Conjugation of Natural Triterpenic Acids with Delocalized Lipophilic Cations: Selective Targeting Cancer Cell Mitochondria

Journal of Personalized Medicine

KonstantinN. Belosludtsev¹  MikhailV. Dubinin¹  DaryaA. Nedopekina²  RinatR. Gubaidullin²  AnnaYu. Spivak² 

[1] Department of Biochemistry, Cell Biology and Microbiology, Mari State University, 424001 Yoshkar-Ola, Russia;Organic Synthesis Laboratory, Institute of Petrochemistry and Catalysis, Russian Academy of Sciences, 450075 Ufa, Russia;

关键词: mitochondria;    mitochondrial targeting;    delocalized lipophilic cations;    anti-cancer agents;    mitocans;    triterpenic acids;   

DOI  :  10.3390/jpm11060470

来源: DOAJ

【 摘 要 】

Currently, a new line of research on mitochondria-targeted anticancer drugs is actively developing in the field of biomedicine and medicinal chemistry. The distinguishing features of this universal target for anticancer agents include presence of mitochondria in the overwhelming majority, if not all types of transformed cells, crucial importance of these cytoplasmic organelles in energy production, regulation of cell death pathways, as well as generation of reactive oxygen species and maintenance of calcium homeostasis. Hence, mitochondriotropic anticancer mitocan agents, acting through mitochondrial destabilization, have good prospects in cancer therapy. Available natural pentacyclic triterpenoids are considered promising scaffolds for development of new mitochondria-targeted anticancer agents. These secondary metabolites affect the mitochondria of tumor cells and initiate formation of reactive oxygen species. The present paper focuses on the latest research outcomes of synthesis and study of cytotoxic activity of conjugates of pentacyclic triterpenoids with some mitochondria-targeted cationic lipophilic molecules and highlights the advantages of applying them as novel mitocan agents compared to their prototype natural triterpenic acids.

【 授权许可】

Unknown