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1.
Background:Despite introduction of modern antiepileptic drugs, 30% of epileptic patients are still drug resistant. Remarkable three-dimensional spatial structure of AdCA, yet the simplicity of the molecule, makes AdCA a promising lead compound. Methods:Sedative/motor impairment and 24-h mortality rate of AdCA were determined in mice. Impact of AdCA on (1) threshold and occurrence of clonic seizures induced by PTZ in mice, (2) incidence of tonic seizures induced by MES in mice, and (3) incidence of generalized seizures and duration of evoked afterdischarges in amygdala-kindled rats, were determined. The role of benzodiazepine receptors in the AdCA effect on clonic seizure threshold was also assessed. Results:AdCA showed sedative effect (TD50 = 224.5 [190.2-289.9] mg/kg). LD50 = 805.5 (715.2–988.1) mg/kg was obtained for AdCA. The compound increased PTZ seizure threshold from 180 mg/kg (p < 0.05) and also inhibited the incidence of clonic seizures (ED50 = 256.3 [107.4-417.3] mg/kg). AdCA also decreased afterdischarge duration (p < 0.01) and the incidence of generalized seizures (ED50 < 50 mg/kg) in the kindled rats. However, AdCA did not protect mice against tonic seizures induced by MES. The benzodiazepine receptor antagonist flumazenil prevented the increase of seizure threshold by AdCA. Conclusion:AdCA possesses anticonvulsant activity in kindling and PTZ models through the activation of benzodiazepine/GABAA receptors with acceptable therapeutic index. Key Words: Anticonvulsants, Flumazenil, Pentylenetetrazole  相似文献   

2.
As part of on-going efforts to use eco-friendly alternatives to chemical pesticides, methanol crude extracts of Plectranthus glandulosus and Callistemon rigidus leaves were sequentially fractionated in hexane, chloroform, ethyl acetate, and methanol to establish the most active fraction(s) against Callosobruchus maculatus in cowpea. Cowpea seeds (25 g) were treated with 0.5, 1, 2, and 4 g/kg of extract to evaluate the contact toxicity and F1 progeny production of the beetles in the laboratory. Mortality was recorded 1, 3, and 7 d postexposure. P. glandulosus hexane fraction was more toxic than the other fractions recording 100% mortality at 4 g/kg, within 7 d with LC50 of 0.39 g/kg. Hexane fraction of C. rigidus showed superior toxicity, causing 100% mortality at 4 g/kg within only 1 d of exposure with LC50 of 1.02 g/kg. All the fractions greatly reduced progeny emergence, with C. rigidus hexane fraction being the best progeny inhibitor. Fractions of P. glandulosus and C. rigidus leaves had sufficient efficacy to be a component of storage pest management package for C. maculatus.  相似文献   

3.
The purpose of this study was to evaluate the hypolipidemic effect of a methanolic extract from Opuntia joconostle seeds fed to mice in a hypercholesterolemic diet. Acute toxicity of the methanolic extract was investigated by an established method. Phenolic composition and antioxidant activity were determined by high-performance liquid chromatography and DPPH, respectively. The total phenolic content of Opuntia joconostle seeds was 47.85?±?1.29 mg gallic acid equivalents/g dry weight. The main phenolic compounds were identified as quercetin, rutin, and cafeic acid. Percent inhibition of DPPH+ was 49.76?±?0.49 %. The oral LD50 for the methanolic extract from the Opuntia joconostle seeds was >5,000 mg/kg BW. Mice fed a hypercholesterolemic diet for six days exhibited significantly (P?≤?0.001) higher plasma lipid levels than mice fed a normal diet. Remarkably, supplementation with methanolic extract from Opuntia joconostle at doses of 1, 2, and 5 g/kg body weight significantly (P?≤?0.001) prevented the increase in total cholesterol, low-density lipoprotein cholesterol, triglycerides level, and atherogenic index. Similar concentrations of the HDL cholesterol were observed in both treated and control groups. A significant dose-dependent reduction in lipid levels was noted for treated groups compared to the hypercholesterolemic group. We attribute this result to the seeds’ phenolic composition. This methanolic extract has potential to be included in short-term hypercholesterolemia treatment regimens as it exhibits hypolipidemic activity with no apparent toxic manifestations.  相似文献   

4.
Background:The polysialylated neural cell adhesion molecule (PSA-NCAM) is expressed in developing brain. Fetal brain damage is caused by different conditions such as seizure and hypoxia. The present study was designed to investigate the effect of maternal seizures on the number of PSA-NCAM positive cells in pup''s hippocampus. Methods: Female Wistar rats were divided into four groups: (a) kindled rats which received PTZ (40 mg/kg, i.p.) during pregnancy from embryonic day 14-19 (E14-E19) every 48 h, (b) kindled rats which did not receive PTZ during pregnancy, (c) non-kindle, pregnant rats which received PTZ injection (40 mg/kg, i.p.) during pregnancy from E14 to E19 every 48 h, and (d) non-kindle, pregnant rats which received injection with an equal volume of normal saline as sham controls. At postnatal day 14 (PD14), rat pups were perfused, and their brain were fixed, embedded and coronal sections stained by immunohistochemistry method. The number of PSA-NCAM positive cells per unit area in the pup''s hippocampus was counted. Results: The number of PSA-NCAM positive cells in the CA1, CA3, and DG fields of pup''s hippocampus, which was obtained from mothers who experienced PTZ injection during pregnancy, was decreased approximately 2.6 (P = 0.001), 2 (P = 0.001), and 2.1 (P = 0.001) times compared with non-PTZ treated maternal groups, respectively. Conclusions: Our study showed that maternal seizures reduced the number of neurons and also PSA-NCAM positive cells per unit area in the offspring hippocampus that it may cause impairment in hippocampal functions.Key Words: Epilepsy, Polysialylated neural cell adhesion molecule (PSA-NCAM), Hippocampus, Seizures  相似文献   

5.
Epilepsy an important CNS (central nervous system) problem that about 1% of world's population suffer of it. The aim of study was to evaluate of anticonvulsant effect of hydroalcoholic extract of Lavandula officinalis. In this study, anticonvulsant activity of the hydroalcoholic extract of Lavandula officinalis (L. officinalis) was studied against chemoconvulsant-induced seizures in male mice. Lavandula officinalis (100, 200, 400, 600 and 800 mg kg(-1)), diazepam (0.15 mg kg(-1)) and normal saline (10 mL kg(-1)) were injected intraperitoneally, respectively in different groups of mice, 30 min before nicotine (5 mg kg(-) i.p.). The onset time intensity and duration of convulsions and the percentage of death were recorded. Also the time-response (0, 15, 30, 45, 60 min before nicotine injection) for most effective dose of plant extract (600 mg kg(-1)) was investigated. The results showed that hydroalcoholic extract of Lavandula officinalis had anticonvulsant effect. The most effective dose of plant extract was 600 mg kg(-1). In time-response study for the most effective dose of extract (600 mg kg(-1)), the onset, duration and intensity of convulsion significantly (p < 0.05) increased, decreased and decreased, respectively for all tested times. The best response observed in 30, 45 and 60 min. The results showed significant anticonvulsant effect for hydroalcoholic extract of Lavandula.  相似文献   

6.
The oceans remain a major source of natural compounds with potential in pharmacology. In particular, during the last few decades, marine cyanobacteria have been in focus as producers of interesting bioactive compounds, especially for the treatment of cancer. In this study, the anticancer potential of extracts from twenty eight marine cyanobacteria strains, belonging to the underexplored picoplanktonic genera, Cyanobium, Synechocystis and Synechococcus, and the filamentous genera, Nodosilinea, Leptolyngbya, Pseudanabaena and Romeria, were assessed in eight human tumor cell lines. First, a crude extract was obtained by dichloromethane:methanol extraction, and from it, three fractions were separated in a Si column chromatography. The crude extract and fractions were tested in eight human cancer cell lines for cell viability/toxicity, accessed with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and lactic dehydrogenase release (LDH) assays. Eight point nine percent of the strains revealed strong cytotoxicity; 17.8% showed moderate cytotoxicity, and 14.3% assays showed low toxicity. The results obtained revealed that the studied genera of marine cyanobacteria are a promising source of novel compounds with potential anticancer activity and highlight the interest in also exploring the smaller filamentous and picoplanktonic genera of cyanobacteria.  相似文献   

7.
One of the most important global problems is protecting food from insect pests. The negative effects of synthetic insecticides on human health led to a resurgence of interest in botanical insecticides due to their minimal ecological side effects. Therefore, the insecticidal potential of hexane, acetone, and methanol extracts of Gnidia kraussiana Meisn roots at 1 and 5g/kg, and neem seed oil (NSO), used as standard insecticide, were evaluated. Ovicidal and larvicidal toxicity was tested by treating freshly laid eggs and larvae at different immature stages of Callosobruchus maculatus (F.). Cowpea (Vigna unguiculata) (L.) Walp seed damage and weight loss were assessed after a storage period of 4 mo. Repellency effects were detected in choice test using a linear olfactometer. All the fractions were toxic to C. maculatus; however, their bioactivities were inversely correlated with products polarity. Extracts proved to be more toxic than the commercial NSO. The acetone extract was more effective against immature stages of C. maculatus than the methanol extract; eggs, first-, and second-instar larvae being the more susceptible. No cowpea seed damage and weight loss were recorded from the seeds treated with hexane and acetone extracts at the dosage of 5 g/kg, after 4 mo of storage. Extracts evoked stronger repellency effects compared with the tested standard insecticide. According to the above, hexane and acetone extracts are good candidates for incorporation in integrated pest management programs for the control of C. maculatus in stored cowpea seeds.  相似文献   

8.
Total lipids from the Brazilian brown seaweed Sargassum vulgare were extracted with chloroform/methanol 2:1 and 1:2 (v/v) at room temperature. After performing Folch partition of the crude lipid extract, the lipids recovered from the Folch lower layer were fractionated on a silica gel column eluted with chloroform, acetone and methanol. The fraction eluted with methanol, presented a strong orcinol-positive band characteristic of the presence of sulfatides when examined by TLC. This fraction was then purified by two successive silica gel column chromatography giving rise to fractions F4I86 and F4II90 that exhibited strong activity against herpes simplex virus type 1 and 2. The chemical structures present in both fractions were elucidated by ESI-MS and 1H/13C NMR analysis HSQC fingerprints based on their tandem–MS behavior as sulfoquinovosildiacylglycerols (SQDGs). The main SQDG present in both fractions and responsible for the anti-herpes activity observed was identified as 1,2-di-O-palmitoyl-3-O-(6-sulfo-α-d-quinovopyranosyl)-glycerol.  相似文献   

9.
Chickpea (Cicer arietinum L.) genotypes, nine kabuli from Mexico and 9 desi from other countries, were investigated for their phenolic profiles and antioxidant activity (AA). Phenolics in methanol extracts (ME) were analyzed by ultra-performance liquid chromatography coupled to diode array detection and mass spectrometry (UPLC-DAD-MS), whereas the AA was measured as Trolox equivalents (TE) by ABTS, DPPH and FRAP methods. Twenty phenolic compounds were identified in the ME and their levels showed a great variability among the chickpea genotypes. Phenolic acids and flavonoids were the most abundant compounds in kabuli and desi genotypes, respectively. The AA values (μmol TE/ 100 g dw) by ABTS (278–2417), DPPH (52–1650), and FRAP (41–1181) were mainly associated with the content of sinapic acid hexoside, gallic acid, myricetin, quercetin, catechin, and isorhamnetin, suggesting they are the main compounds responsible for the AA. The sum of the AA obtained for standards of these compounds evaluated at the concentration found in the extracts accounted for 34.3, 69.8, and 47.0% of the AA in the extract by ABTS, DPPH, and FRAP, respectively. In the AA by DPPH, most of the mixtures of these compounds resulted in synergistic interactions. Three desi genotypes with black seeds (ICC 4418, ICC 6306, and ICC 3761) showed the highest AA and flavonoids content, whereas the most promising kabuli genotypes were Surutato 77, Bco. Sin. 92, and Blanoro that showed the highest values of phenolic acids. These genotypes represent good sources of antioxidants for the improvement of nutraceutical properties in chickpea.  相似文献   

10.
Background:To study the anticancer activity of Plantago major, we assessed the effect of ethanolic, methanolic and acetonic extracts of this plant on HCT-116, SW-480, and HEK-293 cell lines as control. Methods:The cytotoxic activity, biocompatibility, and toxicity were evaluated by MTT assay, hemolysis, and Artemia salina-LD50 (on mice) tests, respectively. The analysis of the extracts was performed by GC-MS analysis. Results:The results showed that all the extracts had the most antiproliferative properties on the HCT-116 cell line. The P. major root extract was more effective than the aerial parts, and IC50 values for ethanolic, methanolic and acetonic root extracts were 405.59, 470.16, and 82.26 µg/mL, respectively on HCT-116 cell line at 72 h. Hemolysis degree of the ethanolic extract of aerial and root parts were approximately 1% at 400 μg/mL.. Using the ethanolic extracts, the Artemia survived every concentration, and no toxicity was observed. One week after the oral administration of different parts of P. major extracts, none of the mice died, even those were administered 2000 mg/kg. The results of GC/MS analysis showed that P. major extracts contain potential anticancer compounds, such as stearic acid (8.61%) in aerial parts of methanolic extract and 1,2- Benzenedicarboxylic acid, mono(2-ethylhexyl)ester (88.07% and 40.63%) in aerial and root parts of acetonic extract of P. major. Conclusions:Our findings suggest that the P. major is a source of potential compounds with antiproliferative properties. Key Words: Gas chromatography-mass spectrometry, HCT-116 cells, Hemolysis, Lethal dose 50  相似文献   

11.
Pinnatoxin G (PnTX-G) is a marine toxin belonging to the class of cyclic imines and produced by the dinoflagellate Vulcanodinium rugosum. In spite of its strong toxicity to mice, leading to the classification of pinnatoxins into the class of “fast-acting toxins”, its hazard for human health has never been demonstrated. In this study, crude extracts of V. rugosum exhibited significant cytotoxicity against Neuro2A and KB cells. IC50 values of 0.38 µg mL−1 and 0.19 µg mL−1 were estimated on Neuro2A cells after only 24 h of incubation and on KB cells after 72 h of incubation, respectively. In the case of Caco-2 cells 48 h after exposure, the crude extract of V. rugosum induced cell cycle arrest accompanied by a dramatic increase in double strand DNA breaks, although only 40% cytotoxicity was observed at the highest concentration tested (5 µg mL−1). However, PnTX-G was not a potent cytotoxic compound as no reduction of the cell viability was observed on the different cell lines. Moreover, no effects on the cell cycle or DNA damage were observed following treatment of undifferentiated Caco-2 cells with PnTX-G. The crude extract of V. rugosum was thus partially purified using liquid-liquid partitioning and SPE clean-up. In vitro assays revealed strong activity of some fractions containing no PnTX-G. The crude extract and the most potent fraction were evaluated using full scan and tandem high resolution mass spectrometry. The dereplication revealed the presence of a major compound that could be putatively annotated as nakijiquinone A, N-carboxy-methyl-smenospongine or stachybotrin A, using the MarinLit™ database. Further investigations will be necessary to confirm the identity of the compounds responsible for the cytotoxicity and genotoxicity of the extracts of V. rugosum.  相似文献   

12.
The bioactivity of compounds produced by Pseudomonas aeruginosa (LN strain), against three Xanthomonas species was investigated under greenhouse conditions and using electron microscopy. Chromatographic fractions EAP, VLC3, VLC4, VLC3d and VLC4f were tested against Xanthomonas axonopodis pv. malvacearum, X. axonopodis pv. phaseoli and X. axonopodis pv. citri by disc diffusion. Fractions with antibiotic activity were tested in vivo under greenhouse conditions and their bioactivity was evaluated. Scanning electron microscopy showed that VLC4f affects biofilm formation while VLC4f and VLC3d both affect cell morphology. The semi-purified fractions controlled bacterial diseases caused by Xanthomonas spp. when sprayed on plants under greenhouse conditions. The VLC4f fraction showed superior results in disease management, reducing the number of lesions on cotton and orange leaves by 94%, and reducing disease severity in bean leaves by 73%. The data suggest that the fractions were effective and have potential as an alternative to conventional bactericides in the control of plant diseases caused by Xanthomonas sp under greenhouse conditions.  相似文献   

13.
The previously known high toxicity and hemagglutinin concentration found in Escumite bean (Phaseolous acutifolius), widely consumed in the south-east of Mexico, induced us to study the cytotoxic effect of these beans on the epithelial cells of the small intestine of rats. Another, less toxic leguminosae, chick-pea (Cicer arietinum), was used for comparison. In vitro tests showed that the viability of the cells was much more affected by the Escumite bean extract than by the chick-pea extract (P<0.001). The cellularity was much diminished when the epithelial cells were treated with Escumite extract (P<0.001), but not with chick-pea extract. In vivo experiments confirmed these findings. The present results suggest that the deleterious effect of some toxicants present in the raw legume is due to an interaction with intestinal epithelium, which, in turn, may cause a reduced absorption of nutrients.  相似文献   

14.
Insecticidal effect of Ungernia severtzovii bulbs extract has been investigated against the grain aphid Schizaphis graminum. LC50 value of the ethanolic extract of U. severtzovii against the female aphids was 0.235% (2.35 g/l). There was 100% mortality of the subsequent nymphs of the treated females at 0.25-1.0%. The extract was equally active against the nymphs at the highest concentrations. Hexane and ethanolic extracts were the most active against the aphids of all the extracts. Fractionation of the hexane extract by TLC yielded three fractions. Fraction II was the most active (>90% mortality) against the aphids. Xanthoxylin was identified as the major constituent in fraction II of the hexane extract and may be responsible for the insecticidal effect of U. severtzovii.  相似文献   

15.
The seeds of five different species ofAcacia, twoAlbizzia, twoErythrina and two species ofMucuna were analysed for their protein and amino acid composition. Some of these seeds are comparable to a popular food legume,Cicer arietinum, in protein and amino acid composition.  相似文献   

16.
This is a report of extraction and identification of 1-O-alkyl glycerol present in the dried leaves of Bauhinia scandens. Fifty percent aqueous ethanolic extract of the plant at room temperature was fractionated over petroleum ether and diethyl ether. The diethyl ether soluble fraction showed positive bioactivity in Brine Shrimp bioassay. Isolation and purification of the active principle was subsequently done from diethyl ether fraction. The diethyl ether fraction was separated into acidic and neutral part. The acid free fraction was screened to be positive in Brine Shrimp bioassay. The NMR spectra (in CDCl3) indicated the probability of its lipoidal nature. The total lipid fraction was resolved into neutral, glyco, and phospho-lipids by column chromatography. Only the neutral fraction showed positive response to Brine Shrimp toxicity test, out of which again a Brine Shrimp positive fraction was separated by thin layer chromatography and identified as 1-O-alkyl glycerol. This fraction was acetylated and GLC analysis of the 1-O-alkyl-2,3-diacetyl glycerol was done. Our results demonstrate that the work may be cited as a nonhazardous and nonchemical management of therapeutic importance.  相似文献   

17.
A comparative study concerning the physicochemical, monomeric composition and biological characters among different fucoidan fractions is presented. Common purification techniques for fucoidan usually involve many steps. During these steps, the important structural features might be affected and consequently alter its biological activities. Three purified fractions were derived from Fucus vesiculosus water extract which, afterwards, were purified by a recently-developed dye affinity chromatography protocol. This protocol is based on dye-sulfated polysaccharide interactions. The first two fractions were obtained from crude precipitated fucoidan at different pH values of the adsorption phase: pH 1 and 6. This procedure resulted in fucoidan_1 and 6 fractions. The other, third, fraction: fucoidan_M, however, was obtained from a buffered crude extract at pH 1, eliminating the ethanol precipitation step. All of the three fractions were then further evaluated. Results revealed that fucoidan_M showed the highest sulfur content (S%), 12.11%, with the lowest average molecular weight, 48 kDa. Fucose, galactose, and uronic acid/glucose dimers were detected in all fractions, although, xylose was only detected in fucoidan_1 and 6. In a concentration of 10 µg·mL−1, Fucoidan_6 showed the highest heparin-like anticoagulant activity and could prolong the APTT and TT significantly to 66.03 ± 2.93 and 75.36 ± 1.37 s, respectively. In addition, fucoidan_M demonstrated the highest potency against HSV-1 with an IC50 of 2.41 µg·mL−1. The technique proved to be a candidate for fucoidan purifaction from its crude extract removing the precipitation step from common purification protocols and produced different fucoidan qualities resulted from the different incubation conditions with the immobilized thiazine toluidine blue O dye.  相似文献   

18.
The effect of thermal processing on the degradation of the phytochemicals in black rice flour by means of fluorescence spectroscopy and degradation kinetics was investigated. In order to investigate the influence of food matrices, a comparative analysis between integral rice flour and different fractions was performed. The preliminary compositional results suggested a higher content in phytochemicals in fraction four of the seven fractions of black rice flour, which was sifting through a sieve with a diameter of 180 μm. The compositional complexity was highlighted by fluorescence spectroscopy. The heat-treatment caused structural changes that led to red- or blue-shifts in maximum emission. The first-order kinetic model was used to describe the mechanism of degradation. The activation energies were 10.07 ± 1.04 kJ/mol for total polyphenolic, 7.26 ± 0.58 kJ/mol for total monomeric anthocyanins and 6.71 ± 1.12 kJ/mol for antioxidant activity in case of integral flour extract. For fraction four extract obtained by, the Ea values were: 3.51 ± 0.53 kJ/mol, 11.49 ± 1.47 kJ/mol, 15.80 ± 1.50 kJ/mol and 19.91 ± 3.27 kJ/mol, respectively. The calculated values of the activation energy revealed higher temperature dependence of total polyphenols in integral flour and of antioxidant activity in fraction four, respectively.  相似文献   

19.
The effect of 7 days of germination on levels of nitrogenous and other nutrition related parameters, protein fractions and in vitro protein digestibility of fluted pumpkin (Telfairia occidentalis) seed was studied. The non-protein nitrogen gradually increased and the protein nitrogen content decreased during germination. Albumin and globulin fractions were found to be the major seed proteins of fluted pumpkin seeds, constituting about 58.6% of the total protein of the ungerminated (raw) seeds. The protein fractions, albumin and glutelin, were observed to increase by 61.5% and 57.0%, respectively, while a 54.6% decrease was noted in the prolamine fraction. The globulin fraction increased at the beginning of germination but decreased at the end. Germination significantly (p 0.05) increased the crude protein, nitrogen solubility and in vitro protein digestibility but decreased the fat, phytic acid and polyphenol contents of the seeds.  相似文献   

20.
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