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Fluorescent labeling of ursolic acid with FITC for investigation of its cytotoxic activity using confocal microscopy.
- Source :
-
Bioorganic chemistry [Bioorg Chem] 2019 Jun; Vol. 87, pp. 876-887. Date of Electronic Publication: 2018 Dec 04. - Publication Year :
- 2019
-
Abstract
- 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.<br /> (Copyright © 2018. Published by Elsevier Inc.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Apoptosis drug effects
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Fluorescent Dyes chemical synthesis
Fluorescent Dyes chemistry
Humans
Isothiocyanates chemistry
MCF-7 Cells
Microscopy, Confocal
Models, Molecular
Molecular Conformation
Structure-Activity Relationship
Triterpenes chemistry
Ursolic Acid
Antineoplastic Agents pharmacology
Fluorescent Dyes pharmacology
Isothiocyanates pharmacology
Triterpenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2120
- Volume :
- 87
- Database :
- MEDLINE
- Journal :
- Bioorganic chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 30538052
- Full Text :
- https://doi.org/10.1016/j.bioorg.2018.11.052