Choline is an essential nutrient that plays an integral role in all stages of the life cycle, with increasing interest in the relationship between choline and neurodevelopment. Choline is a major component in the synthesis of phospholipids, phosphatidylcholine and sphingolipids, and is an essential nutrient for methyl metabolism, acetylcholine synthesis and cell signaling. Choline plays an important role in neurogenesis and neural migration during fetal development, potentially influencing the development and prognosis of neurological disorders, but its mechanism of action is not yet clear. This article reviews the source and metabolism of choline, the effects and mechanism of choline on neurodevelopment and central nervous system related disorders.
Humans ; Choline/metabolism* ; Phosphatidylcholines/metabolism* ; Central Nervous System/metabolism*

OBJECTIVETo investigate the change of the subfractions in existence (big and small polymers) of pulmonary surfactant (PS) and their influence on the decrease in PS activity during early postburn stage.

METHODSForty rabbits were employed in the study and were randomly divided into pre-burn, 0.5 postburn hour (PBH), 2 PBH, 6 PBH and 12 PBH groups with 8 in each group. The BALF (bronchial alveolar lavage fluid) was harvested from each rabbit. The BALF samples were centrifuged, and the supernatant (small polymer) and precipitation (big polymer) were harvested for the determination of the contents of the total phospholipids, lecithin, total protein, and albumin in both polymers.

RESULTSCompared with those in pre-burn group, the above chemical contents of PS in big polymer exhibited no change after burn (P > 0.05), but the contents of albumin and total protein increased obviously in small polymer (P < 0.01). In addition, all the contents in the small polymer increased with the elapse of time. The percentage of lecithin in total phospholipids in small polymers decreased along with the passage of time. The pre-burn contents of total phospholipids, lecithin, TP, albumin, and the percentage of lecithin in total phospholipid in small polymer were (2.23 +/- 0.40),(1.54 +/- 0.11), (16.67 +/- 1.34), (3.65 +/- 0.15) mg/ml and (77.2 +/- 3.7)%, respectively. The above indices in small polymer were (3.15 +/- 0.30), (1.77 +/- 0.08), (106.59 +/- 5.50), (11.21 +/- 0.92) mg/ml and (57.2 +/- 3.5)% respectively at 6PBH.

CONCLUSIONThe ratio of small to big polymers increased obviously, which might be an important factor in inducing the decrease in PS activity during early postburn stage leading finally to pulmonary injury.

Albumins ; analysis ; Animals ; Female ; Male ; Phosphatidylcholines ; analysis ; Phospholipids ; analysis ; Pulmonary Surfactants ; metabolism ; Rabbits ; Smoke Inhalation Injury ; metabolism

Cell Line ; Hepatic Stellate Cells ; cytology ; metabolism ; pathology ; Humans ; Oxidative Stress ; Phosphatidylcholines ; pharmacology ; Transforming Growth Factor beta1 ; metabolism

OBJECTIVETo explore the correlation between the content of lecithin mass and white blood cells (WBC) of the expressed prostatic secretion (EPS) and the concentration of serum PSA in patients with prostatitis, and to study the difference in serum PSA concentration between patients with bacterial prostatitis and those with nonbacterial prostatitis.

METHODSThe serum PSA concentration in 62 patients with prostatitis and 22 controls were measured with ELISA method. The correlation between the content of lecithin mass and WBC of the EPS and the elevation of serum PSA was analyzed. And the serum PSA concentration of bacterial prostatitis (9 patients) and that of nonbacterial inflammatory prostatitis (53 patients) were compared.

RESULTSThe mean concentrations of serum PSA in the prostatitis and the control groups were (1.79 +/- 0.68) microg/L and (0.63 +/- 0.29) microg/L, respectively. The difference of the serum PSA concentration was significant between the prostatitis and the control groups (P < 0.001) as well as between the groups with higher and lower WBC contents in EPS (P < 0.05), but not between the groups with higher (27 patients) and lower (35 patients) lecithin mass contents in EPS (P > 0.05), nor between the groups of bacterial prostatitis and nonbacterial prostatitis (P > 0.05).

CONCLUSIONProstatitis may cause the elevation of serum PSA concentration. The elevated serum PSA correlates with the content of white blood cells in EPS, but not with the content of lecithin mass in EPS, nor with the type of prostatitis, either bacterial or nonbacterial.

Adult ; Humans ; Leukocyte Count ; Male ; Middle Aged ; Phosphatidylcholines ; analysis ; Prostate ; secretion ; Prostate-Specific Antigen ; blood ; Prostatitis ; metabolism

OBJECTIVETo investigate various methods for constructing soybean lecithin (SL)-based vesicles and evaluate the permeation-enhancing effect of SL-based vesicles on the penetration of insulin through buccal mucosa.

METHODSThe ultrasonic method, high speed shear method and high pressure homogenization method were respectively used to prepare the SL-based vesicles, and the particle size of the vesicles was measured with photon correlation spectrometry (PCS). The penetration rate of insulin through porcine buccal mucosa was investigated with the Valia-Chien diffusion cells.

RESULTSThe average particle sizes of 3 formulations of SL-based vesicles were 97.39, 85.60, and 100.60 nm when prepared by ultrasonic method, and were 58.7, 88.7, and 91.9 nm when prepared by high pressure homogenization method. Both vesicles presented good stability. However, the SL-based vesicles prepared by high speed shear method had larger average diameters and were found to be unstable. Transmission electron microscopy showed that SL-based vesicles had a spherical shape and the result accorded with PCS. The permeation flux of insulin of formulation 1 and control solution were 0.0024 and 0.0008 IU x ml(-1) x min(-1), respectively. The accumulative amount of formulation 1 at 180 min was (0.436 +/- 0.010 ) IU x ml(-1), which was 1.46 times higher than the control solution.

CONCLUSIONSThe SL-based vesicles obtained using high pressure homogenization method are characterized by small particle size, narrow distribution, good stability, and powerful permeation-enhancing effect, which enables them to be good carriers for the buccal delivery of insulin.

Absorption ; Administration, Topical ; Chemistry, Pharmaceutical ; Drug Carriers ; administration & dosage ; chemical synthesis ; pharmacokinetics ; Drug Delivery Systems ; methods ; Insulin ; metabolism ; Mouth Mucosa ; metabolism ; Nanotechnology ; methods ; Phosphatidylcholines ; pharmacokinetics ; Soybeans ; chemistry

The eye is a relatively isolated organ and tends to retain or accumulate compounds within itself. Unless the eye possesses a mechanism for detoxifying drugs and chemicals that are carried to ocular tissues via the circulating blood, the compounds may cause visual impairment. The purposes of this experiment was judged by drug metabolizing action by cytochrome P-450 system, distribution and effect of metabolism of arachidonic acid and distribution of lipid peroxide formation and phospholipids in the lens, cornea and choroid-retina of pig ocular tissues. The results were as follows: 1. The activities of mixed-function oxidase, cytochrome P-450 and NADPH-cytochrome C reductase were the highest in the choroid-retina compared to the lens and cornea. 2. The activities of drug metabolizing enzymes, aryl hydrocarbon hydroxylase, 7-ethoxycoumarin-o-deethy lase and benzphetamine-N-demethy lase, heme oxygenase activity, and the activity of arachidonic acid metabolizing enzyme, cyclooxygenase were the highest in the choroid-retina compared to the lens and cornea. 3. Lipid peroxide formation was the highest in the cornea compared to the lens and choroid retina. 4. In distribution of phospholipids, sphingomyelin and phosphatidylcholine were the highest in the choroid-retina compared to the lens and cornea and phosphatidylethanolamine was the highest in the cornea campa red to the lens and choroid-retina. 5. Cytochrome P-450 isoenzyme of pig ocular tissues was confirmed in the same form of MAb(Monoclonal Antibody) PCN(pregenolone-16alpha-carbonitrile) 213-1.
Arachidonic Acid* ; Choroid ; Cornea ; Cytochrome P-450 Enzyme System* ; Cytochromes* ; Heme Oxygenase (Decyclizing) ; Metabolism* ; NADPH-Ferrihemoprotein Reductase ; Oxidoreductases ; Phosphatidylcholines ; Phospholipids ; Prostaglandin-Endoperoxide Synthases ; Retina ; Vision Disorders

BACKGROUND/OBJECTIVES: Consumption of cholesterol-rich foods, such as eggs, has a minimal effect on circulating cholesterol levels in healthy humans. To gain insight, we investigated whether phospholipids rich in eggs (EPL) interfere with intestinal cholesterol absorption in vivo. MATERIALS/METHODS: To investigate the acute effect of EPL on intestinal cholesterol absorption, male C57BL/6J mice were orally administered with 6, 11, or 19 mg of EPL for three days. We also tested the effect of chronic EPL consumption on cholesterol metabolism in the small intestine and the liver in mice with diet-induced hypercholesterolemia. Male C57BL/6J mice were fed a high fat/high cholesterol (HF/HC; 35% fat, 0.25% cholesterol, w/w) diet for 4 weeks to induce hypercholesterolemia, and subsequently the mice were either fed 0, 0.4 or 0.8% (w/w) of EPL for 6 weeks. RESULTS: Intestinal cholesterol absorption was significantly decreased by the highest dose of acute EPL administration compared to control. Chronic EPL supplementation did not significantly alter intestinal cholesterol absorption nor plasma levels of total cholesterol and low-density lipoprotein cholesterol. In the small intestine and the liver, EPL supplementation minimally altered the expression of genes which regulate cellular cholesterol levels. CONCLUSION: Although chronic EPL consumption was not able to counteract hypercholesterolemia in HF/HC-fed mice, acute EPL administration decreased intestinal cholesterol absorption. This study provides in vivo evidence that acute administration of PLs in eggs prevent cholesterol absorption in the intestine, suggesting a mechanism for a minimal effect of egg consumption on circulating cholesterol levels.
Absorption ; Animals ; Cholesterol ; Diet ; Eggs ; Humans ; Hypercholesterolemia ; Intestinal Absorption ; Intestine, Small ; Intestines ; Lipoproteins ; Liver ; Male ; Metabolism ; Mice ; Ovum ; Phosphatidylcholines ; Phospholipids ; Plasma

BACKGROUNDUp to date, there is few satisfactory pharmacotherapy, except for aspirin and heparin, to stop the preeclampsia progression. Although the mechanism of preeclampsia is poorly understood, it has been proven to be associated with coagulation activation. Researches on prophylactic and therapeutic application of anticoagulants may benefit the clinical aspects of preeclampsia individuals. This study aimed to evaluate the effects of Danshensu on maternal syndrome in phosphatidylserine/phosphatidylcholine (PS/PC) microvesicle induced-mouse model.

METHODSSixty-six preeclampsia-like pregnant mice, induced by PS/PC microvesicle administration, were randomly divided into six groups. From days 5.5 to 16.5 of pregnancy, each group was respectively treated as follows: a) mice in group C (n = 12, control group) were injected with 100 microl of filtered phosphate-buffered saline into the tail vein every day; b) group PE (n = 15, preeclampsia model group) were injected in the same way with 100 microl of filtered PS/PC vesicle suspension; c) group H (n = 9, group treated with heparin) were injected with 1 unit heparin together with PS/PC vesicle suspension; d) group A (n = 10, group treated with aspirin) were injected with 20 microg/g aspirin-DL lysine as well; e) group LD (n = 10, group treated with low-dose Danshensu) were injected with 10 microg/g Danshensu; and f) group HD (n = 10, group treated with high-dose Danshensu) were injected with 30 microg/g Danshensu. Systolic blood pressure, total urinary protein levels, blood tests for some hemostatic function parameters (mean platelet counts, plasma antithrombin III activity (AT-III), D-D dimmer levels, and thrombin time), fibrin deposition by phosphotungstic acid hematoxylin staining, and thrombomodulin expression by immunohistochemistry staining in placentas were examined as indices for maternal syndrome.

RESULTSHeparin showed significant effects on maternal syndrome of preeclampsia such as hypertension and proteinuria, and different doses of Danshensu also presented the certain effects. High-dose Danshensu and aspirin all demonstrated better effects than low-dose Danshensu on decreasing blood pressure to normal level, while high-dose Danshensu demonstrated better effects than aspirin and low-dose Danshensu on decreasing proteinuria to normal level. As to Danshensu's effects on hemostatic function, high- and low-dose Danshensu's marked effects on increasing the plasma AT-III activity were the same as that of aspirin and inferior to that of heparin. High-dose Danshensu's better effect on elevating the platelet counts was superior to low-dose Danshensu and aspirin. Low-dose Danshensu's obvious effect on decreasing D-D levels was close to heparin and superior to high-dose Danshensu and aspirin. High- and low-dose Danshensu's significant effects on reduced thrombin time level are same to heparin. Different anticoagulants all played improvement roles in placental fibrin depositions, but heparin and high-dose Danshensu's roles on lowering thrombomodulin expression in placentas were superior to low-dose Danshensu and aspirin. However, anticoagulant function of high-dose Danshensu was still inferior to heparin. We found long-term use of heparin and aspirin, in spite of low-dose administration, could raise the risk of bleeding such as placental abruption and intestinal hemorrhage. But no any side effect was observed in mice treated with different doses of Danshensu in our study.

CONCLUSIONSDanshensu has proven to be effective and safe in ameliorating the prognosis of maternal syndrome in a preeclampsia mouse model. We suggest long-term provision of low-dose Danshensu in pregnancy, leading to an improvement of preeclampsia syndrome with considerable maternal safety.

Animals ; Anticoagulants ; therapeutic use ; Aspirin ; therapeutic use ; Disease Models, Animal ; Female ; Heparin ; therapeutic use ; Lactates ; therapeutic use ; Mice ; Mice, Inbred ICR ; Phosphatidylcholines ; adverse effects ; Phosphatidylserines ; adverse effects ; Placenta ; metabolism ; Pre-Eclampsia ; chemically induced ; prevention & control ; Pregnancy ; Random Allocation ; Thrombomodulin ; metabolism

OBJECTIVECapsaicin transfersomes were prepared and its quality specifications were evaluated.

METHODCapsaicin transfersomes were prepared by high shear dispersing machine and evaluated on the entrapment efficiency, drugs release rate and in vitro skin permeation.

RESULTCapsaicin transfersomes is composed of single unilamellar vesicles, with average size of 150.6 nm. Capsaicin entrapment efficiency achieved 96.7% while concentration of lecithin used was 8%. cumulative release amount of capsaicin was in direct proportion to the ethanol concentration in the medium. The in vitro rate cumulative penetration rate of capsaicin was higher in transfersomes than in cream and suspension in rats. Adomen skin cumulative penetration rate in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men. In the same way,cumulative penetration rate in vitro of capsaicin transfersomes through abdomen skin epidermal membrance was significantly higher than that with derma and full skin in men.

CONCLUSIONEntrapment efficiency of capsaicin transfersomes reached 96.7%, meeting the criterion of China pharmacopia( > 80%), skin penetration of capsaicin was enhanced by a capsaicin transfersomes preparation and was affected by diverse characters and levels of skin.

Administration, Cutaneous ; Analgesics, Non-Narcotic ; administration & dosage ; pharmacokinetics ; Animals ; Capsaicin ; administration & dosage ; pharmacokinetics ; Drug Carriers ; Drug Delivery Systems ; methods ; Humans ; In Vitro Techniques ; Male ; Mice ; Particle Size ; Phosphatidylcholines ; administration & dosage ; chemistry ; pharmacology ; Rats ; Skin ; drug effects ; metabolism ; Skin Absorption ; drug effects

AIMTo study the release and cell uptake characteristics of 9-nitrocamptothecin (9-NC) nanostructured lipid carrier system (NLC) in vitro and its tissue distribution characteristics in vivo.

METHODSMouse peritoneal macrophages were used to investigate the uptake of nanoparticles by cells in vitro. The tissue distribution of 9-nitrocamptothecin solution and stealth nanostructured lipid carrier system (S-NLC) was determined after intravenous administration to mice at a single dose of 1.5 mg kg(-1). The release and crystalloid characteristics were also investigated.

RESULTSX-ray diffraction spectrum showed that 9-NC probably was amorphous in S-NLC. The liquid lipid did not change the characteristics of the solid matrix in nanoparticles. The in vitro release and cell uptake characteristics of stealth and non-stealth 9-NC-NLC were investigated, separately. The results showed that the stealth 9-NC-NLC had sustained-release characteristics and could resist the absorption effect of the additional plasmas to a certain extent. In addition, the cell uptake percentage of stealth 9-NC-NLC was much lower than that of the non-stealth ones. The tissues distribution results showed that 9-NC in the S-NLC was mainly found in the lung, liver, pancreas and ovary/uterus, while the quantity of 9-NC was much lower in heart and kidney. The AUQ(0-t), of S-NLC in blood, ovary/uterus, pancreas, liver and lung were higher than that of 9-nitrocamptothecin solution. The weight-average drug targeting efficiency (Te*) of S-NLC in liver and lung were significantly higher than that of 9-nitrocamptothecin solution. The mean residence times (MRT) of S-NLC was 44 h, while that of 9-nitrocamptothecin solution was 8 h. Therefore, S-NLC showed obvious targeting effects on liver and lung.

CONCLUSIONS-NLC with PEG flexible chains has sustained-release characteristics and can prolong its circulation in blood and have good targeting efficiency on liver and lung.

Animals ; Antineoplastic Agents ; administration & dosage ; chemistry ; pharmacokinetics ; Camptothecin ; administration & dosage ; analogs & derivatives ; chemistry ; pharmacokinetics ; Delayed-Action Preparations ; Drug Carriers ; Drug Delivery Systems ; Female ; Hexoses ; chemistry ; Liver ; metabolism ; Lung ; metabolism ; Macrophages, Peritoneal ; physiology ; Mice ; Nanoparticles ; Particle Size ; Phagocytosis ; Phosphatidylcholines ; chemistry ; Polyethylene Glycols ; chemistry ; Tissue Distribution