Icariin
(Synonyms: 淫羊藿甙; Ieariline) 目录号 : GN10278
淫羊藿甙是一种黄酮醇糖苷。淫羊藿甙抑制PDE5和PDE4活性的IC50分别为432 nM和73.50 μM。
Cas No.:489-32-7
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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| Cell experiment [1]: | |
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Cell lines |
OA chondrocytes |
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Preparation Method |
For the in vitro experiments, we sorted OA chondrocytes into six groups, with the cells in these groups being incubated with blank medium (control), 100 nM rapamycin (rapamycin), 12 mM 3-methyladenine (3-methyladenine), or 20, 40, or 80 µM icariin. AO-PI staining and flow cytometry were performed on the treated chondrocytes to evaluate apoptosis. |
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Reaction Conditions |
20, 40, or 80 µM |
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Applications |
Relative to the control, the apoptotic rate of OA chondrocytes showed an increase from 20.25% to 37.56% after 3-methyladenine treatment and a decrease to 11.76% and 16.12%, 12.75%, and 11.04% after treatment with rapamycin and 20, 40, and 80 µM icariin, respectively. |
| Animal experiment [2]: | |
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Animal models |
BALB/c mice |
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Preparation Method |
MDA‐MB‐231 tumor‐bearing mice and 4T1 tumor‐bearing mice were treated with icariin at 20 and 40 mg/kg. |
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Dosage form |
20 and 40 mg/kg; i.p. |
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Applications |
Treatment with icariin at 20 mg/kg or 40 mg/kg significantly inhibited MDA‐MB‐231 tumor growth and weight in a dose‐dependent manner compared with the control group. |
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References: Tang Y, et al. Icariin alleviates osteoarthritis by regulating autophagy of chondrocytes by mediating PI3K/AKT/mTOR signaling. Bioengineered. 2021 Dec;12(1):2984-2999. |
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Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50 of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator[1]. It has exert anti-oxidative, anti-neuroinflammatory, and anti-apoptotic effects[2].
In vitro experiment it shown that treatment of 10 or 20 μM induced 13.1 ± 2.1% and 18.2 ± 1.6% apoptosis in MDA‐MB‐453 cells respectively in comparison with control group. 4T1 cells were treated with 20 μM icariin triggered cell apoptosis[3].
In vivo, rats were injected in 50 mg/kg Icariin significantly reduced paw swelling in carrageenan-injected animals and ameliorated carrageenan-induced paw histopathological alterations. Icariin obviously increased paw enzymatic and non-enzymatic antioxidants and decreased paw lipid peroxidation. Icariin decreased paw levels of inflammatory cytokines and NF-kB[4].
In vivo, rats were administrated with 25 mg/kg and 50 mg/kg icariin improved depression symptoms via regulation of the PI3K-AKT pathway, boosted the expression of the regulatory methylene p85 and catalytic methylene p110 of PI3K, increased the relative expression of p-AKT, and encouraged the expression of the anti-apoptosis factor Bcl-2, thus elevating the ratio of Bcl-2/Bax[5]. In vivo, C57BL/6 J mice were administrated with 50 mg/kg/d icariin effectively attenuated alcohol consumption-induced atrial structural and electrical remodeling[6].
References:
[1] Xin ZC, et al. Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8.
[2] Jin J, et al. An outline for the pharmacological effect of icariin in the nervous system. Eur J Pharmacol. 2019 Jan 5;842:20-32.
[3] Song L, et al. Icariin-induced inhibition of SIRT6/NF-κB triggers redox mediated apoptosis and enhances anti-tumor immunity in triple-negative breast cancer. Cancer Sci. 2020 Nov;111(11):4242-4256.
[4] El-Shitany NA, Eid BG. Icariin modulates carrageenan-induced acute inflammation through HO-1/Nrf2 and NF-kB signaling pathways. Biomed Pharmacother. 2019 Dec;120:109567.
[5] Cao LH, et al. PI3K-AKT Signaling Activation and Icariin: The Potential Effects on the Perimenopausal Depression-Like Rat Model. Molecules. 2019 Oct 15;24(20):3700.
[6] Yu LM, et al. Icariin attenuates excessive alcohol consumption-induced susceptibility to atrial fibrillation through SIRT3 signaling. Biochim Biophys Acta Mol Basis Dis. 2022 Oct 1;1868(10):166483.
淫羊藿甙是一种黄酮醇糖苷。淫羊藿甙抑制PDE5和PDE4活性的IC50分别为432 nM和73.50 μM。淫羊藿甙也是PPARα激活剂[1]。它具有抗氧化、抗炎和抗细胞凋亡的作用[2]。
体外实验表明，与对照组相比，10或20 μM淫羊藿甙处理分别诱导MDA‐MB‐453细胞凋亡13.1±2.1%和18.2±1.6%。用20 μM 淫羊藿甙处理4T1细胞，引发细胞凋亡[3]。
在体内，大鼠注射50 mg/kg的淫羊藿甙显著减少了卡拉胶注射动物的爪子肿胀，并改善了卡拉胶诱导的爪子组织病理学改变。淫羊藿甙能明显增加爪酶和非酶抗氧化剂，降低爪脂过氧化。淫羊藿甙降低了爪子炎症细胞因子和NF-kB的水平[4]。在体内，给予25 mg/kg和50 mg/kg的淫羊藿甙通过调节PI3K-AKT通路改善抑郁症状，增强PI3K的调节性亚甲基p85和催化性亚甲基p110的表达，增加p-AKT的相对表达，并促进抗凋亡因子Bcl-2的表达，从而提高Bcl-2/Bax的比例[5]。在体内，C57BL/6 J小鼠给予50 mg/kg/d的淫羊藿甙，有效地减轻了饮酒诱导的心房结构和电重构[6]。
| Cas No. | 489-32-7 | SDF | |
| 别名 | 淫羊藿甙; Ieariline | ||
| 化学名 | 5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxychromen-4-one | ||
| Canonical SMILES | CC1C(C(C(C(O1)OC2=C(OC3=C(C2=O)C(=CC(=C3CC=C(C)C)OC4C(C(C(C(O4)CO)O)O)O)O)C5=CC=C(C=C5)OC)O)O)O | ||
| 分子式 | C33H40O15 | 分子量 | 676.65 |
| 溶解度 | ≥ 30.5mg/mL in DMSO | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4779 mL | 7.3893 mL | 14.7787 mL |
| 5 mM | 0.2956 mL | 1.4779 mL | 2.9557 mL |
| 10 mM | 0.1478 mL | 0.7389 mL | 1.4779 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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