journal
https://read.qxmd.com/read/38101718/design-synthesis-and-biological-evaluation-of-betulinic-acid-derivatives-as-potential-inhibitors-of-3cl-protease-of-sars-cov-2
#21
JOURNAL ARTICLE
Yaowen Liu, Tianqing Nie, Jinjun Hou, Huali Long, Zijia Zhang, Min Lei, Yechun Xu, Wanying Wu
During the coronavirus reproduction process, 3-chymotrypsin-like protease (3CLpro) and papain-like protease (PLpro) are accountable for the fragmentation of two polyprotein precursors (pp1a/pp1ab) into substructural proteins. These two proteins are vital for the replication and transcription of the viral genome. Therefore, 3CLpro is a key protein and target for the design of coronavirus inhibitors. In previous studies, we found that betulinic acid has an inhibitory effect on 3CLpro, with 51.5 % inhibition of 3CLpro at 20 µM...
December 13, 2023: Steroids
https://read.qxmd.com/read/38072091/rfamide-related-peptide-3-rfrp-3-receptor-gene-is-expressed-in-mouse-ovarian-granulosa-cells-potential-role-of-rfrp-3-in-steroidogenesis-and-apoptosis
#22
JOURNAL ARTICLE
Xingru Guo, Tianshu Dai, Shihao Wei, Ziming Ma, Hongxi Zhao, Xingang Dan
RFRP-3 is a functional ortholog of avian GnIH and regulates reproductive activities in the gonads of animals. However, the role of RFRP-3 in the function of ovarian granulosa cells in mice remains unclear. First, we detected the expression of the RFRP-3 receptor (GPR147) in the ovarian granulosa cells of mice. Second, the effect of RFRP-3 treatment on estradiol and progesterone secretions from granulosa cells was tested by ELISA. Meanwhile, the expression of genes and proteins regulating steroid hormone synthesis was respectively examined by qPCR and western blot...
December 8, 2023: Steroids
https://read.qxmd.com/read/38049079/molecular-mechanisms-of-dexamethasone-actions-in-covid-19-ion-channels-and-airway-surface-liquid-dynamics
#23
JOURNAL ARTICLE
Brian J Harvey
The COVID-19 pandemic has been a global health crisis of unprecedented magnitude. In the battle against the SARS-CoV-2 coronavirus, dexamethasone, a widely used corticosteroid with potent anti-inflammatory properties, has emerged as a promising therapy in the fight against severe COVID-19. Dexamethasone is a synthetic glucocorticoid that exerts its therapeutic effects by suppressing the immune system and reducing inflammation. In the context of COVID-19, the severe form of the disease is often characterized by a hyperactive immune response, known as a cytokine storm...
December 2, 2023: Steroids
https://read.qxmd.com/read/37984606/biotransformation-of-metenolone-acetate-and-epiandrosterone-by-fungi-and-evaluation-of-resulting-metabolites-for-aromatase-inhibition
#24
JOURNAL ARTICLE
Aerab Abdul Karim, Atia-Tul Wahab, Ambreen Aziz, Nimra Naveed Shaikh, M Iqbal Choudhary
The present study describes the microbial transformation of anabolic drugs, metenolone acetate (1), and epiandrosterone (6). Three new metabolites, 6β,17β-dihydroxy-1-methyl-3-oxo-5α-androst-1-en (2), 5α,15α-dihydroxy-1-methyl-3-oxo-1-en-17-yl acetate (3), 15β-hydroxy-1-methyl-3-oxo-5α-androst-1,4-dien-17-yl acetate (4), and a known metabolite, 17β-hydroxy-1-methyl-4-androstadiene-3-one (5) were obtained by biotransformation of metenolone acetate (1) via Trametes hirsuta mushroom...
November 18, 2023: Steroids
https://read.qxmd.com/read/37979822/sex-steroid-hormones-the-estrous-cycle-and-rapid-modulation-of-glutamatergic-synapse-properties-in-the-striatal-brain-regions-with-a-focus-on-17%C3%AE-estradiol-and-the-nucleus-accumbens
#25
JOURNAL ARTICLE
Stephanie B Proaño, Christiana K Miller, Amanda A Krentzel, David M Dorris, John Meitzen
The striatal brain regions encompassing the nucleus accumbens core (NAcc), shell (NAcs) and caudate-putamen (CPu) regulate cognitive functions including motivated behaviors, habit, learning, and sensorimotor action, among others. Sex steroid hormone sensitivity and sex differences have been documented in all of these functions in both normative and pathological contexts, including anxiety, depression and addiction. The neurotransmitter glutamate has been implicated in regulating these behaviors as well as striatal physiology, and there are likewise documented sex differences in glutamate action upon the striatal output neurons, the medium spiny neurons (MSNs)...
November 16, 2023: Steroids
https://read.qxmd.com/read/37977489/uphill-running-preferred-over-downhill-running-for-recovery-from-glucocorticoid-induced-muscle-atrophy
#26
JOURNAL ARTICLE
Masanobu Murao, Tetsuo Imano, Yoshinobu Sato, Masaaki Nakajima
No abstract text is available yet for this article.
November 15, 2023: Steroids
https://read.qxmd.com/read/37951289/estrogen-sulfotransferase-and-sulfatase-in-steroid-homeostasis-metabolic-disease-and-cancer
#27
JOURNAL ARTICLE
Jingyuan Wang, Ye Feng, Brian Liu, Wen Xie
Sulfation and desulfation of steroids are opposing processes that regulate the activation, metabolism, excretion, and storage of steroids, which account for steroid homeostasis. Steroid sulfation and desulfation are catalyzed by cytosolic sulfotransferase and steroid sulfatase, respectively. By modifying and regulating steroids, cytosolic sulfotransferase (SULT) and steroid sulfatase (STS) are also involved in the pathophysiology of steroid-related diseases, such as hormonal dysregulation, metabolic disease, and cancer...
November 9, 2023: Steroids
https://read.qxmd.com/read/37949336/evaluation-of-structural-and-thermodynamic-insight-of-er%C3%AE-with-dpn-and-derivatives-through-mmgbsa-mmpbsa-methods
#28
JOURNAL ARTICLE
Martiniano Bello
Estrogen receptors (ERs) are nuclear factors that exist as two subtypes: ERα and ERβ. Among the different selective ERβ agonist ligands, the widely used ERβ-selective agonist DPN (diarylpropionitrile) is highlighted. Recent experimental and thermodynamic information between R-DPN and S-DPN enantiomers with ERβ is important for evaluating further the ability of MD simulations combined with end-point methods to reproduce experimental binding affinity and generate structural insight not provided through crystallographic data...
November 8, 2023: Steroids
https://read.qxmd.com/read/37944652/glucocorticoid-signaling-and-the-impact-of-high-fat-diet-on-adipogenesis-in-vivo
#29
JOURNAL ARTICLE
Noah K Babel, Brian J Feldman
Our research used glucocorticoids as a medically relevant molecular probe to identify a previously unrecognized ADAMTS1-PTN-Wnt pathway. We elucidated the role of this pathway in regulating adipose precursor cell (APC) behavior to either proliferate or differentiate in response to systemic cues, such as elevated caloric intake. Further, our studies identified the non-muscle myosin protein MYH9 as a key target of this pathway to modulate adipogenesis in vivo. These findings enable strategies toward developing novel therapeutics for obesity and related metabolic disorders...
November 7, 2023: Steroids
https://read.qxmd.com/read/37939981/selective-transformations-of-friedelanes-isolated-from-cork-smoker-wash-solids
#30
JOURNAL ARTICLE
Mohadese Yaghoobi Anzabi, Piotr Cmoch, Roman Luboradzki, Zbigniew Pakulski
Friedelin (1) and 3-acetoxyfriedel-3-en-2-one (4), commonly known as friedelane triterpenoids, have been isolated from cork smoker wash solids (also known as black wax) on a multi-gram scale. These compounds are valuable starting materials for the synthesis of new friedelane derivatives. Stereoselective reduction of friedelin by treatment with LiAlH4 , sodium, or catalytic hydrogenation results in the formation of both isomers of friedelinol (5 and 7) in excellent yields. Similarly, the reduction of 3-acetoxyfriedel-3-en-2-one gave epi-cerin (14) and a series of isomeric 2,3-diols or α-hydroxyketones...
November 6, 2023: Steroids
https://read.qxmd.com/read/37939980/synthesis-of-methotrexate-betulonic-acid-hybrids-and-evaluation-of-their-effect-on-artificial-and-caco-2-cell-membranes
#31
JOURNAL ARTICLE
Olexander M Semenenko, Victoria V Lipson, Alina O Sadchenko, Olga V Vashchenko, Natalia A Kasian, Liliia V Sviechnikova, Longin M Lisetski, Mykola L Babak, Volodimir M Vakula, Olexander V Borisov, Yuliia V Holota, Sergiy O Zozulya, Petro O Borisko, Olexander V Mazepa
An efficient protocol for the synthesis of novel methotrexate-betulonic acid hybrids with a (tert-butoxycarbonylamino)-3,6-dioxa-8-octanamine (Boc-DOOA) linkage has been developed. Reaction of N-(2-(2-(2-aminoethoxy)ethoxy)ethyl)-betulonamide with methotrexate resulted in a mixture of isomeric conjugates which were separated by column chromatography. Their structures and composition have been fully established by 1 H NMR, 13 C spectra, FAB mass spectrometry and elemental analysis. The identity of conjugates was confirmed by LC-MS data...
November 6, 2023: Steroids
https://read.qxmd.com/read/37926183/influence-of-ethanol-consumption-and-food-intake-on-serum-concentrations-of-endogenous-steroids
#32
JOURNAL ARTICLE
Detlef Thieme, Aniko Krumbholz, Martin Bidlingmaier, Christoph Geffert, Annika Hameder, Andreas Stöver, Matthias Graw, Annekathrin M Keiler
Steroid biosynthesis and biotransformation are based on a cascade of enzymatic processes being highly sensitive to various external influences. Amongst those, ethanol was shown to affect testosterone metabolism. For doping analyses, athlete steroid profiles comprise seven urinary steroid metabolites, of which relevant ratios are significantly increased following ethanol consumption. This effect is presumably based on the lack of hepatic NAD+ -coenzyme as a consequence of ethanol oxidation. Only recently, testosterone (T) and androstenedione (A4) blood profiles have been introduced as additional approach for doping control...
November 3, 2023: Steroids
https://read.qxmd.com/read/37923152/navigating-nonalcoholic-fatty-liver-disease-nafld-exploring-the-roles-of-estrogens-pharmacological-and-medical-interventions-and-life-style
#33
JOURNAL ARTICLE
Qianying Zuo, Nicole Hwajin Park, Jenna Kathryn Lee, Ashlie Santaliz-Casiano, Zeynep Madak-Erdogan
The pursuit of studying this subject is driven by the urgency to address the increasing global prevalence of Non-Alcoholic Fatty Liver Disease (NAFLD) and its profound health implications. NAFLD represents a significant public health concern due to its association with metabolic disorders, cardiovascular complications, and the potential progression to more severe conditions like non-alcoholic steatohepatitis (NASH), fibrosis, and cirrhosis. Liver estrogen signaling is important for maintaining liver function, and loss of estrogens increases the likelihood of NAFLD in postmenopausal women...
November 3, 2023: Steroids
https://read.qxmd.com/read/37884178/navigating-a-plethora-of-progesterone-receptors-comments-on-the-safety-risk-of-progesterone-supplementation-in-women-with-a-history-of-breast-cancer-or-at-high-risk-for-developing-breast-cancer
#34
JOURNAL ARTICLE
Caroline H Diep, Laura J Mauro, Carol A Lange
Progesterone and progestin agonists are potent steroid hormones. There are at least three major types of progesterone receptor (PR) families that interact with and respond to progesterone or progestin ligands. These receptors include ligand-activated transcription factor isoforms (PR-A and PR-B) encoded by the PGR gene, often termed classical or nuclear progesterone receptor (nPR), membrane-spanning progesterone receptor membrane component proteins known as PGRMC1/2, and a large family of progestin/adipoQ receptors or PAQRs (also called membrane PRs or mPRs)...
October 24, 2023: Steroids
https://read.qxmd.com/read/37863411/mechanism-of-skeletal-muscle-atrophy-by-muscle-fiber-types-in-male-rats-under-long-term-fasting-stress
#35
JOURNAL ARTICLE
Takahiro Ieko, Jumpei Fujiki, Yasuhiro Hasegawa, Tomohito Iwasaki, Hidetomo Iwano, Naoyuki Maeda
Fasting induces metabolic changes in muscles, which are differentiated by muscle fiber type. In this study, the mechanism of fasting-induced muscle atrophy in rats was examined to determine the differences between muscle fiber types in energy production. Fasting for 96 h did not alter the weight of the soleus (SOL), a fiber type I muscle, but did significantly reduce the weight of gastrocnemius (GM), a fiber type II muscle. GM, SOL and blood pregnenolone and testosterone levels decreased under fasting, which induced energy deprivation, whereas corticosterone (CORT) levels significantly increased...
October 18, 2023: Steroids
https://read.qxmd.com/read/37827441/differential-induction-of-c6-glioma-apoptosis-and-autophagy-by-3%C3%AE-hydroxysteroid-indolamine-conjugates
#36
JOURNAL ARTICLE
Jan Panada, Valeriya Klopava, Tatsiana Kulahava, Siarhei Koran, Yaroslav Faletrov, Nina Frolova, Elena Fomina, Vladimir Shkumatov
In a previous work, we reported the synthesis of four novel indole steroids and their effect on rat C6 glioma proliferation in vitro. The steroid derived from dehydroepiandrosterone and tryptamine (IS-1) was the most active (52 % inhibition at 10 µM), followed by one of the epimers derived from pregnenolone and tryptamine (IS-3, 36 % inhibition at 10 µM). By contrast, the steroid derived from estrone and tryptamine (IS-2) showed negligible activity at 10 µM...
October 10, 2023: Steroids
https://read.qxmd.com/read/37827440/expression-of-functional-mineralocorticoid-receptor-mr-and-g-protein-coupled-estrogen-receptor-gper-in-human-t-lymphocytes
#37
JOURNAL ARTICLE
Maria Piazza, Brasilina Caroccia, Samuela Carraro, Gian Paolo Rossi
Aldosterone plays a key role in controlling blood pressure (BP) values by maintaining salt, water, and body fluid homeostasis. Excess aldosterone production is associated with arterial hypertension, cardiovascular and metabolic diseases, partly because of generation of an inflammatory state followed by fibrotic changes in the organs that are target of hypertension. Aldosterone exerts genomic effects that are known to be mediated by activation of the mineralocorticoid receptor (MR). Other aldosterone effects, including those usually defined as 'rapid' or 'non genomic', involve additional receptors as the G-protein coupled estrogen receptor (GPER)...
October 10, 2023: Steroids
https://read.qxmd.com/read/37820890/steroid-hormone-mediated-regulation-of-sexual-and-aggressive-behaviour-by-non-genomic-signalling
#38
JOURNAL ARTICLE
DeAsia Davis, Janine Dovey, Shoko Sagoshi, Kongkidakorn Thaweepanyaporn, Sonoko Ogawa, Nandini Vasudevan
Sex and aggression are well studied examples of social behaviours that are common to most animals and are mediated by an evolutionary conserved group of interconnected nuclei in the brain called the social behaviour network. Though glucocorticoids and in particular estrogen regulate these social behaviours, their effects in the brain are generally thought to be mediated by genomic signalling, a slow transcriptional regulation mediated by nuclear hormone receptors. In the last decade or so, there has been renewed interest in understanding the physiological significance of rapid, non-genomic signalling mediated by steroids...
October 9, 2023: Steroids
https://read.qxmd.com/read/37813157/a-novel-and-easy-protocol-to-obtain-6-alkoxy-%C3%AE-4-6-diene-3-one-derivatives-from-available-sterols
#39
JOURNAL ARTICLE
Roxana Martínez-Pascual, Lidia Gabriela Felipe-Zaragoza, Miguel Ángel Peña-Rico, Alain Cruz-Nolasco, Lemuel Pérez-Picaso, Samuel Núñez-López, Adolfo López-Torres, Omar Viñas-Bravo
Herein we report an unprecedented and efficient methodology for accessing 6-alkoxy-Δ4,6 -diene-3-one derivatives. Such scaffolds were serendipitously obtained in the course of the study of the reaction of Δ4 -3-keto steroids with catalytic amounts of iodine in refluxing methanol. A series of 6-methoxy and 6-ethoxy- Δ4,6 -diene-3-ones were prepared from easily-available sterols in a two-step sequence; first, oxidation of sterols furnished the Δ4 -3-keto steroids, which were then refluxed with ethanol or methanol with I2 as catalyst to obtain a series of ten derivatives...
October 7, 2023: Steroids
https://read.qxmd.com/read/37806604/assessment-of-steroid-enzymes-action-in-children-and-adolescents-with-obesity
#40
JOURNAL ARTICLE
Marta Sumińska, Rafał Podgórski, Piotr Fichna, Artur Mazur, Marta Fichna
Rising prevalence of obesity has become an important impulse to investigate basic mechanisms involved in regulating the energy balance. It is widely accepted that steroids are potent factors affecting glucose, fat, and protein metabolism. Our study was aimed to analyze differences in the total amount of selected enzymes implicated in steroid metabolism in a group of children suffering from obesity and those with normal weight, further subdivided according to sex and pubertal stage. Data were obtained from 187 Caucasian children and adolescents, including 113 patients (63 girls, 50 boys) with obesity and 74 (34 girls, 40 boys) normal weight volunteers...
October 6, 2023: Steroids
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