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Literature summary for 1.1.1.146 extracted from

  • Hintzpeter, J.; Stapelfeld, C.; Loerz, C.; Martin, H.J.; Maser, E.
    Green tea and one of its constituents, epigallocatechine-3-gallate, are potent inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (2014), PLoS ONE, 9, e84468.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
(-)-catechin about 98% activity at 0.2 mM Homo sapiens
(-)-epicatechin about 95% activity at 0.2 mM Homo sapiens
(-)-epigallocatechin less than 80% activity at 0.2 mM Homo sapiens
(-)-epigallocatechin 3-gallate potent inhibitor, less than 10% activity at 0.2 mM Homo sapiens
(-)-gallocatechin less than 30% activity at 0.2 mM Homo sapiens
additional information tea extracts inhibit isoform 11beta-HSD1 mediated cortisone reduction, where green tea exhibits the highest inhibitory potency with an IC50 value of 3.749 mg dried tea leaves per ml Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADPH + H+ Homo sapiens
-
 cortisol + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisone + NADPH + H+
-
 Homo sapiens cortisol + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
11beta-HSD1
-
 Homo sapiens
11beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.01874
-
 (-)-epigallocatechin 3-gallate purified enzyme, at pH 7.4 and 37°C Homo sapiens
0.02268
-
 (-)-epigallocatechin 3-gallate unpurified enzyme, at pH 7.4 and 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.05799
-
 for cortisone reduction, at pH 7.4 and 37°C Homo sapiens (-)-epigallocatechin 3-gallate
0.1312
-
 for cortisol oxidation, at pH 7.4 and 37°C Homo sapiens (-)-epigallocatechin 3-gallate