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Induction of Atherosclerotic Plaques Through Activation of Mineralocorticoid Receptors in Apolipoprotein E-deficient Mice
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[The in vitro anti-atherosclerotic activity of compound E0869]

Xiao Wang, Chang Liu, Peng Liu

    Yao Xue Xue Bao = Acta Pharmaceutica Sinica
    |July 31, 2015
    PubMed

    Insights

    Researchers identified E0869 as a compound that up-regulates ATP-binding cassette transporter A1 (ABCA1) and scavenger receptor class B type I (SR-BI/CLA-1). This discovery offers a potential new strategy for treating atherosclerosis by enhancing reverse cholesterol transport.

    Area of Science:

    • Biochemistry
    • Molecular Biology
    • Pharmacology

    Background:

    • ATP-binding cassette transporter A1 (ABCA1) and scavenger receptor class B type I (SR-BI/CLA-1) are crucial for reverse cholesterol transport (RCT).
    • Elevated expression of ABCA1 and SR-BI/CLA-1 is linked to reduced atherosclerosis risk.

    Purpose of the Study:

    • To identify novel up-regulators of ABCA1 and CLA-1 for potential atherosclerosis treatment.
    • Utilized cell-based high-throughput screening models to discover these compounds.

    Main Methods:

    • Screened 20,000 compounds using high-throughput screening.
    • Validated hits using luciferase reporter assays (ABCA1-LUC and bCA-l1-LUC HepG2 cells).
    • Assessed mRNA and protein level changes via Real-Time Quantitative PCR and Western blotting; evaluated lipid accumulation and cholesterol efflux in macrophages.

    Main Results:

    • E0869 was identified as a positive hit, up-regulating ABCA1 and CLA-1 activity by 160% and 175% respectively.
    • E0869 increased mRNA and protein levels of ABCA1, SR-BI/CLA-1, and ABCGJ1 in HepG2 and RAW264.7 cells.
    • E0869 inhibited lipid accumulation and promoted HDL-mediated cholesterol efflux in macrophages.

    Conclusions:

    • E0869 effectively up-regulates ABCA1 and CLA-1 activity.
    • E0869 demonstrates significant anti-atherosclerotic activity in vitro by modulating cholesterol homeostasis.

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