Characterization and pharmacodynamic properties of Arnica montana complex.

A dark brown polymeric complex was isolated from flowering parts of medicinal plant Arnica montana L. by hot alkaline extraction followed by neutralization and multi-step extractions with organic solvents. It was recovered in 5.7% yield, on GPC showed two peaks of molecular mass of 9 and 3.5kDa. The compositional analyses of Arnica complex revealed the presence of carbohydrates (26%), uronic acids (12%), phenolics (1.25mM or 213mg of GAE/1g), and low protein content (∼1%). The carbohydrate moiety was rich mainly in rhamnogalacturonan and arabinogalactan. The antitussive tests showed the reduction of the cough efforts by Arnica complex, however, its total antitussive effect was lower compared with that of codeine, the strongest antitussive agent. The bronchodilatory activity of Arnica complex was similar to salbutamol, a classic antiasthmatic drug, and was confirmed by significantly decreased values of specific airways resistance in vivo and by considerably attenuated the amplitude of acetylcholine and histamine-induced contractions in vitro. Arnica complex did not show any cytotoxic effect on mouse fibroblast cultures and human lung cells, up to the dose of 500µg/mL.

Characterization and biological activity of Solidago canadensis complex.

Polyphenolic-polysaccharide-protein complex has been isolated from flowers of Solidago canadensis L. by hot alkaline extraction procedure. Compositional analyses of S canadensis complex revealed the presence of carbohydrates (43 wt%), protein (27 wt%), phenolics (12 wt%), uronic acids (10 wt%) and inorganic material (8 wt%). The carbohydrate part was rich in neutral sugars (81 wt%) while uronids were determined in lower amount (19 wt%). Monosaccharide analysis of carbohydrate part revealed the presence of five main sugar components, i.e. rhamnose (~23 wt%), arabinose (~20 wt%), uronic acids (~19 wt%), galactose (~17 wt%) and glucose (~14 wt%), and indicated thus the presence of rhamnogalacturonan and arabinogalactan in S. canadensis complex. HPLC analysis of complex showed one single peak of molecule mass at 11.2 kDa. Antitussive activity tests, performed in three doses of Solidago complex, showed the reduction of the number of cough efforts in the dose-dependent manner. Higher doses (50 and 75 mg/kg b.w.) were shown to be by 15 and 20% more effective than that of lower one (25mg/kg b.w.). However, the antitussive effect of the highest dose (75 mg/kg b.w.) was by 10% lower in comparison with that of codeine, the strongest antitussive agent. Besides, the highest dose of the complex (75 mg/kg b.w.) significantly decreased values of specific airways resistance and their effect remained longer as that of salbutamol, a representative of classic antiasthmatic drugs.

Antitussive and bronchodilatory effects of Lythrum salicaria polysaccharide-polyphenolic conjugate.

A high molecular mass polysaccharide-polyphenolic conjugate has been isolated from flowering parts of Lythrum salicaria by hot alkaline extraction. Its chemical analysis revealed 74% of carbohydrates and 17% of phenolics. Compositional analysis of carbohydrate part showed a high GalA content (49%), Rha (25%), Gal (13%) and Ara (9%) residues, and indicated thus rhamnogalacturonan associated with arabinogalactan in Lythrum conjugate. Antitussive activity tests, performed in three doses of Lythrum conjugate - 25, 50 and 75 mg/kg of animal body weight, showed the reduction of the number of cough efforts even 5h after administration. However, their antitussive effects were lower in comparison with that of codeine, the strongest narcotic antitussive agent. The tests evaluating the influence of different doses on airways smooth muscle reactivity revealed more significant effect of Lythrum conjugate in comparison with that of salbutamol, a commercial bronchodilator used in a clinical practice. Measurements of specific airway resistance pointed at both, the dose-dependent bronchodilatory activity and possible participation of bronchodilation on antitussive effect of Lythrum conjugate. This study represents the first sight into pharmacodynamic properties of Lythrum polysaccharide-polyphenolic glycoconjugate.

Effects of the extract from Conyza canadensis on human blood platelet aggregation.

The effects of different parts of extract from medicinal plant Conyza canadensis, used to control bleeding, on human blood platelet aggregation in vitro were investigated. Aqueous extract of Conyza c. from young or old plants, glycoconjugate part, polysaccharide part and aglycon part at the concentrations above 0.75 mg/ml strongly inhibited platelet aggregation induced by collagen (2 microg/ml) in dose-dependent manner. Polysaccharide part isolated from plant extract had the strongest inhibitory effect on aggregation stimulated by collagen and seems to be responsible for antiaggregatory properties.

Fucosylation in synovial fluid as a novel clinical marker for differentiating joint diseases--a preliminary study.

OBJECTIVE: To investigate fucosylation of synovial fluid glycoproteins in patients with rheumatoid arthritis (RA), juvenile arthritis (JIA), gonarthrosis (GA) and reactive arthritis (ReA), referred to traumatized knee (TK). METHODS: Synovial fluid glycoproteins were separated by SDS-PAGE and either silver stained or blotted onto nitrocellulose and probed with the fucose-specific Aleuria aurantia lectin. Five bands were chosen for densitometric analysis. Total fucose content and density of fucosylated epitopes were analyzed. RESULTS: Fucose content was elevated in all patient groups and almost all bands, comparing to TK. The density of fucosylated epitopes was increased in the 42-kDa band of RA and JIA cases, and lowered in the 26-kDa band of RA and JIA, but not in GA. In all RA cases FR 42-kDa > FR 26-kDa. The relation was opposite in 8 out of 9 GA cases. CONCLUSION: The density of fucosylated epitopes differs significantly in particular glycoproteins of synovial fluid in joint diseases and may be of potential diagnostic value in differentiating diseases of inflammatory and degenerative origin.

The membrane-disrupting activity of alpha-aminoalkanephosphonic acids and their derivatives.

The influence of a series of acyclic and cyclic aminophosphonates on the physicochemical properties of model (planar lipid membranes-BLM) and biological (erythrocytes-RBC) membranes was studied. The results obtained were compared with the results of physiological tests performed on the aquatic plant Spirodela oligorrhiza. It was found that the inhibition of plant growth by the compounds studied correlated, although not very highly, with the observed changes in the properties of membranes used. It was also found that both the biological activity of aminophosphonates and their efficiency at modifying the physicochemical parameters of membranes depended on their structural features.

Synthesis, Surface Properties, and Hydrolysis of Chemodegradable Anionic Surfactants: Diastereomerically Pure cis- and trans-2,5-Disubstituted-1,3-dioxanes

In our continuing systematic studies concerning the synthesis, surface properties, and hydrolysis of chemodegradable, diastereomerically pure surface active 2,5-disubstituted 1,3-dioxane derivatives, two new groups of anionic surfactants, sodium cis- and trans-(2-n-undecyl-1,3-dioxan-5-yl)methyl sulfates and sodium cis- and trans-3-[(2-n-undecyl-1,3-dioxan-5-yl)oxy]propanesulfonates, were synthesized and investigated. Surface properties of these surfactants, i.e., surface excess concentration, Gamma, surface area demand per molecule, A, effectiveness of surface tension reduction, Pi, critical micelle concentration, CMC, and standard free energies of adsorption, DeltaGads0, and of micellization, DeltaGmic0, were determined. It was shown that the trans-isomers, in which the configuration of the polar group is equatorial, are more surface active than the cis-isomers with axial configuration of the polar group at the C-5 carbon atom of the 1,3-dioxane ring. The surfactants under study undergo easy hydrolysis reaction in DCl/D2O solution with cleavage of the 1,3-dioxane ring to nonsurface active intermediates. The trans-isomers are hydrolyzed faster than cis-isomers.

Fluorescence investigations on the interaction of rabbit liver D-fructose-1,6-bisphosphate 1-phosphohydrolase with bovine serum albumin.

The interaction of D-fructose-1,6-bisphosphate 1-phosphohydrolase (Fru-P2-ase, EC 3.1.3.11), with bovine serum albumin (BSA) results in the fluorescence quenching of BSA. BSA increases fluorescence anisotropy of Fru-P2-ase modified with o-phthaldialdehyde. A program in Fortran, to simulate the experimental titration curves of BSA with Fru-P2-ase and o-phthaldialdehyde modified Fru-P2-ase with BSA, was written. For fluorescence quenching experiments the best fit was obtained for a model where one subunit of native Fru-P2-ase binds up two molecules of BSA. The determined dissociation constants at 5, 15, 25 and 35 degrees C were 2.2, 1.6, 0.83 and 0.03 microM, respectively.