Norbergenin|79595-97-4|安捷凯

Background

Norbergenin, an O-demethylated derivative of bergenin, can be isolated from rhizomes of Bergenia stacheyi.

Norbergenin shows anti-arthritic activity through modulation of Th1/Th2 cytokine balance, and it inhibits the production of proinflammatory Th1 cytokines (IL-2, IFN-γ and TNF-α) while as potentiate anti-inflammatory Th2 cytokines (IL-4 and IL-5) in the peripheral blood of adjuvant-induced arthritic balb/c mice.[1]

Norbergenin inhibits bovine adrenal tyrosine hydroxylase (TH) activity by 29.0% and 53.4% at a concentration of 20 μg/mL, and exhibited noncompetitive inhibition of TH activity with the substrate L-tyrosine. [2]

Norbergenin shows moderate antioxidant activity (IC50 13 μM in DPPH radical scavenging; 32 μM in superoxide anion scavenging). [3]

Reference:
[[1] Nazir N, et al. J Ethnopharmacol. 2007 Jun 13;112(2):401-5.
[2] Zhang YH, et al. Phytother. Res. 2003 Sep;17(8):967-9.
[3] Takahashi H, et al. Bioorg. Med. Chem. 2003 Apr 17;11(8):1781-8.

Protocol

Kinase experiment [1]:

Inhibition of TH activity: Norbergenin inhibits the bovine adrenal TH activity by 51.0% at 5 μg/mL, 51.6% at 10 μg/mL, 53.4% at 20 μg/mL, respectively.

Cell experiment [2]:

Cell lines

Neuronal cells (Rat)

Preparation method

The solubility of this compound in DMSO is > 1 mM..

Reaction Conditions

3 days

Applications

Norbergenin can enhance antioxidant activity, which can be further related to protecting neurons from damage by ROS

Animal experiment [3]:

Animal models

balb/c mice

Dosage form

5, 10, 20, 40 and 80 mg/kg per oral dose

Applications

Norbergenin inhibit Th1 (IL-2, IFN-γ and TNF-α) and up-regulates Th2 cytokines (IL-4 and IL-5) significantly, and release the symptom of oedema at 40 and 80 mg/kg.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

参考文献:

[1] Nazir N, et al. J Ethnopharmacol. 2007 Jun 13;112(2):401-5.

[2] Zhang YH, et al. Phytother. Res. 2003 Sep;17(8):967-9.

[3] Takahashi H, et al. Bioorg. Med. Chem. 2003 Apr 17;11(8):1781-8.