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Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs
Jin, Le; Dai, Lumei1; Ji, Min; Wang, Hengshan2
2019
Source PublicationBIOORGANIC CHEMISTRY
ISSN0045-2068
Volume85Pages:179
AbstractGlycyrrhetinic 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.
DepartmentLMB
KeywordGlycyrrhetinic acid Anti-tumor Mitochondria Apoptosis
DOI10.1016/j.bioorg.2018.12.036
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Cited Times:4[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.scsio.ac.cn/handle/344004/17873
Collection中科院海洋生物资源可持续利用重点实验室
Affiliation1.Southeast Univ, Sch Biol Sci & Med Engn, Nanjing 210096, Jiangsu, Peoples R China
2.Chinese Acad Sci, South China Sea Inst Oceanol, Key Lab Trop Marine Bioresources & Ecol, Guangzhou 510301, Guangdong, Peoples R China
3.Guangxi Normal Univ, State Key Lab Chem & Mol Engn Med Resources, Sch Chem & Pharmaceut Sci, Guilin 541004, Peoples R China
Recommended Citation
GB/T 7714
Jin, Le,Dai, Lumei,Ji, Min,et al. Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs[J]. BIOORGANIC CHEMISTRY,2019,85:179, 190.
APA Jin, Le,Dai, Lumei,Ji, Min,&Wang, Hengshan.(2019).Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs.BIOORGANIC CHEMISTRY,85,179.
MLA Jin, Le,et al."Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs".BIOORGANIC CHEMISTRY 85(2019):179.
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