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Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs.

Abstract：

:Glycyrrhetinic acid has been usually studied for their anti-tumor activities. However, the low bioavailability and poor aqueous solubility as well as limited intracellular accumulation have limited their utility. In this present study, a series of new glycyrrhetinic acid conjugates with a triphenylphosphonium cation (TTP+) moiety, meant to specifically target them to tumor cells mitochondria, have been designed and synthesized. Among them, compound 2f possessed excellent antitumor activities against the tested human cancer cells, and simultaneously exhibited better cell selectivity between cancer cells and normal cells than glycyrrhetinic acid and HCPT. Moreover, 2f significantly induced cell cycle arrest at the G2/M phase, and effectively inhibited cancer cells proliferation and migration. Mechanism studies revealed that 2f triggered apoptosis through the mitochondrial pathway via the collapse of mitochondrial membrane potential, reactive oxygen species production and the activation of caspase-9 and caspase-3.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Jin L,Dai L,Ji M,Wang H

doi

10.1016/j.bioorg.2018.12.036

subject

Has Abstract

pub_date

2019-04-01 00:00:00

pages

179-190

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)31177-5

journal_volume

85

pub_type

杂志文章

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