title: Synthesis, characterization and anticancer activity of kaempferol-zinc(II) complex.
abstract: According to the previous studies, the anticancer activity of flavonoids could be enhanced when they are coordinated with transition metal ions. In this work, kaempferol-zinc(II) complex (kaempferol-Zn) was synthesized and its chemical properties were characterized by UV-VIS, FT-IR, (1)H NMR, elemental analysis, electrospray mass spectrometry (ES-MS) and fluorescence spectroscopy, which showed that the synthesized complex was coordinated with a Zn(II) ion via the 3-OH and 4-oxo groups. The anticancer effects of kaempferol-Zn and free kaempferol on human oesophageal cancer cell line (EC9706) were compared. MTT results demonstrated that the killing effect of kaempferol-Zn was two times higher than that of free kaempferol. Atomic force microscopy (AFM) showed the morphological and ultrastructural changes of cellular membrane induced by kaempferol-Zn at subcellular or nanometer level. Moreover, flow cytometric analysis indicated that kaempferol-Zn could induce apoptosis in EC9706 cells by regulating intracellular calcium ions. Collectively, all the data showed that kaempferol-Zn might be served as a kind of potential anticancer agent.
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, PR China.
authors.forename: Lv-Ying
authors.initials: LY
authors.lastname: Tu
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicines, Macau University of Science and Technology, Macau 000853, PR China.
authors.forename: Jiang
authors.initials: J
authors.lastname: Pi
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicines, Macau University of Science and Technology, Macau 000853, PR China.
authors.forename: Hua
authors.initials: H
authors.lastname: Jin
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, PR China; State Key Laboratory of Quality Research in Chinese Medicines, Macau University of Science and Technology, Macau 000853, PR China.
authors.forename: Ji-Ye
authors.initials: JY
authors.lastname: Cai
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, PR China. Electronic address: tspdeng@jnu.edu.cn.
authors.forename: Sui-Ping
authors.initials: SP
authors.lastname: Deng
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D044949:Kaempferols / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship; D015032:Zinc / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D044949:Kaempferols; D009942:Organometallic Compounds; C006552:kaempferol; D015032:Zinc
keywords: Apoptosis; Atomic force microscopy; EC9706; Kaempferol-Zn; Spectroscopic analysis