中文名 | 大黄素 |
英文名 | Emodin |
中文别名 | - |
英文别名 | Rheum-emodin; Frangula emodin; Archin; Frangulinic acid; Emodol; Alatinone |
来源 | 何首乌Polygonum multiflorum Thunb.;掌叶大黄Rheum palmatum L.;鸡爪大黄Rheum tanguticum Maxim. ex Regel |
化合物类型 | 醌类(Quinones)>蒽醌>大黄素型蒽醌 |
化学式 | C15H10O5 |
分子量 | 270.24 |
CAS号 | 518-82-1 |
纯度 | 98%, HPLC |
溶剂/溶解度 |
DMSO: 12.5 mg/ml (46.26 mM) Water: < 0.1 mg/ml (insoluble) |
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 | Emodin (Frangula emodin), an anthraquinone derivative isolated from genus Rheum and Polygonum, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice. | ||||
信号通路 | - | ||||
靶点 | Mouse 11β-HSD1 | Human 11β-HSD1 | SARS-CoV | CK2α Wild-type | - |
IC50 | 86 nM | 186 nM | - | - | - |
体外研究 | Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC50 value of 200 μM. Emodin (5-50 μM) inhibits the S protein-pseudotyped retrovirus infectivity in a dose-dependent manner. Emodin blocks the SARS-CoV S protein binding to Vero E6 cells. Emodin inhibits casein kinase-2 (CK2) with IC50s of 5.9, 30.0, and 7.1 μM for CK2α Wild-type, Ile174Ala mutant, and His160Ala mutant at ATP concentration is 50 μM, respectively. The IC50s are 1.40 and 38.00 μM for CK2α Wild-type, and Val66Ala mutant at ATP concentration is 10 μM. Emodin exhibits low inhibitory activity against mouse and human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), with an IC50 higher than 1 mM, indicating that Emodin is more than 5000-fold selective for the human and mouse 11β-HSD1 enzymes over the type 2 isoenzyme. | ||||
体内研究 | Emodin (single oral administration of 100 or 200 mg/kg) inhibits 11β-HSD1 activity in normal C57BL/6J male mice. Emodin (100 mg/kg; oral administration; b.i.d.) improves insulin sensitivity and lipid metabolism, and lowers blood glucose and hepatic PEPCK, and glucose-6-phosphatase mRNA in diet-induced obese (DIO) mice. | ||||
临床实验 | NCT00801268: Polycystic Kidney, Not Applicable. |
1.Tin-Yun Ho, et al. Antiviral Res. 2007,74(2):92-101.
2.Stefania Sarno, et al. Pharmacol Ther. 2002,93(2-3):159-68.
3.Ying Feng, et al. Br J Pharmacol. 2010,161(1):113-26.
包装清单:产品编号 | 产品名称 | 包装 |
SM3021-10mM | 大黄素(98%, HPLC) | 10mM×0.2ml |
SM3021-25mg | 大黄素(98%, HPLC) | 25mg |
SM3021-100mg | 大黄素(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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