Summary of Drug Effects on Phagocytosis
Drug (IC50 μM) . | . | Target . | . | Concentration . | . | Phagocytosis rate (% of control) . |
---|---|---|---|---|---|---|
Genistein (50) | TK | 250 μM | 100 ± 5 | |||
Staurosporin (.007/.0007) | PKA/PKC | 1 μM | 108 ± 4 | |||
Wortmannin (.005) | PI3K/PI4K | 1 μM | 85 ± 15 | |||
LY294002 (1.4) | PI3K | 100 μM | 105 ± 2 | |||
Isotetrandrine (10) | PLA2 | 30 μM | 100 | |||
Aristolochic acid (40) | PLA2 | 50 μM | 103 ± 2 | |||
ONO RS082 (7) | PLA2 | 3.5 μM | 80 ± 10 | |||
PACOCF3 (15) | PLA2 | 20 μM | 100 ± 10 | |||
Calphostin (.05) | PKC | 0.05 μM | 110 ± 5 | |||
Bisindolylmaleimide (.01) | PKC | 20 μM | 105 ± 2 | |||
*Manoalide (.2/1.5) | PLA2/PLC | 40 μM | 2 ± 2 | |||
9 μM | 50 | |||||
*U73122 (2) | PLC | 25 μM | 4 ± 2 | |||
8 μM | 50 | |||||
U73343 (inactive analog) | 25 μM | 85 | ||||
Okadaic acid (.001/.015) | PP2A, PP1 | 0.3 μM | 98 ± 3 | |||
*BAPTA-AM | Ca2+ | 300 μM | 61 ± 2 | |||
EDTA | Ca2+/Mg2+ | 10 μM | 90 ± 5 | |||
EGTA | Ca2+ | 10 μM | 110 ± 10 |
Drug (IC50 μM) . | . | Target . | . | Concentration . | . | Phagocytosis rate (% of control) . |
---|---|---|---|---|---|---|
Genistein (50) | TK | 250 μM | 100 ± 5 | |||
Staurosporin (.007/.0007) | PKA/PKC | 1 μM | 108 ± 4 | |||
Wortmannin (.005) | PI3K/PI4K | 1 μM | 85 ± 15 | |||
LY294002 (1.4) | PI3K | 100 μM | 105 ± 2 | |||
Isotetrandrine (10) | PLA2 | 30 μM | 100 | |||
Aristolochic acid (40) | PLA2 | 50 μM | 103 ± 2 | |||
ONO RS082 (7) | PLA2 | 3.5 μM | 80 ± 10 | |||
PACOCF3 (15) | PLA2 | 20 μM | 100 ± 10 | |||
Calphostin (.05) | PKC | 0.05 μM | 110 ± 5 | |||
Bisindolylmaleimide (.01) | PKC | 20 μM | 105 ± 2 | |||
*Manoalide (.2/1.5) | PLA2/PLC | 40 μM | 2 ± 2 | |||
9 μM | 50 | |||||
*U73122 (2) | PLC | 25 μM | 4 ± 2 | |||
8 μM | 50 | |||||
U73343 (inactive analog) | 25 μM | 85 | ||||
Okadaic acid (.001/.015) | PP2A, PP1 | 0.3 μM | 98 ± 3 | |||
*BAPTA-AM | Ca2+ | 300 μM | 61 ± 2 | |||
EDTA | Ca2+/Mg2+ | 10 μM | 90 ± 5 | |||
EGTA | Ca2+ | 10 μM | 110 ± 10 |
AX2 cells were preincubated for 15 min in the cold with each drug at the indicated concentrations followed by addition of 1 vol of FITC-labeled bacteria and further incubation for 15 min at 23°C. The mean values of two duplicate experiments and the variation are shown. Control: AX2 in Soerensen phosphate buffer, containing when required the same amount of DMSO. The IC50 values are those reported in the literature or provided by the supplier, and refer to in vitro assays or to activity in mammalian cells.
, drugs with inhibitory activity. Drugs were dissolved in DMSO, except manoalide which was dissolved in ethanol. The final dilution of DMSO varied between 120- and 2,000-fold. Phagocytosis was not affected by DMSO at dilutions above 150-, but was inhibited by 20–30% at a dilution of 100-fold. TK, tyrosine kinase; PKA, protein kinase A; PKC, protein kinase C; PI3K, PI4K, PI3, or PI4 kinase; PLA2: phospholipase A2; PLC, phospholipase C; PP2A, PP1: phospho-protein phophatases 2A and 1.