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Literature summary for 5.3.99.3 extracted from

  • Verhoff, M.; Seitz, S.; Paul, M.; Noha, S.M.; Jauch, J.; Schuster, D.; Werz, O.
    Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E2 synthase-1 (2014), J. Nat. Prod., 77, 1445-1451 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
11-oxo-beta-boswellic acid
-
Homo sapiens
3-O-acetyl-28-hydroxylupeolic acid 31.1% residual activity at 0.01 mM Homo sapiens
3-O-acetyllupeolic acid 51.4% residual activity at 0.01 mM Homo sapiens
3-O-acteyl-11-oxo-beta-boswellic acid
-
Homo sapiens
3-O-acteyl-beta-boswellic acid
-
Homo sapiens
3-oxo-8,24-dienetirucallic acid 16.7% residual activity at 0.01 mM Homo sapiens
3alpha-acetoxy-7,24-dienetirucallic acid 20.6% residual activity at 0.01 mM Homo sapiens
3alpha-acetoxy-8,24-dienetirucallic acid 36.8% residual activity at 0.01 mM Homo sapiens
3alpha-hydroxy-7,24-dienetirucallic acid 29.6% residual activity at 0.01 mM Homo sapiens
3alpha-hydroxy-8,24-dienetirucallic acid 3.5% residual activity at 0.01 mM Homo sapiens
3beta-hydroxy-8,24-dienetirucallic acid 29.2% residual activity at 0.01 mM Homo sapiens
4,(23)-dihydro-11-oxo-roburic acid 21.6% residual activity at 0.01 mM Homo sapiens
4,(23)-dihydronyctanthic acid 74.1% residual activity at 0.01 mM Homo sapiens
4,(23)-dihydroroburic acid 92.4% residual activity at 0.01 mM Homo sapiens
beta-boswellic acid
-
Homo sapiens
lupeolic acid 43.1% residual activity at 0.01 mM Homo sapiens
roburic acid 83.9% residual activity at 0.01 mM 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.
Prostaglandin H2 Homo sapiens
-
Prostaglandin E2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Prostaglandin H2
-
Homo sapiens Prostaglandin E2
-
?

Synonyms

Synonyms Comment Organism
microsomal prostaglandin E2 synthase-1
-
Homo sapiens
mPGES-1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0004
-
at pH 7.4 and 4°C Homo sapiens 3alpha-acetoxy-8,24-dienetirucallic acid
0.0004
-
at pH 7.4 and 4°C Homo sapiens 3alpha-acetoxy-7,24-dienetirucallic acid
0.0009
-
at pH 7.4 and 4°C Homo sapiens 3-oxo-8,24-dienetirucallic acid
0.0009
-
at pH 7.4 and 4°C Homo sapiens 3-O-acetyl-28-hydroxylupeolic acid
0.001
-
at pH 7.4 and 4°C Homo sapiens 4,(23)-dihydro-11-oxo-roburic acid
0.0011
-
at pH 7.4 and 4°C Homo sapiens 3alpha-hydroxy-8,24-dienetirucallic acid
0.0012
-
at pH 7.4 and 4°C Homo sapiens 3beta-hydroxy-8,24-dienetirucallic acid
0.003
-
at pH 7.4 and 4°C Homo sapiens 3alpha-hydroxy-7,24-dienetirucallic acid
0.0085
-
at pH 7.4 and 4°C Homo sapiens lupeolic acid
0.01
-
at pH 7.4 and 4°C Homo sapiens 3-O-acetyllupeolic acid
0.01
-
IC50 above 0.01 mM, at pH 7.4 and 4°C Homo sapiens roburic acid
0.01
-
IC50 above 0.01 mM, at pH 7.4 and 4°C Homo sapiens 4,(23)-dihydroroburic acid
0.01
-
IC50 above 0.01 mM, at pH 7.4 and 4°C Homo sapiens 4,(23)-dihydronyctanthic acid