Conjugation of Triterpenic Acids of Ursane and Oleanane Types with Mitochondria-Targeting Cation F16 Synergistically Enhanced Their Cytotoxicity against Tumor Cells

Conjugation of Triterpenic Acids of Ursane and Oleanane Types with Mitochondria-Targeting Cation F16 Synergistically Enhanced Their Cytotoxicity against Tumor Cells

The present work shows the cytotoxic effects of novel conjugates of ursolic, oleanolic, maslinic, and corosolic acids with the penetrating cation F16 on cancer cells (lung adenocarcinoma A549 and H1299, breast cancer cell lines MCF-7 and BT474) and non-tumor human fibroblasts. It has been establishe...

Full description

Saved in:
Bibliographic Details
Published in:Membranes (Basel) Vol. 13; no. 6; p. 563
Main Authors: Dubinin, Mikhail V, Nedopekina, Darya A, Ilzorkina, Anna I, Semenova, Alena A, Sharapov, Vyacheslav A, Davletshin, Eldar V, Mikina, Natalia V, Belsky, Yuri P, Spivak, Anna Yu, Akatov, Vladimir S, Belosludtseva, Natalia V, Liu, Jiankang, Belosludtsev, Konstantin N
Format: Journal Article
Language:English
Published: Switzerland MDPI AG 30-05-2023
MDPI
Subjects:
Acids
Adenocarcinoma
Apoptosis
Breast cancer
Cancer
Cations
Cell cycle
Chromatography
Comparative analysis
Conjugates
Conjugation
Cytotoxicity
F16
Fibroblasts
Liver diseases
Lung cancer
Membrane potential
mitocans
Mitochondria
Molecular structure
Organelles
Oxidative phosphorylation
Phosphorylation
Toxicity
triterpenic acids
Tumor cell lines
Tumor cells
Tumors
Massachusetts
Russia
Germany
mitocans
mitochondria
ROS
F16
cancer
cytotoxicity
oxidative phosphorylation
triterpenic acids
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The present work shows the cytotoxic effects of novel conjugates of ursolic, oleanolic, maslinic, and corosolic acids with the penetrating cation F16 on cancer cells (lung adenocarcinoma A549 and H1299, breast cancer cell lines MCF-7 and BT474) and non-tumor human fibroblasts. It has been established that the conjugates have a significantly enhanced toxicity against tumor-derived cells compared to native acids and also demonstrate selectivity to some cancer cells. The toxic effect of the conjugates is shown to be due to ROS hyperproduction in cells, induced by the effect on mitochondria. The conjugates caused dysfunction of isolated rat liver mitochondria and, in particular, a decrease in the efficiency of oxidative phosphorylation, a decrease in the membrane potential, and also an overproduction of ROS by organelles. The paper discusses how the membranotropic- and mitochondria-targeted effects of the conjugates may be related to their toxic effects.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:2077-0375
2077-0375
DOI:10.3390/membranes13060563