Effects of Mepartricin, a polyene macrolide agent, on fecal excretion and serum concentration of estrogen and number of prostatic estrogen receptors in immature rats

• Published in: The Prostate Vol. 38; no. 1; pp. 17 - 27
• Main Authors: Shakutou, Shuuji, Bandoh, Kohsuke, Yoshinaka, Yasunobu, Kobayashi, Hideyuki, Yamanaka, Hidetoshi
• Format: Journal Article
• Language: English
• Published: New York John Wiley & Sons, Inc 01.01.1999; Wiley-Liss
• Subjects: Administration, Oral; Animals; Anti-Bacterial Agents - pharmacology; Antifungal Agents - pharmacology; Biological and medical sciences; Dose-Response Relationship, Drug; Estrogens - analysis; Estrogens - blood; Feces - chemistry; Genital system. Reproduction; intestinal absorption; Luteinizing Hormone - blood; Male; Medical sciences; Mepartricin - pharmacology; Pharmacology. Drug treatments; polyene antibiotics; Prostate - drug effects; Prostate - metabolism; prostatic hyperplasia; Radioimmunoassay; Rats; Rats, Sprague-Dawley; Receptors, Androgen - analysis; Receptors, Androgen - drug effects; Receptors, Estrogen - analysis; Receptors, Estrogen - drug effects; sex hormones; Spectrophotometry; Testosterone - analysis; Testosterone - blood; Prostate disease; Rat; Hyperplasia; Antiestrogen; Estrogen; Male; Antihormone; Mepartricin; Antifungal agent; Feces; Male genital diseases; Quantitative analysis; Biological receptor; Urinary system disease; Rodentia; Macrolide; Ovarian hormone; Vertebrata; Chemotherapy; Mammalia; Impuberal animal; Treatment; Animal; Sex steroid hormone; Prostate; Hormonal receptor
• ISSN: 0270-4137; 1097-0045
• DOI: 10.1002/(SICI)1097-0045(19990101)38:1<17::AID-PROS2>3.0.CO;2-T

BACKGROUND Mepartricin, an antifungal agent, was investigated for effects on fecal excretion and serum concentration of sex steroids and the number of sex steroid prostatic receptors in immature rats. METHODS Mepartricin was orally administered at 2.5, 5, and 10 mg/kg once daily for 2 weeks. Fecal estrogen and testosterone excretions, serum estrogen, testosterone and luteinizing hormone concentrations, and numbers of prostatic estrogen and androgen receptors were assayed. Prostate weight was also monitored. RESULTS Fecal estrogen excretion showed a dose‐dependent increase, which was significant for the two higher dosages. Conversely, the serum estrogen concentration and prostatic estrogen receptors were significantly decreased. No significant changes in fecal testosterone excretion, serum testosterone and luteinizing hormone concentrations, and prostatic androgen receptors were observed. Prostate weight was significantly reduced at 5 mg/kg, but we did not observe dose‐dependency. CONCLUSIONS Mepartricin increases fecal excretion of estrogen by binding with it in the intestinal tract, which results in reducing the serum estrogen concentration and number of prostatic estrogen receptors. Prostate 38:17–27, 1999. © 1999 Wiley‐Liss, Inc.