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Fourteen flavones (1-14) including twelve polymethoxylated flavones, two A-type proanthocyanidins (oligomeric flavonoids) (15, 16), one benzoyl glucoside (17), one triterpenoid (18), and one phenylpropanoid (19) were isolated from the leaves of the South Asian medicinal plant Ceriscoides campanulata (Roxb.) Tirveng (Rubiaceae). The structures of the compounds were identified based on their spectroscopic and spectrometric data and in comparison with literature data. Isolated compounds were tested in vitro against inflammatory enzymes (COX-2, iNOS), pro-inflammatory cytokines (IL-1ß, IL-6, TNF-α), esophageal squamous carcinoma cell line (TE13), and carbohydrate digestion enzymes (α-amylase, α-glucosidase). Proanthocyanidins 15 and 16 significantly attenuated the LPS-induced inflammatory response of COX-2, iNOS, IL-1ß, IL-6, TNF-α in RAW 264.7 cells. Proanthocyanidins also satisfactorily inhibited the regrowth (64%), migration (51%), and formation of tumor-spheres (48%) in ESCC cell line TE13 at 50% toxic concentration. Compounds 15 and 16 showed the most potent effect against mammalian α-amylase (IC50 8.4 ± 0.3 µM and 3.5 ± 0.0 µM, respectively) compared to reference standard acarbose (IC50 5.9 ± 0.1 µM). As yeast α-glucosidase inhibitors, compounds 15 and 16 also displayed significant activities (IC50 6.2 ± 0.3 and 4.7 ± 0.1 µM, respectively), while compounds 1-6 displayed weaker α-glucosidase inhibitory activities, ranging from 49 to 142 µM, compared to acarbose (IC50 665 ± 42 µM). In an anticholinesterase assay, compounds 1, 2, 6 (IC50 51 ± 2, 53 ± 7, 64 ± 5 µM, respectively), and 4 (IC50 44 ± 1 µM) showed moderate inhibitory activities against acetylcholinesterase and butyrylcholinesterase, respectively. Furthermore, molecular docking and molecular dynamic simulation analyses of compounds 15 and 16 were performed against human pancreatic α-amylase and human lysosomal acid α-glucosidase to elucidate the interactions of these compounds in the respective enzymes' active sites.
Asunto(s)
Carcinoma de Células Escamosas , Diabetes Mellitus , Neoplasias Esofágicas , Proantocianidinas , Rubiaceae , Acetilcolinesterasa/metabolismo , Animales , Butirilcolinesterasa/análisis , Butirilcolinesterasa/metabolismo , Simulación por Computador , Células Epiteliales/metabolismo , Neoplasias Esofágicas/tratamiento farmacológico , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Humanos , Inflamación , Mamíferos/metabolismo , Simulación del Acoplamiento Molecular , Estructura Molecular , Hojas de la Planta/química , Proantocianidinas/análisis , Proantocianidinas/farmacología , alfa-Amilasas , alfa-Glucosidasas/metabolismoRESUMEN
Many Bangladeshi medicinal plants have been used to treat Alzheimer's disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Extracts were prepared using a gentle cold extraction method. In vitro cholinesterase inhibitory effects were measured by Ellman's method in 96-well microplates. Blumea lacera (Compositae) and Cyclea barbata (Menispermaceae) were found to have the highest acetylcholinesterase inhibitory (IC50, 150 ± 11 and 176 ± 14 µg/mL, respectively) and butyrylcholinesterase inhibitory effect (IC50, 297 ± 13 and 124 ± 2 µg/mL, respectively). Cyclea barbata demonstrated competitive inhibition, where Blumea lacera showed an uncompetitive inhibition mode for acetylcholinesterase. Smilax guianensis (Smilacaceae) and Byttneria pilosa (Malvaceae) were also found to show moderate AChE inhibition (IC50, 205 ± 31 and 221 ± 2 µg/mL, respectively), although no significant BChE inhibitory effect was observed for extracts from these plant species. Among others, Thunbergia grandiflora (Acanthaceae) and Mikania micrantha (Compositae) were found to display noticeable AChE (IC50, 252 ± 22 µg/mL) and BChE (IC50, 314 ± 15 µg/mL) inhibitory effects, respectively. Molecular docking experiment suggested that compounds 5-hydroxy-3,6,7,3',4'-pentamethoxyflavone (BL4) and kaempferol-3-O-α-L-rhamnopyranosyl-(1â¶6)-ß-D-glucopyranoside (BL5) from Blumea lacera bound stably to the binding groove of the AChE and BChE by hydrogen-bond interactions, respectively. Therefore, these compounds could be candidates for cholinesterase inhibitors. The present findings demonstrated that Blumea lacera and Cyclea barbata are interesting objects for further studies aiming at future therapeutics for Alzheimer's disease.
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The use of conventional drugs to treat metabolic disorders and the pathological consequences of diabetes further increases the complications because of the side effects, and is sometimes burdensome due to relatively higher costs and occasionally painful route of administration of these drugs. Therefore, shifting to herbal medicine may be more effective, economical, have fewer side effects and might have minimal toxicity. The present review amasses a list of ethnomedicinal plants of 143 species belonging to 61 families, from distinctive domestic survey literature, reported to have been used to treat diabetes by the ethnic and local people of Bangladesh. Leaves of the medicinal plants were found leading in terms of their use, followed by fruits, whole plants, roots, seeds, bark, stems, flowers, and rhizomes. This review provides starting information leading to the search for and use of indigenous botanical resources to discover bioactive compounds for novel hypoglycemic drug development.
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The majority of the population in Bangladesh uses traditional plant-based medicines to manage various ailments, including central nervous system (CNS) disorders. This review presents ethnobotanical information and relevant scientific studies on plants used in traditional healthcare for the management of various CNS disorders in Bangladesh. The information on the medicinal plants of Bangladesh effective against CNS disorders published in scientific journals, books, and reports was compiled from different electronic databases using specific key words. The present article provides comprehensive information on a total of 224 medicinal plant species belonging to 81 families used for the treatment of CNS disorders by the various peoples of Bangladesh. In total, we reviewed more than 290 relevant papers. In this study, leaves were found as the most often used plant organ, followed by roots, fruits, whole plants, barks, seeds, stems, rhizomes, and flowers. The Fabaceae family contributes the highest number of used species, followed by Rubiaceae, Lamiaceae, Cucurbitaceae, Vitaceae, Euphorbiaceae, Malvaceae, and Zingiberaceae. The most frequently used species (in decreasing order) are Asparagus racemosus, Centella asiatica, Stephania japonica, Aegle marmelos, Coccinia grandis, Tabernaemontana divaricata, Bacopa monnieri, Abroma augusta, and Scoparia dulcis. This review may serve as a starting point for a rational search for neuroactive natural products against CNS disorders within the Flora of Bangladesh.
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Anisomeles indica (L.) kuntze is widely used in folk medicine against various disorders including allergy, sores, inflammation, and fever. This research investigated the antinociceptive, anxiolytic and sedative effects of A. indica methanol extract. The antinociceptive activity was assessed with the acetic acid-induced writhing test and formalin-induced flicking test while sedative effects with open field and hole cross tests and anxiolytic effects with elevated plus maze (EPM) and thiopental-induced sleeping time tests were assayed. Computer aided (pass prediction, docking) analyses were undertaken to find out the best-fit phytoconstituent of total 14 isolated compounds of this plant for aforesaid effects. Acetic acid treated mice taking different concentrations of extract (50, 100, and 200 mg/kg, intraperitoneal) displayed reduced the writhing number. In the formalin-induced test, extract minimized the paw licking time of mice during the first phase and the second phase significantly. The open field and hole-cross tests were noticed with a dose-dependent reduction of locomotor activity. The EPM test demonstrated an increase of time spent percentage in open arms. Methanol extract potentiated the effect of thiopental-induced hypnosis in lesser extent comparing with Diazepam. The results may account for the use of A. indica as an alternative treatment of antinociception and neuropharmacological abnormalities with further intensive studies. The compound, 3,4-dihydroxybenzoic acid was found to be most effective in computer aided models.
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BACKGROUND: Alzheimer's disease (AD), one of the major causes of dementia, is an overwhelming neurodegenerative disease that particularly affects the brain, leading to memory loss and impairment of language and judgment capacity. The aim of the present study was to investigate the antioxidant and anticholinesterase properties of the leaves of Elatostema papillosum (EPL) and correlate with their phytochemical profiles, which are relevant to the treatment of AD. METHODS: The dried coarse powder of EPL was extracted with 80% methanol (EPL-M80) by cold extraction method. The resultant EPL-M80 was assessed for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity by the Ellman method. The antioxidant activity was determined by DPPH (1, 1-diphenyl-2-picrylhydrazyl) and hydroxyl radical scavenging assays. Quantitative phytochemical (phenolic and flavonoid contents) analysis of endogenous substances in EPL-M80 was performed by standard spectrophotometric methods. RESULTS: EPL-M80 significantly (p < 0.05) inhibited AChE and BChE activity with IC50 of 165.40 ± 4.01 and 213.81 ± 3.57 µg/mL, respectively in a dose-dependent manner. Additionally, EPL-M80 exhibited strong radical scavenging activity against DPPH (IC50 = 32.35 ± 0.68 µg/mL) and hydroxyl radical (IC50 = 19.67 ± 1.42 µg/mL) when compared to that of standards. EPL-M80 was found to be rich in phenolic (23.74 mg gallic acid equivalent/g of dry extract) and flavonoid (31.18 mg quercetin equivalent/g of dry extract) content. Furthermore, a positive correlation (p < 0.001) was observed between the total phenolics and antioxidant as well as the anticholinesterase potential. CONCLUSIONS: The marked inhibition of AChE and BChE, and potent antioxidant activity of the leaves of Elatostema papillosum highlight its potential to provide an effective treatment for AD.
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Antioxidantes , Encéfalo , Inhibidores de la Colinesterasa , Fitoquímicos , Extractos Vegetales , Urticaceae/química , Enfermedad de Alzheimer , Animales , Antioxidantes/química , Antioxidantes/farmacología , Encéfalo/efectos de los fármacos , Encéfalo/enzimología , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Femenino , Flavonoides , Masculino , Fitoquímicos/química , Fitoquímicos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Ratas , Ratas WistarRESUMEN
BACKGROUND: The present study was planned to investigate the phytochemical, antioxidant, antinociceptive, anticoagulant and cytotoxic activities of the Jacquemontia tamnifolia (L.) Griseb leaf methanol extract (MExJT) in the laboratory using both in vitro and in vivo methods. METHODS: Phytochemical values, namely, total phenolic and flavonoid contents, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect and FeCl3 reducing power effects, were studied by established methods. In vivo antinociceptive activity was performed by acidic acid-induced writhing test and formalin-induced pain test on Swiss albino mice at doses of 125, 250 and 500 mg/kg body weight. The clot lysis and brine shrimp lethality bioassay in vitro were used to evaluate the thrombolytic and cytotoxic activities of the plant extract, respectively. RESULTS: Phytochemical screening illustrates the presence of tannins, saponins, flavonoids, gums and carbohydrates, steroids, alkaloids and reducing sugars in the extract. The results showed the total phenolic content (146.33 g gallic acid equivalents/100 g extract) and total flavonoid content (133.33 g quercetin/100 g). Significant (p<0.05) IC50 values compared to respective standards were recorded in DPPH radical scavenging (289.5 µg/mL) and FeCl3 reduction (245.2 µg/mL). The antinociceptive effect was evaluated in the acetic acid-induced writhing test and formalin-induced pain models in Swiss albino mice with doses of 125, 250 and 500 mg/kg body weight. Significant (p<0.05) inhibition (72.87±2.73%) of writhing response compared to diclofenac sodium was achieved by 500 mg/kg body weight. The extract also significantly inhibited the licking response in both the early phase (51.59±1.57%, p<0.05) and the late phase (64.82±1.87%, p<0.05) in the formalin-induced writhing test. MExJT also showed (38.10±1.79%) clot lytic activity in the thrombolytic test and cytotoxicity with an LC50 value of 31.70 µg/mL in the brine shrimp lethality bioassay. CONCLUSIONS: The plant is a potential source of antioxidants and might have one or more secondary metabolite(s) with central and peripheral analgesic activity. The results also demonstrate that MExJT has moderate thrombolytic and lower cytotoxic properties that may warrant further exploration.
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Anticoagulantes/farmacología , Antioxidantes/farmacología , Convolvulaceae/química , Extractos Vegetales/farmacología , Analgésicos/aislamiento & purificación , Analgésicos/farmacología , Analgésicos/toxicidad , Animales , Anticoagulantes/aislamiento & purificación , Anticoagulantes/toxicidad , Antioxidantes/aislamiento & purificación , Antioxidantes/toxicidad , Artemia/efectos de los fármacos , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Femenino , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Depuradores de Radicales Libres/toxicidad , Concentración 50 Inhibidora , Dosificación Letal Mediana , Masculino , Ratones , Extractos Vegetales/administración & dosificación , Extractos Vegetales/toxicidad , Hojas de la PlantaRESUMEN
BACKGROUND: This study aims to evaluate the scientific basis of traditional application of Persicaria orientalis for reducing pain and inflammation. METHODS: An in vitro method was performed to investigate the presence of the anti-inflammatory activity of methanolic crude extract of P. orientalis. In addition, an in vivo study was conducted in which the hot-plate and tail immersion methods were applied to explore the acute effect of P. orientalis on analgesia. The potency to inhibit chronic inflammation in mice was justified by the carrageenan-induced paw edema and formalin-induced edema methods. For all in vivo testing in animal models (albino mice and rats), plant extract was given via the oral route at doses of 250 mg/kg and 500 mg/kg. RESULTS: The methanolic extract of P. orientalis produced a significant (p<0.001) inhibition of analgesia with a prolongation of pain response time by 61.80% at 500 mg/kg. The extract also exhibited a potential anti-inflammatory (56.99%) effect, which was also statistically significant (p<0.001). The present study suggests that the methanolic extract of P. orientalis has potential anti-inflammatory as well as analgesic activity and this extract is effective in the treatment of both acute and chronic pain. CONCLUSIONS: Our current study revealed pharmacological properties of the methanolic extract of P. orientalis and also gave a solid scientific platform against its traditional use. The protecting ability of P. orientalis against inflammatory stimuli may be due to phenolic or flavonoid compounds which we have found through phytochemical analysis.
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Analgésicos/farmacología , Dimensión del Dolor/efectos de los fármacos , Extractos Vegetales/farmacología , Hojas de la Planta , Polygonaceae , Analgésicos/aislamiento & purificación , Analgésicos/uso terapéutico , Animales , Relación Dosis-Respuesta a Droga , Edema/tratamiento farmacológico , Edema/patología , Humanos , Metanol/farmacología , Metanol/uso terapéutico , Ratones , Dolor/tratamiento farmacológico , Dolor/patología , Dimensión del Dolor/métodos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/uso terapéutico , Ratas , Ratas WistarRESUMEN
BACKGROUND: Persicaria orientalis, an ornamental medicinal plant, has been used in traditional medicine for the treatment of various diseases. Although the plant is reported to have some important pharmacological effects, many medicinal values remain unidentified. Our objective was to evaluate the anti-inflammatory, anti-diarrheal, thrombolytic, and cytotoxic properties of the methanol extract of P. orientalis leaves (Po-MeOH). METHODS: Anti-inflammatory activity was measured by the inhibition of hypotonicity-induced human red blood cell hemolysis and albumin denaturation technique in vitro of Po-MeOH. Diarrheal episodes were examined in mice with castor oil-induced diarrhea. The clot lysis and brine shrimp lethality bioassay in vitro were used to evaluate the thrombolytic and cytotoxic activities of the plant extract, respectively. RESULTS: Using in vitro anti-inflammatory models, the results demonstrated that Po-MeOH at the five different dose ranges from 31.25 to 500 µg/mL significantly (p<0.05) protected (0.98%-50.71%) the erythrocyte membrane against lysis induced by hypotonic medium solution and protein denaturation (38.27%-79.22%) of bovine albumin, respectively. The extract exhibited a significant reduction of severity (75.17%) of castor oil-induced diarrhea in mice at the highest dose of 400 mg/kg compared to loperamide (82.06%) at 5 mg/kg. Po-MeOH also showed 33.14% clot lytic activity in the thrombolytic test and cytotoxicity with LC50 value 58.91 µg/mL in the brine shrimp bioassay. CONCLUSIONS: These findings suggest that Po-MeOH has significant anti-inflammatory and anti-diarrheal effects along with moderate thrombolytic and lower cytotoxic properties that may warrant the further exploration.
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Antiinflamatorios/uso terapéutico , Antidiarreicos/uso terapéutico , Citotoxinas/uso terapéutico , Fibrinolíticos/uso terapéutico , Extractos Vegetales/uso terapéutico , Polygonaceae , Animales , Antiinflamatorios/aislamiento & purificación , Antidiarreicos/aislamiento & purificación , Artemia , Bovinos , Citotoxinas/aislamiento & purificación , Diarrea/inducido químicamente , Diarrea/tratamiento farmacológico , Diarrea/patología , Relación Dosis-Respuesta a Droga , Femenino , Fibrinolíticos/aislamiento & purificación , Humanos , Masculino , Ratones , Extractos Vegetales/aislamiento & purificación , Plantas MedicinalesRESUMEN
BACKGROUND: Ricinus communis (Euphorbiaceae) has previously been reported to possess analgesic, antihistamine, antioxidant and anti-inflammatory activities. This study was designed for isolation, characterization and evaluation of antibacterial and anti-proliferative activities of R. communis seed protein. METHODS: The concentration and molecular weight of R. communis seed protein were estimated by SDS-PAGE and spectrophotometric analysis, respectively. Lectin activity was evaluated by hemagglutination assay on mice blood. In vitro susceptibility of four human pathogenic bacteria including Escherichia coli, Pseudomonas aeruginosa, Enterobacter aerogenes and Staphylococcus aureus was detected using disk diffusion assay, and minimum inhibitory concentration (MIC) value was determined using micro-dilution method. A total of twenty four Swiss albino mice containing Ehrlich's ascites carcinoma (EAC) cells were treated with the crude protein of R. communis at 50 and 100 µg/ml/d/mouse for 6 days. Growth inhibitory activity of R. communis seed protein on EAC cells was determined by haemocytometer counting using trypan blue dye and DAPI (4Î,6-diamidino-2-phenylindole) staining was used to assess apoptotic cells. RESULTS: The protein concentration of six R. communis (castor) varieties ranged between 21-35 mg/ml and molecular weight between 14-200 kDa. Castor protein agglutinated mice blood at 3.125 µg/wall. The seed protein shows considerable antimicrobial activity against E. coli, P. aeruginosa and S. aureus, exhibiting MIC values of 250, 125 and 62.5 µg/ml, respectively. Administration of seed protein led to 54 % growth inhibition of EAC cells at 100 µg/ml. DAPI staining indicates marked features of apoptosis including condensation of cytoplasm, nuclear fragmentation and aggregation of apoptotic bodies etc. CONCLUSION: Our study suggests that the lectin rich R. communis seed protein has strong antibacterial and anticancer activities.
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Antibacterianos/farmacología , Antineoplásicos/farmacología , Proliferación Celular/efectos de los fármacos , Extractos Vegetales/farmacología , Ricinus communis/química , Semillas/química , Animales , Antibacterianos/química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Bangladesh , Ratones , Pruebas de Sensibilidad Microbiana , Neoplasias Experimentales , Extractos Vegetales/química , Proteínas de Plantas/química , Proteínas de Plantas/farmacologíaRESUMEN
BACKGROUND: Ethnopharmacological approach has explored several leads from plant sources to identify potential new drugs for various diseases including pain. Vanda roxburghii R. Br., an epiphytic orchid is widely distributed throughout Bangladesh. The root of this plant has a folkloric reputation to treat inflammations, fever, dyspepsia, bronchitis, hiccough, piles, snake bites, and diseases of the nervous system. In this study therefore, we aimed to investigate antinociceptive and cytotoxic properties of the extracts from the root of V. roxburghii. METHODS: Dried powder of aerial root of V. roxburghii was extracted with methanol (VRM) and the resultant was fractionated into petroleum ether (VRP), chloroform (VRC), ethyl acetate (VRE), and residual aqueous fraction (VRA). The antinociceptive effect of the extracts was evaluated in mice using acetic acid-induced writhing, formalin injection, and hot plate tests. The brine shrimp lethality bioassay in vitro was used to evaluate cytotoxic activity of the plant extracts. RESULTS: In the acetic acid-induced writhing test, mice treated with different fractions (12.5, 25, and 50 mg/kg, i.p.) exhibited reduced number of writhing. Amongst, VRE showed the highest activity at all three concentrations (43.65, 71.34, and 80.23%, respectively) in a dose-dependent manner. Secondly, VRC (12.5, 25, and 50 mg/kg, i.p.) displayed the highest reduction of paw licking time in mice during the first phase of the formalin test (by 15.00, 37.05, and 56.44%, respectively) as well as during the second phase of the test (by 20.55, 49.08, and 59.81%, respectively). In hot plate test, VRE treatment at doses of 25 and 50 mg/kg both increased the highest latency time after 30 min. All fractions showed lower cytotoxicity compared with the standard drug vincristine sulfate in the brine shrimp bioassay. CONCLUSION: Overall studies suggest that the root of V. roxburghii is effective as a potent analgesic with lower toxicity. Our findings support previous claims of traditional uses of V. roxburghii in different inflammatory disorders.
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Analgésicos , Orchidaceae/química , Extractos Vegetales , Analgésicos/administración & dosificación , Analgésicos/química , Analgésicos/farmacología , Animales , Artemia/efectos de los fármacos , Conducta Animal/efectos de los fármacos , Ratones , Modelos Animales , Dimensión del Dolor , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Extractos Vegetales/farmacologíaRESUMEN
BACKGROUND: Alzheimer's disease (AD) is a progressively developing neurodegenerative disorder of the brain in the elderly people. Vanda roxburghii Rbr. root has been used traditionally in Bangladesh as tonic to brain and in the treatment of nervous system disorders including AD. Therefore, we aimed to investigate the cholinesterase inhibitory activities and antioxidant properties of the extracts from V. roxburghii. METHODS: The crude methanol extract from the roots of plant was sequentially fractionated with petroleum ether, chloroform, ethylacetate and water to yield their corresponding extracts. The extracts were assessed for acetylcholinesterase and butyrylcholinesterase inhibitory activity by modified Ellman method and antioxidant property by several assays including ferric reducing antioxidant power, scavenging of 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical and hydroxyl radical, and inhibition of lipid peroxidation. Endogenous substances in the extracts were analyzed by the standard phytochemical methods and active compound was isolated by the chromatographic methods. RESULTS: Chloroform extract was shown to demonstrate strong ferric-reducing antioxidant power and scavenging activity against DPPH and hydroxyl free radicals when compared with the other extracts and the reference standard catechin. The antioxidant effect was further verified by inhibition of lipid peroxidation in rat brain homogenates. Likewise, the chloroform extract exhibited the highest inhibition against both the acetylcholinesterase and butyrylcholinesterase enzymes with IC50 values of 221.13 and 82.51 µg/ml, respectively. Phytochemical screening revealed a large amount of phenolics and flavonoids in the chloroform extract. Bioactivity guided separation techniques led to the isolation of a strong antioxidant from the chloroform extract and its structure was determined as gigantol on the basis of spectral studies. CONCLUSION: These results suggest that the chloroform extract of V. roxburghii, possibly due to its phenolic compounds, exert potential antioxidant and cholinesterase inhibitory activities, which may be useful in the treatment of AD.
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Antioxidantes , Orchidaceae/química , Extractos Vegetales , Polifenoles , Animales , Antioxidantes/química , Antioxidantes/farmacología , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Cloroformo , Inhibidores de la Colinesterasa , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polifenoles/química , Polifenoles/farmacología , RatasRESUMEN
BACKGROUND: Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by loss of memory and cognition. The effective therapeutic options for AD are limited and thus there is a demand for new drugs. Aegle marmelos (Linn.) (A. marmelos) leaves have been used in traditional medicine to promote intellect and enhance memory. In this study, we evaluated A. marmelos for its acetylcholinesterase (AChE) inhibitory activity and antioxidant property in vitro in the treatment of AD. METHODS: A crude methanol extract and four fractions (petroleum ether, chloroform, ethyl acetate and aqueous) were prepared from the leaves of A. marmelos. The preparations were assessed for AChE inhibitory activity by the Ellman method, and their antioxidant properties were assessed by several assays: reducing power, scavenging of 1,1-diphenyl-2-picrylhydrazyl free radical and hydroxyl radical, and inhibition of lipid peroxidation. Qualitative and quantitative analyses of endogenous substances in A. marmelos were performed by the standard phytochemical methods. RESULTS: Among the different extracts tested, the ethyl acetate fraction exhibited the highest inhibition of AChE activity. In the same way, ethyl acetate fraction showed the highest reducing activity and radical scavenging ability towards the 1,1-diphenyl-2-picrylhydrazyl (half maximal inhibitory concentration = 3.84 µg/mL) and hydroxyl free radicals (half maximal inhibitory concentration = 5.68 µg/mL). The antiradical activity of the ethyl acetate fraction appeared to be similar to that of the reference standard butylated hydroxytoluene and catechin used in this study. In addition, the ethyl acetate fraction displayed higher inhibition of brain lipid peroxidation. Phytochemical screening of different extractives of A. marmelos showed the presence of phenols and flavonoids, alkaloid, saponin, glycoside, tannin and steroids. Quantitative analysis revealed higher contents of phenolics (58.79-mg gallic acid equivalent/g dried extract) and flavonoids (375.73-mg gallic acid equivalent/g dried extract) in the ethyl acetate fraction. CONCLUSION: The results suggest that the ethyl acetate fraction of A. marmelos is a significant source of polyphenolic compounds with potential AChE inhibitory property and antioxidant activity and, thus, may be useful in the treatment of AD.