苦味化合物於活化GLP-1分泌之用途METHOD FOR ENHANCING THE SECRETION OF GLP-1 USING BITTER COMPOUNDS

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

13/855,108

專利證號

US 9,446,053 B2

專利獲證名稱

苦味化合物於活化GLP-1分泌之用途METHOD FOR ENHANCING THE SECRETION OF GLP-1 USING BITTER COMPOUNDS

專利所屬機關 (申請機關)

國立臺灣大學

獲證日期

2016/09/20

技術說明

GLP-1 為 incretins hormone 之一，incretin effect係指在進食後，腸道內分泌細胞感測到某些食物成分或營養素，從而分泌胜肽荷爾蒙 (incretin hormone / incretins，GLP-1 & GIP) 刺激胰島素分泌進而降低血糖的生理現象。缺少 incretins 的分泌與加速其清除並非糖尿病的致病因子，但若能增加其分泌或是抑制其清除速率能夠改善其血糖恆定。於第二型糖尿病患者身上發現 GLP-1 仍能維持促進胰島素分泌（insulinotropic）的特性，因此而研發出GLP-1 analogue或抑制GLP-1被dipeptidyl peptidase IV（DPPIV）分解的藥物，應用於糖尿病的治療。GLP-1 analogue為胜肽藥物，需以注射方式施用，十分不便。近年來，促進GLP-1分泌劑亦成為藥物研發的方向，其單獨使用或與DPPIV抑制劑並用可用來改善第2型糖尿病患之胰島素分泌與血糖調節。 1.本發明透過細胞實驗證實，山苦瓜三萜類化合物及十種已知苦味物質於腸道內分泌細胞株之 GLP-1 分泌試驗中，能促進 GLP-1 之分泌。 2.苦味抑制劑添加後對數種樣品之抑制現象，顯示部分苦味物質可能透過腸內分泌細胞之苦味受器之作用，促進 GLP-1 分泌，具有輔助血糖調控之潛力。 In response to food ingestion, enteroendocrine cells release hormones that can stimulate insulin secretion and thereby reducing blood glucose. This is the incretin effect and two such hormones, i.e. GLP-1 and GIP, have been identified. The insulin secretory response to incretins accounts for at least 50% of the total insulin secreted after oral glucose. GLP-1 has become a molecular target for therapeutics of type 2 diabetes mellitus. Two such strategies have already been in clinical practice to treat type 2 DM, namely, GLP-1 analogs and inhibitors of the enzyme dipeptidylpeptidase IV (DPP IV) that degrades both GLP-1 and GIP. An alternative approach is the identification of GLP-1 secretagogues that have the potential, either alone or in combination with DPP IV inhibitors to enhance circulating levels of bioactive GLP-1 in patients with T2D. In this respect, we have demonstrated quite a few bitter compounds can stimulate GLP-1 secretion in a enteroendocrine cell line STC-1 cells.

備註

本部(收文號1090002409)同意該校109年1月7日校研發字第1090000702號函申請終止維護專利(臺大)

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