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]。