Progesterone receptor-mediated actions and the treatment of central nervous system disorders: an up-date of the known and the challenge of the unknown
Publication date: Available online 18 October 2019Source: SteroidsAuthor(s): Susana L. González, María F. Coronel, María C. Raggio, Florencia LabombardaAbstractProgesterone has been shown to exert a wide range of remarkable protective actions in experimental models of central nervous system injury or disease. However, the intimate mechanisms involved in each of these beneficial effects are not fully depicted. In this review, we intend to give the readers a thorough revision on what is known about the participation of diverse receptors and signaling pathways in progesterone-mediated neuroprotective, pro-myelinating and a...
Source: Steroids - October 19, 2019 Category: Drugs & Pharmacology Source Type: research
Anti-androgenic effect of 6-formylindolo[3,2-b]carbazole (FICZ) in LNCaP cells is mediated by the aryl hydrocarbon-androgen receptors cross-talk
In this study, LNCaP cells were exposed to FICZ, CH223191 and flutamide (Flu) alone or in combination in the presence and absence of testosterone. CYP1A1 enzyme activity, cell viability, cellular prostate-specific antigen (PSA) and dihydrotestosterone (DHT) production, mRNA levels of PSA, KLK2, TMPRSS2, and AR genes were measured as endpoints. A declining in the expression of androgen- responsive target genes was seen by either Flu or FICZ in the presence of testosterone. Furthermore, the forced decrease in the expression of AR target genes resulted in 41% and 31% decline in the DHT and PSA concentrations respectively. Tak...
Source: Steroids - October 19, 2019 Category: Drugs & Pharmacology Source Type: research
Crosstalk in the non-classical signal transduction of testosterone and retinol in immature rat testes
This study aimed to investigate the effects of the interaction between testosterone and retinol on the rapid responses of cultured Sertoli cells obtained from 10-day-old immature rat testes. Non-classical actions of testosterone and retinol were investigated, and the activities of L-type voltage-dependent calcium channels (L-VDCC) and voltage-dependent potassium channels (Kv) were determined by measuring 45Ca2+ influx in whole testis. Additionally, the effects of testosterone and retinol on these channels were studied in primary culture of Sertoli cells using the patch-clamp technique. 45Ca2+ influx was used to observe a d...
Source: Steroids - October 15, 2019 Category: Drugs & Pharmacology Source Type: research
Synthesis of cytotoxic urs-12-ene- and 28-nor-urs-12-ene- type conjugates with amino- and mercapto-1,3,4-oxadiazoles and mercapto-1,2,4-triazoles
Publication date: Available online 14 October 2019Source: SteroidsAuthor(s): Sergey A. Popov, Marya D. Semenova, Dmitry S. Baev, Tatiana S. Frolova, Elvira E. Shults, Chengzhang Wang, Māris TurksAbstractA small library of 2-mercapto-1,3,4-oxadiazoles, 2-amino-1,3,4-oxadiazoles and 3-mercapto-1,2,4-triazoles attached to the urs-12-ene- and 28-nor-urs-12-ene skeleton has been obtained. Ursolic acid derived hydrazides have been identified as useful starting materials for the developed synthesis. Ursolic acid hydrazide provided access to oxadiazoles attached directly to C-17 of the ursane core, but synthesis of structurally r...
Source: Steroids - October 15, 2019 Category: Drugs & Pharmacology Source Type: research
Changes of BMI, Steroid Metabolome and Psychopathology in Patients with Anorexia Nervosa During Hospitalization
Publication date: Available online 14 October 2019Source: SteroidsAuthor(s): Josef Bulant, Martin Hill, Marta Velíková, Anna Yamamotová, Pavel Martásek, Hana PapežováAbstractAnorexia nervosa (AN) is associated with various alterations including the dysfunction of the HPA axis and consequently the hypercortisolemia and deficit in sex hormones but the comprehensive evaluation of changes in circulating steroids during the hospitalization of AN patients is lacking. We investigated the effect of realimentation of women with AN during hospitalization on 45 circulating steroids, the relationships between BMI, its change dur...
Source: Steroids - October 15, 2019 Category: Drugs & Pharmacology Source Type: research
Knockdown of PTEN decreases expression of estrogen receptor β and tamoxifen sensitivity of human breast cancer cells
In this study we examined whether expression of ER β in turn might be affected by tumor suppressor PTEN, analyzed the effect of this interaction on tamoxifen response and the co-expression of both genes in human breast cancer samples. After siRNA-mediated PTEN knockdown, Western blot analysis revealed a reduction of ER β protein expression by 67.2% in MCF-7 cells and by 73.6% in T-47D cells (both p<0.01), results which could be verified on the mRNA level. In cells with normal PTEN and ER β status, after 6 days of treatment with 1 µM 4-OH tamoxifen, E2-driven proliferation was decreased by 64.5% in MCF-7 and by 57.7...
Source: Steroids - October 9, 2019 Category: Drugs & Pharmacology Source Type: research
SUMO conjugation as regulator of the glucocorticoid receptor-FKBP51 cellular response to stress
Publication date: Available online 8 October 2019Source: SteroidsAuthor(s): Ana C. Liberman, Maia L. Budziñski, Clara Sokn, Romina P. Gobbini, Maria B. Ugo, Eduardo ArztAbstractIn order to adequately respond to stressful stimuli, glucocorticoids (GCs) target almost every tissue of the body. By exerting a negative feedback loop in the hypothalamic–pituitary–adrenal (HPA) axis GCs inhibit their own synthesis and restore homeostasis. GCs actions are mostly mediated by the GC receptor (GR), a member of the nuclear receptor superfamily. Alterations of the GR activity have been associated to different diseases includin...
Source: Steroids - October 9, 2019 Category: Drugs & Pharmacology Source Type: research
Anti-androgenic effect of 6-formylindolo [3, 2-b] carbazole (FICZ) in LNCaP cells is mediated by the aryl hydrocarbon -androgen receptors cross-talk
In this study, an LNCaP cells were exposed to FICZ, CH223191 and flutamide (Flu) alone or in combination in the presence and absence of testosterone. CYP1A1 enzyme activity, cell viability, cellular prostate-specific antigen (PSA) and dihydrotestosterone (DHT) production, mRNA levels of PSA, KLK2, TMPRSS2, and AR genes were measured as endpoints. A declining in the expression of androgen- responsive target genes was seen by either Flu or FICZ in the presence of testosterone. Furthermore, the forced decrease in AR expression genes resulted in 41% and 31% decline in the DHT and PSA concentrations respectively. Taken together...
Source: Steroids - October 5, 2019 Category: Drugs & Pharmacology Source Type: research
Androgens are effective bronchodilators with anti-inflammatory properties: a potential alternative for asthma therapy
Publication date: Available online 3 October 2019Source: SteroidsAuthor(s): Luis M. Montaño, Edgar Flores-Soto, Bettina Sommer, Héctor Solís-Chagoyán, Mercedes PerusquíaAbstractChanges in plasma androgen levels in asthmatic men may be linked to asthma severity, seemingly acting through nongenomic and genomic effects. Nongenomic effects include rapid relaxation of carbachol or antigenic challenge pre-contracted guinea pig airway smooth muscle (ASM) in vitro: testosterone (TES) blocks L-type voltage dependent Ca2+ channels, stored operated Ca2+ channels, inositol 1,4,5-trisphosphate receptors and promotes prostaglandin ...
Source: Steroids - October 5, 2019 Category: Drugs & Pharmacology Source Type: research
Hormonal balance and nutritional intake in elite tactical athletes
Publication date: Available online 3 October 2019Source: SteroidsAuthor(s): Andrew E. Jensen, Laura J. Arrington, Lorraine P. Turcotte, Karen R. KellyAbstractChronic exposure to multifactorial stress, such as that endured by elite military operators, may lead to overtraining syndrome and negatively impact hormonal regulation. In acute settings (<6 mos), military training has been shown to lead to hormonal dysfunction; however, less is known about the consequences of long-term military training. Thus, the purpose of this study was to determine the chronic effects of military operations and training on the hormone profil...
Source: Steroids - October 5, 2019 Category: Drugs & Pharmacology Source Type: research
Pharmacological Activities of Dehydroepiandrosterone: A Review
Publication date: Available online 3 October 2019Source: SteroidsAuthor(s): Poonam Sahu, Bina Gidwani, H.J. DhongadeAbstractDehydroepiandrosterone (DHEA) is a steroidal hormone secreted by Zonareticularis of the adrenal cortex with a characteristic age related pattern of secretion. These hormones are inactive precursors that are transformed into active sex steroids in peripheral target tissues. These hormones are used for the energy, vitality and the natural support of most bodily functions that involve the endocrine system. DHEA is a 19 carbon steroid hormone, is lipophilic, and can be converted to DHEAs by activity of th...
Source: Steroids - October 5, 2019 Category: Drugs & Pharmacology Source Type: research
Two new 23S,26R-hydroxylated spirostanoid saponins from the fruits of Solanum indicum var. recurvatum
Publication date: Available online 3 October 2019Source: SteroidsAuthor(s): Joseph Sakah Kaunda, Ying-Jun ZhangAbstractSolanum indicum var. recurvatum, distributed mainly in Hekou, Simao and Menghai areas of Yunnan province, China, is characterized by stellate pubescent leaves with irregular lengths and oblong, short, and downwardly curved anthers. The original species, S. indicum, has been used as an anti-inflammatory, wound-healing agent, an analgesic, and for the treatment of rhinitis, cough, and breast cancer in Chinese folk medicine. The variety was chemically studied for the first time, leading to the isolation of tw...
Source: Steroids - October 5, 2019 Category: Drugs & Pharmacology Source Type: research
Discovery and Development of Azasteroids as Anticancer Agents
Publication date: Available online 27 September 2019Source: SteroidsAuthor(s): Nagaraju Birudukota, Mukesh Madan Mudgal, Venkatesh ShanbhagAbstractCancer is the second leading cause of death worldwide following cardiovascular diseases. Cancer can be treated by a variety of techniques including surgery, radiation therapy, immunotherapy, and chemotherapy. Choice of the method can be made based on type, physiologic location and the stage of disease progression. Among chemical methods, steroids find broad applications. Azasteroids have N- substitutions in steroidal rings. This structural modification renders azasteroids advant...
Source: Steroids - September 28, 2019 Category: Drugs & Pharmacology Source Type: research
Molecular mechanisms underlying progesterone receptor action in breast cancer: insights into cell proliferation and stem cell regulation
Publication date: Available online 25 September 2019Source: SteroidsAuthor(s): Mauro E. Cenciarini, Cecilia J. ProiettiAbstractThe ovarian steroid hormone progesterone and its nuclear receptor, the Progesterone Receptor (PR), play an essential role in the regulation of cell proliferation and differentiation in the mammary gland. In addition, experimental and clinical evidence demonstrate their critical role in controlling mammary gland tumorigenesis and breast cancer development. When bound to its ligand, the main action of PR is as a transcription factor, which regulates the expression of target genes networks. PR also ac...
Source: Steroids - September 26, 2019 Category: Drugs & Pharmacology Source Type: research
Synthesis and Antiproliferative Evaluation of Novel Steroid-Benzisoselenazolone Hybrids
Publication date: Available online 20 September 2019Source: SteroidsAuthor(s): Jianguo Cui, Meizhen Wei, Liping Pang, Chunfang Gan, Junan Xiao, Haixin Shi, Junyan Zhan, Zhiping Liu, Yanmin HuangAbstractThe two different types of steroidal benzisoselenazolone hybrids were synthesized by incorporating benzisoselenazolone scaffold into dehydroepiandrosterone and B-norcholesterol. The antiproliferative activity of the synthesized compounds against some carcinoma cell lines were investigated. The results showed that some of these compounds had better inhibitory activity than abiraterone on the proliferation of tumor cells assoc...
Source: Steroids - September 22, 2019 Category: Drugs & Pharmacology Source Type: research
