Research progress of natural borneol resources / 中国中药杂志

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.

Dynamic changes of the main active constituents in valerian rhizome and root (Valeriana amurensis Smir. ex Kom.) during different harvest periods / Cambios dinámicos de los principales constituyentes activos del rizoma y raíz valeriana (Valeriana amurensis Smir. Ex Kom.) durante diferentes períodos de cosecha

Valeriana amurensis Smir. ex Kom. widely distributed in the northeast region of China and some region in Russia and Korea, and its underground parts (roots and rhizomes) being used to cure nervous system diseases such as insomnia. The active components including the essential oil and iridoids of underground parts were investigated in different harvest periods in order to evaluate the quality for the roots and rhizomes of V. amurensis. The content of the essential oil was obtained by hydrodistillation and bornyl acetate in the oil was quantitated by GC-EI. The iridoids, valepotriates were determined by potentiometric titration and the main component, valtrate was quantitated by HPLC-UV. The factors of biomass were considered in the determination of collection period. Statistical analysis of results showed that, the highest content of the essential oil per plant was 22.69 µl in withering period and then 21.58 µl in fruit ripening period, while the highest contents of bornyl acetate, valepotriates and valtrate per plant were 2.82 mg, 31.90 mg and 0.98 mg in fruit ripening period separately. Fruit ripening period was decided as the best harvest period for the content of active constituents and output of drug, and it would provide scientific basis for the artificial cultivation of V. amurensis.

Valeriana amurensis Smir. ex Kom. Se distribuye ampliamente en la región noreste de China y en algunas regiones de Rusia y Corea, y sus partes subterráneas (raíces y rizomas) se utilizan para curar enfermedades del sistema nervioso como el insomnio. Se investigaron los componentes activos, incluidos el aceite esencial y los iridoides de las partes subterráneas de V. amurensis en diferentes períodos de cosecha para evaluar la calidad de las raíces y rizomas. El contenido del aceite esencial se obtuvo mediante hidrodestilación y el acetato de bornilo en el aceite se cuantificó por GC-EI. Los iridoides, valepotriatos se determinaron mediante valoración potenciométrica y el componente principal, el valtrato se cuantificó por HPLC-UV. Los factores de biomasa fueron considerados en la determinación del período de recolección. El análisis estadístico de los resultados mostró que el mayor contenido de aceite esencial por planta fue de 22,69 µl en el período de marchitación y luego de 21,58 µl en el período de maduración de la fruta, mientras que el mayor contenido de acetato de bornilo, valepotriatos y valtrato por planta fue de 2.82 mg, 31.90 mg y 0,98 mg, respectivamente, en el período de maduración de la fruta por separado. Se definió el período de maduración de la fruta como el mejor período de cosecha para el contenido de constituyentes activos y la producción de droga, lo cual proporcionaría una base científica para el cultivo artificial de V. amurensis.

Screening and analysis of key active constituents in Guanxinshutong capsule using mass spectrum and integrative network pharmacology / 中国天然药物

Guanxinshutong capsule (GXSTC) is an effective and safe traditional Chinese medicine used in the treatment of cardiovascular diseases (CVDs) for many years. However, the targets of this herbal formula and the underlying molecular mechanisms of action involved in the treatment of CVDs are still unclear. In the present study, we used a systems pharmacology approach to identify the active ingredients of GXSTC and their corresponding targets in the calcium signaling pathway with respect to the treatment of CVDs. This method integrated chromatographic techniques, prediction of absorption, distribution, metabolism, and excretion, analysis using Kyoto Encyclopedia of Genes and Genomes, network construction, and pharmacological experiments. 12 active compounds and 33 targets were found to have a role in the treatment of CVDs, and four main active ingredients, including protocatechuic acid, cryptotanshinone, eugenol, and borneol were selected to verify the effect of (GXSTC) on calcium signaling system in cardiomyocyte injury induced by hypoxia and reoxygenation. The results from the present study revealed the active components and targets of GXSTC in the treatment of CVDs, providing a new perspective to enhance the understanding of the role of the calcium signaling pathway in the therapeutic effect of GXSTC.

Screening and analysis of key active constituents in Guanxinshutong capsule using mass spectrum and integrative network pharmacology / 中国天然药物

Guanxinshutong capsule (GXSTC) is an effective and safe traditional Chinese medicine used in the treatment of cardiovascular diseases (CVDs) for many years. However, the targets of this herbal formula and the underlying molecular mechanisms of action involved in the treatment of CVDs are still unclear. In the present study, we used a systems pharmacology approach to identify the active ingredients of GXSTC and their corresponding targets in the calcium signaling pathway with respect to the treatment of CVDs. This method integrated chromatographic techniques, prediction of absorption, distribution, metabolism, and excretion, analysis using Kyoto Encyclopedia of Genes and Genomes, network construction, and pharmacological experiments. 12 active compounds and 33 targets were found to have a role in the treatment of CVDs, and four main active ingredients, including protocatechuic acid, cryptotanshinone, eugenol, and borneol were selected to verify the effect of (GXSTC) on calcium signaling system in cardiomyocyte injury induced by hypoxia and reoxygenation. The results from the present study revealed the active components and targets of GXSTC in the treatment of CVDs, providing a new perspective to enhance the understanding of the role of the calcium signaling pathway in the therapeutic effect of GXSTC.

Effect of Borneol on the Permeability of Blood Tumor Barrier Model and its Mechanism Study / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To observe the effect of natural borneol on the permeability of blood tumor barrier (BTB) model and the expression and activation of mitogen-activated protein kinase (MAPKs) signal transduction pathway related protein kinase in vitro.</p><p><b>METHODS</b>C6 rat glioma cells and human umbilical vein endothelial cells (HUVECs) were co-cultured to establish BTB model. Then 4 groups were set up, the blank control group, low, middle, and high dose borneol groups (25, 50, 100 µg/mL), 3 samples collected at 7 time points (0, 10, 30, 60, 120, 180, 240 min, respectively). Blank culture medium was exchanged in the blank control group while medication. Different doses of natural borneol were administered to the 3 borneol groups. Cells were collected at different time points. BTB permeability was determined using horseradish peroxidase (HRP). Expression levels of extracellular signal regulated protein kinase (ERK), phosphorylation extracellular signal regulated protein kinase (P-ERK), P38MAPK, phosphor-P38MAPK, c-Jun N-terminal kinase (JNK), and phosphorylation c-Jun N-terminal kinase (P-JNK) were detected using Western blot.</p><p><b>RESULTS</b>Compared with the same group at min 0, the permeation rate obviously increased (P < 0.01) in the 3 borneol groups at the rest time points. P-ERK expression was elevated first, reached the peak at 30 min, and gradually recovered to the initial level (P > 0.05). Compared with the blank control group, HRP permeation rate increased from 10 min to 240 min (P < 0.01), and expression of P-ERK protein increased at 30 min and 60 min (P < 0.05) in the low dose borneol group; expression of P-JNK protein decreased in the 3 borneol groups at 180 min and 240 min (P < 0.05). Compared with the low dose borneol group, expression of P-ERK protein increased from 10 min to 180 min (P < 0.05), HRP permeation rate increased from 30 min to 180 min (P < 0.05), expression of P-JNK protein decreased at 180 and 240 min (P < 0.05) in the middle dose borneol group. Compared with the middle dose borneol group, HRP permeation rate increased from 10 min to 180 min (P < 0.05), expression of P-ERK protein increased from 10 min to 180 min (P < 0.05), expression of P-JNK protein increased at 180 min and decreased at 240 min (both P < 0.05) in the high dose borneol group.</p><p><b>CONCLUSION</b>Natural borneol arrived at the effect of regulating reversible BTB patency possibly through activating phosphorylation of ERK in MAPKs signal transduction pathway, and further reversibly down-regulating expression of associated proteins.</p>

Borneol is an inducer of rat hepatic CYP2D activity in vivo / 药学学报

Borneol is a traditional Chinese medicine. In the past few years, many studies showed that borneol can improve the bioavailability of other drugs, promoting drugs to cross the blood-brain barrier, so the potential drug interactions between borneol and other medicines have attracted great attention, but the influence of borneol to CYP450 and its isoforms are rarely reported. In this research, male Wistar rats were orally administered by borneol for 7 days, then the mRNA and protein expression and the activities of CYP2D were detected, we also compared the pharmacokinetic parameters of CYP2D's specific substrate between control group and borneol group. The results show that borneol (33, 100 and 300 mg x kg(-1) x d(-1)) have no significant effect on CYP2D, while the activites of CYP2D increased 1.71, 1.97 and 2.89 times comparing to the control group. At the same time, borneol (300 mg x kg(-1) x d(-1)) caused the C(max) decreased 10.6% (P > 0.05), AUC(0-∞) decreased 27.5% (P < 0.01), CL/F increased 41.1% (P < 0.01), V(z)/F increased 23.1% (P > 0.05) of dextromethorphan. Our data provided that borneol speed up dextromethorphan's elimination in vivo. Since the activity of CYP2D can be induced by borneol, the metabolic interactions might happen when borneol and the substrate drug CYP2D are used together.

Combined use of borneol or menthol with labrasol promotes penetration of baicalin through rabbit cornea in vitro

The permeability of most drugs through the eyes is very limited, so finding safe and effective penetration enhancers is of high importance in current ophthalmology research. In this paper, we use a new approach that integrates Chinese and Western medicine to improve the corneal permeability of baicalin, a water- and fat-insoluble target drug, in vitro. Rabbits were divided into three groups. The first group was dosed with borneol [0.05%, 0.1%]. menthol [0.1%, 0.2%], or Labrasol [1%, 2%] individually, the second was dosed with a combination of Labrasol with either borneol or menthol, and the third group received a control treatment. Compared with the control treatment, borneol, menthol, or Labrasol alone clearly improved the permeability of baicalin in vitro. Furthermore, the penetrating effects were significantly increased by combining the application of Labrasol with menthol or borneol. Among the various combined penetration enhancers, 0.1% borneol with 2% Labrasol achieved the best apparent permeability, approximately 16.35 times that of the control. Additionally, the calculation of corneal hydration level and the Draize test demonstrated the safety of these penetration enhancers to the rabbit corneas in vivo. This study confirms that the combined use of borneol or menthol, compounds both derived from Chinese herbs, with Labrasol can improve the corneal permeability of waterand fat-insoluble drugs

Determination of borneol in Fufang Danshen intestinal adhesion pellets and study its in vitro dissolution in different dosage form / 中国中药杂志

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.

Preparation and in vitro evaluation of borneol and folic acid co-modified doxorubicin loaded PAMAM drug delivery system / 药学学报

A novel targeting drug carrier (FA-BO-PAMAM) based on the PAMAM G5 dendrimer modified with borneol (BO) and folic acid (FA) molecules on the periphery and doxorubicin (DOX) loaded in the interior was designed and prepared to achieve the purposes of enhancing the blood-brain barrier (BBB) transportation and improving the drug accumulation in the glioma cells. 1H NMR was used to confirm the synthesis of FA-BO-PAMAM; its morphology and mean size were analyzed by dynamic light scattering (DLS) and transmission electron microscope (TEM). Based on the HBMEC and C6 cells, cytotoxicity assay, transport across the BBB, cellular uptake and anti-tumor activity in vitro were investigated to evaluate the properties of nanocarriers in vitro. The results showed that the nanocarrier of FA-BO-PAMAM was successfully synthesized, which was spherical in morphology with the average size of (22.28 ± 0.42) nm, and zeta potential of (7.6 ± 0.89) mV. Cytotoxicity and transport across the BBB assay showed that BO-modified conjugates decreased the cytotoxicity of PAMAM against both HBMEC and C6 cells and exhibited higher BBB transportation ability than BO-unmodified conjugates; moreover, modification with FA increased the total uptake of DOX by C6 cells and enhanced the cytotoxicity of DOX-polymer against C6 cells. Therefore, FA-BO-PAMAM is a promising nanodrug delivery system in employing PAMAM as a drug carrier and treatment for brain glioma.

Componentes volátiles de Eriope crassipes, Hyptis conferta, H. dilatata, H. brachiata, H. suaveolens y H. mutabilis (Lamiaceae) / Volatile compounds of analysis of Eriope crassipes, Hyptis conferta, H. dilatata, H. brachiata, H. suaveolens y H. mutabilis (Lamiaceae)

This work presents the analysis by GC-MS of volatile metabolites of six Lamiaceae from Arauca (Colombia). In stems and leaves of Eriope crassipes were determined as the most abundants: citronellic acid (53,8 percent and 66,2 percent), and methyl citronellate (15,7 percent and 14,5 percent). In the inflorescences of Hyptis conferta were identified: t-cadinol (49,4 percent), and caryophyllene oxide (13,0 percent). From leaves and flowers of Hyptis dilatata were found: delta-3-carene (11,0 percent and 0,5 por ciento), camphor (43,8 percent and 12,2 percent), bornyl acetate (3,2 percent and 25,5 percent), E-caryophyllene (12,8 percent and 22,3 percent), and palustrol (6,0 percent and 10,3 percent). In the leaves of Hyptis brachiata were recognized: E-caryophyllene (8,3 percent), alpha-humulene (19,8 percent), and germacrene D (13,0 percent). The principal compounds in leaves and flowers of Hyptis suaveolens were: alpha-phellandrene (9,4 percent and 0,4 percent), limonene (10,5 percent and 2,5 percent), 1,8-cineole (1,3 percent and 15,2 por ciento), fenchone (10,8 por ciento and tr), E-caryophyllene (26,3 por ciento and 8,0 por ciento), and germacrene D (6,7 por ciento and 14,0 por ciento). In the leaves of Hyptis mutabilis were determined: sabinene (6,6 percent) beta-elemene (6,8 percent), germacrene D (14,9 percent), beta-selinene (8,8 percent), alpha-selinene (9,1 percent), and bicyclogermacrene (6,1 percent), as the most abundants.

Este trabajo presenta el análisis por GC-MS de los metabolitos volátiles de seis Lamiaceae recolectadas en Arauca (Colombia). En tallos y hojas de Eriope crassipes se determinaron como mayoritarios: ácido citronélico (53,8 por ciento y 66,2 por ciento), y citronelato de metilo (15,7 por ciento y 14,5 por ciento). En las inflorescencias de Hyptis conferta se identificaron: t-cadinol (49,4 por ciento), y óxido de cariofileno (13,0 por ciento). En hojas y flores de Hyptis dilatata se encontraron: delta-3-careno (11,0 por ciento y 0,5 por ciento), alcanfor (43,8 por ciento y 12,2 por ciento), acetato de bornilo (3,2 por ciento y 25,5 por ciento), E-cariofileno (12,8 por ciento y 22,3 por ciento), y palustrol (6,0 por ciento y 10,3 por ciento). En las hojas de Hyptis brachiata se reconocieron: E-cariofileno (8,3 por ciento), alfa-humuleno (19,8 por ciento), y germacreno D (13,0 por ciento). Los compuestos principales en hojas y flores de Hyptis suaveolens fueron: alfa-felandreno (9,4 por ciento y 0,4 por ciento), limoneno (10,5 por ciento y 2,5 por ciento), 1,8-cineol (1,3 por ciento y 15,2 por ciento), fenchona (10,8 por ciento y tr), E-cariofileno (26,3 por ciento y 8,0 por ciento), y germacreno D (6,7 por ciento y 14,0 por ciento). En las hojas de Hyptis mutabilis se determinaron: sabineno (6,6 por ciento), beta-elemeno (6,8 por ciento), germacreno D (14,9 por ciento), beta-selineno (8,8 por ciento), alfa-selineno (9,1 por ciento), y biciclogermacreno (6,1 por ciento), como los más abundantes.

Impact of drug molecules on HP-β-CD compound inclusion / 中国中药杂志

To study the interaction of drugs of different properties, namely puerarin, borneol and catalpol in the process of in- clusion, in order to explore the inclusion regularity of multi-component and multi-property traditional Chinese medicine compound in- clusions. With HP-β-CD as the inclusion material, the freeze-drying method was used to prepare the inclusion. The inclusion between puerarin, borneol and catalpol was tested by measuring the inclusion concentration, DSC and X-ray diffraction. According to the find- ings, when insoluble drugs puerarin and borneol were included simultaneously, and puerarin was overdosed, puerarin included was almost equal to puerarin included, and borneol was not included. When puerarin was under-dosed, and HP-β-CD was overdosed, borne- ol was included, and the simultaneous inclusion was lower than the separate inclusion of borneol. When water-soluble drug catalpol was jointly included with puerarin or borneol, the simultaneous inclusion was almost the same with their separate inclusion, without charac- teristic peak of catalpol in DSC and X-ray diffraction patterns. There is a competition in the simultaneous inclusion between water-solu- ble drugs puerarin and borneol and a stronger competition in puerarin. The water-soluble drug catalpol could be included with HP-β-CD with no impact on the inclusion of puerarin or borneol.

Studies on pharmacological activity of borneol / 中国中药杂志

Borneol is a major component of many medicinal plant essential oils, as well as a popular traditional Chinese medicine. This essay collects the results of the latest domestic and foreign studies, and summarizes and analyzes its activity and reaction mechanism on analgesia, putridity elimination and flesh regeneration, and repair of damaged cells. Moreover, it proposes problems concerning borneol during medical studies, providing support for the in-depth study and exploration of efficacies of precious traditional Chinese medicines as well as the effective utilization and development of innovative medicines.

Study on tissue distribution of borneol in mice by intravenous and intranasal administrations / 中国中药杂志

<p><b>OBJECTIVE</b>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.</p><p><b>METHOD</b>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.</p><p><b>RESULT</b>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.</p><p><b>CONCLUSION</b>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.</p>

Preparation of self-microemulsion drug delivery system of the mixture of paeonol and borneol based on Xingbi Fang / 药学学报

The aim of this study is to prepare self-microemulsifying drug delivery system (SMEDDS) of the mixture of paeonol (Pae) and borneol (Bor). Solubility test, ternary phase diagrams and simplex lattice method were employed to screen and optimize the formulation of the mixture of Pae and Bor-loaded SMEDDS. After formed into microemulsions, the particle diameter (PD) was determined and a TEM was employed to observe the microemulsions' morphology. The contents of Pae and Bor were determined by gas chromatography. As a result, while ethyl oleate (EO) as the oil phase, cremophor EL35 (EL35) as surfactant and Transcutol HP (HP) as cosurfactant, the range of the microemulsion on the ternary phase diagram was larger than other combinations. And at a ratio of 20:45:35, the microemulsions' PD was about 34 nm and the polydispersity index (PI) was about 0.2. There were 16% of Pae, 2% of Bor, 16% of EO, 37% of EL35 and 29% of HP in the prepared SMEDDS. The preparation process of the Pae and Bor-loaded SMEDDS based on Xingbi Fang is simple and feasible. This study provides a reference for the researches on the related traditional Chinese medicine and the related components.

Central composite design-response surface method optimize of fang-bing nasal inhalant from components of traditional Chinese medicine for sedative and sleep aiding / 药学学报

To obtain the optimal preparation technology of Fang-bing nasal inhalant from components of traditional Chinese medicine by central composite design, with an apparatus containing nasal inhalant that simulated the expiration and inspiration of nose, the dissolution in vitro of different optimized inhalant samples designed through central composite design were investigated. The accumulative release of linalool, borneol, menthol was detected with GC. Response surface methodology was used to optimize the conditions of preparation technology by establishing multiple linear regression and second-order quadratic models. Then, deviation was carried out through comparing the observed and predicted values. It was showed that the coefficient of correlation of second-order quadratic model was high. The related coefficient reached 0.999 3, 0.998 0, 0.944 9, separately. The optimum conditions of preparation technology were as following: 84.39% of alcohol concentration, the weight of starch 1.45 g and the weight of carmellose sodium (CMC-Na for short) 1.22 g. The deviations between observed and predicated values showed -0.36%, 1.52%, 2.40%, separately. In this experiment, the established model can describe the good relation between factors and indexes from preparation technology of Fang-bing nasal inhalant and the outcome of prediction is well. This optimal Fang-bing nasal inhalant was used to study its in vivo effect on model rats deprived from sleep and showed sedative and sleep aiding, which will bring an instruction on inhalants of components from traditional Chinese medicine.

Comparative pharmacokinetic studies of borneol in brain and plasma of stroke or sham-operated rats after administration of Xingnaojing / 中国中药杂志

In order to research the pharmacokinetic characteristic of borneol in plasma and brain of stroke rats given XNJ and investigate the influence of stroke on the borneol passing through the blood-brain barrier, this study established the GC to determine the borneol in brain and blood, and made the stroke mode rats by middle carotid artery occlusion (MCAO) and set sham-operated group. After oral administration of Xingnaojing (XNJ) suspension, their blood and brain were collected at different time and detected by GC. The data was analysed by Kinetica. Results showed that in stroke group, the Cmax and AUC0-t of brain and plasma are (1.82 +/- 0.825), (1.35 +/- 0.43) mg x L(-1) and (123.39 +/- 55.82), (87.91 +/- 39.81) mg x L(-1) x min, Te (brain/blood drug ratio) was 70.93%; those pharmacokinetic values were larger than in sham-operated group. We can conclude that the pathological state of stroke can increase the amount of borneol permeating into brain.

Effect of borneol on intestinal absorption of muscone in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To explore the influence of borneol on intestinal absorption of muscone in rats.</p><p><b>METHOD</b>An in situ intestinal circulation perfusion experiment was used to study the changes in intestinal absorption kinetics of muscone before and after being compatible with borneol.</p><p><b>RESULT</b>Compared with the muscone group (MG), the absorption rate constants (Ka), the half-life period (T1/2) and the absorption rate (A) of muscone in the borneol + muscone group (BMG) were on the rise, but with no significant difference; after being compatible with borneol for a long period, Ka, T1/2 and A in the last borneol on muscone group (LBMG) increased, with significant difference (P < 0.05). in duodenum, LBMG showed better effects than MG (T1/2, P < 0.05); and so did in jejunum (Ka, P < 0.05; T1/2, P < 0.05); in ileum, there was no significant statistical difference between LBMG and MG.</p><p><b>CONCLUSION</b>Borneol can promote the intestinal absorption of muscone in rats to some extent.</p>

Research of bornrol promote drugs through blood-brain barrier / 中国中药杂志

Malignant tumor, epilepsy, dementia, cerebral ischemia and other brain diseases have very high rates of disability and mortality. Currently, many drugs are developed to treat such diseases and the effect is obviously. But they can not achieve the purpose to control these diseases because many of the drugs can not pass through the blood-brain barrier (BBB). Therefore, the treatment is not good. Borneol as the represent of the aromatic resuscitation medicine, it has strong fat-soluble active ingredients, small molecular weight, volatile and through the BBB quickly. It can also promote other therapeutic drugs through the BBB. It has two-ways regulations on BBB permeability and the damage of brain tissue is small, this have important theoretical significances and application values.

Effects of aromatic resuscitation drugs on blood brain barrier in cerebral ischemia-reperfusion injury model rats / 中国中药杂志

<p><b>OBJECTIVE</b>To research the effects of moschus, borneol, styrax and benzoinum on the structure and function of blood brain barrier in cerebral ischemia-reperfusion injury model rats.</p><p><b>METHOD</b>Focal middle cerebral artery occlusion (MCAO) was introduced as an in vivo ischemic model in rats. After 2 h MCAO, nylon suture was pulled up 1 cm to give blood reperfusion. After 22 h reperfusion, all animals were decapitated. The ultramicrostructure of blood brain barrier of ischemia hemisphere side in fronto-parietal cortex region by transmission electron microscope, and the content of VEGF and MMP-9 in ischemia side brain tissue were measured by ELISA.</p><p><b>RESULT</b>In model and solvent group rats, the capillary endothelium cells, astro-glial cells and nerve cells in ischemia hemisphere side in fronto-parietal region were emerged in different degree compared with sham-operated groups, which exhibited tight junction between endothelial cells being opened, basal lamina being dissolved, and permeability increasing, and cellularedema. In borneol (0.2 g x kg(-1)) group rats, the structure of three kinds of cells were nearly normal, which tight junction structure was clear, rough endoplasmic reticulum and polyribosome could be found in cytoplasm. In moschus (66.6 mg x kg(-1)) group rats, the structure of capillary endothelium cells and astrocytes were nearly normal as well as the basal lamina, but the electrons in neurons was maldistribution. In styrax (1.332 g x kg(-1)) group rats, astrocytes were nearly normal, while capillary endothelial cells and neurons exhibited oedema in different degrees. And the basal lamina was discontinuous, augmentation of cell spaces in endothelial cells increased the permeability, some endoplasmic reticulum broadened and ribosome ablated. In benzoinum (1.0 g x kg(-1)) group rats, oedema of capillary endothelial cells and astrocytes was significant, basal lamina broke. Meanwhile endoplasmic reticulum broadened as vacuole, the number of ribosome in rough endoplasmic reticulum decreased, crista mitochondriales in some neurons disappeared as vacuole which hint oedema happened. Results also showed that borneol decrease the level of VEGF in ischemia side brain tissue significantly, while has little influence on the level of MMP-9. Moschus showed the tendency to decrease the level of VEGF and MMP-9 in ischemia side brain tissue.</p><p><b>CONCLUSION</b>Aromatic resuscitation drugs showed the protection effect on blood brain barrier in cerebral ischemia-reperfusion injury rats, which the protection effect of moschus and borneol were better than that of styrax and benzoinum. The mechanism of protection effect maybe related to decrease the level of VEGF and MMP-9.</p>

Study on rat nasal absorption in situ of borneol based on single pass perfusion method / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the absorption characteristic of borneol.</p><p><b>METHOD</b>Using single pass perfusion model, the active ingredient of borneol were detected by GC. The drug concentration, perfusion rate and pH value on the absorption of borneol were studied.</p><p><b>RESULT</b>Perfusion rate on the absorption rate constants (Ka) had significant effects. Drug concentration and pH value on the absorption rate constants had no significant impact.</p><p><b>CONCLUSION</b>the absorption of borneol is good by nasal. The absorption rate constants of borneol have no effected by drug concentration. The absorption of borneol is via a simple diffusion.</p>