Binding of mepartricin to sex hormones, a key factor of its activity on benign prostatic hyperplasia
| Autor: | Tiberio Bruzzese, Flavio Peroglio, Domenico Barone, Emiliano Toso |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Male
medicine.medical_specialty Prostatic Hyperplasia Centrifugation Biology In Vitro Techniques urologic and male genital diseases Mepartricin Hormone Antagonists Prostate Internal medicine Drug Discovery medicine Animals Bile Humans Testosterone Gonadal Steroid Hormones Estradiol food and beverages Gallbladder Biological activity Dihydrotestosterone Blood Proteins Hyperplasia medicine.disease Endocrinology medicine.anatomical_structure Mechanism of action Cattle medicine.symptom medicine.drug Hormone Protein Binding |
| Zdroj: | Arzneimittel-Forschung. 51(12) |
| ISSN: | 0004-4172 |
| Popis: | Androgens and estrogens, mainly testosterone (TES) and dihydrotestosterone (DHT) and 17s-estradiol (EST), are widely recognized to regulate the prostate growth and their imbalance with aging, leading to reduction of androgens and relative increase of estrogens, may be responsible for the development of benign prostatic hyperplasia (BPH). Mepartricin (CAS 11121-32-7), a polyene drug for medical treatment of BPH, was assayed in vitro for its ability to bind with 14C-labelled sex hormones, by incubation in buffered saline, serum and bile, followed by centrifugation and dosing of the radioactivity in the supernatant. It proved effective in complexing up to 90 % of TES and DHT in buffered saline and up to 80 % of EST in bile. Due to minimal absorption of oral mepartricin and to much higher entero-hepatic circulation for estrogens than for androgens, the binding effect of mepartricin on EST in the gut should be of particular pharmacological relevance to explain its mechanism of action on BPH. |
| Databáze: | OpenAIRE |
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