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PubMed1988

A non-opioid mechanism in the inhibitory effect of ginseng saponins on electrically evoked contractions of guinea-pig ileum and mouse vas deferens.

Both ginseng total saponins (GTS) and one of its constituents, protopanaxatriol saponins (PT), inhibited the electrically evoked contractions of guinea-pig ileum (GPI) in a concentration dependent manner in a range of 1-100 micrograms/ml, and this effect was irreversible at high concentrations of the saponins. Protopanaxadiol saponins (PD) had a transient and weak effect. On the other hand, in mouse vas deferens (MVD), the contractions were increased by PT and PD, however, GTS was almost without effect. The inhibitory effect of morphine was arithmetically increased by pretreatment with 100 micrograms/ml of these saponins in GPI preparations, while the inhibitory effect of the contractions was potentiated in MVD preparations. Neither the inhibition of contractions in the GPI preparation nor the facilitation of contractions in the MVD preparation by these ginseng saponins was reversed by 1 microM naloxone, in contrast to naloxone antagonism of morphine-induced contractions in both preparations. GTS and PT caused a dose-dependent inhibition of BaCl2-induced contraction of GPI. It is concluded that the mechanism on the inhibitory or facilitated effect of ginseng saponins on electrically evoked contractions in GPI and MVD preparations may be separated from the effect of opioids, and the mechanism may be based on the direct action of the saponins on smooth muscles preparations.

Animals↗
PubMed1975

Chemico-pharmacological studies on saponins of Panax ginseng C. A. Meyer. II. Pharmacological part.

The pharmacological properties of seven pure saponins isolated from Panax ginseng C. A. Meyer were studied. 1. The ginseng saponins showed weak toxicities in mice. Especially, Rg1, Rf and Rb 1, which contained glucose as a sugar component, were weaker in their toxicities than the rest, which contained arabinose and/or rhamnose. It was also noted that the saponins containing protopanaxadiol as sapogenin were more toxic than those containing protopanaxatriol. 2. All the saponins diminished ACh-induced contraction of the isolated ileum of the guinea pig. On the other hand high concentrations of Rb 2 caused contraction of the ileum by itself. 3. All of the saponins induced a decrease in heart rate and showed biphasic actions on the blood pressure in rats, while they little affected respiration. They caused blood pressure fall preceded by slight rise. Among them, Rg 1 showed the most prominent action and it produced a blood pressure rise with doses of 30 to 100 mg/kg. The pressor as well as depressor action was not influenced by the pretreatment with any of atropine, diphenhydramine, phentolamine and propranolol. 4. Rg 1 and Re showed vasodilator action in dogs, the potencies of which were 1/20 and 1/50 of that of papaverine, respectively. Rc and Rb 2 showed very weak vasodilator actions but Rb 1 did not. 5. Among the 7 saponins, Rd, Re and Rb 2 showed more potent hemolytic actions than those of the rest and the potencies were proportional to their toxicities. 6. Whereas single administration of Rf, Re and Rd significantly suppressed the conditioned avoidance response, repeated administration of them caused facilitation of the response. On the other hand, Rb 2 always showed very weak suppressant action. 7. Rg 1, Rf, Re and Rd significantly suppressed the fighting of mice induced by foot shock, while Rb 1, Rb 2 and Re little affected the fighting. 8. All the saponins showed antifatigue action. They markedly increased the movement after compulsory gait and the action was consistent and independent of their action on the movement before compulsory gait. 9. The saponins showed moderate depressant actions on the EEG and the behavior in cats. They were qualitatively similar in their actions, although Rg 1, Re and Rb 2 were more potent than the rest. They also suppressed EEG arousal response induced by electrical stimulation of the mid brain in cats.

Acetylcholine↗
PubMedDate not supplied

[Mechanism of activation of Ehrlich ascites carcinoma cells using the total fraction of saponins from Korean ginseng].

Molecular mechanisms of action of the total fraction of saponins from Red Korean Ginseng on the elements of the intracellular signalling system of the cells of ascitic Ehrlich carcinoma (AEC) were studied. The action of the total fraction of the saponins on the AEC cells was compared with that of the classic activator of such cells i.e. ATP. It was shown that the action of the total fraction of the saponins was similar to that of ATP. In concentrations of 10(-6) to 10(-3) per cent saponin induced an increase of [Ca2+]j mobilizing Ca2+ from the endoplasmic reticulum (ER) and activating the Ca2+ inlet to the cells. The same as in case with the use of ATP the Ca2+ mobilization from ER was reversible. In comparison to ATP saponin induced higher activation of the Ca2+ inlet to ER and the cells. The same as ATP saponin activated the Na+/H+ exchange and the Ca2+ - dependent K+-channels. Out of all the mention-ed parameters only the activation of the Ca2+ inlet to the cells was probably the direct result of the saponin action. The changes in the other parameters were mediated by nonspecific activation of the purine receptor. The analysis of the kinetic data demonstrated that unlike the ATP-dependent activation of the purine receptor the saponins first of all activated the inlet of Ca2+ to the cells and only after that the mobilization of the latter from ER.

Adenosine Triphosphate↗
PubMed1998

ISCOMs and other saponin based adjuvants.

Saponins are chemically a heterogeneous group of sterol glycosides and triterpene glycosides which are common constituents of plants. One source of triterpenoid saponins obtained from the bark of Quillaia saponaria Molina (the soap bark tree) have been known to cause substantial enhancement of immune responses since the 1920s. Despite their use in animal vaccines, the development of saponin-based formulations for human vaccines has been impeded by their complexity and concerns about toxicity. This review briefly covers the use of saponins for animal vaccines but focuses mainly on the development of these adjuvants for use in man. Important aspects include preparation of purified or highly defined saponin fractions, improved understanding of the relationships between adjuvant activity, toxicity and structure of saponins and formulation of saponins into structures with reduced toxicity such as ISCOMs. Recent developments in the understanding of cellular interactions, cytokine induction and the in vivo localisation of saponin containing formulations will also be reviewed.

Journal Article↗
PubMed2001

Acid beverage floc: protein-saponin interactions and an unstable emulsion model.

The occurrence of acid beverage floc (ABF) in acidified carbonated beverages has long been attributed to the presence of saponins. We have examined this assertion and have found evidence to suggest that traces of protein may also be a key factor, along with lipid material present in the floc. Turbidity levels of beet sugar protein (0.001 wt.%) and saponin (0.001 wt.%) solutions were examined over time using spectrophotometry. At neutral pH, no change in turbidity was observed in any combination (individually or mixed). Furthermore, acidified (pH 2) saponin and protein solutions, considered separately, also exhibited no change. However, a mixture of equal concentrations at pH 2 showed an initial increase in turbidity up to 2 h after mixing, followed by a decrease over the ensuing 12 h. Interfacial tension measurements also indicated interactions between the protein and saponin at pH 2. Photon correlation spectroscopy (PCS-Malvern Zetasizer 4) was used to quantitatively examine the particle size distributions and aggregation of a model, highly dilute dispersion, of bromohexadecane in 20 wt.% sucrose solution, prepared with a jet homogenisor. Beet sugar saponin (0.001 wt.%) and protein (0.001 wt.%) were added to the dispersion, and their emulsion-stabilising effects examined via oil droplet size measurement over time. At neutral pH, the size of oil droplets in the dispersion was unaffected by the addition of saponin or protein. At pH 2, the presence of saponin again caused no effect on droplet size. However, in acid conditions, protein appeared to destabilise the dispersion. The results indicate that the key to controlling the ABF problem may be the ratio of saponin to protein in the product, which may or may not stabilise dispersed lipid, depending on their interactions.

Journal Article↗
PubMed1999

Compromised disease resistance in saponin-deficient plants.

Saponins are glycosylated plant secondary metabolites found in many major food crops [Price, K. R., Johnson, I. T. & Fenwick, G. R. (1987) CRC Crit. Rev. Food Sci. Nutr. 26, 27-133]. Because many saponins have potent antifungal properties and are present in healthy plants in high concentrations, these molecules may act as preformed chemical barriers to fungal attack. The isolation of plant mutants defective in saponin biosynthesis represents a powerful strategy for evaluating the importance of these compounds in plant defense. The oat root saponin avenacin A-1 fluoresces under ultraviolet illumination [Crombie, L., Crombie, W. M. L. & Whiting, D. A. (1986) J. Chem. Soc. Perkins 1, 1917-1922], a property that is extremely rare among saponins. Here we have exploited this fluorescence to isolate saponin-deficient (sad) mutants of a diploid oat species, Avena strigosa. These sad mutants are compromised in their resistance to a variety of fungal pathogens, and a number of lines of evidence suggest that this compromised disease resistance is a direct consequence of saponin deficiency. Because saponins are widespread throughout the plant kingdom, this group of secondary metabolites may have general significance as antimicrobial phytoprotectants.

Journal Article↗
PubMed2000

Isolation and evaluation of immunological adjuvant activities of saponins from Polygala senega L.

We have identified saponins in the root of Polygala senega L., a plant indigenous to the Canadian prairies, which display immunopotentiation activity to protein and viral antigens. By two-step extraction and hemolytic activity-guided fractionation by silica flush chromatography six saponin fractions were generated and their HPLC profiles determined. Two dominant fractions, designated as PS-1 and PS-2, were tested for adjuvant activity in mice immunized with ovalbumin, and hens immunized with rotavirus. The resulting adjuvant activity was compared with that of Quil A saponin. The P. senega saponins increased specific antibody levels to the antigens, in both mice and hens. In mice, there was a preferential increase of the IgG2a subclass, and upon in vitro secondary antigen stimulation, high IL-2 and IFN-gamma levels were observed in spleen cell cultures from P. senega saponins-immunized animals. The saponins were tested for their toxicity by lethality in mice and were found to be less toxic at the same dose than their counterpart Quil A. The results of this study indicated the potential of P. senega saponins as vaccine adjuvants to increase specific immune responses.

Adjuvants, Immunologic↗
PubMed2000

Rapid identification of saponins in plant extracts by electrospray ionization multi-stage tandem mass spectrometry and liquid chromatography/tandem mass spectrometry.

Electrospray ionization multi-stage tandem mass spectrometry (ESI-MS(n)) and liquid chromatography coupled with on-line mass spectrometry (LC/MS/MS) were applied to characterize saponins in crude extracts from Panax ginseng. The MS(n) data of the [M - H](-) ions of saponins can provide structural information on the sugar sequences of the saccharide chains and on the sapogins of saponins. By ESI-MS(n), non-isomeric saponins and isomeric saponins with different aglycones can be determined rapidly in plant extracts. LC/MS/MS is a good complementary analytical tool for determination of isomeric saponins. These approaches constitute powerful analytical tools for rapid screening and structural assignment of saponins in plant extracts.

Chromatography, Liquid↗
PubMed2006

ESI-QqTOF-MS/MS and APCI-IT-MS/MS analysis of steroid saponins from the rhizomes of Dioscorea panthaica.

Using high-resolution quadrupole time-of-flight mass spectrometry along with an electrospray ionization source (ESI-QqTOF-MS), accurate molecular weights of 13 steroid saponins extracted from the rhizomes of Dioscorea panthaica were acquired and the corresponding molecular formulae obtained. In order to elucidate the fragmentation pathways of steroid saponins in D. panthaica, 10 authentic samples were investigated using ESI-QqTOF-MS/MS. In addition, atmospheric pressure chemical ionization mass spectrometry combined with ion trap tandem mass spectrometry (APCI-IT-MS/MS) was used to analyze the structures of 13 steroid saponins in D. panthaica. Through the analysis of their tandem mass data, diagnostic fragment ions of the spirostanol and furostanol steroid saponins in D. panthaica were detected as m/z 271.2056 and 253.1951. In addition, four pairs of isomers were detected and the possible structures of four unknown steroid saponins in D. panthaica speculated. ESI-TOF and APCI-MS(n) have proved to be effective tools for research on fragmentation mechanism of steroid saponins and the rapid determination of native steroid saponins in extract mixture, thereby avoiding tedious derivation and separation steps.

Carbohydrate Sequence↗
PubMed2004

Free radicals mediated membrane damage by the saponins acaciaside A and acaciaside B.

Acaciaside A and B, two acylated triterpenoid bisglycoside saponins originally isolated from the funicles of Acacia auriculiformis, are known to have antihelmintic activity. In our previous investigation it was suggested that the conjugated unsaturated system of the saponins is involved in producing the damaging effect of saponins, probably by resulting free radicals that induce membrane damage through peroxidation. Here the interaction of saponins and the microsomal membrane was investigated in the presence and absence of superoxide dismutase, catalase and thiourea. Our results showed that superoxide dismutase significantly blocked the effect of saponins-induced membrane damage. Catalase had only a minor effect on saponins-induced membrane damage and thiourea had no effect. The results suggest that in our model, saponins can generate superoxide anions and initiate lipid peroxidation.

Acacia↗
PubMed2000

Biodegradability of the molluscicidal saponins of Phytolacca dodecandra.

The biodegradability of water-extracted saponins of berries from the Endod plant, Phytolacca dodecandra L'Herit, was evaluated under OECD standardized conditions. Persistence of the saponins was evaluated by determination of saponin concentrations in water over a 30-day period, using a quantitative HPLC method and a semiquantitative hemolytic assay, which is considered a potential field method. The two methods were compared. Bioassays were simultaneously conducted using Biomphalaria glabrata fresh water snails to assess the molluscicidal potency over time. All experiments were carried out in water, which was chemically balanced to sustain snails, and to one set river water was added to the medium to mimic natural conditions. (1) Saponin concentrations in water treated with an aqueous extract of P. dodecandra cultivar E44 were stable for 2 days then rapidly decreased during the third and fourth day. Lethal concentrations to snails were LC50 = 9.6 mg/l (95% CI: 6.3 to 19.4) in one set and LC50 = 6.8 mg/l (95% CI: 5.4 to 12.2) in the other. Adding river water to one set of the experiments had no effect on the mean saponin concentration over time (F = 0.02, P = >0.05). (2) Comparison of the hemolytic assay with the HPLC method showed no significant difference in mean saponin concentrations (t = 0.32, P > 0.05, 95% CI: -2.67 to 3.64), and a correlation of r2 = 0.88 between the two methods. (3) The saponin fraction of an aqueous extract of P. dodecandra was readily biodegraded (t1/2 = 15.8 h), and the complete consumption within a 10-day window indicates ready degradability in aquatic environments under aerobic conditions. (4) These results show that the use of Endod berries for snail control in schistosomiasis-infested water bodies is environmentally acceptable.

Animals↗
PubMed1975

Role of glycosidases in the membranlytic, antifungal action of Saponins.

In studies on the membranlytic action of various saponins on mycelium of Botrytis cinerea and Rhizoctonia solani digitonin, alpha-hederin and tomatin caused considerable leakage of free amino acids, while aescin and theasaponin were less effective. Cyclamin significantly damaged cell membranes of R. solani, but did not change the selective permeability of B. cinerea. Cell membrane disruption was accompanied by an enzymatic conversion of saponins into their corresponding aglycones in cell membrane vicinity, an effect which was significantly inhibited by aldonolactones, known inhibitors of beta-glycosidases. These results lead to the conclusion that the hardly water soluble aglycones are the active part of the saponin molecules, the saponins themselves being only water soluble transport forms. It follows, that the presence of appropriate glycosidases in cell membranes, capable of converting saponins into their aglycones, is a prerequisite for the membranlytic action of saponins. The similarity of the membranlytic effects of saponins towards fungi and erythrocytes is descussed.

Cell Membrane↗
PubMed1984

Interaction of sea cucumber saponins with multilamellar liposomes.

The effect of three sea cucumber saponins, echinoside A, bivittoside D and holothurin A, on multilamellar liposomes was investigated. An ideal osmotic behavior of liposomes was described as a linear relationship between the reciprocal 3/2 s power of absorbance at 450 nm and the osmotic gradient across the membrane. Sea cucumber saponins at concentrations below critical micelle concentration (CMC) disturbed this linear relationship in liposomes composed of egg phosphatidylcholine, phosphatidic acid and cholesterol. Cholesterol-free liposomes were not susceptible to these saponins. Results of optical measurements were consistent with those of transmission electron microscopy, which showed saponin-induced changes in liposomal structure. The lytic activity of sea cucumber saponins on liposomes depended on their chemical structure. These results suggest that sea cucumber saponins as monomers can interact with liposomes and that cholesterol serve as a principal binding site for the sea cucumber saponins.

Animals↗
PubMed1985

Effects of purified ginseng saponins on multilamellar liposomes.

To elucidate the mode of interaction between purified ginseng saponins and liposomes, the effects of ginseng saponins at concentrations below and above their critical micelle concentration on the osmotic behavior of liposomes were observed. Liposomes composed of egg phosphatidylcholine (PC), phosphatidic acid (PA) and/or cholesterol (Ch) behave as an ideal osmometer and this activity was described by the linear relationship between (1/A450)3/2 and Cin/Cout. Total saponin prepared from the lateral roots of ginseng cultivated in Korea interacted with multilamellar liposomes and prevented them from behaving as an ideal osmometer. 20-S-Protopanaxadiol saponin showed similar activity but 20-s-protopanaxatriol saponin had weak activity. Ginsenoside Rb1 whose genin is 20-S-protopanaxadiol, disturbed osmotic behavior of Ch-free liposomes but not Ch-containing liposomes as monomers and lyzed both liposomes as micelles. Rg1 whose genin is 20-S-protopanaxatriol, showed no activity on liposomes with or without Ch. It can be suggested that ginseng saponins may interact with and destroy liposomal membranes and that structure of sugar moiety is an important factor to their activities. Ch is not a target in this interaction but suppresses the activity of ginseng saponins.

Brassica↗
PubMed1995

Crude saponin extracted from Vietnamese ginseng and its major constituent majonoside-R2 attenuate the psychological stress- and foot-shock stress-induced antinociception in mice.

Effects of Vietnamese ginseng (VG) crude saponin and majonoside-R2, a major saponin constituent, on the psychological stress- and foot shock stress-induced antinociception in the tail pinch test were examined in mice. VG crude saponin (6.2, 12.5, and 25 mg/kg, P.O.) attenuated psychological stress- but not foot shock stress-induced antinociceptive response, whereas majonoside-R2 (3, 6.2, and 12.5 mg/kg, P.O. and i.p.), as well as naloxone (2 mg/kg, i.p.), suppressed both psychological stress- and foot shock stress-induced antinociception. Pretreatment with the crude saponin (12.5 mg/kg, P.O.) or majonoside-R2 (6.2 mg/kg, P.O.) for 5 days followed by the treatment in combination with stress for next 5 days did not affect the development of adaptation to foot shock stress, but they significantly suppressed the antinociceptive action of the stress measured on the first, second, and third day during the stress exposure period. Majonoside-R2 (6.2 mg/kg, P.O.) but not the crude saponin (12.5 mg/kg, P.O.) significantly blocked the development of adaptation to psychological stress. These results suggest that VG crude saponin has the suppressing effect on psychological stress- and foot shock stress-induced antinociception and that majonoside-R2 is important for the action of the saponin.

Adaptation, Psychological↗
PubMed1994

Investigation of the diurnal, ontogenetic and seasonal variation in the molluscicidal saponin content of Phytolacca dodecandra aqueous berry extracts.

Daily variation in the content of the saponins of the berries of Phytolacca dodecandra was determined in berries harvested at the full grown green unripe stage of development once every two hours. The saponin content was quantitatively determined by HPLC analysis of the molluscicidal monodesmosidic saponins in the aqueous extract of the crushed berries. No significant daily variations were observed in extracts of berries collected at different times of day (P > 0.05 by ANOVA). But, seasonal variation was apparent in extracts prepared from berries harvested from the same plants once every two weeks. Berries of highest saponin content were those harvested during the dry season and just before the onset of the rainy season. The seasonal variation was attributed to increased water stress during the dry season. Very young racemes had the highest saponin content, while mature berries produced the lowest saponin concentration. There was, however, consistency in the berry saponin composition during the day, season and all stages of berry development.

Carbohydrate Sequence↗
PubMed2003

Acute and subacute toxicities of the saponin mixture isolated from Schefflera leucantha Viguier.

Acute toxicity of the bronchodilator saponin mixture isolated from Schefflera leucantha Viguier leaves was investigated in comparison with the methanol and the water extract of this plant. Oral doses of 5000 mg/kg of the methanol extract, the water extract and the saponin mixture did not produce mortality or significant changes in the general behavior and gross appearance of internal organs of rats. Subacute toxicity of the saponin mixture was evaluated with the dose of 1000 mg/kg, orally for 14 days. An extra group (satellite group) was given saponin mixture and kept for a further 14 days after treatment. All animals did not show signs of toxicity during the experimental period. Liver weights of the saponin-treated and the satellite male groups were higher whereas testis weight were lower than those of the control group which received distilled water. However, the histological examination of various organs revealed that there were no differences between the control and the treated rats. BUN, Cr, AST, ALT and ALP levels increased in saponin-receiving rats. It is possible that the saponin mixture directly impacts on the liver and the kidney functions.

Animals↗
PubMed2002

Effects of long term feeding of Quillaja saponins on sex ratio, muscle and serum cholesterol and LH levels in Nile tilapia (Oreochromis niloticus (L)).

Seventeen-day-old Nile tilapia fry were fed a standard diet (C) or diets containing 50-700 mg kg(-1) Quillaja saponin (QS) extract (groups S50, S150, S300, S500 and S700). After the first 8 weeks, 30 randomly selected tilapia from each of the treatments were placed in separate aquaria and fed the standard diet without saponins from then on (these were designated S50/C, S150/C, S300/C, S500/C and S700/C). The fish grew from an initial average weight of approximately 30 mg to a final average weight of 79 g during the 6-month feeding period. The difference between the average weight of C-fed tilapia and the treatment with the highest average weight after 6 months was 53.5%. The sex ratio of tilapia in the saponin-fed groups deviated from the normal 50:50 male:female ratio, with the S700 group showing a significantly higher number of males. Quillaja saponin stimulated LH release from dispersed tilapia pituitary cells in vitro. This effect was abolished in the presence of dilute calf serum. Serum LH values did not show any diet-dependent trend in either male or female tilapia in vivo. In both continuously saponin-fed and only-initially saponin-fed groups, the average serum (but not muscle) cholesterol levels in males showed an increasing trend (R(2) values of 0.62 and 0.69) with increasing dietary saponin level. It was concluded that dietary QS has the potential to change the sex-ratio in favour of males. More investigations are required to determine the mechanism of action and the optimum dietary level of QS for maximum effects.

Animals↗