RESUMEN
Novel structural analogues of the platelet activating factor (PAF), rac-1-octadecyl-2-allyl-glycerol-3-phosphocholine and rac-1-octadecyl-2-allyl-1-thioglycerol-3-phosphocholine , have been synthesized. The phospholipids obtained showed neither PAF-agonistic nor PAF-antagonistic activity at the concentration of 10(-5) to 10(-7) M.
Asunto(s)
Fosforilcolina/química , Factor de Activación Plaquetaria/síntesis química , Humanos , Factor de Activación Plaquetaria/análogos & derivados , Espectrofotometría InfrarrojaRESUMEN
The pro- and anti-inflammatory activity of new structural analogues of the platelet-activating factor (PAF) was studied. It was found that three PAF analogues inhibit PAF-induced rat paw edema in a dose-dependent manner. The anti-inflammatory activity of one of the PAF analogues upon PAF- or carrageenan-induced inflammation was comparable or in some extent exceeded that of dexamethasone.
Asunto(s)
Antiinflamatorios no Esteroideos/uso terapéutico , Factor de Activación Plaquetaria/análogos & derivados , Factor de Activación Plaquetaria/uso terapéutico , Animales , Antiinflamatorios/uso terapéutico , Aspirina/uso terapéutico , Carragenina , Dexametasona/uso terapéutico , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Indometacina/uso terapéutico , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Masculino , Ratas , Ratas EndogámicasRESUMEN
The influence of the phospholipid platelet activation factor (PAF) was studied on PHA-stimulated proliferation of peripheral blood lymphocytes in patients with bronchial asthma and normal subjects. It was found that influencing on the whole population of lymphocytes PAF suppressed proliferation mainly of T-cells. Besides, the influence of PAF on lymphocyte proliferation seemed to be mediated by monocytes since removal of monocytes from the whole population of mononuclear cells abolished the suppression of lymphocyte proliferation induced by PHA. Pretreatment of lymphocytes with PAF antagonist--BL 8705 almost completely blocked the suppression of lymphocyte proliferation induced by PHA.
Asunto(s)
Linfocitos/efectos de los fármacos , Factor de Activación Plaquetaria/farmacología , Adulto , Asma/sangre , División Celular , Células Cultivadas , Femenino , Humanos , Leucocitos Mononucleares/inmunología , Activación de Linfocitos/efectos de los fármacos , Linfocitos/inmunología , Masculino , Linfocitos T/efectos de los fármacos , Linfocitos T/inmunologíaRESUMEN
Phosphatidylcholines bearing 11-methacryloylaminoundecanoyl or 12-keto-10-octadecanoyl residues were synthesized. Both phosphatidylcholines are easily polymerized under UV irradiation. The second phospholipid produces liposomes which, after polymerization, acquire an increased stability to deteriorating factors (organic solvents, detergents and human plasma).