1. Immunology/Inflammation
    Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
    Epigenetics
  2. COX
    Tyrosinase
    HDAC
  3. Gnetol

Gnetol 

Cat. No.: HY-126052
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Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.

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Gnetol Chemical Structure

Gnetol Chemical Structure

CAS No. : 86361-55-9

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Description

Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities[1][2][3].

IC50 & Target[1][2]

COX-1

0.78 μM (IC50)

Tyrosinase

4.5 μM (IC50)

HDAC

 

In Vitro

The antiproliferative activities of Gnetol are tested in HCT-116, Hep-G2, MDA-MB-231, and PC-3 cell lines by measuring cell viability after treatment with 4.1 μM, 40.9 μM, 204.7 μM, 409.4 μM, and 1023.6 μM. Gnetol shows concentration-dependent reductions in cell viability in cancer cell lines with greatest activity in colorectal cancer[1].
Gnetol at 200 µg/mL significantly offers the highest protection of 54.3% against the toxicant. A lower dose of Gnetol (50 µg/mL) also shields the cell line from the toxic effects of CCl4[3].
The ligand molecule TGF-β and PPARα protein show that Gnetol has the binding affinity of 7.0 and 8.4, respectively[3].

In Vivo

Male Sprague-Dawley rats were cannulated and dosed either intravenously with Gnetol (10 μg/kg) or orally (100 mg/kg). After oral and intravenous administration, Gnetol is detected in both serum and urine as the parent compound and as a glucuronidated metabolite. The bioavailability of Gnetol is determined to be 6%. Gnetol is rapidly glucuronidated and is excreted in urine and via nonrenal routes[1].
Pretreatment of Male NIH Swiss mice (20-35 g) with Gnetol (50mg/kg, SC) is able to increase the latency period to response in analgesia models[1].

Molecular Weight

244.24

Formula

C₁₄H₁₂O₄

CAS No.

86361-55-9

SMILES

OC1=CC=CC(O)=C1/C=C/C2=CC(O)=CC(O)=C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GnetolCOXTyrosinaseHDACCyclooxygenaseHistone deacetylasesAntioxidantantihepatotoxichepatoprotectiveTGF-βPPARαmelaninantinociceptiveantidiabeticanticancerantiproliferativeInhibitorinhibitorinhibit

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