棉酚(gossypol)又称棉籽醇,是一种天然存在于锦葵科的黄色酚类化合物,化学名为2,2′-双-8-甲酸基1,6,7-三羟基-5-异丙基-3-甲基萘,相对分子质量518(分子式:C_(30)H_(30)O_8),它是以1,1′,3,3′取代的2,2′联萘为骨架的化合物,棉酚结构中连接两个萘环的化学键不能自由旋转,具有旋光性。人口服棉酚后胃肠道吸收缓慢,主要经小肠与胃上皮吸收,大部份分泌至胆汁,有明显的肝肠循环。各脏器中以肝脏中的药物浓度最高,其他依次为脾、心脏、肾、肺、肌肉和脂肪组织、睾丸、脑等,存在血脑屏障。主要在肝脏中代谢,并从胆汁排出,主要排泄途径为粪便,约占总排泄率的83.5%,呼气排除占11.73%,尿排泄只占2.51%。人单剂量口服(±)棉酚(20 mg)后的血药浓度达峰时间为4～6h,平均峰浓度为(764.9±326.5)ng·ml~(-1)。可用血管外给药二室模型拟合药时曲线,伴有1.6 h的滞后时间。AUC(5.7～19.3)mg·h·L~(-1),平均值为13.95 mg·h·L~(-1)。终末半衰期 Gossypol, also known as cottonseed alcohol, is a yellow phenolic compound naturally found in the Malvaceae family with chemical name 2,2’-bis-8-formyl 1,6,7-trihydroxy-5- Isopropyl-3-methylnaphthalene, relative molecular mass 518 (molecular formula: C_ (30) H_ (30) O_8) Of the compounds, gossypol structure in the connection of two naphthalene ring chemical bond can not rotate freely, with optical activity. Gastrointestinal absorption of gossypol in humans slowly, mainly absorbed by the small intestine and the stomach epithelium, most of the secretion to the bile, there are obvious enterohepatic circulation. In each organ, the concentration of the drug in the liver is the highest, followed by the spleen, heart, kidney, lung, muscle and adipose tissue, testis, brain, and the like. Mainly in the liver metabolism and excretion from the bile, the main excretion route for excretion, accounting for 83.5% of the total excretion rate, exhaled 11.73% excluded, urinary excretion accounted for only 2.51%. The peak plasma concentration of human oral (±) gossypol (20 mg) was 4 ~ 6h with the average peak concentration of (764.9 ± 326.5) ng · ml ~ (-1). A two-compartment model of extravascular administration can be used to fit the pharmacokinetic profile with a lag time of 1.6 h. AUC (5.7-19.3) mg · h · L -1, with an average value of 13.95 mg · h · L -1. Terminal half-life