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Icariin

CAS No. : 489-32-7

MCE 站：Icariin

产品活性：Icariin 是一种黄酮醇苷。 Icariin 抑制 PDE5 和 PDE4 活性，IC₅₀ 分别为 432 nM 和 73.50 μM。Icariin 也是一种 PPARα 激活剂。

研究领域：Metabolic Enzyme/Protease  |  Cell Cycle/DNA Damage  |  Autophagy

作用靶点：Phosphodiesterase (PDE)  |  PPAR  |  Autophagy

In Vitro: 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.

In Vivo: 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.

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