首页|Design,synthesis and biological evaluation of fluorescent derivatives of ursolic acid in living cells

Design,synthesis and biological evaluation of fluorescent derivatives of ursolic acid in living cells

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Ursolic acid(UA)is a naturally occurring ursane triterpenoid,which exhibits a wide range of unique biological activities.To clarify its mechanism of action(MOA),a series of fluorescent derivatives of UA(5a-c)were designed and synthesized by conjugation with 7-nitrobenzo-2-oxa-1,3-diazole(NBD)fluo-rophore.Among them,5c exhibited similar anti-proliferative activity with UA against HCT116 cells(half maximal inhibitory concentration(IC50)=9.21±0.50 μmol/L).Cell imaging experiment indicated that 5c was rapidly taken up in HCT116 cells in a dose and time-dependent manner.Then,5c was found to lo-calize in endoplasmic reticulum(ER),lysosomes,and mitochondria,but not in nucleus of HCT116 cells by confocal microscopy studies.Preliminary MOA proved that UA induced autophagy with a unique in-tracellular distribution mechanism involving ER and lysosome.In all,our work provides new clues for revealing the molecular mechanism of UA as an antitumor agent.

Pentacyclic triterpenoidUrsolic acidFluorescent derivativesAutophagyApoptosis

Wenyi Mei、Lijuan Xie、Xiaodong Zhang、Cunjian Shi、Fengzhi Wang、Qiqi Fu、Zhenjiang Zhao、Honglin Li、Yufang Xu、Zhuo Chen

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Shanghai Key Laboratory of New Drug Design,State Key Laboratory of Bioreactor Engineering,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China

Innovation Center for AI and Drug Discovery,East China Normal University,Shanghai 200062,China

Lingang Laboratory,Shanghai 200031,China

国家重点研发计划国家自然科学基金国家自然科学基金Shanghai Science and Technology Commission Biomedical Science and Technology Support Special ProjectShanghai Science and Technology Commission Biomedical Science and Technology Support Special ProjectNational Program for Special Supports of Eminent ProfessionalsNational Program for Support of Top-notch Young Professionals

2022YFC3400501818250208215020821S1190790020S11901000

2024

10.1016/j.cclet.2023.108825

中国化学快报(英文版)
中国化学会

中国化学快报(英文版)

CSTPCD
影响因子：0.771
ISSN：1001-8417
年,卷(期)：2024.35(5)
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