Pharmacognosy Department, College of Pharmacy, Cairo University, Kasr el Aini St., P.B. 11562, Cairo, Egypt ; Leibniz Institute of Plant Biochemistry, Dept. of Bioorganic Chemistry, Weinberg 3, D-06120 Halle (Saale), Germany.
Leibniz Institute of Plant Biochemistry, Dept. of Bioorganic Chemistry, Weinberg 3, D-06120 Halle (Saale), Germany.
J Adv Res. 2013 Jul;4(4):417-21. doi: 10.1016/j.jare.2012.07.006. Epub 2012 Sep 4.
Hops (Humulus lupulus L. Cannabaceae) is an economically important crop, that has drawn more attention in recent years due to its potential pharmaceutical applications. Bitter acids (prenylated polyketides) and prenylflavonoids are the primary phytochemical components that account for hops resins medicinal value. We have previously reported on utilizing untargeted NMR and MS metabolomics for analysis of 13 hops cultivars, revealing for differences in α- versus β-bitter acids composition in derived resins. In this study, effect of ratios of bitter α- to β-acids in hop resins to cytotoxicity of hop resins was investigated. In vitro cell culture assays revealed that β-acids were more effective than α-acids in growth inhibition of PC3 and HT29 cancer cell lines. Nevertheless, hop resins enriched in β-acids showed comparable growth inhibition patterns to α-enriched resins and suggesting that bioactivity may not be easily predicted by metabolomics and/or gross metabolic profiling in hops.
啤酒花(Humulus lupulus L. Cannabaceae)是一种具有重要经济价值的作物,近年来由于其在药物方面的潜在应用而受到了更多的关注。苦味酸(类异戊烯基多酮)和类异戊烯基黄酮类化合物是啤酒花树脂药用价值的主要植物化学成分。我们之前曾报道过利用无靶向 NMR 和 MS 代谢组学分析 13 个啤酒花品种,发现衍生树脂中α-与β-苦味酸组成的差异。在这项研究中,我们研究了啤酒花树脂中苦味酸的α-与β-比例对树脂细胞毒性的影响。体外细胞培养实验表明,β-酸在抑制 PC3 和 HT29 癌细胞系生长方面比 α-酸更有效。然而,富含β-酸的啤酒花树脂显示出与富含α-酸的树脂相似的生长抑制模式,这表明生物活性可能不容易通过代谢组学和/或啤酒花中的总体代谢分析来预测。