Inhibitor | Description | IC50 | Ki | Mode of Inhibition | Test System | Marker Reactiona | References |
---|---|---|---|---|---|---|---|
µM (µg/ml) | µM (µg/ml) | ||||||
3-Isomangostin | Constituent of mangosteen | 0.64 | 0.66 | Competitive | HLM | Pacli | Foti et al., 2009 |
6-Gingerol | Constituent of ginger root | (6.5) | HLM | Amo | Mukkavilli et al., 2014 | ||
6-Prenylnaringenin | Prenylflavonoid | 1.9 | HLM | Amo | Yuan et al., 2014 | ||
6-Shogaol | Constitutent of ginger root | (0.8) | HLM | Amo | Mukkavilli et al., 2014 | ||
8-Desoxygartanin | Constituent of mangosteen | 1.85 | 2.80 | Competitive | HLM | Pacli | Foti et al., 2009 |
8-Gingerol | Constituent of ginger root | (0.7) | HLM | Amo | Mukkavilli et al., 2014 | ||
8-Prenylnaringenin (flavaprenin) | Prenylflavonoid | 0.6 | HLM | Amo | Yuan et al., 2014 | ||
9-Hydroxycalabaxanthone | Constituent of mangosteen | 14.1 | HLM | Pacli | Foti et al., 2009 | ||
10-Gingerol | Constituent of ginger root | (0.7) | HLM | Amo | Mukkavilli et al., 2014 | ||
11-Keto-β-boswellic acid | Triterpene | 9.5 | HLM | Pacli | Frank and Unger, 2006 | ||
Acetyl-α-boswellic acid | Triterpene | 65.8 | HLM | Pacli | Frank and Unger, 2006 | ||
Acetyl-β-boswellic acid | Triterpene | 33.4 | HLM | Pacli | Frank and Unger, 2006 | ||
Acetyl-11-keto-β-boswellic acid | Triterpene | 10.1 | HLM | Pacli | Frank and Unger, 2006 | ||
Allocryptopine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Arachidonic acid | Endogenous compound | 7 | Competitive | rCYP2C8 | Pacli | Yamazaki and Shimada, 1999 | |
β-Boswellic acid | Triterpene | 8.7 | HLM | Pacli | Frank and Unger, 2006 | ||
Bo-yang-hwan-o-tang | Oriental herbal medicine | (17,209) | HLM | Pacli | Lee et al., 2012b | ||
BST204 | Dry extract of ginseng | (17.4) | HLM | Rosi | Zheng et al., 2014 | ||
Capnoidine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Cedrol | Sesquiterpene | 41.0 | HLM | Amo | Jeong et al., 2014 | ||
Corybulbine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Corycavamine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Corycavidine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Corydaline | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Corypalmine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Cranberry (powder) | Natural product | (24.7) | HLM | Amo | Albassam et al., 2015 | ||
(24.0) | HLM | Pio | Albassam et al., 2015 | ||||
Cryptopine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
β-Cryptoxanthin | Carotenoid pigment | 13.8 | HLM | Pacli | Zheng et al., 2013 | ||
Cudratricusxanthone | Constituent of Cudrania tricuspidata | 4.69 | 2.2 | Noncompetitive | HLM | Pacli | Sim et al., 2015 |
Curcumin | Diarylheptanoid | 129.7 | rCYP2C8 | DBF | Mach et al., 2010 | ||
DA-9801 | Extract | (449.9) | HLM | Amo | Ji et al., 2013 | ||
Dioscorea nipponica | Extract | (237.1) | HLM | Amo | Ji et al., 2013 | ||
Diosmetin | Flavonoid | 3.13 | Mixed | HLM | Pacli | Quintieri et al., 2011 | |
Ellagic acid | Constitutent of guava leaf | (13.99) | rCYP2C8 | DBF | Kaneko et al., 2013 | ||
(−)-Epigallocatechin-3-gallate | Catechin | 10.9 | 6.8 | Competitive | HLM | Amo | Misaka et al., 2013 |
Eupatilin | Flavone | 104.9 | 101.9 | Competitive | HLM | Amo | Ji et al., 2010 |
Feverfew herb | Natural product | (104–126) | rCYP2C8 | Pacli | Unger and Frank, 2004 | ||
Fisetin | Flavonol | 10.8 | 1.3–6.0 | Mixed | HLM | Pacli | Václavíková et al., 2003 |
Gartanin | Constituent of mangosteen | 6.28 | HLM | Pacli | Foti et al., 2009 | ||
Ginger extract | Extract | (122.5) | HLM | Amo | Mukkavilli et al., 2014 | ||
Green tea extract | Extract | (4.5) | HLM | Amo | Misaka et al., 2013 | ||
Guava leaf extract | Extract | (18.16) | rCYP2C8 | DBF | Kaneko et al., 2013 | ||
Guava leaf polyphenol | Constitutent of guava leaf | (1.45) | rCYP2C8 | DBF | Kaneko et al., 2013 | ||
Gypenosides | Oriental herbal medicine | (20.06) | HLM | Pacli | He et al., 2013 | ||
Hesperedin | Flavonoid | 274.7 | rCYP2C8 | Tolbu | Pang et al., 2012 | ||
Hesperetin | Flavonoid | 68.5 | HLM | Pacli | Quintieri et al., 2011 | ||
168.4 | rCYP2C8 | Tolbu | Pang et al., 2012 | ||||
Hibiscus sabdariffa extract | Extract | (424) | HLM | Amo | Johnson et al., 2013 | ||
Honey | Natural product | (102.9) | (50.5) | Competitive | rCYP2C8 | Amo | Muthiah et al., 2012 |
Honokiol | Constituent of Magnolia | 8.9 | 4.9 | Competitive | HLM | Amo | Jeong et al., 2013 |
Horsetail | Natural product | (93.0) | HLM | Amo | Sevior et al., 2010 | ||
Hops extract | Extract | 0.8 | HLM | Amo | Yuan et al., 2014 | ||
Hunnemannine | Alkaloid | 1–10 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Hyperforin | Constituent of St. John’s Wort | 56 | HLM | Amo | Hokkanen et al., 2011 | ||
Hypoxis hemerocallidea extract | Extract | (192) | HLM | Pacli | Fasinu et al., 2013a | ||
Isocorybulbine | Alkaloid | 10–100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Isoxanthohumol | Prenylflavonoid | 0.2 | HLM | Amo | Yuan et al., 2014 | ||
Jaceosidin | Flavone | 106.4 | 109.4 | Competitive | HLM | Amo | Ji et al., 2010 |
Labisia pumila extracts | Extracts | (2.39–352.3) | (0.70-33.9) | Noncompetitive, mixed | rCYP2C8 | DBF | Pan et al., 2012 |
β-Lapachone | Quinone | 3.8 | HLM | Pacli | Kim et al., 2013a | ||
Liquorice extract | Extract | (14.36–17.06) | HLM | Amo | Li et al., 2015 | ||
Liquorice root | Natural product | (22.6) | HLM | Amo | Sevior et al., 2010 | ||
Luteolin | Flavonoid | 82.0 | rCYP2C8 | Tolbu | Pang et al., 2012 | ||
α-Mangostin | Constituent of mangosteen | 0.88 | 0.64 | Competitive | HLM | Pacli | Foti et al., 2009 |
β-Mangostin | Constituent of mangosteen | 8.39 | HLM | Pacli | Foti et al., 2009 | ||
Mecambridine | Alkaloid | 10–100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Milk thistle extract | Extract | (8.35) | Mixed | HLM | Pacli | Doehmer et al., 2011 | |
Morin | Flavonol | 17.3 | 7.3-12.3 | Mixed | HLM | Pacli | Václavíková et al., 2003 |
Nantenine | Alkaloid | 1–10 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
α-Naphthoflavone | Flavone derivative | 0.36 | HLM | Amo | Nirogi et al., 2015 | ||
Obovatol | Constituent of Magnolia | 11.1 | HLM | Amo | Joo et al., 2013 | ||
Quercetin | Flavonoid | 1.29 | Competitive | rCYP2C8 | Pacli | Rahman et al., 1994 | |
1.14 | Competitive | HLM | Pacli | Rahman et al., 1994 | |||
7 | HLM | Pacli | Dierks et al., 2001 | ||||
1.96-2.35 | Competitive | rCYP2C8 | Amo | Li et al., 2002 | |||
1.56 | Competitive | HLM | Amo | Li et al., 2002 | |||
2.47 | rCYP2C8 | DBF | Yamamoto et al., 2002 | ||||
4.07 | 19.7 | HLM | Taza | Attar et al., 2003 | |||
10.1 | Competitive | HLM | Pacli | Bun et al., 2003 | |||
20.6 | HLM | DBF | Ghosal et al., 2003 | ||||
3.3 | HLM | Pacli | Cai et al., 2004 | ||||
6.3 | HLM | Pacli | Donato et al., 2004 | ||||
2.9 | THLE | DBF | Donato et al., 2004 | ||||
29.5 | THLE | Pacli | Donato et al., 2004 | ||||
3.9–6.2 | rCYP2C8 | Pacli | Unger and Frank, 2004 | ||||
3.33 | rCYP2C8 | Amo | Walsky and Obach, 2004 | ||||
3.06 | HLM | Amo | Walsky and Obach, 2004 | ||||
7.19–8.47 | HLM | Pacli | Kim et al., 2005b | ||||
57.8 | HLM | Amo | Turpeinen et al., 2005 | ||||
3.94 | rCYP2C8 | Amo | Walsky et al., 2005a | ||||
3.3–5.6 | rCYP2C8 | Amo | O'Donnell et al., 2007 | ||||
1.6 | rCYP2C8 | DBF | McClue and Stuart, 2008 | ||||
5.28–5.38 | rCYP2C8 | Pacli | Gao et al., 2010 | ||||
1.33 | rCYP2C8 | Bomcc | Liu et al., 2010a | ||||
0.029 | HLM | Amo | Teng et al., 2010 | ||||
0.49 | Competitive | HLM | Amo | VandenBrink et al., 2011 | |||
0.52 | Competitive | HLM | Monte | VandenBrink et al., 2011 | |||
3.0 | Competitive | HLM | Pacli | VandenBrink et al., 2011 | |||
0.61 | Competitive | HLM | Repa | VandenBrink et al., 2011 | |||
0.61 | Competitive | HLM | Rosi | VandenBrink et al., 2011 | |||
4.20 | 2.07 | Competitive | rCYP2C8 | Amo | Muthiah et al., 2012 | ||
1.39 | HLM | Pacli | Lee et al., 2012a | ||||
46.0 | rCYP2C8 | Tolbu | Pang et al., 2012 | ||||
18.7 | HLM | Pacli | Bymaster et al., 2013 | ||||
(0.59) | rCYP2C8 | DBF | Kaneko et al., 2013 | ||||
(0.3702) | HLM | Amo | Mukkavilli et al., 2014 | ||||
24.5 | rcCYP2C8 | DBF | Pan et al., 2014 | ||||
12.3 | HLM | Rosi-OH | Wu et al., 2014 | ||||
3.40–5.92 | HLM | Amo | Li et al., 2015 | ||||
1.2 | HLM | Amo | Nirogi et al., 2015 | ||||
Piperlonguminine | Alkaloid | 76.2 | HLM | Amo | Song et al., 2014b | ||
Reserveratrol | Stilbenoid | 26.5 | 16.2–20.7 | HLM | Pacli | Václavíková et al., 2003 | |
Saw palmetto | Natural product | (8) | HLM | Amo | Sevior et al., 2010 | ||
(15.4) | HLM | Amo | Albassam et al., 2015 | ||||
(9.6) | HLM | Pio | Albassam et al., 2015 | ||||
Scoulerine | Alkaloid | 10-100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Star fruit (averrhoa carambola) juice | Fruit juice | 2.2b | HLM | Pacli | Zhang et al., 2007b | ||
Sutherlandia frutescens | Herb | (22.4) | HLM | Pacli | Fasinu et al., 2013b | ||
Tanshinol borneol ester | Combination of the natural compounds danshensu and borneol | 105 | rCYP2C8 | Bomcc | Liu et al., 2010b | ||
Thalictricavine | Alkaloid | 10–100 | rCYP2C8 | DBF | Salminen et al., 2011 | ||
Thelephoric acid | Antioxidant | 24.6 | HLM | Amo | Song et al., 2014a | ||
Tiliroside | Flavonoid | 12.1 | 9.4 | Competitive | HLM | Pacli | Sun et al., 2010 |
Tualang honey | Natural product | (102.9) | (50.5) | Competitive | rCYP2C8 | Amo | Muthiah et al., 2012 |
Valerian | Natural product | (523.3) | HLM | Amo | Sevior et al., 2010 | ||
Xanthohumol | Natural product | 1.1 | HLM | Amo | Yuan et al., 2014 |
HLM, human liver microsomes; IC50, inhibitor concentration supporting half of the maximal inhibition; Ki, reversible inhibition constant; n/a, not available; rcCYP2C8, reconstituted CYP2C8; rCYP2C8, recombinant CYP2C8; THLE, immortalized human liver epithelial cells.
↵a Amo, amodiaquine N-deethylation; Bomcc, flurogenic substrate; DBF, dibenzylfluorescein; Monte, montelukast 36-hydroxylation; Pacli, paclitaxel 6α-hydroxylation; Pio, pioglitazone hydroxylation (M-IV); Repa, repaglinide 3′-hydroxylation; Rosi, rosiglitazone N-demethylation; Rosi-OH, rosiglitazone p-hydroxylation; Taza, tazarotenic acid sulfoxidation; Tolbu, tolbutamide methyl hydroxylation.
↵b % (v/v).