Testosterone derivatives and related compounds (such as anabolic-androgenic steroids-AAS) are frequently misused by athletes (both professional and amateur) wishing to promote muscle development and strength or to cover AAS misuse. Even though these agents are vastly regarded as abusive material, they have important pharmacological activities that cannot be easily replaced by other drugs and have therapeutic potential in a range of conditions (e.g., wasting syndromes, severe burns, muscle and bone injuries, anemia, hereditary angioedema). Testosterone and related steroids have been in some countries treated as controlled substances, which may affect the availability of these agents for patients who need them for therapeutic reasons in a given country. Although these agents are currently regarded as rather older generation drugs and their use may lead to serious side-effects, they still have medicinal value as androgenic, anabolic, and even anti-androgenic agents. This review summarizes and revisits the medicinal use of compounds based on the structure and biological activity of testosterone, with examples of specific compounds. Additionally, some of the newer androgenic-anabolic compounds are discussed such as selective androgen receptor modulators, the efficacy/adverse-effect profiles of which have not been sufficiently established and which may pose a greater risk than conventional androgenic-anabolic agents.

• MeSH
• lidé MeSH
• nové syntetické drogy chemie   terapeutické užití   MeSH
• prekurzory léčiv chemie   terapeutické užití   MeSH
• rostliny chemie   MeSH
• steroidy chemie   terapeutické užití   MeSH
• testosteron agonisté   analogy a deriváty   chemie   terapeutické užití   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH

The adrenal glands produce significant amounts of steroid hormones and their metabolites, with various levels of androgenic activities. Until recently, the androgenic potency of these adrenal-derived compounds were not well known, but some recent studies have shown that the production of 11-oxo- and 11beta-hydroxy-derived testosterone and dihydrotestosterone evidently have high androgenic activity. This fact has clinical importance, for instance, in various types of congenital adrenal hyperplasia with androgenization or polycystic ovarian syndrome, and laboratory determinations of these substances could help to better evaluate the total androgen pressure in patients with these disorders. Another area of concern is the treatment of prostate cancer with androgen deprivation, which loses effectiveness after a certain time. The concurrent blocking of the secretion of adrenal C(19)-steroids, whether using corticoids or adrenostatics, could increase the effectiveness of androgen-deprivation therapy.

• MeSH
• androgeny chemie   metabolismus   MeSH
• antagonisté androgenů terapeutické užití   MeSH
• cílená molekulární terapie MeSH
• kongenitální adrenální hyperplazie farmakoterapie   metabolismus   patologie   MeSH
• lidé MeSH
• nádory prostaty farmakoterapie   metabolismus   patologie   MeSH
• testosteron analogy a deriváty   antagonisté a inhibitory   metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH

Photodynamic therapy has become a feasible direction for the treatment of both malignant and non-malignant diseases. It has been in the spotlight since FDA regulatory approval was granted to several photosensitizers worldwide. Nevertheless, there are still strong limitations in the targeting specificity that is vital to prevent systemic toxicity. Here, we report the synthesis and biological evaluation of a novel bimodal oxime conjugate composed of a photosensitizing drug, red-emitting pheophorbide a, and nandrolone (NT), a steroid specifically binding the androgen receptor (AR) commonly overexpressed in various tumors. We characterized the physico-chemical properties of the NT-pheophorbide a conjugate (NT-Pba) and singlet oxygen generation. Because light-triggered therapies have the potential to provide important advances in the treatment of hormone-sensitive cancer, the biological potential of this novel specifically-targeted photosensitizer was assessed in prostatic cancer cell lines in vitro using an AR-positive (LNCaP) and an AR-negative/positive cell line (PC-3). U-2 OS cells, both with and without stable AR expression, were used as a second cell line model. Interestingly, we found that the NT-Pba conjugate was not only photodynamically active and AR-specific, but also that its phototoxic effect was more pronounced compared to pristine pheophorbide a. We also examined the intracellular localization of NT-Pba. Live-cell fluorescence microscopy provided clear evidence that the NT-Pba conjugate localized in the endoplasmic reticulum and mitochondria. Moreover, we performed a competitive localization study with the excess of nonfluorescent NT, which was able to displace fluorescent NT-Pba from the cell interior, thereby further confirming the binding specificity. The oxime ether bond degradation was assayed in living cells by both real-time microscopy and a steroid receptor reporter assay using AR U-2 OS cells. Thus, NT-Pba is a promising candidate for both the selective targeting and eradication of AR-positive malignant cells by photodynamic therapy.

• MeSH
• chlorofyl analogy a deriváty   chemie   farmakologie   MeSH
• fluorescenční mikroskopie MeSH
• fotochemoterapie * MeSH
• fotosenzibilizující látky chemická syntéza   chemie   farmakologie   MeSH
• lidé MeSH
• molekulární struktura MeSH
• nádorové buněčné linie MeSH
• optické zobrazování MeSH
• oximy chemie   farmakologie   MeSH
• povrchové vlastnosti MeSH
• proliferace buněk účinky léků   MeSH
• protinádorové látky chemická syntéza   chemie   farmakologie   MeSH
• screeningové testy protinádorových léčiv MeSH
• testosteron analogy a deriváty   chemie   farmakologie   MeSH
• velikost částic MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

Monitoring of steroid esters in blood serum is desirable in order to detect the possible illegal use of natural hormones as growth promoters. A method for the determination of testosterone propionate, testosterone benzoate, testosterone isocaproate, testosterone decanoate and estradiol benzoate in bovine and porcine blood serum was developed. The procedure consists of protein precipitation and removal of phospholipids using a HybridSPE®-Phospholipid column followed by clean-up on a hydrophilic modified styrene polymer Supel(TM)-Select HLB column and LC-MS/MS measurement. The method was validated according to Commission Decision 2002/657/EC. Decision limits for all analytes were observed in the range 5-30 pg ml(-)(1). The method was shown to be robust for bovine and porcine serum analyses and can be applied for both screening and confirmatory determination in routine residue monitoring.

• MeSH
• chemická precipitace MeSH
• chromatografie kapalinová normy   MeSH
• dihydrotestosteron analogy a deriváty   krev   MeSH
• estradiol analogy a deriváty   krev   MeSH
• fosfolipidy izolace a purifikace   MeSH
• krevní proteiny chemie   MeSH
• limita detekce MeSH
• prasata MeSH
• skot MeSH
• směrnice jako téma MeSH
• tandemová hmotnostní spektrometrie normy   MeSH
• testosteron analogy a deriváty   krev   MeSH
• testosteronpropionát krev   MeSH
• zvířata MeSH
• Check Tag
• skot MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

• MeSH
• androgeny * aplikace a dávkování   farmakologie   škodlivé účinky   MeSH
• antikoncepce * metody   škodlivé účinky   MeSH
• dospělí MeSH
• hodnocení výsledků zdravotní péče * MeSH
• injekce intramuskulární MeSH
• kombinovaná farmakoterapie MeSH
• kontraceptiva * aplikace a dávkování   farmakologie   škodlivé účinky   MeSH
• lidé MeSH
• mladiství MeSH
• mladý dospělý MeSH
• norethindron * analogy a deriváty   aplikace a dávkování   farmakologie   škodlivé účinky   MeSH
• prospektivní studie MeSH
• spermatogeneze * účinky léků   MeSH
• těhotenství MeSH
• testosteron * analogy a deriváty   aplikace a dávkování   farmakologie   škodlivé účinky   MeSH
• Check Tag
• dospělí MeSH
• lidé MeSH
• mladiství MeSH
• mladý dospělý MeSH
• mužské pohlaví MeSH
• těhotenství MeSH
• ženské pohlaví MeSH
• Publikační typ
• souhrny MeSH

The aim of this study was to assess monthly testicular development in the cultured breeding stock of sterlet, Acipenser ruthenus, using histological and serum sex steroid changes. Testicular development in the adult male was examined monthly and showed four distinct phases including resting, pre-spawning, spawning and post-spawning. Also, seasonal changes of the testes were described according to its variations in gonadosomatic index (GSI) during different phases of testicular development. Using histology, we identified continuous spermatogenesis and asynchronous gonad development pattern in the testes of male sterlet, which shows that regulation of annual gonadal cycle is influenced by season. Results also showed variation in the GSI value and number of spermatogenic cells according to each season during annual cycle of gonad, as the highest value of GSI was recorded during spawning phase (spring; March-May). Hormonal profiles of 11-ketotestosterone (11-KT) showed peak, which indicated a seasonal pattern of gonadal development. The 11-KT concentration increased considerably during the spermatogenesis (pre-spawning phase) and remained quite high throughout the pre-spermiation period. In the final phase of testicular development (spawning phase), the 11-KT markedly dropped. This study undertook an examination of complete reproductive development in cultured sterlet sturgeon to provide a valuable guide for the future sterlet studies, and allows comparison of reproductive development between sturgeon species.

• MeSH
• časové faktory MeSH
• roční období MeSH
• rozmnožování fyziologie   MeSH
• ryby fyziologie   MeSH
• spermatogeneze MeSH
• testis anatomie a histologie   diagnostické zobrazování   fyziologie   MeSH
• testosteron analogy a deriváty   krev   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

• MeSH
• androgeny nedostatek   MeSH
• andropauza MeSH
• hypogonadismus diagnóza   farmakoterapie   MeSH
• lidé MeSH
• testosteron analogy a deriváty   aplikace a dávkování   nedostatek   terapeutické užití   MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH

Responsive genes for fish embryos have been identified so far for some endocrine pathways but not for androgens. Using transcriptome analysis and multiple concentration-response modeling, we identified putative androgen-responsive genes in zebrafish embryos exposed to 0.05-5000 nM 11-ketotestosterone for 24 h. Four selected genes with sigmoidal concentration-dependent expression profiles (EC50 = 6.5-30.0 nM) were characterized in detail. The expression of cyp2k22 and slco1f4 was demonstrated in the pronephros; lipca was detected in the liver, and sult2st3 was found in the olfactory organs and choroid plexus. Their expression domains, the function of human orthologs, and a pathway analysis suggested a role of these genes in the metabolism of hormones. Hence, it was hypothesized that they were induced to compensate for elevated hormone levels. The induction of sult2st3 and cyp2k22 by 11-ketotestosterone was repressed by co-exposure to the androgen receptor antagonist nilutamide supporting a potential androgen receptor mediated regulation. Sensitivity (expressed as EC50 values) of sult2st3 and cyp2k22 gene expression induction after exposure to other steroidal hormones (11-ketotestosterone ∼ testosterone > progesterone > cortisol > ethinylestradiol) correlated with their known binding affinities to zebrafish androgen receptor. Hence, these genes might represent potential markers for screening of androgenic compounds in the zebrafish embryo.

• MeSH
• androgenní receptory genetika   MeSH
• androgeny genetika   metabolismus   MeSH
• antagonisté androgenů farmakologie   MeSH
• dánio pruhované embryologie   genetika   MeSH
• embryo nesavčí účinky léků   MeSH
• ethinylestradiol farmakologie   MeSH
• exprese genu účinky léků   MeSH
• imidazolidiny farmakologie   MeSH
• lidé MeSH
• stanovení celkové genové exprese MeSH
• testosteron analogy a deriváty   farmakologie   MeSH
• vývojová regulace genové exprese účinky léků   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

In the last decade, several immunoassays have been published as the alternative/complementary rapid methods for steroid analysis in food supplements. The present review shows a significant amount of food supplements containing banned anabolic androgenic steroids that are not declared as ingredients thus presenting risk for consumers and may lead to positive results in anti-doping controls. Traditional methods for analysis of steroids such as LC/MS and GC/MS were used for monitoring suspect food supplements.

• MeSH
• anabolika * aplikace a dávkování   škodlivé účinky   toxicita   MeSH
• chromatografie afinitní metody   využití   MeSH
• chromatografie plynová metody   využití   MeSH
• doping ve sportu * MeSH
• ELISA metody   využití   MeSH
• hypertenze chemicky indukované   MeSH
• infertilita chemicky indukované   MeSH
• koagulopatie chemicky indukované   MeSH
• lékové postižení jater MeSH
• lidé MeSH
• poranění šlachy chemicky indukované   MeSH
• poruchy metabolismu lipidů chemicky indukované   MeSH
• potravní doplňky * škodlivé účinky   MeSH
• steroidy * analýza   MeSH
• testosteron * analogy a deriváty   škodlivé účinky   MeSH
• zákonodárství lékové MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• práce podpořená grantem MeSH

Di-(2-ethylhexyl) phthalate (DEHP) interferes with male reproductive endocrine system in mammals, however its effects on fish reproduction are largely unknown. We evaluated sperm quality and investigated reproductive endocrine system in mature goldfish (Carassius auratus) exposed to nominal 1, 10, and 100μg/L DEHP. To examine DEHP estrogenic activity, one group of goldfish was exposed to 17β-estradiol (5μg/L E2) for comparison. Following 30d of exposure, sperm production was decreased and suppressed in DEHP and E2 treated goldfish, respectively. Sperm motility and velocity were decreased in goldfish exposed to 100 and 10μg/L DEHP at 15s post-sperm activation, respectively. Compared to control, 11-ketotestosterone (11-KT) levels were decreased at 10 and 1μg/L DEHP at day 15 and 30, respectively. In E2 treated goldfish, 11-KT levels were decreased compared to control during the period of exposure. E2 levels were increased in goldfish exposed to E2, but remained unchanged in DEHP treated goldfish during the period of exposure. StAR mRNA levels encoding regulator of cholesterol transfer to steroidogenesis were decreased in DEHP and E2 treated goldfish following 15 and 30d of exposure, respectively. Luteinizing hormone (LH) levels were decreased in DEHP and E2 treated goldfish following 15 and 30d of exposure, respectively. In DEHP treated goldfish, gnrh3, kiss1 and its receptor (gpr54) mRNA levels did not change during the experimental period. In E2 treated goldfish, gnrh3 mRNA levels were decreased at day 7, but kiss1 and gpr54 mRNA levels were increased at day 30 of exposure. The mRNA levels of genes encoding testicular LH and androgen receptors remained unchanged in DEHP and E2 treated goldfish. In contrast to E2 treated goldfish, vitellogenin production was not induced in DEHP treated goldfish and mRNA levels of genes with products mediating estrogenic effects remained unchanged or decreased. In conclusion, DEHP interferes with testis and pituitary hormonal functions to reduce sperm quality in goldfish and does not exhibit estrogenic activity.

• MeSH
• androgenní receptory genetika   metabolismus   MeSH
• chemické látky znečišťující vodu chemie   toxicita   MeSH
• diethylhexylftalát toxicita   MeSH
• estradiol farmakologie   MeSH
• hormon uvolňující gonadotropiny MeSH
• hypofýza účinky léků   metabolismus   MeSH
• imunoanalýza MeSH
• karas zlatý metabolismus   MeSH
• kisspeptiny genetika   metabolismus   MeSH
• kyselina pyrrolidonkarboxylová analogy a deriváty   MeSH
• lidé MeSH
• luteinizační hormon analýza   MeSH
• messenger RNA metabolismus   MeSH
• motilita spermií účinky léků   MeSH
• receptory spřažené s G-proteiny genetika   metabolismus   MeSH
• spermie účinky léků   fyziologie   MeSH
• testis účinky léků   metabolismus   MeSH
• testosteron analogy a deriváty   analýza   MeSH
• vitelogeniny analýza   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH