copper(II) complexes Dotaz Zobrazit nápovědu
Na karagenínovom edéme na potkanoch bola hodnotená protizápalová aktivita jednojadrových akva-(krezoxyacetáto)meďnatých komplexov zloženia [Cu(ROCH2COO)2(H20)n] (R = 2- a 3-metylfenyl, n = 2; 4-metylfenyl (n = 3), ako aj dvojjadrových fenazón-(o-, m-,p-krezoxyacetáto)meďnatých komplexov zloženia [Cu2(ROCH2COO)4(fzn)2l (fzn = fenazón). Účinok testovaných komplexov sa porovnával navzájom a s voľnými kyselinami. Kyselina salicylová a jej meďnatá soľ (tetrahydrát) boli použité ako porovnávacie štandardy. Všetky zlúčeniny boli aplikované i.p. v jednorazovej dávke 50 μmol/kg (počítané na karboxylátový fragment). Vo všeobecnosti všetky Cu(II)-komplexy boli účinnejšie (71-88 %) ako príslušné volné izomérne kyseliny krezoxyoctové (47, 37, 45 %), s výnimkou diakva-bis(o-krezoxyacetáto)mednatého komplexu (43 %). Rovnako tetrahydrát salicylanu mednatého (57 %) a kyselina salicylová (41 %) boli menej aktívne. Zistená aktivita komplexov je diskutovaná vo vzťahu k ich štruktúre.
In groups of mononuclear aqua(cresoxyacetato)copper(II) complexes of the composition [Cu(ROCH2COO)2(H20)nl (R= 2- and 3-methylphenyl, n = 2; 4-methylphenyl, n =3) and binu- clear phenazone(o-, m-, p-cresoxyacetato)copper(II) complexes of the composition [Cu2(ROCH2COO)4(phz)2l the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. The effects of the complexes were compared with each other and with those of the free acids. Salicylic acid and its cupric salt (tetrahydrate) were used as standards of comparison. All compounds were applied i.p. in a single dose of 50 μmol/kg body weight (calculated for the RCOO-fragment). In general, all Cu(II) complexes tested were clearly more effective (71-88 %) than the corresponding free isomeric cresoxyacetic acids (47, 37, 45 %), with the exception of diaquabis(o-cresoxyacetato)copper(Il) complex (43 %). Copper(II) salicylate tetrahydrate (57 %) and salicylic acid (41 %) were less active, too. The observed activities of complexes are discussed in relation to their structures.
V skupine dvojiadrových meďnatých komplexov zloženia [Cu2(RCOO)4(H2O)2] {R = 2,4-diacetoxyfenyl (I), 2,5-diacetoxyfenyl (II) a 2,6-diacetoxyfenyl (III)} bola hodnotená protizápalová aktivita na karagenínovom edéme na potkanoch. Ako porovnávacie štandardy boli použité: tetrahydrát salicylanu meďnatého (IV) a kyselina salicylová. Všetky zlúčeniny boli podané i.p. v dávke 50 μnol/kg, počítané na R-COO-fragment. Testované meďnaté komplexy boli zjavne účinnejšie ako príslušné voľné diacetoxybenzoové kyseliny, s výnimkou 2,5-diacetoxyderivátu. Priemerná hodnota protizápalovej aktivity meďnatých komplexov klesá v poradí: III (71,0 %) = I (70,6 %) > IV (57,4 %) salicylovej (44,9 %). Vzťah medzi koordinačno-chemickými vlastnosťami a biologickým účinkom testovaných komplexov je diskutovaný.
In a group of binuclear copper (11) complexes of the composition [Cu2(RCOO)4(H20)2] (R = 2,4-(diacetoxyphenyl (1), 2,5-diacetoxyphenyl (II) and 2,6-diacetoxyphenyl (III)), the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. Copper (II) salicylate tetrahydrate (IV) and salicylic acid were used as standards for comparison. All compounds were applied i.p. in a single dose of 50 μmol/kg body weight, calculated for the R-COO-fragment. The Cu(II) complexes tested were clearly more effective than the corresponding free diacetoxybenzoic acids, with an exception for the 2,5-diacetoxy derivative. The average anti-inflammatory activities of copper (II) complexes were decreasing in the following order: III (71.0 %)«(70.6 %) > IV (57.4 %) > II (18.0 %). Of the acids, only 2,6-diacetoxybenzoic acid (45.2 %) was effective at the level of salicylic acid (44.9 %). The relationship between the coordination-chemical properties and the biological effects of the complexes tested is discussed.
Genotoxická aktivita dvojjadrových [Cu2(RCOO)4(N-oxide)2] komplexov (R = 2-chlórfenoxymetyl) bola testovaná voči kmeňom Salmonella typhimurium (TA97, TA100 a TA102) Amesovou metódou in vitro a porovnávaná s aktivitou volných N-oxidov - 4-nitrochinolín-N-oxidom, 4-nitropyridín-N-oxidom a 2-metyl-4-nitropyridín-N-oxidom. Komplexáciou 4-nitrochinolín-N-oxidu s bis(2-chlórfenoxyacetáto)meďnatým fragmentom bol redukovaný jeho mutagénny účinok (9-krát, vzťahované na obsah N-oxidu). V prípade 4-nitropyridín-N-oxidu, 2-metyl-4-mtropyridín-N-oxidu a ich bis(N-oxid)-tetrakis (2-chlórfenoxyacetáto)mednatých komplexov nebol tento fenomén pozorovaný.
Using Ames method in vitro, the genotoxic activity of binuclear [Cu2(RCOO)4(N-oxide)2] complexes (R = 2-chlorophenoxymethyl) was tested against the strains of Salmonella typhimurium (TA97, TA100 and TA102) and compared to that of the free N-oxides - 4-nitroquinoline N-oxide, 4-nitropyridine N-oxide and 2-methyl-4-mtiopyridine N-oxide. Complexation of 4-nitroquinohne N-oxide with bisC2-chlorophenoxyacetato)copper(II) fragment reduced its mutagenic effect (9-times, correlated with N-oxide content). In the case of 4-nitropyridine N-oxide, 2-methyl-4-nitropyridine N-oxide and their bis(N-oxide)tetrakis(2-chlorophenoxyacetato)copper(II) complexes this phenomenon was not observed.
- MeSH
- 4-nitrochinolin-1-oxid aplikace a dávkování MeSH
- chlorfenoly analogy a deriváty aplikace a dávkování MeSH
- měď analogy a deriváty aplikace a dávkování MeSH
- organokovové sloučeniny aplikace a dávkování MeSH
- Salmonella typhimurium MeSH
- techniky in vitro MeSH
- testy genotoxicity MeSH
- testy toxicity MeSH
