@article{8f28be49e2db411289c29c7f7fd4d04e,
title = "Search for Natural Compounds That Increase Apolipoprotein A-I Transcription in HepG2 Cells: Specific Attention for BRD4 Inhibitors",
abstract = "Although increasing apolipoprotein A-I (apoA-I) might lower the cardiovascular disease risk, knowledge on natural compounds that elevate apoA-I transcription is limited. Therefore, the aim of this study was to discover natural compounds that increase apoA-I transcription in HepG2 cells. Since BRD4 inhibition is known to elevate apoA-I transcription, we focused on natural BRD4 inhibitors. For this, the literature was screened for compounds that might increase apoA-I and or inhibit BRD4. This resulted in list A, (apoA-I increasers with unknown BRD4 inhibitor capacity), list B (known BRD4 inhibitors that increase apoA-I), and list C (BRD4 inhibitors with unknown effect on apoA-I). These compounds were compared with the compounds in two natural compound databases. This resulted in (1) a common substructure (ethyl-benzene) in 60% of selected BRD4-inhibitors, and (2) four compounds that increased ApoA-I: hesperetin, equilenin, 9(S)-HOTrE, and cymarin. Whether these increases are regulated via BRD4 inhibition and the ethyl-benzene structure inhibits BRD4 requires further study.",
keywords = "apolipoprotein A-I, BET inhibitor, BRD4, high-density lipoprotein, in silico structural similarity search, natural compounds, CHOLESTEROL EFFLUX CAPACITY, HIGH-DENSITY-LIPOPROTEIN, APOA-I, CARDIOVASCULAR-DISEASE, GENE-EXPRESSION, GLUCOSE-UPTAKE, HDL, ATHEROSCLEROSIS, ERIODICTYOL, DISCOVERY",
author = "{van der Krieken}, {Sophie E.} and {van-der Pijl}, {Pieter C.} and Yuguang Lin and Popeijus, {Herman E.} and Mensink, {Ronald P.} and Jogchum Plat",
note = "Funding Information: We would like to thank M. Konings, M. Beckers and J. Tayyeb for their contribution to cell culture experiments. This research was supported by the Dutch Technology Foundation STW, which is part of the Netherlands Organisation for Scientific Research (NWO), and which is partly funded by the Ministry of Economic Affairs. Contract grant number: 11349. All authors (S.v.d.K., P.v.d.P., Y.L., H.P., R.M., J.P.) substantially contributed to conception and design, acquisition of data, or analysis and interpretation of data. All authors substantially contributed to drafting the article or revising it critically for important intellectual content. All authors substantially contributed to final approval of the version to be published. The authors declare that they have no conflict of interest. Funding Information: We would like to thank M. Konings, M. Beckers and J. Tayyeb for their contribution to cell culture experiments. This research was supported by the Dutch Technology Foundation STW, which is part of the Netherlands Organisation for Scientific Research (NWO), and which is partly funded by the Ministry of Economic Affairs. Contract grant number: 11349. Publisher Copyright: {\textcopyright} 2019 The Authors. Lipids published by Wiley Periodicals, Inc. on behalf of American Oil Chemists' Society",
year = "2019",
month = dec,
day = "8",
doi = "10.1002/lipd.12204",
language = "English",
volume = "54",
pages = "687--695",
journal = "Lipids",
issn = "0024-4201",
publisher = "Wiley",
number = "11-12",
}