Effects of anti-inflammatory [1, 2, 4]triazolo[4, 3-a] [1, 8]naphthyridine derivatives on human stimulated PMN and endothelial cells: an in vitro study

Table 1 Effect of NF161 and NF177 on PGE₂ and PGI₂ production by Il-1α-treated HUVEC

(a)	PGE₂(pg/well)	6-keto-PGF_1α (pg/well)	(b)	PGE₂ (pg/well)	6-keto-PGF_1α (pg/well)
Control	45 ± 8	797 ± 23	Control	58 ± 18	888 ± 30
IL-1α	280 ± 29	3391 ± 98	IL-1α	275 ± 22	4055 ± 22
NF161 10 ^-4 M	295 ± 31	3508 ± 82	NF161 10 ^-4 M	288 ± 17	3990 ± 38
NF161 10 ^-5 M	285 ± 23	3330 ± 49	NF161 10 ^-5 M	277 ± 28	3885 ± 33
NF161 10 ^-6 M	288 ± 28	3452 ± 74	NF161 10 ^-6 M	280 ± 22	3905 ± 55
NF177 10 ^-4 M	260 ± 21	3660 ± 84	NF177 10 ^-4 M	268 ± 17	3875 ± 42
NF177 10 ^-5 M	277 ± 15	3280 ± 94	NF177 10 ^-5 M	256 ± 22	4005 ± 35
NF177 10 ^-6 M	300 ± 24	3220 ± 77	NF177 10 ^-6 M	292 ± 16	4055 ± 44

1. Effects on PGE₂ and PGI₂ production by simultaneous treatment with IL-1α (10 ng/ml) and NF161 or NF177. Twenty hours later, PGE₂ and the stable metabolite of prostacyclin, 6-keto-PGF_1α, were measured in the sample prepared from the medium by EIA as described in the Materials and Methods section (n = 3).
2. Effects of NF161 and NF177 on PGE₂ and PGI₂ production by pre-induced COX-2. IL-1α (10 ng/ml) was added and incubated for 20 h. The cells were washed and NF161 or NF177 were added for a further 30 min. After incubation, PGE₂ and 6-keto-PGF_1α were measured in the sample prepared from the medium (n = 3)

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