Bories G F, Perdu-Durand E F, Sutra J F, Tulliez J E
Laboratoire des Xenobioloques, INRA, Toulouse, France.
Drug Metab Dispos. 1991 Jan-Feb;19(1):140-3.
Biochemical evidence is given of alpha-zearalanol (zeranol), zearalanone, and beta-zearalanol (taleranol) glucurono- and sulfoconjugation in the rat and pig. It is based on the use of liver microsomal and cytosolic fractions, incubation with labeled endogenous coupling substrates, i.e. UDP-glucuronic acid and sulfate, and HPLC profiling of the resulting incubates. It is proved that only monoconjugates are produced, while it is suggested that conjugation occurs on the aromatic ring. Whether it is the C-14 or C-16 hydroxyl group that is conjugated remains to be demonstrated. When comparing the metabolic profiles in vitro with those already obtained in pig plasma, it can be concluded that both glucurono- and sulfoconjugates are produced in vivo.
给出了大鼠和猪体内α-玉米赤霉醇（折仑诺）、玉米赤霉酮和β-玉米赤霉醇（他来诺）葡萄糖醛酸化和硫酸化结合的生化证据。这是基于使用肝脏微粒体和胞质部分，与标记的内源性偶联底物（即尿苷二磷酸葡萄糖醛酸和硫酸盐）一起孵育，并对所得孵育物进行高效液相色谱分析。已证明只产生单结合物，同时表明结合发生在芳环上。尚待证实进行结合的是C-14还是C-16羟基。将体外代谢谱与已在猪血浆中获得的代谢谱进行比较时，可以得出结论，葡萄糖醛酸结合物和硫酸结合物在体内均有产生。
