 11β-hydroxysteroid dehydrogenases (HSD11Bs) play important roles in diabetes, we hypothesize that flavonoids and isoflavonoids may affect diabetes by targeting two isoforms of HSD11B differently. The inhibitory effects of flavonoids (apigenin and quercetin) and isoflavonoids [genistein and (±) equol] on rat and human HSD11B1 and HSD11B2 were analyzed. The potencies of inhibition on human HSD11B1 reductase was in the order of apigenin > quercetin > genistein > (±) equol, with IC50 values of 2...
February 6, 2018: Steroids
Hemerson S da Rosa, Mariana Koetz, Marí Castro Santos, Elisa Helena Farias Jandrey, Vanderlei Folmer, Amélia Teresinha Henriques, Andreas Sebastian Loureiro Mendez
Sida tuberculata (ST) is a Malvaceae species widely distributed in Southern Brazil. In traditional medicine, ST has been employed as hypoglycemic, hypocholesterolemic, anti-inflammatory and antimicrobial. Additionally, this species is chemically characterized by flavonoids, alkaloids and phytoecdysteroids mainly. The present work aimed to optimize the extractive technique and to validate an UHPLC method for the determination of 20-hydroxyecdsone (20HE) in the ST leaves. Box-Behnken Design (BBD) was used in method optimization...
February 3, 2018: Steroids
Fumihiko Igarashi, Mari H Ogihara, Masatoshi Iga, Hiroshi Kataoka
Dietary sterols including cholesterol and phytosterols are essential substrates for insect steroid hormone (ecdysteroid) synthesis in the prothoracic glands (PGs). In a silkworm Bombyx mori, one of the model species of insects, the steroidogenesis has been well demonstrated that cholesterol biotransformation into ecdysone in the PG cells. Because insects lack the ability to synthesize cellular sterol de novo, lipoprotein, lipophorin (Lp), has been thought to be the major cholesterol supply source; however, details of cholesterol behavior from Lp to the PG cells has not been analyzed till date...
January 31, 2018: Steroids
Kateřina Šimůnková, Michaela Dušková, Lucie Kolatorova, Mikuláš Kosák, Martin Hill, Hana Jandíková, Hana Pospíšilová, Monika Šrámková, Drahomíra Springer, Luboslav Stárka
Testing of the adrenal function with ACTH 1-24 (Synacthen test) or insulin (insulin tolerance test-ITT) is commonly used. The question of ongoing debate is the dose of Synacthen. Moreover, it may be important from the physiological point of view besides measurement of cortisol levels and 17α-hydroxy-progesterone to know also the response of other steroids to these test. The plasma levels of 24 free steroids and their polar conjugates were followed after stimulation of 1 μg, 10 μg and 250 μg of ACTH 1-24 and after insulin administration in thirteen healthy subjects...
January 30, 2018: Steroids
Gwyndolin Vail, Troy A Roepke
The last few decades have revealed increasing complexity and depth to our knowledge of receptor-mediated estrogen signaling. Nuclear estrogen receptors (ERs) ERα and ERβ remain the fundamental dogma, but developing research targeting membrane-bound ERs urges for a more expanded view on ER signaling. ERα and ERβ are also involved in membrane-delineated signaling alongside membrane-specific G protein-coupled estrogen receptor 1 (GPER1), ER-X, and the Gq-coupled membrane ER (Gq-mER). Membrane ERs are responsible for eliciting rapid responses to estrogen signaling, and their importance has been increasingly indicated in central nervous system (CNS) regulation of such functions as reproduction, energy homeostasis, and stress...
January 26, 2018: Steroids
Maha Sellami, Wissem Dhahbi, Lawrence D Hayes, Goran Kuvacic, Mirjana Milic, Johnny Padulo
The current study examine the effects of combined sprint and resistance training on serum total testosterone (TT), sex-hormone-binding globulin (SHBG) and cortisol (C), at rest, and in response to the Wingate Anaerobic-Test (WAnT) in 21 and 41years old men. Forty moderately-trained men were randomly assigned to a young trained (YT), young control (YC), middle-aged trained (MAT), and middle-aged control (MAC) group. Before (P1), and after (P2) training, blood samples were collected at rest and after exercise...
January 25, 2018: Steroids
Moacir Marocolo, Julio A Silva-Neto, Octávio Barbosa Neto
Anabolic androgenic steroids are a class of synthetic compounds derived from testosterone, eventually used by athletes, to improve physical performance. However, anabolic steroids can also modify normal cardiovascular function. Thus, we investigated cardiac electrophysiological and autonomic abnormalities in rats, through a electrocardiographic variability protocol during and after interruption of administration of nandrolone decanoate (DECA)anabolic steroid. Twenty male Wistar rats (60-70 days old) received DECA (10 mg...
January 20, 2018: Steroids
Margarida Lorigo, Melissa Mariana, Elisa Cairrao
The Ultraviolet (UV) radiation is emitted by the sun and is part of the electromagnetic spectrum. There are three types of UV rays (UV-A, UV-B and UV-C), however only UV-A and UV-B have biologic effects in humans, with UV-B radiation being primarily responsible for these effects. Among the measures of photoprotection advised by the health authorities, the topical application of sunscreens (containing UV-B filters) is the preferred worldwide. Currently, octylmethoxycinnamate (OMC) is the most commonly used UV-B filter in sunscreens...
January 19, 2018: Steroids
Alejandra Chávez-Riveros, Abigail Cruz Noriega, María Teresa Ramírez Apan, Luis D Miranda, Eugene Bratoeff
Four series of pregnenolone derivatives having one or two α,β-unsaturated carbonyls and an ester moiety at C-3 or C-21 were synthetized to compare their cytotoxicity effect. The final compounds were evaluated on three human cancer cell lines: PC-3 (prostate cancer), MCF-7 (breast cancer), SKLU-1 (lung cancer) and a noncancerous cell line HGF (human gingival fibroblast). Two steroids with a 4-fluorinated benzoic acid ester at C-21 were the most active against lung cancer cell line with IC50 of 13.1±1.2 and 12...
January 19, 2018: Steroids
Nighat Sultana
Steroids are perhaps one of the most widely used group of drugs in present day. Beside the established utilization as immunosuppressive, anti-inflammatory, anti-rheumatic, progestational, diuretic, sedative, anabolic and contraceptive agents, recent applications of steroid compounds include the treatment of some forms of cancer, osteoporosis, HIV infections and treatment of declared AIDS. Steroids isolated are often available in minute amounts. So biotransformation of natural products provides a powerful means in solving supply problems in clinical trials and marketing of the drug for obtaining natural products in bulk amounts...
January 19, 2018: Steroids
Qin Xiao, Cui-Fang Wang, Jun Chen, Chen-Lei Lian, Ying Xu, Lei Xiao, Jie-Qing Liu
Chemical investigation on ethyl acetate extract of the calyces of Nicandra physaloides resulted in the isolation of three new withanolides named as nicphysatone A (1), nicphysatone B (2), nicphysatone C (3), together with five known withanolides, nic 17 (4), nic 7 (5), nic 2 (6), withahisolide G (7) and nicaphysalin B (8). The structures were determined by comprehensive spectroscopic experiments. The discovery enriched the diversity of natural withanolides and could serve as scaffolds for the synthesis of more potent modified withanolides...
January 17, 2018: Steroids
Talita Elisa Berté, Ana Paula Dalmagro, Priscila Laiz Zimath, Ana Elisa Gonçalves, Christiane Meyre-Silva, Cristiani Bürger, Carla J Weber, Diogo Adolfo Dos Santos, Valdir Cechinel-Filho, Márcia M de Souza
Alzheimer's disease (AD) is a neurodegenerative disorder associated with cognitive impairment and cholinergic neuronal death, characteristic of the effect of time on biochemical neuronal function. The use of medicinal plants as an alternative form of prevention, or even as a possible treatment of AD, is therefore interesting areas of research, since the standard drugs have many side effects. Taraxerol (TRX) is a triterpene that has been isolated from several plant species, and its various pharmacological properties have already been identified, such the acetylcholinesterase (AChE) inhibition activity in vitro...
January 17, 2018: Steroids
Wenbao Wang, Yingying Zhang, Guodong Yao, Wei Wang, Xinyue Shang, Yan Zhang, Xiaobo Wang, Shaojie Wang, Shaojiang Song
Sarsasapogenin, a kind of mainly effective component of Anemarrhena asphodeloides Bunge, possesses good antitumor properties. Two series of new sarsasapogenin derivatives were synthesized and evaluated for their cytotoxicities against three human cancer cell lines (HepG2, A549, MCF-7) using the MTT assay. The structure-activity relationship revealed that the N, N-dimethylamino, pyrrolidinyl, and imidazolyl substituted at the C26 position could increase the antitumor efficacy of the 3-oxo sarsasapogenin series of compounds...
January 11, 2018: Steroids
Vinicius Guzzoni, Tatiana Sousa Cunha, Vander José das Neves, Larissa Briet, Rafaela Costa, Maria José Costa Sampaio Moura, Vanessa Oliveira, Maria do Carmo Pinho Franco, Pedro Duarte Novaes, Fernanda Klein Marcondes
Anabolic Androgenic Steroids (AASs) misuse has increased among adolescents and recreational athletes due to their potential effects on muscle hypertrophy. On the other hand, AAS might induce alterations on cardiovascular system, although some controversies regarding AAS on vascular properties remain unknown. To address this question, we aimed to investigate the effects of high doses of nandrolone combined with strenuous resistance training (RT) on function and structure of thoracic aorta. Rats were randomized into four groups: non-trained vehicle (NTV), trained vehicle (TV), non-trained nandrolone (NTN), and trained nandrolone (TN), and submitted to 6 weeks of treatment with nandrolone (5mg/kg, twice a week) and/or resistance training...
January 6, 2018: Steroids
Cristel V Camacho, Ramesh Choudhari, Shrikanth S Gadad
Long noncoding RNAs (lncRNAs) are implicated in several biological processes, including but not limited to cardiovascular physiology, reproduction, differentiation, metabolism, DNA repair, and inflammation. Under normal physiological conditions, expression of lncRNAs is tissue-specific and tightly regulated. In contrast, prevalent cancer types exhibit aberrant expression of lncRNAs. In this context, lncRNAs can drive cancer cell characteristics by controlling gene expression programs related to tumor suppressive and oncogenic functions...
January 6, 2018: Steroids
Cecilia J Proietti, Mauro E Cenciarini, Patricia V Elizalde
Progesterone receptor (PR) is a master regulator in female reproductive tissues that controls developmental processes and proliferation and differentiation during the reproductive cycle and pregnancy. PR also plays a role in progression of endocrine-dependent breast cancer. As a member of the nuclear receptor family of ligand-dependent transcription factors, the main action of PR is to regulate networks of target gene expression in response to binding its cognate steroid hormone, progesterone. Liganded-PR transcriptional activation has been thoroughly studied and associated mechanisms have been described while progesterone-mediated repression has remained less explored...
January 6, 2018: Steroids
Snehal S Ashtekar, Neela M Bhatia, Manish S Bhatia
The steroid, estrogen has been recognized as being important for stimulating the growth of breast cancers primarily mediated via the steroidal estrogen receptor-α (ER-α). Inhibition of estrogen activity by small molecules with increased target specificity has proven to be an effective treatment for breast cancer. After the success stories of SERMs and fulvestrant, there is a need for the development of new small molecule modulating ER-α is due to developing resistance and side effects to current breast cancer therapy...
January 4, 2018: Steroids
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