Galle P R, Theilmann L, Raedsch R, Rudolph G, Kommerell B, Stiehl A
Department of Internal Medicine, University of Heidelberg, F.R.G.
Biochim Biophys Acta. 1989 Jun 28;1003(3):250-3. doi: 10.1016/0005-2760(89)90230-0.
Rat primary liver cells were used to study taurine and glycine conjugation and sulfation of lithocholate. After addition of [14C]lithocholate to the tissue culture medium, synthesis and excretion of amidated and/or sulfated products were investigated for up to 24 h. After incubation for 1 h, more than 83% of the labeled bile salt was amidated but not sulfated and between 5 and 11% was sulfated, with more than 80% of the sulfated bile salts being also amidated. After 24 h, the proportion of sulfated lithocholate had increased to about 23% and more than 99% of the lithocholate sulfate was additionally conjugated with glycine or taurine. Both sulfates and non-sulfates were preferably amidated with taurine. We conclude that in primary rat hepatocytes, (1) lithocholate is rapidly and almost completely conjugated with glycine or taurine (amidated), whereas sulfation of lithocholate (and its amidates) proceeds slowly and even after 24 h represents only a small proportion of the total lithocholate metabolites, and (2) sulfated and unsulfated bile salts are both preferably amidated with taurine.
采用大鼠原代肝细胞研究石胆酸的牛磺酸和甘氨酸结合反应以及硫酸化反应。向组织培养基中加入[14C]石胆酸后，对酰胺化和/或硫酸化产物的合成与排泄进行长达24小时的研究。孵育1小时后，超过83%的标记胆汁盐发生酰胺化但未硫酸化，5%至11%发生硫酸化，其中超过80%的硫酸化胆汁盐也进行了酰胺化。24小时后，硫酸化石胆酸的比例增加到约23%，超过99%的硫酸化石胆酸还与甘氨酸或牛磺酸结合。硫酸盐和非硫酸盐都优先与牛磺酸进行酰胺化反应。我们得出结论，在原代大鼠肝细胞中，(1)石胆酸迅速且几乎完全与甘氨酸或牛磺酸结合（酰胺化），而石胆酸（及其酰胺化物）的硫酸化反应进行缓慢，即使在24小时后，硫酸化石胆酸在石胆酸总代谢产物中所占比例仍较小；(2)硫酸化和未硫酸化的胆汁盐都优先与牛磺酸进行酰胺化反应。
