Sulfotransferase (SULT)
Sulfotransferase (SULT) are transferase enzymes (EC 2.8.2.1) that catalyze the transfer of a sulfate group from a donor molecule to an acceptor alcohol (C-OH) or amine.
Many flavonoids such as quercetin, kaempferol, myricetin, apigenin, and nevadensin are potent inhibitors of SULT in vitro.[3] Note that many of these inhibitors listed below have not been tested in human volunteers, only tested in vitro, and could be completely ineffective clinically.
Sulfotransferase can catalyze the creation of tyramine-O-sulfate from tyramine by means of its C-OH group using 3'-phosphoadenylylsulfate as a cofactor.
Substrate | SULT | End Product |
---|---|---|
Tyramine | Tyramine-O-sulfate | |
![]() |
![]() |
|
Cofactor | Byproduct | |
3'-phosphoadenylylsulfate | adenosine 3',5'-bisphosphate |
SULT1A1 (P-PST)
Potent Inhibitors | Strength | Dosage | Verified in Man |
---|---|---|---|
Bergamottin | significant inhibition[4] | ? | ? |
Daidzein [2][6] (in Kudzu) | 69% inhibition[2] | 0.01 mM | ? |
Denistein | 80% inhibition[2] | 0.01 mM | ? |
Dihydroxybergamottin | significant inhibition[4] | ? | ? |
(-)-Epigallocatechin | 100% inhibition[4] | ? | ? |
(-)-Epigallocatechin gallate (EGCG) | Almost complete inhibition[4] | ? | ? |
(-)-Epicatechin | 100% inhibition[4] | ? | ? |
(-)-Epicatechin gallate (ECG) | Almost complete inhibition[4] | ? | ? |
Fisetin | Potent inhibition[5] | ? | ? |
Galangin | Potent inhibition[5] | ? | ? |
Genistein (in Kudzu) | Potent inhibition[5][6] | ? | ? |
Kaempferol | Potent inhibition[5][6] | ? | ? |
Naringenin | significant inhibition[4] | ? | ? |
Nobiletin | 100% inhibition[4] | ? | ? |
Quercetin [4][5][6] | 100% inhibition[4] | ? | ? |
Tangeretin | 100% inhibition[4] | ? | ? |
Theaflavin | 100% inhibition[4] | ? | ? |
Thearubigin | 100% inhibition[4] | ? | ? |
Inhibitors of Unknown Potency | Strength | Dosage | Verified in Man |
Caffeic acid [1] | ? | ? | ? |
Inducers | Strength | Dosage | Verified in Man |
Gallic acid [1] | ? | ? | ? |
SULT1A3 (M-PST)
Potent Inhibitors | Strength | Dosage | Verified in Man |
---|---|---|---|
Banaba extract | 100% inhibition | 1000 μg/ml[7] | ? |
Banaba extract | 50% inhibition | IC50=7.49 μg/ml[7] | ? |
Bilberry extract | 50% inhibition | IC50=90.0 μg/ml[7] | ? |
Black cohosh extract | 50% inhibition | IC50=21.0 μg/ml[7] | ? |
Catechin | 50% inhibition | IC50=8.3 μg/ml[7] | ? |
(-)-Epicatechin gallate | Almost complete inhibition[4] | ? | ? |
Epigallocatechin | 50% inhibition | IC50=14.6 μg/ml[7] | ? |
(-)-Epigallocatechin gallate (EGCG) | Almost complete inhibition[4] | IC50=22 μg/ml[7] | ? |
Ginko biloba leaf extract | 50% inhibition | IC50=12.3 μg/ml[7] | ? |
Grape seed extract | 100% inhibition | 1000 μg/ml[7] | ? |
Grape seed extract | 50% inhibition | IC50=24.3 μg/ml[7] | ? |
Passion flower extract | 50% inhibition | IC50=78.1 μg/ml[7] | ? |
Rafuma extract | 100% inhibition | 1000 μg/ml[7] | ? |
Saint John’s Wort extract | 50% inhibition | IC50=98.0 μg/ml[7] | ? |
Theaflavin | strong inhibition[4] | ? | ? |
Thearubigin | strong inhibition[4] | ? | ? |
Moderate Inhibitors | Strength | Dosage | Verified in Man |
Daidzein (in Kudzu) | 29% inhibition[2] | 0.01 mM | ? |
Denistein | 19% inhibition[2] | 0.01 mM | ? |
Genistein (in Kudzu) | 50% inhibition[8] | > 25000 nM | ? |
Naringenin | partial inhibition[4] | ? | ? |
Naringin | partial inhibition[4] | ? | ? |
Nobiletin | partial inhibition[4] | ? | ? |
Quercetin | partial inhibition[4] | ? | ? |
Tangeretin | partial inhibition[4] | ? | ? |
Inhibitors of Unknown Potency | Strength | Dosage | Verified in Man |
Bergamottin [4] | ? | ? | ? |
Caffeic acid [1] | ? | ? | ? |
Inducers | Strength | Dosage | Verified in Man |
Gallic acid [1] | ? | ? | ? |
Bibliography
1. Effects of phenolic acids on human phenolsulfotransferases in relation to their antioxidant activity.
Yeh CT, Yen GC. PubMed PMID: 12590501
2. Human thyroid phenol sulfotransferase enzymes 1A1 and 1A3: activities in normal and diseased thyroid glands, and inhibition by thyroid hormones and phytoestrogens.
Ebmeier CC, Anderson RJ. PubMed PMID: 15531517
3. Matrix modulation of the bioactivation of estragole by constituents of different alkenylbenzene-containing herbs and spices and physiologically based biokinetic modeling of possible in vivo effects.
Alhusainy W, van den Berg SJ, Paini A, Campana A, Asselman M, Spenkelink A, Punt A, Scholz G, Schilter B, Adams TB, van Bladeren PJ, Rietjens IM. PubMed PMID: 22649189
4. Inhibitory effects of various beverages on human recombinant sulfotransferase isoforms SULT1A1 and SULT1A3.
Nishimuta H, Ohtani H, Tsujimoto M, Ogura K, Hiratsuka A, Sawada Y. PubMed PMID: 17876860
5. Dietary flavonoids: effects on xenobiotic and carcinogen metabolism.
Moon YJ, Wang X, Morris ME. PubMed PMID: 16289744
6.
Inhibition of rat liver sulfotransferases SULT1A1 and SULT2A1 and glucuronosyltransferase by dietary flavonoids. Mesía-Vela S, Kauffman FC. PubMed PMID: 14742143
7. Inhibitory effects of herbal extracts on the activity of human sulfotransferase isoform sulfotransferase 1A3 (SULT1A3).
Nagai M, Fukamachi T, Tsujimoto M, Ogura K, Hiratsuka A, Ohtani H, Hori S, Sawada Y. PubMed PMID: 19122289
8. Soy and Health 2000: Clinical Evidence, Dietetic Applications
Koen Descheemaeker, Ignace Debruyne; Garant, 2001; ISBN 9044111272, 9789044111279page revision: 32, last edited: 15 Dec 2017 23:37