Federal Research Center Institute of Cytology and Genetics of Siberian Branch of the Russian Academy of Sciences, 10, Lavrentyev Ave., 630090 Novosibirsk, Russia; Novosibirsk Institute of Organic Chemistry of Siberian Branch of the Russian Academy of Sciences, 10, Lavrentyev Ave., 630090 Novosibirsk, Russia; Novosibirsk State University, 2, Pirogov Street, 630090 Novosibirsk, Russia; Federal Research Center of Fundamental and Translational Medicine of Siberian Branch of the Russian Academy of Sciences, 2, Timakov Street, 630117 Novosibirsk, Russia.
Novosibirsk Institute of Organic Chemistry of Siberian Branch of the Russian Academy of Sciences, 10, Lavrentyev Ave., 630090 Novosibirsk, Russia.
Bioorg Chem. 2019 Jun;87:876-887. doi: 10.1016/j.bioorg.2018.11.052. Epub 2018 Dec 4.
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.
荧光标记是研究细胞内过程的一种广泛应用的方法。这种方法在研究天然来源的小分子生物活性物质时越来越受欢迎；它使我们能够估计在它们的影响下发生的重要的细胞内变化。我们提出了一种基于荧光素异硫氰酸酯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，我们选择了在 Ursane 系列中使用最广泛和研究最好的酸 - 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，以评估所提出方法的有效性。对标记的熊果酸渗透和分布动力学的实验追踪表明，当酸进入细胞时，它最初定位于内部膜上，预测的靶标 Akt1/蛋白激酶 B - 一种抑制细胞凋亡的蛋白质 - 位于该位置。
