| 19551737 |
Kovala-Demertzi D, Hadjipavlou-Litina D, Primikiri A, Staninska M, Kotoglou C, Demertzis MA: Anti-inflammatory, antiproliferative, and radical-scavenging activities of tolfenamic acid and its metal complexes. Chem Biodivers. 2009 Jun;6(6):948-60.
Some new complexes of tolfenamic acid (=2-[(2-methyl-3-chlorophenyl) amino] benzoic acid; Htolf) with potentially interesting biological activities are described. The complexes [Mn (tolf)(2)(H (2) O)(2)], [Co (tolf)(2)(H (2) O)(2)], [Ni (tolf (2)(H (2) O)(2)], [Cu (tolf)(2)(H (2) O)](2), and [Zn (tolf)(2)(H (2) O)] were prepared by the reaction of tolfenamic acid, a potent anti-inflammatory drug, with metal salts. The radical-scavenging activities of the complexes were evaluated using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical-scavenging assay. Their ability to inhibit soybean lipoxygenase, beta-glucuronidase, and trypsin-induced proteolysis was studied. Their inhibitory effects on rat paw edema induced by carrageenin was studied and compared with those of tolfenamic acid. The complex [Zn (tolf)(2)(H (2) O)] exhibited the strongest in vivo inhibitory effect at 0.1 mm/kg Body Weight (BW; 93.0+/-0.9%), superior than the inhibition induced by tolfenamic acid at the same molar dose (76.0+/-0.9%). Tolfenamic acid and its metal complexes have been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), and A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The complexes [Mn (tolf)(2)(H (2) O)(2)] and [Cu (tolf)(2)(H (2) O)](2) have shown selectivity against T24 cell line. The IC (50) values of these two complexes against T24 cancer cell lines are in a micromolar range similar or better to that of the antitumor drug cisplatin. |
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