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Hiv and androgen

Jian Wang, Ming Lang, Qianfa Jia
-Pyones are frequently observed as the core in numerous natural products and biologically important molecules. They have exhibited promising biological activities, such as anti-HIV, antimicrobial, antifungal, telomerase inhibition, pheromonal, androgen, cardiotonic, neurotoxic and phytotoxic effects. In medicinal chemistry, α-pyones often serve as convenient precursors for the assembly of other medicinal important structures. Therefore, the development of an efficient synthetic protocol for the construction of diversified -pyrone derivatives tends to be interesting and highly demanded...
May 16, 2018: Chemistry, An Asian Journal
Valeria Romanucci, Chapla Agarwal, Rajesh Agarwal, Christophe Pannecouque, Mauro Iuliano, Gaetano De Tommaso, Tonino Caruso, Giovanni Di Fabio, Armando Zarrelli
New silibinin phosphodiester glyco-conjugates were synthesized by efficient phosphoramidite chemistry and were fully characterized by 2D-NMR. A wide-ranging study focused on the determination of their pKa and E° values as well as on their radical scavenging activities by different assays (DPPH, ABTS+ and HRSA) was conducted. The new glyco-conjugates are more water-soluble than silibinin, and their radical scavenging activities are higher than those of silibinin. The conjugation therefore improves both the water solubilities and antioxidant activities of the flavonolignan moieties...
April 2018: Bioorganic Chemistry
Ana Coelho Gomes, José Maria Aragüés, Sílvia Guerra, Joana Fernandes, Mário Rui Mascarenhas
Hypogonadotropic hypogonadism (HH) is common and occurs prematurely in HIV-infected men. However, HH with very low testosterone has not been described. Three men with normal pubertal development and HIV1 diagnosis at the ages of 22, 34 and 35 years. All complained of decreased libido, anejaculation and erectile dysfunction thirteen years, six months and one year after HIV diagnosis, respectively. Two had depressive syndrome and two were treated with antiretroviral therapy. Laboratory tests revealed isolated HH in all...
2017: Endocrinology, Diabetes & Metabolism Case Reports
Anupriya Dutta, Hajime Uno, Alex Holman, David R Lorenz, Dana Gabuzda
PURPOSE: African American men have the highest incidence of prostate cancer among ethnic groups, and racial disparity is highest in younger men. Prostate cancer prevalence is rising in HIV-infected men due to improved survival on antiretroviral therapies, yet little is known about racial differences in prostate cancer risk by HIV-infection status and age. METHODS: This is a prospective cohort study of prostate cancer risk in 2,800 HIV-infected and -uninfected men who have sex with men (MSM) aged 40-70 years (22% African American) who were enrolled in the multicenter AIDS cohort study from 1996 to 2010...
July 2017: Cancer Causes & Control: CCC
Eric J Ip, Michael A Yadao, Bijal M Shah, Shadi Doroudgar, Paul J Perry, Michael J Tenerowicz, Lindsay Newsom, Amber A Mann, Hermine Mkrtchyan, Harrison G Pope
BACKGROUND: Limited studies based in England and Australia reported misuse of anabolic-androgenic steroids (AAS) among homosexual men to enhance body image. Anecdotally, AAS are also being misused by homosexual men in the United States. Since many AAS and certain performance enhancing drugs (PEDs) are administered via injection, this poses a potential vector for the spread of infectious disease in an already at-risk population. OBJECTIVES: This study compared and contrasted homosexual and heterosexual male gym clients regarding use of AAS and PEDs, use of alcohol and illicit drugs, seroprevalence of infectious disease, engagement in risky injection practices and sexual behaviors, and presence of psychiatric conditions...
June 7, 2017: Substance Use & Misuse
Carson Schlich, Frank Romanelli
Testosterone is derived from Leydig cells and exerts its effects on androgen receptors to influence growth, mood, voice, and several other bodily functions. As men age, their testosterone levels decline. Human immunodeficiency virus (HIV) infection has also been associated with lowered serum testosterone levels. Subtherapeutic levels of testosterone may lead to fatigue, loss of libido, and dysphoria. Exogenous replacement of testosterone can be accomplished by several modalities (oral, topical, injection), with each having distinct advantages and disadvantages...
October 2016: Hospital Pharmacy
Andrew J Chetwynd, Amanda Samarawickrama, Jaime H Vera, Stephen A Bremner, Alaa Abdul-Sada, Yvonne Gilleece, Stephen G Holt, Elizabeth M Hill
BACKGROUND: The use of combination antiretroviral therapy (cART) has substantially improved the outlook for patients with HIV infection. However, lifelong exposure to cART is also associated with adverse metabolic changes and an enhanced risk of renal, hepatic, and cardiovascular dysfunction. This study investigated disruptions of the urinary metabolome of cART-exposed patients, thereby furthering our understanding of some of the side effects of pharmaceutical intervention. METHODS: HIV-positive patients were recruited from an HIV clinic and divided into cART-naive and cART-exposed groups...
February 1, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
Yuchen Zhang, Pavan K Mantravadi, Soma Jobbagy, Wei Bao, John T Koh
The Androgen Receptor (AR) remains the leading target of advanced prostate cancer therapies. Thiosalicylamide analogs have previously been shown to act in cells as acyltransfer catalysts that are capable of transferring cellular acetate, presumably from acetyl-CoA, to HIV NCp7. Here we explore if the cellular acetyl-transfer activity of thiosalicylamides can be redirected to other cellular targets guided by ligands for AR. We constructed conjugates of thiosalicylamides and the AR-binding small molecule tolfenamic acid, which binds the BF-3 site of AR, proximal to the coactivator "FXXLF" binding surface...
October 21, 2016: ACS Chemical Biology
Asa Radix, Jae Sevelius, Madeline B Deutsch
INTRODUCTION: Studies have shown that transgender women (TGW) are disproportionately affected by HIV, with an estimated HIV prevalence of 19.1% among TGW worldwide. After receiving a diagnosis, HIV-positive TGW have challenges accessing effective HIV treatment, as demonstrated by lower rates of virologic suppression and higher HIV-related mortality. These adverse HIV outcomes have been attributed to the multiple sociocultural and structural barriers that negatively affect their engagement within the HIV care continuum...
2016: Journal of the International AIDS Society
M Badawy Abdel-Naser, Christos C Zouboulis
Male fertility can be affected by a variety of organs diseases, including the skin. Several genodermatoses affect the skin and several other organs including the male reproductive system, commonly in the form of cryptorchidism and hypogonadism. The most relevant syndromes are associated with dyschromias, such as deSanctis-Cacchione, poikiloderma congenital, LEOPARD, and H syndrome; others with ichthyosis, such as Rud, and trichothiodystrophy; or a group of unrelated genodermatoses, such as ablepharon macrostomia, Coffin-Siris, Gorlin-Goltz, and Werner...
September 2016: Reviews in Endocrine & Metabolic Disorders
Yu Zhao, Liguo Wang, Shancheng Ren, Lan Wang, Patrick R Blackburn, Melissa S McNulty, Xu Gao, Meng Qiao, Robert L Vessella, Manish Kohli, Jun Zhang, R Jeffrey Karnes, Donald J Tindall, Youngsoo Kim, Robert MacLeod, Stephen C Ekker, Tiebang Kang, Yinghao Sun, Haojie Huang
The androgen receptor (AR) is required for castration-resistant prostate cancer (CRPC) progression, but the function and disease relevance of AR-bound enhancers remain unclear. Here, we identify a group of AR-regulated enhancer RNAs (e.g., PSA eRNA) that are upregulated in CRPC cells, patient-derived xenografts (PDXs), and patient tissues. PSA eRNA binds to CYCLIN T1, activates P-TEFb, and promotes cis and trans target gene transcription by increasing serine-2 phosphorylation of RNA polymerase II (Pol II-Ser2p)...
April 19, 2016: Cell Reports
Wee Loon Ong, Paul Manohar, Jeremy Millar, Peter Royce
OBJECTIVES: To characterise clinicopathological characteristics of prostate cancer among human immunodeficiency virus (HIV)-positive men and to evaluate the current practice patterns in the management of prostate cancer in these men. PATIENTS AND METHODS: We retrospectively reviewed all patients with HIV in the State-wide HIV referral centre in Victoria, who were diagnosed with prostate cancer from 2000 onwards. In all, 12 patients were identified, and the medical records were reviewed to collect data on HIV parameters at the time of prostate cancer diagnosis, as well as prostate cancer clinicopathological characteristics, treatment details and outcomes...
October 2015: BJU International
Ding Yuan, Wu XiuJuan, Zhang Yan, Liang JunQin, Xiang Fang, Yu Shirong, Kang Xiaojing, Feng Yanyan, Wu Weidong, Luo Dong, Lu Qingli, Zhang DeZhi, Pu XiongMing
BACKGROUND: Kaposi sarcoma (KS) has features of both neoplastic growth and hyperplastic proliferation. It is the most common tumor seen in patients with HIV infection. Whether KS is a real tumor or a benign hyperplastic disease is not known. MATERIAL AND METHODS: Tissues from KS and cutaneous hemangioma lesion DNA were extracted, and then digested with methylation-sensitive restriction endonuclease HpaII. Human androgen receptor gene (HUMARA) was amplified with PCR method and the product was separated on 10% denaturing polyacrylamide gels and stained with ethylene dibromide (EB) to show the polymorphism of HUMARA...
2015: Medical Science Monitor Basic Research
Christopher J Mulder, Ryan S Cho, Stephen A Harrison, Katherine Cebe, James M Francis
BACKGROUND: Giant cell hepatitis is a rare entity in adults, accounting for 0.1% to 0.25% of liver disease in adults. Postinfantile giant cell hepatitis is often characterized by multinucleated giant cells on liver biopsy and a fulminant hepatitis. CASE REPORT: An active duty 36-year-old African-American male deployed to Kabul, Afghanistan, presented with jaundice 2 weeks after starting a testosterone analogue. He discontinued the supplement, but his jaundice persisted with up-trending bilirubin...
May 2015: Military Medicine
Yun Hua, Tong Ying Shun, Christopher J Strock, Paul A Johnston
The androgen receptor-transcriptional intermediary factor 2 (AR-TIF2) positional protein-protein interaction (PPI) biosensor assay described herein combines physiologically relevant cell-based assays with the specificity of binding assays by incorporating structural information of AR and TIF2 functional domains along with intracellular targeting sequences and fluorescent reporters. Expression of the AR-red fluorescent protein (RFP) "prey" and TIF2-green fluorescent protein (GFP) "bait" components of the biosensor was directed by recombinant adenovirus constructs that expressed the ligand binding and activation function 2 surface domains of AR fused to RFP with nuclear localization and nuclear export sequences, and three α-helical LXXLL motifs from TIF2 fused to GFP and an HIV Rev nucleolar targeting sequence...
September 2014: Assay and Drug Development Technologies
Vincenzo Rochira, Giovanni Guaraldi
Androgen deficiency occurs frequently in men with human immunodeficiency virus (HIV) infection. Antiretroviral treatments had reduced the prevalence of male hypogonadism. The pathogenesis of testosterone (T) deficiency in HIV is multifactorial. Several mechanisms have been proposed; among them, drugs, fat redistribution, and a poor health status could explain the mechanism leading to gonadotropins inhibition and hypogonadotropic hypogonadism. The diagnosis of hypogonadism in HIV-infected men should be made based on clinical symptoms and a specific workup including T measurement...
September 2014: Endocrinology and Metabolism Clinics of North America
J Pepe, A M Isidori, M Falciano, G Iaiani, A Salotti, D Diacinti, R Del Fiacco, E Sbardella, C Cipriani, S Piemonte, O Raimo, P Biondi, F Biamonte, A Lenzi, S Minisola
The aim of the study was to evaluate the effect of risedronate on bone mineral density (BMD) and bone turnover markers in HIV-infected osteoporotic males, according to their gonadal status. HIV patients were followed up for 24 months and divided into two groups: patients with osteoporosis or osteopenia with fractures (group A, n = 20) and those without (group B, n = 21). Group A and B were further divided according to the presence of reduced androgenizations. Both groups were treated with cholecalciferol 800 I...
November 2014: Endocrine
Donita J Africander, Karl-Heinz Storbeck, Janet P Hapgood
The importance of investigating the molecular mechanism of action of medroxyprogesterone acetate (MPA) and norethisterone acetate (NET-A), two clinically important progestins used in hormone therapy (HT), has been highlighted by clinical evidence showing that MPA and norethisterone (NET) increase the risk of the development of breast cancer in HRT users, and that MPA may increase susceptibility to- and transmission of HIV-1. The aim of this study was to compare the molecular mechanisms of action of MPA, NET-A and progesterone (Prog) via the androgen receptor (AR) in a cell line model that can minimize confounding factors such as the presence of other steroid receptors...
September 2014: Journal of Steroid Biochemistry and Molecular Biology
Luis Bahamondes, M Valeria Bahamondes
BACKGROUND: The first hormonal contraceptive was introduced onto the market in several countries 50 years ago; however, the portfolio of contraceptive methods remains restricted with regards to their steroid composition, their cost, and their ability to satisfy the requirements of millions of women/couples in accordance with their different reproductive intentions, behaviors, cultures, and settings. METHODS: A literature review was conducted using Medline, Embase, and Current Contents databases, up to September 1, 2013 to identify publications reporting new contraceptives in development using combinations of the search terms: contraception, contraceptives, oral contraceptives, patch, vaginal ring, implants, intrauterine contraceptives, and emergency contraception (EC)...
2014: International Journal of Women's Health
Reshmi Srinath, Adrian Dobs
Muscle loss and wasting occurs with aging and in multiple disease states including cancer, heart failure, chronic obstructive pulmonary disease, end-stage liver disease, end-stage renal disease and HIV. Cachexia is defined as a multifactorial syndrome that is associated with anorexia, weight loss and increased catabolism, with increased morbidity and mortality. Currently no therapy is approved for the treatment or prevention of cachexia. Different treatment options have been suggested but many have proven to be ineffective or associated with adverse events...
February 2014: Future Oncology
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