| 生物活性： |
靶点：Casein Kinase（CK）
通路：Cell Cycle;DNA Damage/DNA Repair; Stem Cells
背景说明：Ellagic acid是一种抗氧化剂,为有效的,ATP 竞争性的 CK2 抑制剂。
生物活性：Ellagic acid 是一种天然的抗氧化剂，为有效的，ATP 竞争性的 CK2 抑制剂，IC50 和 Ki 值分别为 40 nM 和 20 nM。[1-3]
In Vitro：鞣花酸是一种有效的CK2抑制剂，IC50为40 nM，Ki为20 nM。鞣花酸还可以阻断其他激酶，如LYN，PKA，SYK，GSK3，FGR和CK1，IC50分别为2.9，3.5，4.3，7.5，9.4和13.0μM，对DYRK1a，CSK，NPM-没有明显影响。 ALK，RET和FLT3(IC50>40μM)。鞣花酸(5-100μM)显示出对Karpas299，SUDHL1，SR786和FE-PD细胞系的抑制活性[1]。鞣花酸(10μM)在辐射处理后对MCF-7细胞显示出细胞毒性作用。鞣花酸(10μM)与辐射(IR)组合显著地削弱了MCF-7细胞形成集落的能力，等同于单独处理。具有IR的鞣花酸还诱导细胞凋亡，并促进MCF-7细胞中前凋亡Bax的上调和Bcl-2的下调[3]。
In Vivo：鞣花酸(EA; 10mg/kg /天; po，14天)使MDA脑含量大幅降低17％，并使大鼠中TNF-α水平降低42％。鞣花酸显著增加5-HT(39％)，多巴胺(DA，71％)和去甲肾上腺素(NE，77％)的脑内容物减少。鞣花酸(10 mg/kg，po，14天)导致大鼠中阿霉素诱导的组织病理学改变减少[2]。
细胞实验：通过MTT测定法测量ALCL细胞活力。简而言之，在加入鞣花酸之前12小时将0.1×10 5个细胞接种到96孔微量培养板上。在存在或不存在药物(鞣花酸)的情况下，在标准组织培养条件下，将细胞在200μL完全RPMI-1640培养基中生长48小时。然后将20μLMTT溶液(5mg/mL)加入细胞悬浮液中4小时。用150μLDMSO溶解细胞内甲crystals晶体，在分光光度计上在540nm处测量的光密度代表一式三份培养物的平均值(±SD)[1]。
动物实验：将50只雄性成年Sprague-Dawley大鼠随机分成如下五组：组(1)口服玉米油作为载体并用作正常对照。组(2)每周两次接受多柔比星(DOX)注射(5mg/kg，ip)，持续14天。组(3)每天两次接受鞣花酸(10mg/kg，po;每天)14天，并且每周两次接受DOX(5mg/kg，ip)持续14天。组(4)每天两次接受迷迭香酸(RA; 75mg/kg，po;每天)14天，并且每周两次接受DOX(5mg/kg，ip)持续14天。组(5)接受鞣花酸(10mg/kg，po;每天)，RA(75mg/kg，po;每天)14天，DOX注射(5mg/kg，ip)，每周两次，持续14天[ 2]。
激酶实验：CK2和CK1磷酸化测定在37℃下在增加量的每种抑制剂(鞣花酸)存在下进行，最终体积为25μL，含有50mM，Tris-HCl pH 7.5，100mM NaCl，12mM MgCl 2，除非另有说明，否则0.02mM [33P-ATP](500-1000cpm/pmol)。可磷酸化底物分别是CK2和CK1的合成肽底物RRRADDSDDDDD(100μM)和RRKHAAIGDDDDAYSITA(200μM)。加入激酶开始反应，10分钟后停止反应。在将等分试样点到磷酸纤维素滤膜上之前，加入5μL的0.5M正磷酸。在放射性标记的样品的SDS-PAGE后，在75mM磷酸底物中洗涤滤膜。 DYRK1A，肽RRRFRPASPLRGPPK测定，酪氨酸激酶活性测定[1]。
数据来源文献：[1]. Cozza G， et al. Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem. 2006 Apr 20;49(8):2363-6.
[2]. Rizk HA， et al. Prophylactic effects of ellagic acid and rosmarinic acid on doxorubicin-induced neurotoxicity in rats. J Biochem Mol Toxicol. 2017 Dec;31(12).
[3]. Ahire V， et al. Ellagic Acid Enhances Apoptotic Sensitivity of Breast Cancer Cells to γ-Radiation. Nutr Cancer. 2017 Aug-Sep;69(6):904-910.
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| 其它标识： |
EC：EINECS 207-508-3
MDL：MFCD00006914
SMILES：O=C1C2=CC(O)=C(O)C(O3)=C2C4=C(C3=O)C=C(O)C(O)=C4O1
InChIKey：AFSDNFLWKVMVRB-UHFFFAOYSA-N
InChI：InChI=1S/C14H6O8/c15-5-1-3-7-8-4(14(20)22-11(7)9(5)17)2-6(16)10(18)12(8)21-13(3)19/h1-2,15-18H
PubChem CID：5281855
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| 基本信息： |
CAS：476-66-4
中文名称：鞣花酸
英文名称：Ellagic acid
别名：Elagostasine;Gallogen
分子式：C14H6O8
分子量：302.19
规格：10mg ; 10mM*1mL in DMSO ; 50mg
溶解性：Soluble in DMSO ≥5mg/mL;Soluble in Ethanol <1mg/m
纯度：HPLC≥98%
外观(性状)：Yellow to brown Solid
储存条件：Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
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| 靶点： |
Casein Kinase（CK） |
产品详情
使用本产品应用案例:
In Vitro
Cell viability
Firstly, passages 3 chondrocytes were seeded into 96-well plates (5,000 cells/well) and incubated for 24 h. Then, the cells incubated with a concentration gradient (12.5, 25, 50 μM) of Ellagic acid (EA) for 24 h and 48 h when the cells reached a confluency of 90 %–95 %. Next, half the cells were incubated in IL-1β (10 ng/ml) for the next 24 h.Finally, 10 μl CCK-8 solution was added to each well for 2 h and the optical density was observed at 450 nm with a spectrophotometer . All experiments were repeated three times.
来源文献:Lin Z, Lin C, Fu C, Lu H, Jin H, Chen Q, Pan J. The protective effect of Ellagic acid (EA) in osteoarthritis: An in vitro and in vivo study. Biomed Pharmacother. 2020 May;125:109845. doi: 10.1016/j.biopha.2020.109845. Epub 2020 Feb 12. PMID: 32058211.
In Vivo
Mice
The mouse osteoarthritis model was established by surgical destabilization of the medial meniscus (DMM). In brief, mice were anesthetized with intraperitoneal injection of 2 % (w/v) pentobarbital (40 mg kg−1,) and then the joint capsule of right knee medial to the patellar tendon was excised. The medial meniscotibial ligaments were cut with microsurgical scissors. Surgery consisting of an arthrotomy was also performed on the left knee joint of mice and the joint was used as the sham group. Ultimately, all of the mice were separated into three groups randomly (n = 15 in each): a control group (sham-operated), OA group (OA) and OA treated with Ellagic acid (EA) group.
来源文献:Lin Z, Lin C, Fu C, Lu H, Jin H, Chen Q, Pan J. The protective effect of Ellagic acid (EA) in osteoarthritis: An in vitro and in vivo study. Biomed Pharmacother. 2020 May;125:109845. doi: 10.1016/j.biopha.2020.109845. Epub 2020 Feb 12. PMID: 32058211.
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