Sulphation of resveratrol, a natural product present in grapes and wine, in the human liver and duodenum
Sulphation of resveratrol, a natural product present in grapes and wine, in the human liver and duodenum
复制标题
DOI：
10.1080/004982500406435
复制
发表时间：
2000-06-01
期刊：
影响因子：
1.8
通讯作者：
Pacifici, GM
中科院分区：
文献类型：
--
作者：
De Santi, C;Pietrabissa, A;Pacifici, GM
1.白藜芦醇是一种存在于葡萄和葡萄酒中的多酚化合物，具有抗癌和保护心血管系统的作用。它存在于饮食中，肝脏和十二指肠硫酸化可能限制该化合物的生物利用度。目的是研究白藜芦醇在人体肝脏和肾脏中的硫酸化作用.建立了白藜芦醇硫酸化反应的放射性分析方法。它采用3 '-磷酸腺苷-5'-磷酸硫酸盐-[S-35]作为硫酸盐供体，白藜芦醇硫酸化速率（平均值+/- SD，pmol/min/mg胞浆蛋白）为90+/-21（肝脏，n = 10）和74+/-60（十二指肠，n = 10，P = 0.082）.白藜芦醇磺基转移酶遵循米氏动力学和K-m，（平均值+/-SD; μ M）为0.63=/-0.03（肝脏，n = 5）和0.50+/-0.26（十二指肠，n = 5，p = 0.39）和V-max（平均值+/-SD，pmol/min/mg细胞溶质蛋白）分别为125+/-31（肝脏，n = 5）和129+85（十二指肠，n = 5，p = 0.62）。类黄酮槲皮素、甲芬那酸和水杨酸（两种常用的非甾体抗炎药）可抑制白藜芦醇硫酸化。白藜芦醇硫酸化对槲皮素的IC 50为12+/-2 pM（肝脏）和15+/-2 pM（十二指肠），对甲芬那酸的IC 50为24+/-3 nM（肝脏）和11+/-0.6 nM（十二指肠），对水杨酸的IC 50为53+/-9 mu M（肝脏）和66+/-4 mu M（十二指肠）。槲皮素是一种存在于葡萄酒、水果和蔬菜中的类黄酮，它能有效地抑制白藜芦醇的硫酸化，这表明饮食中存在的化合物可能会抑制白藜芦醇的硫酸化，从而提高其生物利用度。
1. Resveratrol, a polyphenolic compound present in grapes and wine, has beneficial effects against cancer and protective effects on the cardiovascular system. It is present in the diet, and the hepatic and duodenal sulphation might limit the bioavailability of this compound. The aim was to study the sulphation of resveratrol in the human liver and duodenum.2. A simple and reproducible radiometric assay for resveratrol sulphation was developed. It employed 3'-phosphoadenosine-5'-phosphosulphate-[S-35] as the sulphate donor and the rates of resveratrol sulphation (mean +/- SD, pmol/min/mg cytosolic protein) were 90+/-21 (liver, n = 10) and 74+/-60 (duodenum, n = 10, P = 0.082).3. Resveratrol sulphotransferase followed Michaelis-Menten kinetics and K-m, (mean+/-SD; mu M) was 0.63=/-0.03 (liver, n = 5) and 0.50+/-0.26 (duodenum, n = 5, p = 0.39) and V-max (mean+/-SD, pmol/min/mg cytosolic protein) were 125+/-31 (liver, n = 5) and 129+85 (duodenum, n = 5, p = 0.62).4. Resveratrol sulphation was inhibited by the flavonoid quercetin, by mefenamic acid and salicylic acid, two commonly used non-steroidal anti-inflammatory drugs. IC50 of resveratrol sulphation for quercetin was 12+/-2 pM (liver) and 15+/-2 pM (duodenum), those for mefenamic acid were 24+/-3 nM (liver) and 11+/-0.6 nM (duodenum), and those for salicylic acid were 53+/-9 mu M (liver) and 66+/-4 mu M (duodenum).5. The potent inhibition of resveratrol sulphation by quercetin, a flavonoid present in wine, fruits and vegetables, suggests that compounds present in the diet may inhibit the sulphation of resveratrol, thus improving its bioavailability.