中文名 | 秦皮乙素 |
英文名 | Esculetin |
中文别名 | - |
英文别名 | 6,7-Dihydroxycoumarin; Aesculetin; Cichorigenin; Esculetol |
来源 | 白蜡树Fraxinus chinensis Roxb;续随子Euphorbia lathyris L. |
化合物类型 | 苯丙素类(Phenylpropanoids)>香豆素类(Coumarins) |
化学式 | C9H6O4 |
分子量 | 178.14 |
CAS号 | 305-01-1 |
纯度 | 98%, HPLC |
溶剂/溶解度 |
DMSO: 33 mg/ml (185.2 mM) Ethanol: <1 mg/ml Water: <1 mg/ml |
溶液配制 | 2mg加入1.12ml DMSO,或者每1.78mg加入1ml DMSO,配制成10mM溶液。 |
产品描述 | Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities. | ||||
信号通路 | PI3K/Akt; Cell cycle; Apoptosis | ||||
靶点 | Caspase-3 | Caspase-9 | - | - | - |
IC50 | - | - | - | - | - |
体外研究 | Esculetin decreases cell proliferation by inducing G1 phase cell cycle arrest, which is associated with the down-regulation of cyclin D1/CDK4 and cyclin E/CDK2 complexes by the activation of p27KIP. Esculetin significantly inhibits proliferation of HCC cells in a concentration- and time-dependent manner and with an IC50 value of 2.24 mM. It blocks the cell cycle at S phase and induces apoptosis in SMMC-7721 cells with significant elevation of caspase-3 and caspase-9 activity, but does not affect caspase-8 activity. Esculetin treatment results in the collapse of mitochondrial membrane potential in vitro and in vivo accompanied by increased Bax expression and decreased Bcl-2 expression at both transcriptional and translational levels. Esculetin exerts in vitro and in vivo antiproliferative activity in hepatocellular carcinoma, and its mechanisms involved initiation of a mitochondrial-mediated, caspase-dependent apoptosis pathway. | ||||
体内研究 | Esculetin significantly decreases tumor growth in mice bearing Hepa1-6 cells. Tumor weight is decreased by 20.33, 40.37, and 55.42% with increasing doses of esculetin. Of note, esculetin has no obvious toxicity in this animal study. In a rat experimental model of inflammatory bowel disease induced by trinitrobenzenesulfonic acid, esculetin at the dose of 5 mg/kg displays intestinal anti-inflammatory activity. | ||||
临床实验 | N/A |
1.Xie C, et al. Phytother Res. 2019,33(11):3008-3015.
2.Park SS, et al. Oncol Rep. 2011,25(1):223-30.
3.Wang J, et al. Braz J Med Biol Res. 2015,48(3):245-53.
4.A. Witaicenis, et al. European Journal of Inflammation. 2013,11(2):433-446.
包装清单:产品编号 | 产品名称 | 包装 |
SM1150-10mM | 秦皮乙素(98%, HPLC) | 10mM×0.2ml |
SM1150-25mg | 秦皮乙素(98%, HPLC) | 25mg |
SM1150-100mg | 秦皮乙素(98%, HPLC) | 100mg |
- | 说明书 | 1份 |
-20℃保存,至少一年有效。固体粉末4℃保存,至少一个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:本产品可能对人体有一定的毒害作用,请注意适当防护,以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
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