Khazneh Elian, Hřibová Petra, Hošek Jan, Suchý Pavel, Kollár Peter, Pražanová Gabriela, Muselík Jan, Hanaková Zuzana, Václavík Jiří, Miłek Michał, Legáth Jaroslav, Šmejkal Karel
Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic.
Department of Molecular Biology and Pharmaceutical Biotechnology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackého tř. 1, Brno 61242, Czech Republic.
Molecules. 2016 Mar 25;21(4):404. doi: 10.3390/molecules21040404.
This study was done to identify the content compounds of Achillea wilhelmsii (A. wilhelmsii) and to evaluate its hypoglycemic and anti-hypercholesterolemic activity and effect on inflammatory mediators. The extracts and fractions of A. wilhelmsii were thoroughly analyzed using high performance liquid chromatography (HPLC), and the total content of phenols and flavonoids was determined. The hypoglycemic activity was evaluated in vivo using alloxan-induced diabetic mice. The effect upon inflammatory mediators was evaluated in vitro using the human monocytic leukemia cell line (THP-1). The anti-hypercholesterolemic activity was evaluated in vitro using the 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase assay kit. The water extract (WE)-treated group showed the highest reduction in the fasting blood glucose levels (FBGL). The chloroform fraction (CF) and ethyl acetate fraction (EAF) both showed a significant ability to reduce the secretion of tumor necrosis factor alpha (TNF-α). The EAF, however, also attenuated the levels of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9). The CF showed the most significant 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibition activity. The five main compounds in the CF were isolated and identified. Out of the five compounds in the CF, 1β,10β-epoxydesacetoxymatricarin (CP1) and leucodin (CP2) showed the highest anti-hypercholesterolemic potential. A molecular docking study provided corresponding results.
本研究旨在鉴定蓍草(Achillea wilhelmsii)的成分化合物,并评估其降血糖、抗高胆固醇血症活性以及对炎症介质的影响。采用高效液相色谱法(HPLC)对蓍草的提取物和馏分进行了全面分析,并测定了酚类和黄酮类化合物的总含量。使用四氧嘧啶诱导的糖尿病小鼠在体内评估降血糖活性。使用人单核细胞白血病细胞系(THP-1)在体外评估对炎症介质的影响。使用3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶检测试剂盒在体外评估抗高胆固醇血症活性。水提取物(WE)处理组的空腹血糖水平(FBGL)降低幅度最大。氯仿馏分(CF)和乙酸乙酯馏分(EAF)均显示出显著降低肿瘤坏死因子α(TNF-α)分泌的能力。然而,EAF也降低了基质金属蛋白酶-2(MMP-2)和基质金属蛋白酶-9(MMP-9)的水平。CF显示出最显著的3-羟基-3-甲基戊二酰辅酶A还原酶(HMGR)抑制活性。分离并鉴定了CF中的五种主要化合物。在CF中的五种化合物中,1β,10β-环氧去乙酰氧基母菊内酯(CP1)和亮叶甲素(CP2)显示出最高的抗高胆固醇血症潜力。分子对接研究提供了相应的结果。