Zheng Ziming, Tang Wenqi, Lu Weipeng, Mu Xu, Liu Yuxuan, Pan Xianglin, Wang Kaiping, Zhang Yu
Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
Hubei Province Clinical Research Center for Precision Medicine for Critical Illness, Wuhan, China.
Front Vet Sci. 2022 Jun 3;9:889586. doi: 10.3389/fvets.2022.889586. eCollection 2022.
The β-Glucans widely exist in plants and edible fungi, and their diverse bioactivities and good physicochemical properties have been widely reported. In addition, β-glucan intravenous injections (such as lentinan and schizophyllan) have been clinically used as immunomodulators and antitumor polysaccharides. However, the pharmacokinetic studies of β-glucans only stay on the level of plasma concentration and biodistribution , and little is known about their metabolism and degradation , which severely limits the further application of β-glucans in the field of medicine and biomaterials. The aim of this paper is to explore the metabolism and degradation process of lentinan (as a representative of β-glucans) by labeling it with water-soluble fluorescein 5-([4, 6-Dichlorotriazin-2-yl]amino)fluorescein (DTAF). Fluorescently labeled lentinan (FLNT) was intravenously administered to rats at a single dose of 8 mg/kg. The degradation of LNT in blood, liver, kidney, and urine was evaluated by the gel permeation chromatography. Our results showed that although LNT could be degraded in blood, liver, kidney, and urine, there were still some prototypes until excreted in urine due to the incomplete degradation of LNT in each step. To the best of our knowledge, this is the first report to comprehensively study LNT metabolic degradation in rats. These results provide an important reference for further exploration and application of LNT and other β-glucans.
β-葡聚糖广泛存在于植物和可食用真菌中,其多样的生物活性和良好的理化性质已被广泛报道。此外,β-葡聚糖静脉注射剂(如香菇多糖和裂褶菌多糖)已在临床上用作免疫调节剂和抗肿瘤多糖。然而,β-葡聚糖的药代动力学研究仅停留在血浆浓度和生物分布水平,对其代谢和降解了解甚少,这严重限制了β-葡聚糖在医学和生物材料领域的进一步应用。本文的目的是通过用水溶性荧光素5-([4,6-二氯三嗪-2-基]氨基)荧光素(DTAF)标记香菇多糖(作为β-葡聚糖的代表)来探索其代谢和降解过程。将荧光标记的香菇多糖(FLNT)以8mg/kg的单剂量静脉注射给大鼠。通过凝胶渗透色谱法评估LNT在血液、肝脏、肾脏和尿液中的降解情况。我们的结果表明,尽管LNT可在血液、肝脏、肾脏和尿液中降解,但由于LNT在每个步骤中降解不完全,直到尿液排出时仍有一些原型。据我们所知,这是第一份全面研究大鼠体内LNT代谢降解的报告。这些结果为进一步探索和应用LNT及其他β-葡聚糖提供了重要参考。