musk and isoborneol

To investigate the mechanism of Musk and Borneol on cerebral ischemia and reperfusion injury at different time points of acute phase in rats.. 180 rats were divided into seven groups including sham, ischemia-reperfusion after 24 h and 72 h model group, Musk 50 and 25 mg/kg groups, Borneol 50 and 25 mg/kg groups, and Xingnaojing 10 mL/kg group. Ischemia-reperfusion model was made after administration of each drug. The neurologic impairment scores at different time points after ischemia and reperfusion was evaluated, activities of cyclooxygenase (COX-2) and 5-lipoxygenase (5-LOX) in brain tissue were determined, and the expression of CysLT2 protein and mRNA in hippocampus were explored.. Musk and Borneol significantly improved the neurologic impairment scores of ischemia-reperfusion injury rats, improved the pathological morphology of rats brain tissue, reduced the activities of COX-2 and 5-LOX in brain homogenates,and inhibited the expression of CysLT2 protein in hippocampus.. Musk and Borneol have protective effect on inflammatory injury of acute injury in ischemia-reperfusion injury rats, the mechanism is related to inhibition the activity of COX-2 and 5-LOX in brain.

Topics: Animals; Anti-Inflammatory Agents; Arachidonate 5-Lipoxygenase; Brain; Brain Ischemia; Camphanes; Cyclooxygenase 2; Fatty Acids, Monounsaturated; Rats; Rats, Sprague-Dawley; Reperfusion Injury

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.. 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.. 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.. 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.

Topics: Animals; Benzoin; Blood-Brain Barrier; Brain Ischemia; Camphanes; Disease Models, Animal; Fatty Acids, Monounsaturated; Infarction, Middle Cerebral Artery; Male; Matrix Metalloproteinase 9; Neuroprotective Agents; Plant Extracts; Rats; Reperfusion Injury; Styrax; Vascular Endothelial Growth Factor A

To prepare heart-protecting musk pH-dependent gradient-release pellets and investigate the drug release in vitro and in vivo.. The pH-dependent gradient-release pellet system was prepared by using HPMC, Eudragit L-30D-55 and Eudragit L100-Eudragit S100 (1:5) combinations as coater. The release of borneol and total ginsenoside from pH-dependent gradient-release pellets were determined according to the method of Pharmacopoeia of the People's Republic of China (2000) in the simulated gastrointestinal pH conditions. The gastrointestinal transit and disintegration of pellets was investigated by using gamma-scintigraphic trace in volunteers. The pharmacokinetics of borneol of heart-protecting musk pH-dependent gradient-release pellets was studied in 6 healthy volunteers by GC methods.. The f2 value of release data of borneol and total ginsenoside of the heart-protecting musk pH-dependent gradient-release pellets was 79.6 in the simulated gastrointestinal pH conditions. The gamma-scintigraphic trace evaluation demonstrated that the pellets coated with HPMC, Eudragit L-30D-55 or Eudragit L100-Eudragit S100 (1:5) combinations can disintegrate in stomach, duodenum and jejunum or ileum. The gastrointestinal transit time of pellets was about 5 hours in fasted state and about 6 hours in fed state. The concentration-time curves of borneol of heart-protecting musk pills fit in two-compartment model. The pharmacokinetics data showed that borneol had a short time of absorption and elimination. The mean residence time (MRT) of borneol of heart-protecting musk pills was 2.61 hours. The plasma concentration of borneol of heart-protecting musk sustained-release capsule which consisted of three kinds of pellets coated with HPMC, Eudragit L-30D-55 or Eudragit L100-Eudragit S100 (1:5) combinations was steadier than those of heart-protecting musk pills, its Cmax was lower than and Tmax was near to those of heart-protecting musk pills, its MRT was 4.0 hours, and its relative bioavailability was 96%.. The lipidsoluble borneol and watersoluble total ginsenoside of heart-protecting musk pH-dependent gradient-release pellets can release simultaneously while sustained-releasing in vitro. The heart-protecting musk pH-dependent gradient-release pellets had the characteristics of pH-dependent gradient-releasing and disintegration while transiting in gastrointestinal tract. A characteristic of gradient sustained-release was shown in the concentration-time curves of borneol of heart-protecting musk sustained-release capsule in volunteers.

Topics: Adult; Camphanes; Delayed-Action Preparations; Drug Combinations; Drugs, Chinese Herbal; Fatty Acids, Monounsaturated; Gastrointestinal Transit; Ginsenosides; Humans; Hydrogen-Ion Concentration; Lactose; Male; Materia Medica; Methylcellulose; Oxazines; Polymethacrylic Acids; Random Allocation

Menthol and borneolum have been used widely in traditional Chinese medicine for the treatment of nasal obstruction, but the mechanism has been still unknown. The effects of inhalation of menthol, borneolum, moschus on nasal resistance and airflow sensation were investigated in 52 subjects. All of these medicines could cause a highly significant enhancement of nasal airflow sensation but had no effect on nasal resistance. Therefore this sort of medicine is regarded as pseudo nasal decongestant.

Topics: Adult; Airway Resistance; Camphanes; Fatty Acids, Monounsaturated; Female; Humans; Male; Menthol; Nasal Cavity; Sensation