Microglial activation decreases retention of the protease inhibitor saquinavir: implications for HIV treatment

Table 3 Effect of various pathway activators on [ ³ H]saquinavir accumulation in microglia

Activator	Concentration	Saquinavir transport (% control)
		10 ng/ml LPS^a	Activator alone
TNF-α	10 ng/ml	73 ± 2	98 ± 6
IL-1β	10 ng/ml	77 ± 2	99 ± 2
DEA NONOate	1 μM	61 ± 2	92 ± 5
DEA NONOate	10 μM	61 ± 2	92 ± 4
DEA NONOate	25 μM	61 ± 2	99 ± 6
ET-1	100 nM	61 ± 3	95 ± 2
PMA	1 μM	58 ± 2	94 ± 4
PCN	1 μM	54 ± 2	99 ± 4
PGE₂	1 μM	61 ± 3	103 ± 4

DEA NONOate, 2-(N,N-dimethylamino)-diazenolate-2-oxide; ET-1, endothelin-1; IL-1β, interleukin-1-beta; TNF-α, tumor necrosis factor-alpha; PMA, phorbol-12-myristate-13-acetate; PCN, 5-pregnen-3β-ol-20-one-16α-carbonitrile; PGE_2, prostaglandin E2. ^aIn each separate experiment, 10 ng/ml LPS decreased saquinavir accumulation significantly (^a P < 0.05, statistically significant from untreated controls).

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