PMID- 29859525
OWN - NLM
STAT- MEDLINE
DCOM- 20180813
LR  - 20181202
IS  - 0513-4870 (Print)
IS  - 0513-4870 (Linking)
VI  - 51
IP  - 4
DP  - 2016 Apr
TI  - [In vitro effect and mechanistic study of compound E23869 on lipid metabolism].
PG  - 563-72
AB  - This study was designed to identify inducers of ATP-binding cassette transporter 
      A1(ABCA1) and CD36 and lysosomal integral membrane protein-II analogous-1(CLA-1) 
      and to evaluate the in vitro effect of the active compound on lipid metabolism. 
      Among 20 000 compounds screened, E23869 was found as a positive hit using 
      cell-based high throughput screening models. The up-regulating activities of 
      E23869 in ABCA1p-LUC and CLA-1p-LUC Hep G2 cells were 196% and 198%, 
      respectively. The EC(50) values of E23869 in ABCA1p- LUC and CLA-1p-LUC Hep G2 
      cells were 0.25 mumol.L(-1) and 0.66 mumol.L(-1), respectively. E23869 
      significantly upregulated the protein levels of ABCA1, scavenger receptor class B 
      type I(SR-BI)/CLA-1 and ATP-binding cassette transporter G1(ABCG1) in both 
      macrophages RAW264.7 and L02 cells by Western blotting analysis. Foam cell assay 
      showed that E23869 inhibited lipids accumulations in macrophages RAW264.7. 
      Cholesterol efflux assay showed that E23869 induced HDL-mediated cholesterol 
      efflux in macrophages RAW264.7. Moreover, E23869 up-regulated ABCA1, SR-BI/CLA-1 
      and ABCG1 expressions through activation of PPARalpha and PPARgamma. In addition, E23869 
      weakly promoted in vitro differentiation of mouse preadipocytes 3T3-L1. In 
      conclusion, E23869 up-regulated ABCA1, SR-BI/CLA-1 and ABCG1 expressions to 
      promote cholesterol efflux, which is a good leading compound for regulation of 
      lipid metabolism.
FAU - Yang, Shuang-shuang
AU  - Yang SS
FAU - Xu, Yan-ni
AU  - Xu YN
FAU - Liu, Peng
AU  - Liu P
FAU - Wang, Xiao
AU  - Wang X
FAU - Han, Xiao-wan
AU  - Han XW
FAU - Fan, Zhuo-wen
AU  - Fan ZW
FAU - Si, Shu-yi
AU  - Si SY
LA  - chi
PT  - Journal Article
PL  - China
TA  - Yao Xue Xue Bao
JT  - Yao xue xue bao = Acta pharmaceutica Sinica
JID - 21710340R
RN  - 0 (ABCA1 protein, human)
RN  - 0 (ABCA1 protein, mouse)
RN  - 0 (ABCG1 protein, mouse)
RN  - 0 (ATP Binding Cassette Transporter 1)
RN  - 0 (ATP Binding Cassette Transporter, Subfamily G, Member 1)
RN  - 0 (CD36 Antigens)
RN  - 0 (PPAR alpha)
RN  - 0 (PPAR gamma)
RN  - 0 (Scarb1 protein, mouse)
RN  - 0 (Scavenger Receptors, Class B)
RN  - 97C5T2UQ7J (Cholesterol)
SB  - IM
MH  - ATP Binding Cassette Transporter 1/*metabolism
MH  - ATP Binding Cassette Transporter, Subfamily G, Member 1/*metabolism
MH  - Animals
MH  - Biological Transport
MH  - CD36 Antigens
MH  - Cell Line
MH  - Cholesterol/metabolism
MH  - Foam Cells/drug effects
MH  - Hep G2 Cells
MH  - Humans
MH  - Lipid Metabolism/*drug effects
MH  - Macrophages/drug effects
MH  - Mice
MH  - PPAR alpha/metabolism
MH  - PPAR gamma/metabolism
MH  - RAW 264.7 Cells
MH  - Scavenger Receptors, Class B/*metabolism
MH  - Transcriptional Activation
MH  - Up-Regulation
EDAT- 2016/04/01 00:00
MHDA- 2018/08/14 06:00
CRDT- 2018/06/04 06:00
PHST- 2018/06/04 06:00 [entrez]
PHST- 2016/04/01 00:00 [pubmed]
PHST- 2018/08/14 06:00 [medline]
PST - ppublish
SO  - Yao Xue Xue Bao. 2016 Apr;51(4):563-72.