Endocrine Abstracts

Statins are drugs used for the treatment of hypercholesterolemia. Statins have two chiral centers in their molecules, thus they form four enantiomers (3R5R-, 3R5S-, 3S5R- and 3S5S-). Regarding the most frequently prescribed statins, following enantiopure formulations are used in the clinics: 3R5R-atorvastatin, 3R5S-rosuvastatin and 3R5S-fluvastatin. Individual enantiomers of one drug can qualitatively and quantitatively differ in their biological activities. In some cases, onl...

Several of currently used drugs are chiral compounds. Majority of them are clinically administered as a racemic (equimolar) mixture of enantiomers. Individual enantiomers of one drug can qualitatively and quantitatively differ in their biological activities (pharmacology, toxicology, pharmacokinetics, etc.). Therefore, enantiopure drugs have been developed and introduced to the therapy. Statins are drugs used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reducta...

Regulation of gene expression mediated by thyroid hormones (THs) plays an essential role in variety of physiological processes. It is known that large group of natural and synthetic compounds, generally termed endocrine disruptors, can interfere with endocrine system and thus disrupt homeostasis of hormonal regulation processes in human organism. In order to screen for substances with potential disrupting effects on TH pathway, we developed and characterized human luciferase r...

Vitamin D receptor (VDR) signalling can be affected with a variety of compounds, both endo- or exogenous. However, any disruption of VDR transcriptional activity can exert severe physiological or pathophysiological outcomes. It is therefore of a great importance to have a reliable in vitro screening technique that would provide a tool for efficient identification of agonists and activators of human VDR. In the current work, we described two novel human reporter cell l...

Mycophenolate mofetil (MYC) is widely used in transplant medicine as an immunosuppressant drug to prevent rejection in organ transplantation. In this work we investigated the effect of MYC on the activity of androgen receptor (AR) by employing gene reporter assay (GRA) and PCR in prostate cancer cell line 22Rv1.Slight but significant activation of AR was observed for cells treated with MYC in stably transfected 22Rv1 cells (AIZ-AR). Moreover, significant...

Anthocyanidins are aglycons of anthocyanins, which are plant pigments responsible for floral and fruits color. Anthocyanidins possess beneficial pharmacological properties such as antioxidant, anti-inflammatory, anti-tumor and anti-diabetic. Anthocyanidins are contained in normal diet and might play role in food-drug interactions.The aim of current study was to evaluate the effects of cyanidin, delphinidin, malvidin, pelargonidin and peonidin on the tran...

Androgen receptor (AR, NR3C4) is a 110-kDa ligand-activated transcriptional factor that belongs to the steroid hormone receptor superfamily. It has broad developmental effects and its mutations may have a great impact on pubertal development, genesis of prostatic hyperplasia, and even prostate cancer. Commonly known endogenous ligands of AR are testosterone and 5α-dihydrotestosterone (DHT). In the last years, several drugs and environmental pollutants were identified to a...