PMID- 29803171
OWN - NLM
STAT- MEDLINE
DCOM- 20181005
LR  - 20181005
IS  - 1950-6007 (Electronic)
IS  - 0753-3322 (Linking)
VI  - 104
DP  - 2018 Aug
TI  - Protective effects of gemigliptin against type II collagen degradation in human 
      chondrocytes.
PG  - 590-594
LID - S0753-3322(18)31243-5 [pii]
LID - 10.1016/j.biopha.2018.04.018 [doi]
AB  - Degradation of components of the extracellular matrix such as type II collagen in 
      articular cartilage induced by matrix metalloproteinases (MMPs) has been 
      considered as a major pathological characteristic of osteoarthritis (OA). 
      Gemigliptin is a potent and a highly selective dipeptidyl peptidase-IV (DPP-IV) 
      inhibitor, which has been clinically used as an oral agent for the treatment of 
      type 2 diabetes. However, the effects of gemigliptin on articular cartilage 
      destruction and the pathogenesis of OA remain unknown. In the current study, we 
      addressed for the first time the inhibitory property of gemigliptin against 
      interleukin-1beta (IL-1beta)-induced degradation of type II collagen in human 
      chondrocytes. Our results demonstrate that gemigliptin treatment inhibited the 
      expression of matrix metalloproteinase 1 (MMP-1), matrix metalloproteinase 3 
      (MMP-3), and matrix metalloproteinase 13 (MMP-13) at both the gene and protein 
      levels. Mechanistically, our results indicate that gemigliptin inhibited 
      activation of the nuclear factor-kappaB (NF-kappaB) signaling pathway by suppressing 
      phosphorylation of IkappaB kinase (IKK)/nuclear factor of kappa light polypeptide 
      gene enhancer in B-cells inhibitor alpha (IkappaBalpha) and p38. Our results implicate that 
      gemigliptin treatment might be a potential therapeutic strategy for 
      chondroprotective therapy.
CI  - Copyright (c) 2018. Published by Elsevier Masson SAS.
FAU - Mohetaer, Momin
AU  - Mohetaer M
AD  - Department of Orthopaedics, First Teaching Hospital of Xinjiang Medical 
      University, Urumqi, Xinjiang 830054, China.
FAU - Li, Guoqing
AU  - Li G
AD  - Department of Orthopaedics, First Teaching Hospital of Xinjiang Medical 
      University, Urumqi, Xinjiang 830054, China.
FAU - Wang, Yang
AU  - Wang Y
AD  - Department of Orthopaedics, First Teaching Hospital of Xinjiang Medical 
      University, Urumqi, Xinjiang 830054, China.
FAU - Cao, Li
AU  - Cao L
AD  - Department of Orthopaedics, First Teaching Hospital of Xinjiang Medical 
      University, Urumqi, Xinjiang 830054, China. Electronic address: 
      flyhigh1978@yeah.net.
LA  - eng
PT  - Journal Article
DEP - 20180525
PL  - France
TA  - Biomed Pharmacother
JT  - Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
JID - 8213295
RN  - 0 (Collagen Type II)
RN  - 0 (Interleukin-1beta)
RN  - 0 (LC15-0444)
RN  - 0 (NF-kappa B)
RN  - 0 (Piperidones)
RN  - 0 (Protective Agents)
RN  - 0 (Pyrimidines)
RN  - 139874-52-5 (NF-KappaB Inhibitor alpha)
RN  - EC 2.7.11.24 (Mitogen-Activated Protein Kinases)
RN  - EC 3.4.24.- (Metalloendopeptidases)
SB  - IM
MH  - Cartilage, Articular/*drug effects/metabolism
MH  - Cells, Cultured
MH  - Chondrocytes/*drug effects/*metabolism
MH  - Collagen Type II/*metabolism
MH  - Humans
MH  - Interleukin-1beta/metabolism
MH  - Metalloendopeptidases/metabolism
MH  - Mitogen-Activated Protein Kinases/metabolism
MH  - NF-KappaB Inhibitor alpha/metabolism
MH  - NF-kappa B/metabolism
MH  - Piperidones/*pharmacology
MH  - Protective Agents/*pharmacology
MH  - Pyrimidines/*pharmacology
MH  - Signal Transduction/drug effects
OTO - NOTNLM
OT  - Gemigliptin
OT  - Matrix metalloproteinases
OT  - Osteoarthritis
OT  - Type II collagen
EDAT- 2018/05/29 06:00
MHDA- 2018/10/06 06:00
CRDT- 2018/05/27 06:00
PHST- 2018/02/24 00:00 [received]
PHST- 2018/04/03 00:00 [revised]
PHST- 2018/04/03 00:00 [accepted]
PHST- 2018/05/29 06:00 [pubmed]
PHST- 2018/10/06 06:00 [medline]
PHST- 2018/05/27 06:00 [entrez]
AID - S0753-3322(18)31243-5 [pii]
AID - 10.1016/j.biopha.2018.04.018 [doi]
PST - ppublish
SO  - Biomed Pharmacother. 2018 Aug;104:590-594. doi: 10.1016/j.biopha.2018.04.018. 
      Epub 2018 May 25.