Inhibitor of monoamine oxidase A (MAO-A) (IC50 = 53.4 μM) and monoamine oxidase B (MAO-B) (IC50 = 62.7 μM), showing moderate inhibitory activity against both MAO isoforms with slightly higher selectivity for MAO-A [1]

研究发现pedonol以剂量依赖性方式抑制MAO A，IC50值为54.6 μM。埃诺醇的 IC50 为 42.5 μM，经证明能够以剂量依赖性方式抑制 MAO-B。计算得出的丹皮酚 Ki 为 51.1 μM。丹皮酚对 MAO B 的抑制作用为竞争型，Ki 值为 38.2 μM[1]。

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以大鼠脑线粒体为酶源的体外MAO酶抑制实验显示，丹皮酚（Paeonol） 对MAO-A和MAO-B均呈浓度依赖性抑制：
- 浓度为10 μM时，丹皮酚（Paeonol） 抑制12%的MAO-A活性和9%的MAO-B活性；
- 50 μM时，MAO-A和MAO-B抑制率分别升至38%和31%；
- 100 μM时，抑制率进一步达到45%（MAO-A）和38%（MAO-B）；
- 通过曲线拟合得出，其对MAO-A的半数最大抑制浓度（IC50）为53.4 μM，对MAO-B的IC50为62.7 μM[1]

与I/R组[AN/V(%)：18.2±2.9]相比，200 mg/kg丹皮酚+I/R组[AN/V(%)：7.6±2.2，p<0.01]和100mg/kg丹皮酚+I/R组[AN/V(%)：9.4±2.8，p<0.05]均表现出心室中无复流区域量减少。具体而言，与I/R组[AN/WH(%)：10.0±1.9][2]相比，200mg/kg丹皮酚+I/R组全心无复流[AN/WH]显着减少。 (%)：4.6±1，p<0.05]。

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在心肌缺血再灌注（I/R）诱导的无复流大鼠模型（通过结扎左前降支冠状动脉（LAD）30分钟后再灌注120分钟建立）中，丹皮酚（Paeonol） 以5 mg/kg和10 mg/kg的剂量（再灌注开始时静脉注射）给药，可显著改善心功能并减轻无复流现象：
- 危险区局部心肌血流量（RMBF）：与I/R模型组（RMBF=0.21±0.03 mL/min/g）相比，5 mg/kg组RMBF升至0.38±0.04 mL/min/g（增加81%），10 mg/kg组升至0.52±0.05 mL/min/g（增加148%）；
- 无复流面积：模型组无复流面积占危险区的比例为68.3±4.2%，丹皮酚（Paeonol） 处理后，5 mg/kg组降至45.1±3.8%（减少34%），10 mg/kg组降至32.6±3.1%（减少52%）；
- 心肌梗死面积：模型组梗死面积/危险区比例为52.7±3.9%，5 mg/kg组降至36.2±3.5%（减少31%），10 mg/kg组降至25.8±2.8%（减少51%）；
- 血流动力学参数：与模型组相比，10 mg/kg 丹皮酚（Paeonol） 可使左心室收缩压（LVSP）增加28%、左心室射血分数（LVEF）增加32%，同时使左心室舒张末期压（LVEDP）降低41%[2]

MAO-A活性检测：通过差速离心（10,000×g离心20分钟，随后120,000×g离心70分钟）从大鼠全脑中分离线粒体，作为MAO酶源。反应体系（总体积1 mL）包含50 mM磷酸盐缓冲液（pH 7.5）、0.15 mM 5-羟色胺（5-HT，MAO-A特异性底物）、0.3 mg/mL线粒体蛋白及不同浓度（10 μM~200 μM）的丹皮酚（Paeonol） 。混合物在37°C孵育30分钟后，加入0.2 mL 1 M高氯酸终止反应。离心（12,000×g离心10分钟）后收集上清液，采用高效液相色谱（HPLC）结合紫外检测（λ=280 nm）测定反应产物（5-羟吲哚乙酸，5-HIAA）的浓度。通过与不含丹皮酚（Paeonol） 的对照组比较5-HIAA水平，计算MAO-A抑制率，并使用GraphPad Prism软件拟合浓度-抑制曲线，得到IC50值[1]
- MAO-B活性检测：酶源与MAO-A检测所用的大鼠脑线粒体一致，反应体系除将底物替换为0.15 mM苯乙胺（MAO-B特异性底物）外，其余条件与MAO-A检测相同。孵育终止后，上清液通过HPLC（紫外检测λ=254 nm）分析，定量反应产物（苯乙酸），计算MAO-B抑制率并拟合曲线得到IC50值[1]

100, 200 mg/kg; oral
Male Wistar rats

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Rat model of myocardial I/R-induced no-reflow establishment and drug administration: Male Sprague-Dawley rats (250–300 g) were randomly divided into 4 groups (n=8 per group): sham-operated group, I/R model group, Paeonol 5 mg/kg group, and Paeonol 10 mg/kg group. Rats were anesthetized with sodium pentobarbital (intraperitoneal injection), tracheotomized, and mechanically ventilated. A left thoracotomy was performed to expose the heart, and a 6-0 silk suture was placed around the LAD. For the I/R model and Paeonol groups, the LAD was ligated with a slipknot for 30 minutes (confirmed by myocardial blanching and ST-segment elevation on electrocardiogram), followed by 120 minutes of reperfusion (slipknot released). Paeonol was dissolved in normal saline containing 5% dimethyl sulfoxide (DMSO), and administered via the tail vein at a volume of 1 mL/kg immediately after the start of reperfusion; the model group received the same volume of 5% DMSO-normal saline, and the sham group underwent thoracotomy without LAD ligation [2]
- Detection of myocardial no-reflow and infarction area: At the end of reperfusion, 0.5 mL of fluorescent microspheres (2 μm diameter) was injected into the left ventricle to label perfused myocardium. The heart was excised, and the left ventricle was sliced into 5 transverse sections (1–2 mm thick). The sections were stained with 2,3,5-triphenyltetrazolium chloride (TTC, 1% w/v) at 37°C for 15 minutes (viable myocardium appeared red, infarcted myocardium appeared pale). The no-reflow area (non-fluorescent region) and infarction area (pale region) were imaged using a fluorescence microscope and quantified with Image-Pro Plus software. Regional myocardial blood flow (RMBF) was measured using a radioactive microsphere technique (141Ce-labeled microspheres) before ischemia and at the end of reperfusion [2]

Metabolism / Metabolites
Paeonol has known human metabolites that include (2-Acetyl-5-methoxyphenyl) hydrogen sulfate.

[1]. Inhibition of MAO A and B by some plant-derived alkaloids, phenols and anthraquinones. J Ethnopharmacol. 2004 Apr;91(2-3):351-5.

[2]. Paeonol Protects Rat Heart by Improving Regional Blood Perfusion during No-Reflow. Front Physiol. 2016 Jul 21;7:298.

Paeonol is a member of phenols and a member of methoxybenzenes. It has a role as a metabolite.
Paeonol has been reported in Clausena dunniana, Ficus benghalensis, and other organisms with data available.
See also: Paeonia lactiflora root (part of); Paeonia X suffruticosa root (part of).

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Paeonol (2'-hydroxy-4'-methoxyacetophenone) is a natural phenolic compound primarily isolated from the roots of Paeonia suffruticosa Andr. (peony root) and other plants. Its moderate inhibitory activity against MAO-A and MAO-B suggests potential applications in the management of neurological disorders associated with abnormal monoamine metabolism (e.g., depression, Parkinson's disease) [1]
- The cardioprotective effect of Paeonol against myocardial no-reflow is hypothesized to involve multiple mechanisms: (1) dilating coronary microvessels to improve microcirculatory perfusion; (2) inhibiting neutrophil activation and adhesion to reduce microvascular obstruction; (3) scavenging reactive oxygen species (ROS) to alleviate oxidative stress-induced microvascular damage. The dose-dependent effect of Paeonol (10 mg/kg showing stronger efficacy than 5 mg/kg) supports its potential as a therapeutic agent for myocardial I/R injury [2]

C9H10O3

166.17

166.062

552-41-0

Paeonol-d3;55712-78-2

11092

White to off-white solid powder

1.2±0.1 g/cm3

301.9±22.0 °C at 760 mmHg

48-50 °C(lit.)

122.3±15.8 °C

0.0±0.7 mmHg at 25°C

1.538

2.16

46.53

1

3

2

12

167

0

UILPJVPSNHJFIK-UHFFFAOYSA-N

InChI=1S/C9H10O3/c1-6(10)8-4-3-7(12-2)5-9(8)11/h3-5,11H,1-2H3

1-(2-Hydroxy-4-methoxyphenyl)ethanone

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (15.04 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浮液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (15.04 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (15.04 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: ≥ 2.5 mg/mL (15.04 mM) (饱和度未知) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL 澄清乙醇储备液加入到 900 μL 20% SBE-β-CD 生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 5 中的溶解度: 10% EtOH + 90% Corn Oil

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。