調節血糖中藥複方產品之開發與評估

本研究使用五味子 (Schizandra chinensis Baill.)、黃連 (Coptis chinensis)、番石榴葉 (Psidium guajava L. leaves) 與桑葉 (Morus alba L. leaves) 做為全新的調節血糖中藥複方，首先根據其抑制α-glucosidase能力、抑制DPP-4能力與抑制AGE形成能力 (in vitro) 並配合反應區面法 (response surface methodology, RSM) 尋找其較適配方，接著以動物實驗進一步確認該較適化中藥複方之調節血糖效果。反應曲面法結果顯示較適的調節血糖中藥複方之配方為五味子 (3000 μg/mL)、黃連(80 μg/mL)、番石榴葉 (374.56 μg/mL) 與桑葉 (480 μg/mL)。動物實驗結果則顯示以高熱量飼料餵食小鼠六週可成功誘導成為胰島素阻抗小鼠，而給予調節血糖中藥複方後，可顯著降低其任食血糖值，且在胰島素阻抗性試驗中，調節血糖中藥複方也可顯著降低血糖，以上結果指出此中藥複方調節血糖機制可能是因為其可改善胰島素阻抗性。高劑量中藥複方組的血清中果糖胺含量顯著低於高熱量對照組與正常對照組，也顯示出調節血糖中藥複方可改善中長期血糖值與降低糖尿病併發症發生的風險。此外在動物實驗中我們也發現此中藥複方並不會對於小鼠肝臟與胰臟造成傷害，也不會對於小鼠血漿中的脂質與脂蛋白含量有所影響。Berberine與1-deoxynojirimycin為可能的活性成分，其在中藥複方中的含量分別為4.7 ± 0.4與77.1 ± 1.1 μg/mL，此兩化合物的含量在未來可以當作大量生產時的品管指標。

關鍵字

五味子；黃連；番石榴；桑葉；調節血糖功效； α-glucosidase抑制活性； DPP-4抑制活性； AGE抑制活性；中藥

並列摘要

An anti-diabetic TCM formula consisting of Schizandra chinensis Baill. (SC), Coptis chinensis (CC), Psidium guajava L. leaves (PG) and Morus alba L. leaves (MA) was developed based on its α-glucosidase, DPP-4 and AGE inhibitory activities in vitro using response surface methodology (RSM). Then, the in vivo study was carried out to confirm the anti-diabetic function of the formula. RSM results showed that the optimum anti-diabetic TCM formula is the combination of SC (3000 μg/mL), CC (80 μg/mL), PG (374.56 μg/mL) and MA (480 μg/mL). For in vivo study, insulin resistant mice were induced by high-fat/high-sucrose (HF/HS) feeding for 6 weeks. Administration of the developed formula significantly decreased non-fasting blood glucose in the HF/HS diet mice. Moreover, the formula decreased blood glucose levels in the insulin tolerance test. These results indicated that the anti-diabetic mechanism of the formula might be due to decreased insulin resistance. The serum fructosamine level in high dose group was significantly lower than HF/HS and normal control groups, indicating that the formula could improve middle term glucose levels and reduce risks for complications. In addition, the formula had no adverse effects on liver as well as kidney and it did not change plasma lipid profile parameters. The contents of berberine and 1-deoxynojirimycin in the formula were 4.7 ± 0.4 and 77.1 ± 1.1 μg/mL, respectively. These two compounds can be used as indicators for quality control during production.

並列關鍵字

Schizandra chinensis Baill. ； Coptis chinensis ； Psidium guajava L. ； Morus alba L. ； anti-diabetic effect ； α-glucosidase inhibitory activity ； DPP-4 inhibitory activity ； AGE inhibitory activity ； traditional Chinese medicine