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Metabolism of Terpenoids in Animal Models and Humans
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Borneol is a component in many essential oils; for example, oils of Pinaceae, Salvia officinalis, Rosmarinus officinalis, and Artemisia species (Bornscheuer et al., 2014). Cinnamomum camphora chemotype borneol and Blumea balsamifera, which are rich in (+)- and (–)-borneol, respectively, are used as sources for preparation of bingpian, a drug of traditional Chinese medicine (Zhao et al., 2012). Moreover, borneol is used to give soaps, perfumes, and other products a scent of spruce needles. In vitro studies with rat liver microsomes could provide evidence for four metabolites (Figure 10.1) (Zhang et al., 2008). The main metabolite, camphor, could also be detected in rat plasma (Sun et al., 2014).
Phytotherapeutic Agents in Epilepsy
Published in Vikas Kumar, Addepalli Veeranjaneyulu, Herbs for Diabetes and Neurological Disease Management, 2018
Carvacrol is a monoterpenic phenol present in essential oils of the Labiatae family. (−)-Borneol is a monoterpene found in several species of Artemisia and Dipterocarpaceae. Citral is a mixture of two geometrical isomers (neral and geranial), present as a component of some citrus oils. All the three compounds have been shown to possess anticonvulsant activity effect against PTZ-induced and MES seizures.85 Mechanistic studies suggest that the GABAergic neurotransmitter system might be involved in the anti-convulsant activity of (−)-borneol. A recent comparative study with 12 naturally occurring substances for protection against MES-induced tonic seizures in mice has concluded that only (−)-borneol produced a 75% protection thus suggesting that borneol is worthy of consideration as a potentially favorable compound in epileptology.86
Effect of different doses of borneol on the pharmacokinetics of vinpocetine in rat plasma and brain after intraocular administration
Published in Xenobiotica, 2020
Qun Ma, Manman Dai, Huimin Zhang, Luyu Bai, Ning He
Borneol, as a traditional drug, has attracted increasing attention and can rapidly cross the BBB due to its low molecular mass and high lipid solubility (Wang et al., 2014; Xiong et al., 2013). Borneol is widely used in a variety of medical formulations, often as an adjuvant, such as in “Su Xiao Jiu Xin Wan,” “An Gong Niu Huang Wan,” and “Su He Xiang Wan,” which are used to prevent and treat cardiovascular and cerebrovascular diseases (Tang et al., 2005; Zhao et al., 2002). Adjuvants can target other components in formulations to tissues or organs, such as the brain (Zhao et al., 2012). Studies have demonstrated that borneol exerts antibacterial, anti-inflammatory, antiviral, cardioprotective and neuroprotective effects (Xiao et al., 2012). It can improve drug permeation through the skin, gastrointestinal mucous membranes, nasal mucosa, and the cornea, resulting in enhanced bioavailability of co-delivered drugs (Mei et al., 2006; Zhang et al., 2019). Several studies have also shown that borneol could promote the accumulation of drugs in brain tissue and improved brain bioavailability kaempferol (Zhang et al., 2015), gastrodin (Cai et al., 2014), puerarin (Gao et al., 2010), and geniposide. Thus, we chose borneol as an absorption enhancer to improve the penetration in the mucosa, accelerate the transport of materials, and enhance brain targeting following intraocular administration.
Natural borneol sensitizes human glioma cells to cisplatin-induced apoptosis by triggering ROS-mediated oxidative damage and regulation of MAPKs and PI3K/AKT pathway
Published in Pharmaceutical Biology, 2020
Wen-qiang Cao, Xiao-qian Zhai, Ji-wei Ma, Xue-qi Fu, Bai-song Zhao, Pu Zhang, Xiao-yan Fu
Borneol (C10H18O) is a bicyclic monoterpene extracted from the resin and volatile oil of dipterocarp (Wu et al. 2016). Borneol has been broadly applied in food and drug industry and is available as synthetic (SB) and natural borneol (NB) (Qi et al. 2013; Wu et al. 2016). Considering the mucosa stimulus and hepatotoxicity of SB, NB has more potential for further commercial applications. NB effectively improves the permeability of drugs by regulating intestinal mucous or blood–brain barrier (Cai et al. 2008; Duan et al. 2016; Xing et al. 2016). NB can also enhance the efficacy of chemo-drugs against various cancer cell lines by increasing the intracellular drug accumulation and modulating ROS-mediated DNA damage with the involvement of MAPKs activation and Akt inactivation (Chen, Li Su, and Chen 2015; Chen, Li, Su, Li, et al. 2015; Liu et al. 2018; Meng et al. 2018). The action of NB in chemo-sensitization is constantly being confirmed. Nevertheless, data on the synergistic effects of NB and cisplatin in human glioma treatment are limited. Therefore, the present study aims to verify whether NB plays a role in cisplatin-induced glioma cell apoptosis. The underlying mechanisms were also illuminated by the detection of ROS generation and related protein expressions.
Brain-targeted intranasal delivery of dopamine with borneol and lactoferrin co-modified nanoparticles for treating Parkinson’s disease
Published in Drug Delivery, 2019
Shengnan Tang, Aiping Wang, Xiuju Yan, Liuxiang Chu, Xiucheng Yang, Yina Song, Kaoxiang Sun, Xin Yu, Rongxia Liu, Zimei Wu, Peng Xue
Although the intranasal delivery method has many advantages, rapid clearing of drugs or formulation by the mucociliary system in the nose limit its applications. Hence, it is important to develop a newer method that can allow the drug to remain in the nasal cavity for a longer period, for instance, by using chitosan with mucoadhesive nature enhancing the nasal retention time (Ahmad et al., 2017b) or enhancing the permeability across the epithelial membrane (Tzeyung et al., 2019). Borneol is a bicyclic monoterpene and is widely applied to traditional Chinese medicine (Bhatia et al., 2008). It has anti-epileptogenic (Ehrnhofer-Ressler et al., 2013) and anti-inflammatory effects (Tambe et al., 2016). In particular, it can enhance the brain penetration and transport of other drugs to improve bioavailability and enhance the distribution of drugs across various physical barriers such as the nasal mucosa and the blood-brain barrier (Qi et al., 2013). Although borneol is effective in promoting drug transport to the brain (Ren et al., 2013), drugs could still be metabolized at non-targeting tissues, which will cause serious adverse effects. In our previous studies (Bi et al., 2016; Yan et al., 2018), lactoferrin (Lf) was found to be an effective biological ligand for drug delivery to the striatum. The Lf receptor is overexpressed on the apical surface of respiratory epithelial cells and in the capillaries and neurons related to neurodegenerative diseases such as PD and Alzheimer’s disease (Suzuki et al., 2005; Elfinger et al., 2007; Liu et al., 2013; Meng et al., 2018).