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GABAA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。
| 生物活性 | Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potentcyclooxygenase-2 (COX-2)inhibitor. Humulone acts as a positive modulator ofGABAAreceptorat low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic andapoptosis-inducing properties[1][2][3]. |
| IC50& Target[1][2][3] | |
体外研究
(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].
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体内研究
(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].
| 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. |
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| 结构分类 | - Ketones, Aldehydes, Acids
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| 来源 | - Plants
- Moraceae
- Humulus lupulusL.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(137.95 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7589 mL | 13.7946 mL | 27.5893 mL | | 5 mM | 0.5518 mL | 2.7589 mL | 5.5179 mL | | 10 mM | 0.2759 mL | 1.3795 mL | 2.7589 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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