title: Potent anticancer activity of a new bismuth (III) complex against human lung cancer cells.
abstract: The aim of this work is experimental study of an interesting bismuth(III) complex derived from pentadentate 2,6-pyridinedicarboxaldehyde bis(4N-methylthiosemicarbazone), [BiL(NO3)2]NO3{L=2,6-pyridinedicarboxaldehyde bis(4N-methylthiosemicarbazone)}. A series of in vitro biological studies indicate that the newly prepared [BiL(NO3)2]NO3greatly suppressed colony formation, migration and significantly induced apoptosis of human lung cancer cells A549 and H460, but did not obviously decrease the cell viability of non-cancerous human lung fibroblast (HLF) cell line, showing much higher anticancer activities than its parent ligands, especially with half maximum inhibitory concentration (IC50) <3.5μM. Moreover, in vivo study provides enough evidence that the treatment with [BiL(NO3)2]NO3effectively inhibited A549 xenograft tumor growth on tumor-bearing mice (10mgkg-1, tumor volume reduced by 97.92% and tumor weight lightened by 94.44% compared to control) and did not indicate harmful effect on mouse weight and liver. These results suggest that the coordination of free ligand with Bi(III) might be an interesting and potent strategy in the discovery of new anticancer drug candidates.
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China. Electronic address: ouyangrz@usst.edu.cn.
authors.forename: Ruizhuo
authors.initials: R
authors.lastname: Ouyang
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Cancer Institute, Tongji University School of Medicine, Shanghai 200092, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Tong
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Feng
authors.affiliation: Cancer Institute, Tongji University School of Medicine, Shanghai 200092, China.
authors.forename: Yaoqin
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Cancer Institute, Tongji University School of Medicine, Shanghai 200092, China.
authors.forename: Huihong
authors.initials: H
authors.lastname: Tao
authors.affiliation: Cancer Institute, Tongji University School of Medicine, Shanghai 200092, China.
authors.forename: Xiaoshen
authors.initials: X
authors.lastname: Zhang
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Tianyu
authors.initials: T
authors.lastname: Zong
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Penghui
authors.initials: P
authors.lastname: Cao
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Xiong
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Guo
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China.
authors.forename: Yuhao
authors.initials: Y
authors.lastname: Li
authors.affiliation: University of Shanghai for Science and Technology, Shanghai 200093, China. Electronic address: yqmiao@usst.edu.cn.
authors.forename: Yuqing
authors.initials: Y
authors.lastname: Miao
authors.affiliation: Cancer Institute, Tongji University School of Medicine, Shanghai 200092, China. Electronic address: shuangzhou@tongji.edu.cn.
authors.forename: Shuang
authors.initials: S
authors.lastname: Zhou
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001729:Bismuth / Q000737:chemistry / Q000494:pharmacology*; D001835:Body Weight / Q000187:drug effects; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008099:Liver / Q000187:drug effects; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D015394:Molecular Structure; D009579:Nitrobenzoates / Q000737:chemistry; D011726:Pyridinium Compounds / Q000737:chemistry; D047368:Tumor Burden / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D009579:Nitrobenzoates; D011726:Pyridinium Compounds; C533175:pyridinium 2,4-dinitrobenzoate; D001729:Bismuth
keywords: Anticancer activity; Bi(III) complex; Drug; Human lung cancer; Thiosemicarbazones; in vivo