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Humulone

CAS No. : 26472-41-3

MCE 国际站：Humulone

产品活性：Humulone (α-Lupulic acid) 是一种异戊二烯化间苯三酚衍生物，是一种有效的环氧合酶 2 (COX-2) 抑制剂。Humulone 在低微摩尔浓度下作为 GABA_A 受体的正调节剂。Humulone 是一种骨吸收抑制剂。Humulone 具有抗氧化、抗血管生成和诱导细胞凋亡的特性。

研究领域：Immunology/Inflammation | Neuronal Signaling | Membrane Transporter/Ion Channel | Apoptosis

作用靶点：COX | GABA Receptor | Apoptosis

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.
Humulone (0.1-10000 nM; for 12 h) suppresses the TNFα-induced increase of cyclooxygenase-2 mRNA.
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.

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.
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.
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.

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