Identification of Upregulators of Human ATP-Binding Cassette Transporter A1 via High-Throughput Screening of a Synthetic and Natural Compound Library

Rutaecarpine suppresses atherosclerosis in ApoE−/− mice through upregulating ABCA1 and SR-BI within RCT

“…Human hepatoma HepG2 cells, ABCA1p-LUC HepG2 ( 20 ), CLA1p-LUC HepG2 ( 21 ), and murine peritoneal macrophage cell line RAW264.7 ( 22 ) were maintained by our laboratory. HepG2 cells were grown in MEM medium (Hyclone) supplemented with 10% heat-inactivated FBS (medium A).…”

“…The goal of this study was to identify small-molecular upregulators of ABCA1 and SR-BI/CLA-1 expression from 20,000 natural or synthetic compounds using the highthroughput screening models that we have established ( 20,21 ). After several rounds of screening, we found for the fi rst time that the natural compound rutaecarpine (RUT) upregulated expression of the two target genes (ABCA1 and SR-BI/CLA-1) at the same time without cytotoxicity on the screening cells.…”

“…The mice on the chow diet received carboxymethylcellulose sodium (CMC-Na) as the untreated control group. Mice on the high-fat diet (HFD) (0.15% cholesterol and 20% fat) received CMC-Na as the model group, simvastatin (5 mg/kg), or RUT [10,20, and 40 mg/kg, as RUT (L), RUT (M) and RUT (H), respectively]. RUT and simvastatin were given intragastrically daily.…”

“…domain, LBD) and pBIND-LXR ␤ -LBD] were constructed as previously described ( 35 ). ABCA1, CLA-1 transcriptional activity assay, and pBIND-LXR ␣ /LXR ␤ -LBD/GAL4 chimera reporter assay were performed as previously described using ABCA1p-LUC HepG2 ( 20 ), CLA1p-LUC HepG2 ( 21 ), and HepG2 cells, respectively. And these cells were treated with RUT at the indicated concentrations for 18 h at 37°C.…”

Computational fishing of new DNA methyltransferase inhibitors from natural products

“…(ABCA1), a membrane transporter that directly contributes to high-density lipoprotein (HDL) biogenesis [102].…”