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(-)-Epicatechin

(-)-Epicatechin (Epicatechin)属于天然产物，是一种COX-1抑制剂（IC50=3.2 μM），具有细胞渗透性。通过阻断NF-κB的p65亚基核定位，抑制IL-1β诱导的iNOS表达，具有显著抗炎活性。

CAS号

490-46-0

分子式

C15H14O6

主要靶点

COX|Endogenous Metabolite|Ferroptosis

仅限科研使用

Cat No : CM00724

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Synonyms

COX|Endogenous Metabolite|(-)-Epicatechol|L-Epicatechin|Epicatechol|Epicatechin|epi-Catechin|EndogenousMetabolite|Ferroptosis|表儿茶素

验证数据展示

  • CAS No.: 490-46-0

    (-)-Epicatechin
    CAS#: 490-46-0

产品信息

(-)-Epicatechin (Epicatechin) belongs to natural products and is a COX-1 inhibitor (IC50 = 3.2 μM) with cell permeability. By blocking the nuclear localization of the p65 subunit of NF-κB, this compound inhibits IL-1β-induced iNOS expression and possesses significant anti-inflammatory activity.

CAS号 490-46-0
分子式 C15H14O6
主要靶点 COX|Endogenous Metabolite|Ferroptosis
主要通路 免疫与炎症|神经科学|代谢|凋亡
分子量 290.27
纯度 98.61%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 COX|Endogenous Metabolite|(-)-Epicatechol|L-Epicatechin|Epicatechol|Epicatechin|epi-Catechin|EndogenousMetabolite|Ferroptosis|表儿茶素

靶点活性

MDA-MB-231 cells:85 μM|COX-1:3.2 μM

体内活性

方法：采用26月龄C57BL/6老年小鼠，灌胃给予(-)-Epicatechin（1 mg/kg，每日两次）连续2周（溶剂为水）；另对6名中年受试者（41±5岁）给予(-)-Epicatechin胶囊（25 mg，每日两次）连续7天，检测肌肉调节因子及手握力。 结果：(-)-Epicatechin降低老年小鼠升高的肌肉抑制素和β-半乳糖苷酶，增加follistatin和Myf5；在人类中增加手握力（~7%）及血浆follistatin/肌肉抑制素比率，逆转衰老相关变化。[2] 方法：采用5月龄C57BL/6雄性小鼠，随机分为对照组、训练组、训练后停训14天给予安慰剂（水）组和训练后停训14天给予(-)-Epicatechin（1 mg/kg，灌胃，每日两次）组，检测骨骼肌毛细血管密度、VEGF-A/TSP-1表达、氧化酶活性及耐力。 结果：与安慰剂组相比，(-)-Epicatechin显著增加停训小鼠骨骼肌毛细血管密度和氧化酶活性，维持线粒体复合物IV和细胞色素c氧化酶活性，减少VEGF-A/TSP-1比值下降，耐力保持与训练组相当。[3]

体外活性

方法：用(-)-Epicatechin处理Panc-1、U87、MIA PaCa-2癌细胞及人正常成纤维细胞，检测线粒体呼吸、氧气消耗及联合辐射下的辐射敏感性、Chk2磷酸化和p21诱导水平。 结果：(-)-Epicatechin仅刺激Panc-1细胞线粒体呼吸和氧气消耗；选择性提高癌细胞辐射敏感性（Panc-1、U87、MIA PaCa-2的REF分别为1.7、1.5、1.2），对正常成纤维细胞无增强（REF=0.9）；联合辐射时，仅在癌细胞中增加Chk2磷酸化和p21诱导。[1]

溶解度

0.5% CMC-Na:5 mg/mL (17.23 mM);DMSO:80 mg/mL (275.61 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);50% PEG300+50% Saline:5 mg/mL (17.23 mM);H2O:2.25 mg/mL (7.75 mM)

细胞实验

Panc-1 cells are seeded into T-150 flasks and on the next day, cells are treated with different concentrations of (-)-epicatechin for 1 h, then harvested and solubilized in 10 mM HEPES (pH 7.4), 40 mM KCl, 1%Tween-20, 1 μM oligomycin, 1 mM PMSF,10 mM KF, 2 mM EGTA, and 1 mM Na3VO4. COX activity is measured in the presence of 20 mM ascorbate and 200 μM substrate cytochrome c from cow heart.(Only for Reference)

参考文献

1.Elbaz, Hosam A et al. Epicatechin stimulates mitochondrial activity and selectively sensitizes cancer cells to radiation. PloS one vol. 9,2 e88322. 6 Feb. 2014.
2.Gutierrez-Salmean, Gabriela et al. Effects of (-)-epicatechin on molecular modulators of skeletal muscle growth and differentiation. The Journal of nutritional biochemistry vol. 25,1 (2014): 91-4.
3.Hüttemann, Maik et al. (-)-Epicatechin maintains endurance training adaptation in mice after 14 days of detraining. FASEB journal : official publication of the Federation of American Societies for Experimental Biology vol. 26,4 (2012): 1413-22.
4.Jang S A, Hwang Y H, Kim T, et al. Anti-Osteoporotic and Anti-Adipogenic Effects of the Water Extract of Drynaria roosii Nakaike in Ovariectomized Mice Fed a High-Fat Diet[J]. Molecules. 2019, 24(17): 3051.
5.Shim K S, Hwang Y H, Jang S A, et al. Ethanol Extract of Amomum tsao-ko Ameliorates Ovariectomy-Induced Trabecular Loss and Fat Accumulation[J]. Molecules. 2021, 26(4): 784.
6.Shim K S, Hwang Y H, Jang S A, et al. . Water Extract of Lysimachia christinae Inhibits Trabecular Bone Loss and Fat Accumulation in Ovariectomized Mice[J]. Nutrients.  2020, 12(7): 1927.

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