Matches in SemOpenAlex for { <https://semopenalex.org/work/W4313891684> ?p ?o ?g. }
- W4313891684 endingPage "1290" @default.
- W4313891684 startingPage "1290" @default.
- W4313891684 abstract "The nuclear receptors—liver X receptors (LXR α and β) are potential therapeutic targets in cardiovascular and neurodegenerative diseases because of their key role in the regulation of lipid homeostasis and inflammatory processes. Specific oxy(phyto)sterols differentially modulate the transcriptional activity of LXRs providing opportunities to develop compounds with improved therapeutic characteristics. We isolated oxyphytosterols from Sargassum fusiforme and synthesized sidechain oxidized sterol derivatives. Five 24-oxidized sterols demonstrated a high potency for LXRα/β activation in luciferase reporter assays and induction of LXR-target genes APOE, ABCA1 and ABCG1 involved in cellular cholesterol turnover in cultured cells: methyl 3β-hydroxychol-5-en-24-oate (S1), methyl (3β)-3-aldehydeoxychol-5-en-24-oate (S2), 24-ketocholesterol (S6), (3β,22E)-3-hydroxycholesta-5,22-dien-24-one (N10) and fucosterol-24,28 epoxide (N12). These compounds induced SREBF1 but not SREBP1c-mediated lipogenic genes such as SCD1, ACACA and FASN in HepG2 cells or astrocytoma cells. Moreover, S2 and S6 enhanced cholesterol efflux from HepG2 cells. All five oxysterols induced production of the endogenous LXR agonists 24(S)-hydroxycholesterol by upregulating the CYP46A1, encoding the enzyme converting cholesterol into 24(S)-hydroxycholesterol; S1 and S6 may also act via the upregulation of desmosterol production. Thus, we identified five novel LXR-activating 24-oxidized sterols with a potential for therapeutic applications in neurodegenerative and cardiovascular diseases." @default.
- W4313891684 created "2023-01-10" @default.
- W4313891684 creator A5016852056 @default.
- W4313891684 creator A5019407946 @default.
- W4313891684 creator A5023547046 @default.
- W4313891684 creator A5026769131 @default.
- W4313891684 creator A5032174537 @default.
- W4313891684 creator A5033340316 @default.
- W4313891684 creator A5038817068 @default.
- W4313891684 creator A5041911790 @default.
- W4313891684 creator A5044420311 @default.
- W4313891684 creator A5045683286 @default.
- W4313891684 creator A5050153201 @default.
- W4313891684 creator A5051568733 @default.
- W4313891684 creator A5054300273 @default.
- W4313891684 creator A5061307026 @default.
- W4313891684 creator A5068012448 @default.
- W4313891684 creator A5071412244 @default.
- W4313891684 creator A5081302685 @default.
- W4313891684 creator A5087385740 @default.
- W4313891684 date "2023-01-09" @default.
- W4313891684 modified "2023-10-14" @default.
- W4313891684 title "Identification of Side Chain Oxidized Sterols as Novel Liver X Receptor Agonists with Therapeutic Potential in the Treatment of Cardiovascular and Neurodegenerative Diseases" @default.
- W4313891684 cites W1556918753 @default.
- W4313891684 cites W1863223166 @default.
- W4313891684 cites W1910673291 @default.
- W4313891684 cites W1967286688 @default.
- W4313891684 cites W1967938147 @default.
- W4313891684 cites W1975478041 @default.
- W4313891684 cites W1977936595 @default.
- W4313891684 cites W1979983109 @default.
- W4313891684 cites W1988437641 @default.
- W4313891684 cites W1990840172 @default.
- W4313891684 cites W1994554610 @default.
- W4313891684 cites W1996168740 @default.
- W4313891684 cites W2002455454 @default.
- W4313891684 cites W2008811967 @default.
- W4313891684 cites W2011945569 @default.
- W4313891684 cites W2020988004 @default.
- W4313891684 cites W2024851295 @default.
- W4313891684 cites W2029354866 @default.
- W4313891684 cites W2032156966 @default.
- W4313891684 cites W2042851429 @default.
- W4313891684 cites W2043174118 @default.
- W4313891684 cites W2049639031 @default.
- W4313891684 cites W2052606483 @default.
- W4313891684 cites W2053158987 @default.
- W4313891684 cites W2057365200 @default.
- W4313891684 cites W2058205407 @default.
- W4313891684 cites W2058292520 @default.
- W4313891684 cites W2058765765 @default.
- W4313891684 cites W2060225582 @default.
- W4313891684 cites W2076855772 @default.
- W4313891684 cites W2077302895 @default.
- W4313891684 cites W2078976507 @default.
- W4313891684 cites W2085807394 @default.
- W4313891684 cites W2088436733 @default.
- W4313891684 cites W2094900070 @default.
- W4313891684 cites W2101284986 @default.
- W4313891684 cites W2105216461 @default.
- W4313891684 cites W2111981713 @default.
- W4313891684 cites W2112632255 @default.
- W4313891684 cites W2118475205 @default.
- W4313891684 cites W2118633678 @default.
- W4313891684 cites W2119338638 @default.
- W4313891684 cites W2121609761 @default.
- W4313891684 cites W2123652234 @default.
- W4313891684 cites W2130855478 @default.
- W4313891684 cites W2133276659 @default.
- W4313891684 cites W2134443036 @default.
- W4313891684 cites W2140869639 @default.
- W4313891684 cites W2140911607 @default.
- W4313891684 cites W2150111302 @default.
- W4313891684 cites W2155858151 @default.
- W4313891684 cites W2162406652 @default.
- W4313891684 cites W2171705910 @default.
- W4313891684 cites W2332865962 @default.
- W4313891684 cites W2518932391 @default.
- W4313891684 cites W2550922779 @default.
- W4313891684 cites W2559956261 @default.
- W4313891684 cites W2735562440 @default.
- W4313891684 cites W2777727712 @default.
- W4313891684 cites W2782808534 @default.
- W4313891684 cites W2790674462 @default.
- W4313891684 cites W2791856739 @default.
- W4313891684 cites W2792961077 @default.
- W4313891684 cites W2797040186 @default.
- W4313891684 cites W2808548053 @default.
- W4313891684 cites W2914222102 @default.
- W4313891684 cites W2921655682 @default.
- W4313891684 cites W2923634234 @default.
- W4313891684 cites W2953849385 @default.
- W4313891684 cites W2964710007 @default.
- W4313891684 cites W2965145194 @default.
- W4313891684 cites W2996512908 @default.
- W4313891684 cites W3111196826 @default.
- W4313891684 cites W3122109881 @default.
- W4313891684 cites W3135121064 @default.