Effect on CYPs and prostaglandin activity

Author

Test System

Exposure

Characterisation of test substance

Main outcome measure

Outcome

Dugasani et al., 2010

Mouse leukaemic monocyte (RAW 264.7)
 macrophages and human polymorphonuclear neutrophils (PMN).

1, 3 and 6 uM.

[6]-gingerol, [8]-gingerol, [10]-gingerol
 and [6]-shogaol.

compare the antioxidant and antiinflammatory
 activities of gingerols and their natural analogues to determine their structure–activity
 relationship and molecular mechanisms.

Dose dependant inhibition of activated PGE2 release. Inhibition reached 58, 66, 73 and 87%, respectively, at 6uM.

Jolad et al., 2004

HL-60 cells.

Not specified.

ginger constituents: gingerols, shogaols, 3-dihydroshogaols, gingerdiols.

Effects of ginger components on LPS-induced PGE2 production.

No cytotoxicity demonstrated.

Jolad et al., 2005

HL-60 cells.

Not specified.

Ginger constituents containing gingerols, shogaols, 3-dihydroshogaols, gingerdiols.

Effects of ginger components on LPS-induced PGE2 production.

Inhibition of LPS-stimulated
 PGE2 production (IC50 = 0.05 0.08 ug/ml) with Gingerol fractions. 

Kim et al., 2012

Human liver microsomes.

0.05–5 ug/ml.

Aqueous ethanolic ginger extract (30% EtOH).

Inhibitory effect on CYP450-mediated drug metabolism. 

Concentration-dependent
 inhibitory effects on CYP2C19; IC50 value of 3.8 g/ml.

Kimura et al., 2010;

Human CYP3A4 and CYP2C9 microsomes.

Not specified.

 NA

Inhibitory effect on CYP3A4 and CYP2C9 activity.

significant inhibition of CYP3A4 IC50 5.1u g/ml or CYP2C9 IC50 (10ug/ml) activity.

Lantz et al., 2007

U937 cells

0.1 ug/ml for 6 hrs.

Ginger extract and mixtures of 6-, 8- 10-gingerols and 6-, 8-, 10-shogaols.

Effect on inflammatory
 mediator production.

No effect on COX-2 expression.

Mukkavilli et al., 2014

Human liver microsomes.

Ginger extract: 500 mg/ml (containing 15 mg/
 ml 6G, 3.4 mg/ml 8G, 3.9 mg/ml 10G, 3.0 mg/ml 6S); All
 individual components of gingerols assessed at 100 mg/mL
 (equivalent to 29 mg/ml 6G, 32 mg/ml 8G, 35 mg/ml 10G and
 28 mg/ml of 6S).

Ginger extract: (containing 6-Gingerol, 8-Gingerol, 10-Gingerol, 6-Shogaol). All
 individual components of gingerols were assessed at 100 mg/mL
 equivalent to 29 mg/mL 6G, 32 mg/mL 8G, 35 mg/mL 10G and
 28 mg/mL of 6S.

effect of ginger extract and major 
 constituents on CYP P450 enzyme activity. 

Inhibition of CYP1A2 (IC50 -
 221.5 mg/ml) by ginger extract. No effect on CYP2A6; maximum inhibition on CYP2B6: IC50
 - 22 mg/ml; IC50 - 122.5 mg/mL against CYP2C8
 in the presence of amodiaquine; IC50 - 93.5 mg/mL against CYP2C9,
 in the presence of diclofenac; Inhibition of CYP3A in the presence of testosterone: no effect in the presence of midazolam.