• Journal of the Korean Society of Food Science and Nutrition
• /
• v.27 no.3
• /
• pp.518-524
• /
• 1998

Liposomes have been widely employed as biomembrane-mimetic system and drug-delivery system. In these applications, the low stability of liposomes has been the most serious problem. They have relatively short half-lives and easily lysed through interactions with biological components. This study was performed to investigate the effects of godulbaegi extracts on the fludity of phospholipid liposomes. We used dipalmitoyl phosphatidylcholine(DPPC) liposomes which make most stable liposomes among the other phosphatidylcholines. The thermograms of the DPPC liposomal bilayers incorporated with the hexane extract of godulbaegi(Ixeris sonchifolia H.) were obtained, and the enthalpy changes and the sizes of cooperative unit of the transition were calculated. The incorporation of the Ixeris sonchifolia H. into the liposomal bilayers effectively reduced the transition temperature at which the transition from gel state to liquid-crystalline state occurs, broadened the thermogram peaks, and reduced the ratio of van't Hoff to calorimetric enthalpies. These results indicate indicate that the godulbaegi extracts (Ixeris sonchifolia H.) have significant effects on the fluidity of biological membrance.

• Archives of Pharmacal Research
• /
• v.7 no.1
• /
• pp.17-22
• /
• 1984

Effects of total ginseng saponin, 20-S-protopanaxadiol saponin, 20-S-protopanaxatriol saponin and playcodon saponin on the osmotic behavior of liposomes were investigated by optical measurement. These saponins showed different activities on liposomal membrane, and cholesterol in liposomes was an important factor to this variation of saponin activities.

• YAKHAK HOEJI
• /
• v.35 no.1
• /
• pp.11-14
• /
• 1991

Ro09-0198, a cyclic peptide isolated from culture filtrates of Streptoverticillium griseove-rticillatum, induced platelet aggregation and serotonin release simultaneously. LDH release was not observed. Addition of peptide to rat platelet, loaded with $Ca^{2+}$ chelator quin-2, caused immediate rise in cytosolic free $Ca^{2+}$. Liposomal membrane containing phosphatidylethanolamine was damaged by peptide and released $^{45}Ca$ dose dependently.

• Journal of Pharmaceutical Investigation
• /
• v.41 no.4
• /
• pp.205-210
• /
• 2011

Genistein (GT), a major isoflavone found in soybeans, has a potent antioxidant effect that protects the skin from UV-induced damages and malignant melanoma. In order to enhance the cellular uptake of GT, liposome/Tat complexes were prepared by an electrostatic interaction of anionic liposome (DMPC/DCP, 9:1 in molar ratio) with Tat peptide (0.02 to 0.08 mole), one of the well-known cell penetrating peptide (CPP). As the amount of Tat increased, the size increased but the zeta potential decreased. In vitro release study with dialysis membrane elicited GT release from liposomal preparations in a controlled manner. The addition of Tat increased GT release, especially for the initial period. In the cellular uptake study by incubating B16 melanoma cells with various liposomal preparations containing GT, B16 melanoma cells demonstrated a time-dependent increase of drug accumulation. Compared to the aqueous GT suspension, intracellular uptake was substantially enhanced by anionic liposomal formulation and further increased by the complex formulation. Therefore, liposome/ Tat complex might be a good candidate for facilitating intracellular drug delivery.

• Archives of Pharmacal Research
• /
• v.15 no.4
• /
• pp.309-316
• /
• 1992

The effects of lipid peroxidation on the fluidity of the lipid bilayers of the human erythrocyte ghosts and egg-lecithin phospholipid liposomes have been studied. For the measurements of the peroxidation extent and the fluidity of the membranes, the thiobarbituric acid-reactive substances and the fluorescence depolarization of 1, 6-diphynyl-1, 3, 5-hexatriene labelled into the membrane were employed, respectively. The lipid peroxidation was performed in hypoxanthine/xanthine oxidase/ferrous ion, and hydrogen peroxide/ferrous ion systems. The results of these experiments show that both of the xanthine oxidase and hydrogen peroxide systems effectively. The lipid peroxidation decreased the fluidity of the membranes, especially at the very early stage of the peroxidation reaction. The decrease in the fluidity of membrane by the lipid peroxidation has been ascribed to the alteration of the polyunsaturated acyl chains of lipids and cross linkages among the membrane components. However, under drastic condition of lipid peroxidation, tdhe fluidity of the membrane rather increased possibly due to the deterioration of the membrane integrity by the peroxidation. Morphological change of the erythrocyte on peroxidation has also been observed.

• YAKHAK HOEJI
• /
• v.38 no.2
• /
• pp.131-139
• /
• 1994

Calcein-encapsulated small unilamellar vesicles of various lipid composition were prepared using the sonication technique, and their stabilities at $20^{\circ}C$ were examined by measuring calcein leakage from the liposomes. The fluidity of these liposomal bilayers was also investigated by measuring the fluorescence polarization of DPH labelled into the liposomes. The results showed that liposomes made of PC mixtures with different acyl chain length were very stable, which may be due to the formation of interdigitated bilayer structure. The addition of cholesterol further stabilized these PC liposomes. However, addition of cholesterol reduced the encapsulation efficiences of liposomes. The fluidity of the liposomes was significantly decreased by cholesterol in the liquid crystalline state, but not changed in the gel state. These results suggest that the enhanced stability of PC mixture liposomes may be ascribed to the formation of stable interdigitated bilayer structure. In membrane-mimetic and drug-delivery studies, vesicles made of mixtures of various phospholipids are recommended instead of addition of cholesterol to the phospholipid.

• Toxicological Research
• /
• v.6 no.1
• /
• pp.109-119
• /
• 1990

Ro09-0198, a cyclic peptide isolated from culture filtrates of Streptoverticillium griseoverticillatum, induced lysis of erythrocytes. Ro-09-0198-induced hemolysis was temperature-dependent and the sensitivity of hemolysis differed greatly among animal species. Preincubation of the peptide with phosphatidylethanolamine reduced the hemolytic activity, whereas other phospholipids present in erythrocytes in nature had no effect. A study of the structural requirements on phosphatidylethanolamine necessary for interaction with the peptide indicates that Ro09-0198 recognizes strictly a particular chemical structure of phosphatidylethanolamine: dialkylphosphoethanolamine as well as 1-acylglycerophosphoethanolamine showed the same inhibitory effct on hemolysis induced by Ro09-0198 as diacylphosphatidyl-ethanolamine, whereas phosphoethanolamine gave no inhibitory effect. Neither phosphatidyl-N-monomethylethanolamine nor alkylphosphopropanolamine had an inhibitory effect. Proton resonances of the peptide were observed in dimethyl sulfoxide solution in the presence of 1-dodecanoyl-sn-glycerophosphoethanolamine. This peptide caused permeability increase and aggregation of liposomes containing phosphatidylethanolamine. A glycerol backbone and a primary amino group of phosphatidylethanolamine are necessary for interaction with Ro09-0198 to cause membrane damage. Ro09-0198 induced a selective permeability change on liposomes. Glucose and umbelliferyl phosphate were effluxed significantly, but sucrose was only slightly permeable and inulin could not be released. Platelet aggregation and serotonin release simultaneously induced by Ro09-0198. Addition of peptide to rat platelet, loaded with the fluorescent $Ca^{++}$ chelator quin-2, caused immediate rise in cytosolic free $Ca^{++}$ to liposomal membrane containing phosphatidylethanolamine was observed dose dependently.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.22 no.3
• /
• pp.323-327
• /
• 1993

The effect of soyasaponin on the liposomal phospholipid membrane was investigated by differential scanning calorimetry (DSC). Soyasaponins were obtained and the enthalpy changes and the sizes of cooperative unit of the transition were calculated. The thermograms of L-$\alpha$-dimyristoyl phosphatidylcholine (DMPC) incorporated with soyasaponin showed that the phase transition temperature was significantly lowered and the peak was broadened. This was attributed to the possibility that incorporation of soyasaponin into the lipid bilayers reduced the cooperative unit of phospholipid bilayers. These results indicate soyasaponin might have significant effect on the fluidity of biological membrane.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1996.04a
• /
• pp.286-286
• /
• 1996

In order to elucidate the mechanism of action of transdermal absorption-enhancing compounds, i.e., pyrrolidone derivatives (2-pyrrolidone, 1-methyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, 1,5-dimethyl-pyrrolidone and 5-methyl-2-pyrrolidone), multilamellar liposome was prepared from the simulated stratum corneum lipid and employed as a model system for the barrier function of the stratum corneum. The liposomal membrane of the stratum corneum lipid liposome (SCLL) behaves as an osmometer and has an excellent barrier function. In addition, its phase transition temperatures are similar to those of human stratum corneum intercellular lipid region. Therefore, SCLL seems to be a useful skin model. To estimate the barrier function of SCLL, the osmotic behavior of SCLL was measured in the presence of pyrrolidone derivatives and the effect on the phase transition temperature of SCLL was also investigated using differential calorimetry. Above a certain concentration (MLAC), enhances perturb the barrier function of the liposome. The relationship between MLACs and the partition coefficient of the pyrrolidone derivatives was observed; the greater the partition coefficients, the smaller the MLAC. This suggests that the more hydrophobic enhancers penetrate into the lipid layer more easily and reduce the barrier function of membrane more effectively. The results of differential scanning thermograms of the SCLL suggest that the pyrrolidone derivatives had incorporated into the lipid layer in the liposome and increased the fluidity of the lipid layer in the liposome. Such activity might have some correlation with the transdermal absorption-enhancing activity these compounds.

• Journal of Life Science
• /
• v.12 no.2
• /
• pp.144-150
• /
• 2002

This experiment was designed to investigate the antioxidant effects of Chrysanthemum coronarium L. (CC) fractions on the liposomal phospholipid membranes. The sample CC was extracted and fractionated into five different types, methanol (CCMM), hexane (CCMH), ethylacetate (CCMEA), butanol (CCMB), and aqueous (CCMA) fractions. The antioxidant activities of CC fractions in oxidized dilinoleoylphosphatidylcholine (DLPC) liposomes were examined by spectrophotometry measuring conjugated dienes. The oxidation indices of five CC fractions exhibited weaker antioxidant activities than that of BHT in oxidized DLPC liposomes, however, showing much similar antioxidant activities of $\alpha$-tocopherol in the oxidized DLPC liposomes, which is known as a potent antioxidant. Among CC fractions, CCMM and CCMA in oxidized DLPC liposomes showed rather effective than $\alpha$-tocopherol after 2 h. These results strongly indicate that bioactive substances in CC fractions have a kind of function as potent antioxidants against biomembrane oxidation.