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Drug-Target Interaction

Drug

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PubChem ID:5281051
Structure:
Synonyms:
(component of) Hypericum spp (st. John's wort)
1,3,4,6,8,13-Hexahydroxy-10,11-dimethylphenanthro [1,10,9,8-opqra]perylene-7,14-dione P-conformer
1,3,4,6,8,13-Hexahydroxy-10,11-dimethylphenanthro(1,10,9,8-opqra)perylene-
1,3,4,6,8,13-Hexahydroxy-10,11-dimethylphenanthro(1,10,9,8-opqra)perylene-7,14-dione
1,3,4,6,8,13-hexahydroxy-10,11-dimethylphenanthro[1,10,9,8-opqra]perylene-7,14-dione
1:6:8:10:11:13-hexahydroxy-3:4-dimethyl-meso-naphthodianthrene-7:14-dione
4,5,7,4',5',7'-Hexahydroxy-2,2'-dimethyl-mesonapthtodianthron
4,5,7,4',5',7'-Hexahydroxy-2,2'-dimethylnaphthodianthrone
548-04-9
56690_FLUKA
56690_SIGMA
AIDS-000117
AIDS-052002
AIDS000117
AIDS052002
Ambap348
BiomolKI2_000040
BiomolKI_000032
C07606
C30H16O8
CHEBI:5835
Cyclo werrol
Cyclo-Werol
Cyclosan
DRG-0113
EINECS 208-941-0
hipericina
HSCI1_000202
Hypericin
Hypericin & Visible light
Hypericin from Hypericum perforatum
hypericine
Hypericum Extract
Hypericum red
Hyperizin
LMPK13040001
LS-175574
NCGC00162454-01
NCGC00163378-01
NCI60_003879
NCI60_006799
NSC 407313
NSC 622946
NSC407313
NSC622946
phenanthro[1,10,9,8-opqra]perylene-7,14-dione, 1,3,4,6,8,13-hexahydroxy-10,11-dimethyl-
Phenanthro[1,10,9,8-opqra]perylene-7,14-dione,1,3,4,6,8,13-hexahydroxy-10,11-dimethyl-, stereoisomer
VIMRxyn
ZINC03780340

Target

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Uniprot ID:DUOX2_HUMAN
Synonyms:
Dual oxidase 2
Large NOX 2
Long NOX 2
NADH/NADPH thyroid oxidase p138-tox
NADPH oxidase/peroxidase DUOX2
NADPH thyroid oxidase 2
p138 thyroid oxidase
Thyroid oxidase 2
EC-Numbers:1.11.1.-
1.6.3.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

7487096
Inhibition of neutrophil superoxide generation by hypericin, an antiretroviral agent.. T Nishiuchi; T Utsumi; T Kanno; Y Takehara; H Kobuchi; T Yoshioka; A A Horton; T Yasuda; K Utsumi (1995) Archives of biochemistry and biophysics display abstract
We previously reported that phorbol 12-myristate 13-acetate (PMA)-induced superoxide (O2.-) generation of neutrophils was inhibited by hypericin, a photosensitizing pigment found in St. Johnswort (herb Hypericin triquetrifolium Turra), via a mechanism involving protein kinase C (PKC). To obtain further insights into the mechanism of inhibition, the effects of hypericin on stimulation-dependent O2.- generation and related enzymes of neutrophils were investigated. Hypericin inhibited O2.- generation of neutrophils induced by PKC-dependent and -independent stimuli in a light- and concentration-dependent manner. Oxygen was required for the light-dependent inhibition by hypericin. NADPH oxidase activity in a cell-free system and TNF-alpha-induced tyrosyl phosphorylation of neutrophil proteins were also inhibited by hypericin in a concentration- and light-dependent manner. However, tyrosine kinase of p60src, an enzyme not bound to a membrane, was not inhibited either in the light or in the dark. Oxygen uptake of neutrophils by photosensitization with hypericin resulted in the formation of singlet oxygen (1O2), O2.-, and hydroxyl radical (.OH) and enhanced lipid peroxidation. The formation of 1O2 was inhibited by azide, a quencher of 1O2, but not by desferrioxamine (DSF), a ferric ion chelator. By contrast, both generation of .OH and lipid peroxidation were inhibited by DSF but not by azide. Furthermore, PMA-induced O2.- generation inhibited by hypericin partially recovered in the presence of azide but not DSF. These results suggested that the light-dependent inhibition of O2.- generation by hypericin might be due to inhibition of tyrosine kinase, PKC, and NADPH oxidase via an oxygen-dependent mechanism, possibly through both Type I and II photosensitization mechanisms.