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Icariin Sale

(Synonyms: 淫羊藿甙; Ieariline) 目录号 : GN10278

Icariin is a flavonol glycoside.

Icariin Chemical Structure

Cas No.:489-32-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥261.00
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50mg
¥269.00
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100mg
¥450.00
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实验参考方法

Cell experiment [1]:

Cell lines

OA chondrocytes

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.

Reaction Conditions

20, 40, or 80 µM

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]:

Animal models

BALB/c mice

Preparation Method

MDA‐MB‐231 tumor‐bearing mice and 4T1 tumor‐bearing mice were treated with icariin at 20 and 40 mg/kg.

Dosage form

20 and 40 mg/kg; i.p.

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.

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.
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.

产品描述

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].

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]

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.

[1] 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.

[2] 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.

Chemical Properties

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
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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
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