| 中文名 | 欧前胡素 |
| 英文名 | Imperatorin |
| 中文别名 | 白茅苷；前胡素；主人草素；白芷乙素；欧芹属素乙；前胡内酯 |
| 英文别名 | Marmelide; Ammidin; Marmelosin |
| 来源 | 白芷Angelica dahurica （Fisch. ex Hoffm.）Benth. et Hook. f. ex Franch. et Sav；前胡Peucedanum praeruptorum Dunn |
| 化合物类型 | 苯丙素类(Phenylpropanoids)>香豆素(Coumarins) |
| 化学式 | C16H14O4 |
| 分子量 | 270.28 |
| CAS号 | 482-44-0 |
| 纯度 | 98%, HPLC |
| 溶剂/溶解度 |
Water: < 0.1 mg/ml (insoluble); DMSO: 50 mg/ml (184.99 mM) |
| 溶液配制 | 5mg加入1.85ml DMSO，或者每2.70mg加入1ml DMSO，配制成10mM溶液。 |
| 产品描述 | Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM. | ||||
| 信号通路 | - | ||||
| 靶点 | NO Synthesis | BChE | TRPV1 | - | - |
| IC50 | 9.2 μM | 31.4 μM | 12.6±3.2 μM | - | - |
| 体外研究 | Imperatorin is a plant secondary metabolite belonging to the coumarins-specifically the furanocoumarins. Imperatorin enhances the GABA-induced chloride ion current (IGABA) through the α1β2γ2S receptors. Imperatorin potentiates IGABA at 100 μmol by 50.5±16.3 % and at 300 μmol by 109.8±37.7 %, respectively. Imperatorin, together with Phellopterin, found in the roots of A. dahurica, inhibit [3H]diazepam binding to the benzodiazepine site of the rat brain GABAA receptor in vitro with an IC50 of 12.3 μmol for Imperatorin and 400 nmol for Phellopterin. Imperatorin, in a concentration ranging from 3.5 to 14 mmol, significantly and irreversibly inhibits GABA-T in a time-dependent and concentration-dependent manner, by irreversibly binding with the active site of GABA-T.Imperatorin is a reversible acetylcholinesterase (AChE) inhibitor, and acts in dose-dependent manner. The AChE and BChE inhibitory activities of Imperatorin and a crude extract from the fruits of Angelica archangelica L. is tested by the spectrophotometric method at concentrations of 12.5, 25, 50, and 100 μg/ml. Imperatorin displays low inhibition towards AChE (13.75-46.11 %), whereas it has remarkable inhibitory effect against BChE (37.46-83.98 %). Imperatorin shows selectivity toward BChE rather than AChE, with an IC50 for BChE of 31.4 μmol. Imperatorin, together with (+)-Byakangelicol, are found to be the most effective BACE-1 inhibitors, with IC50s of 91.8 and 104.9 μmol, respectively. Imperatorin (IC50=9.2 μmol) is also effective as an inhibitor of NO synthesis. Imperatorin is a weak agonist of TRPV1, a channel implicated in detecting several noxious stimuli, exhibiting EC50 of 12.6±3.2 μM. | ||||
| 体内研究 | At doses of 10 and 20 mg/kg and 30 min after injection, Imperatorin shows an anxiolytic effect and improved different stages of memory and learning processes-both acquisition and consolidation. It is also shown that acute administration Imperatorin at doses of 10 and 20 mg/kg reduced the anxiogenic effect of nicotine (0.1 mg/kg, subcutaneous, s.c.). At 30 and 40 mg/kg, i.p. Imperatorin significantly potentiates the anticonvulsant activity of carbamazepine against maximal electroshock-induced seizures expressed by lowering the ED50 from 10.8 to 6.8 mg/kg (by 34 %) and 6 mg/kg (by 42 %), respectively. Moreover, Imperatorin at 30 mg/kg and carbamazepine at 6.8 mg/kg shows increases the total brain concentration of carbamazepine from 1.260 to 2.328 μg/ml (by 85%), which may be caused by modifying the blood-barrier permeability or acting like an inhibitor of multi-drug resistance proteins. Imperatorin, a naturally occurring furanocoumarin, inactivates gamma-aminobutyric acid transaminase and inhibits acetylcholinesterase activity. Imperatorin administered acutely at the doses of 5 and 10 mg/kg prior to the injection of scopolamine (1 mg/kg) improves memory acquisition and consolidation impaired by scopolamine. Furthermore, repeatable (7 days, twice daily) administration of the highest dose of Imperatorin (10 mg/kg) significantly attenuates the effects of scopolamine on memory acquisition, whereas the doses of 5 and 10 mg/kg of this furanocoumarin are effective when memory consolidation is measured. | ||||
| 临床实验 | N/A | ||||
1.Kozioł E, et al. Phytochem Rev. 2016,15:627-649.
2.Chen X, et al. J Biol Chem. 2014,289(14):9600-10.
3.Budzynska B, et al. Psychopharmacology (Berl). 2015,232(5):931-42.
包装清单：| 产品编号 | 产品名称 | 包装 |
| SM1123-10mM | 欧前胡素(98%, HPLC) | 10mM×0.2ml |
| SM1123-25mg | 欧前胡素(98%, HPLC) | 25mg |
| SM1123-100mg | 欧前胡素(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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