Stiehl A, Ast E, Czygan P, Fröhling W, Raedsch R, Kommerell B
Gastroenterology. 1978 Mar;74(3):572-7.
In 5 patients with cirrhosis of the liver sulfated and nonsulfated [14C]cholic acid and [14C]chenodeoxycholic acid were administered intravenously and the specific activity curves were determined. Specific activities declined exponentially and pool sizes, synthesis rates, and turnover rates of bile acids were calculated on the basis of a one-pool system. The biological half-life of cholic acid was 4.3 +/- 1.6 days (mean +/- SEM) and of chenodeoxycholic acid was 2.8 +/- 1.2 days. The half-life of cholic acid sulfate was 0.7 +/- 0.5 day and of chenodeoxycholic acid sulfate was 0.8 +/- 0.5 day. The pool size of cholic acid was 513 +/- 103 mg, of chenodeoxycholic acid, 477 +/- 77 mg, of cholic acid sulfate, 4.7 +/- 1.0 mg, and of chenodeoxycholic acid sulfate, 38.7 +/- 4.0 mg. The daily synthesis of cholic acid was 90 +/- 14 mg, of chenodeoxycholic acid, 118 +/- 6 mg, of cholic acid sulfate, 7.2 +/- 2.1 mg, and of chenodeoxycholic acid sulfate was 32.6 +/- 3.2 mg. The data indicate that sulfate esters of bile acids are significantly more rapidly excreted than are unsulfated bile acids. More than one-fourth of the chenodeoxycholic acid but less than one-tenth of the cholic acid formed was sulfated. The preferential sulfation of chenodeoxycholic acid is responsible for the more rapid turnover of chenodeoxycholic acid in comparison to cholic acid. Sulfation enhances the excretion and thereby prevents the accumulation of hepatotoxic concentrations of chenodeoxycholic acid in patients with cirrhosis of the liver.
对5例肝硬化患者静脉注射硫酸化和非硫酸化的[14C]胆酸及[14C]鹅去氧胆酸，并测定其比活度曲线。比活度呈指数下降，并根据单池系统计算胆汁酸的池大小、合成率和周转率。胆酸的生物半衰期为4.3±1.6天（均值±标准误），鹅去氧胆酸的生物半衰期为2.8±1.2天。硫酸胆酸的半衰期为0.7±0.5天，硫酸鹅去氧胆酸的半衰期为0.8±0.5天。胆酸的池大小为513±103mg，鹅去氧胆酸为477±77mg，硫酸胆酸为4.7±1.0mg，硫酸鹅去氧胆酸为38.7±4.0mg。胆酸的每日合成量为90±14mg，鹅去氧胆酸为118±6mg，硫酸胆酸为7.2±2.1mg，硫酸鹅去氧胆酸为32.6±3.2mg。数据表明，胆汁酸的硫酸酯排泄速度明显比未硫酸化的胆汁酸快。形成的鹅去氧胆酸中有超过四分之一被硫酸化，但胆酸被硫酸化的比例不到十分之一。鹅去氧胆酸的优先硫酸化导致其周转率比胆酸更快。硫酸化增强了排泄，从而防止肝硬化患者体内鹅去氧胆酸的肝毒性浓度积累。
