Department of Pharmacy Practice, Center of Excellence for Innovation in Chemistry, Pharmacological Research Unit, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, 65000, Thailand.
J Nat Med. 2013 Apr;67(2):303-10. doi: 10.1007/s11418-012-0682-7. Epub 2012 Jun 27.
Black pepper (Piper nigrum L.) lowers blood lipids in vivo and inhibits cholesterol uptake in vitro, and piperine may mediate these effects. To test this, the present study aimed to compare actions of black pepper extract and piperine on (1) cholesterol uptake and efflux in Caco-2 cells, (2) the membrane/cytosol distribution of cholesterol transport proteins in these cells, and (3) the physicochemical properties of cholesterol micelles. Piperine or black pepper extract (containing the same amount of piperine) dose-dependently reduced cholesterol uptake into Caco-2 cells in a similar manner. Both preparations reduced the membrane levels of NPC1L1 and SR-BI proteins but not their overall cellular expression. Micellar cholesterol solubility of lipid micelles was unaffected except by 1 mg/mL concentration of black pepper extract. These data suggest that piperine is the active compound in black pepper and reduces cholesterol uptake by internalizing the cholesterol transporter proteins.
黑胡椒（Piper nigrum L.）具有体内降低血脂和体外抑制胆固醇摄取的作用，胡椒碱可能介导这些作用。为了验证这一点，本研究旨在比较黑胡椒提取物和胡椒碱对（1）Caco-2 细胞中胆固醇摄取和流出、（2）这些细胞中胆固醇转运蛋白的膜/细胞质分布以及（3）胆固醇胶束的物理化学性质的作用。胡椒碱或黑胡椒提取物（含有等量的胡椒碱）以相似的方式剂量依赖性地降低 Caco-2 细胞中胆固醇的摄取。两种制剂均降低 NPC1L1 和 SR-BI 蛋白的膜水平，但不影响其整体细胞表达。脂质胶束的胆固醇溶解度除了受 1mg/mL 浓度的黑胡椒提取物影响外，不受影响。这些数据表明，胡椒碱是黑胡椒中的活性化合物，通过内化胆固醇转运蛋白来减少胆固醇摄取。
