Wang Limei, Rotter Susanne, Ladurner Angela, Heiss Elke H, Oberlies Nicholas H, Dirsch Verena M, Atanasov Atanas G
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.
Molecules. 2015 Dec 31;21(1):E55. doi: 10.3390/molecules21010055.
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.
水飞蓟素是从水飞蓟（Silybum marianum L. Gaertn）种子中提取的一种具有肝脏保护作用的黄酮木脂素和黄酮类混合物。本研究调查了水飞蓟素的主要生物活性成分水飞蓟宾A、水飞蓟宾B、异水飞蓟宾A、异水飞蓟宾B、水飞蓟宁、水飞蓟素、异水飞蓟素和紫杉叶素对THP-1衍生巨噬细胞中重要的胆固醇流出转运蛋白ABCA1表达的影响。研究发现，所研究的四种化合物，即异水飞蓟宾A、水飞蓟宾B、水飞蓟素和异水飞蓟素，能显著诱导ABCA1蛋白表达，且不影响细胞活力。此外，异水飞蓟宾A作为一种部分PPARγ激动剂，被发现能以浓度依赖的方式促进THP-1巨噬细胞中的胆固醇流出。这些发现首次表明水飞蓟素活性成分具有ABCA1蛋白上调活性，并为其在心血管疾病背景下的进一步研究提供了新途径。
