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Molecules 2016, 21(1), 55;

Silymarin Constituents Enhance ABCA1 Expression in THP-1 Macrophages

Department of Pharmacognosy, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria
Department of Chemistry & Biochemistry, University of North Carolina at Greensboro, Greensboro, NC 27402, USA
Author to whom correspondence should be addressed.
Academic Editor: Milen I. Georgiev
Received: 30 November 2015 / Revised: 27 December 2015 / Accepted: 29 December 2015 / Published: 31 December 2015
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Silymarin is a hepatoprotective mixture of flavonolignans and flavonoids extracted from the seeds of milk thistle (Silybum marianum L. Gaertn). This study investigates the effect of major bioactive constituents from silymarin, silybin A, silybin B, isosilybin A, isosilybin B, silydianin, silychristin, isosilychristin, and taxifolin, on the expression of ABCA1, an important cholesterol efflux transporter, in THP-1-derived macrophages. Four of the studied compounds, isosilybin A, silybin B, silychristin and isosilychristin, were found to significantly induce ABCA1 protein expression without affecting cell viability. Moreover, isosilybin A, a partial PPARγ agonist, was found to promote cholesterol efflux from THP-1 macrophages in a concentration-dependent manner. These findings first show ABCA1 protein up-regulating activity of active constituents of silymarin and provide new avenues for their further study in the context of cardiovascular disease. View Full-Text
Keywords: ABCA1; silymarin; isosilybin A; cholesterol efflux; macrophages; flavonolignans ABCA1; silymarin; isosilybin A; cholesterol efflux; macrophages; flavonolignans

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Wang, L.; Rotter, S.; Ladurner, A.; Heiss, E.H.; Oberlies, N.H.; Dirsch, V.M.; Atanasov, A.G. Silymarin Constituents Enhance ABCA1 Expression in THP-1 Macrophages. Molecules 2016, 21, 55.

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