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1.
Turk J Pharm Sci ; 18(1): 3-9, 2021 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-33631923

RESUMO

OBJECTIVES: The present study aimed to evaluate the nootropic activity of Limonia acidissima in rats. MATERIALS AND METHODS: Methanolic extract of Limonia acidissima was used to evaluate nootropic activity, piracetam (200 mg/kg, i.p.) was used as a standard, and scopolamine (1 mg/kg, i.p.) was used to induce amnesia. The effect of drugs on learning and memory in rats was evaluated by using the Y-maze task and elevated plus maze on scopolamine-induced amnesia models. Locomotor activity was performed using an actophotometer. Also, levels of acetylcholinestrease, including histopathological examination of rat brains, were assessed. RESULTS: Methanolic extract of Limonia acidissima showed increased alteration of the behavior response and percentage spontaneous alteration with the Y-maze task. In the elevated plus maze scopolamine-induced amnesia model, methanolic extract of Limonia acidissima showed a decrease in transfer latency, which is indicative of cognition improvement. Methanolic extract increased locomotor activity in rats and decreased the levels of acetylcholinestrease enzyme significantly. A histopathological study with both low and high doses of extract showed effective regenerative scores as compared to normal control, negative control and standard treatment. CONCLUSION: The results suggested that the administration of methanolic extract of Limonia acidissima enhances learning and memory in different experimental models. The histopathological study revealed the neuroprotective property of the extract. The study indicates that the extract may be used in the treatment of Alzheimer's disease.

2.
Comb Chem High Throughput Screen ; 24(3): 415-422, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32503404

RESUMO

The extracts and the compounds isolated from Phyllanthus amarus Schumm and Thonn (Family: Euphorbiaceae) have shown a wide spectrum of pharmacological activities including antiviral, antibacterial, antiplasmodial, antimalarial, antimicrobial, anticancer, antidiabetic, hypolipidemic, antioxidant, hepatoprotective, nephroprotective and diurectic properties. BACKGROUND: This investigation was aimed at exploring the anxiolytic potential of Phyllanthus amarus standardized extracts and predict probable role of marker phyto constitutents. OBJECTIVE AND METHODS: Three standardized extracts of Phyllanthus amarus plant viz. standardized aqueous extract of Phyllanthus amarus whole plant (PAAE), standardized methanolic extract of P. amarus leaf (PAME) and the standardized hydro-methanolic extract of P. amarus leaf (PAHME) were tested in the classical animal models of anxiety: Elevated plus-maze model and Light & Dark Exploration test. RESULTS: The lower doses of the tannin rich extract (PAHME) of the P. amarus possess significant anxiolytic activity compared to lignin rich (PAME) and aqueous extracts (PAAE), while at a higher dose (400mg/kg) the results of all three extracts appears to be potentially sedative. While the molecular docking studies support these probable anxiolytic, the sedative effects of the Phyllanthus amarus extracts could be due to the interaction of tannins and lignans with the GABAbenzodiazepine receptor complex. CONCLUSION: The results of the present study indicate that the tannin-rich extract of the P. amarus may have potential clinical applications in the management of anxiety. It can be further studied for optimum dosage to be used as a future of anti-anxiety drug development or as a standardized Phytomedicine.


Assuntos
Ansiolíticos/farmacologia , Glucosídeos/farmacologia , Taninos Hidrolisáveis/farmacologia , Lignanas/farmacologia , Phyllanthus/química , Extratos Vegetais/farmacologia , Animais , Ansiolíticos/química , Ansiolíticos/isolamento & purificação , Ansiedade/tratamento farmacológico , Feminino , Glucosídeos/química , Glucosídeos/isolamento & purificação , Taninos Hidrolisáveis/química , Taninos Hidrolisáveis/isolamento & purificação , Lignanas/química , Lignanas/isolamento & purificação , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
3.
Curr Drug Deliv ; 15(6): 755-764, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29424315

RESUMO

The imbalance of hydrophilicity and lipophilicity along with a large molecular size (due to a unique chemical structure) of natural compounds or plant actives poses a significant challenge for their absorption through a biological membrane and thus, alters the therapeutic efficacy. Therefore, it is desirable to have a novel approach for such formulation in order to improve the solubility and bioavailability of these phytoconstituents as a phospholipid complexation. Herbal drugs are precisely, embedded and bound by phospholipids to form vesicular structures which are amphoteric in nature. Thus, the phytolipid complex technology is unique, in the respect that it has a higher stability profile owing to its amphoteric nature or owing to its solubility in aqueous as well as oil media. It also exhibits a greater absorption and bioavailability, as the drug molecules are embedded in the pockets of the phytosomal assembly, therefore, with more drug loading capability, protection from the gastric environment, and subsequently inactivation in gastro-intestinal tract (GIT). Phytolipid complexes have a great potential in the field of medicine, pharmaceuticals and cosmetics due to improved pharmacokinetics and pharmacological attributes. The present review explores the various aspects of phytolipid complexes concerning the phospholipids, vesicles, choice of ingredients, phytolipid complexation, advantages, preparation methods and their applications.


Assuntos
Sistemas de Liberação de Medicamentos , Fosfolipídeos/química , Animais , Portadores de Fármacos/química , Humanos
4.
Int J Biol Macromol ; 105(Pt 1): 463-470, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28705502

RESUMO

The objective of this study was to synthesize and characterize citric acid crosslinked carboxymethyl tamarind gum (CMTG) hydrogels films. The hydrogel films were characterized by Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, solid state 13C-nuclear magnetic resonance (13C NMR) spectroscopy and differential scanning calorimeter (DSC). The prepared hydrogel films were evaluated for the carboxyl content and swelling ratio. The model drug moxifloxacin hydrochloride was loaded into hydrogels films and drug release was studied at pH 7.4. The hemolysis assay was used to study the biocompatibility of hydrogel films. The results of ATR-FTIR, solid state 13C NMR and DSC confirmed the formation of ester crosslinks between citric acid and CMTG. The total carboxyl content of hydrogel film was found to be decreased when amount of CMTG was increased. The swelling of hydrogel film was found to be decreased with increase in curing temperature and time. CMTG hydrogel films showed high drug loading with non-Fickian release mechanism suggesting controlled release of drug. The hydrogel films were found to be biocompatible. It can be concluded that the citric acid can be used for the preparation of CMTG hydrogel films. Further, CMTG hydrogel film can be used potentially for controlled release of drug.


Assuntos
Ácido Cítrico/química , Portadores de Fármacos/química , Portadores de Fármacos/síntese química , Hidrogéis/química , Hidrogéis/síntese química , Gomas Vegetais/química , Tamarindus/química , Técnicas de Química Sintética , Portadores de Fármacos/farmacologia , Liberação Controlada de Fármacos , Fluoroquinolonas/química , Hemólise/efeitos dos fármacos , Humanos , Hidrogéis/farmacologia , Moxifloxacina
5.
Indian J Gastroenterol ; 26(4): 167-9, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-17986743

RESUMO

AIMS: To compare the performance of monoethylglycinexylidide (MEGX) test and conventional liver function tests (LFT) in differentiating between healthy volunteers and patients with different severity of liver cirrhosis, as judged using Child-Pugh (CP) classification. METHODS: One hundred and four patients with cirrhosis (CP class A, 47; B, 32; C, 25) and 25 healthy volunteers were studied between January 2005 to June 2006. In these subjects, conventional LFT were done, and serum specimens collected 15, 30 and 60 minutes after lidocaine injection were analyzed for MEGX. RESULTS: Conventional liver function tests showed minor differences between healthy volunteers and patients with Child class A, whereas these discriminated well between patients with Child class C and healthy volunteers. The changes in ALT, AST, bilirubin, albumin, AP and PT values were statistically significant in CP class B and C but not in class A when compared with healthy volunteers. MEGX concentration at 60 min was significantly higher in healthy volunteers (131.2 ng/mL) as compared to patients with cirrhosis (CP A - 51.3 ng/mL; CP B - 37.1 ng/mL; CP C - 17.3 ng/mL). There were significant differences (p <0.001) among all four groups (healthy volunteers and patients with CP classes A, B and C) for MEGX concentrations at each time point. MEGX test correlated well with CP scores (p <0.0001). CONCLUSION: MEGX test is a useful marker to stratify patients with liver cirrhosis based on liver function.


Assuntos
Lidocaína/análogos & derivados , Cirrose Hepática/diagnóstico , Cirrose Hepática/fisiopatologia , Adulto , Idoso , Biomarcadores/sangue , Estudos de Casos e Controles , Feminino , Humanos , Lidocaína/sangue , Lidocaína/metabolismo , Cirrose Hepática/sangue , Cirrose Hepática/metabolismo , Testes de Função Hepática , Masculino , Pessoa de Meia-Idade , Sensibilidade e Especificidade , Índice de Gravidade de Doença
6.
Saudi J Gastroenterol ; 13(3): 118-23, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-19858627

RESUMO

BACKGROUND: The existing conventional liver function tests (LFTs) are indirect, inferior and have limited prognostic value. Therefore, the monoethylglycinexylidide (MEGX) test, which provides a direct measure of the actual functional state of the liver, is proposed as a real-time liver function test. The objective of this study was to assess the prognostic value of the MEGX test in cirrhosis by comparing it with Child-Turcotte-Pugh (CTP), the Mayo end stage liver disease (MELD) and discriminant function (DF) scores. MATERIALS AND METHODS: The study was carried out in Satara, India during the period of January 2005 to June 2006 and included 79 adult alcoholic cirrhotic patients. The serum specimen from each patient was analyzed using conventional LFTs and the MEGX test. The prognostic scores-CTP, MELD and DF scores were calculated and statistical analyses was performed. RESULTS: Based on receiver operating characteristic (ROC) curves, the MELD score and MEGX60 showed excellent sensitivity and specificity. The comparison of area under ROC curves showed that MELD and MEGX60 had superior prognostic accuracy when compared to other scores. Kaplan-Meier survival curves for corresponding cutoff values clearly differentiated between patients with different survival times. CONCLUSION: The MEGX test has shown more sensitivity, specificity and accuracy than CTP and DF scores in determining cases with the possibility of three- and six-month survival. Thus, it can be concluded that MEGX test along with MELD, is an effective prognostic tool in the hands of clinicians for predicting short-term survival.

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