1. Immunology/Inflammation
    Neuronal Signaling
    Membrane Transporter/Ion Channel
    Apoptosis
  2. COX
    GABA Receptor
    Apoptosis
  3. Humulone

Humulone (Synonyms: α-Lupulic acid)

Cat. No.: HY-N6084
Handling Instructions

Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.

For research use only. We do not sell to patients.

Humulone Chemical Structure

Humulone Chemical Structure

CAS No. : 26472-41-3

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Description

Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties[1][2][3].

IC50 & Target[1][2][3]

COX-2

 

In Vitro

Humulone (0.1, 1, 10, 100, 1000, 10000 nM; for 12 h) with with 10 ng/ml TNFα dose-dependently decreases the amount of released PGE2 with an IC50 of about 30 nM in MC3T3-E1 cells. Humulone reduces cyclooxygenase activity of the TNFK-treated cells[1].
Humulone (0.1-10000 nM; for 12 h) suppresses the TNFα-induced increase of cyclooxygenase-2 mRNA[1].
Humulone hardly affects the cyclooxygenase-1 activity below 10 μM, whereas inhibits the cyclooxygenase-2 activity with an IC50 of about 1.6 μM in MC3T3-E1 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Humulone (10 or 20 mg/kg; IP; single dose) shortens sleep onset and increases the duration of sleep induced by pentobarbital and decreases the spontaneous locomotion in open field at 20 mg/kg[2].
Humulone (10 μmol; applied topically to the dorsal shaved area) pre-treatment significantly inhibited TPA (10 nmol)-induced COX-2 expression in Female ICR mice (6-7 weeks of age) skin[3].
Humulone (1, 10 μmol; applied topical; pre-treatment 30 min) suppresses TPA-induced NF-κB DNA binding. Humulone attenuates TPA-stimulated nuclear translocation of p65 and p50 subunit proteins of NF-κB[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/cAnNRj mice (9-11 weeks of age)[2]
Dosage: 10 or 20 mg/kg
Administration: IP; pre-treatment before sodium pentobarbital (35 mg/kg; i.p.) and ethanol (3.5 g/kg)
Result: Significantly decreased the latency and prolonged the duration of sleep induced by pentobarbital at 20 mg/kg dose. These effects were not observed at a lower dose of 10 mg/kg.
Showed no effect on the onset of sleep induced by ethanol, but significantly increased sleep duration dose-dependently.
Molecular Weight

362.46

Formula

C₂₁H₃₀O₅

CAS No.
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