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Chemistry, 13 C-NMR Study and Pharmacology of Two Saponins from Colubrina asiatica
Abstract
From the leaves of COLUBRINA ASIATICA B RONGEN (Rhamnaceae) two saponins have been isolated and structurally elucidated, mainly by (13)C-NMR-spectroscopic methods, as jujubogenin-3-O-[2-O-acetyl-3-O-(3-O-beta-D-xylopyranosyl-4-O-acetyl-beta-D-glucopyranosyl)-alpha-L-arabinoside] (colubrinoside) and jujubogenin-3-O- [2-O-acetyl -3-O- (2-O- beta -D- xylopyranosyl-beta-D-glucopyranosyl)-alpha-L-arabinoside] (colubrin) respectively. Both saponins inhibit the spontaneous motility of mice, even at low doses (1 mg/ kg), they show an antagonistic effect on amphetamine and exert a synergistic activity on chlordiazepoxide.
... The effectiveness of most herbal medicines is attributed to various active ingredients in combination. For example, saponins show antagonistic activity against amphetamines, a sedative property [23,28,29,17]. It is therefore likely that A. africanus has saponins which contributes in part to the effects observed on the central nervous system. ...
... Several phytochemical studies proved that tannins exert sedative activity. Saponins also have potent sedative activity [21]. Furthermore, it is already reported that flavonoids have potent sedative and anxiolytic effects [22]. ...
... In addition, our preliminary phytochemicals screening detected several metabolites, including phenols, alkaloids, terpinoids, steroids, flavonoid, sterols, and saponins [18]. It is reported that such metabolites present in the plant extract possess anxiolytic and antidepressant effect [89,90]. Moreover, GC-MS analysis of MEHC demonstrated 40 potential bioactive constituents, wherein vitamin E and three important phenolic compounds, such as, 3-((4Z, 7Z)-heptadeca-4, 7-dien-1-yl) phenol, (Z)-3-(pentadec-8-en-1-yl) phenol, and 3-pentadecyl-, (Z)-3-(heptadec-10-en-1-yl) phenol were found [18], which might also directly or indirectly be involved in the above mentioned pharmacological activities of MEHC. ...
Holigarna caustica (Dennst.), a popular plant used in folk medicine in Bangladesh, is often used by the local folk practitioner to treat a variety of chronic diseases. The present research is an attempt to find out an innovative therapeutic prospect for the management of neuropsychiatric disorders. The methanol extract of H. caustica leaves (MEHC) were utilized on various behavioral tests for assessing anxiolytic, anti-depressant, and anti-inflammatory activities. The antioxidant potentials and quantitative phytochemicals were evaluated through spectrophotometric methods. Results revealed that treatment of MEHC (200 and 400 mg/kg) significantly reduced anxiety like behaviors in mice, particularly, 400 mg/kg efficiently improved % of entries and time spent (p < 0.05) in the open arms in elevated plus maze test, whereas, superior head dipping tendency (p < 0.05) was observed in hole-board test. In contrast, mice treated with 200 mg/kg revealed better anxiolytic effect in both open field and hole-cross tests. During antidepressant evaluation, mice administrated with MEHC exhibited active behaviors (swimming and struggling) in forced swimming and tail suspension tests. In parallel, MEHC manifested a noteworthy (p < 0.001) suppression of inflammatory response induced by histamine. The MEHC also showed strong antioxidant activities in 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) (IC50: 57.64 μg/mL) scavenging, H2O2 (IC50: 51.60 μg/mL) scavenging, and ferric reducing power assay. The levels of total phenol, flavonoid, flavonol, condensed tannin, and antioxidant were estimated as higher in MEHC. Moreover, 11 compounds were documented as bioactive, displayed good binding affinities to potassium channel receptor, human serotonin receptor, cyclooxygenase (COX-1 and 2), and xanthine oxidoreductase enzyme targets in molecular docking experiments. Furthermore, ADME/T and Prediction of Activity Spectra for Substances (PASS) analyses exposed their drug-likeness, nontoxic upon consumption, and likely pharmacological actions. Overall, the H. caustica is potentially bioactive as evident by in vivo, in vitro, and computational analysis. Our findings support the folkloric value of this plant, which may provide a potential source towards developing drug leads.
... Several phytochemical studies proved that tannins exert sedative activity. Saponins also have potent sedative activity [23]. Moreover, it is already reported that flavonoids have potent sedative and anxiolytic effects [24]. ...
Background: Thunbergia erecta (Acanthaceae) is the most abundant medicinal plant in different parts of Bangladesh where it is known as “nilghonta”. It has been used as traditional medicine for insomnia, depression and anxiety management. However, no scientific evidence of T. erecta belonging to neuropharmacological activity has been reported. The aim of present study was to investigate in vivo sedative and anxiolytic activities of methanol extract from the leaves of T. erecta in Swiss Albino mice. Methods: Sedative activity of METE was investigated using open field, hole cross and thiopental sodium-induced sleeping time test model whereas anxiolytic activity was screened by elevated-plus maze, light-dark box, hole-board and marble burying test method in mice at 200 and 400 mg/kg doses. The acute toxicity study and phytochemical analysis of METE also carried out. Diazepam used as the positive control for the following behavioral pharmacology test. Results: METE exhibited significant (p < 0.001) sedative effect by decreasing the number of (square and hole) crossed by mice in open field and hole cross tests in a dose-dependent (200 & 400 mg/kg) manner. In thiopental sodium-induced, sleeping time test METE significantly (p < 0.001) shortened the latency period and prolonged the sleeping time in a dose dependent (200 & 400 mg/kg) manner. Elevated plus maze (EPM) and light-dark box test results explicated that mice preferred open arms and light part instead of close arms and dark part significantly (p < 0.001). In hole board and marble burying test METE (200 & 400 mg/kg) reduced (p < 0.001) the number of head dipping and number of marble burying respectively. However, Phytochemical screening of METE revealed the presence of flavonoids, glycosides, tannins saponin, carbohydrates and alkaloids. Conclusion: The experimental result indicates T. erecta contains phytoconstituents that possess sedative and anxiolytic activity which traditionally used in insomnia, depression and anxiety management.
... A decoction of leaves and bark is traditionally used as a treatment for skin diseases, fruits as a fish poison and soap substitute, and the roots as a cure for inner fever and thirst (Mc Cormick 2007). Previous phytochemical studies of Colubrina species, including our recent investigation of the branches of C. asiatica (Sangsopha et al. 2018) demonstrated the presence of jujubogenin glycosides (Wagner et al. 1983;Seaforth et al. 1992;Oulad-Ali et al. 1994;ElSohly et al. 1999;Li et al. 1999;Lee et al. 2000), ceanothane triterpenes (Roitman and Jurd 1978), lupane triterpenes (Roitman and Jurd 1978;Baxter and Walkinshaw 1988) flavonoid glycosides (Guinaudeau et al. 1971;Guinaudeau et al. 1976;Guinaudeau et al. 1981), as well as the bisbenzylisoquinoline alkaloid O-methyldauricine (Tschesche et al. 1970). Further investigation of the EtOAc and MeOH extracts of the air-dried roots of C. asiatica gave two new triterpenoids, 3,7-O,O-dibenzoyl ceanothic acid methylester (1) and 3-O-acetyl-7-O-benzoyl ceanothic acid methylester (2), together with nine known compounds, ceanothic acid (3) (Roitman and Jurd 1978), 24-hydroxyceanothic acid (4) (Lee et al. 1992), zizyberenalic acid (5) (Kundu et al. 1989), alphitolic acid (6) (Baxter and Walkinshaw 1988), betulinic acid (7) (Sharma et al. 2010), b-sitosterol-3-O-glucoside (8) (Faizi et al. 2001), squalene (9) (Huang et al. 2009), 3 00 ,2 000 -O-acetylcolubrin (10) and 3 00 -O-acetylcolubrin (11) (Lee et al. 2000) (Figure 1). ...
Two new ceanothane triterpenes, 3,7-O,O-dibenzoyl ceanothic acid methylester (1) and 3-O-acetyl-7-O-benzoyl ceanothic acid methylester (2), along with nine known compounds (3-11), were isolated from the roots of Colubrina asiatica. The isolated compounds were identified by spectroscopic evidence. Compounds 1 and 2 showed antimalarial activity against Plasmodium falciparum with IC50 values of 4.67 and 3.07 µg/mL, respectively. Compound 2 also showed antimycobacterial activity against Mycobacterium tuberculosis (MIC 6.25 µg/mL). In addition, compounds 1, 2, 10 and 11 showed cytotoxicity against three cancer cell lines (KB, NCI-H187 and MCF-7) with IC50 values ranging from 8.32 to 46.72 µg/mL.
... The leaves and bark are used traditionally as a decoction for the treatment of skin diseases and the roots as a cure for fever and thirst (Phonsena 2007). Previous reports of compounds from the leaves of C. asiatica and related Colubrina species led to the isolation of saponins (Wagner et al. 1983;Seaforth et al. 1992;Oulad-Ali et al. 1994;Lee et al. 2000;Li et al. 1999;ElSohly et al. 1999), triterpenes (Roitman & Jurd 1978;Baxter & Walkinshaw 1988) as well as alkaloids and phenolic compounds (Guinaudeau et al. 1976 As part of our research on Thai medicinal plants containing potential bioactive compounds, air-dried branches of C. asiatica were investigated. Both EtOAc and MeOH extracts showed activity against Plasmodium falciparum, Mycobacterium tuberculosis and cytotoxicity towards three cancer cell lines. ...
Sixteen compounds were isolated from a Thai medicinal plant, Colubrina asiatica. The isolated compounds were elucidated on the basis of spectroscopic methods (IR, 1D and 2D NMR) as six triterpene acids (1-6), five steroids (7-11), one benzoic acid derivative (12), two peptides (13 and 14), one sesquiterpenoid (15) and one jujubogenin (16). Compounds 3 and 10 showed antimalarial activity against Plasmodium falciparum. Compound 5 showed antimycobacterial activity. Moreover, compounds 3, 5, 6, 10 and 14 exhibited weak cytotoxicity against cancer cell lines. Compounds 1-15 have been isolated for the first time from this plant.
... Taken together, it could be suggested that the behavioural action (sedation, hypo-activity) of the very high doses of aqueous extract was correlated to GABAergic neurotransmission in the brain (Taïwe et al., 2012b;Chapman et al., 1983). The efficacy of most herbal remedies could be attributed to various active principles the plant (Dubois et al., 1986;Wagner et al., 1983). ...
Extracts of Feretia apodanthera Del. (Rubiaceae) have been extensively used in traditional Cameroonian medicine to treat a variety of diseases, including some neurological disorders. The present study was aimed to tests the anticonvulsant properties of the aqueous extract and the alkaloid fraction of the stem barks of Feretia apodanthera. The anticonvulsant investigation was carried out against bicuculline-, picrotoxin-, pentylenetetrazol-, Methyl-β-carboline-3-carboxylate-, N-Methyl-D-aspartate-, 4-aminopyridine-, and maximal electroshock-induced seizures or turning behavior in mice. The aqueous extract protected mice against bicuculline-, picrotoxin-, pentylenetetrazol-, Methyl-β-carboline-3-carboxylate-, N-methyl-D-aspartate −, 4-aminopyridine- and maximal electroshock-induced seizures or turning behavior. Also, N-Methyl-D-aspartate-, 4-aminopyridine- and maximal electroshock- induced seizures or turning behavior, were significantly antagonized by the alkaloid fraction (80 mg/kg) from Feretia apodanthera. The total protection of mice provided by the aqueous extract against convulsions induced by pentylenetetrazol or picrotoxin was anagonized by flumazenil, a specific antagonist of the benzodiazepine site in the GABAA receptor complex.
The aqueous extract of Feretia apodanthera (but not the alkaloid fraction) increased the brain GABA content and inhibited the GABA transaminase activity.
In conclusion, Feretia apodanthera was revealed possessing anticonvulsant effects in mice, likely via the GABAergic neurotransmission.
... Saponins were suggested to exhibit antidepressant-like effects via the activation of cAMP response element-binding protein brain-derived neurotrophic factor pathway in the hippocampus in mice [35]. Triterpenoid and saponins were also reported to affect sedation by agonism of GABA-A receptor complex [36][37][38]. The presence of these phytochemicals may be responsible for the observed pharmacological activities of the extract. ...
Stem bark and leaves of Lophira alata (Family: Ochnaceae) have been used traditionally for their anti-psychotic, anti-convulsant and anxiolytic properties. Since no existing data was found on the neurobehavioural properties, this study was carried out to evaluate some neurobehavioural properties of the aqueous extract of the stem bark of L. alata in animal models.
The oral mean lethal dose (LD50) of the extract was estimated, and preliminary phytochemical screening was conducted. Lophira alata extract (200, 400 and 800 mg/kg, p.o.) was investigated for antidepressant effect using the forced swim and tail suspension tests, and the anxiolytic potential was assessed using the stair case and hole board tests. Pentylenetetrazole-induced convulsion test was used to investigate the anticonvulsant potential of the extract.
The LD50 was estimated to be >5000 mg/kg. Oral administration of L. alata extract produced a significant (p<0.05) non-dose-dependent decrease in the period of immobility in both the forced swim and tail suspension tests. While a significant decrease (p<0.05) in episodes of grooming was recorded in the staircase test, the number of head dips was not significantly reduced (p>0.05) in the hole board test. In the pentylenetetrazole-induced convulsion, a non-dose-dependent increase in onset of tonic-clonic seizures and protection from death was recorded.
The results obtained suggest that the aqueous stem bark extract of L. alata possesses neurobehavioural properties which may account for its use in ethnomedicine.
... The Tabernaemontana crispa showed the presence of high amount of alkaloids (Manske, 1960). Two saponins namely colubrinoside and coubrin have been isolated from leaves of Colubrina asiatica showed an antagonistic effect on amphetamine and exert a synergistic activity on chlordiazepoxide (Wagner et al., 1983). ...
... Some compound already described in this plant could depress the central nervous system. Saponins have been shown to have sedative property and decrease spontaneous motor activity in experimental animals 23,24 . ...
Argyreia speciosa, a woody climber is widely used in ayurveda for the treatment of neurological disorders. This work researched the action of the n-hexane (n-HF), chloroform (CF), ethyl acetate (EAF) and water (WF) fractions of hydroalcoholic extract of roots of Argyreia speciosa on the central nervous system. All the fractions (100, 200 and 500 mg/kg, p.o.) were evaluated for neuro-pharmacological activity using spontaneous motor activity and pentobarbital-induced sleeping time in mice. Chlorpromazine was used as a positive control. Central nervous system depressant activity was observed with all the fractions as indicated by the results in which they reduced spontaneous motor activity and potentiated pentobarbital induced hypnosis in mice. These results suggest that the active principles present in the root of Argyreia speciosa may responsible for central nervous depressant activity.
... It is well known that plants [20,21,22], isolated constituents from plants [23,24] and synthetic drugs like benzodiazepines and Phenobarbital [25] possess anxiolytic and sedative activity. At the higher doses diazepam (20 mg/kg p.o.) in rats [26] chlordesmethyldiazepam (bezodiazepine receptor full agonist) and desmethyldiazepam (benzodiazepine receptor agonist, metabolite of diazepam) at 5 mg/kg i.p., in mice showed decreased activity in open field test which was concluded as sedative effect [27]. ...
The petroleum ether, alcoholic and water extracts of Decalepis hamiltonii root were evaluated for anxiolytic activity using elevated plus maze model (EPM) and open field test (OFT) in mice. The alcohol extract exhibited potent anxiolytic effects at 10, 30 and 100 mg/kg., i.p. in both methods whereas petroleum ether and water extract were less effective. Presence of saponins, phenols and tannins may contribute to the anxiolytic activity of Decalepis hamiltonii root.
... The therapeutic benefits of traditional remedies might depend upon a combination of constituents . For instance saponins have been reported to show potent sedative activity, they have also been shown to have antagonistic activity on amphetamine (Wagner et al., 1983 ) and also known to inhibit spontaneous motor activity in mice (Dubois et al., 1986). It is, therefore, likely that the saponin content of this extract might be contributing in part to the observed pharmacological effects. ...
... The efficacy of most herbal remedies is attributed to various active principles in combination. For instance, saponins have been shown to have antagonistic activity against amphetamine, sedative property, and decrease spontaneous activity in experimental animals ( Amos et al., 2005;Dubois et al., 1986;Wagner et al., 1983). It is therefore probable that the saponins that are present in abundance in the extract might contribute in part for the observed central nervous system effects. ...
Crassocephalum bauchiense (Hutch.) Milne-Redh (Asteraceae) has been used as a medicine for the treatment of epilepsy, insomnia, dementia and psychotic disorders in Cameroonian traditional medicine.
This study was designed to examine whether the aqueous extract and the alkaloid fraction prepared from the leaves of Crassocephalum bauchiense possess antipsychotic and sedative properties in rodents.
The rectal temperature of mice was recorded with a probe thermometer at a constant depth. Novelty-induced rearing behavior is used to evaluate a central excitatory locomotor behavior in mice. The antipsychotic effects of the extracts were assessed using the apomorphine animal model of psychosis. The catalepsy test was tested based on the ability of the leaves extracts of Crassocephalum bauchiense to alter the duration of akinesia by placing the naive mice with both forelegs over a horizontal bar. The extracts of Crassocephalum bauchiense effects were evaluated on sodium pentobarbital-induced sleeping time. In addition, gamma-aminobutyric acid concentrations in the brain treated mice were also estimated.
The aqueous extract and the alkaloid fraction from Crassocephalum bauchiense caused dose-dependent inhibition of novelty-induced rearing behavior, decreased the apomorphine-induced stereotypy and fighting, and had significant fall of the body temperature. The aqueous extract prolonged the sodium pentobarbital sleeping time. This prolongation was not reversed by bicuculline, a light-sensitive competitive antagonist of GABA(A) receptors complex. However, the effect of the aqueous extract on sodium pentobarbital-induced sleeping time was blocked by N-methyl-β-carboline-3-carboxamide, a partial inverse agonist of the benzodiazepine site in the GABA(A) receptor complex and flumazenil, a specific antagonist of the benzodiazepine site in the GABAA receptor complex. In biochemical experiments, the concentration of the inhibitory amino acid, gamma-aminobutyric acid, was significantly increased in the brain of animals treated with the aqueous extract of Crassocephalum bauchiense and sodium valproate.
The results show that the antipsychotic and sedative properties of Crassocephalum bauchiense are possibly mediated via the blockade of dopamine D-2 receptors and GABAergic activation, respectively. However, pharmacological and chemical studies are continuing in order to characterize the mechanism(s) responsible for these neuropharmacological actions and also to identify the active substances present in the extracts of Crassocephalum bauchiense.
... The efficacy of most herbal remedies is attributed to various active principles in combination. For instance, saponins have been shown to have antagonistic activity against amphetamine, sedative property, and decrease spontaneous activity in experimental animals (Wagner et al., 1983;Dubois et al., 1986). It is therefore probable that the saponins that are present in abundance in the extract might contribute in part for the observed CNS effects. ...
The present study evaluated the neuropharmacological effects of the aqueous extract of Nauclea latifolia root bark in rodents. Effects on the spontaneous motor activity (SMA), exploratory behaviour, pentobarbital sleeping time, apomorphine-induced stereotypic behaviour and motor coordination (rota-rod performance) were investigated. The extract (50–200 mg/kg p.o.) significantly (P < 0.05) decreased the SMA and exploratory behaviour in mice and prolonged pentobarbital sleeping time in rats dose-dependently. The extract also remarkably attenuated the intensity of apomorphine-induced stereotypy dose-dependently in mice, but had no effect on motor coordination as determined by the performance on rota-rod. These results indicate the presence of psychoactive substances in the aqueous extract of the root bark of Nauclea latifolia.
... The preliminary phytochemical screening revealed the presence of tannins, cardiac glycosides, anthraquinones, saponins, steroids, triterpenes and flavonoids, which may be responsible for the observed pharmacological activities of the extract. In this plant, tannins were found to be most abundant phytoconstituent, it might be responsible for the observed pharmacological activity of the plant or in combination with the other constituents as other studies showed that saponins have potent sedative activity (Wagner et al., 1983;Amos et al., 2001). Further, natural and synthetic flavonoids are potent anxiolytic agents without sedative effects (Herberlain et al., 1994). ...
Balanites aegyptiaca is a native plant from the dry tropical areas of Africa and Arabia. It has been used in traditional medicine to treat psychoses, epilepsy, rheumatism and for the management of cough, liver and spleen conditions for many years. The plant is also used as antihelmintic and molluscicide.
The present studies aimed at investigating the behavioral properties of ethanol extract of the root of this medicinal plant, which is already in common applications in the Nigerian traditional medicine.
The intraperitoneal and oral mean lethal dose (LD(50)) of the extract was determined using the Lorke's method. The preliminary phytochemical screening of the extract was carried out to identify the secondary metabolites in the extract. Furthermore, the behavioral properties of the extract were evaluated using diazepam-induced sleep, open field test, staircase test and beam walking assay all in mice.
The extract significantly (p<0.001) prolonged the duration diazepam (20mg/kg i.p)-induced sleep in mice dose dependently. However, the extract showed no significant effect on the onset of diazepam-induced sleep. In the open field test, the extract (150 and 300 mg/kg) and diazepam (0.05 mg/kg) produced a significant (p<0.05, p<0.005 and p<0.001) decrease in the number of square crossings. There was no significant effect on the number of centre square crossing following the administration of the extract. The extract (75 and 150 mg/kg) and diazepam (0.05 mg/kg) produced a significant (p<0.05) decrease in the number of rearing suggestive of sedation. In the staircase experiment there was a decrease in the number of upward step climbing as well as number of rearing suggesting anxiolytic and sedative properties of the extract. In the beam walking assay the extract did not produce any significant increase in the time taken to complete task as compared to diazepam 1mg/kg which was significant at p<0.05. Furthermore, 30 mg/kg of the extract and diazepam 1mg/kg showed significant (p<0.05) mean number of foot slips, suggesting that the central nervous system depressant activity might not necessarily due to peripheral neuromuscular blockade.
The result indicates that the extract of Balanites aegyptiaca possess biologically active compound(s) that have anxiolytic and sedative properties, which support the ethnomedicinal use of the plant as antipsychotic and antiepileptic agents.
... Saponins also can induce diarrhea (Lalitha et al., 1990), mollify ulcers (Muto et al., 1987), relieve analgesia (Lei et al., 1984;Oshima et al., 1984) and fever (Gan and Chen, 1982), as well as having sedative properties (Wagner et al., 1983;Choi and Woo, 1987). ...
Three saponin-rich extracts (20, 60, 100% methanol), four 100% methanol subfractions and seven independently acquired fractions (A-G) from guar meal, Cyamopsis tetragonoloba L. (syn. C. psoraloides), were evaluated for antimicrobial and hemolytic activities. These activities were compared against quillaja bark (Quillaja saponaria), yucca (Yucca schidigera), and soybean (Glycine max) saponins in 96-well plates using eight concentrations (0.01 to 1.0 and 0.1 to 12.5 mg extract/mL). Initial guar meal butanol extract was 4.8 ± 0.6% of the weight of original material dry matter (DM). Butanol extract was purified by preparative reverse-phase C-18 chromatography. Two fractions eluted with 20, and one each with 60, and 100% methanol with average yields of 1.72 ± 0.47, 0.88 ± 0.16, 0.91 ± 0.16 and 1.55 ± 0.15% of DM, respectively. Further purification of the 100% methanol fraction using normal-phase silica gel preparatory high pressure liquid chromatography eluted 4 peaks at 16, 39, 44 and 46 min. Only the 100% methanol fraction, its 16 min peak, F and G fractions, and quillaja saponin, exhibited both hemolytic and antibacterial activities against Staphylococcus aureus, Salmonella Typhimurium and E. coli, but 20 and 60% methanol fractions stimulated Lactobacillus spp. growth. Guar meal (0 or 5%) was added to diets fed to chicks from 1 to 21 days of age. Chicks fed both diets were unchallenged or challenged with 5 x 103 Eimeria tenella sporulated oocysts at 10 days. Guar meal diets reduced oocysts shed per gram of feces, body weight, and feed efficiency. Adding 2.5% guar meal, 1% guar gum, or 0.125% saponin-rich guar meal extract to diets fed to chicks to 21 days of age showed that guar meal increased the cfu concentrations of digesta more than controls following a challenge with 107 cfu of Clostridium perfringens at 14 days. Body weights of chicks fed guar meal and saponin-rich extract were significantly lower than control body weights at 21 days of age, whereas the weekly feed to gain ratio of chicks fed saponin-rich extract was higher than controls. Guar meal reduced severity of Eimeria tenella infection and guar saponin-rich extract exhibited antimicrobial activity against several common poultry pathogens.
... The therapeutic benefits of traditional remedies might depend upon a combination of constituents. For instance saponins have been reported to show potent sedative activity, they have also been shown to have antagonistic activity on amphetamine (Wagner et al., 1983) and also known to inhibit spontaneous motor activity in mice (Dubois et al., 1986). It is, therefore, likely that the saponin content of this extract might be contributing in part to the observed pharmacological effects. ...
Effects of the aqueous extract of Sphaeranthus senegalensis Vaill. (Family: Compositae) were studied on spontaneous motor activity, exploratory behaviour, rota-rod performance and pentobarbital sleeping time in mice. Preliminary phytochemical evaluation and acute toxicity (LD(50)) values were also studied. The extract (50 and 100 mg/kg p.o.) produced reduction in spontaneous motor activity, exploratory behaviour and motor coordination and prolonged pentobarbital sleeping time. Glycosides, saponins and tannins were shown to be present in the extract. The i.p. LD(50) in mice was 2735.61 and 5000 mg/kg orally. The results suggest that the aqueous extract of S. senegalensis contains some active principles, which may be sedative in nature.
... On the other hand, the sedative activity observed may be attributed to the phytochemical constituents reported in the plant (Delaveau et al., 1979) especially the saponins. Saponins have been implicated in opioid receptor mechanism (Huong et al., 1995) through antagonistic activity (Wagner et al., 1983) by binding on the sensory nerve terminals. ...
The neuropharmacological activities of the aqueous extract of Diospyros mespiliformis stem bark were screened in mice. The extracts effect on pentobarbital-induced sleeping time, pentylenetetrazole induced seizure, spontaneous motor activity (SMA), exploratory behaviour, and rota-rod performance (motor coordination) were evaluated. The extract (100 and 200 mg/kg p.o.) produced a significant (P<0.05) prolongation of pentobarbital-induced sleeping time, and reduced the SMA and exploratory behaviour. The extract prolonged onset of the phases of seizure activity but did not protect mice against lethality induced by pentylenetetrazole. It also failed to affect the motor coordination test. These results suggest that the extract contained an agent with neuropharmacological activity that may be sedative in nature.
... On the other hand, the sedative activity observed may be attributed to the phytochemical constituents reported in the plant (Delaveau et al., 1979) especially the saponins. Saponins have been implicated in opioid receptor mechanism (Huong et al., 1995) through antagonistic activity (Wagner et al., 1983) by binding on the sensory nerve terminals. ...
Indigenous and traditional peoples have made major contributions to the enhancement and conservation of the world's biodiversity. Although this is increasingly recognized in international discourse, rights of these peoples to continue their traditional practices are threatened by the globalized economy. Science implicitly denies their contribution to biodiversity conservation and enhancement by referring to their lands as 'wild' or 'wilderness'. It also effectively undermines their rights by claiming that the biodiversity fostered by their traditional practices is a global resource. In order to counter these threats, we need not only to strengthen the rights of indigenous and traditional peoples, but also to reverse global trends that substitute economic and utilitarian models for the holistic concept of the 'sacred balance'.
... The therapeutic benefits of traditional remedies are often attributed to a combination of active constituents (Amos et al., 2001c). For instance, saponins are known to have antagonistic activity against amphetamine, sedative property, and decrease spontaneous motor activity in experimental animals (Wagner et al., 1983;Dubois et al., 1986). It is therefore, probable that the saponins component of the extract might contribute in part for the observed pharmacological activities. ...
The central nervous system (CNS) activity of the methanolic extract of Ficus platyphylla stem bark was studied on locomotor activity, pentobarbital sleeping time, exploratory behaviour, amphetamine-induced hyperactivity, apomorphine-induced stereotypy, active-avoidance and performance on tread mills (rota-rod), using mice and rats. The results revealed that the extract significantly reduced the locomotor and exploratory activities in mice, prolonged pentobarbital sleeping time in rats, attenuated amphetamine-induced hyperactivity and apomorphine-induced stereotypy in mice, dose-dependently. The extract significantly suppressed the active-avoidance response in rats, with no significant effect on motor co-ordination as determined by the performance on rota-rod. The results suggest that the extract may possess sedative principles with potential neuroleptic properties.
... The therapeutic benefits of traditional remedies are often attributed to a combination of active constituents (Amos et al., 2001c ). For instance, saponins are known to have antagonistic activity against amphetamine, sedative property, and decrease spontaneous motor activity in experimental animals (Wagner et al., 1983; Dubois et al., 1986 ). It is therefore , probable that the saponins component of the extract might contribute in part for the observed pharmacological activities. ...
Purpose of the study was to investigate the effects of daily oral feeding 15% of powdered leaves of Murraya koeingii (MK) (commonly called as Curry patta) and 10% powder of seeds of Brassica juncea (BJ) (commonly called as Rai) for 60 days on serum glucose concentrations and kidney functions in streptozotocin (STZ; 100mg/kg) diabetic rats. Serum glucose levels, body weight, urine volume, serum creatinine, and urinary albumin (UAE) levels were monitored on day 0, 10, 25, 40, and 70 of the experiment. After 60 days of STZ administration, urine volume per day and UAE levels were significantly higher (P<0.0005) in diabetic controls (DC) as compared to normal controls (NC). Although feeding of the MK/BJ showed a trend towards improvement in most of the parameters, results were not statistically different from the DC except in serum creatinine values in BJ-fed rats on day 70. Thus, these plants can be best utilized by promoting them as preferable food adjuvants for diabetic patients.
Migraine is a common, chronic, incapacitating neuro vascular disorder characterized by attacks of severe headache, autonomic nervous system dysfunction, and,
Exploration of high-entropy alloys for hydrogen storage has recently attracted attention owing to their serious defects, high-entropy induced reduction of thermodynamic stability and abundant raw metal elements. In this study, new Zr-based high-entropy alloys with Laves phases were designed where their structure and hydrogen storage properties were adjusted by introducing Mg element. The results show that the addition of Mg element makes the crystal structure of Zr2MgV2−xFexCrNi (x = 0 and 1) alloys change from AB2 type to A3B4 type structure, which further leads to the improvement of their hydrogen storage capacity and hydrogen sorption kinetics. The Zr2MgV2CrNi and Zr2MgVFeCrNi high-entropy alloys can rapidly absorb 0.8 wt% (0.43 H/M) and 0.9 wt% (0.48 H/M) hydrogen at room temperature, respectively, three times higher than those of the Zr-based alloys without Mg-substitution. And more importantly, the absorbed hydrogen of Zr2MgV2CrNi and Zr2MgVFeCrNi high-entropy alloys can be partially released at room temperature with distinct desorption processes. These capacity and kinetic enhancements should be related to the higher lattice parameters, lower electron concentration, severe lattice distortion and smaller average valence electron concentration (VEC) of those alloys. The development of Mg-containing Zr-based high-entropy alloys with Laves phases provides a new idea for the design of new hydrogen storage materials.
Objectives:
Fever is a condition when the body experiences an increase in average body temperature above normal level. Maja fruit (Crescentia cujete L.) contains chemical compounds including alkaloid, flavonoid, saponin, and terpenoid, suspected as potential antipyretics.
Methods:
The study aimed to determine the antipyretic activity of ethanol extract of Maja fruit. A total of 25 male white mice of the DDY strain (20-30 g). These treatments divided into three groups with a dose extract of 125, 250, 500 mg/kg BW, standard groups of ibuprofen 400 mg/kg BW, and control groups of CMC-Na 1%. Mice were injected intraperitoneally with 0.1 cc of DPT vaccine-induced. Observations were made by measuring the rectal temperatures of mice using a digital thermometer before DPT vaccine injected or average temperatures, at 0 min (after DPT vaccine injected), 60, 120, 180, and 240 min after administering the test material. The differences between the positive control group, test group, and the negative control group were compared using statistical analysis using one-way variance analysis (ANOVA). The results were considered statistically when the value is (p<0.05).
Results:
The above phytochemical screening results showed that alkaloids, flavonoids, and saponins were present in the Maja fruit powder and extract (C. cujete L.). Based on the results of the statistical analysis obtained, i.e., Group II was not significantly different from Group III and Group IV (p≤0.05) and was significantly different from Group I and Group V. Group I was significantly different from Group II, Group III and Group IV and was not significantly different from Group V (p≥0.05).
Conclusions:
The study showed that Maja fruit mice's antipyretic behavior at doses of 125, 250, and 500 mg/kg BW was confirmed as a result in reducing the body temperature of male mice. The 500 mg/kg BW dosage of Maja fruit extract (C. cujete L) effectively reduced fever.
Background
This study was designed to evaluate the anxiolytic and hypoglycemic potential of methanolic extract of Cissus adnata Roxb. is a crucial medicinal plant used in many disorders belongs to Vitaceae family.
Methods
Elevated plus maze (EPM) test and hole board test was applied for the anxiolytic activity with the Swiss albino mice. The hypoglycemic activity was measured by the glucose tolerance test in mice model. The capacity to produce the desired effect of the plant extract (200 and 400 mg/kg) was compared with the anxiolytic drug of standard diazepam (1 mg/kg i.p.) and anti-diabetic drug glibenclamide (10 mg/kg i.p.), respectively.
Results
The phytochemical screening of Cissus adnata extract exposed the presence of carbohydrate, phenol, flavonoid, saponins, cardiac glycoside , tannin, and gum. The anxiolytic effect was detected in both experiments which significantly raised the number of head dips and the time spent in the open arm of the EPM (p<0.05) as the dose enlarged. Hypoglycemic study of the extracts shows better effect by reducing blood glucose level.
Conclusions
The better anxiolytic and hypoglycemic activities in the present study are due to the existence of various phytochemical constituents like saponins, flavonoids, terpenoids, phenols, and tannins in this methanolic extract.
Es wurden intensiv weiterbearbeitet: Polyphenole, Anthrachinone und biogenetisch verwandte Körper, Alkaloide und Saponine und Sapogenine. Über Nutzpflanzen (mit zahlreichen Synonymen) vgl. S. 829–835, 1882 von Rudolf Mansfelds Kulturpflanzen-Verzeichnis (vide Ref. [1], S. 372 in Bd. VIII) und für Ziziphus (= Zizyphus)-Arten Ref. [2]). Eine schöne Arbeit mit zahlreichen blattanatomischen Abbildungen (Haare, Gerbstoffzellen, Drusen von Calciumoxalat) wurde der nordamerikanischen (Süd-Canada bis Guatemala) Gattung Ceanothus gewidmet (3).
Glinus oppositifolius
is a small herb, widely used in the traditional medicine of Bangladesh in treatment of a variety of diseases and disorders such as insomnia, pain, inflammation, jaundice, and fever. The present study evaluated the sedative and anxiolytic potentials of the ethanol extract of leaves of
G. oppositifolius
(EEGO) in different behavioral models in mice. The sedative activity of EEGO was investigated using hole cross, open field, rotarod, and thiopental sodium- (TS-) induced sleeping time determination tests, where the elevated plus maze (EPM) and light-dark box (LDB) exploration tests were employed to justify the anxiolytic potentials in mice at the doses of 50, 100, and 200 mg/kg. The results demonstrated that EEGO significantly inhibited the exploratory behavior of the animals both in hole cross and in open field tests in a dose-dependent manner. It also decreased motor coordination and modified TS-mediated hypnosis in mice. In addition, EEGO showed anxiolytic potential by increasing the number and time of entries in the open arm of EPM, which is further strengthened by increase in total time spent in the light part of LDB. Therefore, this study suggests the sedative and anxiolytic properties of the leaves of
G. oppositifolius
and supports the traditional use of this plant in treatment of different psychiatric disorders including insomnia.
This review covers the isolation and structure determination of triterpenoids including squalene derivatives, lanostanes, cycloartanes, dammaranes, euphanes, tirucallanes, tetranortriterpenoids, quassinoids, lupanes, oleananes, friedelanes, ursanes, hopanes, isomalabaricanes and saponins. The literature from January to December 2003 is reviewed and 215 references are cited.
The neuropharmacological activities of the aqueous extract of Alangium salvifolium (Linn.f.) stem bark extract were screened in rat. The extract effect on pentobarbital-induced sleeping time, pentylenetetrazole induced seizure, spontaneous motor activity (SMA), exploratory behaviour and rota-rod performance (motor coordination) were evaluated. The extract (100 and 200 mg/kg p.o.) produced a significant (p < 0.05) prolongation of pentobarbital-induced sleeping time and reduced the spontaneous motor activity and exploratory behaviour. The extract prolonged onset of the phases of seizure activity but did not protect rats against lethality induced by pentylenetetrazole. It also failed to affect the motor coordination test. These results suggest that the extract contained an agent with neuropharmacological activity that may be sedative in nature.
A dammarane derivative dihydrojujubogenin-2-en-1-one, which possesses a skeleton and pharmacophore partially similar to those of Territrem B, a potent AChE inhibitor, was synthesized via three different paths. The anti-AChE activity of this compound and related analogue was measured.
AbstractA practical method for large‐scale preparation of acid‐labile aglycones including protopanaxadiol, protopanaxatriol, cycloastragenol, and jujubogenin from the corresponding glycoside containing fraction was developed. The key point of this improved method is to generate and maintain the critical reaction conditions, anhydrous and strongly basic, in situ. This effort over comes the weakness of the reported method for oxidative cleavage of glycones and scales up the preparation of these acid‐labile aglycones for further studies.
Plant saponins are a group of naturally occuring triterpene or steroid glycosides which include a large number of biologically and pharmacologically active compounds. Saponins have been shown in both in vitroand in vivoexperimental test systems during the last decade to possess a broad spectrum of biological and pharmacological activities. This review will summarize some of the recent advances concerning cancer-related activity, immunostimulating, immunoadjuvant, antihepatotoxic, antiphlogistic, antiallergic, molluscicidal, hemolytic, antifungal, antiviral, and hypoglycemic activities. In addition, the effects on the cardiovascular system and the central nervous system will be discussed together with other miscellaneous effects. Studies of structure/activity relationships and mechanism of action will be presented.
A new bitter saponin containing a novel seco ring D dammarane triterpenoid aglycone has been isolated from the bark of Colubrina elliptica. The structure was determined from a series of 2-D NMR experiments.
This paper reviews the important biological and pharmacological activities of saponins reported over the last few years. These include cancer-related activity, as well as antiphlogistic and antiallergic, immunomodulating, antihepatotoxic, antiviral, hypoglycemic, antifungal and molluscicidal activities. The action of saponins on the cardiovascular, central nervous, and endocrine systems and other miscellaneous effects are also discussed.
A new triterpene saponin was isolated from the roots ofAmpelozizyphus amazonicus together with the known 3-O-β-d-glucopyranosyl-20-O-α-l-rhamnopyranosyljujubogenin and the known triterpenes melaleucic acid, 3β,27α-dihydroxylup-20(29)-en-28β-oic acid, betulinic acid, betulin, lupeol. The structure of this saponin was elucidated as 3-O-[β-d-glucopyranosyl(1→2)α-l-arabinopyranosyl]-20-O-α-l-rhamnopyranosyljujubogenin by spectral analysis and chemical transformations.
Three new bitter saponins, designated mabioside A, B and C, were isolated from the bark of Colubrina elliptica and were determined to be 3-O-[-JL-rhamnopyranosy]-(1 → 6)-β-D-glucopyranosyl-15-O-[β-D- glucopyranosyl] mabiogenin, 3-O-[-L-rhamnopyranosy]-(1 → 6)-[β-D-glucopyranosyl-(1 → 2)]-β-D-glucopyranosyl}mabiogenin and 3-O-[-L-rhamnopyranosyl-(1 → 6)-β-D-glucopyranosyl] mabiogenin, respectively. The structures were elucidated by using a combination of 2D NMR techniques (H-H COSY, H-H DQF-COSY, RCT-COSY, C-H COSY, FLOCK, NOESY).
The synthesis of analogues of the potent acetylcholinesterase inhibitor, Territrem B, was carried out starting from the naturally occurring jujubogenin glycosides. Dihydrojujubogenin-2-en-1-one (1), a dammarane derivative that possesses a skeleton and pharmacophore partially similar to those of Territrem B, was synthesized via three different paths. The derivative 21, which contains two potential pharmacophores, was also synthesized. The anti-AChE activity of the analogues was measured. The aromatic ring moiety seemed to be less important when compared with the 2-en-1-one pharmacophore.
Triterpenoid saponins isolated from various sources are reviewed. The recent techniques used in their isolation and structure elucidation are discussed. A compilation of the triterpenoid saponins isolated and characterized during the period 1979–1986 along with their occurrence is included. The biological activities of the triterpenoid saponins are also covered.
Three new triterpenoid saponins were isolated from the barks of Zizyphus joazeiro and characterized as jujubogenin 3-O-α-l-arabinofuranosyl-(1 → 2)-[β-d-glucopyranosyl(1 → 3)]-α-l-arabinopyranoside, its 4‴-O-sulphate and 3″,4‴-di-O-sulphate, respectively. FAB-MS was useful in providing information on the molecular weight of the complex oligoglycoside sulphates.
Nauclea latifolia Smith (Rubiaceae) is a small tree found in tropical areas in Africa. It is used in traditional medicine to treat malaria, epilepsy, anxiety, pain, fever, etc. Objective: The aim of this study was to investigate the effects of Nauclea latifolia roots decoction on the peripheral and central nervous systems and its possible mechanisms of action.
The analgesic investigation was carried out against acetic acid-induced writhing, formalin-induced pain, hot-plate and tail immersion tests. The antipyretic activity was studied in Brewer's yeast-induced pyrexia in mice. Rota-rod test and bicuculline-induced hyperactivity were used for the assessment of locomotor activity.
Nauclea latifolia induced hypothermia and had antipyretic effects in mice. The plant decoction produced significant antinociceptive activity in all analgesia animal models used. The antinociceptive effect exhibited by the decoction in the formalin test was reversed by the systemic administration of naloxone, N(ω)-L-nitro-arginine methyl ester or glibenclamide. In contrast, theophylline did not reverse this effect. Nauclea latifolia (antinociceptive doses) did not exhibit a significant effect on motor coordination of the mice in Rota-rod performance. Nauclea latifolia protected mice against bicuculline-induced behavioral excitation.
Overall, these results demonstrate that the central and peripheral effects of Nauclea latifolia root decoction might partially or wholly be due to the stimulation of peripheric opioid receptors through the action of the nitric oxide/cyclic monophosphate guanosin/triphosphate adenosine (NO/cGMP/ATP)-sensitive- K(+) channel pathway and/or facilitation of the GABAergic transmission.
Ampelozizyphus amazonicus Ducke is a plant used in Brazilian folk medicine to both prevent malaria and act as a depurative.
We have investigated the effects of an ethanol crude extract of roots of Ampelozizyphus amazonicus (CEAaD), a chemically characterized saponin mixture (SAPAaD), as well as a saponin-free fraction (SAPAaD-free) obtained from CEAaD on diuresis in rats.
Wistar rats under ad libitum water conditions or water deprivation for 12h prior to the start of the experiment were volume-expanded with 0.9% NaCl (4% body weight, by gavage) containing either CEAaD, SAPAaD, or SAPAaD-free at the doses indicated in the text. Rats were individually housed in metabolic cages, and urine volume was measured every 30 min throughout the experiment (3 h).
CEAaD increased urine volume in rats under conditions of both free access to water and under water deprivation. In the latter condition, CEAaD (150 mg/kg) increased the urine volume from zero to 0.9+/-0.1 ml/120 min, n=6). Similarly, the SAPAaD-free (50-200 mg/kg) mixture also increased the urine volume. In contrast, SAPAaD (12.5-1000 mg/kg) produced a significant reduction (p<0.01) in diuresis under conditions of both water deprivation and with free access to water prior to the start of the experiment.
Our data indicate that CEAaD contains compounds that cause both diuresis and antidiuresis and that the antidiuretic effect is due mainly to the presence of saponins.
Saponins occur widely in plant species and exhibit a range of biological properties, both beneficial and deleterious. This review, which covers the literature to mid 1986, is concerned with their occurrence in plants and their effects when consumed by animals and man. After a short discussion on the nature, occurrence, and biosynthesis of saponins, during which the distinction between steroidal and triterpenoid saponins is made, the structures of saponins which have been identified in a variety of plants used as human foods, animal feedingstuffs, herbs, and flavorings are described. Many of these compounds have been characterized only during the last 2 decades, and modern techniques of isolation, purification, and structural elucidation are discussed. Particular consideration is given to mild chemical and enzymatic methods of hydrolysis and to recent developments in the application of NMR and soft ionization MS techniques to structural elucidation. Methods currently used for the quantitative analysis of saponins, sapogenols, and glycoalkaloids are critically considered; advances in the use of newer methods being emphasized. The levels of saponins in a variety of foods and food plants are discussed in the context of the methods used and factors affecting these levels, including genetic origin, agronomic, and processing variables, are indicated. Critical consideration is given to the biological effects of saponins in food which are very varied and dependent upon both the amount and chemical structure of the individual compounds. The properties considered include membranolytic effects, toxic and fungitoxic effects, adverse effects on animal growth and performance, and the important hypocholesterolemic effect. A final section deals briefly with the pharmacological effects of saponins from ginseng, since use of this plant is increasing in certain sections of western society as well as being traditional in the Orient.
A new C31 dammarane-type triterpenoid saponin has been isolated from the roots of Ampelozizyphus amazonicus. Its structure was elucidated to be ampelozigenin-15 alpha-O-acetyl- 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside by 1D and 2D NMR spectroscopic methods, and by chemical transformations. Ampelozigenin is a novel triterpene, (20R,22R)-16 beta,22:16 alpha, 30-diepoxydammar-24(24')- methylene-3 beta, 15 alpha, 20-triol.
Three novel saponins, mabiosides C-E, were isolated from the bark of Colubrina elliptica together with the known mabioside B and [alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->3)-alpha-L- arabinopyranosyl]-(1-->3)-jujubogenin. All the structures were established by spectroscopic methods.
A new triterpenoid saponin, bacoside A3, a constituent of bacosides the saponin mixture of Bacopa monniera, was isolated and characterized. Its structure was established as 3-beta-[O-beta-D-glucopyranosyl(1-->3)-O- [alpha-L-arabinofuranosyl(1-->2) ]O-beta-D-glucopyranosyl)oxy]jujubogenin by chemical and spectral analyses. The cis-isomer of ebelin lactone was also obtained as one of the artefacts of the aglycone and its structure revised.
High-field nmr experiments have been used to determine the structures of three new saponins, zizyphoisides C, D, and E [1-3], isolated from Alphitonia zizyphoides, a medicinal plant found in the Samoan rain forest. The saponins consist of the aglycone, jujubogenin, to which are attached three sugar units and an unsaturated side-chain. The three compounds are similar except for the location of an acetyl group on one of the sugar units.
Antifungal assay-guided isolation of the 95% ethanol extract of the stems of Colubrina retusa yielded jujubogenin 3-O-alpha-L-arabinofuranosyl(1-->2)-[beta-D-glucopyranosyl (1-->3)]-alpha-L-arabinopyranoside (1), which showed modest growth-inhibitory effects against Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus (MICs, 50 microg/mL). In addition, two new minor saponins, jujubogenin 3-O-alpha-L-arabinofuranosyl(1-->2)-[2-O-(trans, cis)p-coumaroyl-beta-D-glucopyranosyl(1-->3)]-alpha-L-arabinopy ranosi de (2), and jujubogenin 3-O-(5-O-malonyl)-alpha-L-arabinofuranosyl (1-->2)-[beta-D-glucopyranosyl(1-->3)]-alpha-L-arabinopyranoside (3), were obtained. Saponin 2 was marginally active against only C. neoformans, with a MIC of 50 microg/mL, while 3 was inactive. NMR spectroscopy was used extensively for the structure determination of these compounds. The previously reported ambiguity of the NMR assignments of jujubogenin saponins for carbons -26 to -29 was clarified by a comprehensive analysis of the NMR spectra of 1.
Three new jujubogenin glycosides, namely, 3' '-O-acetylcolubrin (1); 3' ',2' "-O-diacetylcolubrin (2), and 3' '-O-acetyl-6' '-O-trans-crotonylcolubrin (3), were isolated from the leaves of Colubrina asiatica, in addition to the known colubrin, rutin, and kaempferol 3-O-rutinoside. Compounds 1-3 were isolated and purified via a combination of chromatographic procedures, and determined structurally using spectroscopic methods.
Behavioral effects of the aqueous extract of Guiera senegalensis on the central nervous system of mice and rats were investigated. Spontaneous motor activity, pentobarbital sleeping time, amphetamine-stereotyped behavior, exploratory activity and performance on treadmills (rota-rod) were evaluated. The results revealed that the aqueous extract of G. senegalensis reduced spontaneous motor activity in mice, prolonged the duration of pentobarbital sleeping time in rats and attenuated amphetamine-induced stereotype behavior in rats. The extract also decreased exploratory activity in mice and had no observable effects on motor coordination (rota-rod) at the doses tested. The results suggested that the crude aqueous extract of G. senegalensis possesses some biologically active principles that are sedative in nature.
The major alkaloid from the bark of Colubrina asiatica was isolated and identified as O-methyl-dauricine (III).
Acid hydrolysis of the saponin of the seeds of Zizyphus jujuba afforded ebelin lactone, which yielded the sapogenin, jujubogenin, on Smith-de Mayo degradation. The mechanism of conversion of jujubogenin into ebelin lactone has been elucidated. Hovenoside G of Hovenia dulcis and bacoside A of Bacopa monniera which produce ebelin lactone on acid hydrolysis have also been found to yield jujubogenin on Smith-de Mayo degradation.
Ebelin lactone was obtained on hydrolysis of the saponin fraction of the seeds of Zizyphus jujuba Mill. var. spinosus Hu.
Proton decoupled and undecoupled 13C n.m.r. spectra have been measured on a number of hexopyranoses. The direct coupling constants between the anomeric carbon atoms and protons {1J[13C–H(1)]} were found to be ca. 160 in the β-anomers and ca. 170 Hz in the α-anomers; the difference of ca. 10 Hz between pairs of anomers was found in almost all cases. Chemical shifts and 1J(13CH) values of the other carbon atoms in the pyranose rings were also measured.
Two new flavonol triosides have been isolated from the leaves of Colubrina faralaotra (Rhamnaceae) and their structures elucidated as kaempferol-3-O-[β-d-glucopyranosyl-(1 → 3)-4″′-O-acetyl-α-l-rhamnopyranosyl-(1 → 6)-β-d-galactopyranoside] and the corresponding quercetin analogue mainly by 1H and 13C NMR spectroscopy (including T1, measurements).
The acute toxicity and the sedative action of spinosin isolated fromZizyphus seeds have been tested with mice.
Spinosin possessed a very weak toxicity and at relatively high dose showed a significant sedative action in a ladder-climbing
test, a potentiation of hexobarbital-induced hypnosis and an antagonistic effect on caffeine-induced hyperactivity.
Pharmacological properties of fractions obtained from Zizphus seeds were estimated by a screening method consisting of 5 tests: neuropharmacological observations in mice, tests on the respiratory and cardiovascular systems in rats, tests on the isolated guinea pig ileum, potentiation of hexobarbital anesthesia; and inhibition of writhing syndrome induced by acetic acid. Z No. 2, Z No. 3 and Z No. 5 were found to have sedative activity as a result of tests I and IV, and were estimated to have analgesic and antiinflammatory properties from test V. Z No. 5a was shown to have the strongest activities. Blood pressure showed a prolonged elevation by fat and oil soluble fractions, which were not eliminated by phentolamine or hexamethonium. Water soluble fractions caused a transient hypotension partially eliminated by atropine but not by diphenhydramine or propranolol. Increase of the contraction induced by nicotine was produced by all fractions. Increase of the contraction induced by serotonin was produced by fat and oil fractions. Water soluble fractions showed cholinergic activity. Papaverine like activity was noted in Z No. 3.