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Jiwang Tang, Jianxiu Wang, Liejiang Yuan, Yong Xiao, Xiu Wang, Zong Yang
Dummy molecularly imprinted polymer microspheres (DMIPMS) towards estrogens were synthesized by Pickering emulsion polymerization employing genistein (GEN) as a dummy template molecule. The FTIR analysis indicated the successful preparation of the imprinted polymers, and the characterization results of scanning electron microscopy and nitrogen adsorption desorption measurement indicated that the obtained DMIPMS are in possess of regular spherical shapes, porous structures and narrow diameter distribution, a BET surface area of 402...
February 15, 2019: Steroids
Nanuli Sh Nadaraia, Lela Sh Amiranashvili, Maia Merlani, Meri L Kakhabrishvili, Nana N Barbakadze, Athina Geronikaki, Anthi Petrou, Vladimir Poroikov, Ana Ciric, Jarmila Glamoclija, Marina Sokovic
Fourteen steroid compounds were in silico evaluated using computer program PASS as antimicrobial agents. The experimental studies evaluation revealed that all compounds have good antibacterial activity with MIC at range of 0.003-0.96 mg/mL and MBC 0.06-1.92 mg/mL. Almost all compounds except of compound 4 (3β-acetoxy-1/ -p-chlorophenyl-3/ -methyl-5α-androstano[17,16-d]pyrazoline) were more potent than Ampicillin, and they were equipotent or more potent than Streptomycine. All compounds exhibited good antifungal activity with MIC at 0...
February 15, 2019: Steroids
Tânia Martins Vieira, Wagner Costa Rossi Junior, Flávia Da Ré Guerra, Bruno Damião, Petrus Pires Marques, Alessandra Esteves
Testosterone cypionate and Stanozolol are Anabolic-Androgenic Steroids (AAS) which are synthetic substances that possess functions similar to testosterone. The use of these substances has increased considerably among youngsters and sports practitioners aiming better performance of with aesthetic purposes. The major concern is the effects caused by the inappropriate use of the substances, such as hypertension, myocardial ischemia, and left ventricle hypertrophy. The objective of the present research was to measure the diameter of the left ventricle lumen and the thickness of the left ventricle myocardium in mice submitted to supraphysiological doses of AAS...
February 14, 2019: Steroids
A V Polikarpova, I S Levina, N V Sigai, I V Zavarzin, I A Morozov, P M Rubtsov, A A Guseva, O V Smirnova, T A Shchelkunova
Progesterone (P4) and its analogues regulate various reproductive processes, such as ovulation, implantation, pregnancy maintenance and delivery. In these processes, an important role is played by the immune cells recruited to the female reproductive organs and tissues, where they are exposed to the action of P4. Progestins regulate cellular processes, acting through nuclear steroid receptors (nSRs), membrane P4 receptors (mPRs), and through the sensors. It remains unclear, what type of receptors is used by P4 and its derivatives to exert their effect on the immune cells and how similar their effects are in different types of these cells...
February 9, 2019: Steroids
Tokutaro Yamaguchi, Joo-Ho Lee, A-Rang Lim, Eun-Ji Yu, Tae-Jin Oh
Recently, studies on the steroidal hormone activity in the brain have attracted attention, and the influences of the varied glucosides and their artificial derivatives have been discussed; additionally, it has been suggested that glucosides are the synthetic precursors of glucuronide as a label molecule. However, glucosides are formed with 11α-hydroxyprogesterone (1), which is important as a blood pressure regulator, but anti-androgen activity remains unknown. Using UDP-glucosyltransferase, glucoside synthesis was successful in linking β-D -glucopyranose and β-D -laminaribiose to 11α oxygen of 1 at a high conversion ratio, and full assignment structure was analyzed for the two glucosides by high-resolution quadrupole-time flight electrospray ionization-mass spectrometry, 1D (1 H and 13 C) NMR and 2D (COSY, ROESY, HSQC-DEPT and HMQC) NMR...
February 9, 2019: Steroids
Shu Liu, Zhiqing Wang, Jianhui Jiang, Haimei OuYang, Sisi Wei, Jinqun Liang, Nuan Chen, Weihong Zeng, Liying Chen, Xunjie Xie
Androgen insensitivity syndrome (AIS), a rare X-linked recessive genetic disorder with a normal 46, XY karyotype, is caused by defect of androgen receptor gene (AR) leading to resistance of the target tissues to androgenic hormones. There is a wide spectrum of clinical presentations of AIS, ranging from male infertility, hypospadias to completely normal female external genitalia. Here, we describe a 15-year old, phenotypically female individual, who visited our clinic for primary amenorrhea. The physical examination revealed normal female external genitalia, normal breast development, as well as sparse pubic hair and absence of axillary hair...
February 8, 2019: Steroids
Zi-Ru Wang, Gang Li, Li-Xia Ji, Hang-Hang Wang, Han Gao, Xiao-Ping Peng, Hong-Xiang Lou
A new ergosterol derivative, 23R-hydroxy-(20Z,24R)-ergosta-4,6,8(14),20(22)-tetraen-3-one (1), and a biosynthetically related known compound, (22E,24R)-ergosta-4,6,8(14),22-tetraen-3-one (2), were isolated from the co-culture between endophytic fungus Pleosporales sp. F46 and endophytic bacterium Bacillus wiedmannii Com1 both inhibiting in the medicinal plant Mahonia fortunei. The structure of the new compound 1 was determined by extensive spectroscopic analysis using HRMS and NMR, together with the modified Mosher's ester method...
February 6, 2019: Steroids
Robert N Hanson, Emmett McCaskill, Edward Hua, Pakamas Tongcharoensirikul, Robert Dilis, Jessa L Silver, Timothy A Coulther, Mary Jo Ondrechen, David Labaree, Richard B Hochberg
A series consisting of substituted benzoylbenzamide derivatives of 17α-E-vinyl estradiol 6a-i and 7a-d was prepared in good overall yields from the corresponding novel iodinated benzoylbenzamide precursors using Pd(0)-catalyzed Stille coupling. Biological evaluation using competitive binding assays indicated that all compounds were effective ligands for the ERα- and ERβ-LBD (RBA = 0.5-10.0% of estradiol). Most of the compounds expressed lower stimulatory (agonist) potency (RSA <0.2-0.5%) compared to their binding affinity, however, the meta-substituted isomer 6h demonstrated a level of efficacy (RSA = 5...
February 6, 2019: Steroids
Nisal Gajadeera, Robert N Hanson
The development of fluorescent ligands for the estrogen receptor (ER) continues to be of interest. Over the past 20 years, most efforts have focused on appending an expanding variety of fluorophores to the B-, C- and D-rings of the steroidal scaffold. This review highlights the synthesis and evaluation of derivatives substituted primarily at the 6-, 7α- and 17α-positions, culminating with our recent work on 11β-substituted estradiols, and proposes an approach to new fluorescent imaging agents that retain high ER affinity...
February 6, 2019: Steroids
Larissa Rugila S Stopa, Camila F de Souza, Geisielle Fernandes Santos, Andressa B Martins, Renan Nascimento Ferreira, Fábio Goulart de Andrade, Cristiane Mota Leite, Dimas A M Zaia, Cassia Thaïs B V Zaia, Ernane Torres Uchoa
Glucocorticoids (GC) increase food intake and body weight in humans and rodents, and chronic stress and GC treatment-induced enhancement on plasma concentration of GC leads to obesity and metabolic changes. In response to hypercaloric treatment, males were shown to be more susceptible to obesity compared to females, demonstrating that intersexual differences may affect energy homeostasis. The objective of the current study was to evaluate the effects of prolonged (28 days) treatment with dexamethasone or corticosterone in intact rats, both male and female, on food intake, body weight gain, Lee index, weights and area of adipocytes of retroperitoneal and perigonadal+perirenal adipose tissues, glucose tolerance test (GTT) and plasma concentrations of free fatty acids, cholesterol and triglycerides...
February 6, 2019: Steroids
Barbara Seroka, Zenon Łotowski, Agnieszka Wojtkielewicz, Przemysław Bazydło, Ewelina Dudź, Agnieszka Hryniewicka, Jacek W Morzycki
Two series of cholestane-based diamines (1,2 and 1,3) were synthesized using simple and efficient procedures. The convenient substrates for these syntheses were cholesteryl mesylate and tosylate, which were converted to appropriate amines via easily obtained azides. The final diamines were prepared using a substitution reaction with bromoacetonitrile (in the case of 1,2-diamines) or condensation with acrylonitrile (in the case of 1,3-diamines), followed by the reduction of intermediate aminonitriles. Furthermore, the other two amines were synthesized from 16-dehydropregnenolone acetate using aza-Michael addition as a key step...
February 6, 2019: Steroids
Andrea Poch, Felipe Villanelo, Soledad Henriquez, Paulina Kohen, Alex Muñoz, Jerome F Strauss, Luigi Devoto
An estradiol metabolite, 2-methoxyestradiol (2ME), has emerged as an important regulator of ovarian physiology. 2ME is recognized as a potent anti-angiogenic agent in clinical trials and laboratory studies. However, little is known about its molecular actions and its endogenous targets. 2ME is produced by human ovarian cells during the normal menstrual cycle, being higher during regression of the corpus luteum, and is postulated to be involved in the anti-angiogenic process that plays out during luteolysis...
February 6, 2019: Steroids
Konstantina Kalyvianaki, Athanasios A Panagiotopoulos, Panagiotis Malamos, Eleni Moustou, Maria Tzardi, Efstathios N Stathopoulos, Georgios S Ioannidis, Kostas Marias, George Notas, Panayiotis A Theodoropoulos, Elias Castanas, Marilena Kampa
Accumulating evidence during the last decades revealed that androgens exert membrane-initiated actions leading to the modulation of significant cellular processes, important for cancer cell growth and metastasis (including prostate and breast), that involve signaling via specific kinases. Collectively, many nonclassical, cell surface-initiated androgen actions are mediated by novel membrane androgen receptors (mARs), unrelated to nuclear androgen receptors. Recently, our group identified the G protein coupled oxo-eicosanoid receptor 1 (OXER1) (a receptor of the arachidonic acid metabolite, 5-oxoeicosatetraenoic acid, 5-oxoETE) as a novel mAR involved in the rapid effects of androgens...
January 29, 2019: Steroids
David E Cantonwine, Thomas F Mcelrath, Britton Trabert, Xia Xu, Joshua Sampson, James M Roberts, Robert N Hoover, Rebecca Troisi
Experimental studies suggest that shallow uterine cytotrophoblastic invasion in preeclampsia may be associated with alterations in estrogen metabolism. The objective of this study was to examine the association of parent estrogens and their metabolites between preeclamptics and normotensive controls at three time points during pregnancy. Methods Parent estrogens and their metabolites were measured in urine by high-performance liquid chromatography-tandem mass spectrometry in 66 singleton preeclampsia cases and 137 matched controls...
January 24, 2019: Steroids
Marwa Abdeltawab Mohammed, Mohamed O Mahmoud, Ashraf Sayed Awaad, Gehad Mohamed Gamal, Dina Abdelfatah
BACKGROUND: Glucocorticoids (GCs)have various uses in the medicine in different specialties. However, GCs administration is usually accompanying with multiple side effects such as hyperglycemia and hyperlipidemia. Alpha lipoic acid (ALA) has been documented to posse anti-diabetic properties. AIM OF THE STUDY: this study highlights the role of ALA in avoiding dexamethasone induced metabolic disturbance. MATERIALS & METHODS: 30 rats were randomly divided into 5 groups: Group (1): Control group; Groups 3,4, and 5: rats received dexamethasone 1mg/kg/day for 10 days; Groups 2, 4, and 5: Rats received ALA 100mg/kg/ day all the duration of the study, 2 weeks before dexamethasone, or concomitant with dexamethasone respectively...
January 23, 2019: Steroids
Rengfei Shi, Xiangyang Tian, Yu Feng, Zepeng Cheng, Jianqiang Lu, Darrell W Brann, Quanguang Zhang
Age-related muscle wasting (sarcopenia) is accompanied by a decrease in estrogen levels which can compromise the health of aging women. Recent studies have shown that the key enzyme of estrogen synthesis (aromatase) is detected in the skeletal muscle. The purpose of this study was to investigate the effects of exercise on the expression of aromatase and the synthesis of sex steroid hormones in skeletal muscle following exercise training. Ovariectomized rats were divided into two groups, treadmill running group (25 m/min, 60 min/day, 6 days/week) and sedentary group...
January 18, 2019: Steroids
Anna V Glyakina, Nicolai I Strizhov, Mikhail V Karpov, Nikita V Dovidchenko, Bakhyt T Matkarimov, Ludmila V Isaeva, Vera S Efimova, Mikhail A Rubtsov, Ludmila A Novikova, Marina V Donova, Oxana V Galzitskaya
Cytochrome P450scc (CYP11A1) is a mammalian mitochondrial enzyme which catalyzes cholesterol side chain cleavage to form pregnenolone. Along with cholesterol, some other steroids including sterols with a branched side chain like β-sitosterol are the substrates for the enzyme, but the activity towards β-sitosterol is rather low. Modification of the catalytic site conformation could provide more effective β-sitosterol bioconversion by the enzyme. This study was aimed to find out the amino acid residues substitution of which could modify the conformation of the active site providing possible higher enzyme activity towards β-sitosterol...
January 11, 2019: Steroids
Jiayu Liu, Ping He, Limin Lin, Yining Zhao, Wentong Deng, Hejiazi Ding, Qing Li, Zhong Wang
Human aldo-keto reductase AKR1C3 (type 2 3α-hydroxysteroid dehydrogenase/type 5 17β-hydroxysteroid dehydrogenase) is involved in testosterone and estrogen metabolism. AKR1C3 expression is relatively low in most tissues and high in prostate and mammary glands in regulating androgen and estrogen levels. However, in many cancers, overexpression of AKR1C3 was observed, thus prompting the development of therapeutics targeting AKR1C3. To facilitate the development of AKR1C3 targeting therapeutics, evaluating the expression of AKR1C3 is vital...
January 10, 2019: Steroids
Neus Fabregat-Cabello, Stéphanie D Peeters, Tugba Yilmaz, Étienne Cavalier, Caroline M Le Goff
BACKGROUND: Androstanediol glucuronide is linked to a range of disorders of peripheral androgen formation and action, such as in hirsutism and acne. Nowadays its accurate quantification is still challenging and there are just a few LC-MS/MS methods available. Besides, their reference intervals for normal European populations by LC-MS/MS, including prepubertal and pubertal children, have not been reported yet. METHODS: Validation of the proposed new methodology was performed at 3 levels in triplicate during 3 different days...
January 6, 2019: Steroids
Abdul Wajid, Malik Shoaib Ahmad, Sammer Yousuf, Atia-Tul-Wahab, Almas Jabeen, Atta-Ur-Rahman, M Iqbal Choudhary
Biotransformation of a synthetic progestonic hormone dydrogesterone (1), C21 H28 O2 , with a plant pathogenic fungus Macrophomina phaseolina yielded two new 2 and 3, and a known 4 metabolites. These analogues were identified as, 3β,11α-dihydroxy-5β,9β,10α-pregna-7-ene-6,20-dione (2), 15β-hydroxy-9β,10α-pregna-4,6-diene-3,20-dione (3), and 8α-hydroxy-9β,10α-pregna-4,6-diene-3,20-dione (4). Major structural changes were observed in metabolite 2. New metabolite 3 showed anti-inflammatory potential, and was found to be the potent inhibitor of intracellular reactive oxygen species (ROS) from whole blood phagocytes (IC50 = 4...
January 6, 2019: Steroids
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