生物活性 | Avicularin is an orally active flavonoid. Avicularin inhibitsNF-κB(p65),COX-2andPPAR-γactivities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities[1][3]. |
IC50& Target[2][3] | |
体外研究 (In Vitro) | Avicularin (10-300 μM, 1 h) suppresses NO and PGE2production in LPS-stimulated RAW 264.7 cells[1]. Avicularin (10-300 μM, 1 h) exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 cells[1]. Avicularin (25-100 μg/mL, 48 h) decreases cell proliferation, cell migration and invasion in Huh7 cells[2]. Avicularin (25-100 μg/mL, 48 h) induces apoptosis via the downregulation of NF-κB (p65) and COX-2 and the upregulation of PPAR-γ[2]. Avicularin (50 μM, 6 days) decreases the intracellular lipids, along with decreased PPARγ, C/EBPα, and aP2 mRNA levels in 3T3-L1 cells[3]. Avicularin (50 μM, 6 days) suppresses GLUT4-Mediated glucose uptake in 3T3-L1 cells[3]. Avicularin (2.5-10 μM, 2 h) inhibits ECM degradation and inflammation via TRAF6/MAPK activation in rat and human chondrocytes[4].
Cell Proliferation Assay[2] Cell Line: | Huh7 cells | Concentration: | 25, 50, 100 μg/mL | Incubation Time: | 12, 24, 36 and 48 h | Result: | Inhibited cell proliferation in a dose-dependent manner. |
Western Blot Analysis[1] Cell Line: | RAW 264.7 cells | Concentration: | 10, 30, 100, 300 μM | Incubation Time: | 1 h | Result: | Inhibited LPS-induced protein expression of iNOS and COX-2, release of pro-inflammatory cytokine IL-1β, degradation of cytosolic IκB, and phosphorylation of ERK. |
RT-PCR[3] Cell Line: | 3T3-L1 cells | Concentration: | 50 μM | Incubation Time: | 6 days | Result: | Decreased PPARγ, C/EBPα, and aP2 mRNA levels approximately 28.7, 69.5, and 18.3%, respectively. |
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体内研究 (In Vivo) | Avicularin (injected in articular cavity of the knee, 0.5-2 mg/kg, twice a week for 4 weeks) attenuates the development of OA (osteoarthritis) in ACLT-induced rats[4]. Avicularin (oral administration, 50 and 100 mg/kg, for 21 days) attenuates memory Impairment in rats with amyloid Beta-induced Alzheimer's disease[5].
Animal Model: | ACLT (anterior cruciate ligament transection)-induced rats[4] | Dosage: | 0.5, 1, 2 mg/kg | Administration: | Injected into the articular cavity of the right knee, twice a week for 4 weeks. | Result: | Alleviated the tibial subchondral osteolysis, reduces bone loss, and increases the bone mass of tibial subchondral bone. Attenuated ECM degradation, the loss of Aggrecan and Collagen II in ACLT-induced rats. Decreased the MMP3 and MMP13 protein level. |
Animal Model: | Rats with amyloid Beta-induced Alzheimer's disease[5] | Dosage: | 25, 50, and 100 mg/kg | Administration: | Oral administration, for 21 days | Result: | Enhanced cognition activity, and reversed the effects of amyloid beta-induced inflammatory response and excessive oxidative stress. |
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来源 | - Plants
- Lauraceae
- Lindera aggregata(Sims) Kosterm.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°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 : 100 mg/mL(230.23 mM;Need ultrasonic) 配制储备液 1 mM | 2.3023 mL | 11.5115 mL | 23.0229 mL | 5 mM | 0.4605 mL | 2.3023 mL | 4.6046 mL | 10 mM | 0.2302 mL | 1.1511 mL | 2.3023 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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