Table 1 The antagonistic activities of NSAIDs against Farnesoid X Receptor (FXR) using yeast two hybrid assays

From: FXR antagonism of NSAIDs contributes to drug-induced liver injury identified by systems pharmacology approach

Classification

Drug name

FXR activation (10 μM)

FXR inhibition (10 μM)

IC50 (μM)

Salicylates

Aspirin

1.12

41.68%

NS

 

Diflunisal

1.31

93.32%

8.48

Propionic acid derivatives

Ibuprofen

1.27

96.20%

1.08

 

Fenoprofen

1.27

63.35%

5.59

 

Flurbiprofen

1.65

94.98%

0.78

Acetic acid derivatives

Indomethacin

0.99

66.27%

5.76

 

Diclofenac

1.24

88.66%

1.71

Enolic acid derivatives(Oxicams)

Piroxicam

1.13

30.69%

NS

 

Tenoxicam

1.05

16.90%

NS

Selective COX-2 inhibitors (Coxibs)

Celecoxib

1.12

28.30%

NS

 

Rofecoxib

1.18

39.90%

NS

Pyrazolones

Phenylbutazone

0.99

91.88%

0.7

Control

GS

ND

60.72%

6.47

 

CDCA

2.7

ND

ND

 

DMSO

1

0

ND

  1. Data represents average values of at least triplicate measurements determined by yeast two hybrid assays. This system employs the interaction between hFXR-LBD and the coactivator SRC1. The inhibition rate (%) was calculated using the equation: [(GACDCA-GAtreated)/(GACDCA-GADMSO)] × 100%, GA indicates α-galactosidase activity. Attempts to determine IC50 values were made if the inhibition rate at 10 μM was larger than 50%. ND: not determined. NS: not significance, IC50 > 25 μM.
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