Wedelolactone 通过直接抑制 IKK 复合物抑制 lps 诱导的caspase-11表达。Wedelolactone 抑制5-Lox，其IC50值为 2.5 μM。Wedelolactone 通过下调 PKCε 诱导的 caspase 依赖的前列腺癌细胞凋亡，而不抑制 Akt。Wedelolactone 可从鳢肠中提取，可用于癌症的研究。
| 生物活性 | Wedelolactone suppresses LPS-inducedcaspase-11expression by directly inhibits theIKKComplex. Wedelolactone also inhibits5-lipoxygenase(5-Lox) with anIC50of 2.5 μM. Wedelolactone induces caspase-dependentapoptosisin prostatecancercells via downregulation ofPKCεwithout inhibitingAkt. Wedelolactone can extract from Eclipta alba, and it can be used for the research ofcancer[1][2][3]. |
| IC50& Target[1][2][3] | Caspase-11 | 5-LOX 2.5 μM (IC50) | Apoptosis |
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体外研究
(In Vitro) | Wedelolactone (0-5 μg/mL; 0-21 d) enhances bone marrow mesenchymal stem cells (BMSC) differentiation towards osteoblasts[3].Wedelolactone (0-6 μg/mL; 0-9 d) inhibits GSK3β activity and increases β-catenin and runx2 nuclear accumulation in BMSC, and inhibits the effect of RANKL[3].Wedelolactone (0-5 μg/ml; 60 min) inhibits GSK3β activity and proves GSK3β is the target of wedelolactone[3].Wedelolactone (0-5 μg/ml; 6 d) inhibits c-src, c-fos and cathepsin k expression level[3].
Cell Differentiation Assay[3] | Cell Line: | Mouse BMSC | | Concentration: | 0-5 μg/mL | | Incubation Time: | 0, 6, 9, 12 and 21 days | | Result: | Increased Mouse BMSC into osteoblastic cells and dose-dependently increased the activity of alkaline phosphatase at incubation for 9 days. |
Western Blot Analysis[3] | Cell Line: | Mouse BMSC and RAW264.7 cells | | Concentration: | 0-5 μg/mL | | Incubation Time: | 0-9 days | | Result: | Decreased GSK3β expression level and up-regulated GSK3β phosphorylation, nuclear accumulation of β-catenin and runx2 in BMSC. Inhibited RANKL-induced phosphorylation of NF-κB/p65 and the expression level of c-fos and c-Src. |
Cell Viability Assay[3] | Cell Line: | Mouse BMSC | | Concentration: | 0.1, 1.25, 2.5, 5 μg/ml | | Incubation Time: | 60 min | | Result: | Inhibited GSK3β activity with an IC50of 21.7 μM weeker than staurosporin which is a GSK3β inhibitor and proved GSK3β is a target. |
RT-PCR[3] | Cell Line: | RAW264.7 cells | | Concentration: | 0, 0.6, 1.25, 2.5 and 5 μg/mL | | Incubation Time: | 6 days | | Result: | Inhibited the expression of osteoclast differentiation related marker genes c-src, c-fos and cathepsin in RAW264.7 cells. |
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体内研究
(In Vivo) | Wedelolactone (10 mg/kg; i.p. every 2 days for 4 weeks) decreases bone volumn and trabecular number at the femur after ovarietomy, and prevents the VOX-induced bone loss[3].
| Animal Model: | Ovariectomized 9-week-old mice[3] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; 10 mg/kg every 2 days; for 4 weeks | | Result: | Inhibited osteoclast activity and stimulated osteoblast differentiation to achieved osteoprotective effect. |
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| 来源 | - Plants
- Compositae
- Eclipta prostrata(Linn.) Linn.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(397.77 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.1822 mL | 15.9109 mL | 31.8218 mL | | 5 mM | 0.6364 mL | 3.1822 mL | 6.3644 mL | | 10 mM | 0.3182 mL | 1.5911 mL | 3.1822 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-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
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此方案可获得 ≥ 2.08 mg/mL (6.62 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%corn oil Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.62 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 20.8 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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