Natural Borneol Research Articles

Transcriptome analysis revealed the role of moderate exogenous methyl jasmonate treatments in enhancing the metabolic pathway of L-borneol in the Blumea balsamifera.

Blumea balsamifera L. (Ainaxiang) DC. is a perennial herb of the compositae family. It is also the primary source of natural borneol. Endo-borneol, the principal medical active element in B. balsamifera, is anti-inflammatory, antioxidant, and analgesic; enhances medicine absorption; refreshes; and is used as a spice and in cosmetic. Industrialization of B. balsamifera is limited by its low L-borneol concentration. Thus, understanding the accumulation pattern of the secondary metabolite endo-borneol and its synthesis process in secondary metabolism is critical for increasing B. balsamifera active ingredient content and cultivation efficiency. In this work, B. balsamifera was treated with varying concentrations (1.00 and 10.00 mmol/L) of methyl jasmonate (MeJA) as an exogenous foliar activator. The physiological parameters and L-borneol concentration were then assessed. Transcriptome sequencing of B. balsamifera-induced leaves was used to identify key genes for monoterpene synthesis. The treatment effect of 1 mmol/L MeJA was the best, and the leaves of all three leaf positions accumulated the highest L-borneol after 120h, correspondingly 3.043 mg·g-1 FW, 3.346 mg·g-1 FW, and 2.044 mg·g-1 FW, with significant differences from the control. The main assembly produced 509,285 transcripts with min and max lengths of 201 and 23,172, respectively. DEG analysis employing volcano blots revealed 593, 224, 612, 2,405, 1,353, and 921 upregulated genes and 4, 123, 573, 1,745, 766, and 763 downregulated genes in the treatments D1_1vsCK, D1_10vsCK, D2_1vsCK, D2_10vsCK, D5_1vsCK, and D5_10vsCK. Interestingly, when exposed to MeJA treatments, the MEP pathway's unigenes express themselves more than those of the MVA route. Finally, when treated with 1 mmol/L, the genes DXR, DXS, and GPS showed increased expression over time. At the same time, a 10 mmol/L therapy resulted in elevated levels of ispH and GGPS. Our preliminary research indicates that exogenous phytohormones can raise the level of L borneol in B. balsamifera (L.) DC when given in the appropriate amounts. The most significant discovery made while analyzing the effects of different hormones and concentrations on B. balsamifera (L.) DC was the effect of 1 mmol/L MeJA treatment.

Transgelin Promotes Glioblastoma Stem Cell Hypoxic Responses and Maintenance Through p53 Acetylation.

Glioblastoma (GBM) is a lethal cancer characterized by hypervascularity and necrosis associated with hypoxia. Here, it is found that hypoxia preferentially induces the actin-binding protein, Transgelin (TAGLN), in GBM stem cells (GSCs). Mechanistically, TAGLN regulates HIF1α transcription and stabilizes HDAC2 to deacetylate p53 and maintain GSC self-renewal. To translate these findings into preclinical therapeutic paradigm, it is found that sodium valproate (VPA) is a specific inhibitor of TAGLN/HDAC2 function, with augmented efficacy when combined with natural borneol (NB) in vivo. Thus, TAGLN promotes cancer stem cell survival in hypoxia and informs a novel therapeutic paradigm.

Dynamic migration mechanism of borneol synergistic polyethylene glycol for the construction of silicon-acrylate antifouling coating

Silicone-based coatings are vulnerable to marine fouling organisms in static environments, which seriously hampers its practical application. Here, an amphiphilic acrylate polymer is designed by hydrophilic polyethylene glycol and antibacterial borneol, which is introduced into polydimethylsiloxane (PDMS) by covalent linking to prepare antifouling coatings. XPS and CA tests prove that amphiphilic acrylate polymer can migrate to coating surface in the marine environment to maximize antifouling properties. Mytilus edulis foot protein adhesion test find it can weaken interface force between Mefp-3 and surface. Laboratory antifouling performance evaluations confirm that the coatings are effective against the adhesion of bacteria (86.72 % reduction for E. coli), diatoms (87.76 % reduction for Nitzschia closterium). The good antifouling properties of coatings are ascribed to the synergistic effect among unique bicyclic monoterpene structure of natural non-toxic borneol and amphiphilic acrylate polymer on surface of coatings. Moreover, the coating is less harmful to the marine ecological balance than traditional coatings containing toxic biocides due to the introduction of natural non-toxic borneol. This work contributes new insights in the exploration of environmentally friendly coating with excellent static antifouling performance.

Fabrication of an anti-fouling coating based on epoxy resin with a double antibacterial effect via an in situ polymerization strategy

The hull and subsea equipment are often plagued by widespread marine biofouling, so developing a sustainable environmental protection antifouling paint is urgent. The study designed and developed an antifouling composite coating system (E44-Ag-PGI) with a synergistic antibacterial effect based on the dual strategy of the bacteriostatic effect of stereochemical structure on polymer surface and release sterilization of metal nanoparticles. Firstly, an antifouling agent (PGI) was prepared by simple radical polymerization by combining glycidyl methacrylate with borneol, a complex bicyclic monoterpene structure extracted from plants. Then bisphenol A epoxy resin with strong adhesion to metal was selected as the base material. The synthetic antifouling agent with epoxy groups was polymerized in situ into the epoxy resin network, and compared with pure epoxy resin, the elongation at break of E44-Ag-PGI coating with 20 % PGI content increased from 40.37 % to 124.8 %, which was mainly attributed to the introduction of a soft chain of antifouling agent polymer, which improved the flexibility of the coating. Meanwhile, the antibacterial efficiency of the coating against Pseudomonas aeruginosa and Staphylococcus aureus was 97.69 % and 95.9 %, respectively. This excellent antibacterial performance was mainly attributed to the synergistic antibacterial action of natural borneol and AgNPs. In addition, the biofilm and diatom resistance experiments of the coating showed that the coating also has an excellent antifouling effect. This provided a new research idea for environmentally friendly antifouling coatings.

High solid and low viscosity waterborne polyurethane acrylate with excellent anti-corrosion and anti-bacterial performances

The design and preparation of great corrosion resistance and high-solid waterborne polyurethane dispersion with low viscosity is still a challenge in the field of the polyurethane industry. Herein, we developed a simple method involving a core-shell process to prepare a core-shell structured waterborne polyurethane acrylate dispersion (WPUAD). First, isobornyl acrylate, a derivative of natural product borneol, dihydroxylated by a thiol-ene click reaction was used to prepare oil-based polyurethane acrylate as prepolymer A (core) and waterborne polyurethane acrylate as prepolymer B (shell). Then, the core-shell WPUAD was obtained by mixing and emulsifying the two prepolymer at a certain ratio. The study reveals that the core-shell structured WPUAD not only has a low viscosity (~1330 mPa.s) but also holds a high-solid content (~ 60 wt%). At the same time, the highly solid WPUAD has excellent stability with no breast breakage even after more than 1 year of storage. In addition, various electrochemical measurements, water contact angles, and water absorption tests were performed to determine the anti-corrosive properties of the WPUAD-derived coatings. The results show that the WPUA coatings exhibit significantly enhanced anticorrosion with respect to the single prepolymer B derived coatings, which is attributed to their high cross-linking density resulting from the core-shell structure and the introduction of hydrophobic isobornyl acrylate. In addition, because of the introduction of the dihydroxylated isobornyl acrylate as chain extenders, the WPUA coating has great anti-bacterial adhesion properties with an anti-bacterial efficiency of 82.3 %. We believe that our work provides a generic preparation method to obtain a commercially available high-solid WPUAD with excellent anti-corrosion properties.

A silicone coating containing natural borneol fluorinated side chains with excellent static antifouling properties

Nowadays, the development of sustainable nontoxic antifouling coatings is urgent. In this work, the isobornyl as antifouling groups and dodecfluoroheptyl were introduced into the silicone side chains to prepare the environment-friendly silicone antifouling coatings. The synergistic effect of natural borneol and dodecfluoroheptyl improved the static antifouling ability of silicone coating. The coatings exhibited good optical clarity (>92%, 400–800 nm), high adhesion (>2 MPa, steel plates) and excellent fouling release and self-cleaning ability. For example, PDMS-F-PIBO-23 coating had excellent antibacterial and antifouling activities. It’s antibacterial resistance to marine bacteria (Pseudomonas sp.) reached 95.6%, which reduced the coverage area of biofilm by 86.9%, and effectively prevented the adhesion of diatoms. This remarkable antibacterial and antifouling performance was attributed to the complex molecular structure of natural non-toxic borneol and the enrichment of fluoropolymers. Field tests at Yellow Sea showed that the coating had good antifouling ability and could be used for >6 months. Most importantly, compared with traditional coatings containing toxic fungicides, the coating is less harmful to the marine ecological balance. This research provides more possibilities for marine antifouling coatings design and preparation which is expected to be applied in marine, medical and other antipollution fields.

Protective effects of three kinds of borneol on different brain regions in acute cerebral ischemia/reperfusion model rats

This study compared the ameliorating effects of L-borneol, natural borneol, and synthetic borneol on the injury of different brain regions in the rat model of acute phase of cerebral ischemia/reperfusion(I/R) for the first time, which provides a reference for guiding the rational application of borneol in the early treatment of ischemic stroke and has important academic and application values. Healthy specific pathogen-free(SPF)-grade SD male rats were randomly assigned into 13 groups: a sham-operation group, a model group, a Tween model group, a positive drug(nimodipine) group, and high-, medium-, and low-dose(0.2, 0.1, and 0.05 g·kg~(-1), respectively) groups of L-borneol, natural borneol, and synthetic borneol according to body weight. After 3 days of pre-administration, the rat model of I/R was established by suture-occluded method and confirmed by laser speckle imaging. The corresponding agents in different groups were then administered for 1 day. The body temperature was monitored regularly before pre-administration, days 1, 2, and 3 of pre-administration, 2 h after model awakening, and 1 d after model establishment. Neurological function was evaluated based on Zea-Longa score and modified neurological severity score(mNSS) 2 h and next day after awakening. The rats were anesthetized 30 min after the last administration, and blood was collected from the abdominal aorta. Enzyme-linked immunoassay assay(ELISA) was employed to determine the serum levels of tumor necrosis factor-alpha(TNF-α), interleukin-6(IL-6), IL-4, and transforming growth factor-beta1(TGF-β1). The brain tissues were stained with triphenyltetrazolium chloride(TTC) for the calculation of cerebral infarction rate, and hematoxylin-eosin(HE) staining was used for observing and semi-quantitatively evaluating the pathological damage in different brain regions. Immunohistochemistry was employed to detect the expression of ionized calcium binding adapter molecule 1(IBA1) in microglia. q-PCR was carried out to determine the mRNA levels of iNOS and arginase 1(Arg1), markers of polarization phenotype M1 and M2 in microglia. Compared with the sham-operation group, the model group and the Tween model group showed significantly elevated body temperature, Zea-Longa score, mNSS, and cerebral infarction rate, severely damaged cortex, hippocampus, and striatum, increased serum levels of IL-6 and TNF-α, and decreased serum levels of IL-4 and TGF-β1. The three borneol products had a tendency to reduce the body temperature of rats 1 day after modeling. Synthetic borneol at the doses of 0.2 and 0.05 g·kg~(-1), as well as L-borneol of 0.1 g·kg~(-1), significantly reduced Zea-Longa score and mNSS. The three borneol products at the dose of 0.2 g·kg~(-1) significantly reduced the cerebral infarction rate. L-borneol at the doses of 0.2 and 0.1 g·kg~(-1) and natural borneol at the dose of 0.1 g·kg~(-1) significantly reduced the pathological damage of the cortex. L-borneol and natural borneol at the dose of 0.1 g·kg~(-1) attenuated the pathological damage of hippocampus, and 0.2 g·kg~(-1) L-borneol attenuated the damage of striatum. The 0.2 g·kg~(-1) L-borneol and the three doses of natural borneol and synthetic borneol significantly reduced the serum level of TNF-α, and the 0.1 g·kg~(-1) synthetic borneol reduced the level of IL-6. L-borneol and synthetic borneol at the dose of 0.2 g·kg~(-1) significantly inhibited the activation of cortical microglia, and 0.2 g·kg~(-1) L-borneol up-regulated the expression of Arg1 and down-regulated the expression level of iNOS. In conclusion, the three borneol products may alleviate inflammation to ameliorate the pathological damage of brain regions of rats in the acute phase of I/R by inhibiting the activation of microglia and promoting the polarization of microglia from M1 type to M2 type. The protective effect on brain followed a trend of L-borneol > synthetic borneol > natural borneol. We suggest L-borneol the first choice for the treatment of I/R in the acute phase.

Natural borneol serves as an adjuvant agent to promote the cellular uptake of piperlongumine for improving its antiglioma efficacy

Piperlongumine (PL) can selectively inhibit the proliferation of various cancer cells by increasing reactive oxygen species (ROS) level to cause a redox imbalance in cancer cells rather than in normal cells. However, the clinical application of PL is limited by its poor cellular uptake. Natural borneol (NB) is extracted from the fresh branches and leaves of Cinnamomum camphora (L.) Presl. with the purity of (+)-borneol no less than 96.0%. NB has been often used as an adjuvant agent to promote the cellular uptake of other drugs. This study aims to investigate the effect of NB on the cellular uptake of PL for improving its antiglioma efficacy and underlying mechanism. NB obviously promoted the cellular uptake of PL with a 1.3-fold increase in the maximum peak concentration and an earlier peak time of 30 min in C6 glioma cells. The cellular uptake of PL was enhanced by NB through down-regulating the expression levels of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2). The combination of NB and PL significantly induced higher levels of ROS, which increased apoptosis and enhanced G2/M cycle arrest of C6 glioma cells, compared to PL alone administration. NB-enhanced antiglioma efficacy of PL without side effects was confirmed in tumor-bearing mice, which was attributed to the improved cellular uptake of PL. The distribution of PL in the tumor tissue of combined group increased 2.39 times than that of PL-treated group. We firstly report NB as an adjuvant agent to improve the antiglioma efficacy of PL in a ROS-dependent manner, which is due to the enhanced cellular uptake of PL by NB though down-regulating the expression levels of ABCB1 and ABCG2. This work provides a new strategy to promote the cellular uptake of PL with great potential for the treatment of glioma.

Thirteen Dipterocarpoideae genomes provide insights into their evolution and borneol biosynthesis

Dipterocarpoideae, the largest subfamily of the Dipterocarpaceae, is a dominant component of Southeast Asian rainforests and is widely used as a source of wood, damar resin, medicine, and essential oil. However, many Dipterocarpoideae species are currently on the IUCN Red List owing to severe degradation of their habitats under global climate change and human disturbance. Genetic information regarding these taxa has only recently been reported with the sequencing of four Dipterocarp genomes, providing clues to the function and evolution of these species. Here, we report on 13 high-quality Dipterocarpoideae genome assemblies, ranging in size from 302.6 to 494.8 Mb and representing the five most species-rich genera in Dipterocarpoideae. Molecular dating analyses support the Western Gondwanaland origin of Dipterocarpaceae. Based on evolutionary analysis, we propose a three-step chromosome evolution scenario to describe the karyotypic evolution from an ancestor with six chromosomes to present-day species with 11 and 7 chromosomes. We discovered an expansion of genes encoding cellulose synthase (CesA), which is essential for cellulose biosynthesis and secondary cell-wall formation. We functionally identified five bornyl diphosphate synthase (BPPS) genes, which specifically catalyze the biosynthesis of borneol, a natural medicinal compound extracted from damar resin and oils, thus providing a basis for large-scale production of natural borneol in vitro.

Natural borneol enhances the anti-cerebral ischaemia efficacy of formononetin in MCAO/R rats by promoting its delivery in the brain.

Objectives Due to its high morbidity, high mortality, and high disability, stroke has been the first cause of death and the major cause of adult disability in China. Natural borneol has been widely utilized in Traditional Chinese Medicine to promote drug absorption. Formononetin is a natural isoflavonoid with potent neuroprotective activity but poor brain delivery. Methods This study aimed to screen the optimum proportion that natural borneol promotes formononetin entry into the brain, evaluate the anti-cerebral ischaemia efficacy of formononetin/natural borneol combination in middle cerebral artery occlusion/reperfusion model rats, and clarify the possible mechanism for natural borneol's promoting formononetin delivery in the brain. Key findings Our studies exhibited that natural borneol remarkably promoted formononetin entry into the brain when combined with formononetin in a 1 : 1 molar ratio and notably improved neuro-behavioural scores and reduced the infarct of middle cerebral artery occlusion/reperfusion model rats. This study further discovered that the enhanced anti-cerebral ischaemia effect resulted from natural borneol increasing the permeability of the blood-brain barrier to elevate formononetin concentration in the brain rather than the pharmacodynamic synergy or addition between formononetin and natural borneol. Conclusions The study provides a good strategy to screen drug combinations for the treatment of brain disease by combining natural borneol with other drugs.

Effects of Natural Borneol on Germ Tube Formation and Preformed Biofilm Activity in Candida albicans

Candida albicans infection mainly occurs in patients with suppressed immune function and is the main pathogen of nosocomial infections. The use of natural products aimed at controlling fungal diseases is considered an interesting alternative to synthetic fungicides due to their lower adverse reactions and the lower cost of plant preparations compared to modern conventional pharmaceuticals. Natural borneol has a long history of treating ulcers and local infections in traditional Chinese medicine. In this study, we present an analysis of the in vitro effects of natural borneol on planktonic cells of C albicans in the liquid and vapor phases. We also investigated the effects of natural borneol on germ tube formation and mature biofilm activity of C albicans. We found that vapor-phase borneol (minimum inhibitory concentration [MIC] 0.4 mg/cm3) inhibited C albicans more effectively than in the liquid phase (MIC 2 mg/mL). The C albicans germ tube decreased by 99% to 60% at sub-MICs of 0.5 to 0.125 mg/mL. The inhibitory effects of 0.25, 0.5, 1, 2, and 4 mg/mL borneol on the biofilm activity were 33.7%, 48.6%, 49.9%, 52.9%, and 58.2%, respectively. Natural borneol may have potential in the treatment and prevention of C albicans infections.

Borneol as Adjuvant Chemotherapy: A New Way for the Development of Novel Chemotherapeutic

Nature has generously open life-saving remedies to mankind by offering evolutionarily optimized drug like bimolecular in the form of several natural products. These marvelous gifts of nature have been serving as most suitable candidates against the treatment of multiple disorders and particularly for cancer (2nd leading cause of death, cancer) due to their pleiotropic mode of action on target molecules. Current review intends to provide an update on the bioactivities of such gifts from nature, natural borneol, which is the major bioactive constituents of traditionally used medicines. Borneol is a monoterpenoid, isolated from different medicinal plants and have strong potential to be used against multiple disorders such as bacterial and inflammatory infections. Recently it is investigated that borneol has a great potential of inhibiting the growth of multiple neoplasms such as hepatocellular carcinoma, neuroblastoma, glioma, esophageal squamous cell carcinoma, ovarian and lung cancer. Moreover, by regulating the BBB junctions it also increases the drug concentration in cancer cells, this shows that its combine use with already practiced therapeutics may increase the efficacy of these therapeutics against cancer cells. In this review we will summarize all the studies on anticancer activity of borneol, our primary goal will be to discuss the combined use of borneol with other clinically used drugs to improve their efficacy against human cancers.

A Study on the Mechanism of the Sedative-hypnotic Effect of Cinnamomum camphora chvar. Borneol Essential Oil Based on Network Pharmacology.

In this paper, we investigated the sedative-hypnotic effect of Cinnamomum camphora chvar. Borneol essential oil (BEO, 16.4% borneol), a by-product of steam distillation of Cinnamomum camphora chvar. Borneol, from which natural crystalline borneol (NCB, 98.4% borneol) is obtained. Using locomotor activity tests and pentobarbital sodium-induced sleep test, it was found that BEO significantly reduced locomotor activity (p < 0.05), shortened sleep latency (p < 0.0001), prolonged sleep duration (p < 0.05), and had a sedative-hypnotic effect. We constructed the "components-targets-signaling pathways" and "proteinprotein interaction" (PPI) network of BEO using network pharmacology. The results show that the 24 active components of BEO acted on 17 targets, mainly through response to alkaloid and catecholamine transport, and neuroactive ligand-receptor interaction. The PPI network identified 12 key proteins, mainly dopamine receptor (DR)D2, opioid receptor mu 1 (OPRM1), and opioid receptor kappa 1 (OPRK1), and we further analyzed the active components and targets of BEO through molecular docking. The results showed that the active components and targets obtained by network pharmacology analyses had good binding activity, which reflected their multi-component, multi-target, multi-pathway action characteristics. This paper provides a theoretical basis for further study of the mechanism of action of BEO in the treatment of insomnia.

Evaluation of the analgesic potential and safety of Cinnamomum camphora chvar. Borneol essential oil

ABSTRACT Cinnamomum camphora chvar. Borneol essential oil (BEO, 18.2% v/v borneol) is a by-product of steam distillation to produce natural crystalline borneol (NCB, 98.4% v/v borneol). Given the known medicinal properties of borneol, the analgesic function and safety were studied. Horn’s method and the Draize test revealed a gender difference in mice regarding acute oral LD50, i.e., low-toxicity to female mice (2749 mg/kg), but practically nontoxic to male mice (5081 mg/kg). There was no acute and skin or eye irritation when BEO was applied directly, if the BEO concentration was less than 50%. The analgesic effect of BEO was evaluated by the glacial acetic acid-induced writhing pain model. Continuous topical application of BEO to the abdomen of mice for 6 d, significantly reduced observed writhing in mice (p < 0.001) with a strong dose-response relationship (r = −0.9006). Concomitantly, the levels of the serum pain-related mediators, prostaglandin E2 (PGE2) and transient receptor potential melastatin-8 (TRPM8) were significantly reduced (p < 0.001), and the latter showed a strong dose-response relationship (r = −0.9427). Therefore, BEO had similar analgesic functions to borneol and was demonstrated to be safe for medicinal use.

Bioinspired Durable Antibacterial and Antifouling Coatings Based on Borneol Fluorinated Polymers: Demonstrating Direct Evidence of Antiadhesion.

Substituting natural products for traditional poison-killing antifouling agents is an efficient and promising method to alleviate the increasingly serious ecological crisis and aggravate the loss due to marine biofouling. Herein, the successful synthesis of poly(methyl methacrylate-co-ethyl acrylate-co-hexafluorobutyl methacrylate-co-isobornyl methacrylate) copolymer (PBAF) with borneol monomers and fluorine by a free radical polymerization method is reported. The PBA0.09F coating exhibits outstanding antibacterial and antifouling activity, achieving 98.2% and 92.3% resistance to Escherichia coli and Staphylococcus aureus, respectively, and the number of Halamphora sp. adhesion is only 26 (0.1645 mm2) in 24 h. This remarkable antibacterial and antifouling performance is attributed to the incorporation of fluorine components into the copolymer, which induces a low surface energy and hydrophobicity and the complex molecular structure of the natural nontoxic antifouling agent borneol. In addition, the results showed that the contents of the adhesion-related proteins mfp-3, mfp-5, and mfp-6 were significantly reduced, which proved that natural substances affect the secretion of biological proteins. Importantly, the PBAF coating exhibits excellent environmental friendliness and long-term stability. The antifouling mechanism is clarified, and an effective guide for an environmentally friendly antifouling coating design is proposed.

Antifouling and Antibacterial Polymer-Coated Surfaces Based on the Combined Effect of Zwitterions and the Natural Borneol.

The development and application of natural antibacterial materials have always been the focus of biomedical research. Borneol as a natural antibacterial compound has received extensive attention. However, the hydrophobicity caused by its unique structure limits its application range to a certain extent. In this study, we combine zwitterionic 2-methacryloyloxyethyl phosphorylcholine (MPC) with a complex bicyclic monoterpene structure borneol compound and prepare an excellent antifouling and antibacterial surface via the Schiff-base bond. The prepared coating has excellent hydrophilicity verified by the contact angle (CA), and its polymer layer is confirmed by X-ray photoelectron spectroscopy (XPS). The zwitterion MPC and borneol moieties in the copolymer play a coordinating role, relying on super hydration and the special stereochemical structure to prevent protein adsorption and inhibit bacterial adhesion, respectively, which are demonstrated by bovine serum albumin (BSA) adsorption and antibacterial activity test. Moreover, the water-soluble borneol derivative as the antibacterial surfaces we designed here was biocompatible toward MRC-5 (lung fibroblasts), as showed by in vitro cytotoxicity assays. Such results indicate the potential application of the as-prepared hydrophilic surfaces in the biomedical materials.

Research progress of natural borneol resources

Natural borneol is an important traditional Chinese medicine herb with resuscitation-inducing, antipyretic and analgesic effects, and has been widely used in the fields of medicine, perfume and chemical industry. At present, natural borneol is short supply, with promising market development prospects. This paper summarized the distribution of borneol plant resources, cultivation status and molecular biological research progress, in the expectation of providing basis and ideas for the research and application of natural borneol.

The anti-inflammatory potential of Cinnamomum camphora (L.) J.Presl essential oil in vitro and in vivo

Ethnopharmacological relevanceBorneol was widely used in traditional Chinese medicine formulas due to its pharmacological activities, e.g. sedative, anti-inflammatory, and anti-ischemic properties. Cinnamomum camphora (L.) J.Presl essential oil (BEO) is a by-product of natural crystalline borneol (NCB) production obtained by steam distillation of Cinnamomum camphora (L.) J.Presl leaves, and borneol was the main component of BEO. This study aims to investigate the anti-inflammatory effect of BEO and its corresponding mechanisms through in vitro and in vivo studies. Materials and methodsHuman erythrocyte membrane stability assay and the acute inflammation murine model (xylene-induced ear edema) were chosen to evaluate the anti-inflammatory effect of BEO. Expression of inflammatory mediators, including interleukin (IL)-1β, IL-6, and tumor necrosis factor α (TNF-α) was determined by real-time quantitative polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assays (ELISA). The functional compounds in the BEO were identified by using gas chromatography-mass spectrometry (GC-MS). The steady-state transdermal diffusion rates of BEO and BEO nano-emulsion with were also determined in this study. Cytotoxicity of BEO was analyzed by cell counting kit-8 (CCK-8) assay. ResultsThe BEO showed a high human erythrocyte membrane stabilization by inhibiting heat-induced hemolysis (IC50 = 5.29 mg/mL) and hypotonic solution-induced hemolysis (IC50 = 0.26 mg/mL) in vitro. The BEO was topically applied to mice auricles, both single and repeated administration significantly reduced xylene-induced auricle swelling (p < 0.0001). Expression of inflammatory mediators, including interleukin (IL)-1β, IL-6, and tumor necrosis factor α (TNF-α) in serum and tissue was significantly downregulated (p < 0.05), so as to the mRNA expression of IL-1β (p＜0.05) and TNF-α (p < 0.001). A total of 43 components were identified and quantified by GC-MS. The most abundant was borneol [178.3 mg/mL, 20.9% (m/v)], followed by β-caryophyllene (116.3 mg/mL), camphor (115.2 mg/mL), and limonene (89.4 mg/mL). For determining the skin permeability of BEO, the steady-state transdermal diffusion rates of BEO and BEO nano-emulsion were determined to be 6.7 and 8.9 mg/cm2·h, respectively. ConclusionIt is suspected that the anti-inflammatory effects in vivo and in vitro were derived from the above-mentioned components in the BEO. These findings will facilitate the development of BEO as a new and natural therapeutic agent for inflammatory skin conditions.

Engineering EHD1-Targeted Natural Borneol Nanoemulsion Potentiates Therapeutic Efficacy of Gefitinib against Nonsmall Lung Cancer

Despite the effective targeting of the epidermal growth factor receptor (EGFR), the use of gefitinib (GFT) for nonsmall cell lung cancer (NSCLC) treatment meets a failure because of the insufficient drug accumulation in the tumor region. Therefore, developing chemosensitizers of GFT with synergistic therapeutic effects is urgently needed for advanced cancer therapy. Herein, a natural chemosensitizer, natural borneol (NB), is reformulated as an oil-in-water nanoemulsion to enhance its solubility, distribution, and to ultimately increase the therapeutic index with GFT. The nanolization of NB (NBNPs) displays stronger targeted delivery and cytotoxicity than NB by selectively identifying eight specific protein targets in A549 NSCLC cells as revealed by the proteomic studies. Consistently, NBNPs realize stronger chemosensitization effects than NB with GFT by effectively regulating EGFR/EHD1-mediated apoptosis in A549 NSCLC cells. Owing to the satisfying synergistic effect between NBNPs and GFT, the combined therapy not only enhances the anticancer ability of GFT against NSCLC proliferation but also avoids heavy double toxicity in vivo. This finding demonstrates the effective synergism between NBNPs and GFT with clear mechanistic investigation and is expected to extend the application of NBNPs as a novel chemosensitizer for advanced cancer chemotherapy.

Biocides: Durable Antibacterial Cotton Fabrics Based on Natural Borneol‐Derived Anti‐MRSA Agents (Adv. Healthcare Mater. 11/2020)

In article number 202000186 by Liangzhi Hong, Jianyu Su and coworkers, a water-soluble antibacterial agent is developed by integrating membrane-active natural borneol with a hydrophilic PDMAEMA chain. Cotton fabrics with sustained antibacterial activity can be fabricated by grafting the borneol-based antibacterial agents on the surface.