Abstract
Metal complexation in general improves the biological properties of ligands. We have previously measured the anticancer effects of the oxidovanadium(IV) cation with chrysin complex, VO(chrys)2. In the present study, we synthesized and characterized a new complex generated by the replacement of one chrysin ligand by phenanthroline (phen), VO(chrys)phenCl, to confer high planarity for DNA chain intercalation and more lipophilicity, giving rise to a better cellular uptake. In effect, the uptake of vanadium has been increased in the complex with phen and the cytotoxic effect of this complex proved higher in the human lung cancer A549 cell line, being involved in its mechanisms of action, the production of cellular reactive oxygen species (ROS), the decrease of the natural antioxidant compound glutathione (GSH) and the ratio GSH/GSSG (GSSG, oxidized GSH), and mitochondrial membrane damage. Cytotoxic activity studies using the non-tumorigenic HEK293 cell line showed that [VO(chrys)phenCl] exhibits selectivity action towards A549 cells after 24 h incubation. The interaction with bovine serum albumin (BSA) by fluorometric determinations showed that the complex could be carried by the protein and that the binding of the complex to BSA occurs through H-bond and van der Waals interactions.
Highlights
Chrysin (Scheme 1) is a natural polyphenol with several biological activities, such as antioxidant, anticancer, antiviral, and neuroprotective
These results suggest that the metal ion is interacting with chrysin through C=O and the deprotonated C(5)–O group and with the N atoms of phen
It is known that once the complex is added to living cells, it could undergo several chemical interactions with the oxidant and antioxidant cellular systems, including ligand release, but the differences in the anticancer effect between the free ligands and the vanadium complex could demonstrate the efficacy of the vanadium compound
Summary
Chrysin (Scheme 1) is a natural polyphenol with several biological activities, such as antioxidant, anticancer, antiviral, and neuroprotective. SchemeW1.eDhraawveopf rtehveisoturusclytusrteuodficehdrythsien.anticancer behavior of chrysin and chrysin oxidovanadium(IV) metal complex on osteoblast like cells [5], breast cancer cells [6], and human lunWgeAh5a4v9ecapnrceevriocuelsllsy[7s]tuadnidedshtohweeadntthicaatnccoemr pbleehxaavtiioonr iomf pcrhorvyesidnthaendbiochlorgyiscianl eofxfie-cts doovfanthaedpiuomly(pIVh)enmoel.taTlhceomseplelecxtioonn oofsttehoebhlaestet rliokceyccelilclsb[a5s]e, bprheeanstancathnrcoelrinceell(sp[h6e]n, a) nindchluud-ed maans lausnegcoAn5d49ligcaanndceirscreelllaste[7d] taontdheshfoawctetdhatthpatlacnoamr plilgeaxnadtisoncoiomrpdrinoavteeddtthoembeiotalolsgiccoaul ld effbecintsdoDf tNhAe ptohlryopuhgehnionlt.eTrhcaelasetiloenctitoonboafsethpeahirest,eirmocpyrcolvicinbgastehephaenntiacnatnhcreorlianceti(opnhoenf )biinn-ary clucdoemdpalesxaes,eacsonwdellligaasncdonifserelliaptoepdhtiolictihtey ftaoctthtehcaotmplpaonuanrdlisg[a8n].dOs ncolyoradfienwatteedrntaormy cehtarlyssin coumldetbalincdomDpNleAxeths rwouergehrienptoercteadlaatinodn thoebGasae(IpIIa)i,rCs,ui(mIIp),raonvdinRguth(IeI)a-cnhtircyasnince-arnaccitliloanryoafrobinmarayticocmhepllaetxoers,saysstwemellsapsrcoovnefdermlioproepchyiltioctitoyxitco thaencofmrepeocuhnrydssin[8]i.nOdniflyfearefnewt ctaenrcnearrycell chrliynseins [m9–e1t1a]l.complexes were reported and the Ga(III), Cu(II), and Ru(II)-chrysin-ancillary aroImn athtiec chuerrlaetnotrwsyosrtke,mwsepdroesviegdnmthoerehectyetrootloexpicticth[aVnOf(rcehercyhsr)ypshineninCld]icffoemrepnltecxaanicmering celtloliennehsa[n9–c1e1t]h.e biological behavior of the VO(chrys) complex.
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