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Galangin

CAS No. : 548-83-4

產品活性：Galangin (Norizalpinin) is?an?agonist/antagonist?of the?arylhydrocarbon?receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.

研究領域：Metabolic Enzyme/Protease  |  Autophagy

作用靶點：Cytochrome P450  |  Autophagy

結構分類：黃酮類  |  黃酮醇  |  酚類  |  多酚類

來源：植物  |  姜科  |  高良姜

In Vitro: Galangin (Norizalpinin)?inhibits the catabolic breakdown of DMBA, as measured by thin-layer chromatography, in a dose-dependent manner.?Galangin?also inhibits the formation of DMBA-DNA adducts, and prevents DMBA-induced inhibition of cell growth.?Galangin?causes a potent, dose-dependent inhibition of?CYP1A1?activity, as measured by ethoxyresorufin-O-deethylase?activity, in intact cells and in microsomes isolated from DMBA-treated cells. Analysis of the inhibition kinetics by double-reciprocal plot demonstrates that?galangin?inhibits CYP1A1?activity?in a noncompetitive manner.?Galangin?causes an increase in the level of?CYP1A1?mRNA, indicating that it may be an?agonist?of the?aryl?hydrocarbon?receptor, but it inhibits the induction of?CYP1A1?mRNA by DMBA or by 2,3,5,7-tetrachlorodibenzo-p-dioxin (TCDD).?Galangin?also inhibits the DMBA- or TCDD-induced transcription of a reporter vector containing the?CYP1A1?promoter. Galangin treatment inhibits cell proliferation and induced autophagy (130 μM) and apoptosis (370 μM). In particular, galangin treatment in HepG2 cells causes (1) an accumulation of autophagosomes, (2) elevated levels of microtubule-associated protein light chain 3, and (3) an increased percentage of cells with vacuoles. p53 expression is also increased. The galangin-induced autophagy is attenuated by the inhibition of p53 in HepG2 cells, and overexpression of p53 in Hep3B cells restored the galangin-induced higher percentage of cells with vacuoles to normal level.

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