Synthesis, characterization and cytotoxicity of alkylated quercetin derivatives
Author(s):
Xinran Bao , Han Liao , Jiao Qu , Yong Sun , Xin Guo , Enxia Wang , Yuhong Zhen
Abstract:
Quercetin, a ubiquitous flavonol, represents a promising leading drug for development of new chemotherapeutic agents. However, its limited cytotoxicity to cancer cells hampers its clinical use. In order to obtain novel quercetin derivatives with superior cytotoxicity, seven alkylated quercetin derivatives were synthesized. Solubility of these derivatives was determined by turbidimetry. Cytotoxicity of the high-soluble derivatives against MCF-7 cells and caco-2 cells was determined using MTT assay. Among these seven products, 7-O-butylquercetin had the highest solubility in DMEM medium and 7-O-geranylquercetin had the most potent cytotoxicity. Further study on cytotoxicity of 7-O-geranylquercetin on NCI-H446, A549, MGC-803 and SGC-7901 cell lines revealed potential antiproliferative effects. The 7-O-geranylquercetin is a broad spectrum cytotoxic agent and it may be a promising leading drug for cancer chemotherapy.
Keywords:
Language:
English
Published:
Iranian Journal of Pharmaceutical Research, Volume:15 Issue: 3, Summer 2016
Pages:
329 to 335
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