Pinocembrin
(Synonyms: 乔松素; (+)-Pinocoembrin; Dihydrochrysin; Galangin flavanone) 目录号 : GN10120
Pinocembrin是一种黄酮类化合物，是竞争性的组氨酸脱羧酶（HDC）抑制剂。
Cas No.:480-39-7
Sample solution is provided at 25 µL, 10mM.
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Pinocembrin is a flavonoid compound and a competitive histidine decarboxylase (HDC) inhibitor[1]. Pinocembrin has multiple biological activities, such as antibacterial, anti-inflammatory, antioxidant and neuroprotective effects[2, 3].
In vitro, Pinocembrin (25-200µM) treatment of A549 cells for 24-72h reduced cell viability, proliferation, promoted cell apoptosis, and reduced cell autophagy in a dose- and time-dependent manner[4]. Pinocembrin (100µM) treatment of colorectal cancer HT29 and HCT116 cells inhibited cell proliferation, migration, and invasiveness, and inhibited epithelial-mesenchymal transition[5]. Pinocembrin (25-100µM) treatment of ovarian cancer SKOV3 cells for 48h inhibited cell proliferation and migration and promoted cell apoptosis, and downregulated the mRNA levels of N-cadherin and GABAB receptors[6].
In vivo, oral administration of Pinocembrin (50mg/kg) to diabetic encephalopathy (DE) mice for 10 days significantly improved the behavioral and cognitive impairments of DE mice in the open field task and Morris water maze, significantly increased the neuronal survival rate in the frontal cortex and hippocampal CA3 region, inhibited the nuclear translocation of NF-κB in the cerebral cortex and hippocampus of mice, and reduced the expression of DETNF-α[7].
References:
[1] Hanieh H, Islam V I H, Saravanan S, et al. Pinocembrin, a novel histidine decarboxylase inhibitor with anti-allergic potential in in vitro[J]. European Journal of Pharmacology, 2017, 814: 178-186.
[2] Rasul A, Millimouno F M, Ali Eltayb W, et al. Pinocembrin: a novel natural compound with versatile pharmacological and biological activities[J]. BioMed research international, 2013, 2013(1): 379850.
[3] Shen X, Liu Y, Luo X, et al. Advances in biosynthesis, pharmacology, and pharmacokinetics of pinocembrin, a promising natural small-molecule drug[J]. Molecules, 2019, 24(12): 2323.
[4] Gong H. Pinocembrin suppresses proliferation and enhances apoptosis in lung cancer cells in vitro by restraining autophagy[J]. Bioengineered, 2021, 12(1): 6035-6044.
[5] Jiang L, Yang Y, Feng H, et al. Pinocembrin inhibits the proliferation, migration, invasiveness, and epithelial-mesenchymal transition of colorectal cancer cells by regulating LACTB[J]. Cancer Biotherapy & Radiopharmaceuticals, 2022, 37(7): 527-536.
[6] Gao J, Lin S, Gao Y, et al. Pinocembrin inhibits the proliferation and migration and promotes the apoptosis of ovarian cancer cells through down-regulating the mRNA levels of N-cadherin and GABAB receptor[J]. Biomedicine & Pharmacotherapy, 2019, 120: 109505.
[7] Pei B, Sun J. Pinocembrin alleviates cognition deficits by inhibiting inflammation in diabetic mice[J]. Journal of neuroimmunology, 2018, 314: 42-49.
Pinocembrin是一种黄酮类化合物，是竞争性的组氨酸脱羧酶（HDC）抑制剂[1]。Pinocembrin具有多种生物活性，例如抗菌、抗炎、抗氧化和神经保护作用等[2, 3]。
在体外，Pinocembrin（25-200µM）处理A549细胞24-72h，以剂量和时间依赖性方式降低了细胞活力，减少了增殖并促进了细胞的凋亡，减少了细胞的自噬[4]。Pinocembrin（100µM）处理结直肠癌HT29和HCT116细胞，抑制了细胞的增殖、迁移、侵袭性，抑制了上皮-间质转化[5]。Pinocembrin（25-100µM）处理卵巢癌SKOV3细胞48h，抑制了细胞的增殖和迁移并促进细胞凋亡，下调了N-钙粘着蛋白和GABAB受体的mRNA水平[6]。
在体内，Pinocembrin（50mg/kg）通过口服治疗糖尿病脑病（DE）小鼠10天，显著改善了DE小鼠在旷场任务和Morris水迷宫中的行为和认知障碍，显著增加了额叶皮质和海马CA3区域的神经元存活率，抑制了小鼠大脑皮层和海马中的NF-κB的核转位并降低DETNF-α的表达[7]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were treated with different concentration of Pinocembrin (25, 50, 100, 150 and 200µM) for 24, 48 and 72h, respectively to detect cell viability by Cell counting kit-8 (CCK-8) assay. |
Reaction Conditions | 25, 50, 100, 150, 200µM; 24, 48, 72h |
Applications | Pinocembrin reduces the cell viability of A549 cells in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | ICR mice |
Preparation Method | The ICR mice were fasted overnight and then were administered a single intraperitoneal injection of STZ (50mg/kg) freshly dissolved in 0.1M citrate buffer (pH 4.21) to induce diabetes. Mice were randomly divided into four groups of 15 animals each, which included the control, Diabetic encephalopathy (DE), DE+Vehicle and DE+Pinocembrin groups. At 24h after induction of diabetes, Pinocembrin (50mg/kg/day, in saline) was orally administered to the DE+Pinocembrin groups until the end of experiment After administration of STZ for 10 days, the locomotor activities and exploratory behaviors of mice were examined in an open field. |
Dosage form | 50mg/kg/day; 10 days; p.o. |
Applications | Pinocembrin significantly improved the behavior and cognitive deficits of DE mice in open field tasks and the Morris water maze. Pinocembrin also markedly increased neuronal survival in the frontal cortex and hippocampal CA3 region. Pinocembrin could suppress the nuclear translocation of NF-κB and decrease TNF-α expression in the cerebral cortex and the hippocampus of DE mice. |
References: | |
| Cas No. | 480-39-7 | SDF | |
| 别名 | 乔松素; (+)-Pinocoembrin; Dihydrochrysin; Galangin flavanone | ||
| 化学名 | (2S)-5,7-dihydroxy-2-phenyl-2,3-dihydrochromen-4-one | ||
| Canonical SMILES | C1C(OC2=CC(=CC(=C2C1=O)O)O)C3=CC=CC=C3 | ||
| 分子式 | C15H12O4 | 分子量 | 256.25 |
| 溶解度 | DMSO : 125 mg/mL (487.80 mM) | 储存条件 | Store at 2-8°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9024 mL | 19.5122 mL | 39.0244 mL |
| 5 mM | 0.7805 mL | 3.9024 mL | 7.8049 mL |
| 10 mM | 0.3902 mL | 1.9512 mL | 3.9024 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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