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https://www.readbyqxmd.com/read/29327585/photoinduced-generation-of-acyl-radicals-from-simple-aldehydes-access-to-3-acyl-4-arylcoumarin-derivatives-and-evaluation-of-their-antiandrogenic-activities
#1
Kazuki Kawaai, Tomoaki Yamaguchi, Eiji Yamaguchi, Satoshi Endo, Norihiro Tada, Akira Ikari, Akichika Itoh
A novel photocatalysis to construct the 3-acyl-4-arylcoumarin framework from simple aldehyde with ynoate is described. The reac-tion proceeded through an acyl radical intermediate generated by hydrogen atom abstraction from aldehyde followed by reaction with ynoate and then cyclization to afford coumarins. This valuable radical cyclization reaction gave over 20 coumarin derivatives in moderate to good yields with inexpensive 2-tBu-anthraquinone as a catalyst. In addition, synthetic coumarins were investigated for 5α-dihydrotestosterone (DHT)-induced secretion of prostate-specific antigen (PSA) levels and cell proliferation of androgen-dependent CWR22Rv1 cells...
January 12, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29322301/effects-of-short-term-dhea-intake-on-hormonal-responses-in-young-recreationally-trained-athletes-modulation-by-gender
#2
Katia Collomp, Corinne Buisson, Nicolas Gravisse, Soraya Belgherbi, Zakaria Labsy, Manh-Cuong Do, Olivier Gagey, Sophie Dufay, Nancy Vibarel-Rebot, Michel Audran
BACKGROUND: Dehydroepiandrosterone (DHEA) figures on the World Anti-Doping Agency list of prohibited substances in sport because it is assumed that athletes expect a significant increase in testosterone through DHEA administration. The literature on the hormonal effects of DHEA intake nevertheless appears to be very scant in healthy young subjects, especially women. PURPOSE: We examined the effects of DHEA on adrenal and gonadal hormones, IGF1 and free T3 in healthy young male and female recreationally trained volunteers...
January 10, 2018: Endocrine
https://www.readbyqxmd.com/read/29318957/research-brief-self-reports-of-a-constellation-of-persistent-antiandrogenic-estrogenic-physical-and-psychological-effects-of-finasteride-usage-among-men
#3
Alicia A Walf, Shan Kaurejo, Cheryl A Frye
Our research objective is to understand more, through subjective, self-reports on discussion boards/forums, persons' experiences associated with the use of drugs that alter androgen metabolism, such as finasteride. Finasteride is an orally active, specific inhibitor of 5α-reductase, which is localized to many androgen-dependent tissues. Finasteride inhibits the conversion of testosterone (T) to dihydrotestosterone (DHT), and is commonly used to treat benign prostatic hypertrophy (BPH) and male pattern baldness (MPB), both disorders associated with elevated DHT levels and 5α-reductase activity in the prostate and hair follicles, respectively...
January 1, 2018: American Journal of Men's Health
https://www.readbyqxmd.com/read/29315373/female-offspring-from-chronic-hyperandrogenemic-dams-exhibit-delayed-puberty-and-impaired-ovarian-reserve
#4
Zhiqiang Wang, Mingjie Shen, Ping Xue, Sara A DiVall, James Segars, Sheng Wu
Female offspring of many species exposed to high doses of androgens in utero experience endocrine dysfunction during adulthood. The phenotype of offspring from females with pre-pregnancy hyperandrogenemia and impaired ovulation, however, has not been examined. We developed a mouse model of hyperandrogenemia by implanting a low dose dihydrotestosterone (DHT) pellet 15 days before conception. The serum DHT levels in dams treated with the pellet were 1.7 to 2 fold higher (p<0.005) than levels in dams without DHT...
January 5, 2018: Endocrinology
https://www.readbyqxmd.com/read/29312607/androgen-enhances-the-activity-of-ets-1-and-promotes-the-proliferation-of-hcc-cells
#5
Hui Ren, Bo Ren, Jiabin Zhang, Xiaofeng Zhang, Lixin Li, Lingzhan Meng, Zhijie Li, Jia Li, Yinjie Gao, Xuemei Ma
The expression of androgen receptor (AR) has been detected in hepatocellular cancer (HCC). However, there is no universal model detailing AR's function and mechanism in HCC. This study's results show that treatment with dihydrotestosterone (DHT), an endogenous androgen, promoted HCC cells' proliferation and up-regulated the transcription factor activity of ETS-1 (E26 transformation specific sequence 1), which mediates the migration and invasion of cancer cells via protein-protein interaction between AR and ETS-1...
December 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29305509/transcriptional-responses-of-pseudomonas-aeruginosa-to-potable-water-and-freshwater
#6
Erika L English, Kristin C Schutz, Graham G Willsey, Matthew J Wargo
Many Pseudomonas aeruginosa infections are derived from residential, recreational, or surface water sources, thus, these environments represent an important pre-infection niche. To better understand P. aeruginosa biology in these environments, we quantified transcriptional changes by microarray after exposure to diluted LB, diluted R2B, potable tap water, and freshwater from a eutrophic pond. qRT-PCR confirmed conservation of these responses in other water sources, and competition experiments were used to test the importance of three implicated metabolic pathways...
January 5, 2018: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/29289577/longitudinal-serum-and-urine-steroid-metabolite-profiling-in-a-46-xy-infant-with-prenatally-identified-por-deficiency
#7
Hiroyuki Ono, Chikahiko Numakura, Keiko Homma, Tomonobu Hasegawa, Seiji Tsutsumi, Fumiko Kato, Yasuko Fujisawa, Maki Fukami, Tsutomu Ogata
Although POR deficiency (PORD) is assumed to be accompanied by excessive placental androgen accumulation and enhanced adrenal and testicular androgen production via the backdoor pathway as well as compromised testicular androgen production via the frontdoor pathway, there is no direct evidence for the flux of excessive placental androgens into the fetal circulation and for the production of dihydrotestosterone (DHT) via the backdoor pathway. We examined longitudinal serum and urine steroid metabolite profiles in a 46,XY infant with PORD who was prenatally identified because of the progressive fetal masculinization and maternal virilization from the mid-gestation and the presence of fetal radio-humeral synostosis and was confirmed to have compound heterozygous mutations of POR (p...
December 28, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29278848/bisphenol-a-antagonizes-the-rapidly-modulating-effect-of-dht-on-spinogenesis-and-long-term-potentiation-of-hippocampal-neurons
#8
Yang Yang, Zhaoqing Fang, Yuhua Dai, Yu Wang, Yufeng Liang, Xiaoyu Zhong, Qinwen Wang, Yizhong Hu, Zigui Zhang, Donghong Wu, Xiaohong Xu
Bisphenol A (BPA), a common environmental endocrine disruptor, modulates estrogenic, antiestrogenic, and antiandrogenic effects throughout the lifespan. Recent studies found more obvious adverse effect of BPA on some neurobehavior in males than that in females. In this study, BPA at 10-100 nM rapidly increased the densities of the dendrite spine and synapse in cultured hippocampal neurons of rats in vitro within 1 h. Co-treatment of BPA (100 nM) with dihydrotestosterone (DHT, 10 nM) or with 17β-E2 (10 nM) completely eliminated the promotion of DHT or 17β-E2 in the densities of the dendritic spine and synapse...
December 23, 2017: Chemosphere
https://www.readbyqxmd.com/read/29261512/lncrna-part1-modulates-toll-like-receptor-pathway-to-influence-cell-proliferation-and-apoptosis-in-prostate-cancer-cells
#9
Ming Sun, Donghua Geng, Shuqiang Li, Zhaofu Chen, Wenyan Zhao
We investigated thoroughly the effect of lncRNA PART1 on prostate cancer cells proliferation and apoptosis, through regulating Toll-like receptor (TLR) pathways. LncRNA PART1 expression was also examined by qRT-PCR in human tissues and cells lines LNCaP and PC3. After transfection with si-PART1 or control constructs, the cell viability was measured by MTS and colony formation assay. In addition, the apoptosis rate of the prostate cancer cells was validated by TUNEL staining. Relationships between lncRNA PART1 expression and TLR pathway genes were demonstrated by qRT-PCR and Western blotting...
June 27, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/29247133/dihydrotestosterone-induces-pro-angiogenic-factors-and-assists-homing-of-msc-into-the-cardiac-tissue
#10
Mirel-Adrian Popa, Maria-Cristina Mihai, Alina Constantin, Viorel Şuică, Cătălin Ţucureanu, Raluca Costache, Felicia Antohe, Raghvendra K Dubey, Maya Simionescu
The use of mesenchymal stem cells (MSC) as a therapeutic tool in cardiovascular diseases is promising. Since androgens exert some beneficial actions on the cardiovascular system, we tested our hypothesis that this hormone could promote MSC-mediated repair processes, also. Cultured MSCs isolated from Wharton's jelly were exposed to 30 nM dihydrotestosterone (DHT) for 1 or 4 days and the effects of the hormone on their growth/migration/adhesion and the underlying mechanisms were assessed. Results were obtained by real-time cell impedance measurements, and DNA quantification showed that DHT increased MSC proliferation by ~30%...
January 2018: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/29237170/functional-impact-of-novel-androgen-receptor-mutations-on-the-clinical-manifestation-of-androgen-insensitivity-syndrome
#11
Reginaldo J Petroli, Olaf Hiort, Dagmar Struve, Julia K Gesing, Fernanda C Soardi, Angela M Spínola-Castro, Karla Melo, Ivo J Prado Arnhold, Andréa T Maciel-Guerra, Gil Guerra-Junior, Ralf Werner, Maricilda P de Mello
Androgens are responsible for the development and maintenance of male sex characteristics. Dysfunctions in androgen action due to mutations in the androgen receptor gene (AR) can lead to androgen insensitivity syndrome (AIS) that can be classified as mild (MAIS), partial (PAIS), or complete (CAIS). We have analyzed functional effects of p.Ser760Thr, p.Leu831Phe, p.Ile899Phe, p.Leu769Val, and p.Pro905Arg mutations and the combination p.Gln799Glu + p.Cys807Phe that were identified in patients with PAIS or CAIS...
December 14, 2017: Sexual Development: Genetics, Molecular Biology, Evolution, Endocrinology, Embryology, and Pathology of Sex Determination and Differentiation
https://www.readbyqxmd.com/read/29237093/serum-androgens-and-psa-levels-in-androgenetic-alopecia-is-there-a-difference-between-frontal-and-vertex-baldness
#12
Anna Lis-Święty, Hubert Arasiewicz, Irmina Ranosz-Janicka, Ligia Brzezińska-Wcisło
BACKGROUND: Androgenetic alopecia (AGA) seems to be a marker of increased risk of prostate cancer (PCa). OBJECTIVE: We sought to investigate potential pathophysiological differences between frontal and vertex balding that might have the impact on the incidence of PCa. METHODS: Serum concentrations of testosterone (T), dihydrotestosterone (DHT) and prostate-specific antigen (PSA) were measured in 88 subjects with AGA. RESULTS: We have examined sixty patients with frontal baldness and 28 patients with vertex baldness...
December 13, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29232631/ambiguous-genitalia-a-social-dilemma-in-bangladesh-a-case-report
#13
Mohiuddin Ahsanul Kabir Chowdhury, Rashidul Anwar, Arnab Saha
INTRODUCTION: Ambiguous Genitalia is a form of birth defect in which sex of the newborn cannot be readily distinguishable because of atypical appearance of the external genitalia. CASE REPORT-CLINICAL FINDINGS: The patient, an 8 months old baby, was identified as a female baby since birth; but, some senior members of their neighborhood raised confusion regarding sex differentiation of the child. On examination, there was enlarged clitoris or micropenis, bifid scrotum or labioscrotal fold, and separate presence of urethral and vaginal orifices...
December 8, 2017: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/29225278/physiochemical-properties-and-resorption-progress-of-porcine-skin-derived-collagen-membranes-in-vitro-and-in-vivo-analysis
#14
Yin-Zhe An, You-Kyoung Kim, Su-Min Lim, Yeong-Ku Heo, Mi-Kyung Kwon, Jae-Kook Cha, Jung-Seok Lee, Ui-Won Jung, Seong-Ho Choi
The aim of the present study was to evaluate the physiochemical properties and resorption progress of two cross-linked, porcine skin-derived collagen membranes and compare their features with those of a membrane without cross-linking (Bio-Gide® [BG], Geistlich Biomaterials, Wolhusen, Switzerland). Three porcine skin-derived collagen membranes, dehydrothermally (DHT) crosslinked (experimental), DHT and 1-ethyl-3(3-dimethylaminopropyl)-carbodiimide (DHT/EDC) cross-linked (experimental) and BG were investigated for their morphology, enzyme resistance, and tensile strength in vitro and biodegradation in vivo...
December 8, 2017: Dental Materials Journal
https://www.readbyqxmd.com/read/29224108/negative-impact-of-testosterone-deficiency-and-5%C3%AE-reductase-inhibitors-therapy-on-metabolic-and-sexual-function-in-men
#15
Abdulmaged M Traish
Androgens are steroid hormones with pleotropic and diverse biochemical and physiological functions, and androgen deficiency exerts a negative impact on human health. Testosterone (T) either directly or via its transformation into the more potent metabolite 5α-dihydrotestosterone (5α-DHT) or via aromatization into estradiol (E2) modulates important biochemical signaling pathways of human physiology and plays a critical role in the growth and/or maintenance of functions in a host of tissues and organs. T and 5α-DHT play an important role in regulating physiology of the muscle, adipose tissue, liver, bone, and central nervous system, as well as reproductive and sexual functions...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29216878/adaptive-phenotype-drives-resistance-to-androgen-deprivation-therapy-in-prostate-cancer
#16
Nicoletta Ferrari, Ilaria Granata, Matteo Capaia, Marina Piccirillo, Mario Rosario Guarracino, Roberta Venè, Antonella Brizzolara, Andrea Petretto, Elvira Inglese, Martina Morini, Simonetta Astigiano, Adriana Agnese Amaro, Francesco Boccardo, Cecilia Balbi, Paola Barboro
BACKGROUND: Prostate cancer (PCa), the second most common cancer affecting men worldwide, shows a broad spectrum of biological and clinical behaviour representing the epiphenomenon of an extreme heterogeneity. Androgen deprivation therapy is the mainstay of treatment for advanced forms but after few years the majority of patients progress to castration-resistant prostate cancer (CRPC), a lethal form that poses considerable therapeutic challenges. METHODS: Western blotting, immunocytochemistry, invasion and reporter assays, and in vivo studies were performed to characterize androgen resistant sublines phenotype in comparison to the parental cell line LNCaP...
December 8, 2017: Cell Communication and Signaling: CCS
https://www.readbyqxmd.com/read/29204121/abnormal-cftr-affects-glucagon-production-by-islet-%C3%AE-cells-in-cystic-fibrosis-and-polycystic-ovarian-syndrome
#17
Wen Qing Huang, Jing Hui Guo, Chun Yuan, Yu Gui Cui, Fei Yang Diao, Mei Kuen Yu, Jia Yin Liu, Ye Chun Ruan, Hsiao Chang Chan
Glucagon, produced by islet α cells, functions to increase blood glucose. Abnormal glucose levels are often seen in cystic fibrosis (CF), a systematic disease caused by mutations of the CF transmembrane conductance regulator (CFTR), and in polycystic ovarian syndrome (PCOS), an endocrine disorder featured with hyperandrogenism affecting 5-10% women of reproductive age. Here, we explored the role of CFTR in glucagon production in α cells and its possible contribution to glucagon disturbance in CF and PCOS...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/29203347/effect-of-dry-heat-treatment-on-physical-property-and-in-vitro-starch-digestibility-of-high-amylose-rice-starch
#18
Im Kyung Oh, In Young Bae, Hyeon Gyu Lee
The influence of dry heat treatment (DHT) of high amylose rice starch was investigated on starch digestibility and physical properties and their characteristics were compared through the PCA analysis. High amylose rice starch was prepared by DHT under different temperatures (110, 130, and 150°C) and times (0, 1, 2, and 4hours). The gelatinization temperature and enthalpy decreased as temperature and time increased, revealing the change of semi-crystalline region. There were significant increases in gel strength and pasting viscosity above 130°C, whereas gel strength and pasting viscosity were reduced with increasing heating time...
December 1, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29194865/finasteride-accelerates-prostate-wound-healing-after-thulium-laser-resection-through-dht-and-ar-signalling
#19
Ruizhe Zhao, Xingjie Wang, Chenyi Jiang, Fei Shi, Yiping Zhu, Boyu Yang, Jian Zhuo, Yifeng Jing, Guangheng Luo, Shujie Xia, Bangmin Han
OBJECTIVES: Urinary tract infection, urinary frequency, urgency, urodynia and haemorrhage are common post-operative complications of thulium laser resection of the prostate (TmLRP). Our study mainly focuses on the role of finasteride in prostate wound healing through AR signalling. MATERIALS AND METHODS: TmLRP beagles were randomly distributed into different treatment groups. Serum and intra-prostatic testosterone and DHT level were determined. Histological analysis was conducted to study the re-epithelialization and inflammatory response of the prostatic urethra in each group...
November 30, 2017: Cell Proliferation
https://www.readbyqxmd.com/read/29194818/rapid-non-genomic-modulation-by-neurosteroids-of-dendritic-spines-in-the-hippocampus-androgen-estrogen-and-corticosteroid
#20
REVIEW
Gen Murakami, Yasushi Hojo, Asami Kato, Yoshimasa Komatsuzaki, Shigeo Horie, Mika Soma, Jonghyuk Kim, Suguru Kawato
Memories are stored in synapses which consist of axon terminals and dendritic spines. Dendritic spines are postsynaptic structures of synapses and essential for synaptic plasticity and cognition. Therefore, extensive investigations about functions and structures of spines have been performed. Sex steroids and stress steroids have been shown to modulate hippocampal synapses. Although rapid modulatory action of sex steroids on synapses has been studied in hippocampal neurons over several decades, its essential molecular mechanisms have not been fully understood...
December 1, 2017: Journal of Neuroendocrinology
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