1. Metabolic Enzyme/Protease Autophagy Apoptosis NF-κB Immunology/Inflammation Cell Cycle/DNA Damage Epigenetics
  2. Drug Metabolite Autophagy Apoptosis Reactive Oxygen Species (ROS) Keap1-Nrf2 MMP Caspase PARP MDM-2/p53
  3. Homoeriodictyol

Homoeriodictyol  (Synonyms: 高圣草酚)

目录号: HY-N8210 纯度: 99.83%
COA 产品使用指南 技术支持

Homoeriodictyol 是一种具有口服活性,可以穿透血脑屏障的苦味掩盖黄烷酮。Homoeriodictyol 通过 NCOA4 介导的铁蛋白自噬 (autophagy) 增强突触相关蛋白表达。Homoeriodictyol 通过抑制 NLRP3 炎症小体改善小鼠的记忆障碍。Homoeriodictyol 通过激活 Nrf2 和抑制线粒体功能障碍保护人类内皮细胞免受氧化损伤。Homoeriodictyol 增强 ROS 活性诱导细胞凋亡 (apoptosis),表现出抗癌作用。Homoeriodictyol 在体外抑制雄激素耐药前列腺癌细胞的存活和迁移。Homoeriodictyol 在小鼠体内发挥抗伤害感受活性。

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Homoeriodictyol

Homoeriodictyol Chemical Structure

CAS No. : 446-71-9

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Other Forms of Homoeriodictyol:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo[1][2][3][4][5][6].

IC50 & Target[4]

Caspase 3

 

Caspase-9

 

体外研究
(In Vitro)

Homoeriodictyol (0.1-1 μM) 在 Corticosterone (HY-B1618) 诱导的 SH-SY5Y 细胞中,可提高细胞活力、PSD-95、SYN、P62 和 FTH 水平,并降低 LC3 和 NCOA4 水平[1]
Homoeriodictyol (10 μM/L,24 小时) 在 N9 小胶质细胞中可恢复细胞活力和迁移水平,并降低炎症因子水平[2]
Homoeriodictyol (0-20 μM,16 小时) 可上调 MDA-MB-231 细胞中 Nrf2 和 γGCS 的蛋白水平[3]
Homoeriodictyol (1-5 μM,12-24 小时) 在 H2O2 诱导的 EA.hy926 细胞中可预防线粒体功能障碍和细胞凋亡,降低 MMP、细胞色素 C、tAIF、裂解胱天蛋白酶-3、-9 和 PARP 的水平 [3]
Homoeriodictyol (0-5 μM,2-24 小时) 在 EA.hy926 细胞中通过在蛋白质水平诱导 Nrf2 并增强 Nrf2 的稳定性来激活 Nrf2 通路[3]
Homoeriodictyol (100-500 μg/mL,24 小时) 在 MCF-7、HeLa 和 HT-29 细胞中表现出细胞毒性和浓度依赖性溶酶体毒性,增强细胞内 ROS 生成,并诱导线粒体功能障碍[4]
Homoeriodictyol (500 μg/mL, 24 小时) 在 MCF-7、HeLa 和 HT-29 细胞中可增加 subG1 峰,并增加 p53、caspase 3、caspase 9、bax 和 SOD1 基因的表达[4]
Homoeriodictyol (0-250 μM, 24-72 小时) 可降低 PC3 细胞的细胞活力,IC50 为 118.15 μM,诱导细胞凋亡,抑制 PC3 细胞的细胞迁移[6]

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

ELISA Assay[2]

Cell Line: N9 microglial cells
Concentration: 10 μM/L
Incubation Time: 24 h
Result: Reduced levels of IL-1β and IL-18.

Cell Migration Assay [2]

Cell Line: N9 microglial cells
Concentration: 10 μM/L
Incubation Time: 24 h
Result: Restored migration levels.

Western Blot Analysis[3]

Cell Line: MDA-MB-231 cells
Concentration: 0, 2.5, 5 ,10, 20 μM
Incubation Time: 16 h
Result: Upregulated the protein levels of Nrf2 and γGCS.

Apoptosis Analysis[3]

Cell Line: H2O2-induced EA.hy926 cells
Concentration: 2, 5 μM
Incubation Time: 24 h
Result: Decreased apoptosis cells.

Immunofluorescence[3]

Cell Line: EA.hy926 cells
Concentration: 2, 5 μM
Incubation Time: 12 h
Result: Activated the nuclear translocation of Nrf2 protein.

Western Blot Analysis[3]

Cell Line: EA.hy926 cells
Concentration: 1, 2, 5 μM
Incubation Time: 2, 4, 6, 8, 12, 16 h
Result: Activated the nuclear translocation of Nrf2 protein.
Increased protein levels of Nrf2, NQO1, and γGCS, continued to increase Nrf2 protein levels over the 24 hours tested.

RT-PCR[3]

Cell Line: EA.hy926 cells
Concentration: 1, 2, 5 μM
Incubation Time: 24 h
Result: Did not affect mRNA level of Nrf2, but upregulated the levels of NQO1 and GCLM.

Immunofluorescence[3]

Cell Line: H2O2-induced EA.hy926 cells
Concentration: 2, 5 μM
Incubation Time: 12 h
Result: Reduce MMP levels.
Reduced cytochrome C protein levels in the cytoplasm and mitochondria.
Inhibited tAIF production and blocks AIF translocation from mitochondria to the nucleus.

Western Blot Analysis[3]

Cell Line: H2O2-induced EA.hy926 cells
Concentration: 1, 2, 5 μM
Incubation Time: 12 h
Result: Reduced cytochrome C protein levels in the cytoplasm and mitochondria.
Inhibited tAIF production and blocks AIF translocation from mitochondria to the nucleus.
Inhibited H2O2-induced activations of cleaved caspases -3, -9 and PARP.

Immunofluorescence[4]

Cell Line: MCF-7, HeLa, and HT-29 cells
Concentration: 500 μg/mL
Incubation Time: 24 h
Result: Increased the green fluorescence of DCF, increased the fluorescence of Rh123 fluorescence.

Cell Cycle Analysis[4]

Cell Line: MCF-7, HeLa, and HT-29 cells
Concentration: 500 μg/mL
Incubation Time: 24 h
Result: Increased the subG1 peaks.

RT-PCR[4]

Cell Line: MCF-7, HeLa, and HT-29 cells
Concentration: 100 μg/mL
Incubation Time: 24 h
Result: Increased the expressions of p53, caspase 3, caspase 9, bax, and SOD1 genes.

Apoptosis Analysis[6]

Cell Line: PC3 cells
Concentration: PC3 cells
Incubation Time: 72 h
Result: Induced apoptosis, reduced cell density and disrupted cell morphology, enhanced the efficacy of Docetaxel (HY-B0011) leading to higher apoptosis rates.
Increased the mRNA expression of BAX, CASP3, CASP8, and CYCS, upregulated TP53, along with enhanced expression of caspases in combination with Docetaxel.

Cell Migration Assay [6]

Cell Line: PC3 cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Reduced migration, reduced TWIST, SNAIL, and ZEB1 mRNA expression levels by 59%, 68%, and 42%, respectively, compared to untreated cells.
体内研究
(In Vivo)

Homoeriodictyol (10 mg/kg/d,口服,4 周) 通过抑制 NLRP3 炎症小体来减轻阿尔茨海默症昆明小鼠模型中的炎症,从而改善 Aβ25-35 诱导的记忆障碍[2]
Homoeriodictyol (50 μg/kg,腹腔注射,一次) 在瑞士白化小鼠模型中通过中枢和外周通路表现出抗伤害活性[5]

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

Animal Model: Aβ25-35-induced AD kunming mice (Male, 7 weeks old) model[1]
Dosage: 10 mg/kg/d
Administration: p.o., 4 weeks
Result: Improved memory impairment and cognitive dysfunction, alleviated hippocampal neuronal damage.
Decreased the levels of Aβ1-40, Aβ1-42, and p-Tau in the hippocampus.
Reduced oxidative stress in the brain, reduced the levels of ROS, apoptosis and MDA, increased the levels of GSH-Px and SOD.
Resulted in increased numbers of NK cells, Th cells, Tc cells, and DCs, and decreased numbers of MDSCs and Treg cells in peripheral blood and splenic tissues.
Had excellent anti-inflammatory effects, reduced the protein expression levels of NLRP3, Caspase-1, and ASC, and the inflammatory factors IL-18 and IL-1β in brain tissue.
Animal Model: Swiss albino mice (adult male, 24-28 g) model[5]
Dosage: 50, 100, 150, and 200 μg/kg
Administration: i.p., once
Result: Lowered the writhing responses to acetic acid, showed a dose-responsive relation analgesic effect.
Increased the time respond to thermal pain on a hot plate.
Decreased the licking times in both the early and late phases after formalin injection, alleviated pain in the formalin test.
Lessened licking time after Capsaicin (HY-10448) injection, indicating a dose-responsive effect.
Reduced paw licking times, mitigated glutamate-induced pain responses.
Clinical Trial
分子量

302.28

Formula

C16H14O6

CAS 号
性状

固体

颜色

White to off-white

中文名称

高圣草酚

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (165.41 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3082 mL 16.5410 mL 33.0819 mL
5 mM 0.6616 mL 3.3082 mL 6.6164 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (4.14 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (4.14 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

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, 6 months; -20°C, 1 month (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3082 mL 16.5410 mL 33.0819 mL 82.7048 mL
5 mM 0.6616 mL 3.3082 mL 6.6164 mL 16.5410 mL
10 mM 0.3308 mL 1.6541 mL 3.3082 mL 8.2705 mL
15 mM 0.2205 mL 1.1027 mL 2.2055 mL 5.5137 mL
20 mM 0.1654 mL 0.8270 mL 1.6541 mL 4.1352 mL
25 mM 0.1323 mL 0.6616 mL 1.3233 mL 3.3082 mL
30 mM 0.1103 mL 0.5514 mL 1.1027 mL 2.7568 mL
40 mM 0.0827 mL 0.4135 mL 0.8270 mL 2.0676 mL
50 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6541 mL
60 mM 0.0551 mL 0.2757 mL 0.5514 mL 1.3784 mL
80 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0338 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8270 mL
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