Gross C J, Henderson L M
Biochim Biophys Acta. 1984 May 16;772(2):209-19. doi: 10.1016/0005-2736(84)90046-4.
The process by which L- and D-carnitine are absorbed was investigated using the live rat and the isolated vascularly perfused intestine. A lumenal dose of 2-6 nmol in the perfused intestine resulted in less than 5% transport of either isomer to the perfusate in 30 min. The L-isomer was taken up by the intestinal tissue about twice as rapidly as the D-isomer by both the perfused intestine (52.8% and 21.6%, respectively) and the live animal (80% and 50%, respectively) in 30 min. After 1 h 90% of the L-carnitine had accumulated in the intestinal tissue and was released to the circulation over the next several hours. Accumulation of D-carnitine reached a maximum of 80% in 2 h and release to the circulations was similar to that of L-carnitine. Uptake of both L-[14C]carnitine and acetyl-L-[14C]carnitine was more rapid in the upper jejunal segment than in other portions of the small intestine. Acetylation occurred in all segments, resulting in nearly 50% conversion to this derivative in 5 min. Increasing the dose of L-carnitine reduced the percent acetylation. The uptake of both isomers was a saturable process and high concentrations of D-carnitine, acetyl-L-carnitine and trimethylaminobutyrate inhibited L-carnitine uptake. In the live animal after 5 h, the distribution of isotope from L-[14C]carnitine and D-[3H]carnitine differed primarily in the muscle where 29.5% of the L-carnitine and 5.3% of the D-carnitine was found and in the urine where 2.9% of the L-carnitine and 7.1% of the D-carnitine was found. The renal threshold for L-carnitine was 80 microM and for D-carnitine 30 microM, in the isolated perfused kidney. Approx. 40% of the L-carnitine but none of the D-carnitine excreted in the urine was acetylated. L-Carnitine and D-carnitine competed for tubular reabsorption.
利用活体大鼠和离体血管灌注肠,研究了左旋肉碱和右旋肉碱的吸收过程。在灌注肠中给予2 - 6纳摩尔的肠腔剂量,30分钟内两种异构体向灌注液的转运均不到5%。在30分钟内,左旋异构体被灌注肠(分别为52.8%和21.6%)和活体动物(分别为80%和50%)吸收进入肠组织的速度约为右旋异构体的两倍。1小时后,90%的左旋肉碱在肠组织中积累,并在接下来的几个小时内释放到循环中。右旋肉碱的积累在2小时时达到最大值80%,向循环中的释放与左旋肉碱相似。左旋[14C]肉碱和乙酰左旋[14C]肉碱在上段空肠的摄取比小肠其他部位更快。乙酰化发生在所有节段,5分钟内几乎有50%转化为该衍生物。增加左旋肉碱的剂量会降低乙酰化百分比。两种异构体的摄取都是一个可饱和的过程,高浓度的右旋肉碱、乙酰左旋肉碱和三甲氨基丁酸会抑制左旋肉碱的摄取。在活体动物5小时后,左旋[14C]肉碱和右旋[3H]肉碱的同位素分布主要在肌肉和尿液中有所不同,在肌肉中发现29.5%的左旋肉碱和5.3%的右旋肉碱,在尿液中发现2.9%的左旋肉碱和7.1%的右旋肉碱。在离体灌注肾中,左旋肉碱的肾阈值为80微摩尔,右旋肉碱为30微摩尔。尿液中排泄的左旋肉碱约40%被乙酰化,而右旋肉碱没有。左旋肉碱和右旋肉碱竞争肾小管重吸收。