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Literature summary for 3.4.23.46 extracted from

  • Lv, L.; Yang, Q.Y.; Zhao, Y.; Yao, C.S.; Sun, Y.; Yang, E.J.; Song, K.S.; Mook-Jung, I.; Fang, W.S.
    BACE1 (beta-secretase) inhibitory chromone glycosides from Aloe vera and Aloe nobilis (2008), Planta Med., 74, 540-545.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(6R)-2,6-anhydro-5-O-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-[2-[(2R)-2-hydroxypropyl]-7-methoxy-5-methyl-4-oxo-4H-chromen-8-yl]-L-glucitol inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 7.4% in B103 neuroblastoma cells at 30 ppm Homo sapiens
(6R)-2,6-anhydro-6-[7-methoxy-5-methyl-4-oxo-2-[(1E)-prop-1-en-1-yl]-4H-chromen-8-yl]-L-glucitol inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 12.3% in B103 neuroblastoma cells at 30 ppm Homo sapiens
1,5-anhydro-1-[7-hydroxy-2-[(2S)-2-hydroxypropyl]-5-methyl-4-oxo-4H-chromen-8-yl]hexitol 37.2% inhibition at 0.1 mM Rattus norvegicus
1,5-anhydro-1-[7-hydroxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]-2-O-[(E)-2-(4-hydroxyphenyl)ethenyl]hexitol 39.5% inhibition at 0.1 mM Rattus norvegicus
1,5-anhydro-1-[7-methoxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol 41.0% inhibition at 0.1 mM Rattus norvegicus
1,5-anhydro-2-O-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1-[7-hydroxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol 36.4% inhibition at 0.1 mM Rattus norvegicus
1,5-anhydro-2-O-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1-[7-methoxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol 48.7% inhibition at 0.1 mM Rattus norvegicus
2'-O-coumaroyl-(S)-aloesinol 51.9% inhibition at 0.1 mM Rattus norvegicus
2'-O-[p-methoxy-(E)-cinnamoyl]-(S)-aloesinol 34.1% inhibition at 0.1 mM Rattus norvegicus
8-C-glucosyl-(R)-aloesol 39.2% inhibition at 0.1 mM Rattus norvegicus
8-C-glucosyl-7-methoxy-(R)-aloesol 26.8% inhibition at 0.1 mM Rattus norvegicus
8-C-glucosyl-7-O-methylaloediol
-
Rattus norvegicus
allo-aloeresin D
-
Rattus norvegicus
aloeresin D 71.5% inhibition at 0.1 mM Rattus norvegicus
aloesin 37.5% inhibition at 0.1 mM Rattus norvegicus
C-2'-decoumaroyl-aloeresin G 72.0% inhibition at 0.1 mM Rattus norvegicus
N-benzyloxycarbonyl-Val-Leu-leucinal
-
Rattus norvegicus
rebaichromone
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
B-103 cell
-
Rattus norvegicus
-
commercial preparation recombinant enzyme Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(7-methoxycoumarin-4-yl)-acetyl-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Arg-Lys-(2,4-dinitrophenyl)-Arg-Arg-NH2 + H2O
-
Rattus norvegicus ?
-
?
7-methoxycoumarin-4-yl-acetyl-SEVNLDAEFR-(2,4-dinitrophenyl)K-RR + H2O
-
Homo sapiens ?
-
?
amyloid precursor protein + H2O
-
Rattus norvegicus amyloid protein 1-42 + ?
-
?

Synonyms

Synonyms Comment Organism
BACE1
-
Rattus norvegicus
beta-secretase
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0116
-
-
Rattus norvegicus N-benzyloxycarbonyl-Val-Leu-leucinal
0.0205
-
-
Rattus norvegicus C-2'-decoumaroyl-aloeresin G
0.0205
-
pH 4.0, 25°C Homo sapiens (6R)-2,6-anhydro-6-[7-methoxy-5-methyl-4-oxo-2-[(1E)-prop-1-en-1-yl]-4H-chromen-8-yl]-L-glucitol
0.039
-
-
Rattus norvegicus aloeresin D
0.039
-
pH 4.0, 25°C Homo sapiens (6R)-2,6-anhydro-5-O-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-[2-[(2R)-2-hydroxypropyl]-7-methoxy-5-methyl-4-oxo-4H-chromen-8-yl]-L-glucitol