Haas Michael J, Onstead-Haas Luisa M, Naem Emad, Wong Norman C W, Mooradian Arshag D
Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, University of Florida , Jacksonville, FL , USA and.
Pharm Biol. 2014 Sep;52(9):1119-27. doi: 10.3109/13880209.2013.879187. Epub 2014 Mar 17.
Black seed [Nigella sativa L. (Ranunculaceae)] has been shown in animal models to lower serum cholesterol levels.
In order to determine if extracts from black seed have any effects on high-density lipoprotein (HDL), we characterized the effects of black seed extract on apolipoprotein A-I (apo A-I) gene expression, the primary protein component of HDL.
Hepatocytes (HepG2) and intestinal cells (Caco-2) were treated with black seed extracts, and Apo A-I, peroxisome proliferator-activated receptor α (PPARα), and retinoid-x-receptor α (RXRα) were measured by Western blot analysis. Apo A-I mRNA levels were measured by quantitative real-time polymerase chain reaction and apo A-I gene transcription was measured by transient transfection of apo A-I reporter plasmids.
Extracts from black seeds significantly increased hepatic and intestinal apo A-I secretion, as well as apo A-I mRNA and gene promoter activity. This effect required a PPARα binding site in the apo A-I gene promoter. Treatment of the extract with either heat or trypsin had no effect on its ability to induce apo A-I secretion. Treatment with black seed extract induced PPARα expression 9-fold and RXRα expression 2.5-fold. Furthermore, the addition of PPARα siRNA but not a control siRNA prevented some but not all the positive effects of black seed on apo A-I secretion.
Black seed extract is a potent inducer of apo A-I gene expression, presumably by enhancing PPARα/RXRα expression.
We conclude that black seed may have beneficial effects in treating dyslipidemia and coronary heart disease.
在动物模型中已证明黑种草籽（毛茛科黑种草属植物）可降低血清胆固醇水平。
为了确定黑种草籽提取物对高密度脂蛋白（HDL）是否有任何影响，我们对黑种草籽提取物对载脂蛋白A-I（apo A-I）基因表达（HDL的主要蛋白质成分）的影响进行了表征。
用黑种草籽提取物处理肝细胞（HepG2）和肠细胞（Caco-2），通过蛋白质印迹分析测量apo A-I、过氧化物酶体增殖物激活受体α（PPARα）和视黄醇X受体α（RXRα）。通过定量实时聚合酶链反应测量apo A-I mRNA水平，并通过瞬时转染apo A-I报告质粒测量apo A-I基因转录。
黑种草籽提取物显著增加肝脏和肠道apo A-I分泌，以及apo A-I mRNA和基因启动子活性。这种作用需要apo A-I基因启动子中的PPARα结合位点。用热或胰蛋白酶处理提取物对其诱导apo A-I分泌的能力没有影响。用黑种草籽提取物处理可使PPARα表达增加9倍，RXRα表达增加2.5倍。此外，添加PPARα siRNA而非对照siRNA可部分但并非完全阻止黑种草籽对apo A-I分泌的积极作用。
黑种草籽提取物是apo A-I基因表达的有效诱导剂，可能是通过增强PPARα/RXRα表达。
我们得出结论，黑种草籽可能对治疗血脂异常和冠心病有有益作用。
