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The present investigation deals with the evaluation of the wound healing efficacy of sandalwood bark-derived carbon nanospheres loaded with curcumin-embedded polyvinyl alcohol (PVA) nanofiber membranes (NF). Carbon nanospheres (CNS) were prepared by pyrolyzing sandal wood bark powder at 750 °C. The morphology was confirmed by field emission scanning electron micrographs and a rich amount of carbon was confirmed by the energy dispersive X-ray technique. Curcumin, an active wound healing drug was loaded onto synthesized CNS and confirmed by ATR-IR studies. Drug-loaded CNS were anchored in a PVA matrix via electrospun nanofiber fabrication. The fabricated nanofiber membranes were characterized and evaluated for wound healing efficiency. The cytotoxicity assay proved the non-toxic nature of the prepared PVA/CNS-curcumin-loaded NF. Membranes with active CNS/drug showed better antimicrobial activity against S. aureus and E. coli, which was estimated using the zone of inhibition (ZOI) test. The in vitro scratch wound healing assay of prepared PVA/CNS-curcumin nanofibers was efficient enough and showed 92 to 98% wound closure, which was greater than the control (without drug) nanofiber membranes. The PVA nanofiber matrix with interconnected structure and carbon nanostructures together enhanced the wound healing efficacy of the considered wound healing membrane, which is a promising novel approach for future wound healing patches.
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The present study was undertaken to explore the effect of Chromium-D-phenylalanine (Cr (D-phe)3) on the reproduction and development of Drosophila melanogaster. Cr (D-phe)3 was synthesized and characterized by infrared spectral analysis, melting point (DSC), and UV spectral analysis. D. melanogaster was raised in corn flour agar medium containing 0, 5, 10, 15, and 20 µg/mL of Cr (D-phe)3. The effect of Cr (D-phe)3 was evaluated by observing the larval period, pupal period, percentage of egg hatching, morphometric analysis of eggs, larvae, pupae and adults, fertility, fecundity, lifespan of the emerged flies, and levels of antioxidant enzymes such as catalase, glutathione-S-transferase (GST), and superoxide dismutase (SOD) in the supernatant of flies homogenate suspension. The study results indicate that Cr (D-phe)3 showed beneficial effects on reproduction and development in D. melanogaster. Cr (D-phe)3 significantly improved the larval period, pupal period, percentage of egg hatching, morphometric characters of the larva, pupa, and adult, fertility, fecundity, and lifespan of D. melanogaster. Moreover, Cr (D-phe)3 also significantly elevated the levels of catalase (p < 0.01), GST (p < 0.05), and SOD (p < 0.01) in D. melanogaster, and results were statistically significant at the dose of 15 µg/mL. The study results indicate that Cr (D-phe)3 has a positive effect on the reproduction and development of D. melanogaster. The literature review revealed that there is a strong relationship between the physiology of metabolism, oxidative stress and reproduction and development. Several studies propose that Cr(III) influences insulin sensitivity and thereby the metabolism of carbohydrates, proteins, and fats. Cr (D-phe)3 also has antioxidant and anti-inflammatory properties. Hence, the observed beneficial effects of Cr (D-phe)3 on reproduction and development of D. melanogaster may be attributed to its physiological effect on carbohydrate, protein, and lipid metabolism and its antioxidant and anti-inflammatory properties.
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In the title hydrated complex, [Co(C15H10ClN3)2]Cl2·4H2O, the complete dication is generated by symmetry. The CoN6 moiety shows distortion from regular octa-hedral geometry with the trans bond angles of two N-Co-N units being 160.62â (9)°. In the crystal, O-Hâ¯Cl and C-Hâ¯O inter-actions link the components into (001) sheets. The title compound exhibits blue-light emission, as indicated by photoluminescence data, and a HOMO-LUMO energy separation of 2.23â eV was obtained from its diffuse reflectance spectrum.
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Nanotechnology is opening up new opportunities in drug delivery, including oral delivery, and it may reduce toxicity and increase drug ability. Presently, researchers are expanding their knowledge in the development of oral nanomedicine to extend the scope of oral drug delivery and exhibit excellent platforms for drug transportation, target, and controlled release. The present review is an attempt to define updated oral nanostructured systems for the delivery of a wide range of drugs. The review also focuses on the use of different polymeric and other materials, technologies adopted, and benefits/drawbacks of delivery systems.
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Preparações de Ação Retardada/administração & dosagem , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Nanopartículas/química , Nanotecnologia/métodos , Administração Oral , Química Farmacêutica , Preparações de Ação Retardada/farmacocinética , Liberação Controlada de Fármacos , Emulsões/química , Absorção Gastrointestinal , Humanos , Polímeros/química , Distribuição TecidualRESUMO
BACKGROUND: Embelia ribes is claimed in Indian traditional medical practice to be useful in the treatment of nervous diseases. Embelin, an alkyl substituted hydroxy benzoquinone, is a major active constituent of E. ribes. The present preliminary study was intended to evaluate antipsychotic activity of embelin against apomorphine-induced climbing behaviour in mice and stereotyped behaviour in rats. METHODS: Two doses of embelin (5 and 10mg/kg) were administered once daily for 15days before exposure to apomorphine. On the concluding day of pre-treatment, after apomorphine-injection, the rodents were assessed for climbing and stereotyped behaviours according to the published scoring system. Thereafter, neurotransmitters (dopamine, noradrenaline and serotonin) levels were estimated in rodent brains. RESULTS: Embelin pre-treatment significantly inhibited apomorphine-induced climbing and stereotyped behaviours in mice and rats, respectively. Further, embelin also statistically reversed elevated levels of dopamine, noradrenaline and serotonin neurotransmitters in the brain of mice and rats. Embelin showed more significant results at high dose (10mg/kg) than low dose (5mg/kg) in both the tested models. CONCLUSION: Considering the present pharmacological profile of embelin, it is suggested that embelin possesses antipsychotic activity in the treatment of psychotic disorders. However, further research is warranted for evaluating its exact mechanism of action.
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Antipsicóticos/farmacologia , Benzoquinonas/farmacologia , Embelia/química , Transtornos Psicóticos/tratamento farmacológico , Animais , Apomorfina/farmacologia , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Camundongos , Neurotransmissores/metabolismo , Extratos Vegetais/farmacologia , Transtornos Psicóticos/metabolismo , Ratos , Ratos WistarRESUMO
Present study was designed to evaluate the effect of chromium-d-phenylalanine complex (Cr (d-phe)3) on indomethacin-induced inflammatory bowel disease (IBD) in rats. Adult Wistar rats were pretreated with vehicle/Cr (d-phe)3 (30, 60 and 90µg/kg, p.o.) for 11days. On day 8 and 9, after one h of the above mentioned treatment, indomethacin (7.5mg/kg/day,s.c.) was administered to induce IBD. On day 12, blood samples were collected from animals for lactate dehydrogenase (LDH) estimation and ileum was isolated for macroscopic scoring, biochemical estimation (lipid peroxidation, reduced glutathione and myeloperoxidase activity) and histopathological study. Administration of indomethacin significantly altered the serum LDH, macroscopic and microscopic appearance and biochemical parameters in ileum tissue. Cr (d-phe)3, at all the tested doses, caused a significant reversal of changes induced by indomethacin. Present study demonstrates the protective effect of Cr (d-phe)3 against indomethacin-induced IBD in rats. The observed protective effect might be attributed to the antioxidant and anti-inflammatory properties of Cr (d-phe)3.
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Anti-Inflamatórios não Esteroides/toxicidade , Compostos de Cromo/farmacologia , Indometacina/toxicidade , Doenças Inflamatórias Intestinais/induzido quimicamente , Fenilalanina/farmacologia , Animais , Compostos de Cromo/química , Glutationa , Peroxidação de Lipídeos , Peroxidase/metabolismo , Fenilalanina/química , Ratos , Ratos Wistar , Sulfassalazina/farmacologiaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Traditionally Cassia glauca (CG) has been used to treat diabetes. AIM OF THE STUDY: The study was undertaken to evaluate anti-diabetic and antioxidant activity of polyphenolic enriched extract of CG in standardized streptozotocin (STZ)-induced diabetic rats. MATERIALS AND METHODS: The effect of ethanol (CGE) and water (CGW) extracts of CG (200 and 400mg/kg) treatment were evaluated in STZ (50mg/kg, iv) induced diabetic rats. On 10th day, oral glucose tolerance test and degree of insulin resistance was calculated. On 13th day, insulin tolerance test was performed to know the peripheral utilization of glucose. On 15th day, blood glucose, lipid profiles and endogenous antioxidant levels were estimated. In addition, the effects on oral glucose/sucrose tolerance test in normal rats. Further, HPLC fingerprinting profile of CGE and simultaneous quantification of biomarkers were carried out. RESULTS: Supplementation with CGE and CGW significantly reduced STZ-induced deleterious effects and improved glucose tolerance, and insulin tolerance. In addition, supplementation also decreased oxidative stress by improving endogenous antioxidant levels. Furthermore, administration significantly improves sucrose tolerance suggesting that extract possess inhibition of α-glucosidase enzyme. Further, HPLC studies revealed that CGE contains three bioactive polyphenolic compounds viz., rutin (0.10±0.01mg/g), luteolin-7-glucoside (0.06±0.01mg/g) and isorhoifolin (0.7±0.05mg/g). CONCLUSION: Observed beneficial outcome of CG might be attributed to the presence of polyphenolic compounds and mediated by interacting with multiple targets of diabetes and oxidative stress. Taken together, this study provided the scientific evidence for the traditional use of CG.
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Cassia/química , Diabetes Mellitus Tipo 1/tratamento farmacológico , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Animais , Antioxidantes/metabolismo , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/patologia , Diabetes Mellitus Tipo 1/patologia , Relação Dose-Resposta a Droga , Teste de Tolerância a Glucose , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Resistência à Insulina , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Polifenóis/administração & dosagem , Polifenóis/isolamento & purificação , Ratos , Ratos Wistar , EstreptozocinaRESUMO
Sickness behaviour is a coordinated set of adaptive behavioural changes that develop in ill individuals during the course of an infection. It is relevant to understanding depression and some aspects of the suffering that in cancer. Embelin has been reported to possess antiinflammatory, neuroprotective and anxiolytic assets and has been shown to inhibit nuclear factor κB pathway and cytokine production. The present study was undertaken to investigate the effect of embelin isolated from Embelia ribes Burm in lipopolysaccharide (LPS)-induced sickness behaviour in mice. Adult male Swiss albino mice were pre-treated with embelin (10 and 20 mg/kg, p.o.) or dexamethasone (1 mg/kg, i.p.) for 3 days and then challenged with LPS (400 µg/kg, i.p.). At different time intervals of post-LPS challenge, sickness behaviour was evaluated in the animals by battery of behavioural tests (plus maze, open field, light-dark box, forced swim, social behaviour assessment, sucrose preference and food and water intake). Levels of oxidative stress makers (reduced glutathione and lipid peroxidation) in mice brain were also analysed. LPS induced behavioural alterations, anhedonia and anorexia, in mice. Pre-treatment with embelin attenuated behavioural changes induced by LPS. In addition, embelin prevented anhedonia, anorexia and ameliorated brain oxidative stress markers. The experimental outcomes of the present study demonstrated protective effect of embelin in LPS-induced sickness behaviour in mice. Copyright © 2016 John Wiley & Sons, Ltd.
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Benzoquinonas/química , Medicina Herbária/métodos , Comportamento de Doença/efeitos dos fármacos , Lipopolissacarídeos/efeitos adversos , Animais , Lipopolissacarídeos/farmacologia , Masculino , Camundongos , Estresse OxidativoRESUMO
3-Nitropropionic acid (3-NP) causes severe neurotoxicity in animals, which depicts Huntington's disease (HD) in humans. Embelin, the main active constituent of Embelia ribes, has been reported to possess various pharmacological actions, mainly anti-inflammatory, antioxidant, anticonvulsant and neuroprotective. The aim of the present study was to evaluate the neuroprotective effect of embelin against 3-NP induced experimental HD in rats. Adult Wistar rats were pretreated with vehicle/embelin (10 and 20mg/kg p.o.) for 7 days. From 8th day onwards, embelin was co-treated with 3-NP (15mg/kg, i.p.) for 7 days. At the end of the treatment schedule, animals were evaluated for behavioral alterations and brain homogenates were used for estimation of oxidative stress parameters (lipid peroxidation, reduced glutathione, catalase and glutathione-S-transferase). 2,3,5-Triphenyl tetrazolium chloride (TTC) stained brain slices were used for lesion size measurement. Administration of 3-NP significantly altered the behavioral and neuronal antioxidant status and caused significant neuronal damage in striatal region. Embelin, at both the tested doses, caused a significant reversal of behavioral and antioxidant status alterations and reversed the striatal neuronal damage induced by 3-NP. These findings suggest the neuroprotective effect of embelin against HD. The observed protective effect might be attributed to the antioxidant properties of embelin.
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Benzoquinonas/farmacologia , Doença de Huntington/prevenção & controle , Fármacos Neuroprotetores/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Animais , Comportamento Animal , Benzoquinonas/administração & dosagem , Peso Corporal , Encéfalo/patologia , Catalase/metabolismo , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Glutationa/metabolismo , Glutationa Transferase/metabolismo , Doença de Huntington/induzido quimicamente , Peroxidação de Lipídeos/fisiologia , Locomoção , Fármacos Neuroprotetores/administração & dosagem , Nitrocompostos/toxicidade , Propionatos/toxicidade , Ratos , Ratos WistarRESUMO
OBJECTIVE: To assess the anthelmintic acivity of Bacillus cereus and Bacillus pumilus metabolites. MATERIALS AND METHODS: The successive solvent extractions with petroleum ether, ethyl acetate and methanol. The solvent extracts were tested for anthelmintic activity against Pheretima posthuma at 20 mg/ml concentration. The time of paralysis and time of death of the worms was determined for all the extracts. Albendazole was taken as a standard reference and sterile water as a control. RESULTS: All the sample extracts showed significant anthelmintic activity in paralyzing the worms comparable with that of the standard drug. The time of death exhibited by BP metabolites was close to the time exhibited by standard. CONCLUSION: The study indicates both bacteria Bacillus cereus and Bacillus pumilus have anthelmintic activity indicating potential metabolites in them.
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BACKGROUND: Silajatu (Shilajit; SJ) is claimed in traditional Indian medical practice to be useful in the treatment of nervous disorders, epilepsy and as antistress. AIM: To investigate whether SJ possesses antiepileptic and antipsychotic activities in rodents. MATERIALS AND METHODS: Isonicotinyl hydrazine (INH), pentylenetetrazole (PTZ), apomorphine, phenytoin, diazepam, haloperidol and other chemicals of analytical grade were procured from standard companies. The antiepileptic activity of SJ was assessed using maximal electro shock (MES)-induced seizures in rats, INH and PTZ-induced seizures in mice. The antipsychotic effect of SJ was evaluated using apomorphine-induced climbing and stereotyped behaviours respectively, in mice and rats. SETTINGS AND DESIGNS: SJ (25 and 50 mg/kg, p.o.) was given orally once daily for 15 days in all the rodent models. On the test day, SJ was administered 1 h prior to electric shock or chemical inducers (INH/PTZ/apomorphine) in experimental animals; the animals were then observed for different phases of seizures and psychotic behaviours. In addition, gamma-aminobutyric acid (GABA) content in the brain of rats and mice was estimated in seizure models. STATISTICAL ANALYSIS: The data were expressed as mean ± standard error of mean. Statistical comparisons were performed by one-way ANOVA followed by Tukey's post-test using Graph Pad Prism version 5.0, USA. A P < 0.05 was considered significant. RESULTS AND CONCLUSIONS: SJ pretreatment significantly inhibited the seizures induced by MES, INH and PTZ in a dose dependent manner. Further, SJ augmented brain GABA levels to normal, decreased by INH and PTZ in mice brain. SJ pretreatment also significantly inhibited the climbing and stereotyped behaviours induced by apomorphine. The present data seems to confirm the antiepileptic activity of SJ which may be because of enhancing the GABAergic system. The antipsychotic activity observed may be due to anti-dopaminergic and/or GABA-mimetic actions.
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Alterations in antiretroviral pharmacokinetics during pregnancy must be understood for the drugs to be used safely and effectively. Present study is an attempt to understand the potential changes in raltegravir plasma and cerebrospinal fluid pharmacokinetics during pregnancy in late pregnant and non-pregnant rats. In vitro plasma protein binding, metabolic stability, intravenous blood-brain barrier (BBB) permeability and oral pharmacokinetic studies were performed. Raltegravir concentrations in different matrices were measured using LC-MS/MS. Raltegravir plasma protein binding remained similar in both groups, whereas, metabolic stability was significantly lower in pregnant rats than the non-pregnant rats liver microsomes. In oral pharmacokinetic study, peak plasma concentrations and systemic exposures were significantly lower (â¼37%) and clearance was significantly higher (â¼61%) in late pregnant rats compared to non-pregnant rats. However, unlike plasma pharmacokinetics, CSF pharmacokinetic profile of raltegravir was similar in both pregnant and non-pregnant rats. Following intravenous administration, raltegravir showed higher BBB permeability in pregnant rats compared to non-pregnant rats. But the mean CSF-to-plasma ratio was significantly higher in pregnant rats compared to non-pregnant rats suggesting higher brain penetration in pregnant rats. In conclusion, pregnancy significantly affected the plasma pharmacokinetics, whereas cerebrospinal fluid pharmacokinetics remained fairly similar in pregnant and non-pregnant rats. Although current plasma pharmacokinetic data is in contradiction to the reported human data, pregnancy-specific pharmacokinetic changes observed in the current study emphasize the need for close therapeutic monitoring while treating the pregnant population and also warrants the need for additional clinical data with larger group of patients.
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Líquido Cefalorraquidiano/metabolismo , Plasma/metabolismo , Pirrolidinonas/farmacocinética , Animais , Barreira Hematoencefálica/metabolismo , Feminino , Gravidez , Raltegravir Potássico , Ratos , Ratos Sprague-DawleyRESUMO
Trichoderma harzianum was isolated from local dumpsites of Shivamogga District for use in the biodegradation of polyethylene. Soil sample of that dumpsite was used for isolation of T. harzianum. Degradation was carried out using autoclaved, UV-treated, and surface-sterilized polyethylene. Degradation was monitored by observing weight loss and changes in physical structure by scanning electron microscopy, Fourier transform infrared spectroscopy, and nuclear magnetic resonance spectroscopy. T. harzianum was able to degrade treated polyethylene (40%) more efficiently than autoclaved (23%) and surface-sterilized polyethylene (13%). Enzymes responsible for polyethylene degradation were screened from T. harzianum and were identified as laccase and manganese peroxidase. These enzymes were produced in large amount, and their activity was calculated using spectrophotometric method and crude extraction of enzymes was carried out. Molecular weight of laccase was determined as 88 kDa and that of manganese peroxidase was 55 kDa. The capacity of crude enzymes to degrade polyethylene was also determined. By observing these results, we can conclude that this organism may act as solution for the problem caused by polyethylene in nature.
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Polietileno/metabolismo , Poluentes do Solo/metabolismo , Trichoderma/fisiologia , Biodegradação Ambiental , Monitoramento Ambiental , Lacase/química , Espectroscopia de Ressonância Magnética , Microscopia Eletrônica de Varredura , Solo/química , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
A novel series of 2,5,6-trisubstituted imidazo[2,1-b][1,3,4]thiadiazoles 4(a-d) and 7(a-i) were rationally designed through QSAR based pharmacophore approach and synthesized from 5-(1,3-benzodioxol-5-yl)-[1,3,4]thiadiazol-2-amine (1). The structures of these compounds were established by IR, (1)H NMR, (13)C NMR, HRMS technique. All the compounds were evaluated for their in vitro antihyperlipidemic activity using trition induced hyperlipidemic model. The newly synthesized title compound 7d, 7e and 7h showed a significant decrease in the serum, TCH, TG LDL and VLDL values along with an increase in serum HDL levels as compared to standard drug Fenofibrate. The treated groups also showed significant decrease in the atherogenic index, LDL:HDL risk ratios and the level of SGOT, SGPT and ALP activities compared to cholesterol induced hyperlipidemic control group.
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Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/uso terapêutico , Imidazóis/uso terapêutico , Tiadiazóis/uso terapêutico , Animais , Desenho de Fármacos , Hepatócitos/efeitos dos fármacos , Hipolipemiantes/síntese química , Hipolipemiantes/química , Imidazóis/síntese química , Imidazóis/química , Masculino , Modelos Moleculares , Estrutura Molecular , Relação Quantitativa Estrutura-Atividade , Ratos , Ratos Wistar , Relação Estrutura-Atividade , Tiadiazóis/síntese química , Tiadiazóis/químicaRESUMO
Monosodium glutamate (MSG) is a popular flavour enhancer used in food industries; however, excess MSG is neurotoxic. Oxidative stress is well documented in MSG induced neurotoxicity. The compounds having antioxidant and anti-inflammatory properties reportedly possess beneficial effects against various neurotoxic insults. Calendula officinalis Linn. flower extract (COE) is known for its potent antioxidant and anti-inflammatory activities. Hence, this present study has been designed to evaluate the neuroprotective effect of COE on MSG-induced neurotoxicity in rats. Adult Wistar rats were administered systemically for 7 days with MSG and after one h of MSG injection, rats were treated with COE (100 and 200 mg/kg) orally. At the end the treatment period, animals were assessed for locomotor activity and were sacrificed; brains were isolated for estimation of LPO, GSH, CAT, TT, GST, Nitrite and histopathological studies. MSG caused a significant alteration in animal behavior, oxidative defense (raised levels of LPO, nitrite concentration, depletion of antioxidant levels) and hippocampal neuronal histology. Treatment with COE significantly attenuated behavioral alterations, oxidative stress, and hippocampal damage in MSG-treated animals. Hence, this study demonstrates that COE protects against MSG-induced neurotoxicity in rats. The antioxidant and anti-inflammatory properties of COE may be responsible for its observed neuroprotective action.
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ETHNOPHARMACOLOGICAL RELEVANCE: Chromolaena odorata Linn., is used in traditional Indian medicine in the treatment of diabetes and eye problems. AIM OF THE STUDY: The present study was designed to investigate the effect of the ethanol extract Chromolaena odorata leaves (ACO) in streptozotocin (STZ; 45 mg/kg, i.v) induced diabetes and cataract in rats. MATERIALS AND METHODS: Different doses of ACO (200 and 400mg/kg) was administered once daily for eight weeks to STZ-induced diabetic rats. To know the mechanism of action of title plant, AUC(glucose), AUC(insulin), Homeostatic Model Assessment (HOMA), insulin tolerance test (ITT) and glucose uptake by rat hemi-diaphragms were carried out. Further, cataract score was taken once in a week upto eight weeks and opacity index was measured. HPLC fingerprinting profiling of ACO was also carried out. RESULTS: Administration of ACO exhibited significant reduction in glucose, HOMA, lipid profiles and significantly improved glucose and insulin tolerance, glycogen content, glucose uptake by skeletal muscle, serum insulin and HDL-c levels. In addition, ACO also decreased oxidative stress by improving endogenous antioxidants. Further, treatment of ACO showed significantly reduced onset and extent of cataract. CONCLUSION: The present data suggested that the treatment of ACO reversed the STZ-induced diabetes and cataract in rats. The observed beneficial effects may be mediated by interacting with multiple targets operating in diabetes mellitus and its complication. Taken together, this study provided the scientific evidence for the traditional use of Chromolaena odorata.
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Catarata/tratamento farmacológico , Chromolaena/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Antioxidantes/metabolismo , Diafragma/efeitos dos fármacos , Diafragma/metabolismo , Etanol/química , Feminino , Glucose/metabolismo , Teste de Tolerância a Glucose/métodos , Glicogênio/metabolismo , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Insulina/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Extratos Vegetais/química , Folhas de Planta/química , Ratos , Ratos WistarRESUMO
AIM AND OBJECTIVES: To evaluate anxiolytic effect of stem bark ethanol and chloroform extracts of Erythrina mysorensis in mice. MATERIALS AND METHODS: The anxiolytic activity was examined by using the elevated plus maze (EPM) and open field test (OFT), and motor coordination by rotarod test (RRT). Twenty four Swiss albino male mice were divided into four groups of six mice each. Group 1 received vehicle (normal saline); group 2 received diazepam (1 mg/kg); groups 3 and 4 received ethanolic and chloroform extract of Erythrina mysorensis, 200 and 400 mg/kg p.o., respectively. RESULTS: Mice treated with diazepam (1 mg/kg, p.o.) showed significant (P < 0.001) increase ini the percentage of open arms entries and time spent whereas, in closed arm the number of entries and time spent were significantly (P < 0.05) decreased. Oral administration of chloroform and ethanol extract of E. mysorensis exhibited significant (P < 0.05) increase in the number of open arm entries and time spent with significant (P < 0.05) reduction in number of entries and time spent in the closed arm as compared to group 1. Chloroform and ethanol extracts treated mice also produced significant increase in the number of rearings (P < 0.05), assisted rearings and number of squares crossed (P < 0.01). Rotarod test showed significant (P < 0.01) reduction in motor activity at 45 min with diazepam and E. mysorensis extracts (400 mg/kg) as compared to groups 3 and 1. CONCLUSION: Erythrina mysorensis possess significant anxiolytic activity in the mice. It can be a promising anxiolytic agent.
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Ansiolíticos/uso terapêutico , Ansiedade/tratamento farmacológico , Erythrina , Extratos Vegetais/uso terapêutico , Animais , Ansiolíticos/isolamento & purificação , Ansiolíticos/farmacologia , Ansiedade/psicologia , Avaliação Pré-Clínica de Medicamentos/métodos , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Aprendizagem em Labirinto/fisiologia , Camundongos , Casca de Planta , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Distribuição AleatóriaRESUMO
Two new series of quinoline incorporated benzimidazole derivatives (4a-i and 8a-f) were synthesized from substituted aniline and isatin through multi-step reaction. 6-substituted-4-carboxyquinolines (3a,b and 7) were synthesized by multi component one pot reactions (via Doebner reaction and Pfitzinger reaction respectively) and the targeted benzimidazole derivatives were obtained by the reaction of 6-substituted-4-carboxyquinolines (3a,b and 7) with substituted aromatic diamines in acidic media. All the newly synthesized compounds were characterized by IR, NMR mass spectral study and also by C, H, N analyses. The final compounds were screened for their in-vitro antibacterial and antifungal activity by well plate method (zone of inhibition). The results revealed that, compounds 4c, 4d, 8c and 8d showed significant antibacterial activity. The compound 8b was found to be potent antifungal agent. 4a, 8a and 8f showed moderate to good antimicrobial activity as compared to the standard drugs against all tested microbial strains.
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Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Fungos/efeitos dos fármacos , Quinolinas/química , Anti-Infecciosos/química , Benzimidazóis/química , Técnicas de Química SintéticaRESUMO
CONTEXT: Leptadenia reticulata Linn. (Asclpiadaceae) commonly known as "dodi," is an Indian medicinal plant which is known to have ethno-medical uses such as stimulant, tonic, immunostimulant and is one of the ingredient in ayurvedic formulation called as "Chawanprash," which is widely used in India to increase the strength of immune system. OBJECTIVE: The aim of present study is to evaluate immunomodulatory and antioxidant activity of ethanolic extract of L. reticulata L. leaves in rodents. METHODS: Haemagglutinating antibody (HA) titre, haematological profile (Hb, WBC, RBC), lipid peroxidation (LPO), reduced glutathione (GSH), superoxide dismutase (SOD), catalase (CAT), delayed type of hypersensitivity (DTH) response, neutrophil adhesion test and carbon clearance assay were determined by in vivo experiments. RESULTS: The evaluation of immunomodulatory potential of L. reticulata (100, 200 mg/kg, p.o.) evoked a significant dose-dependent increase in antibody titre values; DTH reaction induced by SRBC and potentiated percentage neutrophil adhesion to nylon fibers as well as phagocytosis in carbon clearance assay. Also it caused significant increase in haematological profile, GSH, SOD, CAT activity and significantly decreased LPO levels in cyclophosphamide-induced immunosuppressed rats. CONCLUSION: The results obtained in this study indicate that L. reticulata possesses potential immunomodulatory and antioxidant activity and can play a major role in reducing the risk to develop immunodeficiency disorders.