Determination of 22 phospholipids in serum by ultra performance liquid chromatography-tandem mass spectrometry / 中华劳动卫生职业病杂志

Objective: To establish ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of 22 phospholipids in serum. Methods: In September 2022, Using synthetic non endogenous phospholipids as internal standard, phospholipids in serum were extracted by methanol-dichloromethane (2∶1, V/V) protein precipitation method. Chromatographic separation was achieved on an ACQUITY UPLC BEH shield RP18 column, and the mobile phase was methanol/water (5∶95, V/V) containing 10 mM ammonium formate and methanol. Detection was performed in multiple reaction monitoring mode with ion mode switching. And the method was applied by analyzing phospholipids in the serum of coal workers' pneumoconiosis patients. Results: The 22 phospholipids showed good linear relationships in their respective concentration ranges and the correlation coefficients were higher than 0.990. The spiked recoveries of the 22 phospholipids were 81.03%-121.63% at the three spiked levels. The intra-assay were less than 14.52%, and the inter-assay were less than 15.00%. Conclusion: The method with the advantages of simplicity, stability and high sensitivity, and it can be used for the analysis of phospholipids in serum.

The role of lipids and fatty acid metabolism in the development of prostate cancer

The reprogramming of lipid metabolism and signaling pathways is the central aspect of cancer biology. It is hypothesized that tumor cells can alter the lipid spectrum in order to fulfill their metabolic requirements. Furthermore, they can alter potential tumors and suppressive mechanisms in which lipids' involvement is essential. Recently, more attentions have been given on the alteration of lipid metabolism during prostate cancer development, and investigations have shown unique regulation of "de novo" lipid synthesis in cancer cells. Cancer cells often use newer pathways and enzymes to simplify the synthesis of fatty acids, and the newly synthesized lipids affect cellular processes, which impacts cancer cell proliferation and survival outcomes. Herein, we aimed to study the influence of lipid profile alterations on the development of prostate cancer. We found that the total amounts of lipids and phospholipids were increased within tissues from men with the malignant prostate tumor as compared with the benign prostate tissue. Significant changes were also observed in the composition of saturated and unsaturated fatty acids within the malignant tumor tissues. Intensification of lipid peroxidation has also been observed in malignant prostate tumors compared to benign prostate tumors. Collectively, these findings further highlights the fact that lipid and fatty acids play unique regulatory roles in the cellular development of prostate malignant transformation.

Comparative Studies on the Physicochemical Characteristics and Lipid Contents of Desert Date (Balanites aegyptiaca (L.) Del) Kernel and Pulp Oils

Aims: This work is aimed at investigating physicochemical parameters and compositions of fatty acid, phospholipid and sterol of desert date (Balanites aegyptiaca) kernel and pulp. Study Design: Balanites aegyptiaca fruit is one of the oldest feed-stocks in Africa of which little or no attention has been given to it. The plant plays a diverse cultural and traditional role in different societies. Therefore, it is very important to explore more about the chemical composition of the kernel and pulp oils of Balanites aegyptiaca; since it is currently attracting considerable research interest as a result of its diverse beneficial properties. Methodology: The physicochemical parameters, fatty acids, phospholipids and phytosterols of B. aegyptiaca seed and pulp oils have been analyzed and compared with the standards and that of conventional oil for easy assessment of their suitability for nutritional and industrial applications. Results: The results of some physicochemical parameters of kernel and pulp oils were acid value (26.35 and 15.60 mg KOH/g), peroxide value (3.82 and 5.90 meq/kg), saponification value (162.40 and 198.60 mg KOH/g), iodine value (55.20 and 142.50 mg of I/100 g), specific gravity (0.93 and 0.92), kinematic viscosity (2.12 and 1.65 St) and refractive index (1.41 and 1.39), respectively. The most concentrated fatty acids were palmitic acid (14.53%) < linoleic acid (35.65%) < oleic acid (38.27%) for the kernel oil while that of pulp oil were linolenic acid (8.21%) < oleic acid (16.80%) < palmitic acid (32.70%) < linoleic acid (33.56%). Arachidic, behenic, lignoceric and myristic acids were all present in small quantities with none of them recording up to 1.0% in either of the samples. Caprylic, capric and lauric acids were determined but not detected in both oils. The fatty acid composition of kernel and pulp oils contained a healthy mixture of all the types of saturated and unsaturated fatty acids. The value of polyunsaturated/saturated index (P/S) which is associated to the impact on human health was higher in the pulp oil (2.47). Phosphatidylcholine had the highest content in both oils that is 75.99 and 25.88 mg/100 g, respectively. The total values of phytosterols for kernel and pulp oils were 85.00 and 9.87 mg/100 g, respectively. Conclusion: Balanites aegytiaca kernel and pulp oils have the potential to substitute several materials used in manufacturing oil in the chemical and pharmaceutical industries. However, in order to extend usage, these oils should be refined in order to improve the colour and taste.

Advances in lipid metabolism during Chlamydia infection / 中华微生物学和免疫学杂志

Chlamydia, a gram-negative obligate intracellular pathogen, is a major cause of human reproductive tract, eye and respiratory tract infections. It replicates in a special membrane-binding chamber called inclusion and survives in the host′s hostile intracellular environment through secreting effectors, but requires host-derived lipids to grow and develop in the cells. Emerging evidences suggest that Chlamydia has evolved a variety of strategies to meet its lipid needs by interacting with host cell compartments and redirecting the transport pathway to its intracellular niche. This paper briefly described the pathway for obtaining host lipids and the mechanism of lipid metabolic during Chlamydia infection.

2,3,5,4'-Tetrahydroxystibane-2-O-β-D-glucoside induces liver injury by disrupting bile acid homeostasis and phospholipids efflux / 中国中药杂志

Polygonum multiflorum is a traditional Chinese herbal medicine and has many biological activities such as hair-blacking, anti-atherosclerosis, anti-inflammatory and anti-aging. However, the liver injury induced by P. multiflorum has aroused wide attention in recent years. 2,3,5,4'-tetrahydroxystibane-2-O-β-D-glucoside(TSG) is a main component of P. multiflorum, but the role of TSG in inducing liver injury is unclear. The aim of present study was to evaluate TSG's potential liver injury and effects on bile acid homeostasis and phospholipids efflux. C57 BL/6 J mice received intraperitoneal administration of 400 mg·kg~(-1) of TSG daily for 15 days, and then biochemical indexes of liver injury and changes of phospholipid content were detected. The changes of bile acid compositions were detected by LC-MS/MS. The results showed TSG 400 mg·kg~(-1) significantly increased the content of serum total bile acid(TBA) and alkaline phosphatase(ALP). Elevated free bile acid levels were observed in TSG-treated groups, including β-muricholic acid(β-MCA), ursodeoxycholic acid(UDCA), hyodeoxycholic acid(HDCA), chenodeoxycholic acid(CDCA), deoxcholic acid(DCA) in serum and β-MCA, CDCA in liver. TSG inhibited the protein expression of farnesoid X receptor(FXR) and down stream bile salt export pump(BSEP), which may result in the accumulation of bile acid. TSG also inhibited the expression of 25-hydroxycholesterol-7 alpha-hydroxylase(CYP7 B1), which may disturb the alternative pathway for bile acid synthesis. In addition, intraperitoneal injection of TSG 400 mg·kg~(-1) significantly decreased the content of phospholipids in bile. The research showed that TSG significantly inhibited the expression of multidrug resistance protein 2(MDR2) and destroyed the regular distribution of MDR2 on the bile duct membrane of liver. In vitro results showed that the IC_(50) of TSG on HepG2 cells was about 1 500 μmol·L~(-1) and TSG at 500 μmol·L~(-1)(for 24 h) could destroy the distribution of MDR2 on the bile duct membrane of liver. In conclusion, TSG induced liver injury by disrupting bile acid homeostasis and phospholipids efflux.

Different preparations of magnolol: Preparation, characterization and pharmacokinetics comparative study in SD rats / 中草药

Objective: To prepare magnolol solid dispersions (Mag-SD), magnolol phospholipids complex (Mag-PC) and magnolol solid lipid nanoparticles (Mag-SLN), and compare their effects on the pharmacokinetics in vivo. Methods: Solvent evaporation method was used to prepare Mag-SD and Mag-PC. Their existential state of Mag in Mag-SD and Mag-PC were analyzed by X-ray power diffraction (XRPD). High pressure homogenization method was employed to prepare Mag-SLN, its particle size and Zeta potential were also studied. The dissolution in vitro of Mag-SD, Mag-PC and Mag-SLN were also studied compared to magnolol suspension. SD rats in each group were administered intragastrically with magnolol, Mag-SD, Mag-PC and Mag-SLN, respectively. The concentration of magnolol in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. The pharmacokinetic behavior and bioavailability of magnolol, Mag-SD, Mag-PC and Mag-SLN were also compared. Results: The results of XRPD indicated that magnolol showed an amorphous state in Mag-SD and Mag-PC. The average particle size and Zeta potential of Mag-SLN was (161.37 ± 3.77) nm and (-29.16 ± 1.83) mV, respectively. The results of dissolution in vitro indicated that the cumulative dissolution of magnolol was 30.6% within 12 h. Mag-SD, Mag-PC and Mag-SLN enhanced its cumulative dissolution to 96.3%, 76.4% and 45.9%, respectively. The results of pharmacokinetics in vivo showed that Cmax, AUC0-t and AUC0-∞ of Mag-SD, Mag-PC and Mag-SLN were enhanced greatly compared to magnolol suspension. Mag-PC, Mag-SD and Mag-SLN increased its Cmax from (429.67 ± 53.12) ng/mL to (533.62 ± 59.01), (721.73 ± 103.44) and (1 063.21 ± 108.22) ng/mL, respectively. The bioavailability of Mag-SD, Mag-PC and Mag-SLN were enhanced to 1.38, 2.12 and 3.45 times, respectively. Conclusion: Mag-SD, Mag-PC and Mag-SLN could promote the absorption of magnolol in SD rats notably. In addition, Mag-SLN could give a better effect on the bioavailability.

Role of crotoxin in coagulation: novel insights into anticoagulant mechanisms and impairment of inflammation-induced coagulation

Snake venom phospholipases A2 (svPLA2) are biologically active toxins, capable of triggering and modulating a wide range of biological functions. Among the svPLA2s, crotoxin (CTX) has been in the spotlight of bioprospecting research due to its role in modulating immune response and hemostasis. In the present study, novel anticoagulant mechanisms of CTX, and the modulation of inflammation-induced coagulation were investigated. Methods: CTX anticoagulant activity was evaluated using platelet poor plasma (PPP) and whole blood (WB), and also using isolated coagulation factors and complexes. The toxin modulation of procoagulant and pro-inflammatory effects was evaluated using the expression of tissue factor (TF) and cytokines in lipopolysaccharide (LPS)-treated peripheral blood mononuclear cells (PBMC) and in WB. Results: The results showed that CTX impaired clot formation in both PPP and WB, and was responsible for the inhibition of both intrinsic (TF/factor VIIa) and extrinsic (factor IXa/factor VIIIa) tenase complexes, but not for factor Xa and thrombin alone. In addition, the PLA2 mitigated the prothrombinase complex by modulating the coagulation phospholipid role in the complex. In regards to the inflammation-coagulation cross talk, the toxin was capable of reducing the production of the pro-inflammatory cytokines IL-1β, IL-6 and TNF-α, and was followed by decreased levels of TF and procoagulant activity from LPS-treated PBMC either isolated or in WB. Conclusion: The results obtained in the present study recognize the toxin as a novel medicinal candidate to be applied in inflammatory diseases with coagulation disorders.(AU)

Lipoprotein(a): An independent, genetic, and causal factor for cardiovascular disease and acute myocardial infarction

Lipoprotein(a) [Lp(a)] is a circulating lipoprotein, and its level is largely determined by variation in the Lp(a) gene (LPA) locus encoding apo(a). Genetic variation in the LPA gene that increases Lp(a) level also increases coronary artery disease (CAD) risk, suggesting that Lp(a) is a causal factor for CAD risk. Lp(a) is the preferential lipoprotein carrier for oxidized phospholipids (OxPL), a proatherogenic and proinflammatory biomarker. Lp(a) adversely affects endothelial function, inflammation, oxidative stress, fibrinolysis, and plaque stability, leading to accelerated atherothrombosis and premature CAD. The INTER-HEART Study has established the usefulness of Lp(a) in assessing the risk of acute myocardial infarction in ethnically diverse populations with South Asians having the highest risk and population attributable risk. The 2018 Cholesterol Clinical Practice Guideline have recognized elevated Lp(a) as an atherosclerotic cardiovascular disease risk enhancer for initiating or intensifying statin therapy.

Comparative study of preparation, characterization and pharmacokinetics of three preparations of osthole / 中草药

Objective: To prepare osthole solid dispersions (Ost-SD), osthole phospholipids complex (Ost-PC), and osthole nanosuspensions (Ost-NS), and compare their effects on the pharmacokinetics in SD rats in vivo. Methods: Solvent evaporation method was used to prepare Ost-SD and Ost-PC. Their existential state of Ost in Ost-SD and Ost-PC were analyzed by X-ray power diffraction (XRPD). High pressure homogenization method was employed to prepare Ost-NS, its particle size and Zeta potential were studied. The dissolution in vitro of Ost-SD, Ost-PC, and Ost-NS were also studied compared to Ost suspension. SD rats in each group were ig administered with Ost, Ost-SD, Ost-PC, and Ost-NS, respectively. The concentration of Ost in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. The pharmacokinetic behavior and bioavailability were also been compared. Results: The results of XRPD indicated that Ost showed an amorphous state in Ost-SD and Ost-PC. The average particle size and Zeta potential of Ost-NS were (161.37 ± 3.77) nm and (-29.16 ± 1.83) mV, respectively. The results of dissolution in vitro indicated that the dissolution of Ost was improved greatly by Ost-SD, Ost-PC, and Ost-NS. The results of pharmacokinetics in vivo showed that Cmax, AUC0~t and AUC0~∞ of Ost-SD, Ost-PC, and Ost-NS were enhanced greatly compared to Ost. The bioavailability of Ost-SD, Ost-PC,and Ost-NS were enhanced to 165.92%, 138.46%, and 259.35%, respectively. Conclusion: Ost-SD, Ost-PC, and Ost-NS can enhance the bioavailability of Ost in SD rats notably. In addition, Ost-NS can give a better effect.

Preparation, characterization and pharmacokinetics of dihydromyricetin phospholipids complex loaded by nanostructured lipid carriers / 中草药

Objective: To prepare dihydromyricetin (DMY) phospholipids complex (DMY-PC) and its nanostructured lipid carriers (DMY-PC-NLC), and carry out in vitro and in vivo evaluation. Methods: DMY-PC was prepared by solvent evaporation method. High pressure homogenization method was used to prepare DMY-PC-NLC. Orthogonal test was employed to optimize the ratio of solid/liquid lipid, dose of lipids materials, dose of DMY-PC and the concentration of emulsifier of poloxamer. The lyophilized powder of DMY-PC-NLC was prepared with 5% of mannitol as protective agent. The comparation of in vitro release and pharmacokinetics between DMY-PC and DMY-PC-NLC was also studied. Results: DMY was in an amorphous state in DMY-PC. The results of 1HNMR showed that the structure of DMY was not changed. The optimized prescription of DMY-PC-NLC determined by orthogonal test was as follow: The ratio of solid/liquid lipid was 5:1, dose of lipids materials was 325 mg, dose of DMY-PC was 45 mg and the concentration of emulsifier of poloxamer was 0.9%. The average size, Zeta potential, entrapment efficiency and drug loading of DMY- PC-NLC was (197.25 ± 4.42) nm, (-18.2 ± 2.1) mV, (71.68 ± 1.36)% and (3.94 ± 0.24)%, respectively. The in vitro release model was accord with Weibull model and the equation was lnln(1-Mt/M∞)=0.700 1 lnt-1.954 1 (r = 0.971 4). The relative bioavailability of DMY-PC and DMY-PC-NLC were enhanced to 1.63 and 3.22 times compared to DMY, respectively. Conclusion: Compared with DMY-PC, the absorption was promoted by DMY-PC-NLC in further, and the bioavailability of DMY was enhanced effectively.

Two kinds of luteolin solid dispersion: Preparation, characterization, and pharmacokinetic behaviors in SD rats in vivo / 中草药

Objective To prepare luteolin solid dispersions (Lut-SD) and luteolin phospholipids complex solid dispersions (Lut-PC-SD), and compare the effects of two kinds of solid dispersions on the bioavailability in vivo. Methods PVP K30 was employed as carrier, and solvent evaporation method was used to prepare Lut-SD and Lut-PC-SD. Their existential state of luteolin in solid dispersions was analyzed by X-ray power diffraction (XRPD). The solubility and dissolution rate were also studied. SD rats in each group were administered intragastrically with Lut, Lut-SD, and Lut-PC-SD, respectively. Their blood samples were collected at different time intervals. Diosmetin was used as internal standard, the concentration of Lut in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. Results The results of XRPD indicated that Lut showed an amorphous state in Lut-SD and Lut-PC-SD. The solubility of Lut was enhanced from (61.09 ± 0.09) μg/mL to (365.33 ± 0.38) μg/mL and (401.14 ± 0.19) μg/mL by Lut-SD and Lut-PC-SD, repectively. The dissolution of Lut was also improved greatly by the two kinds of solid dispersions. Compared to Lut, the bioavailability of Lut-SD and Lut-PC-SD was enhanced to 150.10% and 204.52%, repectively. Conclusion Lut-SD and Lut-PC-SD both could enhance the bioavailability of Lut in SD rats notably. In addition, Lut-PC-SD could give a better effect.

The synergistic mechanisms of oxidized phospholipids and lipoprotein-associated phospholipase A2 associated with Lp ( a ) in promoting atherosclerosis / 中华检验医学杂志

Lipoprotein ( a ) [ Lp ( a ) ] is considered a causal risk factor for the formation and development of atherosclerosis ( AS).High plasma levels of Lp ( a) is recognized as a predictor of coronary heart disease. However, the pathogenic mechanisms of Lp ( a ) are still unknown. Recent studies demonstrated that a key role in the proatherogenic effects of Lp ( a ) may be linked to its oxidized phospholipids ( OxPL) content.Lipoprotein-associated phospholipase A 2 ( Lp-PLA2 ) is another important factor in Lp( a) functionality.OxPL are hydrolyzed by Lp-PLA2 into lysophosphatidylcholine ( lyso-PC) and oxidized free fatty acid(OxFFA), which are important inflammatory factors on promoting the occurrence and development of AS.The present review article describes Lp-PLA2 hydrolyzing OxPL associated with Lp (a). The process induces inflammatory factors , which promote development of AS .OxPL and Lp-PLA2 can be used as new targets of cardiovascular diseases , which have clinical application value to predict potential cardiovascular diseases .

Study on Quantitative Structure-Retention Relationships of Microemulsion Electrokinetic ChromatographyUsing Phospholipids as Surfactant / 分析化学

Some new types of microemulsion using phospholipids as the main surfactant were prepared for electrokinetic chromatography and the quantitative structure-retention relationship of neutral solutes in these microemulsion electrokinetic chromatography (MEEKC) systems was studied by solvation parameters model.By using dynamic coating capillary, and with dimethyl sulfoxide (DMSO) and dodecyl benzene as the marker of electroosmotic flow and microemulsion droplets, a total of 17 kinds of stable microemulsions containing soybean phospholipids or other surfactants were prepared and the linear salvation energy relationship equations were developed for these MEEKC systems with 26 small neutral compounds.The coefficients of linear solvation energy relationship (LSER) equations were used to evaluate the similarity of two MEEKC systems.Results indicated that LSER characteristics of phospholipids-MEEKC systems were similar to those of other microemulsion systems.The volume and hydrogen bond basicity of solutes were mostly contributed to the retention in MEEKC.The different types and concentration of oil phase had no evident influence on the retention.

Lipid corneal degeneration after trabeculectomy with mitomicin 0. 02%

ABSTRACT One patient with a history of trabeculectomy with Mitomicin C 0.02%, but no history of systemic disorders, exhibited unilateral corneal lipid infiltrates, together with deep stromal vascularization. She was treated with a bevacizumab injection and penetrating keratoplasty. No sign of recurrence was noted after one year post-operative.

RESUMO Um paciente com história de trabeculectomia com Mitomicina C 0,02%, sem doenças sistêmicas pré-existentes, apresentou infiltrado lipídico corneano unilateral associado à vascularização intraestromal profunda. Injeção subconjuntival de Bevacizumabe foi realizada e posterior ceratoplastia penetrante. Não houve sinais de recorrência em um ano.

Total salinity stress on physico-chemical characterization of lecithin isolated from soya bean oil seeds grown in the coastal region of south, India.

Phospholipid is very essential in the balanced diet. The vegetarian people in the coastal area are habitant of using edible oil seeds as daily food grains. Salinity of water during cultivation decreases the accumulation of oil content (12-15%) in seeds. Present experiment was focused on total salinity and ionic stress on physiochemical characterization of extracted lecithin from soya bean oil under saline and non-saline cultivations. The experiment proves that the percentage of phospholipids in oil and lecithin is decreased by 1.02% and 8.08%, respectively under saline cultivation. The phospholipids of the lecithin were qualitatively identified by thin-layer chromatography (TLC) and high performance of liquid chromatography (HPLC). The Rf values for phosphatidyl-ethanolamine (PE), phosphatidyl-serine (PS), phosphatidyl-inositol (PI) and phosphatidyl-choline (PC) of samples were well related to the standard. HPLC spectrum is well resolved and the retention time (RT) is correlated the standard with high precision. Quantisation of phospholipids shows a variation in the average percentage of PC, PI, PS and PE as 17.925, 9.125, 5.9, 15.1 for saline cultivation and 22.25, 12.025, 8.525, 18.975 for non-saline cultivation. Average decrease in the percentage in saline cultivation is due to the total salinity and ionic (Na+Cl-) stress of water.

Direct Analysis of Phospholipids in Biological Tissues Using Internal Exlractive Electrospray Ionization Mass Spectrometry / 分析化学

Phospholipids and their metabolites play an important role in a variety of cellular processes including cell-cell adhesion, cell growth and differentiation, apoptosis, phagocytosis as well as storage of energy. In this study, the phospholipid composition of cancer tissue and adjacent normal tissue from humans and animals were analyzed by internal extractive electrospray ionization mass spectrometry ( iEESI-MS ) . Extractive solvent at high voltage (+5. 5 kV) was injected into tissue samples using a fused silica capillary at a flow rate of 0. 5-1 μL/min, producing fine charged droplets containing analytes of tissue samples at the tip of the sample. Charged droplets were directly sampled to the atmospheric inlet of a mass spectrometer. Out of 21 different ratios of CH3 OH ∶H2 O solvent mixture, the ratio CH3 OH ∶ H2 O=30∶70 ( V/V ) showed the optimal phospholipids extraction and visibility in MS. A large number of phospholipids from different tissue samples ( such as cancer tissue and adjacent normal tissue of lung cancer, esophageal cancer tissue, pork, beef, porcine heart and porcine lung) were obtained simultaneously by iEESI-MS analysis. The experimental results demonstrated that iEESI-MS was characterized by minimal sample pretreatment, low sample consumption, and rapid analysis ( the analysis time per sample was less than 1 min) , and the selectivity and sensitivity of iEESI-MS could be improved by choosing proper solvent. Importantly, the experimental results provided new information for further studies of phospholipids in biological tissues.

The absorption of baicalin phospholipid complex in rat stomach and intestine / 中国药学杂志

OBJECTIVE: To study the absorption kinetics of baicalin phospholipid complex in rats stomach and intestine. METHODS: Using rats in vivo stomach and intestinal absorption mode, the drug concentration by in situpefusion in rats were determined by HPLC to comparise the stomach, whole intestine absorption and metabolism characteristics among baicalin, baicalin phospholipid complex and physical mixture, and the sub-bowel absorption and metabolism characteristics of baicalin phospholipid complex. RESULTS: The percentage of per hour absorpion in the stomach of baicalin, baicalin phospholipid complex and physical mixture shows little difference among them. The whole intestine absorption of baicalin phospholipid complex was better than the baicalin and physical mixture, which is (2 940.87±1.45) μg,(1 373.23±3.21) μg, (992.66±3.65) μg, respectively. Baicalin phospholipid complex has extensive absorption window in the whole intestine and duodenum is the best. The absorption percentage of duodenum, jejunum, ileum and colon is 51.81%, 32.29%, 29.56%, 11.80%,respectively. CONCLUSION: Baicalin phospholipid complex can significantly enchance absorption of baicalin in rat gastrointestinal tract.

Preparation and characterization of cucurbitacin B phospholipids complex and its in vitro antitumor activity / 中草药

Objective: To prepare cucurbitacin B phospholipids complex (CuB-PLC) and evaluate its physicochemical properties and in vitro antitumor activity. Methods: CuB-PLC was prepared using solvent evaporation method and optimized by Box-Behnken design. The oil-water partition coefficient, particle size, and morphology of CuB-PLC were investigated; X-ray diffraction (XRD) spectroscopy and infrared (IR) spectroscopy were used to analyze the formation machenism of CuB-PLC. MTT method was used to determine the in vitro antitumor activity of CuB-PLC. Results: The optimal formulation protocol for CuB-PLC was as follows: Tetrahydrofuran was taken as the reaction medium, phospholipids-cucurbitacin B molar ratio, reaction concentration of cucurbitacin B, reaction temperature and time were 1:1, 1.5 mg/mL, 60℃, and 3 h, respectively. The complex rate and particle size for the optimized CuB-PLC was 97.15% and (521.30 ± 10.50) nm, and the polydispersity index (PDI) was 0.133 2 ± 0.024 0. MTT experiments showed that the half of the HepG-2 cell proliferation inhibition concentration (IC50) values of CuB and CuB-PLC were 42.55 and 27.61 μmol/L. Conclusion: CuB-PLC is successfully developed under the optimized protocol, possessing high complex rate, and enhanced solubility in water, and the inhibition on HepG-2 cell proliferation is significantly enhanced, which provides the reference for the further research of CuB.

Composite phospholipids liposomes: research advances / 国际药学研究杂志

Liposomes are a kind of common drug delivery system in pharmaceutics. They can be used as the dosage form of water insoluble drugs to improve their bioavailability. However, these traditional liposomes have some disadvantages such as low encapsulation efficiency, instability and drug leakage in a long term of storage, which have limited the development of dosage form products based on liposomes. Recently, a novel kind of liposomes, namely composite phospholipids liposomes, has been devel-oped. Compared to traditional liposomes, composite phospholipids liposomes have a very promisingly application prospect due to their advantages including higher encapsulation efficiency and drug-loading efficiency, good stability and no drug leakage. This article re-viewes the research progress in the composite phospholipids liposomes, including their composition, structure, preparation method, function property and recent application in pharmaceutics.

Efeito da administração In Bolus da heparina sódica no remodelamento de partículas lepoprotéicas associadas ao transporte reverso do colesterol / In bolus administration the effect of heparin sodium in remodeling lepoprotéicas particles associated with reverse cholesterol transport

Introdução: as doenças cardiovasculares acometem milhares de pessoas no mundo. Destas, a doença arterosclerótica está entre as de maior morbimortalidade. Para a avaliação da necessidade de intervenções hemodinâmicas e/ou revascularização miocárdica, há a necessidade da realização do cateterismo (CATE), procedimento de imagem indicado para evidenciar pontos de obstrução e determinar a melhor estratégia cirúrgica. Para a realização do CATE utiliza-se heparina sódica (5000 UI) in bolus. Atualmente, sabe-se que a heparina interfere no remodelamento de partículas lipoproteicas por liberação da lipoproteína lipase (LPL) e da lipase hepática (LH), essa ação pode alterar o transporte reverso do colesterol (TRC), em função de modificações no metabolismo das lipoproteínas. Métodos: foram selecionados por conveniência 20 pacientes, 10 do sexo masculino e 10 do sexo feminino, ambos os sexos, entre 45 e 73 anos, admitidos no Hospital Ana Neri, submetidos à cineangiocoronariografia (CATE)...

Introduction: cardiovascular diseases affect thousands of people worldwide. Of these, the atherosclerotic disease is one of the most morbidity and mortality. To evaluate the need for hemodynamic interventions and / or CABG, the catheterization (CATE) is performed, an imaging procedure to evidence obstruction and to determine the best surgical strategy. To perform CATE, is necessary to use in bolus sodium heparin (5000 IU). Currently, it is known that heparin interferes with the remodeling of the lipoprotein particles by releasing lipoprotein lipase (LPL) and hepatic lipase (HL), this action may alter the reverse cholesterol transport (TRC), by changes in lipoprotein metabolism. Methods: were selected by convenience 20 patients, 10 male and 10 female, both gender, between 45 and 73 years old, admitted to the Hospital Ana Neri, who underwent coronary angiography (CATE)...