A Novel Flavonoid C-Glycosides Integrated Tablet for Improved Dissolution, Pancreatic Repair, and Insulin Mediated Glucose Regulation in Type 2 Diabetic Rats
圖文摘要說明
本研究旨在克服黃酮 C-醣苷 (FCGs) 水溶性差、生物利用度低的限制，因此利用傳統抗糖尿病植物決明 (Cassia mimosoides L.) 的富含 FCGs 提取物，開發出優化的 CM F4 藥片製劑；體外分析（對應流程圖上方的溶出度和 HPLC 分析）證實，CM F4 成功提高了 FCGs 的釋放和穩定性，為體內療效奠定基礎；隨後在糖尿病大鼠模型中進行體內藥理研究，結果顯示 CM F4 顯著降低了空腹血糖並改善了葡萄糖耐受性；其作用機制包括恢復胰腺 β 細胞結構（對應流程圖左下方的胰腺組織學）和增加胰島素水平，進而透過調節關鍵碳水化合物代謝酶和上調 PI3K/AKT 和 AMPK 等胰島素信號傳導通路（對應流程圖右下方的葡萄糖代謝）來改善全身代謝；總之，本研究證明 CM F4 是一種新型製劑，能有效增強植物來源 FCGs 的抗糖尿病功效，為 2 型糖尿病管理提供了一個有前景的植物藥學解決方案。
Abstract
Flavonoid C-glycosides (FCGs) are polyphenols with a stable C–C glycosidic bond, known for antidiabetic and antioxidant effects. However, their poor water solubility and low dissolution limit oral bioavailability. To overcome these limitations, a tablet formulation (Cassia mimosoide-formulation batch 4, CM F4) was developed using a FCG-rich ethyl acetate extract of Cassia mimosoides L. (CM-EA), a plant traditionally known for its antidiabetic properties. The optimized formulation improved tablet disintegration, stability, and significantly enhanced FCG release, confirmed by in vitro dissolution and HPLC analysis. In high-fat diet and streptozotocin-induced diabetic rats, CM F4 reduced fasting blood glucose, improved glucose tolerance, restored pancreatic β-cell architecture, and increased insulin levels. It also modulated key carbohydrate-metabolizing enzymes and upregulated insulin signaling proteins, particularly PI3K/AKT and AMPK pathways. This study presents CM F4 as a novel tablet formulation that enhances the dissolution and in vivo antidiabetic efficacy of plant-derived FCGs, offering a promising phytopharmaceutical approach for type 2 diabetes management.
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