Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 27, Issue 10, Pages 2231-2238Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-018-2230-9
Keywords
Podophyllotoxin; Lonidamine; Antitumor activity; Leukemia cells; Molecular docking
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Funding
- Department of Science and Technology of Guizhou Province [[2017]1219, [2014]7565, [2014]7557]
- Ministry of Education Chunhui Project Foundation of China [Z2015008]
- Academic Youth & Innovation Exploration of Zunyi Medical University
- National First-Rate Construction Discipline of Guizhou Province (Pharmacy) [YLXKJS-YX-04]
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A novel podophyllotoxin-lonidamine hybrid was synthesized, and evaluated for its in vitro cytotoxicity by CCK-8 assay. The conjugate, Da, exhibited comparable antiproliferative activity in human normal and multidrug-resistance leukemia cancer cells. Flow cytometry suggested that Da could induce G2 phase cycle arrest and apoptosis of resistant K562/VCR cells, simultaneously increase the mitochondrial membrane depolarization. Furthermore, immunocytochemistry showed that Da could significantly disrupt the microtubule organization in K562/VCR cells. Molecular modeling demonstrated that Da was able to bind into the colchicine site of tubulin.
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