Fluorescent labeling of ursolic acid with FITC for investigation of its cytotoxic activity using confocal microscopy.,Bioorganic Chemistry

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Fluorescent labeling of ursolic acid with FITC for investigation of its cytotoxic activity using confocal microscopy.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-12-04 , DOI: 10.1016/j.bioorg.2018.11.052
Tatiana S Frolova ₁ , Alla V Lipeeva ₂ , Dmitry S Baev ₃ , Sergey I Baiborodin ₄ , Кonstantin E Orishchenko ₄ , Alexey V Kochetov ₅ , Olga I Sinitsyna ₅

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Fluorescent labeling is a widely-used approach in the study of intracellular processes. This method is becoming increasingly popular for studying small bioactive molecules of natural origin; it allows us to estimate the vital intracellular changes which occur under their influence. We propose a new approach for visualization of the intracellular distribution of triterpene acids, based on fluorescent labeling by fluoresceine isothiocyanate. As a model compound we took the most widely-used and best-studied acid in the ursane series - ursolic acid, as this enabled us to compare the results obtained during our research with the available data, in order to evaluate the validity of the proposed method. Experimental tracing of the dynamics of penetration and distribution of the labeled ursolic acid has shown that when the acid enters the cell, it initially localizes on the inner membranes where the predicted target Akt1/protein kinase B - a protein that inhibits apoptosis - is located.

中文翻译：

用 FITC 荧光标记熊果酸，使用共聚焦显微镜研究其细胞毒性活性。

荧光标记是细胞内过程研究中广泛使用的方法。这种方法在研究天然来源的生物活性小分子方面变得越来越流行。它使我们能够估计在它们的影响下发生的重要细胞内变化。我们提出了一种基于异硫氰酸荧光标记的三萜酸细胞内分布可视化的新方法。作为模型化合物，我们采用了熊烷系列中最广泛使用和研究最深入的酸 - 熊果酸，因为这使我们能够将研究过程中获得的结果与现有数据进行比较，以评估所提出的方法的有效性方法。对标记熊果酸渗透和分布动态的实验追踪表明，当熊果酸进入细胞时，它最初定位于内膜，预测的目标 Akt1/蛋白激酶 B（一种抑制细胞凋亡的蛋白质）就位于该处。

更新日期：2018-12-04

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