[Saponins and sapogenins from Barringtonia].
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Effects of saponins extracted from Bupleuri Radix (saikosaponin) and the corresponding aglycones on hypotonic or hyperthermic hemolysis were investigated. Low concentrations of saikosaponins protect or stabilize rat erythrocytes against both hypotonic and heat-induced hemolysis. Minor modifications of the aglyconic part of the saikosaponin have enormous effects on the membrane stabilizing potency. Saikogenins also protect erythrocytes from hypotonic hemolysis but do not show any prevention of heat-induced hemolysis. It is suggested that saikogenins react with erythrocyte membranes in a quite different manner from saponins and that the existence of the sugar moiety plays an important role in the reaction with membranes as does a slight modification of the molecular structure in the aglyconic part.
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MeOH extract of Kochia scoparia was fractionated into CHCl3-, EtOAc- and BuOH extracts and the last fraction were hydrolyzed by 3%-NaOH (MeOH-H2O) to compare the bioactivities on antinociceptive and anti-inflammatory effects. Silica gel column chromatography of BuOH fraction afforded a large amount of 3-O-beta-D-xylopyranosyl (1-->3)-beta-D-glucuronopyranosyl oleanolic acid (momordin lc, 4) and that of acid hydrolysate of BuOH fraction gave 3-O-beta-D-glucuronopyranosyl oleanolic acid (momordin lb, 3), its 6'-O-methyl ester (2) and oleanolic acid (1). Silica gel column chromatography of alkaline hydrolysate afforded a large amount of 4. MeOH extract and both EtOAc- and BuOH fractions were active in the rheumatoidal rat induced Freund's complete adjuvant reagent (FCA) whereas CHCl3 fraction was inactive. Compound 1 and 4 showed significant activities in the same assay but oleanolic acid 3-O-glucuronopyranoside (3) showed no activity. These fashions were also observed in carrageenan-induced edema of the rat and in the antinociceptive activity tests undertaken in hot plate- and writhing methods. These results suggest that momordin lc and its aglycone, oleanolic acid, could be active principles for rheumatoid arthritis.
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