Table 5.
Natural compounds.
| Number | Compound | Structure | Cell-free assay
|
Effects in human blood cells or A549 cells
|
Ref. | ||||
|---|---|---|---|---|---|---|---|---|---|
| IC50 against mPGES-1 | COX-1 | COX-2 | PGE2 | Other COX-1- derived prostanoids‡ | Other COX-2- derived prostanoids§ | ||||
| 16 | Curcumin |
|
0.3 | NI† | NI | Decrease in LPS-stimulated HWB‡(EC50= 15 μM) | Decrease in 12-HHT in unchallenged HWB (EC50= 19 μM) | Decrease in β6-keto in LPS-stimulated PGF1α HWB only at higher dose (30 μM) | [82] |
|
| |||||||||
| 17 | EGCG |
|
1.8 | IC50> 30 μM |
NI | Decrease in LPS-stimulated HWB (EC50> 30 μM) | ND | No effect on 6-keto and 12-HHT in PGF1α LPS-stimulated HWB (at 30 μM) | [83] |
|
| |||||||||
| 18 | Garcinol |
|
0.3 | IC50= 12 μM | NI | Decrease in IL-1β-stimulated A549 cells (EC50 ~10 μM) Decrease in LPS- stimulated HWB (EC50= 30 μM) |
Decrease in 12-HHT (EC50= 11 μM) and TXB2 (EC50 = 16 μM) in unchallenged human platelets No effect on 12-HHT in unchallenged HWB (up to 33 μM) |
No effect on 6-keto PGF1αin IL-1β-stimulated A549 cells (up to 33 μM) No effect on 6-keto PGF1αin LPS- stimulated HWB (up to 30 μM) | [84] |
|
| |||||||||
| 19 | Myrtu-commulone |
|
1 | IC50> 15 μM | NI | Decrease in IL-1β-stimulated A549 cells (EC50= 30 μM) Decrease in LPS-stimulated HWB |
No effect on 12-HHT in unchallenged HWB (up to 33 μM) | No effect on 6-oxo PGF1αin IL-1β-stimulated A549 cells (up to 33 μM) | [85] |
|
| |||||||||
| 20 | Arzanol |
|
0.4 | IC50= 17.5 μM | NI | Decrease in LPS-stimulated human monocyte (EC50= 9 μM) Decrease in LPS-stimulated HWB (EC50 ~30 μM) |
Decrease in 12-HHT (EC50= 2.3 μM) and TBA2 (EC50= 2.9 μM) in unchallenged human platelets | Decrease in β6-keto PGF1αin IL-1β-stimulated A549 cells moderately (EC50≥ 30 μM) No effect on TXB2 and 6-keto PGF1αin LPS- stimulated HWB (at 30 μM) | [86] |
|
| |||||||||
| 21 | Boswellic acids | (AKBA)
|
3 | ND | ND | Decrease in IL-1β-stimulated A549 cells (EC50 = 20–30 μM) Only β-BA decreases LPS- stimulated HWB (EC50= 10 μM) | β-BA: No effect on 12-HHT in unchallenged HWB (at 50 μM) | No effect on 6-keto PGF1αin IL-1β-stimulated A549 cells (at 30 μM) No effect on 6-keto PGF1α and TXB2in LPS- stimulated HWB (at 10 μM) | [87] |
| 22 | (β–BA)
|
5 | ND | ND | |||||
| 23 | (KBA)
|
10 | ND | ND | |||||
|
| |||||||||
| 24 | Hyperforin |
|
1 | IC50= 12 μM | NI | Decrease in LPS- stimulated HWB (EC50 ~3 μM) Decrease in AA- stimulated HWB (EC50= 0.25 μM) | No effect on 12-HHT in unchallenged HWB (up to 33 μM) | No effect on 6-keto PGF1α and TXB2in LPS- stimulated HWB (up to 30 μM) No effect on 6-keto PGF1αin AA-stimulated HWB (up to 30 μM) | [88] |
†
NI: No significant inhibition up to 30 or 33 μM.
‡
COX-1-derived prostanoids are measured in HWB or COX-1 expressing human platelets stimulated with Ca2+-inophore plus AA, but not challenged by LPS.
§
COX-2-derived prostanoids are measured in LPS-stimulated HWB or IL-1b-stimulated A549 cells (low COX-1 and induced COX-2).
AKBA: 3-O-acetyl-11-keto-β-boswellic acid; β-BA: β-boswellic acid; HWB: Human whole-blood; KBA: 11-keto-β-boswellic acid; ND: Not determined.