Center for Natural Product Research, Faculty of Chemistry, University of Havana, Havana 10400, Cuba.
Department of Chemistry, Federal University of Maranhão, São Luis, Maranhão 65080-805, Brazil.
Molecules. 2020 May 2;25(9):2134. doi: 10.3390/molecules25092134.
(Kunth) R. M. King & H. Robinson is a species of flowering shrub in the family Asteraceae, native to the Caribbean and Texas. The aim of this work was to compare the quantitative chemical composition of extracts obtained from in its flowering and vegetative stages with the antioxidant potential and to determine the effects on P-glycoprotein (P-gp) function. The quantitative chemical composition of the extracts was determined quantifying their major flavonoids by UPLC-ESI-MS/MS and by PCA analysis. The effects of the extracts on P-gp activity was evaluated by Rhodamine 123 assay; antioxidant properties were determined by DPPH, FRAP and inhibition of lipid peroxidation methods. The obtained results show that major flavonoids were present in higher concentrations in vegetative stage than flowering stage. In particular, the extracts obtained in the flowering season showed a significantly higher ability to sequester free radicals compared to those of the vegetative season, meanwhile, the extracts obtained during the vegetative stage showed a significant inhibitory effect against brain lipid peroxidation and a strong reductive capacity. This study also showed the inhibitory effects of all ethanolic extracts on P-gp function in 4T1 cell line; these effects were unrelated to the phenological stage. This work shows, therefore, the first evidence on: the inhibition of P-gp function, the antioxidant effects and the content of major flavonoids of . According to the obtained results, the species (Kunth) R. M. King & H. Robinson could be a source of new potential inhibitors of drug efflux mediated by P-gp. A special focus on all these aspects must be taking into account for future studies.
（昆斯）R.M.金和 H.罗宾逊是菊科开花灌木的一个物种，原产于加勒比海和德克萨斯州。这项工作的目的是比较开花期和营养期提取液的定量化学成分与抗氧化潜力，并确定对 P-糖蛋白（P-gp）功能的影响。通过 UPLC-ESI-MS/MS 和 PCA 分析定量测定提取物中主要类黄酮的含量来确定提取物的定量化学成分。通过 Rhodamine 123 测定法评估提取物对 P-gp 活性的影响；通过 DPPH、FRAP 和抑制脂质过氧化方法测定抗氧化特性。所得结果表明，营养期的主要类黄酮浓度高于花期。特别是，开花期提取液比营养期提取液具有更高的清除自由基能力，而营养期提取液对脑脂质过氧化具有显著的抑制作用和较强的还原能力。本研究还表明，所有乙醇提取物对 4T1 细胞系中 P-gp 功能均有抑制作用；这些作用与物候期无关。因此，这项研究首次证明了：（1）对 P-gp 功能的抑制作用；（2）抗氧化作用；（3）主要类黄酮的含量。根据获得的结果，（昆斯）R.M.金和 H.罗宾逊物种可能是一种新的潜在 P-糖蛋白介导的药物外排抑制剂的来源。在未来的研究中，必须特别关注所有这些方面。
