Honokiol (Synonyms: NSC 293100)

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.