Intestinal absorption, organ distribution, and urinary excretion of the rare sugar D-psicose.
Intestinal absorption, organ distribution, and urinary excretion of the rare sugar D-psicose.
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DOI：
10.2147/dddt.s60247
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发表时间：
2014
期刊：
影响因子：
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通讯作者：
Tokuda M
中科院分区：
文献类型：
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作者：
Tsukamoto I;Hossain A;Yamaguchi F;Hirata Y;Dong Y;Kamitori K;Sui L;Nonaka M;Ueno M;Nishimoto K;Suda H;Morimoto K;Shimonishi T;Saito M;Song T;Konishi R;Tokuda M
本研究的目的是评估肠道吸收、器官分布和尿液对稀有糖D-psicose的消除，D-psicose是一种目前正在研究的d -果糖的3碳立体异构体，已被发现对高血糖和高脂血症有很强的疗效。本研究使用放射性D-psicose进行，它是由放射性D-allose酶促合成的。Wistar大鼠在口服和静脉给药后2小时及单次口服给药（100 mg/kg体重）后7天，在不同时间点测量全血、尿和器官中的浓度。通过静脉注射100 mg/kg体重的14c标记的D-psicose或葡萄糖给C3H小鼠进行放射自显影。口服D-psicose后，D-psicose很容易进入血液。1 h血药浓度最高（48.5±15.6 μg/g）。1小时内排尿率为20%，2小时内排尿率为33%。仅在肝脏中检测到对器官的积聚。静脉给药后血药浓度下降，半衰期为57分钟，1小时内排尿率高达近50%。与口服给药的结果类似，仅在肝脏中检测到对器官的积累。单次口服7天后，其在全身的残留量均小于1%。小鼠放射自显影结果与大鼠相似。肝、肾、膀胱均可见14c标记D-psicose的高信号。有趣的是，在大脑中没有观察到D-psicose的积累。D-psicose口服吸收良好，口服和静脉给药消除迅速，作用时间短。该研究为D-psicose的进一步药物开发提供了有价值的药动学数据。由于研究结果主要基于动物实验，因此有必要开展人体试验来研究其代谢途径，这将为D-psicose的人体摄入和食品应用提供重要指导。
The purpose of this study was to evaluate intestinal absorption, organ distribution, and urinary elimination of the rare sugar D-psicose, a 3-carbon stereoisomer of D-fructose that is currently being investigated and which has been found to be strongly effective against hyperglycemia and hyperlipidemia. This study was performed using radioactive D-psicose, which was synthesized enzymatically from radioactive D-allose. Concentrations in whole blood, urine, and organs were measured at different time points until 2 hours after both oral and intravenous administrations and 7 days after a single oral administration (100 mg/kg body weight) to Wistar rats. Autoradiography was also performed by injecting 100 mg/kg body weight of 14C-labeled D-psicose or glucose intravenously to C3H mice. Following oral administration, D-psicose easily moved to blood. The maximum blood concentration (48.5±15.6 μg/g) was observed at 1 hour. Excretion to urine was 20% within 1 hour and 33% within 2 hours. Accumulation to organs was detected only in the liver. Following intravenous administration, blood concentration was decreased with the half-life=57 minutes, and the excretion to urine was up to almost 50% within 1 hour. Similarly to the results obtained with oral administration, accumulation to organs was detected only in the liver. Seven days after the single-dose oral administration, the remaining amounts in the whole body were less than 1%. Autoradiography of mice showed results similar to those in rats. High signals of 14C-labeled D-psicose were observed in liver, kidney, and bladder. Interestingly, no accumulation of D-psicose was observed in the brain. D-psicose was absorbed well after oral administration and eliminated rapidly after both oral and intravenous administrations, with short duration of action. The study provides valuable pharmacokinetic data for further drug development of D-psicose. Because the findings were mainly based on animal study, it is necessary to implement human trials to study the metabolism pathway, which would give an important guide for human intake and food application of D-psicose.