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.

New Palladium(II) and Platinum(II) Complexes Based on Pyrrole Schiff Bases: Synthesis, Characterization, X-ray Structure, and Anticancer Activity

“…In this way, the sterically bulky groups shield the labile ligands, therefore reducing the rate of hydrolysis and substitution long enough for the complexes to bind to the desired target. Second, the trans-geometry complexes have not been widely explored as anticancer agents despite literature reports that they could exhibit cytotoxicity equivalent to or greater than that of cisplatin. − …”

Synthesis, characterization, spectroscopic studies and biological evaluation of Schiff bases derived from 1–hydroxy-2-acetonapthanone

“…Schiff bases contains azomethine (-C=N-) linkage and are usually derived by the condensation of carbonyl compounds (aldehydes/ketones) with primary aliphatic/aromatic/heteroaromatic amines. Schiff bases are known for their antitumor [1, 2, 3, 4, 5, 6, 7, 8], antifungal [9, 10, 11, 12, 13], antiviral [14], antibacterial [9, 10, 11, 12, 15, 16, 17] and anticancer [18, 19] activities. Schiff bases find many applications including acid catalyst [20, 21, 22, 23], reduction catalyst [24, 25], oxidation catalyst [26, 27, 28, 29, 30, 31], dye [32, 33] and it also exhibit special liability towards metal ions [34, 35, 36, 37].…”

Synthesis and characterization of new Schiff base derived from 2-amino-5-(substituted phenyl) thiadiazole, substituted aromatic aldehyde and acetyl acetone

“…Mostly, Schiff bases containing azomethine (-C=N-) type of linkage which introduces condensation reaction of carbonyl compound such as aldehydes & ketones with primary aliphatic or aromatic amines. Schiff bases are well known for their antitumor, antifungal, antiviral, antibacterial, and antiinflammatory activity [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19] . Today researchers are very much interested to make various types of heterocyclic compounds with help of universal multicomponent route which is more economic, affordable and simple one for the synthesis in one pot manner (without intermediate formation).…”