Department of Foods and Nutrition, Kookmin University, Seoul 02707, Korea.
Molecules. 2020 Nov 24;25(23):5503. doi: 10.3390/molecules25235503.
Although a variety of beneficial health effects of natural flavonoids, including chrysin, has been suggested, poor solubility and bioavailability limit their practical use. As a promising delivery system, chrysin-loaded phytosomes (CPs) were prepared using egg phospholipid (EPL) at a 1:3 molar ratio and its antidiabetic effects were assessed in db/db diabetic mice. Male C57BLKS/J-db/db mice were fed a normal diet (control), chrysin diet (100 mg chrysin/kg), CP diet (100 mg chrysin equivalent/kg), metformin diet (200 mg/kg) or EPL diet (vehicle, the same amount of EPL used for CP preparation) for 9 weeks. Administration of CP significantly decreased fasting blood glucose and insulin levels in db/db mice compared with the control. An oral glucose tolerance test and homeostatic model assessment for insulin resistance were significantly improved in the CP group ( < 0.05). CP treatment suppressed gluconeogenesis via downregulation of phosphoenolpyruvate carboxykinase while it promoted glucose uptake in the skeletal muscle and liver of db/db mice ( < 0.05). The CP-mediated improved glucose utilization in the muscle was confirmed by upregulation of glucose transporter type 4, hexokinase2 and peroxisome proliferator-activated receptor γ during treatment ( < 0.05). The CP-induced promotion of GLUT4 plasma translocation was confirmed in the skeletal muscle of db/db mice ( < 0.05). Based on the results, CP showed greater antidiabetic performance compared to the control by ameliorating insulin resistance in db/db mice and phytosome can be used as an effective antidiabetic agent.
尽管天然黄酮类化合物（包括白杨素）具有多种有益的健康作用，但较差的溶解度和生物利用度限制了它们的实际应用。作为一种有前途的递药系统，我们使用 1:3 摩尔比的蛋黄磷脂（EPL）制备了白杨素载体制剂（CPs），并在 db/db 糖尿病小鼠中评估了其抗糖尿病作用。雄性 C57BLKS/J-db/db 小鼠喂食正常饮食（对照）、白杨素饮食（100mg 白杨素/kg）、CP 饮食（100mg 白杨素当量/kg）、二甲双胍饮食（200mg/kg）或 EPL 饮食（载体，与 CP 制备相同量的 EPL）9 周。与对照相比，CP 给药显著降低了 db/db 小鼠的空腹血糖和胰岛素水平。CP 组的口服葡萄糖耐量试验和胰岛素抵抗稳态模型评估显著改善（<0.05）。CP 处理通过下调磷酸烯醇丙酮酸羧激酶来抑制糖异生，同时促进 db/db 小鼠骨骼肌和肝脏中的葡萄糖摄取（<0.05）。CP 治疗期间葡萄糖转运蛋白 4、己糖激酶 2 和过氧化物酶体增殖物激活受体 γ 的上调证实了 CP 介导的肌肉葡萄糖利用改善（<0.05）。在 db/db 小鼠的骨骼肌中证实了 CP 诱导的 GLUT4 血浆易位增加（<0.05）。基于这些结果，CP 通过改善 db/db 小鼠的胰岛素抵抗显示出比对照更好的抗糖尿病作用，并且载体制剂可以用作有效的抗糖尿病药物。
