2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. Phosphodiesterase (PDE) NF-κB Keap1-Nrf2 Reactive Oxygen Species (ROS) TNF Receptor Nuclear Factor of activated T Cells (NFAT) Akt ERK p38 MAPK NO Synthase Interleukin Related COX JNK
  4. Sappanone A

Sappanone A 是一种从 sappan L 中发现的具有口服活性的同型异黄烷酮。Sappanone A 是一种 PDE4 和 NF-κB 抑制剂，具有抗炎和抗氧化作用。Sappanone A 通过激活 Nrf2 通路诱导 HO-1 表达。Sappanone A 还能抑制 RANKL 诱导的破骨细胞生成。Sappanone A 在炎症相关和心血管疾病的研究中具有很大的潜力。

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Sappanone A Chemical Structure

Sappanone A Chemical Structure

CAS No. : 102067-84-5

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10 mM * 1 mL in DMSO ￥770
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5 mg ￥700
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10 mg ￥1100
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25 mg ￥2400
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Sappanone A 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

Sappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular [1][2][3][4][5].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
RAW264.7 IC50
5.7 μM
Compound: 7
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs
[PMID: 23234407]
RAW264.7 IC50
8.3 μM
Compound: 7
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA
[PMID: 23234407]
RAW264.7 IC50
9.3 μM
Compound: Sappanone A
Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation for 24 hrs by Griess assay
Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation for 24 hrs by Griess assay
[PMID: 28038832]
体外研究
(In Vitro)

Sappanone A (5-30 μM，预处理 1 h，再处理 24 h) 在 RAW264.7 细胞中以浓度依赖性方式抑制 LPS 诱导的 NO、IL-6 和 PGE 2产生 (IC50 分别为 6.8、11.2 和 12.6 μM)，且无细胞毒性[1]。
Sappanone A (5-30 μM，24 h) 在 RAW264.7 细胞中通过激活 Nrf2 诱导 HO-1 表达和抑制 LPS 诱导的 NF-κB 的活化，发挥抗炎作用[1]。
Sappanone A (0-50 μM) 显著抑制 PDE4 酶活性，降低 RAW264.7 巨噬细胞中 LPS 诱导的 TNF-α 产生[2]。
Sappanone A (0.007-1.0 mM，40 min) 具有优异的还原 Fe3+ 和络合 Fe2+ 能力，显示出优异的抗氧化活性[2]。
Sappanone A (3-30 μM，7 days) 抑制 RANKL 诱导的小鼠 bone marrow-derived macrophage (BMM) 破骨细胞生成[3]。
Sappanone A (0-30 μM，7 days) 抑制 BMM 中 RANKL 诱导的 NFATc1 激活和 AKT 磷酸化[3]。
Sappanone A (10-30 μM，预处理 1 小时，再处理 24 小时) 在 HG 诱导的肾小球系膜细胞模型中，阻断 NF-κB 通路抑制炎症反应[5]。

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

Sappanone A 相关抗体:

RT-PCR[1]

Cell Line: RAW264.7cells
Concentration: 5, 15, 30 μM
Incubation Time: 24 h
Result: Reduced the mRNA levels of iNOS, COX-2, and IL-6 in a concentration-dependent manner.
Increased HO-1 mRNA expression level in a concentration-dependent manner, and HO-1 mRNA increased 3 hours after treatment, peaked at 6 hours, and returned to basal levels at 24 hours.
Induced HO-1 expression by activating Nrf2, resulting in a concentration-dependent increase in the mRNA levels of NQO1 and GCLC.

Western Blot Analysis[3]

Cell Line: BMM cells
Concentration: 0, 3, 10, 30 μM
Incubation Time: 7 days
Result: Increased the phosphorylation levels of ERK, p38 and JNK mitogen-activated protein kinases (MAPKs) in a time-dependent manner and pretreatment.
Inhibited RANKL-induced NFATc1 expression.
体内研究
(In Vivo)

Sappanone A (20, 50 mg/kg，i.p.，单次给药) 在 LPS 诱导的 C57BL/6 小鼠模型中保护小鼠免于死亡[1]。
Sappanone A (50, 100 mg/kg，i.p.，每天两次，连续七天) 显著减轻 LPS 诱发的小鼠急性肺损伤 (ALI)，且无明显毒副作用[2]。
Sappanone A (50 mg/kg，i.p.，一天隔一天注射，共注射八天) 在 LPS 诱导的小鼠骨质流失模型中，对体内破骨细胞形成有抑制作用[3]。
Sappanone A (20 mg/kg，i.p.，单次给药) 在心肌缺血再灌注损伤 (MIRI) 大鼠模型中，可减少心肌坏死和细胞凋亡，促进心脏功能的恢复[4]。
Sappanone A (10-30 mg/kg，i.g.，一天一次，连续十二周) 在 Streptozotocin (HY-13753) 诱发的糖尿病小鼠模型中，剂量依赖性的方式减轻高血糖期间的肾脏损伤[5]。

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

Animal Model: ALI in Institute of Cancer Research mice (male 20-25 g) was established by intratracheal instillation of 0.5 mg/kg LPS in 100 μl saline solution.[2]
Dosage: 50,100 mg/kg
Administration: i.p., twice a day for seven consecutive days, 1 h prior to LPS injection
Result: Significantly reduced the production of TNF-α in lung tissue, protein content in BALF, and MPO activity.
Had a good effect on the growth, development and behavior of mice, and no death or obvious toxic side were observed.
Animal Model: Institute of Cancer Research mice (male 6 weeks) injected with LPS (5 mg/kg)[3]
Dosage: 50 mg/kg
Administration: i.p., injected every other day for a total of eight days
Result: LPS-induced significant decreased in the number of TRAP-positive osteoclasts.
Had a good effect on the growth, development and behavior of mice, and no death or obvious toxic side were observed.
Animal Model: Wistar rats (male 250 g) MIRI model (hearts were isolated and underwent 30-min ischemia, followed by 120-min reperfusion)[4]
Dosage: 20 mg/kg
Administration: i.p., one dose, 1 h prior to heart isolation
Result: Reduce myocardial ischemia-reperfusion injury and myocardial infarction area.
Significantly improved LVDP and ±dp/dt values at 30, 60, and 120 min of reperfusion, indicating that it promoted the recovery of cardiac function after ischemia-reperfusion.
Inhibited ischemia-reperfusion-induced cardiomyocyte apoptosis by reducing cell apoptosis and inhibited the expression of cleaved caspase-3.
Significantly reduced the content of ROS and MDA in ischemic myocardium, and increased the activity of SOD and GSH-Px in ischemic myocardium.
Downregulated the expression of Keap1, decreased the level of Nrf2 in the cytoplasm, and increased the level of Nrf2 in the nucleus, and also activated the transcriptional activity to upregulate the expression of Nrf2 target genes (HO-1 and NQO1).
Enhanced the phosphorylation of Nfr2 through the PKC or PI3K pathway.
Animal Model: Streptozotocin (50 mg/kg, i.p., 5 consecutive days) induced diabetic C57BL/6J mice (20-23 g, 6-8 weeks)[5]
Dosage: 10, 20, 30 mg/kg
Administration: i.g., once a day for twelve consecutive weeks
Result: Showed that the increase of serum creatinine and BUN was significantly attenuated, and the 24-hour urine protein of mice was significantly reduced.
Alleviated the pathological changes in Streptozotocin-treated mice, reduced the production of fibrotic molecules transforming growth factor β1 (TGF-β1) and collagen IV (Col-IV), and decreased the expression of inflammatory cytokines interleukin 1β (IL-1β) and tumor necrosis factor α (TNF-α).
分子量

284.26

Formula

C16H12O5
CAS 号
性状

固体

颜色

Light yellow to 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

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 : 100 mg/mL (351.79 mM; 超声助溶 (<60°C); 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 3.5179 mL 17.5895 mL 35.1791 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 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: ≥ 2.08 mg/mL (7.32 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (7.32 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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

只
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

纯度: 99.87%

COA (284 KB) HNMR (294 KB) LCMS (96 KB)

产品使用指南 (1538 KB)
参考文献

Sappanone A 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, 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 3.5179 mL 17.5895 mL 35.1791 mL 87.9477 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL 17.5895 mL
10 mM 0.3518 mL 1.7590 mL 3.5179 mL 8.7948 mL
15 mM 0.2345 mL 1.1726 mL 2.3453 mL 5.8632 mL
20 mM 0.1759 mL 0.8795 mL 1.7590 mL 4.3974 mL
25 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5179 mL
30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9316 mL
40 mM 0.0879 mL 0.4397 mL 0.8795 mL 2.1987 mL
50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7590 mL
60 mM 0.0586 mL 0.2932 mL 0.5863 mL 1.4658 mL
80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sappanone A102067-84-5Phosphodiesterase (PDE)NF-κBKeap1-Nrf2Reactive Oxygen Species (ROS)TNF ReceptorNuclear Factor of activated T Cells (NFAT)AktERKp38 MAPKNO SynthaseInterleukin RelatedCOXJNKNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRPKBProtein kinase BExtracellular signal regulated kinasesNitric oxide synthasesNOSILCyclooxygenasec-Jun N-terminal kinaseInflammationRAW264.7 cellsoxidative stressC57BL/6 miceICR miceInhibitorinhibitorinhibit

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