Department of Medicinal Chemistry, University of Florida, Gainesville, Florida, United States of America.
Department of Pharmacodynamics, University of Florida, Gainesville, Florida, United States of America.
PLoS One. 2018 May 24;13(5):e0197940. doi: 10.1371/journal.pone.0197940. eCollection 2018.
Kava is regaining its popularity with detailed characterizations warranted. We developed an ultraperformance liquid chromatography high-resolution tandem mass spectrometry (UPLC-MS/MS) method for major kavalactones (kavain, dihydrokavain, methysticin, dihydromethysticin and desmethoxyyangonin) with excellent selectivity and specificity. The method has been validated for different matrices following the Food and Drug Administration guidance of analytical procedures and methods validation. The scope of this method has been demonstrated by quantifying these kavalactones in two kava products, characterizing their tissue distribution and pharmacokinetics in mice, and detecting their presence in human urines and plasmas upon kava intake. As expected, the abundances of these kavalactones differed significantly in kava products. All of them exhibited a large volume of distribution with extensive tissue affinity and adequate mean residence time (MRT) in mice. This method also successfully quantified these kavalactones in human body fluids upon kava consumption at the recommended human dose. This UPLC-MS/MS method therefore can be used to characterize kava products and its pharmacokinetics in animals and in humans.
卡瓦正在重新获得人们的青睐，这是有充分理由的。我们开发了一种超高效液相色谱-高分辨串联质谱（UPLC-MS/MS）方法，用于检测主要的卡瓦内酯（卡瓦酮、二氢卡瓦酮、甲氧基卡瓦酮、二氢甲氧基卡瓦酮和去甲氧基醉椒素），该方法具有出色的选择性和特异性。该方法已按照美国食品和药物管理局（FDA）分析程序和方法验证指南对不同基质进行了验证。该方法的适用范围通过以下方式得到了证明：在两种卡瓦产品中定量这些卡瓦内酯，在小鼠中对其组织分布和药代动力学进行表征，并在摄入卡瓦后检测其在人尿液和血浆中的存在。正如预期的那样，这些卡瓦内酯在卡瓦产品中的丰度差异很大。所有这些卡瓦内酯在小鼠中都表现出较大的分布容积、广泛的组织亲和力和足够的平均驻留时间（MRT）。该方法还成功地在人体推荐剂量下摄入卡瓦后对人体液中的这些卡瓦内酯进行了定量。因此，该 UPLC-MS/MS 方法可用于对卡瓦产品及其在动物和人体中的药代动力学进行表征。
