Costunolide ((+)-Costunolide) 是一种天然的倍半萜内酯,它具有抗氧化、抗炎、抗过敏、骨重塑、神经保护、促进毛发生长、抗癌和抗糖尿病的特性。Costunolide 可诱导乳腺癌细胞周期阻滞和凋亡 (apoptosis)。
生物活性 | Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest andapoptosison breastcancercells[1][2][3]. |
IC50& Target | Human Endogenous Metabolite |
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体外研究 (In Vitro) | Costunolide inhibits the colony formation, migrative and invasive abilities of the H1299 cells in a dose or time dependent manner[2]. Costunolide (6.7-215.2 μM; 24 hours) inhibits the viability of H1299 cells in a dose-dependent manner, with an IC50of 23.93 μM[2]. Costunolide (12.0-48.0 μM; 48 hours) induces apoptosis in H1299 cells[2]. Costunolide (12-48.0 μM; 6-12 hours) regulates metastasis- and proliferation-associated mRNA expression[2]. Costunolide regulates epithelial-to-mesenchymal transition (EMT)-associated protein expression[2]. Costunolide regulates c-Myc mediated apoptosis signaling and 14-3-3-mediated signaling pathways in breast cancer cells[3].
Cell Viability Assay[2] Cell Line: | H1299 cells | Concentration: | 6.7 μM, 13.5 μM, 26.9 μM, 107.6 μM, 215.2 μM | Incubation Time: | 24 hours | Result: | Inhibited the viability of H1299 cells (MTT assay). |
Apoptosis Analysis[2] Cell Line: | H1299 cells | Concentration: | 0 μM, 12.0 μM, 24.0 μM, 48.0 μM | Incubation Time: | 48 hours | Result: | Significantly promoted apoptosis at 24.0 μM and 48.0 μM. |
RT-PCR[2] Cell Line: | H1299 cells | Concentration: | 0 μM, 12.0 μM, 24.0 μM, 48.0 μM | Incubation Time: | 6 hours, 12 hours | Result: | Regulated the metastasis- and proliferation-associated mRNA levels in a dose-dependent manner. |
Western Blot Analysis[2] Cell Line: | H1299 cells | Concentration: | 0 μM, 12.0 μM, 24.0 μM, 48.0 μM | Incubation Time: | 48 hours | Result: | Significantly inhibited the EMT of H1299 cells. |
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体内研究 (In Vivo) | Costunolide (20 mg/kg; i.p; daily; for 30 days) inhibits breast cancer through c-Myc/p53 and AKT/14-3-3 pathway[3].
Animal Model: | 4 weeks old female BALB/c nude mice, MDA-MB-231 cells xenograft mouse models[3] | Dosage: | 20 mg/kg | Administration: | Intraperitoneal injection, daily, for 30 days | Result: | Reduced the expression levels of c-Myc and p-AKT and elevated the expression levels of p53 and p-14-3-3. |
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来源 | - Plants
- Compositae
- Aucklandia lappaDecne
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : ≥ 49 mg/mL(210.92 mM) Ethanol : 25 mg/mL(107.61 mM;ultrasonic and warming and heat to 60℃) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 4.3044 mL | 21.5220 mL | 43.0441 mL | 5 mM | 0.8609 mL | 4.3044 mL | 8.6088 mL | 10 mM | 0.4304 mL | 2.1522 mL | 4.3044 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 (sealed storage, away from moisture and 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% EtOH 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.76 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 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% EtOH 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.76 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 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% EtOH 90%corn oil Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.76 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 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (8.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (8.95 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。 5. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (8.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (8.95 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。 6. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (8.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (8.95 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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