A soluble androgen receptor in the cytoplasm of the male mastomys prostate

Summary A steroid receptor protein was isolated from the cytoplasmic fraction of Mastomys prostate. Following in vivo and in vitro labelling of the tissue with tritiated testosterone or dihydrotestosterone, samples were analysed by gel exclusion chromatography or sucrose density gradient centrifugation. A steroid receptor complex was isolated on Sephadex G-200. Analysis of the steroids associated with this complex showed that the major part of the bound radioactivity was 5 -dihydrotestosterone. The binding was inhibited by unlabelled testosterone and could not be demonstrated in the liver cytosol. Using sucrose desity gradient centrifugation, the dihydrotestosterone receptor complex sedimented at 5.6 s together with heavier aggregates. In the presence of 0.4 M KCl a single complex was sedimented at 4. 6 s. The results demonstrate a receptor protein in the cytosol of the Mastomys prostate which binds to dihydrotestosterone and is comparable to that of rat prostate.     

Molecular modeling, structure activity relationship and immunomodulatory properties of some lupeol derivatives

Currently, scientists are focused on developing drug-like compounds as an alternative to the available immunosuppressive drugs with less side effects. Therefore, in the current study we tried to generate derivatives of lupeol and investigate their primary effects on the immune system. In the second part, a computational approach, integrating molecular docking, and molecular dynamics simulation was used to assess the likely mechanism of action and the preliminary analysis of the structure activity relationship (SAR). Our goal for this research was to develop an in-depth SAR for the design of future immunosuppressive lupeol analogs with the potential clinical use.     

Suppressive effects of surgical stress on circulating androgens during and after prostatectomy

Changes in circulating testosterone (T) and dihydrotestosterone (DHT) levels were investigated 2 days before and 2, 7, 30 and 60 days after retropubic prostatectomy in 28 patients with benign prostatic hypertrophy. Following operation the concentrations of both steroids declined and reached minimal levels 2 days after surgery. One month post-operatively testosterone had recovered to its pre-operative value, whilst the recovery of dihydrotestosterone to its pre-operative level required a minimum period of 2 months. These data indicate the need for careful interpretation of any androgen measurement following surgery.     

Differential androgen uptake by the lobes of the rhesus monkey prostate.

The prostate of the rhesus monkey (Mucacca mulatta) consists of a cranial and a caudal lobe. The uptake of [3H] testosterone by these 2 lobes has been measured and compared with control tissues. A significantly higher uptake of radioactivity was found in the caudal lobe when compared to cranial as well as other control tissues. The uptake of radioactivity by the caudal and cranial lobes was suppressed when unlabelled testosterone was introduced into the incubation media. The relationship between these 2 lobes of the monkey prostate and the central and peripheral zones of the human prostate is described.     

The use of 123I labelled oestradiol in detecting the human prostate using a gamma camera.

123I labelled oestradiol was administered into patients with either benign hypertrophy or malignancy of the prostate, in order to detect the prostate. Using a gamma camera the results showed considerable radioactivity in the bladder-prostate region. The exact anatomical position of the prostate was determined by emptying the bladder and introducing 123I labelled sodium iodide into the balloon of the catheter already inserted in the bladder. The results demonstrated that the detected radioactivity in this region was in the bladder rather than the prostate. This conclusion was later confirmed by the presence of high level of the radioactivity in the urine and the extremely low concentration of the radioactivity in the prostate after the removal of the gland.     

Circulating unconjugated 5 alpha-androstane-3 alpha, 17 beta-diol in elderly men and patients with prostatic tumours

Circulating levels of 5 alpha-androstane-3 alpha,17 beta-diol (diol) were measured in 24 elderly men (50-80 years) without prostatic tumours and compared with 32 patients (54-84 years) with benign prostatic hypertrophy (BPH) and 32 patients (51-85 years) with carcinoma of the prostate (Ca). The mean +/- s.e.m. for serum concentrations of diol in patients with BPH, Ca and normals were 813 +/- 43, 524 +/- 35 and 635 +/- 28 pmol/l, respectively. There were significant differences between the mean values of these groups. The increased level of diol in BPH patients, when compared to the normals, corresponds to our previous report of elevated levels of its precursor, namely 5 alpha-dihydrotestosterone (DHT), in these patients. Although the mean values for diol were significantly different between the BPH and Ca patients, the scattered values within each group could not be utilized as an index to differentiate the two groups of patients.