Study on pharmacokinetics of fucoidan and low molecular weight fucoidan from Saccharina japonica after oral administration to mice
Study on pharmacokinetics of fucoidan and low molecular weight fucoidan from Saccharina japonica after oral administration to mice
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糖精中岩藻依聚糖和低分子岩藻依聚糖小鼠口服药动学研究
DOI：
10.1007/s00343-022-2225-8
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发表时间：
2022
影响因子：
1.6
通讯作者：
Quanbin Zhang
中科院分区：
文献类型：
--
作者：
Jiaojiao Tan;Yimin Song;Jing Wang;Ning Wu;Yang Yue;Quanbin Zhang
褐藻，Sacchairna japonica，已经在传统中药中使用了一千多年。口服给药岩藻依聚糖或低分子量岩藻依聚糖（LMWF）从S。豆豉可以改善慢性肾脏疾病的肾功能障碍，抑制糖尿病血管并发症。在许多研究中，发现LMWF比高分子量的岩藻依聚糖硫酸酯更有效。然而，LMWF的药代动力学仍不清楚。比较ICR小鼠口服高分子量（136 kDa）和低分子量（9.5 kDa）岩藻依聚糖硫酸酯的药代动力学。由于岩藻糖是岩藻多糖的主要和代表性单糖，我们通过测定小鼠血清中岩藻糖浓度来评价岩藻多糖和LMWF的药代动力学。岩藻依聚糖和LMWF在口服给药后均被吸收。以60 mg/kg的剂量经口给予小鼠岩藻依聚糖硫酸酯和低分子量海藻酸钠，岩藻依聚糖硫酸酯和低分子量海藻酸钠的最大浓度（Cmax）分别为2.5 h（0.66±0.32 mg/L）和1.5 h（1.01±0.56 mg/L）。LMWF的曲线下面积（AUC 0 −t）似乎比岩藻依聚糖更高，吸收更快。LMWF在单次给药30 mg/kg小鼠中的估计生物利用度为28.3%。此外，经口给药后，发现LMWF广泛扩散至不同组织，肾脏中的浓度最高，为19.93±7.02 µg/g。本研究首先对LMWF的药代动力学进行了研究，以帮助了解LMWF的功能。我们的研究结果揭示了基于LMWF的药物开发的潜力。
The brown seaweed,Sacchairna japonica, has been used in traditional Chinese medicine for over one thousand years. Oral administration of fucoidan or low molecular weight fucoidan (LMWF) fromS. japonicacould ameliorate kidney dysfunction in chronic kidney diseases and inhibit diabetic vascular complications. In many studies, LMWF was found to be more potent than fucoidan with high molecular weight. However, the pharmacokinetics of LMWF still remains unclear. The purpose of the research is to compare the pharmacokinetics of fucoidan with high molecular weight (136 kDa) with that low molecular weight (9.5 kDa) after oral administration to ICR mice. Since fucose is the main and representative monosaccharide of fucoidans, we evaluate the pharmacokinetics of fucoidan and LMWF by determining the fucose concentration in mice serum. Both fucoidan and LMWF were absorbed following oral administration. Fucoidan and LMWF were provided to mice by oral administration with 60 mg/kg and the maximum Concentration (Cmax) was found at 2.5 h (0.66±0.32 mg/L) for Fucoidan and 1.5 h (1.01±0.56 mg/L) for LMWF, respectively. It seems that LMWF had a higher area under the curve (AUC0−t) and was absorbed more quickly than fucoidan. The estimated bioavailability of LMWF was 28.3% in the mice treated with a single dose of 30 mg/kg. In addition, LMWF was found widely spreaded into different tissues following oral administration and the highest concentration was found in kidney at 19.93±7.02 µg/g. In this study, we first studied the pharmacokinetics of LMWF, in order to help to understand the function of LMWF. And our results shed light on the potential of development of drugs based on LMWF.