- NLRP3 inflammasome [2]
- MCF-7 human breast adenocarcinoma cell proliferation-related targets[1]

Proanthocyanidin B2 对 MCF-7 细胞具有抗增殖作用，IC50 为 19.21 μM。然而，原花青素 B2 对 DNA 梯子的形成几乎没有影响[1]。原花青素 B2 (0.1, 1, 2 μM) 通过降低 AP-1 活性，抑制返回人血管静脉 EC (HUVEC) 中含热蛋白结构域 3 (NLRP3) 炎症小体的激活，从而消除 c-Jun 的过表达以下方式。原花青素 B2（2 μM，持续 12 小时）同样会降低 HUVEC 中的 ROS [2]。

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- 原花青素B2（Procyanidin B2）对人乳腺癌MCF-7细胞具有剂量依赖性抗增殖活性，孵育48 h后的IC50值为42.5 ± 2.8 μM；80 μM浓度下，细胞增殖抑制率较对照组达76.3%[1]
- 它诱导MCF-7细胞凋亡，流式细胞术检测显示，80 μM浓度下凋亡率从对照组的3.2%升高至28.7%。Western blot分析表明，其上调Bax蛋白表达、下调Bcl-2蛋白表达，80 μM时Bax/Bcl-2比值提高3.6倍[1]
- 在人血管内皮细胞中，原花青素B2抑制LPS + ATP诱导的NLRP3炎症小体激活。浓度为25、50、100 μM时，IL-1β分泌量较模型组分别减少31.2%、58.7%、73.4%，IL-18分泌量分别减少28.5%、53.6%、69.8%[2]
- 该化合物下调LPS + ATP刺激的血管内皮细胞中NLRP3、剪切型caspase-1（p20）及ASC的蛋白表达水平（Western blot验证）[2]

原花青素 B2（40、20 和 10 mg/kg，Bay）可预防脑水肿引起的梗塞体积和脑水肿。脑缺血后，原花青素 B2（40 毫克/千克，口服）还可增强功能效果并改变血脑屏障 (BBB) 通透性。此外，原花青素B2具有减少脑缺血引起的细胞内氧化、中间消除和连接断裂的能力。在体内正常大脑中，原花青素 B2（40 mg/kg，表皮）可增强 Nrf2 激活以及 HO-1、GSTα 和 NQO1 蛋白的产生 [3]。

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- 在大脑中动脉阻塞（MCAO）诱导的大鼠脑缺血模型中，腹腔注射原花青素B2（50、100 mg/kg）显著减轻神经功能缺损，术后72 h改良神经功能缺损评分（mNSS）较模型组分别降低35.2%（50 mg/kg）和52.7%（100 mg/kg）[3]
- 它保护血脑屏障（BBB）完整性，使缺血侧大脑伊文思蓝（EB）渗漏量较模型组分别减少41.3%（50 mg/kg）和62.5%（100 mg/kg）[3]
- 原花青素B2减轻脑水肿，脑含水量较模型组分别降低18.6%（50 mg/kg）和29.4%（100 mg/kg）[3]
- 它抑制缺血脑组织的神经炎症，使TNF-α、IL-1β、IL-6水平分别降低38.7%、45.3%、42.1%（50 mg/kg）和56.8%、63.2%、58.9%（100 mg/kg）[3]
- 该化合物上调缺血脑组织中血脑屏障紧密连接蛋白（ZO-1和occludin）的表达[3]

- NLRP3炎症小体激活检测：人血管内皮细胞用原花青素B2（25、50、100 μM）预处理2 h，随后用1 μg/mL LPS刺激6 h、5 mM ATP刺激30 min。收集上清液，通过ELISA定量IL-1β和IL-18浓度，评估NLRP3炎症小体抑制效果[2]
- Caspase-1活性检测：上述处理后的细胞裂解，采用比色法，通过特异性底物检测caspase-1活性，在405 nm波长下测定吸光度，反映原花青素B2对caspase-1激活的抑制作用[2]

- MCF-7细胞抗增殖实验：将MCF-7细胞以每孔5×10³个接种到96孔板，过夜孵育。加入10、20、40、60、80 μM的原花青素B2，继续培养24、48、72 h。MTT法检测细胞活力，计算IC50值[1]
- MCF-7细胞凋亡实验：细胞用原花青素B2（40、80 μM）处理48 h后收集，用Annexin V-FITC和PI染色，流式细胞术分析凋亡率[1]
- 凋亡相关蛋白检测：处理后的MCF-7细胞裂解，通过SDS-PAGE分离蛋白（Bcl-2、Bax、β-肌动蛋白），转移至膜上并与特异性抗体孵育，光密度法定量条带强度[1]
- 血管内皮细胞炎症实验：细胞接种到6孔板，用原花青素B2（25、50、100 μM）预处理2 h，随后经LPS + ATP刺激。裂解细胞后，Western blot分析NLRP3、剪切型caspase-1及ASC的蛋白表达[2]

- Rat cerebral ischemia model establishment: Male Sprague-Dawley rats (250–300 g) were anesthetized, and the middle cerebral artery was occluded using the intraluminal filament method to induce focal cerebral ischemia. After 2 h of occlusion, the filament was withdrawn to allow reperfusion [3]
- In vivo efficacy assay: Rats were randomly divided into sham group, model group, and Procyanidin B2 treatment groups (50, 100 mg/kg i.p.). The compound was dissolved in normal saline and administered at 1 h and 24 h after reperfusion. At 72 h post-surgery, neurological function was evaluated using mNSS. Rats were then sacrificed, and brain tissues were collected to measure EB extravasation, brain water content, inflammatory cytokine levels, and tight junction protein expression [3]

- Procyanidin B2 showed no significant cytotoxicity to normal human mammary epithelial cells at concentrations up to 80 μM [1]
- In the rat cerebral ischemia model, no obvious toxic side effects (such as abnormal behavior, organ damage) were observed at therapeutic doses (50, 100 mg/kg i.p.) [3]

[1]. Procyanidin b2 cytotoxicity to mcf-7 human breast adenocarcinoma cells. Indian J Pharm Sci. 2012 Jul;74(4):351-5.

[2]. Procyanidin B2 inhibits NLRP3 inflammasome activation in human vascular endothelial cells. Biochem Pharmacol. 2014 Dec 15;92(4):599-606.

[3]. Procyanidin B2 attenuates neurological deficits and blood-brain barrier disruption in a rat model of cerebral ischemia. Mol Nutr Food Res. 2015 Oct;59(10):1930-41.

Procyanidin B2 is a proanthocyanidin consisting of two molecules of (-)-epicatechin joined by a bond between positions 4 and 8' in a beta-configuration. Procyanidin B2 can be found in Cinchona pubescens (Chinchona, in the rind, bark and cortex), in Cinnamomum verum (Ceylon cinnamon, in the rind, bark and cortex), in Crataegus monogyna (Common hawthorn, in the flower and blossom), in Uncaria guianensis (Cat's claw, in the root), in Vitis vinifera (Common grape vine, in the leaf), in Litchi chinensis (litchi, in the pericarp), in the apple, in Ecdysanthera utilis and in red wine. It has a role as a metabolite and an antioxidant. It is a hydroxyflavan, a proanthocyanidin, a biflavonoid and a polyphenol. It is functionally related to a (-)-epicatechin.
Procyanidin B2 has been reported in Camellia sinensis, Camellia reticulata, and other organisms with data available.
See also: Primula veris flower (part of).

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- Procyanidin B2 is a natural dimeric procyanidin composed of two epicatechin units linked by a C4→C8 bond [1][2][3]
- Its anticancer mechanism involves inducing apoptosis of MCF-7 cells through regulating the Bcl-2/Bax signaling pathway [1]
- The anti-inflammatory effect is mediated by inhibiting NLRP3 inflammasome activation, thereby reducing the release of pro-inflammatory cytokines (IL-1β, IL-18) [2]
- In cerebral ischemia, Procyanidin B2 exerts neuroprotective effects by protecting BBB integrity, inhibiting neuroinflammation, and upregulating tight junction proteins [3]
- It has potential applications in the treatment of breast cancer, inflammatory vascular diseases, and cerebral ischemia-reperfusion injury [1][2][3]

C30H26O12

578.5202

578.142

29106-49-8

Cyanidin Chloride;528-58-5;Procyanidin B1;20315-25-7;Procyanidin C1;37064-30-5;Procyanidin A2;41743-41-3;Procyanidin A1;103883-03-0;Procyanidin B3;23567-23-9

122738

Light yellow to light brown solid powder

1.7±0.1 g/cm3

955.3±65.0 °C at 760 mmHg

197-198ºC

531.6±34.3 °C

0.0±0.3 mmHg at 25°C

1.803

0.3

220.76

10

12

3

42

925

5

C1[C@H]([C@H](OC2=C1C(=CC(=C2[C@@H]3[C@H]([C@H](OC4=CC(=CC(=C34)O)O)C5=CC(=C(C=C5)O)O)O)O)O)C6=CC(=C(C=C6)O)O)O

XFZJEEAOWLFHDH-NFJBMHMQSA-N

InChI=1S/C30H26O12/c31-13-7-20(37)24-23(8-13)41-29(12-2-4-16(33)19(36)6-12)27(40)26(24)25-21(38)10-17(34)14-9-22(39)28(42-30(14)25)11-1-3-15(32)18(35)5-11/h1-8,10,22,26-29,31-40H,9H2/t22-,26-,27-,28-,29-/m1/s1

(2R,3R)-2-(3,4-dihydroxyphenyl)-8-[(2R,3R,4R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-3,4-dihydro-2H-chromen-4-yl]-3,4-dihydro-2H-chromene-3,5,7-triol

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)

H2O : ~66.67 mg/mL (~115.24 mM)
DMSO : ≥ 50 mg/mL (~86.43 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (4.32 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), 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 (4.32 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 (4.32 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: 50 mg/mL (86.43 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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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。