Effect of CH-123, a pyrido (1,2-a) pyrimidine derivative on the elevated activity of lysosomal enzymes of rabbit aorta and liver in experimental atherosclerosis

2区 · 医学

Article

作者: S. Viral ; G.G. Ecsedi ; E.J. Hidvégi

The effect of CH-123 (3-carbethoxy-6-methyl-1-9-(carboxy-methyl)-1-4-oxo-6,7,8,9-tetrahydro-4H-pyrid o(1,2a)pyrimidine) was investigated on the activity of 4 lysosomal enzymes: beta-glucuronidase, beta-galactosidase, N-acetyl-beta-glucosaminidase and acid phosphatase obtained from aortic smooth muscle and liver cells of rabbits. Animals were fed on a 2% cholesterol diet for 4 weeks and used an experimental atherosclerotic group. In drug-treated groups, after 4 weeks of cholesterol feeding the diet was changed to regular food and the animals were treated daily either with 50 mg/kg CH-123 or with 250 mg/kg Clofibrate. The postnuclear supernatant of homogenates of liver and aortic cells was isolated, lysosomes were fractionated by sucrose density gradient centrifugation, and the activity of enzymes was measured. In cholesterol-fed animals the enzyme activities of aorta and liver was 3-5 times higher than in the control, i.e. in the group of rabbits fed regular food. On Clofibrate treatment the enzyme activities were 2-3 times higher, but on treatment with CH-123, they were only 1.2-1.8 times above the control. Experiments suggest that CH-123 treatment suppresses the elevated lysosomal marker enzyme activities in aortic and liver cells of atherosclerotic animals.

1979-01-01·Arzneimittel-Forschung

The effect of some pyrimido-pyrimidine derivatives on blood coagulation and platelet aggregation.

Article

作者: Blaskó, G ; Pálos, L A ; Bédi, J

Two pyrimido-pyrimidine derivatives, Chinoin 105 and Chinoin 123, respectively, were investigated with respect to the inhibition potency on platelet aggregation. It was shown that Chinoin 105 is a powerful inhibitor of aggregation of thrombocytes without effect on routine coagulation parameters in vitro. Chinoin 123 has a moderately inhibitory effect on the investigated reactions. An additive effect of Chinoin 105 to the inhibitory potential of PGE1 on platelet aggregation was proven.

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