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Open AccessArticle

The Dietary Furocoumarin Imperatorin Increases Plasma GLP-1 Levels in Type 1-Like Diabetic Rats

Department of Childhood Education and Nursery, Chia Nan University of Pharmacy and Science, Rende, Tainan City 71710, Taiwan
Division of Pediatrics, Chi-Mei Medical Center, Yong Kang, Tainan City 71003, Taiwan
Department of Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung City 81201, Taiwan
Department of Psychosomatic Internal Medicine, Kagoshima University Graduate School of Medical and Dental Sciences, Kagoshima 890-8520, Japan
Department of Medical Research, Chi-Mei Medical Center, Yong Kang, Tainan City 71003, Taiwan
Department of Nursing, Tzu Chi University of Science and Technology, Hualien City 97005, Taiwan
Institute of Medical Science, College of Health Science, Chang Jung Christian University, Guei-Ren, Tainan City 71101, Taiwan
Authors to whom correspondence should be addressed.
Nutrients 2017, 9(11), 1192;
Received: 9 September 2017 / Revised: 26 October 2017 / Accepted: 26 October 2017 / Published: 30 October 2017
Imperatorin, a dietary furocoumarin, is found not only in medicinal plants, but also in popular culinary herbs, such as parsley and fennel. Recently, imperatorin has been shown to activate GPR119 in cells. Another GPR, GPR131, also called TGR5 or G-protein-coupled bile acid receptor 1 (GPBAR1), is known to regulate glucose metabolism. Additionally, TGR5 activation increases glucagon-like peptide (GLP-1) secretion to lower blood sugar levels in animals. Therefore, the present study aims to determine whether the effects of imperatorin on GLP-1 secretion are mediated by TGR5. First, we transfected cultured Chinese hamster ovary cells (CHO-K1 cells) with the TGR5 gene. Glucose uptake was confirmed in the transfected cells using a fluorescent indicator. Moreover, NCI-H716 cells, which secrete GLP-1, were used to investigate the changes in calcium concentrations and GLP-1 levels. In addition, streptozotocin (STZ)-induced type 1-like diabetic rats were used to identify the effects of imperatorin in vivo. Imperatorin dose-dependently increased glucose uptake in CHO-K1 cells expressing TGR5. In STZ diabetic rats, similar to the results in NCI-H716 cells, imperatorin induced a marked increase of GLP-1 secretion that was reduced, but not totally abolished, by a dose of triamterene that inhibited TGR5. Moreover, increases in GLP-1 secretion induced by imperatorin and GPR119 activation were shown in NCI-H716 cells. We demonstrated that imperatorin induced GLP-1 secretion via activating TGR5 and GPR119. Therefore, imperatorin shall be considered as a TGR5 and GPR119 agonist. View Full-Text
Keywords: imperatorin; triamterene; GPR119; TGR5; transfection; sitagliptin imperatorin; triamterene; GPR119; TGR5; transfection; sitagliptin
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Wang, L.-Y.; Cheng, K.-C.; Li, Y.; Niu, C.-S.; Cheng, J.-T.; Niu, H.-S. The Dietary Furocoumarin Imperatorin Increases Plasma GLP-1 Levels in Type 1-Like Diabetic Rats. Nutrients 2017, 9, 1192.

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