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.
Animals ; Biological Transport ; drug effects ; Blood-Brain Barrier ; drug effects ; metabolism ; Bornanes ; pharmacology ; Brain ; drug effects ; metabolism ; Humans

OBJECTIVETo study the absorption and transportation characteristic of 1-ephedrine (LEP), d-pseudoephedrine (DPEP), d-norpseudoephedrine (DNPE) isolated from Herba Ephedrae, which were classified the alkaloids, in human intestinal epithelium.

METHODCaco-2 (the human colon adeno carcinoma cell lines) cells monolayer was used as an intestinal epithelial cell model. The permeability of the three alkaloids from apical side (AP side) to basolateral side (BL side) or from BL side to AP side was evaluated. The concentration of the three alkaloids was measured by HPLC coupled with UV detector. Transportation parameters and apparent permeability coefficients (P(app)) were then calculated, and P(app) values were compared with the reported values for model compounds, propranolol and atenolol.

RESULTThe P(app) values of the three alkaloids in the bi-directional transportation were quantitative degree of 1.0 x 10(-5) cm x s(-1), which was comparable with the P(app), value of propranolol, which is a transcellular transportation marker and a well-transported compound with a P(app) > or = 1.0 x 10(-5) cm x s(-1). The absorption and transportation of the three alkaloids were positive correlation to the concentration of 10-200 mol x L(-1).

CONCLUSIONLEP, DPEP and DNPE can be absorbed across intestinal epithelial cells by passive diffusion mechanism, and are well absorbed compounds.

Absorption ; Alkaloids ; pharmacokinetics ; Biological Transport ; Caco-2 Cells ; Cell Membrane Permeability ; drug effects ; Drugs, Chinese Herbal ; pharmacokinetics ; Ephedra ; chemistry ; Humans ; Intestinal Mucosa ; drug effects ; metabolism ; Models, Biological

OBJECTIVETo investigate the absorption mechanism of oxysophocarpine across Caco-2 cell monolayer model.

METHODThe safety concentration of oxysophocarpine in Caco-2 cell was first selected by using MTT method. Then the Caco-2 cell monolayers drug transport model was assigned to study the bi-direction transport mechanism of oxysophocarpine by evaluating the influent factors such as time, concentration, pH, P-gp inhibitor of verapamil, on its absorption characterization.

RESULTIn the Caco-2 cell monolayer model, the transport volume was correlated positively with the time and concentration of oxysophocarpine, and affected by pH value. Verapamil had no influence on its transport since the transport of oxysophocarpine from apical (AP) to basolateral (BL) was similar to the transport from basolateral to apical.

CONCLUSIONThe intestinal absorption mechanism of oxysophocarpine was deduced as passive transference by Caco-2 cell monolayer model.

Alkaloids ; pharmacokinetics ; Biological Transport ; Caco-2 Cells ; Cell Membrane Permeability ; drug effects ; Drugs, Chinese Herbal ; pharmacokinetics ; Humans ; Intestinal Absorption ; drug effects ; Models, Biological

OBJECTIVETo evaluate the influence of borneol on nasal absorption enhancement of ligustrazine.

METHODThe rats were randomly divided into 3 groups: Xiongbing nasal spray group (group A), Chuanxiong nasal spray group (group B) and Xiongbing group by decoction intragastric administration (group C). All the rats were decapitated at several time points after administration. The whole brains of rats were taken to homogenate and detected the concentrations of ligustrazine.

RESULTCompared with group B and C, group A has its characteristics: quick absorption, quick distribution and quick excretion of ligustrazine.

CONCLUSIONNasal administration is a quick-acting way for ischemic cerebral vessel insufficientia. Borneol promoted nasal absorption of ligustrazine into brain.

Animals ; Biological Transport ; drug effects ; Bornanes ; pharmacology ; Drug Administration Routes ; Female ; Kinetics ; Male ; Nose ; drug effects ; metabolism ; Pyrazines ; administration & dosage ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

OBJECTIVEDehydroandrographolide (DP) from Andrographis paniculata (Burm. F.) Nees is a potential anticancer agent. This study aimed to investigate the oral bioavailability and intestinal disposition of DP to provide useful information for the development of DP as a new candidate anticancer drug.

METHODSThe pharmacokinetics of DP was evaluated in rats, and its intestinal disposition was determined using cultured Caco-2 cells and a single-pass rat intestinal perfusion model.

RESULTSThe oral bioavailability of DP was 11.92% in rats. The apparent permeability coefficient (P(app)) of DP from the basolateral side (B) to the apical side (A) (5.37×10(-5) cm/s) of the Caco-2 model was roughly equal to that from A to B (4.56×10(-5) cm/s), suggesting no involvement of the efflux transporter(s). In the perfusion model, no significant difference was found in the effective permeability (P*(eff)) of DP between the 4 segments of the intestine. No significant metabolism of DP was detected in the intestinal perfusates. The amount of DP found in the bile was only about 0.1% of the absorbed amount. The P*(eff) and bile amounts of DP were not significantly increased by P-glycoprotein (P-gp) inhibitor or breast cancer resistant protein (BCRP) inhibitor (P>0.05).

CONCLUSIONThe bioavailability of DP was 11.92% in rats. DP has good absorption and metabolism stability in the intestine. The efflux transporters such as P-gp and BCRP do not participate in DP transport.

Administration, Oral ; Animals ; Biological Availability ; Biological Transport ; Caco-2 Cells ; Diterpenes ; administration & dosage ; pharmacokinetics ; Humans ; Intestinal Absorption ; Intestines ; drug effects ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo explore the transmembrane transport and metabolism of diammonium glycyrrhizinate in intestines of rats.

METHODAn Ussing Chamber model were used to investigate the transmembrane transport of diammonium glycyrrhizinate (GZ), the concentrations of diammonium glycyrrhizinate and its two metabolites were determined by HPLC.

RESULTThe permeability coefficients of GZ in difference intestinal mucous membranes were ranged from 0.3 x 10(-6) cm x s(-1) to 1.1 x 10(-6) cm x s(-1). The metabolism of GZ in enterocytes during its transport process was negligible. The concentration of diammonium glycyrrhizinate and pH had limit effects on the transport amount and the permeability coefficients of GZ.

CONCLUSIONGZ is a low permeability drug, but it can be absorbed at all segments of the small intestine in rats. Ileum is the major absorption region of GZ.

Animals ; Biological Transport ; Cell Membrane Permeability ; Glycyrrhizic Acid ; metabolism ; pharmacokinetics ; Hydrogen-Ion Concentration ; Intestine, Small ; chemistry ; drug effects ; metabolism ; Male ; Models, Biological ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo investigate the absorption and transport mechanism of magnolol in Caco-2 cell model.

METHODSA human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the absorption and transport of magnolol, the effects of time, donor concentration, P-gp inhibitor verapamil, pH and temperature on the absorption and transport of magnolol were investigated. The determination of magnolol was performed by high performance liquid chromatography, then the values of apparent permeability coefficient (P app ) and P ratio Basolateral-to-Apical (BL-to-AP)/Apical-to-Basolateral (AP-to-BL) were calculated.

RESULTSIn Caco-2 cell model, comparing the amounts of transport of AP-to-BL and BL-to-AP, the latter was larger. At the same donor concentration, either the amounts of transport of AP-to-BL or BL-to-AP increased with increase in donor concentration and incubation time. Verapamil could significantly improve the amounts of transport of AP-to-BL. The transport of AP-to-BL and BL-to-AP depended on temperature, and there was no significant effect of pH on the transport of AP-to-BL.

CONCLUSIONMagnolol could be transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport, at the same time, the efflux mechanism could be involved.

Biological Transport ; drug effects ; Biphenyl Compounds ; metabolism ; Caco-2 Cells ; Chromatography, High Pressure Liquid ; Humans ; Hydrogen-Ion Concentration ; drug effects ; Intestinal Absorption ; drug effects ; Lignans ; metabolism ; Models, Biological ; Temperature ; Time Factors ; Verapamil ; pharmacology

OBJECTIVETo observe the effect of novel air neuromodulator H2S on platelet function of L-Arg transport for discussing H2S of effect on platelet function.

METHODSSaturate H2S solution as donate made rat rich platelet plasma and pre-incubation rat platelet with different density of H2S. To measure the velocity of L-Arg transport in platelet by radioactivity technique.

RESULTSAt different concentrations of H2S (6.25, 12.5, 25, 50, 100 micromol/L), the velocity of L-Arg transport was lower than that in control. H2S reduced rapidly the Vmax and velocity of L-Arg transport in platelet (P < 0.05) and this effect had no effect to Km.

CONCLUSIONH2S can affect platelet function by changing rapidly platelet L-Arg transport system function.

Animals ; Arginine ; metabolism ; Biological Transport ; drug effects ; Blood Platelets ; drug effects ; metabolism ; Hydrogen Sulfide ; metabolism ; pharmacology ; Male ; Rats ; Rats, Sprague-Dawley

Pineapple (Ananas comosus) leaves contain mainly phenolic components with antioxidant and hypolipidemic effects. One of the principle components is p-coumaric acid. In this study, the transport behavior of p-coumaric acid, was observed after the administration of pineapple leaf phenols in vitro. Simultaneously, the effect of the phenols on glucose, total cholesterol and triglycerides transportation and metabolism in HepG2 cells was also observed. The results showed that the phenols had good transport characteristics. 5 min after the administration, p-coumaric acid of the phenols could be detected, and the content of p-coumaric acid reached the peak concentration after 60 min of the administration. p-coumaric acid of phenols have time-and dose-dependent manner. While promoting glucose transporter (GLUT4) and low density lipoprotein receptor (LDLR) expression, the phenols decreased intracellular lipid content. This reduction of intracellular lipid content was highly correlated with the promotion of lipoprotein lipase (LPL) and hepatic triglyceride lipase (HTGL) expression, while the reduction of intracellular glucose levels was correlated with glycogen synthesis in the cells.
Ananas ; chemistry ; Biological Transport ; drug effects ; Cholesterol ; metabolism ; Glucose ; metabolism ; Hep G2 Cells ; Humans ; Lipid Metabolism ; drug effects ; Plant Extracts ; pharmacology ; Plant Leaves ; chemistry

Aluminum (Al) is the most abundant metal element in the earth's crust. On acid soils, at pH 5.5 or lower, part of insoluble Al-containing minerals become solubilized into soil solution, with resultant highly toxic effects on plant growth and development. Nevertheless, some plants have developed Al-tolerance mechanisms that enable them to counteract this Al toxicity. One such well-documented mechanism is the Al-induced secretion of organic acid anions, including citrate, malate, and oxalate, from plant roots. Once secreted, these anions chelate external Al ions, thus protecting the secreting plant from Al toxicity. Genes encoding the citrate and malate transporters responsible for secretion have been identified and characterized, and accumulating evidence indicates that regulation of the expression of these transporter genes is critical for plant Al tolerance. In this review, we outline the recent history of research into plant Al-tolerance mechanisms, with special emphasis on the physiology of Al-induced secretion of organic acid anions from plant roots. In particular, we summarize the identification of genes encoding organic acid transporters and review current understanding of genes regulating organic acid secretion. We also discuss the possible signaling pathways regulating the expression of organic acid transporter genes.
Aluminum ; toxicity ; Anions ; Biological Transport ; drug effects ; Citric Acid ; metabolism ; Malates ; metabolism ; Oxalic Acid ; metabolism ; Plant Roots ; drug effects ; metabolism ; Signal Transduction ; physiology