Honokiol
(Synonyms: 和厚朴酚; NSC 293100) 目录号 : GN10664
和厚朴酚（Honokiol）是一种具有多种生物活性天然双酚类化学物质，靶向多种信号分子，具有有效的抗氧化、抗炎、抗血管生成和抗癌等活性，还具有广谱抗菌和抗人类免疫缺陷病毒（HIV）活性。
Cas No.:35354-74-6
Sample solution is provided at 25 µL, 10mM.
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Honokiol is a natural bisphenol chemical with multiple biological activities. It targets multiple signaling molecules and has effective antioxidant, anti-inflammatory, anti-angiogenic and anti-cancer activities. It also has broad-spectrum antibacterial and anti-human immunodeficiency virus (HIV) activities[1, 2]. Honokiol can inhibit the activation of serine/threonine kinase (Akt) and can pass through the blood-brain barrier[3].
In vitro, Honokiol (5, 10μM) treated platelet cells for 0.5-5min, 1 minute after convulsant stimulation, significantly inhibited the phosphorylation of Lyn and PLCγ2, and the amount of p47 protein was significantly reduced after 3min[4]. Honokiol (20-100μM) treated melanoma cell lines (SK-MEL2 and MeWo cells) for 24-72h, reduced the cell viability of both cell lines in a dose- and time-dependent manner, increased the cytosolic cytochrome c content, elevated caspase activity, and increased mitochondrial depolarization[5].
In vivo, Honokiol (5mg/kg) treated rats undergoing cecal ligation and puncture (CLP) surgery by a single intraperitoneal injection restored the morphological changes in rat kidney tissue, reduced the production of oxidative stress and inflammatory cytokines, decreased the levels of nitric oxide (NO) and inducible nitric oxide synthase (iNOS), and inhibited the activation of NF-κB signaling[6]. Honokiol (0.2mg/kg) treated mice with doxorubicin (Dox)-induced heart injury by intraperitoneal injection for 35 days significantly alleviated the cardiotoxicity of Dox, improved cardiac function and reduced cardiomyocyte apoptosis, and activated PPARγ signaling in cardiomyocytes[7].
References:
[1] Ong C P, Lee W L, Tang Y Q, et al. Honokiol: a review of its anticancer potential and mechanisms[J]. Cancers, 2019, 12(1): 48.
[2] Rauf A, Patel S, Imran M, et al. Honokiol: An anticancer lignan[J]. Biomedicine & Pharmacotherapy, 2018, 107: 555-562.
[3] Joo Y N, Eun S Y, Park S W, et al. Honokiol inhibits U87MG human glioblastoma cell invasion through endothelial cells by regulating membrane permeability and the epithelial-mesenchymal transition[J]. International journal of oncology, 2014, 44(1): 187-194.
[4] Lee T Y, Chang C C, Lu W J, et al. Honokiol as a specific collagen receptor glycoprotein VI antagonist on human platelets: Functional ex vivo and in vivo studies[J]. Scientific Reports, 2017, 7(1): 40002.
[5] Mannal P W, Schneider J, Tangada A, et al. Honokiol produces anti‐neoplastic effects on melanoma cells in vitro[J]. Journal of surgical oncology, 2011, 104(3): 260-264.
[6] Li N, Xie H, Li L, et al. Effects of honokiol on sepsis-induced acute kidney injury in an experimental model of sepsis in rats[J]. Inflammation, 2014, 37: 1191-1199.
[7] Huang L, Zhang K, Guo Y, et al. Honokiol protects against doxorubicin cardiotoxicity via improving mitochondrial function in mouse hearts[J]. Scientific reports, 2017, 7(1): 11989.
和厚朴酚（Honokiol）是一种具有多种生物活性天然双酚类化学物质，靶向多种信号分子，具有有效的抗氧化、抗炎、抗血管生成和抗癌等活性，还具有广谱抗菌和抗人类免疫缺陷病毒（HIV）活性[1, 2]。 Honokiol能抑制丝氨酸/苏氨酸激酶（Akt）的活化，能透过血脑屏障[3]。
在体外，Honokiol（5、10μM）处理血小板细胞0.5-5min，在惊厥素刺激后1min，显著抑制了Lyn和PLCγ2的磷酸化，3min后p47蛋白的数量也显著减少[4]。Honokiol（20-100μM）处理黑色素瘤细胞系（SK-MEL2和MeWo细胞）24-72h，以剂量和时间依赖的方式降低了两种细胞系的细胞活力，增加了胞质细胞色素c含量，升高了半胱天冬酶活性，并使线粒体去极化增加[5]。
在体内，Honokiol（5mg/kg）通过单次腹腔注射治疗接受盲肠结扎穿刺（CLP）手术的大鼠，恢复了大鼠肾脏组织的形态变化，减少了氧化应激和炎症细胞因子的产生，降低了一氧化氮（NO）和诱导型一氧化氮合酶（iNOS）的水平，并抑制了NF-κB信号的激活[6]。Honokiol（0.2mg/kg）通过腹腔注射治疗阿霉素（Dox）诱导的心脏损伤小鼠35天，显著减轻了Dox的心脏毒性，改善了心脏功能并减少了心肌细胞凋亡，激活了心肌细胞中的 PPARγ信号传导[7]。
| Cell experiment [1]: | |
Cell lines | Platelets |
Preparation Method | Washed platelets (1.2 × 109 cells/ml) were preincubated with or without honokiol (5μM and 10μM) or the solvent control (0.5% DMSO), followed by the addition of 5ng/mL of convulxin to trigger platelet activation at the indicated times (0.5 to 5min). The cells were collected, and the subcellular extracts were analyzed for the presence of phosphorylated Lyn, phospholipase Cγ2 (PLCγ2), and p47. |
Reaction Conditions | 5, 10μM; 0.5 to 5min |
Applications | At 1min after convulsin stimulation, honokiol(5μM and 10μM) significantly inhibited the phosphorylation of Lyn and PLCγ2. After 3 minutes, the amount of phosphorylated p47 protein in convulsin-activated platelets was reduced. |
| Animal experiment [2]: | |
Animal models | SD rats |
Preparation Method | SD rats were randomly divided into three groups. The control group consisted of untreated and sham-operated rats. Untreated SD rats that underwent cecal ligation and puncture(CLP) surgery were designated as the CLP group. In the CLP+honokiol group, honokiol dissolved in DMSO was intraperitoneally injected into the rats at a dose of 5mg/kg 30min after CLP treatment. All animals were killed 24h after CLP or sham surgery. Blood samples were collected from peripheral blood vessels of rats under anesthesia. Kidney tissues were immediately collected and stored at −80°C or fixed with 4% paraformaldehyde according to the purpose of analysis. |
Dosage form | 5mg/kg; i.p. |
Applications | Treatment with honokiol officinalis restored the morphological changes of renal tissue in rats with CLP, reduced the production of oxidative stress and inflammatory cytokines, decreased the levels of nitric oxide (NO) and inducible nitric oxide synthase (iNOS), and inhibited the activation of NF-κB signaling. |
References: [1] Lee T Y, Chang C C, Lu W J, et al. Honokiol as a specific collagen receptor glycoprotein VI antagonist on human platelets: Functional ex vivo and in vivo studies[J]. Scientific Reports, 2017, 7(1): 40002. [2]Li N, Xie H, Li L, et al. Effects of honokiol on sepsis-induced acute kidney injury in an experimental model of sepsis in rats[J]. Inflammation, 2014, 37: 1191-1199. | |
| Cas No. | 35354-74-6 | SDF | |
| 别名 | 和厚朴酚; NSC 293100 | ||
| 化学名 | 2-(4-hydroxy-3-prop-2-enylphenyl)-4-prop-2-enylphenol | ||
| Canonical SMILES | C=CCC1=CC(=C(C=C1)O)C2=CC(=C(C=C2)O)CC=C | ||
| 分子式 | C18H18O2 | 分子量 | 266.33 |
| 溶解度 | ≥ 83mg/mL in DMSO | 储存条件 | Store at 2-8°C |
| 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 | 3.7547 mL | 18.7737 mL | 37.5474 mL |
| 5 mM | 0.7509 mL | 3.7547 mL | 7.5095 mL |
| 10 mM | 0.3755 mL | 1.8774 mL | 3.7547 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。
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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: >98.50%
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