【摘 要】
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Berberine (BBR) exhibits diverse bioactivities,including anticancer activity;but its poor druggability limits its applications.In this study,we designed and syn
【机 构】
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Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of C
论文部分内容阅读
Berberine (BBR) exhibits diverse bioactivities,including anticancer activity;but its poor druggability limits its applications.In this study,we designed and synthesized a series of 9-0 position modified BBR derivatives aiming to improve its cell permeability and anticancer activity,utilizing a long alkyl chain branched by hydroxyl group and methoxycarbonyl group.Among these compounds,B10 showed 3.6-fold higher intracellular concentration than BBR,as well as 60-fold increased anti-proliferation activity against human lung cancer A549 cells compared with BBR,Treatment with B10 (1,2 μM) induced apoptosis of A549 cells.Further investigations showed that B10 treatment dose-dependently affected mitochondrial functions,including oxygen consumption rate (OCR),mitochondrial membrane potential (MMP) and the morphology of mitochondria in A549 cells.Therefore,this work offers a new way for BBR structural modification through improving cell membrane permeability to affect mitochondrial functions and potential anti-tumor therapy in the future.
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