Glycycoumarin 是一种有效的抗痉挛剂。Glycycoumarin 是甘草的主要生物活性香豆素,具有抗痉挛活性。Glycycoumarin 还具有保肝作用。Glycycoumarin 可用于腹痛和肝脏疾病的研究。
生物活性 | Glycycoumarin is a potentantispasmodicagent. Glycycoumarin is a major bioactive coumarin of licorice and exhibits antispasmodic activity. Glycycoumarin also has hepatoprotective effect. Glycycoumarin can be used for the research of abdominal pain and liver diseases[1][2]. |
体外研究 (In Vitro) | Glycycoumarin, (25 μM; 24 h) combining with ABT-737 (12.5 μM) synergistically, induces cell death in multiple types of liver cancer cell HepG2[2]. Glycycoumarin is highly effective against alcoholic liver disease, nonalcoholic fatty liver disease, acetaminophen-induced hepatotoxicity, and liver cancer through mechanisms involved in activation of Nrf2 antioxidant system, stimulation of AMPK-mediated energy homeostasis, induction of autophagy degradation process, and inhibiting oncogenic kinase T-lymphokine-activated killer cell-originated protein kinase activity[3].
Cell Viability Assay[2] Cell Line: | HepG2, SMMC-7721, and Huh-7 | Concentration: | 10, 20, 25, 30, and 40 μM | Incubation Time: | 24 hours | Result: | Induced cell death in multiple types of liver cancer cell lines in a dose-dependent manner. |
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体内研究 (In Vivo) | Glycycoumarin (30 μM-0.3 nM; 5 min) has an inhibitory effect on smooth muscle contraction induced by various types of stimulants through the inhibition of PDEs, especially isozyme 3, followed by the accumulation of intracellular cAMP[1].
Glycycoumarin (10 mg/kg; i.p.; once daily for 4 d) enhances tumor growth inhibition in HepG2 xenograft model in mice and shows synergistical effect withABT-737(HY-50907)[2].
Animal Model: | Male ICR mice (aged 6 weeks, weight 25-30 g)[1] | Dosage: | 30 μM-0.3 nM, 5 min | Administration: | | Result: | Inhibited the contraction induced by various types of stimulants, such as CCh, KCI, BaCI(2), and A23187 (calcium ionophore III). Enhanced the relaxation induced by forskolin on CCh-evoked contraction and also enhances the relaxation effect of rolipram. Associated with dose-dependent accumulation of cAMP. |
Animal Model: | HepG2 cancer cells xenograft model in male BALB/c athymic nude mice (6-7 weeks old)[2] | Dosage: | 10 mg/kg | Administration: | Intraperitoneal injection; once daily for 4 days; ABT-737 group was given 100 mg/kg i.p. | Result: | Inhibited tumor growth and resulted a reduction of the final tumor weight by 17%. |
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结构分类 | - Phenylpropanoids
- Coumarins
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来源 | - Plants
- Leguminosae
- Glycyrrhiza uralensisFisch.
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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 | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(678.65 mM;Need ultrasonic) 配制储备液 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL | 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL | 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |
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此方案可获得 ≥ 2.08 mg/mL (5.65 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 (5.65 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.65 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 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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