| 中文名 | 淫羊藿苷 |
| 英文名 | Icariin |
| 中文别名 | 淫羊藿甙 |
| 英文别名 | Ieariline |
| 来源 | 淫羊藿Epimedium brevicornu Maxim. |
| 化合物类型 | 黄酮类(Flavonoids)>黄酮>黄酮醇 |
| 化学式 | C33H40O15 |
| 分子量 | 676.66 |
| CAS号 | 489-32-7 |
| 纯度 | 98%, HPLC |
| 溶剂/溶解度 |
DMSO: ≥ 34 mg/ml (50.25 mM); Water: < 0.1 mg/ml (insoluble) |
| 溶液配制 | 10mg加入1.48ml DMSO，或者每6.77mg加入1ml DMSO，配制成10mM溶液。 |
| 产品描述 | Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator. | ||||
| 信号通路 | Autophagy | ||||
| 靶点 | PDE5 | PDE4 | PPARα | - | - |
| IC50 | 432 nM | 73.50 μM | - | - | - |
| 体外研究 | Icariin is a cGMP-specific PDE5 inhibitor. The inhibitory effects of Icariin on PDE5 and PDE4 activities are investigated by the two-step radioisotope procedure with 3H-cGMP/3H-cAMP. The potency of selectivity of Icariin on PDE5 (PDE4/PDE5 of IC50) is 167.67 times. Cell viability is measured in the present study to evaluate whether Icariin protect endothelial HUVECs from injuries induced by oxidized low-density lipoprotein (ox-LDL). The exposure of the cells to ox-LDL for 24 h significantly decreases the cell viability compared with control group (P<0.05). However, Icariin can inhibit cell injury induced by ox-LDL in a concentration-dependent manner, and has significant difference (P<0.05) compared with ox-LDL-simulated group. Icariin protects BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway. | ||||
| 体内研究 | Icariin is a PPARα activator, induces Cyp4a10 and Cyp4a14, and regulates the mRNA levels of lipid metabolism enzymes and proteins, including fatty acid binding protein, fatty acid oxidation in mitochondria and in peroxisome. Icariin is effective in the treatment of hyperlipidemia. To understand the effect of Icariin on lipid metabolism, effects of Icariin on PPARα and its target genes are investigated. Mice are treated orally with Icariin at doses of 0, 100, 200, and 400 mg/kg, or Clofibrate (500 mg/kg) for five days. Liver total RNA is isolated and the expressions of PPARα and lipid metabolism genes are examined. PPARα and its marker genes Cyp4a10 and Cyp4a14 are induced 2-4 fold by Icariin, and 4-8 fold by Clofibrate. The fatty acid (FA) binding and co-activator proteins Fabp1, Fabp4 and Acsl1 are increased 2-fold. The mRNAs of mitochondrial FA β-oxidation enzymes (Cpt1a, Acat1, Acad1 and Hmgcs2) are increased 2-3 fold. The mRNAs of proximal β-oxidation enzymes (Acox1, Ech1, and Ehhadh) are also increased by Icariin and Clofibrate. The expression of mRNAs for sterol regulatory element-binding factor-1 (Srebf1) and FA synthetase (Fasn) are unaltered by Icariin. The lipid lysis genes Lipe and Pnpla2 are increased by Icariin and Clofibrate. Adult rats are treated orally with Icariin at doses of 0 (control), 50, 100, or 200 mg/kg body weight for 35 consecutive days. The results show that Icariin has virtually no effect on the body weight or organ coefficients of the testes or epididymides. However, 100 mg/kg Icariin significantly increases epididymal sperm counts. In addition, 50 and 100 mg/kg Icariin significantly increase testosterone levels. Furthermore, 100 mg/kg Icariin treatment also affects follicle stimulating hormone receptor (FSHR) and claudin-11 mRNA expression in Sertoli cells. Superoxide dismutase (SOD) activity and malondialdehyde (MDA) levels are measured in the testes; 50 and 100 mg/kg Icariin treatment improve antioxidative capacity, while 200 mg/kg Icariin treatment upregulates oxidative stress. | ||||
| 临床实验 | NCT01979133: Bipolar Disorder|Substance Use Disorder, Phase 3; NCT02112123: the Pharmacokinetic Profile of Icariin in Humans, Phase 1. | ||||
1.Xin ZC, et al. Asian J Androl. 2003,5(1):15-8.
2.Lu YF, et al. Molecules. 2014,19(11):18179-91.
3.Hu Y, et al. Int J Clin Exp Med. 2015,8(3):3585-9.
4.Chen M, et al. Molecules. 2014,19(7):9502-14.
5.Liu D, et al. Life Sci. 2020,253:117730.
包装清单：| 产品编号 | 产品名称 | 包装 |
| SM2199-10mM | 淫羊藿苷(98%, HPLC) | 10mM×0.2ml |
| SM2199-25mg | 淫羊藿苷(98%, HPLC) | 25mg |
| SM2199-100mg | 淫羊藿苷(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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