Extracted from Alpinia officinarum Hance;Suitability:DMSO,hot methanol,chloroform mixed solvent;Store the product in sealed,cool and dry condition
CAS：548-83-4
分子式：C15H10O5
分子量：270.23
纯度：98%
存储：Store at -20°C

Background:

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

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[1]. 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[2].

参考文献:
[1]. Ciolino HP, et al. The flavonoid galangin is an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor. Br J Cancer. 1999 Mar;79(9-10):1340-6.
[2]. Wen M, et al. Galangin induces autophagy through upregulation of p53 in HepG2 cells. Pharmacology. 2012;89(5-6):247-55.