PMID- 29808897
OWN - NLM
STAT- MEDLINE
DCOM- 20181009
LR  - 20220408
IS  - 2042-650X (Electronic)
IS  - 2042-6496 (Linking)
VI  - 9
IP  - 6
DP  - 2018 Jun 20
TI  - Comparative efficacy of vanilloids in inhibiting toll-like receptor-4 
      (TLR-4)/myeloid differentiation factor (MD-2) homodimerisation.
PG  - 3344-3350
LID - 10.1039/c8fo00136g [doi]
AB  - Vanilloid (4-hydroxy-3-methoxyphenyl benzenoid) containing foods are reported to 
      possess many biological activities including anti-inflammatory properties. 
      Homodimerisation of the Toll-like receptor-4 (TLR-4)/Myeloid differentiation 
      factor 2 (MD-2) complex results in life-threatening complications in inflammatory 
      disorders. In this study, we report activity of vanilloids in inhibition of 
      TLR-4/MD-2 homodimersization and their molecular interactions with the receptor. 
      The inhibitory activities of vanilloids were assessed in vitro by determining 
      their antagonistic actions of lipopolysaccharide from Escherichia coli (LPSEc) in 
      activation of TLR-4/MD-2 homodimerisation in TLR-4/MD-2/CD-14 transfected HEK-293 
      cells. The in vitro anti-inflammatory activity of vanilloids was also determined 
      using RAW 264.7 cells. All the vanilloids were found to be active in the 
      inhibition of TLR-4/MD-2 homodimersiation and nitric oxide production in RAW 
      264.7 cells. Rigid and flexible molecular docking studies were performed to gain 
      insight into interactions between vanilloids and the binding site of the 
      TLR-4/MD-2 complex.
FAU - Mai, Chun-Wai
AU  - Mai CW
AD  - Department of Pharmaceutical Chemistry, School of Pharmacy, International Medical 
      University (IMU), Bukit Jalil, 57000, Kuala Lumpur, Malaysia. 
      mallikarjunarao@imu.edu.my.
FAU - Kang, Yew Beng
AU  - Kang YB
FAU - Hamzah, Ahmad Sazali
AU  - Hamzah AS
FAU - Pichika, Mallikarjuna Rao
AU  - Pichika MR
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - England
TA  - Food Funct
JT  - Food & function
JID - 101549033
RN  - 0 (Benzaldehydes)
RN  - 0 (LY96 protein, human)
RN  - 0 (Lymphocyte Antigen 96)
RN  - 0 (TLR4 protein, human)
RN  - 0 (Toll-Like Receptor 4)
RN  - CHI530446X (vanillin)
SB  - IM
MH  - Animals
MH  - Benzaldehydes/*pharmacology
MH  - Dimerization
MH  - Humans
MH  - Lymphocyte Antigen 96/*chemistry/immunology
MH  - Macrophages/drug effects/immunology
MH  - Mice
MH  - Protein Binding/drug effects
MH  - Toll-Like Receptor 4/*chemistry/immunology
EDAT- 2018/05/29 06:00
MHDA- 2018/10/10 06:00
CRDT- 2018/05/30 06:00
PHST- 2018/05/29 06:00 [pubmed]
PHST- 2018/10/10 06:00 [medline]
PHST- 2018/05/30 06:00 [entrez]
AID - 10.1039/c8fo00136g [doi]
PST - ppublish
SO  - Food Funct. 2018 Jun 20;9(6):3344-3350. doi: 10.1039/c8fo00136g.