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The effects of Cassia auriculata and Cardiospermum halicacabum teas on the steady state blood level and toxicity of carbamazepine.

A study was conducted using male Wistar rats as the experimental model, to compare the effects of concurrent administration of herbal tea prepared from dried flowers of Cassia auriculata or aerial parts of Cardiospermum halicacabum and carbamazepine, on (a). steady state serum levels of the prescription drug, and (b). changes in toxicity (as assessed by changes in general behaviour, haematological parameters, and liver and kidney function) that may occur due to drug interaction. Results demonstrate that in rats receiving the Cassia auriculata tea and carbamazepine, the blood levels of the prescription drug were significantly enhanced by 47.1% (P<0.04), when compared with the levels in animals receiving only carbamazepine for the same time period, with no apparent changes in toxicity. In animals receiving the Cardiospermum halicacabum tea, there were no significant changes in the blood levels of carbamazepine or drug-related toxicity. Cassia auriculata tea has therefore the potential to influence the bioavailability of carbamazepine, and hence its therapeutic actions. Concurrent ingestion of carbamazepine with herbal teas containing Cassia auriculata is therefore best avoided by patients under treatment for epilepsy.

Animals↗

Two new antifungal saponins from the Tibetan herbal medicine Clematis tangutica.

Bioassay-guided fractionation of the ethanol extract of the aerial parts of Clematis tangutica led to the isolation of two new antifungal triterpene saponins. Their structures were determined to be 3- O-alpha- L-arabinopyranosyl hederagenin 28- O-alpha- L-rhamnopyranosyl ester ( 1) and 3- O-beta- D-glucopyranosyl-(1--> 4)-alpha- L-arabinopyranosyl hederagenin 28- O-alpha- L-rhamnopyranosyl ester ( 2) on the basis of spectral data and chemical evidence. Inhibitory activities of the two saponins against seven fungal strains were evaluated. Compounds 1 and 2 showed evident antifungal activity (MIA approximately 2.5 micrograms/disc) against Saccharomyces cerevisiae, similar to the positive control amphotericin B and ordinary activities (MIA approximately 10 micrograms/disc) against Penicillium avellaneum UC-4376, Candida glabrata, Trichosporon beigelii and Pyricularia oryzae. Compound 2 is a better antifungal agent than compound 1 against most of the fungal strains that were tested.

Antifungal Agents↗

Trypanocidal constituents in plants 6. 1) Minor withanolides from the aerial parts of Physalis angulata.

Further study of the methanol extract of the aerial parts of Physalis angulata (Solanaceae) resulted in the isolation of new withanolides, designated physagulins L, M and N, together with known withanolide, physagulin D and flavonol glycoside, quercetin 3-O-rhamnosyl-(1-->6)-galactoside. The chemical structures of these new withanolides were elucidated by detailed spectroscopic analyses to be (20R,22R)-15alpha-acetoxy-5alpha,6beta,14beta,17beta,27-pentahydroxy-1-oxo-witha-2, 24-dienolide, (20S,22S)-15alpha-acetoxy-5alpha,6beta,14alpha,23beta-tetrahydroxy-1-oxo-witha-2,16,24-trienolide and (20S,22R)-15alpha-acetoxy-5beta,6beta-epoxy-14alpha-hydoxy-3beta-methoxy-1-oxo-witha-16,24-dienolide, respectively. All these compounds showed weak trypanocidal activity against trypomastigotes, an infectious form of Trypanosoma cruzi, the etiologic agent for Chagas' disease. Withanolides obtained in the previous paper showed considerable trypanocidal activity, suggesting the structure-activity relationships.

Animals↗

Five new triterpene glycosides from Lysimachia foenum-graecum and evaluation of their effect on the arachidonic acid metabolizing enzyme.

Five new oleanane-type triterpene saponins, named foenumosides A ( 1), B ( 2), C ( 3), D ( 4) and E ( 5), were isolated from the aerial parts of Lysimachia foenum-graecum Hance. Their structures were identified on the basis of 1D and 2D NMR techniques, including H-H COSY, HMQC, HMBC, HMQC-TOCSY, ROESY experiments as well as chemical methods. We have evaluated the cytotoxity of 1 - 5 against rat and human polymorphonuclear leukocytes and the effect of 5 on the arachidonic acid metabolizing enzyme. All compounds showed a high degree of toxicity except for compound 5, while 5 notably reduced the production of leukotriene B (4) (LTB (4)) from rat peritoneal leukocytes with an IC (50) value of 74 microM without inhibiting human elastase. Compound 5 also reduced the production of 12-HHTrE and 12-HETE by 14 % and 50 % as a measurement for cyclooxygenase-1 and 12-lipoxygenase inhibition at 100 microM.

Animals↗

Essential oil composition of aerial parts of Angelica glauca growing wild in North-West Himalaya (India).

Fresh aerial parts of Angelica glauca, growing wild in Kashmir valley in higher Himalaya (Jammu and Kashmir, India), collected at flowering stage from different locations, on hydro-distillation provided a refreshing light pale coloured essential oil with characteristic floral woody flavour. The oil was found to be a complex mixture of mono- and sesquiterpenes and 34 compounds accounting for nearly 97.4% of the oil were characterized with the help of capillary GC, GC-MS, and NMR. Major compounds of the oil were characterized as alpha-phellandrene (13.5%), trans-carveol (12.0%), beta-pinene (11.7%), thujene (7.5%), beta-caryophyllene oxide (7.2%), beta-caryophyllene (7.0%), gamma-terpinene (6.7%), nerolidol (6.5%), beta-bisabolene (5.2%) and germacrene D (4.5%). It is the first report to exploit the essential oil from Himalayan A. glauca herb collected at flowering stage.

Angelica↗

Anticholinesterase activity in an alkaloid extract of Huperzia saururus.

Huperzia saururus (Lam.) Trevis. (Lycopodiaceae) is used widely in Argentinian traditional medicine as an aphrodisiac and for memory improvement. An aqueous extract from the aerial parts was obtained by decoction, revealing the presence of alkaloids, among other constituents. By partition with organic solvent in alkaline media, alkaloids were extracted and then purified by gel permeation. We studied the anticholinesterase activity in vitro of the alkaloid extract using erythrocyte membranes and human serum as sources of acetylcholinesterase and pseudocholinesterase, respectively. The results show a marked inhibition of true acetylcholinesterase with an IC50 value of 0.58 microg/ml. Low inhibition of pseudocholinesterase was observed (IC50 value = 191 microg/ml). This shows a selectivity of the extract for the true acetylcholinesterase. Furthermore, chemical study of the bioactive extract was performed by GC-MS, revealing the presence of seven Lycopodium alkaloids, including some not identified previously: sauroxine, 6-hydroxylycopodine, N-acetyllycodine, lycopodine, lycodine, N-methyllycodine, and clavolonine. Further investigations will be undertaken in order to discover which compound/s are responsible for the aqueous extract's acetylcholinesterase activity.

Acetylcholinesterase↗

Isolation and on-line identification of antioxidant compounds from three Baccharis species by HPLC-UV-MS/MS with post-column derivatisation.

The aqueous extracts of aerial parts of Baccharis trimera (Less.) DC., B. crispa Spreng. and B. usterii Heering (Asteraceae) displayed significant radical scavenging activity in a diphenylpicrylhydrazole (DPPH)/TLC assay. In order to rapidly identify the active principles, the crude extracts were analysed by HPLC-UV, and an HPLC-micro-fractionation of the extract of B. usterii was performed. Six quinic acids derivatives (1-6) were isolated from B. usterii by MPLC. The fractions were monitored by DPPH/TLC assay and a series of radical-scavenging quinic acid derivatives could be identified. The comparison of the HPLC profiles of the extracts of B. usterii, B. trimera and B. crispa was performed. In order to obtain complementary on-line structural information for all peaks of interest, HPLC-MS/MS together with HPLC-UV involving post-column addition of UV shift reagents was undertaken on the crude extract. The interpretation of these data permitted the on-line identification of known compounds, some of which are reported for the first time in this plant.

Antioxidants↗

Studies on the analgesic and anti-inflammatory effects of Sideritis candicans Ait. var. eriocephala Webb aerial part.

Different extracts and fractions from Sideritis candicans Ait. var. eriocephala Webb aerial part were investigated for their analgesic, anti-inflammatory and antimicrobial activities in mice. Results indicated that the extracts assayed showed anti-nociceptive activities because they were able to reduce the nociceptive response to chemical pain stimuli, such as in the acetic acid-induced writhing test. Moreover the extracts also possessed anti-inflammatory activity against carrageenan-induced paw oedema and TPA-induced ear oedema, being the chloroform fraction the most active. Further fractionation and analysis of this fraction revealed that the analgesic and anti-inflammatory activities found could be related in part to the presence of phytosterols, alpha and beta amyrin triterpenic derivatives and ent-kaurene type diterpenes in this species, since some of these compounds are endowed with these activities.

Acetic Acid↗

Antibacterial and cytotoxic activity of prenylated bicyclic acylphloroglucinol derivatives from Hypericum amblycalyx.

Two new bicyclic acylphloroglucinol derivatives, hypercalyxone A (1-[5,7-dihydroxy-2-methyl-3-(3-methyl-but-2-enyl)-2-(4-methyl-pent-3-enyl)-chroman-8-yl]-2-methyl-propan-1-one, 1) and B (1-[5,7-dihydroxy-2-methyl-3-(3-methyl-but-2-enyl)-2-(4-methyl-pent-3-enyl)-chroman-8-yl]-2-methyl-butan-1-one, 2), have been isolated from the petroleum ether extract of the aerial parts of Hypericum amblycalyx, together with two further compounds (1-[5,7-dihydroxy-2-methyl-2-(4-methyl-pent-3-enyl)-chroman-8-yl]-2-methyl-propan-1-one, 3 and 1-[5,7-dihydroxy-2-methyl-2-(4-methyl-pent-3-enyl)-chroman-8-yl]-2-methyl-butan-1-one, 4), which have been described only as semi-synthetic products. In addition, the known triterpene lup-20(29)-en-3-one was obtained. Structure elucidation was based on 1D and 2D NMR studies, as well as on data derived from mass spectrometry. The four acylphloroglucinol derivatives were evaluated for their cytotoxic and antibacterial activity. All compounds showed moderate cytotoxic activity against KB and Jurkat T cancer cells. Especially compounds 3 and 4 exhibited a strong antibacterial activity against different Gram-positive strains.

Anti-Infective Agents↗

Hepatoprotective activity of aqueous-methanol extract of Artemisia vulgaris.

The effect of a crude extract of the aerial parts of Artemisia vulgaris (Av.Cr) was investigated against D-galactosamine (D-GalN) and lipopolysaccharide (LPS) induced hepatitis in mice. Co-administration of D-GalN (700 mg[sol ]kg) and LPS (1 microg[sol ]kg) significantly (p < 0.05) raised the plasma levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in mice in the toxin group compared with the values in the control group. Pre-treatment of mice with different doses of Av.Cr (150-600 mg[sol ]kg) significantly (p < 0.05) reduced the toxin-induced rise in plasma ALT and AST. The hepatoprotective effect was further verified by histopathology of the liver, which showed improved architecture, absence of parenchyma congestion, decreased cellular swelling and apoptotic cells, compared with the findings in the toxin group of animals. These findings scientifically validated the traditional use of Artemisia vulgaris for various liver disorders.

Animals↗

Myricetin as the active principle of Abelmoschus moschatus to lower plasma glucose in streptozotocin-induced diabetic rats.

The antihyperglycemic action of myricetin, purified from the aerial part of Abelmoschus moschatus (Malvaceae), was investigated in streptozotocin-induced diabetic rats (STZ-diabetic rats). Bolus intravenous injection of myricetin decreased the plasma glucose concentrations in a dose-dependent manner in STZ-diabetic rats. Myricetin at the effective dose (1.0 mg/kg) significantly attenuated the increase of plasma glucose induced by an intravenous glucose challenge test in normal rats. A stimulatory effect of myricetin on glucose uptake of the soleus muscles isolated from STZ-diabetic rats was obtained in a concentration-dependent manner from 0.01 to 10.0 micromol/L. The increase of glucose utilization by myricetin was further characterized using the enhancement of glycogen synthesis in isolated hepatocytes of STZ-diabetic rats. These results suggest that myricetin has an ability to enhance glucose utilization to lower plasma glucose in diabetic rats lacking insulin.

Abelmoschus↗

Antidermatophyte activity of medicago extracts and contained saponins and their structure-activity relationships.

Saponin-rich extracts of Medicago sativa L. have been shown to display antifungal activity against a range of common fungibut only a few individual saponins have been tested against dermatophytes. Total saponins were separately obtained from roots and aerial parts of Medicago sativa, M. murex, M. arabica and M. hybrida. Nineteen saponins and three parent triterpenoids, were tested against three dermatophytic fungi Microsporum gypseum, Trichophyton interdigitale and T. tonsurans using mircowell plate serial dilution assay to determine the Minimum Inhibitory Concentration (MIC). Miconazole was used as a positive control. T. tonsurans appeared to be the most sensitive of the dermatophytes to the active compounds. Aglycones showed less antifungal effect than the glycosides, which displayed a range of activities. Monodesmosidic glycosides of medicagenic acid were the most active compounds, especially the 3-O-beta-D-glucopyranoside, which displayed MIC less than 0.09mm against all three fungi, although those of hederagenin and zanhic acid also showed weak activity (MIC 3.3mm against two fungal species). Bidesmosidic saponins had weaker activity than monodesmosidic ones. This corresponds to activity of these and similar compounds against other fungal species but this is the first comprehensive report of activity of Medicago saponins against dermatophytes.

Antifungal Agents↗

Diterpenes from the aerial parts of Salvia candelabrum and their protective effects against lipid peroxidation.

A methanolic extract of the aerial parts of Salvia candelabrum was subjected to multiple chromatographic separation under the guidance of anti-lipid peroxidation assay. From the most active fractions seven abietane and seco-abietane diterpenes were isolated by preparative TLC purification. Besides candesalvoquinone, candelabroquinone, 12- O-methylcandesalvone B, candesalvone B methyl ester and candelabrone (all reported earlier), the known candesalvone B and the new candesalvolactone were identified. The structures were established by means of mass spectroscopy and advanced 2D NMR methods. All the identified compounds were evaluated for antioxidant activity in enzyme-dependent (IC (50) values 3.49 - 10.42 microM) and enzyme-independent (IC (50) values 1.40 - 13.40 microM) systems of lipid peroxidation. All compounds displayed marked concentration-dependent effects in both tests as compared with those of authentic ascorbic, rosmarinic and caffeic acids. The differences in antioxidant capacities observed in the enzyme-independent system allowed conclusions concerning structure-activity relationships.

Antioxidants↗

Antimicrobial activity of the essential oil and extracts of Cordia curassavica (Boraginaceae).

In traditional Mexican medicine Cordia curassavica (Jacq) Roemer & Schultes is used to treat gastrointestinal, respiratory and dermatological disorders in Zapotitlán de las Salinas, Puebla (México). The aim of this work was to investigate antimicrobial activity of the essential oil, obtained by using Clevenger distillation apparatus, and hexane, chloroform and methanol extracts from aerial parts of Cordia curassavica. Antimicrobial activity was evaluated against 13 bacteria and five fungal strains. The oil and extracts exhibited antimicrobial activity against Gram-positive and Gram-negative bacteria and five fungal strains. Sarcina lutea and Vibrio cholerae were the strains more sensitive to the essential oil effect (MIC=62 microg/mL) and Vibrio cholerae for the hexane extract (MIC=125 microg/mL). Rhyzoctonia solani was the strain more sensitive to the essential oil effect (IC(50)=180 microg/mL) and Trichophyton mentagrophytes for the hexane extract (IC(50)=230 microg/mL). The essential oil was examined by GC and GC-MS. A total 11 constituents representing 96.28% of the essential oil were identified: 4-methyl,4-ethenyl-3-(1-methyl ethenyl)-1-(1-methyl methanol)cyclohexane (37.34%), beta-eudesmol (19.21%), spathulenol (11.25%) and cadina 4(5), 10(14) diene (7.93%) were found to be the major components. The present study tends to confirm the use in the folk medicine of Cordia curassavica in gastrointestinal, respiratory and dermatological diseases.

Animals↗

Binding studies for serotoninergic, dopaminergic and noradrenergic receptors of Valeriana adscendens Trel. extracts.

Valeriana adscendens Trel. (Valerianaceae) is a psychoactive plant usually used in magical-therapeutic rituals in traditional practices of the Northern Peruvian Andes. Previous studies have been carried out on extracts of aerial parts in order to validate its traditional use. The results indicated that Valeriana adscendens exerts important effects on the central nervous system. Aim of the present study is to evaluate if the effects on the central nervous system of Valeriana adscendens extracts can be associated with interaction with some CNS receptors. In this work we examined affinity and selectivity of two Valeriana adscendens extracts (methanolic and aqueous) towards 5-HT(1A), 5-HT(2A), 5-HT(2C) serotononergic, D(1) and D(2) dopaminergic, alpha(1) and alpha(2) noradrenergic receptors by a preliminary binding screen. The results show weak affinity to 5-HT(1A) for the aqueous extract. Both extracts showed affinity for D(1) receptors, but only for the methanolic extract the IC(50) value was determinable (30.14 microg/ml). No affinity for 5-HT(2A), 5-HT(2C) serotononergic receptors, alpha(1) and alpha(2) noradrenergic receptors and D(2) receptors was recorded for the extracts.

Animals↗

Hydroalcohol extract and fractions of Stachys lavandulifolia Vahl: effects on spontaneous motor activity and elevated plus-maze behaviour.

The present study aimed to investigate the anxiolytic effects of four fractions of Stachys lavandulifolia Vahl. The aerial parts of the plant were extracted with petroleum ether (PF), ethyl acetate (EF), butanol (BF) and water (AF) and tested for spontaneous motor activity and elevated plus-maze (EPM) behaviour in mice. The hydroalcohol extract (HE) and different fractions of S. lavandulifolia were administered intraperitoneally to male Syrian mice, at various doses, 30 min before the behavioural evaluation. The HE of S. lavandulifolia (at 50 mg/kg) increased the percentage of time spent (39%) and the percentage of arm entries in the open arms (53%). The HE (50 mg/kg), PF (25 and 50 mg/kg), EF (25 and 50 mg/kg) and AF (50 mg/kg) of S. lavandulifolia significantly increased the percentage of time spent and the percentage of arm entries in the open arms. The BF up to a dose of 50 mg/kg had no significant effects on any of the measured parameters in the EPM. The spontaneous locomotor activity was significantly decreased in animals injected with each plant fractions, compared with that of saline. The EF and AF showed the least and the most reduction in the activity, respectively. The anxiolytic effects of EF, PF and AF could be related to their content of flavonoids, phenylpropanoids or terpenoids.

Animals↗

Anticoagulant and antifibrinogenolytic properties of the aqueous extract from Bauhinia forficata against snake venoms.

The aqueous extract from aerial parts of Bauhinia forficata was able to neutralize the clotting activity induced by Bothrops and Crotalus crude venoms. The clotting time, upon human plasma, induced by B. moojeni venom was significantly prolonged. Clotting and fibrinogenolytic activities induced by isolated thrombin-like enzyme from Bothrops jararacussu were totally inhibited after incubation at different ratios. The extract was not able to neutralize the hemorrhagic activity induced by an Bothrops venoms, but it efficiently inhibited the edema induced by Crotalus durissus terrificus venom and isolated PLA2s. In addition, it did not inhibited the phospholipase A2 activity of Bothrops snake venoms. Interaction studies between Bauhinia forficata extract and snake venoms, when analyzed by SDS-PAGE, did not reveal any apparent degradation of the venom proteins. This extract is a promising source of natural inhibitors of serine-proteases involved in blood clotting disturbances induced by snake venoms.

Animals↗

Monoclonal antibodies against an arabinogalactan-protein from pressed juice of Echinacea purpurea.

Pressed juices of the aerial parts of Echinacea purpurea are used as non-specific immunostimulants, and arabinogalactan-proteins (AGPs) have been shown to be part of the active principle. Monoclonal antibodies against an AGP from pressed juice of Echinacea purpurea with complement-stimulating activity have been established by means of hybridoma techniques. To test the specificity of the antibodies, several other arabinogalactan-proteins from suspension cultures of Echinacea purpurea, the roots of Echinacea pallida, the aerial parts of Rudbeckia hirta, the roots of Baptisia tinctoria and gum arabic as well as an arabinogalactan from larch wood were tested in a competitive ELISA for cross reactivities. Chemical modifications at the periphery of the AGP molecules either by reduction of uronic acids or by dearabinosylation had no influence on the reactivity of the molecules towards the antibodies. For further characterization of the epitope, different Ara-Gal-oligosaccharides were used as antigens. A hexasaccharide consisting of a backbone of four molecules of 6-linked beta- D-Gal p, the second and the fourth of them branched at O-2 to an alpha- L-Ara f residue showed weak but reproducible cross reactivity, indicating that the antibodies may be at least in part directed to the carbohydrate moiety of the AGP. Testing of anti-AGP antibodies JIM 8 and LM 2 revealed good reactivity of LM 2 with the Echinacea AGP, whereas Jim 8 showed only very weak interaction.

Animals↗