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
Tyramine.png tyramine_O-sulfate.png
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, 9789044111279
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