Gentiopicroside

Catalog No.S3777 Synonyms: Gentiopicrin

Gentiopicroside Chemical Structure

Molecular Weight(MW): 356.32

Gentiopicroside (GE), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.

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Biological Activity

Description Gentiopicroside (GE), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
Targets
CYP2A6 [1]
(in human liver microsomes)
CYP2E1 [1]
(in human liver microsomes)
In vitro

Gentiopicroside (GE) is a non-competitive inhibitor of CYP2A6 at lower concentrations and a competitive inhibitor at higher concentrations. Gentiopicroside does not produce inhibition of CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities. However, a significant increase of CYP1A2 and CYP3A4 activity is observed at high concentrations. In cultured human hepatocytes no significant induction of CYP1A2, CYP3A4 or CYP2B6 is observed[1].

In vivo Gentiopicroside (GE) has a low bioavailability (%F) after oral administration, which may be attributed to the first-pass metabolism in the gut wall or liver, metabolism or decomposition in the intestine by bacterial microflora, and/or poor absorption from the gastrointestinal tract. The Phase I clinical study shows that after intravenous infusion of 80, 240, and 400 mg GE, the mean Cmax are 3.501±0.566 μg/ml, 9.865±1.237 μg/ml, and 16.95±2.571 μg/ml, respectively[1]. GPS can act as hepatoprotective, cholagogic, anti-inflammatory, and antibacterial agents[2].

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: Wistar rats
  • Formulation: --
  • Dosages: 200 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.25 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.32
Formula

C16H20O9

CAS No. 20831-76-9
Storage powder
in solvent
Synonyms Gentiopicrin

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID