GLP-1 secretion is stimulated by 1,10-phenanthroline via colocalized T2R5 signal transduction in human enteroendocrine L cell.
Glucagon-like peptide-1 (GLP-1) hormone is known to regulate blood glucose by an insulinotropic effect and increases proliferation as and also prevents apoptosis of pancreatic β cells. We know that GLP-1 is secreted by nutrients such as fatty acids and sweet compounds but also bitter compounds via stimulation of G-protein coupled receptors (GPCRs) in the gut. Among these, bitter compounds are multiply-contained in phytochemicals or artificial materials and perceived as ligands of various bitter taste receptors. We hypothesized that GLP-1 hormone is secreted through stimulation of a single bitter taste receptor by 1,10-phenanthroline which is known agonist of taste receptor type 2 member 5 (T2R5). To prove this hypothesis, we used the representatively well-known 1,10-phenanthroline as ligand of single receptor and evaluated the existence of T2R5 by double-labeling immunofluorescence and then 1,10-phenanthroline is able to secrete GLP-1 hormone through stimulation of T2R5 in human enteroendocrine cells. Consequently, we verify that GLP-1 hormone is colocalized with T2R5 in the human duodenum and ileum tissue and is secreted by 1,10-phenanthroline via T2R5 signal transduction in differentiated human enteroendocrine L cells.
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
Jiyoung
J
Park
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
Ki-Suk
KS
Kim
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
Kang-Hoon
KH
Kim
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
In-Seung
IS
Lee
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
Hyeon-soo
HS
Jeong
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
Yumi
Y
Kim
College of Korean Medicine, Institute of Korean Medicine, Kyung Hee University, Heogi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: hjjang@khu.ac.kr.
Hyeung-Jin
HJ
Jang
D002460:Cell Line; D004386:Duodenum / Q000187:drug effects / Q000378:metabolism; D019858:Enteroendocrine Cells / Q000187:drug effects* / Q000378:metabolism; D052216:Glucagon-Like Peptide 1 / Q000032:analysis / Q000378:metabolism*; D006801:Humans; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D010618:Phenanthrolines / Q000494:pharmacology*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000032:analysis / Q000378:metabolism*; D000098706:Taste Receptors, Type 2
D010618:Phenanthrolines; D043562:Receptors, G-Protein-Coupled; D000098706:Taste Receptors, Type 2; D052216:Glucagon-Like Peptide 1; C025205:1,10-phenanthroline
1,10-Phenanthroline; Bitter taste receptor; Enteroendocrine cell; T2R5; Taste receptor type 2 member 5