Chair of Food Science, Institute of Nutritional Science, Justus Liebig University Giessen, Heinrich-Buff-Ring 26-32, 35392 Giessen, Germany.
Department of Chromatography, Faculty of Chemistry, Maria Curie-Sklodowska University, Maria Curie-Sklodowska Sq. 3, 20031 Lublin, Poland.
Molecules. 2023 Feb 5;28(4):1535. doi: 10.3390/molecules28041535.
Planar chromatography has recently been combined with six different effect-directed assays for three golden root ( L.) samples. However, the profiles obtained showed an intense tailing, making zone differentiation impossible. The profiling was therefore improved to allow for the detection of individual bioactive compounds, and the range of samples was extended to 15 commercial golden root products. Further effect-directed assays were studied providing information on 15 different effect mechanisms, i.e., (1) tyrosinase, (2) acetylcholinesterase, (3) butyrylcholinesterase, (4) β-glucuronidase, and (5) α-amylase inhibition, as well as endocrine activity via the triplex planar yeast antagonist-verified (6-8) estrogen or (9-11) androgen screen, (12) genotoxicity via the planar SOS-Umu-C bioassay, antimicrobial activity against (13) Gram-negative and (14) Gram-positive bacteria, and (15) antioxidative activity (DPPH• radical scavengers). Most of the golden root profiles obtained were characteristic, but some samples differed substantially. The United States Pharmacopeia reference product showed medium activity in most of the assays. The six most active compound zones were further characterized using high-resolution mass spectrometry, and the mass signals obtained were tentatively assigned to molecular formulae. In addition to confirming the known activities, this study is the first to report that golden root constituents inhibit butyrylcholinesterase (rosin was tentatively assigned), β-glucuronidase (rosavin, rosarin, rosiridin, viridoside, and salidroside were tentatively assigned), and α-amylase (stearic acid and palmitic acid were tentatively assigned) and that they are genotoxic (hydroquinone was tentatively assigned) and are both agonistic and antagonistic endocrine active.
近年来,平面色谱已与六种不同的效价导向测定法结合,用于三种金根(金)样品。然而,所得图谱显示出强烈的拖尾,使得区带分化成为不可能。因此,对图谱进行了改进,以允许检测单个生物活性化合物,并将样品范围扩展到 15 种商业金根产品。进一步的效价导向测定法研究提供了关于 15 种不同作用机制的信息,即(1)酪氨酸酶,(2)乙酰胆碱酯酶,(3)丁酰胆碱酯酶,(4)β-葡萄糖醛酸酶和(5)α-淀粉酶抑制作用,以及通过三重平面酵母拮抗剂验证的内分泌活性(6-8)雌激素或(9-11)雄激素筛选,(12)平面 SOS-Umu-C 生物测定法的遗传毒性,(13)革兰氏阴性和(14)革兰氏阳性细菌的抗菌活性,以及(15)抗氧化活性(DPPH•自由基清除剂)。获得的大多数金根图谱具有特征性,但有些样品差异很大。美国药典参考产品在大多数测定中显示出中等活性。进一步使用高分辨率质谱对六个最活跃的化合物区带进行了表征,并对获得的质量信号进行了初步分配,以确定分子式。除了证实已知的活性外,本研究首次报道金根成分抑制丁酰胆碱酯酶(松香被暂定分配),β-葡萄糖醛酸酶(rosavin、rosarin、rosiridin、viridoside 和 salidroside 被暂定分配)和α-淀粉酶(硬脂酸和棕榈酸被暂定分配),并且它们具有遗传毒性(对苯二酚被暂定分配),并具有激动和拮抗内分泌活性。