Hämäläinen E, Korpela J T, Adlercreutz H
Gut. 1987 Apr;28(4):439-45. doi: 10.1136/gut.28.4.439.
The effect of oxytetracycline (1 g/day for five days) on the enterohepatic recycling of oestrogens and on plasma sex hormone concentrations was assessed in healthy men. Plasma oestrone (E1), oestradiol-17 beta (E2), 4-androstenedione (A), 5 alpha-dihydrotestosterone (5 alpha-DHT), total and free testosterone (T and free T), binding capacity of sex hormone binding globulin, luteinizing hormone, dehydroepiandrosterone-sulphate, urinary total E1, E2, and oestriol (E3), and oestriol-3-glucuronide (E3-3G) and faecal unconjugated and conjugated E1, E2, and E3 were measured by radioimmunoassay (RIA). Treatment with the antibiotic significantly increased the excretion of faecal conjugated oestrogens, which parallelled a decrease in urinary oestrogen excretion, especially of E3. The effect on urinary E3 could be explained almost entirely by the simultaneous decrease of urinary E3-3G concentrations. In urine and faeces the E2/E3 and E1 + E2/E3 ratios increased, probably because of the diminished reductive metabolism of oestrogens in the gut. No significant effects on plasma unconjugated oestrogen concentrations were observed. Moreover, in the present study oxytetracycline had no remarkable effect on plasma total, or free T concentrations, nor on other plasma hormones measured. Our results suggest that enterohepatic recycling and intestinal metabolism of oestrogens may be significant in men. The mechanism of action of antibiotics on oestrogen metabolism probably involves decreased hydrolysis by beta-glucuronidase of oestrogen conjugates by the intestinal contents, diminishing the reabsorption of aglycones of oestrogen conjugates and resulting in faecal loss of the steroids.
在健康男性中评估了土霉素(1克/天,共五天)对雌激素肝肠循环及血浆性激素浓度的影响。采用放射免疫分析法(RIA)测定血浆雌酮(E1)、雌二醇-17β(E2)、4-雄烯二酮(A)、5α-双氢睾酮(5α-DHT)、总睾酮和游离睾酮(T和游离T)、性激素结合球蛋白结合能力、促黄体生成素、硫酸脱氢表雄酮、尿总E1、E2和雌三醇(E3)、雌三醇-3-葡萄糖醛酸苷(E3-3G)以及粪便中未结合和结合的E1、E2和E3。抗生素治疗显著增加了粪便中结合雌激素的排泄,这与尿雌激素排泄减少并行,尤其是E3。对尿E3的影响几乎完全可以由尿E3-3G浓度同时降低来解释。在尿液和粪便中,E2/E3和E1 + E2/E3比值升高,可能是因为肠道中雌激素的还原代谢减少。未观察到对血浆未结合雌激素浓度有显著影响。此外,在本研究中,土霉素对血浆总睾酮或游离T浓度以及所测的其他血浆激素均无显著影响。我们的结果表明,雌激素的肝肠循环和肠道代谢在男性中可能很重要。抗生素对雌激素代谢的作用机制可能涉及肠道内容物中β-葡萄糖醛酸酶对雌激素结合物水解减少,减少雌激素结合物苷元的重吸收,导致类固醇随粪便流失。