To explore the effect of long-time propofol infusion on myocardial enzymes, mitochondrial cytochrome C and ATP in rabbits. 
 Methods: A total of 18 New Zealand rabbits were randomly divided into 3 groups: a control group, a propofol group and an intralipid group. The rabbits were continuously infused with 0.9% normal saline in the control group, 1% propofol in the propofol group, and 10% intralipid in the intralipid group, respectivey. The arterial blood was collected at 0, 8, 16 h and the end of experiment to examine creatine kinase (CK) and creatine kinase isoenzyme (CK-MB). In the end, the myocardial mitochondria from myocardial tissues was separated by differential centrifugation, and mitochondrial cytochrome C content and adenosine triphosphate (ATP) levels were examined by high performance liquid chromatography.
 Results: Compared with the control group, the release of cytochrome C from mitochondria were increased in the propofol group and the intralipid group (both P<0.05), but there was no significant difference between them (P>0.05). There was also no significant difference in the ATP content of the mitochondria among the 3 groups (P>0.05). The levels of CK were increased at 8, 16 and 24 h after infusion in the propofol group and the intralipid group compared with that before the infusion (all P<0.05); compared with the control group, the levels of CK were increased at 8, 16 and 24 h after infusion in the propofol group and the intralipid group (all P<0.05); compared with the intralipid group, the levels of CK were increased at 8, 16 and 24 h after infusion in the propofol group (all P>0.05); compared with the control group, the levels of CK-MB were obviously increased in the infusion of propofol for 24 h in the propofol group (P<0.05).
 Conclusion: The levels of serum CK increase after the infusion of propofol and intralipid for a long time, and the levels of CK-MB also elevate in the infusion of propofol. Propofol and intralipid can increase the release of myocardial mitochondrial cytochrome C, but they don't affect the ATP production in myocardial mitochondrial.
Adenosine Triphosphate ; metabolism ; Animals ; Creatine Kinase ; blood ; metabolism ; Creatine Kinase, MB Form ; blood ; metabolism ; Cytochromes c ; metabolism ; Emulsions ; administration & dosage ; pharmacology ; Infusions, Intravenous ; Mitochondria ; drug effects ; Myocardium ; chemistry ; enzymology ; Phospholipids ; administration & dosage ; pharmacology ; Polyphosphates ; Propofol ; administration & dosage ; pharmacology ; Rabbits ; Soybean Oil ; administration & dosage ; pharmacology

According to Chinese and foreign literatures and reports in recent years, this article introduced the latest advance in studies on phospholipid compound of traditional Chinese medicines in terms of its preparation mechanism, preparation process, characterization and transmembrane absorption. Under appropriate conditions, traditional Chinese medicines could generate phospholipid compound, whose physico-chemical property differs from the original drug, with a better absorption and improved bioavailability. Therefore, there is huge room for further study and development of phospholipid compound with traditional Chinese medicines.
Absorption ; Animals ; Biological Availability ; Humans ; Medicine, Chinese Traditional ; Phospholipids ; chemistry ; pharmacology

OBJECTIVETo compare the pharmaceutical properties and the anti-tumor activities of three kinds of stealth liposomes prepared with different phospholipid composition containing brucine.

METHODStealth liposomes with different phospholipids composition, such as soybean phosphatidycholine (SPC), hydrogenated soybean phosphatidylcholine (HSPC) and the complex of SPC and HSPC, were prepared by ammonium sulfate transmembrane gradient method. Pharmaceutical properties such as shape, encapsulation efficiency and size of three stealth liposomes were compared intensively. Anti-tumor activity of SPC, HSPC and novel stealth liposomes composed of both SPC and HSPC were compared by established mouse liver cancer H22 model. Meanwhile, the mice body weight and immune organ weight were also compared.

RESULTThe encapsulation efficiency of novel, SPC and HSPC stealth liposomes were 77.7%, 64.8% and 74.8%, respectively. The mean diameters of them were less than 100 nm. The tumor inhibition rate of novel, HSPC and SPC stealth liposomes were 57.88%, 49.15%, 23.37%, respectively. The mice body weight, thymus gland index of three stealth liposomes group and spleen index of novel stealth liposomes group had no significant difference with the negative group while SPC and HSPC stealth liposomes group increased the spleen index.

CONCLUSIONPhospholipids composition is the key factor which determines the antitumor activity of brucine-loaded stealth liposomes.

Animals ; Antineoplastic Agents ; chemistry ; pharmacology ; Body Weight ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Humans ; Liposomes ; adverse effects ; chemistry ; Mice ; Particle Size ; Phospholipids ; chemistry ; Strychnine ; analogs & derivatives ; chemistry

This study was to report the effect of Tangshen Formula on phospholipids metabolism in diabetic nephropathy patients. A normal phase-HPLC-TOF/MS method was used in this study for the determination of seven species of phospholipids in human plasma. Then, the concentration changes of potential phospholipids biomarkers were discussed in diabetic nephropathy phase III and phase IV patients among different groups, including before and 3, 6 months after administration of Tangshen Formula. Significant increases of PE750, PI885, PC792, PC826, PC830, PC854 and PC802 levels were observed 6 months after administration of Tangshen Formula and conventional western medicine, as well as a decrease of LPC540 level, when compared with those before medication. Concentrations of all the potential phospholipids biomarkers showed a tendency towards normal levels; however, both the improvement degree and onset time of these compounds were not same. Additionally, Tangshen Formula treatment based on conventional western medicine treatment was more efficient in adjusting the levels of these compounds when compared with western medicine treatment alone, especially for the phase IV patients. These results indicated that Tangshen Formula was capable in regulating and improving phospholipids metabolism in diabetic nephropathy patients, which may be related with the direct or indirect inhibition of protein kinase C pathway and the corresponding reduction of phospholipase A2 activity. Therefore, Tangshen Formula may be used as an effective drug for diabetic nephropathy therapy, at least as an adjunctive therapeutic drug.
Diabetic Nephropathies ; blood ; metabolism ; Double-Blind Method ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Glycerophospholipids ; blood ; Humans ; Lysophosphatidylcholines ; blood ; Phospholipases A2 ; metabolism ; Phospholipids ; blood ; classification ; Plants, Medicinal ; chemistry ; Protein Kinase C ; metabolism ; Signal Transduction ; Sphingomyelins ; blood

The injury of tumor blood vessels will break up the nutrition supply for the tumor. In this paper, we investigated the effects exerted by high intensity focused ultrasound (HIFU) combined with ultrasound microbubble agent on blood vessels. Ultrasound diagnosis was used to find the goat hepatic blood vessels each being approximately 3mm in diameter. HIFU was focused on the blood vessels. The acoustic power was 250W; HIFU irradiating Mode was line scan (the length of the line: 10 mm; speed: 3 mm/s; irradiating time: 30s). In the experimental group, 0.03 ml/kg SonoVue was injected into the goat before HIFU irradiation,while normal saline was given to the control group. The goats were killed at 24h after HIFU irradiation, then goat liver tissues and blood vessels of target area were taken out. HE staining and Victoria's blue and Ponceau's staining of tissue section showed that the endothelial cells of blood vessels dropped off and became necrosed, and the continuity of blood vessels was interrupted. HIFU combined with SonoVue will damage large blood vessels on HIFU focus, but there is no evident discrepancy between the group with SonoVue and the group without SonoVue.
Animals ; Blood Vessels ; diagnostic imaging ; pathology ; Female ; Goats ; High-Intensity Focused Ultrasound Ablation ; methods ; Male ; Microbubbles ; Phospholipids ; pharmacology ; Sulfur Hexafluoride ; pharmacology ; Ultrasonic Therapy ; methods ; Ultrasonography

In order to research into the cytology mechanism of anti-virus action of total flavone of Scutellaria barbata (TFSB), the effects of TFSB on host cells membrane potential, Na(+)-K(+)-ATPase activity and membrane fluidity after parainfluenza virus type1 (PIV-1) infection were studied. The changes of membrane potential which was fluorescent labeled with DiBAC4(3) and its changes were measured by flow cytometer. Phosphorus determination method and spectrophotometry were used to measure the Na(+)-K(+)-ATPase activity of Hep-2 cells membrane after PIV-1 infection. Hep-2 cells membrane phospholipids were fluorescent labeled with NBD-C6-HPC and membrane fluidity was measured by confocal scanning laser microscope. The result demonstrated that post PIV-1 infection membrane potential decreased significantly and the membrane was in a state of hyperpolarization, Na(+)-K(+)-ATPase activity increased significantly and membrane fluidity decreased significantly. There was no apparent interfere effect of TFSB on the changes of membrane potential and Na(+)-K(+)-ATPase activity after PIV-1 infection, while membrane fluidity improved significantly. It was indicated that the cytology mechanism of PIV-1 infection might be related to membrane hyperpolarization, Na(+)-K(+)-ATPase activity increase and membrane fluidity decrease. TFSB can improve membrane fluidity and prevent the infection by protecting the cell membrane. But it is possible that the anti-PIV-1 mechanisms of TFSB had nothing to do with membrane potential and Na(+)-K(+)-ATPase activity.
Antiviral Agents ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Membrane ; drug effects ; Flavones ; isolation & purification ; pharmacology ; Humans ; Laryngeal Neoplasms ; pathology ; virology ; Membrane Fluidity ; drug effects ; Membrane Potentials ; drug effects ; Parainfluenza Virus 1, Human ; drug effects ; Phospholipids ; metabolism ; Plants, Medicinal ; chemistry ; Respirovirus Infections ; drug therapy ; Scutellaria ; chemistry ; Sodium-Potassium-Exchanging ATPase ; metabolism

OBJECTIVETo investigate the effect of synthetic drug QTY06 on chronic airway inflammation and mucoprotein expression induced by intratracheal (i.t) instillation of lipopolysaccharide (LPS).

METHODSChronic airway inflammation was induced by i.t instillation of LPS in rats. Phospholipids content and the number of leucocytes in bronchoalveolar lavage fluid (BALF), pathological and immunochemical changes were examined 3 weeks after LPS instillation. The effect of QTY06 on chronic airway inflammation was observed.

RESULTAfter treatment with QTY06, phospholipids in BALF was significantly increased, and the percentages of neutrophils and lymphocytes were decreased as well as the total number of leucocytes. Compared with the model group, pathological examination showed that tracheitis, bronchitis and pulmonary interstitial inflammation in QTY06 groups were significantly attenuated; epithelial damage was alleviated, infiltration of inflammatory cells reduced and the number of goblet cells decreased. QTY06 significantly decreased MUC5ac expression in trachea and bronchiole epithelium, and reduced the optical density and mucins area (%) as detected by image analysis in rats with chronic airway inflammation.

CONCLUSIONQTY06 can reduce and inhibit the chronic airway inflammation induced by LPS in rats, and increase the content of phospholipids in pulmonary surfactant and inhibit the hypersecretion of airway mucins.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; therapeutic use ; Bronchitis ; chemically induced ; drug therapy ; Bronchoalveolar Lavage Fluid ; chemistry ; Lipopolysaccharides ; Male ; Mucin 5AC ; secretion ; Phospholipids ; analysis ; Rats ; Rats, Sprague-Dawley ; Respiratory Mucosa ; drug effects ; secretion

Curcumin (from the rhizome of Curcuma longa) is well documented for its medicinal properties in Indian and Chinese systems of medicine where it is widely used for the treatment of several diseases. Epidemiological observations are suggestive that curcumin consumption may reduce the risk of some form of cancers and provide other protective biological effects in humans. These biological properties have been attributed to curcuminoids that have been widely studied for their anti-inflammatory, anti-angiogenic, antioxidant, wound healing and anti-cancer effects. In this study we have investigated on the effect of a curcumin phospholipid complex on mammary epithelial cell viability. HC11 and BME-UV cell lines, validated models to study biology of normal, not tumoral, mammary epithelial cells, were used to analyse these effects. We report that curcumin acts on STAT-3 signal pathway to reduce cell viability and increase apoptosis evaluated by the the amount of activated caspase 3. Further it reduces MAPK and AKT activations. JSI-124, a STAT-3 inhibitor (100 nM) was able to block the negative effect of curcumin on cell viability and caspase 3 activation. Finally the negative effect of cucumin on cell viability has been impaired in STAT-3i HC11, where STAT-3 protein was greatly reduced by shRNA-interference. These results indicate that curcumin presents a potential adverse effect to normal mammary epithelial cells and that it has a specific effect on signal trasduction in mammary epithelium.
Animals ; *Apoptosis ; Caspase 3/metabolism ; Cattle ; Cell Differentiation/drug effects ; Cell Survival/drug effects ; Curcuma/chemistry ; Curcumin/*adverse effects ; Enzyme Activation ; Epithelial Cells/cytology/*drug effects ; MAP Kinase Signaling System/physiology ; Mammary Glands, Animal/cytology ; Mice ; Oncogene Protein v-akt/metabolism ; Phospholipids/*pharmacology ; STAT3 Transcription Factor/antagonists & inhibitors/*physiology ; Signal Transduction/drug effects/*physiology ; Triterpenes/pharmacology

Nobiliside A (Nob A) liposomes were prepared. Its assay method of content and encapsulation efficiency (EE) were established, and hemolytic activity with Nob A solution in vivo and in vitro were compared. Preparative method, phospholipid content, ratio of phospholipid to cholesterol and ratio of drug to lipids were optimized by single factor exploration. According to the optimized results, 3 batches of Nob A liposomes were prepared, then high performance liquid chromatography coupled with evaporative light scattering detector (HPLC-ELSD) method was used to determine the content of Nob A and minicolumn centrifugation method to determine EE, transmission electron microscope was used to detect the morphology and laser scatter analysis to evaluate particle sizes of the liposomes. The hemolytic activity was studied both in vivo and in vitro. The results indicated that HPLC-ELSD method and minicolumn centrifugation method used in this study are simple, applicable and accurate for the determination of the content and EE of Nob A liposome respectively . Nob A liposomes have a high EE with spherical shape and uniform size by using the film ultrasonication technique. When the ratio of phospholipid to cholesterol was 2:1 and the ratio of Nob A to lipids was 1:40, the mean EE of Nob A liposomes was 95.7% and the mean diameter was 87.6 nm. Liposomes inhibited the hemolytic activity of Nob A in vivo and in vitro sharply. As for its low hemolytic activity in vivo and in vitro, Nob A liposomes are optimistic to be used by intravenous injection.
Animals ; Cholesterol ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Drug Compounding ; methods ; Drug Delivery Systems ; Female ; Hemolysis ; drug effects ; Liposomes ; chemistry ; pharmacology ; Male ; Materia Medica ; administration & dosage ; adverse effects ; isolation & purification ; Particle Size ; Phospholipids ; chemistry ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Saponins ; administration & dosage ; adverse effects ; isolation & purification ; Sea Cucumbers ; chemistry

To investigate the absorption mechanism of diammonium glycyrrhizinate (GL) for oral use in rat intestine as well as the effect of phospholipids on GL and its metabolite glycyrrhetic acid (GA), in situ single pass intestinal perfusion model and the rat single-pass intestinal perfusion with mesenteric cannulation model were used and the concentrations of GL and GA in perfusate and blood were determined by HPLC. The apparent permeability values (Papp) of GA with or without phospholipids are 7.98 and 5.73 cm x min(-1), respectively, whereas the permeability of GL had no significant statistical difference. The results showed that phospholipids can increase the absorption extent and speed of GA. This action can be used in the research and development of the new drugs of the glycyrrhiza.
Animals ; Chromatography, High Pressure Liquid ; Glycyrrhetinic Acid ; blood ; pharmacokinetics ; Glycyrrhizic Acid ; blood ; pharmacokinetics ; Intestinal Absorption ; drug effects ; Male ; Mesenteric Veins ; metabolism ; Perfusion ; Phospholipids ; pharmacology ; Portal Vein ; metabolism ; Rats ; Rats, Sprague-Dawley