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[Effect of ginseng ginsenosides on phase transitions of dipalmitoylphosphatidylcholine membranes].

The influence of dammaran triterpene glycosides (ginsenosides Rb1 and Rg1) from Panax Ginseng C.A. Meyer and their aglycones on the phase transfers of multilayer vesicles of dipalmitoylphosphatidyl choline was studied. Ginsenosides Rb1 and Rg1 and aglycone 20(S) protopanaxatriol insignificantly modified the lipid gel phase and only in concentrations close to the equimolar ones insignificantly damaged the lipid covers and decreased the size of the cooperative unit. Aglycone 20(S) protopanaxadiol (PD) induced the formation of the second phase with a more solid cover of the lipids but a lower size of the cooperative unit by comparison with that of the pure lipid. The presence of cholesterol in an amount up to 5 mol per cent slightly influenced the interaction of the agents with the gel phase except for PD. In the presence of cholesterol PD did not induce the formation of the two phases and in an amount of 100 mol per cent eliminated the major transfer. The study suggested that PD interacted with the gel phase and did not penetrate into the bilayer deeper than the glycerol skeleton of the lipid molecule.

1,2-Dipalmitoylphosphatidylcholine↗

Effects of triterpenoid glycosides of the dammaran series and their aglycons on phase transitions of dipalmitoylphosphatidylcholine.

The effects of triterpenoid glycosides from Korean red ginseng Panax C.A. Meyer and their aglycons on the phase transitions of model DPPC membranes were studied by microcalorimetry. Glycosides Rb1, Rg1, 20(S) protopanaxadiol only slightly interacted with the DPPC gel phase and caused no formation of new phases. At concentrations close to equimolar values, the glycosides slightly disturbed the packing of lipids and induced the formation of the second phases with more dense lipid packing but smaller sizes of the cooperative domains as compared with pure lipid. Cholesterol (3%) produced no effect on the DPPC interaction with Rb1, Rg1 and panaxatriol but affected the DPPC interaction with panaxadiol. At equimolar panaxadiol/DPPC ratio and in the presence of 3% cholesterol, panaxadiol completely eliminated the main transition.

1,2-Dipalmitoylphosphatidylcholine↗

Iscom, a delivery system for parenteral and mucosal vaccination.

The iscom is a supramolecular spherical structure, about 40nm in diameter, built up by structure-forming and immunomodulating quillaja triterpenoids, lipids and antigens. Iscoms with a defined quillaja triterpenoid formulation named QH 703 are in human trials. The advantages of using the particulate iscom form of quillaja components are (i) that local reactions at the site of injection can be avoided; a manifold higher dose of quillaja components in iscoms than in free form can be injected without causing side effects; (ii) considerably lower doses of both quillaja components and antigens are required to obtain a certain level of immune response. The iscom particle targets the antigen and adjuvant components to both the endosomal and cytosolic pathways for antigen presentation, resulting in both MHC class I and class II restricted immune responses. Further, iscoms induce APC to produce IL-1, IL-6 and IL-12 and a TH1 type of response with enhanced IL-2 and IFN-gamma production. Iscoms are now constructed to target the mucosal lymphatic systems. Iscoms administered intranasally induce secretory IgA responses in lungs and distant mucosal membranes e.g. in the genital tract.

Drug Delivery Systems↗

[The structure activity relationship of saikosaponins and glycyrrhizin derivatives for Na+, K(+)-ATPase inhibiting action].

The study on structure-activity relationship of saikosaponins and glycyrrhizin derivatives for Na+, K(+)-ATPase inhibiting action has been made in vitro. The results showed that the order of potency of inhibitory effect of saikosaponins on Na+, K(+)-ATPase is as follows: b1 > d > b2 > b4 > a > b3 > e > c. The chemical structure C23-OH, C16-OH and the C11, C13 conjugated double diene of saikosaponins are important for its inhibitory activity. The inhibitory potency of glycyrrhizin (GL), glycyrrhetinic acid (GA) and carbenoxolone (CX) for Na+, K(+)-ATPase activity is as follows: GA > or = CX > GL. In addition, the inhibitory effect of saikosaponin d on Na+, K(+)-ATPase was found to be non-competitive.

Cell-Free System↗

[Chemical constituents of the roots of Bupleurum longicaule Wall. ex DC. var. franchetii de Boiss and B. chaishoui Shan et Sheh].

From the roots of Bupleurum longicaule var. franchetii, B. chaishoui and the official species B. chinense, ten saikosaponins have been isolated and identified as saikosaponin a, saikosaponin d, saikosaponin c, saikosaponin e, saikosaponin b2, 2"-O-acetylsaikosaponin a, 3"-O-acetylsaikosaponin a, 3"-O-acetylsaikosaponin d, 6"-O-acetylsaikosaponin a and 6"-O-acetylsaikosaponin d respectively. It has been shown that the chemical constituents of these three Bupleurum plants are very similar, therefore, the medicinal value of B. longicaule var. franchetii and B. chaishoui is further verified.

Apiaceae↗