title: Antitumor activity of a Trans-thiosemicarbazone schiff base palladium (II) complex on human gastric adenocarcinoma cells.
abstract: The development of transition-metal-based antitumor drug candidates increases the metallopharmaceuticals study dramatically. Two trans-thiosemicarbazone-based, Schiff base palladium (Pd) (II) complexes, DMABTSPd (TSPd) and DMABPTSPd (PTSPd), were prepared and characterized as described in our previous study. Here, we investigated whether the two complexes have antitumor effect on human gastric adenocarcinoma cell lines, BGC-823 and SGC-7901, compared with normal human gastric mucosal epithelial cell line, Ges-1. The results show that the Pd complex with the bare amino group (DMABTSPd(TSPd)) can inhibit cell viabilities and induce apoptosis in human gastric carcinoma cells, rather than the Pd complex without the bare amino group (DMABPTSPd (PTSPd)). This occurs via a mitochondrial-related pathway by down-regulating the level of Bcl-2 expression and up-regulating the level of Bid expression. Meanwhile, DMABTSPd (TSPd) suppressed tumor growth via a mitochondrial-related pathway in a nude mouse tumor xenograft model derived from BGC-823 cells. These findings demonstrate that DMABTSPd (TSPd) is worthy of further structural optimization and representing a promising Pd complex for the development of a new antitumor therapeutic agent.
authors.affiliation: School of Medicine, University of Xiamen, Xiamen, 361102, P. R. China.
authors.forename: Bingchang
authors.initials: B
authors.lastname: Zhang
authors.affiliation: School of Medicine, University of Xiamen, Xiamen, 361102, P. R. China.
authors.forename: Haiqing
authors.initials: H
authors.lastname: Luo
authors.affiliation: College of Chemistry and Chemical Engineering, University of Xiamen, Xiamen, 361005, P. R. China.
authors.forename: Qinjuan
authors.initials: Q
authors.lastname: Xu
authors.affiliation: College of Chemistry and Chemical Engineering, University of Xiamen, Xiamen, 361005, P. R. China.
authors.forename: Lirong
authors.initials: L
authors.lastname: Lin
authors.affiliation: School of Medicine, University of Xiamen, Xiamen, 361102, P. R. China.
authors.forename: Bing
authors.initials: B
authors.lastname: Zhang
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000473:pathology; D000818:Animals; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D005260:Female; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010165:Palladium / Q000737:chemistry / Q000494:pharmacology*; D012545:Schiff Bases; D013274:Stomach Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013882:Thiosemicarbazones / Q000737:chemistry / Q000494:pharmacology*; D023041:Xenograft Model Antitumor Assays
chemical_list: D056831:Coordination Complexes; D012545:Schiff Bases; D013882:Thiosemicarbazones; D010165:Palladium
keywords: a nude mouse tumor xenograft model; antitumor activity; human gastric adenocarcinoma cells; trans-thiosemicarbazone Schiff base palladium (II) complex