2. Anti-infection Immunology/Inflammation MAPK/ERK Pathway Stem Cell/Wnt JAK/STAT Signaling Apoptosis Metabolic Enzyme/Protease NF-κB PI3K/Akt/mTOR
  3. Beta-lactamase COX Interleukin Related Bacterial JNK ERK p38 MAPK STAT Apoptosis NO Synthase Nuclear Factor of activated T Cells (NFAT) Lactate Dehydrogenase Reactive Oxygen Species (ROS) SOD Akt Caspase Bcl-2 Family
  4. 3′,4′,7-Trihydroxyflavone

3′,4′,7-Trihydroxyflavone 

目录号: HY-N2736 纯度: ≥98.0%
COA 产品使用指南 技术支持

3′,4′,7-Trihydroxyflavone 是一种具有口服活性的 OXA-48 (IC50 = 1.89 μM)/COX-1 (IC50 = 36.37 μM) 抑制剂。3′,4′,7-Trihydroxyflavone 有抗氧化和抗炎作用，抑制炎症因子 (如 IL-6, IL-8, 和 TNF-α 的释放)。3′,4′,7-Trihydroxyflavone 抑制 H2O2 诱导的神经元细胞凋亡 (apoptosis) 和 ROS 积累，并通过抑制 JNK-STAT1 通路发挥抗神经炎症作用。3′,4′,7-Trihydroxyflavone 对耐多药革兰氏阴性肠道细菌 (bacteria) 具有抗菌和抗生素修饰活性。3′,4′,7-Trihydroxyflavone 通过 NFATc1 抑制 RANKL 诱导的破骨细胞形成。 3′,4′,7-Trihydroxyflavone 激活 CREB-BDNF 轴，恢复 Scopolamine (HY-N0296) 诱导的小鼠记忆缺陷。

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3′,4′,7-Trihydroxyflavone

3′,4′,7-Trihydroxyflavone Chemical Structure

CAS No. : 2150-11-0

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3′,4′,7-Trihydroxyflavone 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

3′,4′,7-Trihydroxyflavone is an orally active inhibitor of OXA-48 (IC50 = 1.89 μM) and COX-1 (IC50 = 36.37 μM). 3′,4′,7-Trihydroxyflavone exhibits antioxidant and anti-inflammatory properties, inhibiting the release of inflammatory cytokines such as IL-6, IL-8, and TNF-α. 3′,4′,7-Trihydroxyflavone inhibits H2O2-induced neuronal apoptosis and ROS accumulation, and exerts anti-neuroinflammatory effects by suppressing the JNK-STAT1 pathway. 3′,4′,7-Trihydroxyflavone exhibits antimicrobial and antibiotic-modifying activities against multidrug-resistant Gram-negative enteric bacteria. 3′,4′,7-Trihydroxyflavone inhibits RANKL-induced osteoclast formation via NFATc1. 3′,4′,7-Trihydroxyflavone activates the CREB-BDNF axis and restores scopolamine (HY-N0296)-induced memory deficits in mice[1][2][3][4][5][6][7][8][9].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
49.3 μM
Compound: 12
Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
[PMID: 19572738]
HEK293 IC50
> 40 μM
Compound: Fig 20, R2C1
Inhibition of telomerase extracted from HEK293 cells using 5'-bAATCCGTCGAGCAGAGTT as primer assessed as polymerization of telomeric repeats to the end of the primers after 2 hrs by Flash-Plate assay
Inhibition of telomerase extracted from HEK293 cells using 5'-bAATCCGTCGAGCAGAGTT as primer assessed as polymerization of telomeric repeats to the end of the primers after 2 hrs by Flash-Plate assay
10.1039/C0MD00241K
HEK293 IC50
> 40 μM
Compound: 1d
Inhibition of human telomerase from HEK293 cell extracts by Flash-Plate assay
Inhibition of human telomerase from HEK293 cell extracts by Flash-Plate assay
[PMID: 15588081]
Neutrophil IC50
13.5 μM
Compound: 3d
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
[PMID: 23871908]
Neutrophil IC50
14.7 μM
Compound: 3d
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
[PMID: 23871908]
Neutrophil IC50
3.7 μM
Compound: 3d
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay
[PMID: 23871908]
Neutrophil IC50
5.2 μM
Compound: 3d
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay
[PMID: 23871908]
Peritoneal macrophage IC50
26 μM
Compound: kp15
Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
[PMID: 27955927]
体外研究
(In Vitro)

3′,4′,7-Trihydroxyflavone (0.1-20 μM, 24 小时) 可增强 SH-SY5Y 细胞的活力，并使其在 Scopolamine (HY-N0296) 诱导的损伤中存活[1]。
3′,4′,7-Trihydroxyflavone (0.1-100 µM) 可降低 TNFα 刺激的 HaCaT 细胞中 IL-6 和 IL-8 的分泌，IC50 分别为 17.8、126.2 µg/mL，最大抑制率分别为 74.4、40.2 %，使 HaCaT 细胞活力降低至 74%[2]。
3′,4′,7-Trihydroxyflavone (50 µM，64 μg/mL) 可抑制 OXA-48 活性，抑制率为 80%，与 β-内酰胺类抗生素结合使用对 BW25113 ∆acrA∆bamB (OXA-48) 表现出抗菌活性[3]。
3′,4′,7-Trihydroxyflavone (1-20 μM，30 分钟) 可防止 H2O2 诱导的 SH-SY5Y 和海马神经元细胞的细胞死亡以及乳酸脱氢酶 (LDH) 释放[4]。
3′,4′,7-Trihydroxyflavone (1-20 μM，30 分钟) 可抑制 H2O2 诱导的 SH-SY5Y 细胞的细胞凋亡特征，逆转诱导的细胞核坏死，并凝结细胞收缩[4]。
3′,4′,7-Trihydroxyflavone (0.5-20 μM，30 分钟) 可抑制 H2O2 诱导的 SH-SY5Y 细胞中 ROS 积累、SOD、CAT 和 GSH 还原，F-κB p65 从胞质溶胶向细胞核易位的激活[4]。
3′,4′,7-Trihydroxyflavone (1-20 μM，30 分钟) 可抑制 H2O2 诱导的 SH-SY5Y 细胞中 JNK、p38、ERK 1/2 MAPKs 和 PI3K/Akt 水平的磷酸化，Bax，caspase-3，caspase-9 和 PARP 水平的上调，Bcl-2 和 Bcl-xL 水平下调，细胞色素 c 的释放以及 MMP 的丢失[4]。
3′,4′,7-Trihydroxyflavone 显示对 12 种革兰氏阴性菌大肠杆菌、产气肠杆菌和肺炎克雷伯菌具有抗菌活性，MIC 值范围为 4 至 256 μg/mL[5]。
3′,4′,7-Trihydroxyflavone 可提高 Tetracycline (HY-A0107) 和 Erythromycin (HY-B0220) 对 80% 测试细菌的活性，FIC 值范围为 0.5 至 < 0.062[5]。
3′,4′,7-Trihydroxyflavone (0.1-100 μM) 在 0.1-30 µM 时没有影响，但在 100 µM 时会降低 MG6 细胞的细胞活力[6]。
3′,4′,7-Trihydroxyflavone (0.1-10 μM，6-48 小时) 在 LPS (HY-D1056) 诱导的 MG6 细胞中可降低 NO、TNF-α 和 iNOS 水平，抑制 STAT1 磷酸化和总 STAT1 表达[6]。
3′,4′,7-Trihydroxyflavone (0.1-10 μM，0.5 小时) 可抑制 LPS 诱导的 MG6 细胞中的 JNK 磷酸化，但不抑制 p38 或 ERK 磷酸化[6]。
3′,4′,7-Trihydroxyflavone (0.1-10 μM，24-48 小时) 可抑制 IFN-γ 诱导的 MG6 细胞中的 NO 释放、iNOS 表达和 STAT1 磷酸化[6]。
3′,4′,7-Trihydroxyflavone (0-5 μg/mL，1-7 天) 可抑制 RANKL 诱导的 BMMs 形成和骨吸收[7]。
3′,4′,7-Trihydroxyflavone (5 μg/mL，7 天) 可通过 Blimp-1 和 p38 MAPK 通路抑制 RANKL 诱导的 BMMs NFATc1 表达[7]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

3′,4′,7-Trihydroxyflavone 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1, 5, 10, and 20 μM
Incubation Time: 24 h
Result: Enhanced the cell viability and survival against Scopolamine (HY-N0296)-induced damage.

Apoptosis Analysis[4]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1, 5, 10, and 20 μM
Incubation Time: 30 min
Result: Inhibited apoptosis, reversed H2O2-induced nuclear necrosis and condensation, and cell shrinkage.

Immunofluorescence[4]

Cell Line: SH-SY5Y cells
Concentration: 0.5, 1, 5, 10, and 20 μM
Incubation Time: 30 min
Result: Reduced ROS, SOD, CAT and GSH fluorescence intensity.
Increased the fluorescence intensity of MMP and rhodamine 123, eliminated cytochrome c diffusion caused by H2O2.

Western Blot Analysis[4]

Cell Line: SH-SY5Y cells
Concentration: 1, 5, 10, and 20 μM
Incubation Time: 30 min
Result: Reduced the phosphorylation of Akt, JNK, p38 MAPK, and Akt to 40.64%, 111%, 105%, and 95% of the control value, respectively.
Inhibited the upregulation or downregulation of Bax and Bcl-xL to 118% and 62% of control values, respectively at 1 µM, inhibited the upregulation or downregulation of Bax, Bcl-2, and Bcl-xL to 111%, 87%, and 82% of control values, respectively, at 5 µM, inhibited the upregulation or downregulation of Bax, Bcl-2, and Bcl-xL to 102%, 98%, and 93% of control values, respectively at 20 µM.
Reduced the release of cytochrome c from mitochondria to the cytosol.
Significantly inhibited the increase in cleaved PARP, cleaved caspase-3 and cleaved caspase-9.

Western Blot Analysis[6]

Cell Line: LPS-induced MG6 cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 0.5, 6, 24 h
Result: Reduced iNOS levels.
Inhibited STAT1 phosphorylation and total STAT1 expression.
Inhibited JNK phosphorylation but not p38 or ERK phosphorylation.

Western Blot Analysis[6]

Cell Line: IFN-γ-induced MG6 cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 24 h
Result: Inhibited NO release and increased iNOS expression.
Inhibited STAT1 phosphorylation but did not inhibit the increase in total STAT1 levels.

RT-PCR[7]

Cell Line: BMMs
Concentration: 5 μg/mL with RANKL (100 ng/mL) and M-CSF (30 ng/mL)
Incubation Time: 7 days
Result: Suppressed the mRNA expression levels of CTR and cathepsin K.
Suppressed the expression of DC-STAMP and ATP6v0d2 induced by RANKL. Decreased the mRNA level of Blimp1.

Western Blot Analysis[7]

Cell Line: BMMs
Concentration: 5 μg/mL with RANKL (200 ng/mL)
Incubation Time: 30 min
Result: Abolished RANKL-induced NFATc1 expression, but not c-Fos protein expression.
Suppressed phosphorylation of p38.
体内研究
(In Vivo)

3′,4′,7-Trihydroxyflavone (10/50 mg/kg，口服，每日一次，3 天/每周三次，共 28 天；10 ng，ICV，每周两次，共 28 天) 通过诱导 CREB-BDNF 激活，改善 Scopolamine 诱发的认知缺陷小鼠模型中的长期增强 (LTP)，发挥神经保护作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Scopolamine-induced cognitive deficits mice (male C57BL/6J, 8 weeks old) model[1]
Dosage: 10/50 mg/kg
Administration: p.o., once a day, 3 days/three times per week, 28 days
Result: Improved cognitive abilities at 50 mg/kg.
Had no acute cognitive improvement after three days.
Restored ACh and ChAT levels and reduced AChE activity, increased BDNF mRNA and protein levels, and restored pCREB levels at 50 mg/kg.
Increased the number of neurons and restored astrocyte levels (GFAP marker).
Animal Model: Scopolamine-induced cognitive deficits mice (male C57BL/6J, 8 weeks old) model[1]
Dosage: 10 ng
Administration: ICV, twice a week, 28 days
Result: Improved spontaneous change, novel object recognition index and passive avoidance, acetylcholine activity, and restored acetylcholinesterase and choline acetyltransferase activities.
Induced the enhancement of the CREB-BDNF signaling pathway and increased LTP.
分子量

270.24

Formula

C15H10O5
CAS 号
性状

固体

颜色

Off-white to light yellow

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

RT, protect from light

In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

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1 mM 3.7004 mL 18.5021 mL 37.0041 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL
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储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用，-20°C储存时，请在1年内使用。

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参考文献

3′,4′,7-Trihydroxyflavone 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用，-20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7004 mL 18.5021 mL 37.0041 mL 92.5104 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL 18.5021 mL
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Keywords:

3′,4′,7-Trihydroxyflavone2150-11-0Beta-lactamaseCOXInterleukin RelatedBacterialJNKERKp38 MAPKSTATApoptosisNO SynthaseNuclear Factor of activated T Cells (NFAT)Lactate DehydrogenaseReactive Oxygen Species (ROS)SODAktCaspaseBcl-2 Familyβ-lactamaseCyclooxygenaseILc-Jun N-terminal kinaseExtracellular signal regulated kinasesNitric oxide synthasesNOSLDHSuperoxide DismutasePKBProtein kinase Bflavonoid aglyconecognitive deficits mice modelSH-SY5Y cellsHaCaT cellMG6 cellsBMMsInhibitorinhibitorinhibit

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