PMID- 31054273
OWN - NLM
STAT- MEDLINE
DCOM- 20191111
LR  - 20191111
IS  - 1879-0712 (Electronic)
IS  - 0014-2999 (Linking)
VI  - 854
DP  - 2019 Jul 5
TI  - G-protein coupled receptor 55 agonists increase insulin secretion through 
      inositol trisphosphate-mediated calcium release in pancreatic beta-cells.
PG  - 372-379
LID - S0014-2999(19)30302-4 [pii]
LID - 10.1016/j.ejphar.2019.04.050 [doi]
AB  - G-protein coupled receptor 55 (GPR55) is an orphan G-protein coupled receptor, 
      which is activated by endocannabinoids and lipid transmitters. Recently, GPR55 
      was shown to play a role in glucose and energy homeostasis, and insulin secretion 
      is essential to maintain glucose homeostasis in the body. In Type 2 Diabetes 
      Mellitus (T2DM), chronic insulin resistance and a progressive decline in beta-cell 
      function result in beta-cell dysfunction, this leads to defect in insulin secretion, 
      which is the key process in the development and progression of T2DM. GPR55 
      agonists were shown to increase insulin secretion, however the underlying 
      mechanisms were not fully understood. Therefore the aim of the present study was 
      to examine the effects of potent GPR55 agonists, O-1602 and abnormal cannabidiol 
      (Abn-CBD), on glucose-induced insulin secretion in a mouse pancreatic beta-cell 
      line, MIN6, and the underlying mechanisms with a focus on intracellular calcium 
      (Ca(2+)). Our results demonstrated that O-1602 and Abn-CBD increased 
      glucose-induced insulin secretion in MIN6 cells, which was abolished by a PLC 
      inhibitor, U73122. Glucose-induced Ca(2+) transients were enhanced by O-1602 and 
      Abn-CBD, and this was significantly reduced by U73122 and inositol trisphosphate 
      (IP(3)) receptor inhibitors, 2-aminoethoxydiphenyl borate (2-APB) and 
      xestospongin C, as well as by Y-27632, a Rho-associated protein kinase (ROCK) 
      inhibitor. Interestingly, O-1602 and Abn-CBD could directly induce intracellular 
      Ca(2+) transients through IP(3)-mediated Ca(2+) release. In conclusion, GPR55 
      agonists increased insulin secretion through calcium mobilisation from 
      IP(3)-sensitive ER stores in beta-cells.
CI  - Copyright (c) 2019 Elsevier B.V. All rights reserved.
FAU - Vong, Chi Teng
AU  - Vong CT
AD  - State Key Laboratory of Quality Research in Chinese Medicine, Institute of 
      Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, 
      Macau.
FAU - Tseng, Hisa Hui Ling
AU  - Tseng HHL
AD  - State Key Laboratory of Quality Research in Chinese Medicine, Institute of 
      Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, 
      Macau.
FAU - Kwan, Yiu Wa
AU  - Kwan YW
AD  - School of Biomedical Sciences, Faculty of Medicine, The Chinese University of 
      Hong Kong, Shatin, N.T., Hong Kong, China.
FAU - Lee, Simon Ming-Yuen
AU  - Lee SM
AD  - State Key Laboratory of Quality Research in Chinese Medicine, Institute of 
      Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, 
      Macau.
FAU - Hoi, Maggie Pui Man
AU  - Hoi MPM
AD  - State Key Laboratory of Quality Research in Chinese Medicine, Institute of 
      Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, 
      Macau. Electronic address: maghoi@um.edu.mo.
LA  - eng
PT  - Journal Article
DEP - 20190501
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (4-(3-3,4-p-menthadien-(1,8)-yl)olivetol)
RN  - 0 (GPR55 protein, mouse)
RN  - 0 (Inositol 1,4,5-Trisphosphate Receptors)
RN  - 0 (Inositol Phosphates)
RN  - 0 (Receptors, Cannabinoid)
RN  - 0 (Resorcinols)
RN  - 0 (inositol trispyrophosphate)
RN  - 19GBJ60SN5 (Cannabidiol)
RN  - 317321-41-8 (O-1602 compound)
RN  - EC 2.7.11.1 (rho-Associated Kinases)
RN  - EC 3.1.4.11 (Phospholipase C beta)
RN  - IY9XDZ35W2 (Glucose)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Animals
MH  - Calcium/*metabolism
MH  - Cannabidiol/analogs & derivatives/pharmacology
MH  - Cell Line, Tumor
MH  - Glucose/pharmacology
MH  - Inositol 1,4,5-Trisphosphate Receptors/metabolism
MH  - Inositol Phosphates/*metabolism
MH  - Insulin Secretion/*drug effects
MH  - Insulin-Secreting Cells/cytology/*drug effects/*metabolism
MH  - Mice
MH  - Phospholipase C beta/metabolism
MH  - Receptors, Cannabinoid/*metabolism
MH  - Resorcinols/pharmacology
MH  - Up-Regulation/drug effects
MH  - rho-Associated Kinases/metabolism
OTO - NOTNLM
OT  - Calcium
OT  - GPR55
OT  - Inositol trisphosphate
OT  - Insulin secretion
OT  - Pancreatic beta-cells
EDAT- 2019/05/06 06:00
MHDA- 2019/11/12 06:00
CRDT- 2019/05/05 06:00
PHST- 2019/01/27 00:00 [received]
PHST- 2019/04/19 00:00 [revised]
PHST- 2019/04/30 00:00 [accepted]
PHST- 2019/05/06 06:00 [pubmed]
PHST- 2019/11/12 06:00 [medline]
PHST- 2019/05/05 06:00 [entrez]
AID - S0014-2999(19)30302-4 [pii]
AID - 10.1016/j.ejphar.2019.04.050 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2019 Jul 5;854:372-379. doi: 10.1016/j.ejphar.2019.04.050. Epub 
      2019 May 1.