用於活化PPARγ表現或降低血糖之香椿萃取物Use of toona sinensis extract for preparing compositions for activating expression of PPARγ

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

102109874

專利證號

I 516260

專利獲證名稱

用於活化PPARγ表現或降低血糖之香椿萃取物Use of toona sinensis extract for preparing compositions for activating expression of PPARγ

專利所屬機關 (申請機關)

國立成功大學

獲證日期

2016/01/11

技術說明

Thiazolidinedione ( TZD )類藥物可活化過氧化小體增生活化受體 (peroxisome proliferator activated receptor gamma, PPARγ)以增加胰島素敏感性來降低血糖。香椿 ( Toona sinesis Roem ) 具有調節血糖的功效，但其降血糖作用與PPARγ基因表現與活化的關聯則未明。首先以PPARγ-LBD ( ligand binding domain ) luciferase assay篩選不同醇水比例的香椿葉 ( Toona sinesis leaves, TSL ) 萃取物 ( TSL-E1 ~ TSL-E6) 活化PPARγ基因的能力；再以3T3-L1脂肪前驅細胞模式分析香椿萃取物對細胞內之脂肪形成以及對PPARγ蛋白質表現的影響。由細胞實驗的結果，篩選出最佳活性效果的萃取物，並利用高脂飼料 ( High fat diet, HFD; 54 % energy by fat ) 誘發的C57BL/6高血糖小鼠模式，連續八週餵食不同劑量之香椿萃取物與pioglitazone ( PIO )，觀察萃取物調節血糖、血脂之效果，及對脂肪組織 PPARγ 基因表現的影響。同時，運用高效液能層析儀 ( HPLC ) 及液相層析質譜儀 (LC-MS ) 分離萃取物中主要成分，並進一步以脂肪前驅細胞偵測 PPARγ 基因表現。總結實驗結果發現，多種香椿萃取物均可活化PPARγ基因，但以TSL-E6的作用最佳。細胞與動物模式的結果顯示，TSL-E6可增加PPARγ mRNA與蛋白質表現，減少脂肪細胞之油滴堆積，具有調節動物血糖的效果。推論TSL-E6的成份可能與PPARγ ligand的作用相似，可參與調節PPARγ基因表現與血糖的作用，未來可進一步研究TSL-E6調節PPARγ表現之分子機制與應用價值。 Different Toona sinensis Roem leaves (TSL) extracts prepared by series of ethanol/water were used to examine their PPARγ activities using PPARγ-LBD（ligand binding doman）luciferase expression system in HepG2 cell line. Meanwhile, adigogenesis, PPARγ expression, and hypoglycemic effect of TSL extracts were also investigated using both 3T3-L1 adipocytes cell and high fat diet (HFD, 54 % energy by fat) induced hyperglycemic C57BL/6 mice model. The active compounds in TSL extracts were identified using HPLC and LC-MS analysis, and further confirmed by PPARγ expression in 3T3-L1 cells for PPARγ activation. The PPARγ-LBD luciferase assay indicated that TSL-E6 was the candidates of PPARγ ligands. Moreover, the analysis of Oil red O stain showed that the treatment of TSL-E6 suppressed the lipid accumulation in adipocytes. The PPARγ gene and protein expressions, and its downstream aP2 gene expression were elevated in the adipose tissue of hyperglycemic mice with TSL-E6 treatment for 8 weeks.

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