Leifert Wayne R, Abeywardena Mahinda Y
Commonwealth Scientific and Industrial Research Organisation, Division of Human Nutrition, PO Box 10041, Adelaide BC, SA 5000, Australia.
Nutr Res. 2008 Dec;28(12):842-50. doi: 10.1016/j.nutres.2008.09.001. Epub 2008 Nov 8.
Accumulating evidence suggests that grape seed and wine polyphenol extracts possess a diverse array of actions and may be beneficial in the prevention of inflammatory-mediated disease such as cardiovascular disease and cancer. This study aimed to determine whether the reported pleiotropic effects of several polyphenolic extracts from grape seed products or red wine would also include inhibition of cholesterol uptake and cell proliferation, and inhibit a known specific target of the inflammatory process, that is, 5-lipoxygenase (5-LOX). Incubation of HT29, Caco2, HepG2, or HuTu80 cells in a medium containing [(3)H]cholesterol in the presence of a grape seed extract (GSE) or red wine polyphenolic compounds (RWPCs) inhibited [(3)H]cholesterol uptake by up to 66% (which appeared maximal). The estimated IC(50) values were 60 and 83 microg/mL for RWPC and GSE, respectively. Similar cholesterol uptake inhibitory effects were observed using the fluorescent cholesterol analogue NBD cholesterol. The inhibition of cholesterol uptake was independent of the sample's (GSE and RWPC) potent antioxidative capacity. Red wine polyphenolic compound and GSE dose dependently inhibited HT29 colon adenocarcinoma cell proliferation, which was accompanied by an increase in apoptosis. In addition, RWPC and GSE inhibited 5-LOX activity with the IC(50) values being 35 and 13 microg/mL, respectively. Two of 3 other GSEs tested also significantly inhibited 5-LOX activity. Inhibition of cholesterol uptake and proinflammatory 5-LOX activity may be beneficial in preventing the development of chronic degenerative diseases such as cardiovascular disease and cancer.
越来越多的证据表明，葡萄籽和葡萄酒中的多酚提取物具有多种作用，可能有助于预防炎症介导的疾病，如心血管疾病和癌症。本研究旨在确定葡萄籽产品或红酒中几种多酚提取物所报道的多效性作用是否还包括抑制胆固醇摄取和细胞增殖，并抑制炎症过程中一个已知的特定靶点，即5-脂氧合酶（5-LOX）。在含有[³H]胆固醇的培养基中，将HT29、Caco2、HepG2或HuTu80细胞与葡萄籽提取物（GSE）或红酒多酚化合物（RWPCs）一起孵育，可使[³H]胆固醇摄取最多抑制66%（似乎已达到最大值）。RWPC和GSE的估计半数抑制浓度（IC₅₀）值分别为60和83微克/毫升。使用荧光胆固醇类似物NBD胆固醇也观察到了类似的胆固醇摄取抑制作用。胆固醇摄取的抑制与样品（GSE和RWPC）的强大抗氧化能力无关。红酒多酚化合物和GSE剂量依赖性地抑制HT29结肠腺癌细胞增殖，同时伴有细胞凋亡增加。此外，RWPC和GSE抑制5-LOX活性，IC₅₀值分别为35和13微克/毫升。测试的其他3种GSE中有2种也显著抑制5-LOX活性。抑制胆固醇摄取和促炎的5-LOX活性可能有助于预防慢性退行性疾病，如心血管疾病和癌症的发生。
