title: Synthesis, Characterization and Cytotoxicity of Alkylated Quercetin Derivatives.
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.
authors.affiliation: Clinical Medicine of Seven-year-program, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: Xin-Ran
authors.initials: XR
authors.lastname: Bao
authors.affiliation: College of Pharmacy, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: Han
authors.initials: H
authors.lastname: Liao
authors.affiliation: College of Pharmacy, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: Jiao
authors.initials: J
authors.lastname: Qu
authors.affiliation: College of Pharmacy, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Sun
authors.affiliation: College of Pharmacy, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: Xin
authors.initials: X
authors.lastname: Guo
authors.affiliation: College of Pharmacy, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: En-Xia
authors.initials: EX
authors.lastname: Wang
authors.affiliation: College of Pharmacy, Dalian Medical University, No.9 Lvshun Southern Road, Lvshunkou District, Dalian 116044, P. R. China.
authors.forename: Yu-Hong
authors.initials: YH
authors.lastname: Zhen
keywords: Alkyl derivatives; Cytotoxicity; Quercetin; Selective alkylation