RESUMO
The 1-O-stearoyl-2-O-[3H] arachidonyl-sn-glycero-3-phosphocholine, introduced in the culture medium, was taken up by the peritoneal macrophages activated by the ionophore A 23187. After intracellular phospholipase A2 activity, the [3H] arachidonic acid was found in cells and in extracellular fluids. It also reached the eicosanoid synthesis. When it was introduced in the culture medium with the tritiated phospholipid, the 1, 2 di-O-hexadecyl-rac-glycero-3-phosphocholine, which has a non hydrolysable alkylated structure in the 2 position of the glycerol, inhibited the intracellular phospholipase A2, then contributed to lower the eicosanoid synthesis.
Assuntos
Macrófagos/enzimologia , Cavidade Peritoneal/citologia , Fosfolipases A/metabolismo , Éteres Fosfolipídicos/farmacologia , Fosfolipídeos/farmacologia , Animais , Calcimicina/farmacologia , Eicosanoides/biossíntese , Ácidos Graxos não Esterificados/biossíntese , Masculino , Fosfolipases A/antagonistas & inibidores , Fosfolipases A2 , Ratos , Ratos WistarAssuntos
Anti-Inflamatórios não Esteroides/farmacologia , Benzamidas/farmacologia , Química Encefálica/efeitos dos fármacos , Edema Encefálico/metabolismo , Dinoprostona/metabolismo , Animais , Benzamidas/administração & dosagem , Inibidores de Ciclo-Oxigenase , Dinoprostona/análise , Masculino , Ratos , Ratos EndogâmicosRESUMO
A new synthesis is proposed for cordiachromene A (CCA), a bioactive component of the ascidian Aplidium antillense Gravier, using a method producing a racemic mixture. The anti-inflammatory activities of a natural extract and a chemically synthetic form of CCA were assessed in vivo by carrageenan-induced rat-paw edema. The activity of synthetic CCA was confirmed by a test on kaolin-induced granuloma in the rat. Strong activities were measured for both CCA, but comparison of results of the first test suggests that only the natural optically active isomer has an anti-inflammatory effect. CCA is similar to indomethacin in its effect on carrageenan-induced rat-paw edema and ten times as active as phenylbutazone.