Concentrations Of Borneol Research Articles

Borneol essential oil: Enzyme-assisted extraction, inhibitory effect on Propionibacterium acnes, and study on acne treatment mechanism based on network pharmacology-molecular docking

Borneol essential oil (BEO), a plant essential oil derived from hydrodistillation of fresh branches and leaves of Cinnamomum camphora (L.). This study optimized cellulase and xylanase-assisted BEO, extraction using an orthogonal design. Additionally, it explored the inhibitory effects of BEO on Propionibacterium acnes and elucidated the anti-bacterial mechanisms via molecular docking. Furthermore, the acne treatment mechanism of BEO was investigated using network pharmacology-molecular docking. The findings indicated that the concentration of borneol in BEO was 2.34 times higher than that achieved through hydrodistillation. This enhancement was achieved by adding enzymes in a volume equivalent to 2 % of the raw material, followed by a 2-hour enzymolysis process conducted at 40℃. BEO exhibited a significant inhibition zone of 31.6±0.5 mm against Propionibacterium acnes. Molecular docking analysis revealed that six, three, and one chemical components in BEO exhibited molecular binding energies exceeding 5.00 kJ/mol with key target proteins involved in the pathogenesis of Propionibacterium acnes: deoxyribonuclease I (DNase I), dermatan sulfate (DsA1), and Christie, Atkins, Munch-Peterson (CAMP), respectively. This indicates a close relationship between the chemical components and the target proteins. Network pharmacology analysis identified 40 common targets between BEO and acne formation, from which 12 key targets were identified. Among these, ovarian steroidogenesis exhibited the highest degree of enrichment in the signaling pathway. These findings provide a scientific foundation for the development of acne treatment cosmetics utilizing BEO.

Chemical Composition of Essential Oil from Fresh Salvia Rosmarinus from Jordan at Different Drying Methods

The composition of essential oil is affected by different drying methods. The present study aimed to evaluate the effect of drying methods (shade-drying (SD), oven-drying(OD), and freeze-drying (FD)) on the essential oils composition of Salvia rosmarinusat. The extracted S. rosmarinusessential oil samples subjected to different drying methods were extracted by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC-MS). Eighty-three compounds were tentatively identified, with 1,8-cineole, ?-pinene, ?-fenchene, and bornyl being the major components. The shade-dried method best maintained the composition of rosemary essential oil and showed the best retention of ?-Pinene, 1,8-Cineole, the most important compounds, as well as ?-terpineol and safranal. The oven-dried method displayed the worst results, with a significant loss of 37 compounds. However, oven-drying produces a significant increase in the concentrations of borneol, iso-menthol, ?-terpineol, camphor, and bornyl acetate.

USING ACTIVE CARBONS TO DEODORIZE FLORENTINE WATER

The presence of biologically active substances (BAS) in the composition of fir hydrolate allows the use of this waste from essential oil production in the manufacture of functional food products. However, the specific taste and aroma of the hydrolate limits its use without prior preparation in the production, in particular of beverages. The purpose of the work is to study the possibility of using carbon-containing sorbents to extract compounds that negatively affect the organoleptic properties of fir hydrolate without a significant change in biologically active substances. The object of study is fir hydrolat (florentine water), obtained in the process of fir oil production by steam distillation. Activated carbons of BAU-A and ABG grades acted as adsorbents. The effect of hydrolate treatment with sorbents (static and dynamic methods) was assessed by changing the composition of the hexane extract of the hydrolate by gas-liquid chromato-mass spectrometry (Agilent 6890N chromatograph), as well as organoleptically. The main components of the original hydrolate are borneol and bornyl acetate. When using the infusion method (static method), the taste and aroma of the hydrolate are optimized only after 3 and 8 hours of contact with BAU-A and ABG coals, respectively, at a dose of 10–12 g/100 cm3, however, the concentration of borneol in comparison with the initial value decreases by 4 times (coal BAU-A). Treatment of hydrolate by filtration (dynamic method) through a layer of adsorbent at a rate of 0.3–1.2 dm3/h significantly reduces the severity of organoleptic characteristics. At the same time, the use of coal of the ABG grade contributes to an increase in the amount of borneol by 15%, of the BAU-A grade by 50% in relation to the initial value. The observed changes are due both to the properties of the adsorbents used and to multiple processes (redox, catalytic) occurring on the surface of the coals. The results obtained allow us to speak about the fundamental possibility of using activated carbons for the treatment of fir hydrolates to extract compounds that worsen the taste and aroma characteristics, while maintaining the main biologically valuable components. The work needs to be continued in the direction of searching for new sorbents and optimizing processing conditions.

Borneol-based antisolvent-induced in situ forming matrix for crevicular pocket delivery of vancomycin hydrochloride

Given its safety and apparent low aqueous solubility, borneol may serve as a matrix forming component of anti-solvent based in situ forming matrixes (ISMs) for crevicular pocket targeting. Drug-free and vancomycin hydrochloride-loaded borneol ISMs were evaluated for pH, density, viscosity, contact angle, surface tension, matrix formation, drug release behavior, in vitro degradability and antimicrobial activities. Density and pH values of borneol-based ISMs decreased with increasing borneol concentration. Given their markedly low viscosity could facilitate better injectability. The contact angles of the drug-free and vancomycin HCl-loaded borneol ISMs increased after being in contact with the agarose gel or the bulge tissue of porcine due to phase inversion. A dense borneol crystal matrix formed after using the highly concentrated ISM corresponded to fast matrix formation. The borneol-based ISM exhibited a sustainable drug release longer than 14 days with a diffusion-controlled release mechanism. Moreover, the developed ISM exhibited strong antimicrobial activities against various microbes. Thus, the vancomycin HCl-loaded borneol-based ISM is a potentially effective local anti-solvent-based ISM for periodontitis treatment via crevicular pocket injection.

Surface Tension/Contact Angle Characters of Aprotic Binary Borneol-Dimethyl Sulphoxide Mixture

Borneol and dimethyl sulphoxide (DMSO) have been used as the skin penetration enhancers. Different concentrated borneol solutions in aprotic DMSO were prepared as the binary mixtures and determined their surface tension and contact angle behaviors using goniometer. Low borneol concentration minimized the surface tension and there was nearly stable contact angle for 30-70% borneol solutions. The trend contact angle value was decreased on glass slide, acrylic and LDPE whereas increasing on agarose gel and porcine tissues including buccal mucosa, gum and tongue with borneol concentration dependence. However, the borneol-DMSO binary mixture exhibited high wettability owing to its contact angle on glass surface was less than 90°. The solvent exchange between DMSO of borneol solutions and aqueous phase form agarose gel and porcine tissues including tongue, gum and buccal mucosa initiated the phase transformation from solution into matrix-like and promoted the higher contact angle with borneol concentration dependence. The understanding of surface tension and contact angle behaviors of aprotic borneol-DMSO binary mixture is useful for developing them into in situ forming gel for drug delivery such as in the oral cavity.

Borneol promotes apoptosis of Human Glioma Cells through regulating HIF-1a expression via mTORC1/eIF4E pathway.

The main reason for the failure of malignant glioma treatment is local tumor recurrence. Tumor cells in hypoxic microenvironment activate HIF-1 α transcription, and thus promoting tumor invasion and metastasis is one of the important reasons. In our previous study, we clearly established that borneol opens the blood-brain tumor barrier and its related mechanism. However, the effects of borneol itself on glioma proliferation have not yet been elucidated. Therefore, in this study, we evaluated the effect of borneol on glioma by constructing in vivo SD rat brain glioma model and in vitro human primary cultured glioma cell model. We found that borneol could suppress the proliferation of primary glioma cells and the tumor volume of SD rat brain glioma. Further, we measured the apoptosis effect induced by borneol in human primary cultured glioma cells. The results showed that the higher the concentration of borneol, the higher the apoptosis rate of human primary cultured glioma cells, but the effect was reversed after transfection of HIF-1 overexpression plasmid; In addition, borneol could downregulate the expression of Bcl-2 and upregulation the expression of Bax and caspase-3, similarly, the effect was also reversed after transfection of HIF-1 overexpression plasmid, suggesting that the apoptosis effect induced by borneol in human primary cultured glioma cells is mediated via HIF-1α. Moreover, the bioinformatics analysis of correlation between HIF-1α and apoptosis-related factors based on CGGA database showed that there was a positive correlation between the expression of eIF4E and HIF-1 α (P < 0.05), and in patients with high expression of eIF4E and HIF-1α had poor survival and prognosis (P<0.001). It was further discovered that in the human primary cultured glioma cells borneol regulated HIF-1a expression via mTORC1/eIF4E pathway. In conclusion, the findings of the present study suggest that HIF-1α may be a key factor in borneol induced apoptosis of glioma cells, and mTORC1 / eIF4E pathway is involved in the HIF-1α regulation by borneol in malignant glioma. Our results not only reveal the target and molecular mechanism and action of borneol leading to promote apoptosis in glioma cells, but also provide experimental basis and theoretical support for the clinical application of borneol.

Borneol and poly (ethylene glycol) dual modified BSA nanoparticles as an itraconazole vehicle for brain targeting

Itraconazole (ITZ) can be used for the treatment of cryptococcus neoformans meningitis and aspergillus brain abscess. While, the inherent hydrophobicity of ITZ and the existence of blood brain barrier (BBB) limit its applications as a central nervous system drug. In this study, a novel brain targeting drug delivery system based on bovine serum albumin (BSA) was constructed for enhancing ITZ distribution in brain. Firstly, ITZ was loaded into BSA nanoparticles (ITZ-NPs) with 11.6% of drug loading. Subsequently, the nanoparticles were modified with borneol (BO) and polyethylene glycol (PEG) (PEG/BO-ITZ-NPs). The resulting nanoparticles retained their nanosize (186.3nm), uniform and spherical morphology, and negative surface charge (-21.03mV). Cell uptake studies showed that compared with ITZ-NPs, PEG/BO-ITZ-NPs had significantly increased uptake in bEnd.3 cells, and the increase in BO concentration was beneficial for the cellular uptake of NPs. Moreover, PEG/BO-ITZ-NPs displayed an approximately 3.5-fold higher area under the curve in rats and about 2-fold higher brain distribution in mice than that of Sporanox®, i.e. ITZ solubilized by hydroxylpropyl-β-cyclodetrin, after i.v. administration. In a word, BO and PEG dual modified BSA nanoparticles may potentially serve as an ITZ vehicle for brain targeting.

Improved Oral Absorption of Poorly Soluble Curcumin via the Concomitant Use of Borneol.

In this study, borneol, a natural active compound was applied to improve the bioavailability of curcumin (CUR). In order to increase CUR solubility and dissolution, solid dispersions (SDs) were prepared with the matrix of polyvinylpyrrolidone (PVP) at various ratios by solvent evaporation method. CUR was evidenced to exist as amorphous state in solid dispersion by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Fourier-transform infrared spectroscopy (FT-IR) was utilized to confirm intermolecular hydrogen bonding. The SD at the ratio of 1:3 (CUR:PVP) exhibited the optimal solubility and dissolution rate in various media. The results of ex vivo permeability studies by everted gut sac method showed that the apparent permeability coefficients (Papp) of CUR in SD across the duodenum, jejunum, and ileum had been significantly improved by co-incubation of borneol, and the improvement degree relied on the concentration of borneol. The pharmacokinetic results in rats indicated that the AUC0-t of CUR-SD (40mg/kg) co-administration of borneol (90mg/kg) were 2.53-fold higher than CUR-SD alone, and 19.41-fold higher than pure CUR (200mg/kg) with borneol (90mg/kg). Therefore, the combination of borneol and solid dispersion strategy provide a potential approach to enhance the oral bioavailability of CUR.

Enhancing both oral bioavailability and brain penetration of puerarin using borneol in combination with preparation technologies

Now there are few good oral preparations of puerarin used in cerebrovascular diseases because of its poor oral absorption caused by the low water solubility and the poor penetration into brain. In this study, three oral formulations of puerarin, nanocrystals suspension (NCS), inclusion compounds solution (ICS) and self-microemulsifying drug delivery system (SMEDDS) were prepared with borneol as an oral brain-targeting enhancer. A rat syngeneic in vitro model of the brain–blood barrier (BBB) was established to investigate effects of borneol on the permeability of puerarin across the BBB. The pharmacokinetics of puerarin in mice after oral administration was investigated by a high performance liquid chromatography-mass spectrometry/mass spectrometry (HPLC-MS/MS) method. The in vitro BBB model study showed the permeability of puerarin was increased significantly (p < 0.05) and the value of transepithelial electrical resistance at 2 h was decreased significantly (p < 0.01) when the concentration of borneol was over 12.5 μg/mL compared with the control group. The pharmacokinetics results indicated borneol with doses of over 50 mg/kg could obviously increase both intestinal absorption and brain penetration of puerarin. With co-administration of borneol (100 mg/kg), the AUC of puerarin both in plasma (AUCplasma) and in brain (AUCbrain) for SMEDDS were significantly higher than those for NCS (p < 0.01) and ICS (p < 0.05). These results suggested borneol in combination with SMEDDS could improve both the oral absorption and the brain penetration of puerarin in mice, which was promising for the development of an oral formulation of puerarin used in cerebrovascular diseases.

Borneol promotes oral absorption and penetration into brain of puerarin and catalpol

To investigate the effect of borneol on the oral absorption and penetration into brain of puerarin and catalpol from cell level and animal level, and screen the concentration of borneol that is suitable for Zige compound oral preparation. Blood-brain barrier(BBB) model was established by co-culture of primary brain microvessel endothelial cells(BMEC) and astrocytes(As) in rats, and it was used to investigate the effect of borneol(concentration from 6.25 to 100 mg•L⁻¹) on the transport of puerarin and catalpol. The pharmacokinetics of puerarin and catalpol in plasma and brain of rats were compared after intragastric administration of borneol solution (0, 25, 50 and 100 mg•kg⁻¹) immediately followed by puerarin(200 mg•kg⁻¹) and catalpol(45 mg•kg⁻¹) nanocrystal suspension. Barrier function was basically formed after co-culturing of brain microvascular endothelial cells and astrocytes for 7 d. The permeability of puerarin and catalpol across blood-brain barrier was increased significantly(P<0.05) and transendothelial electrical resistance(TEER) values at 2 h were decreased significantly(P<0.01) when the concentration of borneol was between 12.5 to 100 mg•L⁻¹ as compared with the control group. Borneol at the dose of 50 mg•kg⁻¹ and 100 mg•kg⁻¹ could significantly increase the oral absorption of puerarin(P<0.05), but there was no obvious effect for catalpol. AUCbrain/AUCblood for puerarin was highest with borneol at dose of 100 mg•kg⁻¹ (P<0.05), while AUCbrain/AUCblood for catalpol was highest with borneol at dose of 50 mg•kg⁻¹ (P<0.05). AUCbrain was highest at 100 mg•kg⁻¹ for puerarin(P<0.05); while for catapol, it was highest at 50 mg•kg⁻¹, but it was not significantly different from 100 mg•kg⁻¹. In conclusion, borneol could increase the amount of puerarin and catalpol in brain after oral administration and the optimized dose shall be 100 mg•kg⁻¹.

Determination of borneol in Fufang Danshen intestinal adhesion pellets and study its in vitro dissolution in different dosage form

The borneol was included with β-CD and prepared Fufang Danshen intestinal adhesion pellets. GC method for determination of borneol in Fufang Danshen intestinal adhesion pellets was established to study its in vitro dissolution and make a comparison with the Fufang Danshen tablet, in this way, the rationality of dosage form was evaluated. The first method of dissolution determination was used for determining the in vitro dissolution of borneol in Fufang Danshen intestinal adhesion pellets in artificial intestinal juice, and Fufang Danshen tablet in artificial gastric juice and intestinal juice, respectively. Result shows: the concentration of borneol in Fufang Danshen intestinal adhesion pellets and Fufang Danshen tablet was 0.79% and 0.80%, respectively. Its in vitro dissolution was nearly 70% within 12 h in Fufang Danshen intestinal adhesion pellets, and in Fufang Danshen tablet, the dissolution was about 60% within 20 min and more than 90% within 40 min, and in artificial gastric juice, was less than 20% within 40 min but more than 80% till 150 min. Research suggests that in comparison with Fufang Danshen tablet, in vitro dissolution of borneol in the Fufang Danshen intestinal adhesion pellets showed an obvious sustained release behavior. The borneol in Fufang Danshen intestinal adhesion pellets was included with β-CD and prepared enteric preparations. To some extent, the stimulation on stomach and intestinal mucosa can be reduced and safety can be improved.

Interactions of borneol with DPPC phospholipid membranes: a molecular dynamics simulation study.

Borneol, known as a “guide” drug in traditional Chinese medicine, is widely used as a natural penetration enhancer in modern clinical applications. Despite a large number of experimental studies on borneol’s penetration enhancing effect, the molecular basis of its action on bio-membranes is still unclear. We carried out a series of coarse-grained molecular dynamics simulations with the borneol concentration ranging from 3.31% to 54.59% (v/v, lipid-free basis) to study the interactions of borneol with aDPPC(1,2-dipalmitoylsn-glycero-3-phosphatidylcholine) bilayer membrane, and the temperature effects were also considered. At concentrations below 21.89%, borneol’s presence only caused DPPC bilayer thinning and an increase in fluidity; A rise in temperature could promote the diffusing progress of borneol. When the concentration was 21.89% or above, inverted micelle-like structures were formed within the bilayer interior, which led to increased bilayer thickness, and an optimum temperature was found for the interaction of borneol with the DPPC bilayer membrane. These findings revealed that the choice of optimal concentration and temperature is critical for a given application in which borneol is used as a penetration enhancer. Our results not only clarify some molecular basis for borneol’s penetration enhancing effects, but also provide some guidance for the development and applications of new preparations containing borneol.

Enhancing effect of borneol and muscone on geniposide transport across the human nasal epithelial cell monolayer.

Geniposide is widely used in the treatment of cerebral ischemic stroke and cerebrovascular diseases for its anti-thrombotic and anti-inflammatory effects. Recent studies demonstrated that geniposide could be absorbed promptly and thoroughly by intranasal administration in mice and basically transported into the brain. Here, we explored its transport mechanism and the effect of borneol and muscone on its transport by human nasal epithelial cell (HNEC) monolayer. The cytotoxicity of geniposide, borneol, muscone and their combinations on HNECs was evaluated by the MTT assay. Transcellular transport of geniposide and the influence of borneol and muscone were studied using the HNEC monolayer. Immunostaining and transepithelial electrical resistance were measured to assess the integrity of the monolayer. The membrane fluidity of HNEC was evaluated by fluorescence recovery after photobleaching. Geniposide showed relatively poor absorption in the HNEC monolayer and it was not a P-gp substrate. Geniposide transport in both directions significantly increased when co-administrated with increasing concentrations of borneol and muscone. The enhancing effect of borneol and muscone on geniposide transport across the HNEC may be attributed to the significant enhancement on cell membrane fluidity, disassembly effect on tight junction integrity and the process was reversible. These results indicated that intranasal administration has good potential to treat cerebrovascular diseases.

Distillation Time Effect on Essential Oil Yield, Composition, and Antioxidant Capacity of Sweet Sagewort (Artemisia annua L.) Oil

Sweet sagewort, also known as sweet wormwood (Artemisia annua L.), contains essential oil and other natural products. The objective of this study was to evaluate the effect of eight different distillation times (DTs; 1.25 minutes, 2.5 minutes, 5 minutes, 10 minutes, 20 minutes, 40 minutes, 80 minutes, and 160 minutes) on A. annua essential oil and its antioxidant capacity. Highest essential oil yield was achieved at 160-minute DT. The concentration of camphor (8.7% to 50% in the oil) was highest at the shorter DT and reached a minimum at 160-minute DT. The concentration of borneol showed a similar trend as the concentration of camphor. The concentrations of some constituents in the oil were highest at 2.5-minute DT (alpha-pinene and camphene), at 10 minutes (paracymene), at 20 minutes (beta-chamigrene and gamma-himachalene), at 80 minutes [transmuurola-4(15),5-diene and spathulenol], at 80- to 160-minute DT (caryophylene oxide and cis-cadin-4-en-ol), or at 160-minute DT (beta-caryophyllene, transbeta-farnesene, and germacrene-D). The yield of individual constituents reached maximum at 20- to 160-minute DT (camphor) at 80- to 160-minute DT [paracymene, borneol, transmuurola-4(15),5-diene, and spathulenol], or at 160-minute DT (for the rest of the oil constituents). DT can be used to attain A. annua essential oil with differential and possibly targeted specific chemical profile. The highest antioxidant capacity of the oil was obtained at 20-minute DT and the lowest from the oil in the 5-minute DT. This study suggests that literature reports on essential oil content and composition of A. annua could be compared only if the essential oil was extracted at similar DTs. Therefore, DT must be reported when reporting data on essential oil content and composition of A. annua.

Influence of borneol and muscone on geniposide transport through MDCK and MDCK-MDR1 cells as blood–brain barrier in vitro model

The objective of this study was (1) to characterize geniposide transport through MDCK and MDCK-MDR1 cell lines to confirm its transport mechanism and (2) to evaluate the effect of borneol and muscone as enhancers of geniposide transport in the BBB models so as to explore the enhancement mechanism. Transport studies of geniposide were performed in both directions, from apical to basolateral and from basolateral to apical sides. Drug concentrations were analyzed by HPLC. Geniposide showed relatively poor absorption in MDCK and MDCK-MDR1 cells, apparent permeability coefficients ranging from 0.323×10(-6) to 0.422×10(-6) cm/s. The in vitro experiments showed that geniposide transport in both directions was not concentration dependent and saturable, indicating purely passive diffusion. The efflux ratio of geniposide was less than 2 in the two cell models, which suggested that geniposide was not P-gp substrates. Geniposide transport in both directions significantly increased when co-administrated with increasing concentrations of borneol and muscone. Actin staining results indicated that borneol and muscone increased geniposide transport in the BBB models may attribute to disassembly effect on tight junction integrity.

Study on tissue distribution of borneol in mice by intravenous and intranasal administrations

To develop a GC-FID method to determine borneol's concentration in mouse tissues, and to investigate the tissue distribution after intravenous and intranasal administrations of borneol. Mouse brains, hearts, livers, spleens, lungs and kidneys were collected at 1, 3, 5, 10, 20, 30, 60, 90, 120 min after administration of borneol with the dose of 30.0 mg x kg(-1). The drug in tissues was extracted with ethyl acetate, and borneol's concentration detected by GC, with octadecane as the internal standard. The calibration curve showed a good linear relationship. Extraction recoveries, inter-day and intra-day precisions and stability were in conformity with the analytical requirements of biological samples. Borneol was mainly distributed in most tissues, more in heart, brain and kidney, and less in liver, spleen and lung. The established GC-FID method is applicable for content determination of borneol in tissues. After intravenous and intranasal administrations in mice, borneol is mainly distributed in abundant blood-supply tissues. After intranasal administration, brain tissues showed the highest target coefficient and target effectiveness.

Study on pharmacokinetics of borneol in rats injected with novel-Xingnaojing by GC-FID

To develop a GC-FID method for the determination of borneol concentration in rat plasma and to investigate the pharmacokinetics after injection of novel-Xingnaojing. Novel-Xingnaojing was injected via by caudal vein injection. The blood samples were collected by posterior orbital venous plexus approach at 0.5, 1, 3, 5, 8, 12, 20, 30, 45 min. The drug in plasma was extracted with ethyl acetate and then detected by GC-FID, octadecane was used as the internal standard. The pharmacokinetic parameters were calculated by the software of Kinetica. The calibration curve was good linear in the range of 1.67-16.67 mg x L(-1). The extraction recoveries of low, medium and high concentration were (92.81 +/- 1.11)%, (85.38 +/- 0.86)% and (84.58 +/- 0.58)%, respectivley. And the RSDs of within-day and between-day were below 3.00%. Plasma concentration of borneol was consistent with the two-compartment open model. The pharmacokinetic parameters were that the t1/2alpha was (1.18 +/- 0.20) min, the t1/2beta was (22.27 +/- 6.85) min, the C(max)(Calc) was (18.76 +/- 2.10) mg x L(-1), the MRT was (23.84 +/- 7.67) min(-1), and the AUC was (100.00 +/- 15.85) mg x min x L(-1). The GC-FID method developed can be applied to determination and pharmacokinetics. The borneol in novel-Xingnaojing is distributed and metabolized fast after being administrated.

Effects of borneol on the intestinal transport and absorption of two P-glycoprotein substrates in rats

As the most prevalent route of delivery, oral administration has the challenge of potentially low bioavailability in part because P-glycoprotein (P-gp) in the intestinal tract affects absorption. Therefore, absorption enhancers or P-gp inhibitors are strategies to solve this problem. The aim of the present study was to investigate the effects of borneol on transportation of colchicine and rhodamine123, two P-gp substrates, in rats. In vitro transportation was assessed with a diffusion chamber system with isolated rat intestines. Different concentrations of borneol (10, 40 and 80 μg/mL) were prepared in solutions with two P-gp substrates compared with blank solutions. The in vivo effects on colchicine were assessed by a pharmacokinetic study. Borneol enhanced the absorptive transport of two P-gp substrates, which was relevant to the concentration. A pharmacokinetic study showed that in the presence of borneol, a significant increase in C(max) and AUC(0→8) of colchicine occurred when compared to colchicine alone. The study showed that borneol affected two P-gp substrates in the intestine, possibly by inhibiting the effects of P-gp and enhancing intestinal absorption of drugs. Therefore, borneol could be developed as a P-gp inhibitor and absorptive enhancer.

Volatile flavor composition of gamguk (Chrysanthemum indicum) flower essential oils

The volatile composition of the essential oil from fresh gamguk (Chrysanthemum indicum) flowers was investigated. The volatile constituents were extracted by the hydro distillation method. Volatile compositional changes of gamguk prepared via different drying methods (shade- and freeze-drying methods) were also determined. Total 36, 63, and 55 volatiles constituents were confirmed in the essential oil from fresh and shade-, and freeze-dried flowers. Ketones were predominant in the volatiles of gamguk flowers (%): fresh, 43.8; shade dried, 30.3; and freeze dried, 36.1. Camphor was the most abundant volatile component in all samples, and the content of borneol was also remarkable. The content of camphor was higher in fresh sample than those of dried samples while borneol concentration was significantly increased in the dried samples.

Effects of borneol on the level of DNA damage induced in primary rat hepatocytes and testicular cells by hydrogen peroxide

The aim of this paper was to evaluate genotoxic effects of borneol and its ability to change DNA-damaging effects of H2O2 in rat hepatocytes and testicular cells. Both in vitro and ex vivo approaches were used in the case of hepatocytes. Testicular cells were tested only ex vivo, i.e. shortly after isolation from rats supplemented by borneol. Cytotoxicity of borneol increased in in vitro conditions in a concentration-dependent manner and it was associated with DNA-damaging effects at toxic concentrations. While non-toxic concentrations of borneol applied in vitro protected cells against H2O2-induced DNA damage and interfered only partly with rejoining of H2O2-induced DNA strand breaks, cytotoxic concentrations of borneol manifested synergy with H2O2, i.e. enhanced DNA-damaging effects of H2O2. On the other side, borneol given to rats in drinking water decreased the level of DNA damage induced by H2O2 in both hepatocytes and testicular cells. Our results show that though at higher concentrations (2-h treatment with >2mM borneol >0.3084mg/ml) borneol acts cytotoxically and genotoxically on primary hepatocytes cultured in vitro, if given to rats during 7 days in a daily concentration of 17.14 or 34.28mg/kg it reduces genotoxicity of H2O2 in both hepatocytes and testicular cells.