Handelin 是来自Chrysanthemum boreale的愈创木酚内酯二聚体,它通过下调NF-κB信号传导和促炎性细胞因子的产生而具有强大的抗炎活性。
生物活性 | Handelin is a guaianolide dimer fromChrysanthemum borealethat has potent anti-inflammatory activity by down-regulatingNF-κBsignaling and pro-inflammatory cytokine production[1]. |
体外研究 (In Vitro) | Handelin (Compound 1; 10-40 μM; RAW 264.7 cells) treatment suppresses the LPS-induced (1 μg/mL) overexpression of iNOS and COX-2 protein levels in a concentration-dependent manner. Handelin also suppresseS the induction of pro-inflammatory cytokines TNF-α and IL-1β in LPS-stimulated RAW 264.7 cells. Handelin also suppresses the activation of mitogen-activated protein kinases, including ERK and JNK signaling[1]. Handelin (Compound 1; 10-40 μM; RAW 264.7 cells) treatment significantly reduces the iNOS and COX-2 mRNA levels in LPS- stimulated RAW 264.7 cells. The transcriptional activity of NF-κB stimulated with LPS is also suppressed by Handelin. In addition, the LPS-stimulated upregulation of miRNA-155 expression is suppressed by Handelin[1].
RT-PCR[1] Cell Line: | RAW 264.7 cells | Concentration: | 10 μM, 20 μM, 40 μM | Incubation Time: | 5 hours | Result: | iNOS and COX-2 mRNA levels were significantly reduced. The transcriptional activity of NF-κB stimulated with LPS was also suppressed and the LPS-stimulated upregulation of miRNA-155 expression was also suppressed. |
Western Blot Analysis[1] Cell Line: | RAW 264.7 cells | Concentration: | 10 μM, 20 μM, 40 μM | Incubation Time: | | Result: | Suppressed the LPS-induced overexpression of iNOS and COX-2 protein levels in a concentration-dependent manner. Suppressed the induction of pro-inflammatory cytokines TNF-α and IL-1β, and also also suppressed the activation of mitogen-activated protein kinases, including ERK and JNK signaling in LPS-stimulated RAW 264.7 cells. |
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体内研究 (In Vivo) | Handelin (Compound 1; 10-20 mg/kg; oral administration; for 30 mintues; male Sprague-Dawley rats) treatment inhibits acute inflammation in carrageenan-induced paw edema model. The serum level of IL-1β is also inhibited by Handelin in a carrageenan-induced paw edema model[1].
Animal Model: | Male Sprague-Dawley (SD) rats (150-170 g, 5 weeks old) injected with carrageenan[1] | Dosage: | 10 mg/kg, 20 mg/kg | Administration: | Oral administration; for 30 mintues | Result: | Inhibited acute inflammation in carrageenan-induced paw. The serum level of IL-1β was also inhibited. |
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来源 | - Plants
- Compositae
- Chrysanthemum boreale
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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 : 16.67 mg/mL(30.16 mM;Need ultrasonic) 配制储备液 1 mM | 1.8094 mL | 9.0472 mL | 18.0943 mL | 5 mM | 0.3619 mL | 1.8094 mL | 3.6189 mL | 10 mM | 0.1809 mL | 0.9047 mL | 1.8094 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: 1.67 mg/mL (3.02 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (3.02 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 16.7 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: 1.67 mg/mL (3.02 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (3.02 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 16.7 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.67 mg/mL (3.02 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (3.02 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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