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1.
Langmuir ; 34(4): 1447-1456, 2018 01 30.
Artigo em Inglês | MEDLINE | ID: mdl-29281292

RESUMO

Bioactive nanomaterials, namely: ruthenium hydrous oxide (or ruthenium oxy-hydroxide), RuOx(OH)y and also a surface-conjugated novel material of the same within the template of an amino acid molecule, l-cysteine, have been studied. These compounds have been prepared through a simple wet chemical route, under physiological conditions, such that they could be suitably used in anticancer applications. Several physical methods were used for the nanomaterial characterization, e.g.: thermal analysis of the as prepared ruthenium hydrous oxide by differential scanning calorimetry (DSC) followed by thermal gravimetric analysis (TGA). This confirms that the material is a precursor for anhydrous nanocrystalline ruthenium oxide (RuO2), as is affirmed by powder X-ray diffraction pattern. Also, optical spectroscopic absorption (UV-vis and FT-IR) study of these nanoparticles (NPs) to ascertain their surface conjugation with l-cysteine have been performed. Besides these, surface morphology of the NPs were studied by field emission scanning electron microscopy (FE-SEM) along with their elemental purity check through energy dispersive X-ray analysis (EDX). Their surface chemical microenvironments were examined by X-ray photo electron spectroscopy (XPS). The hydrodynamic size of the prepared NPs were measured through dynamic light scattering (DLS) studies. Further, biological consequences of these NPs on cancerous HeLa cells and their cytotoxicity effects have been reported with MTT assay, such an application has not been reported so far.


Assuntos
Antineoplásicos/química , Cisteína/química , Nanopartículas Metálicas/química , Compostos de Rutênio/química , Varredura Diferencial de Calorimetria , Difusão Dinâmica da Luz , Células HeLa , Humanos , Microscopia Eletrônica de Varredura , Difração de Raios X
2.
Int J Mol Sci ; 17(10)2016 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-27669220

RESUMO

Amaranthus spinosus Linn. (Family: Amaranthaceae) has been shown to be useful in preventing and mitigating adverse pathophysiological conditions and complex diseases. However, only limited information is available on the anticancer potential of this plant. In this study, we examined the antiproliferative and pro-apoptotic effects of a novel fatty acid isolated from A. spinosus-(14E,18E,22E,26E)-methyl nonacosa-14,18,22,26 tetraenoate-against HepG2 human liver cancer cells. We used 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to determine cell viability, flow cytometry assay for cell cycle analysis, and Western blot analysis to measure protein expression of Cdc2), cyclin B1, Bcl-2-associated X protein (Bax), and B-cell lymphoma 2 (Bcl-2). The MTT assay showed that the fatty acid markedly inhibited the proliferation of HepG2 cells in a dosage-dependent fashion, with a half maximal inhibitory concentration (IC50) value of 25.52 µmol/L. This antiproliferative result was superior to that of another known fatty acid, linoleic acid (IC50 38.65 µmol/L), but comparable to that of standard anticancer drug doxorubicin (IC50 24.68 µmol/L). The novel fatty acid also induced apoptosis mediated by downregulation of cyclin B1, upregulation of Bax, and downregulation of Bcl-2, resulting in the G2/M transition arrest. Our results provide the first experimental evidence that a novel fatty acid isolated from A. spinosus exhibits significant antiproliferative activity mediated through the induction of apoptosis in HepG2 cells. These encouraging results may facilitate the development of A. spinosus fatty acid for the prevention and intervention of hepatocellular carcinoma.


Assuntos
Amaranthus/química , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Ácidos Graxos Insaturados/farmacologia , Amaranthus/metabolismo , Antineoplásicos/farmacologia , Ciclina B1/metabolismo , Regulação para Baixo/efeitos dos fármacos , Ácidos Graxos Insaturados/química , Ácidos Graxos Insaturados/isolamento & purificação , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Regulação para Cima/efeitos dos fármacos , Proteína X Associada a bcl-2/metabolismo
3.
Pharm Biol ; 54(10): 2364-7, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27043360

RESUMO

CONTEXT: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as ''spiny pigweed'', is used in both Indian traditional system and folk medicine for treatment of infectious diseases for a long time in several traditional herbal medicinal preparations. A novel fatty acid [(14E, 18E, 22E, 26E)-methyl nonacosa-14, 18, 22, 26 tetraenoate] is the major metabolite present. OBJECTIVE: This study examines the antibacterial potential of the fatty acid isolated from the A. spinosus against some Gram-positive and Gram-negative bacteria. MATERIALS AND METHODS: Three Gram-positive and seven Gram-negative bacterial strains were used for antibacterial assay. The minimum inhibitory concentration (MIC) of the fatty acid was analysed by dilution method and the effects of the fatty acid on the bacterial membrane were studied in detail by flow cytometry analysis. RESULTS AND DISCUSSION: All the studied bacterial strains were found to be inhibited at a concentration of 100 µg/mL. Staphylococcus aureus ML-59, Bacillus lycheniformis 10341, Shigella boydii 8, Vibrio cholera 811, Vibrio cholera 854 and Vibrio alginolyteus were susceptible and sensitive to the tested fatty acid with a MIC value of 25 µg/mL. It proved a full spectrum of antibacterial activity associated with alterations in the permeability of bacterial membranes. CONCLUSION: The fatty acid from the A. spinosus possesses potent antibacterial action.


Assuntos
Amaranthus , Antibacterianos/farmacologia , Ácidos Graxos Insaturados/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Extratos Vegetais/farmacologia , Amaranthus/química , Antibacterianos/isolamento & purificação , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Permeabilidade da Membrana Celular/efeitos dos fármacos , Ácidos Graxos Insaturados/isolamento & purificação , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Negativas/metabolismo , Bactérias Gram-Positivas/crescimento & desenvolvimento , Bactérias Gram-Positivas/metabolismo , Testes de Sensibilidade Microbiana , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais
4.
Pharm Biol ; 54(11): 2536-2546, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27225970

RESUMO

CONTEXT: Termitomyces clypeatus (Lyophyllaceae) is a filamentous edible mushroom, having ethnomedicinal uses. However, information about the antioxidant, anticancer and antitumour properties of this mushroom remains to be elucidated. OBJECTIVE: The study examines the in vitro antioxidant, anticancer and in vivo antitumour activity of T. clypeatus. MATERIALS AND METHODS: Antioxidant activity was evaluated with seven in vitro assays. Cytotoxicity of T. clypeatus was tested against a panel of cancer cells lines including U373MG, MDA-MB-468, HepG2, HL-60, A549, U937, OAW-42 and Y-79 using MTT assay. The antitumour activity of aqueous extract was evaluated against Ehrlich ascites carcinoma (EAC) tumour model in Swiss albino mice. RESULTS: HPLC analysis of aqueous extract revealed the presence of sugar entities. Termitomyces clypeatus showed excellent in vitro antioxidant activity. Termitomyces clypeatus was found cytotoxic against all cancer cells, among which it showed higher activity against U937 (IC50 25 ± 1.02 µg/mL). Treatment of EAC-bearing mice with varied doses of aqueous extract significantly (p < 0.01) reduced tumour volume, viable tumour cell count and improved haemoglobin content, RBC count, mean survival time, tumour inhibition and % increase life span. The enhanced antioxidant status in treated animals was evident from the decline in the levels of lipid peroxidation, increased levels of glutathione, catalase and superoxide dismutase. DISCUSSION: The analyzed data indicate that the aqueous extract of T. clypeatus exhibits significant antitumour activity, which might be due to the antioxidant effects on EAC bearing hosts. CONCLUSION: Termitomyces clypeatus possesses anticancer activity, valuable for application in food and drug products.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Termitomyces , Animais , Carcinoma de Ehrlich/tratamento farmacológico , Carcinoma de Ehrlich/patologia , Linhagem Celular Tumoral , Radical Hidroxila/metabolismo , Masculino , Camundongos , Superóxidos/metabolismo
5.
Pharm Biol ; 53(4): 600-4, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25339411

RESUMO

CONTEXT: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as "spiny pigweed", is used both in the Indian traditional system and in folk medicine to treat diabetes. OBJECTIVE: The present study evaluates the scientific basis of antidiabetic activity of chloroform fraction of methanol extract of A. spinosus and of an isolated constituent of A. spinosus. MATERIALS AND METHODS: HPLC analysis was performed to determine the purity and the amount of the constituent present in the plant extract. The yeast α-glucosidase inhibition technique was used to determine the antidiabetic activity of A. spinosus. Acarbose was used as a standard. An appropriate therapeutic approach for preventing diabetes mellitus and obesity is to retard the absorption of glucose by inhibition of α-glucosidase. RESULTS: One novel fatty acid with strong α-glucosidase inhibitory activity - (14E, 18E, 22E, 26E) - methyl nonacosa-14, 18, 22, 26 tetraenoate [1] (IC50 value 6.52 µM/mL) and ß-sitosterol [2] were purified. Compound 1 was found to be more potent than the methanol extract. HPLC quantitative analysis revealed that 0.15% of compound 1 and 0.06% of compound 2 were present in the plant extract. CONCLUSION: This novel fatty acid can potentially be developed as a novel natural nutraceutical for the management of diabetes.


Assuntos
Amaranthus/química , Ácidos Graxos Insaturados/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Hipoglicemiantes/isolamento & purificação , Metanol/química , Extratos Vegetais/química , Sitosteroides/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Ácidos Graxos Insaturados/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/farmacologia , Sitosteroides/farmacologia , Leveduras/enzimologia , alfa-Glucosidases/genética
6.
Eur J Med Chem ; 264: 115990, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38039791

RESUMO

Free fatty acid receptor 1 (FFAR1 or GPR40) is a potential target for treating type 2 diabetes mellitus (T2DM) and related disorders that have been extensively researched for many years. GPR40/FFAR1 is a promising anti-diabetic target because it can activate insulin, promoting glucose metabolism. It controls T2DM by regulating glucose levels in the body through two separate mechanisms: glucose-stimulated insulin secretion and incretin production. In the last few years, various synthetic GPR40/FFAR1 agonists have been discovered that fall under several chemical classes, viz. phenylpropionic acid, phenoxyacetic acid, and dihydrobenzofuran acetic acid. However, only a few synthetic agonists have entered clinical trials due to various shortcomings like poor efficacy, low lipophilicity and toxicity issues. As a result, pharmaceutical firms and research institutions are interested in developing synthetic GPR40/FFAR1 agonists with superior effectiveness, lipophilicity, and safety profiles. This review encompasses the most recent research on synthetic GPR40/FFAR1 agonists, including their chemical classes, design strategies and structure-activity relationships. Additionally, we have emphasised the structural characteristics of the most potent GPR40/FFAR1 agonists from each chemical class of synthetic derivatives and analysed their chemico-biological interactions. This work will hopefully pave the way for developing more potent and selective synthetic GPR40/FFAR1 agonists for treating T2DM and related disorders.


Assuntos
Diabetes Mellitus Tipo 2 , Humanos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Insulina/metabolismo , Receptores Acoplados a Proteínas G/agonistas , Glucose , Relação Estrutura-Atividade
7.
Eur J Pharmacol ; 944: 175588, 2023 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-36791843

RESUMO

Cancer is amongst the deadliest and most disruptive disorders, having a much higher death rate than other diseases worldwide. Human cancer rates continue to rise, thereby posing the most significant concerns for medical health professionals. In the last two decades, researchers have gone past several milestones in tackling cancer while gaining insight into the role of apoptosis in cancer or targeting various biomarker tools for prognosis and diagnosis. Apoptosis which is still a topic full of complexities, can be controlled considerably by B-cell lymphoma 2 (BCL-2) and its family members. Therefore, targeting proteins of this family to prevent tumorigenesis, is essential to focus on the pharmacological features of the anti-apoptotic and pro-apoptotic members, which will help to develop and manage this disorder. This review deals with the advancements of various epigenetic regulators to target BCL-2 family proteins, including the mechanism of several microRNAs (miRNAs) and long non-coding RNAs (lncRNAs). Similarly, a rise in natural and synthetic molecules' research over the last two decades has allowed us to acquire insights into understanding and managing the transcriptional alterations that have led to apoptosis and treating various neoplastic diseases. Furthermore, several inhibitors targeting anti-apoptotic proteins and inducers or activators targeting pro-apoptotic proteins in preclinical and clinical stages have been summarized. Overall, agonistic and antagonistic mechanisms of BCL-2 family proteins conciliated by epigenetic regulators, natural and synthetic agents have proven to be an excellent choice in developing cancer therapeutics.


Assuntos
Neoplasias , Proteínas Proto-Oncogênicas c-bcl-2 , Humanos , Apoptose , Proteínas Reguladoras de Apoptose/metabolismo , Epigênese Genética , Neoplasias/tratamento farmacológico , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo
8.
Artigo em Inglês | MEDLINE | ID: mdl-22690244

RESUMO

In the present study, the hepatoprotective activity of ethanolic extracts of Cassia sophera Linn. leaves was evaluated against carbon-tetrachloride- (CCl(4)-) induced hepatic damage in rats. The extracts at doses of 200 and 400 mg/kg were administered orally once daily. The hepatoprotection was assessed in terms of reduction in histological damage, changes in serum enzymes, serum glutamate oxaloacetate transaminase (AST), serum glutamate pyruvate transaminase (ALT), serum alkaline phosphatase (ALP), total bilirubin, and total protein levels. The substantially elevated serum enzymatic levels of AST, ALT, ALP, and total bilirubin were restored towards the normalization significantly by the extracts. The decreased serum total protein level was significantly normalized. Silymarin was used as standard reference and exhibited significant hepatoprotective activity against carbon tetrachloride-induced hepatotoxicity in rats. The biochemical observations were supplemented with histopathological examination of rat liver sections. The results of this study strongly indicate that Cassia sophera leaves have potent hepatoprotective action against carbon tetrachloride-induced hepatic damage in rats. This study suggests that possible activity may be due to the presence of flavonoids in the extracts.

9.
Pharm Biol ; 50(9): 1151-6, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22849439

RESUMO

CONTEXT: In the Indian traditional system of medicine, Melothria heterophylla (Lour.) Cogn., (Cucurbitaceae) is prescribed for the treatment of diabetes mellitus. OBJECTIVE: In the present study, the antidiabetic effect of ethanol extract of Melothria heterophylla (EEMH), and its active isolated constituents were investigated in streptozotocin (STZ)-induced diabetic Swiss albino rats. METHOD: Successive Soxhlet extraction of the dried total aerial parts with petroleum ether for defatting and then with ethanol (95%) to obtain ethanol extract, which was concentrated under reduced pressure. Hyperglycemia was induced in rats by STZ (50 mg/kg, body weight). Twenty-four hours after STZ induction, respective groups of diabetic rats received EEMH (200 and 400 mg/kg, body weight), gallic acid (GA) (2 and 4 mg/kg, body weight), and rutin (RU) (2 and 4 mg/kg, body weight), respectively, orally daily for 15 days. Glibenclamide (0.5 mg/kg, orally) served as reference. Blood glucose levels and change in body weight were measured on every 5(th) day during 15 days of treatment. Biochemical parameters, viz., serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT), alkaline phosphatase (ALP) and serum insulin, were measured. RESULTS: EEMH and its active constituents significantly (p < 0.01) normalized blood glucose levels and serum biochemical parameters as compared to those of STZ controls. Both GA (4 mg/kg) and RU (4 mg/kg) exhibited maximum glucose lowering effect (69.1 and 66.7%, respectively) in diabetic rats compared to the other dose (2 mg/kg) at the end of the study. EEMH, gallic acid and RU also showed significant increase in serum insulin, and body weight of STZ-induced diabetic rats. CONCLUSION: Therefore, ethanol extract of Melothria heterophylla, GA and RU demonstrated remarkable antidiabetic activity in STZ-induced diabetic rats.


Assuntos
Cucurbitaceae/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hiperglicemia/prevenção & controle , Hipoglicemiantes/uso terapêutico , Fitoterapia , Componentes Aéreos da Planta/química , Extratos Vegetais/uso terapêutico , Animais , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/fisiopatologia , Etnofarmacologia , Ácido Gálico/administração & dosagem , Ácido Gálico/efeitos adversos , Ácido Gálico/isolamento & purificação , Ácido Gálico/uso terapêutico , Insuficiência Hepática/complicações , Insuficiência Hepática/prevenção & controle , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/efeitos adversos , Hipoglicemiantes/isolamento & purificação , Índia , Insulina/sangue , Insulina/metabolismo , Secreção de Insulina , Fígado/efeitos dos fármacos , Fígado/fisiopatologia , Masculino , Extratos Vegetais/administração & dosagem , Extratos Vegetais/efeitos adversos , Extratos Vegetais/isolamento & purificação , Ratos , Rutina/administração & dosagem , Rutina/efeitos adversos , Rutina/isolamento & purificação , Rutina/uso terapêutico , Estreptozocina , Testes de Toxicidade Aguda , Redução de Peso/efeitos dos fármacos
10.
Int J Biol Macromol ; 199: 36-41, 2022 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-34971639

RESUMO

Agarose is a seaweed-based polysaccharide and is widely used for the separation of nucleic acids in molecular biology. Cross-linked agarose beads are also used as solid-phase matrices in size exclusion chromatography for the separation of proteins. To find the application of agarose for the separation of oil/water emulsion and protein, herein hydrophobic derivative of the seaweed biopolymer [MW (1.27 ± 0.17) × 10 5 g/mol; sulphate content (0.29 ± 0.09) %, gel strength (2242 ± 21) g/cm2] is prepared by reacting the biopolymer with stearic acid and was used to prepare a composite membrane on polyester fabric. The oil and BSA rejection performance of the composite membrane was greater than 98%. The rejection rate increased with the increase in polymer content in the respective membranes for both oil/water and protein separation. The composite membrane showed a stable oil/water emulsion and protein separation performance over a period of six hours. Due to the biodegradable nature of the major components of the membrane, it has the potential for industrial applications.


Assuntos
Alga Marinha , Purificação da Água , Emulsões/química , Interações Hidrofóbicas e Hidrofílicas , Sefarose , Purificação da Água/métodos
11.
Planta Med ; 77(8): 804-8, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21154199

RESUMO

This article describes the antihyperglycemic activity, in vivo antioxidant potential, effect on hemoglobin glycosylation, estimation of liver glycogen content, and in vitro peripheral glucose utilization of bacosine, a triterpene isolated from the ethyl acetate fraction (EAF) of the ethanolic extract of Bacopa monnieri. Bacosine produced a significant decrease in the blood glucose level when compared with the diabetic control rats both in the single administration as well as in the multiple administration study. It was observed that the compound reversed the weight loss of the diabetic rats, returning the values to near normal. Bacosine also prevented elevation of glycosylated hemoglobin in vitro with an IC50 value of 7.44 µg/mL, comparable with the one for the reference drug α-tocopherol. Administration of bacosine and glibenclamide significantly decreased the levels of malondialdehyde (MDA), and increased the levels of reduced glutathione (GSH) and the activities of superoxide dismutase (SOD) and catalase (CAT) in the liver of diabetic rats. Bacosine increased glycogen content in the liver of diabetic rats and peripheral glucose utilization in the diaphragm of diabetic rats in vitro, which is comparable with the action of insulin. Thus, bacosine might have insulin-like activity and its antihyperglycemic effect might be due to an increase in peripheral glucose consumption as well as protection against oxidative damage in alloxanized diabetes.


Assuntos
Bacopa/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Glicemia/metabolismo , Catalase/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/prevenção & controle , Feminino , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Glibureto/farmacologia , Hemoglobinas Glicadas/metabolismo , Insulina/sangue , Insulina/metabolismo , Insulina/farmacologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Glicogênio Hepático/metabolismo , Masculino , Malondialdeído/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo , alfa-Tocoferol/farmacologia
12.
Life Sci ; 273: 119270, 2021 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-33640402

RESUMO

Stem cells (SCs) are clonogenic cells that develop into the specialized cells which later responsible for making up various types of tissue in the human body. SCs are not only the appropriate source of information for cell division, molecular and cellular processes, and tissue homeostasis but also one of the major putative biological aids to diagnose and cure various degenerative diseases. This study emphasises on various research outputs that occurred in the past two decades. This will give brief information on classification, differentiation, detection, and various isolation techniques of SCs. Here, the various signalling pathways which includes WNT, Sonic hedgehog, Notch, BMI1 and C-met pathways and how does it effect on the regeneration of various classes of SCs and factors that regulates the potency of the SCs are also been discussed. We also focused on the application of SCs in the area of regenerative medicine along with the cellular markers that are useful as salient diagnostic or curative tools or in both, by the process of reprogramming, which includes diabetes, cancer, cardiovascular disorders and neurological disorders. The biomarkers that are mentioned in various literatures and experiments include PDX1, FOXA2, HNF6, and NKX6-1 (for diabetes); CD33, CD24, CD133 (for cancer); c-Kit, SCA-1, Wilm's tumor 1 (for cardiovascular disorders); and OCT4, SOX2, c-MYC, EN1, DAT and VMAT2 (for neurological disorders). In this review, we come to know the advancements and scopes of potential SC-based therapies, its diverse applications in clinical fields that can be helpful in the near future.


Assuntos
Diferenciação Celular , Medicina Regenerativa , Células-Tronco/citologia , Células-Tronco/fisiologia , Animais , Humanos , Transdução de Sinais
13.
Saudi Pharm J ; 18(3): 173-8, 2010 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23964177

RESUMO

Antihyperglycemic and hypolipidemic effects of ethanol extract of aerial parts of Melothria maderaspatana and Coccinia indica were evaluated in STZ induced diabetes in Sprague-Dawley rats. The rats were concurrently treated with 100 or 200 mg/kg b.w. p.o. for 14 days. The changes in fasting blood glucose level and body weight were measured in 5 days interval. After 14 days experimental period, rats were sacrificed by cervical decapitation, blood and liver samples were collected. Biochemical estimation of plasma glucose, cholesterol, triglycerides, LDL, HDL, SGOT, SGPT and ALP were done from blood sample. The liver glycogen content was estimated using standard procedure from homogenized liver sample. Administration of EEMm or EECi to STZ-diabetic rats caused significant antihyperglycemic and hypolipidemic effects (p < 0.001). The extracts were also found to be significantly effective (p < 0.001; p < 0.05) on recovery of altered biochemical parameters and decreased body weight in treated animals. Glibenclamide (0.5 mg/kg b.w.) was used as standard in present study.

14.
Medicines (Basel) ; 6(2)2019 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-31137810

RESUMO

Background: Melothria heterophylla (family: Cucurbitaceae), commonly known as kudari, is used in the Indian traditional medicine to treat various inflammation-associated diseases, such as asthma, arthritis and pain. However, the anti-inflammatory active components of this plant have not been identified yet. The aim of this study was to investigate the potential analgesic and anti-inflammatory activities of a compound, quercetin-3-methoxy-4'-glucosyl-7-glucoside, isolated from M. heterophylla. Methods: The anti-inflammatory activity was determined using carrageenan- and dextran-induced rat paw edema as well as cotton pellet-induced granuloma in rats, whereas the analgesic activity was analyzed using acetic acid-induced writhing, hot plate and tail flick response in mice. The test compound was orally administered at a dose of 5, 10 or 15 mg/kg. The cyclooxygenase-1 (COX-1)- and COX-2-inhibitory capacity of the test compound was studied by enzyme immunosorbent assay. Results: Quercetin-3-methoxy-4'-glucosyl-7-glucoglucoside at 15 mg/kg exhibited a maximum inhibition of carrageenan-induced inflammation (50.3%, p < 0.05), dextran (52.8%, p < 0.05), and cotton pellets (41.4%, p < 0.05) compared to control animals. At the same dose, it showed a 73.1% inhibition (p < 0.05) of the pain threshold in acetic acid-induced writhing model. It also exhibited a considerable analgesic activity by prolonging the reaction time of the animals based on hot plate as well as tail flick response. The test compound was found to inhibit COX-1 (IC50 2.76 µg/mL) and more efficiently, COX-2 (IC50 1.99 µg/mL). Conclusions: Quercetin-3-methoxy-4'-glucosyl-7-glucoside possessed substantial analgesic and anti-inflammatory activities possibly due to inhibition of prostaglandin production, supporting the ethnomedicinal application of M. heterophylla to treat various inflammatory disorders.

15.
Nat Prod Res ; 33(22): 3287-3292, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29724132

RESUMO

Betulinic acid was first time isolated via bioactivity-guided fractionation from ethyl acetate extract of Nyctanthes arbor-tristis leaves. Its structure was established by FTIR, 1H and 13C- nuclear magnetic resonance and high-resolution mass spectrometry. It had shown excellent inhibition of anti-inflammatory properties with IC50 of 10.34 µg/mL (COX-1), 12.92 µg/mL (COX-2), 15.53 µg/mL (5-LOX), 15.21 µg/mL (Nitrite), 16.65 µg/mL (TNF-α), and also exhibited potent antioxidant activity with IC50 of 18.03 µg/mL. The anticancer activity of betulinic acid was evaluated against different human cancer cell lines. It showed significant cytotoxicity against various cancer cell lines with an IC50 of 6.53 (HepG2), 9.34 (A549), 14.92 (HL-60), 16.90 (MCF-7), 17.07 (HCT-116), 13.27 (PC-3), and 12.55 µM (HeLa). This is the first report on isolation and identification of the unreported lupane-type triterpenoid, betulinic acid from leaves of Nyctanthes arbor-tristis, which showed potent anti-inflammatory, antiproliferative, and antioxidant activity in vitro assays.


Assuntos
Oleaceae/química , Extratos Vegetais/farmacologia , Triterpenos/isolamento & purificação , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antineoplásicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Fracionamento Químico , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Triterpenos Pentacíclicos , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Análise Espectral , Triterpenos/farmacologia , Ácido Betulínico
16.
ISRN Pharmacol ; 2013: 789613, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24369507

RESUMO

A variety of active constituents with wide range of pharmacological actions have been reported with Centella asiatica. The present study was undertaken to assess analgesic and anti-inflammatory properties of its leaf extracts. Dried leaves were defatted with petroleum ether and extracted with chloroform and methanol. Both chloroform and methanol extracts were evaluated for analgesic activity through tail clip, tail flick, tail immersion, and writhing assay tests at doses of 50, 100, and 200 mg/kg using Swiss albino mice. On the other hand, anti-inflammatory assay was performed by carrageenan induced paw edema of methanol extract at 100 and 200 mg doses in Wistar albino rat. Dextropropoxyphene and indomethacin were employed as a standard for analgesic and anti-inflammatory studies, respectively. Our present study demonstrated that Centella asiatica bears significant analgesic and anti-inflammatory activities in those models.

17.
Singapore Med J ; 53(10): 676-80, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23112020

RESUMO

INTRODUCTION: We aimed to analyse the pregnancy outcome of women with extrahepatic portal vein obstruction. METHODS: This was a retrospective observational analysis conducted at the Institute of Postgraduate Medical Education and Research, Kolkata, India, between January 2007 and September 2009. A total of 41 pregnancies in 24 women were evaluated. RESULTS: All women conceived spontaneously (maternal age 20-35 years). 17 women had moderate-to-severe anaemia, and five women had pancytopenia. Variceal bleeding occurred in ten women during pregnancy, which was managed successfully with endoscopic sclerotherapy in eight women and endoscopic variceal ligation in two women. Preterm labour (14.63%), postpartum haemorrhage (7.31%), abortion (4.87%) and pregnancy-induced hypertension (4.87%) were observed in the 41 pregnancies. There were 39 live births and almost all mothers delivered vaginally, except for four who underwent Caesarean section for obstetric indications. Prematurity (15.38%), low birth weight (10.25%), admission to the neonatal intensive care unit (12.82%), stillbirth (2.56%) and neonatal death (2.56%) were noted in the newborns. CONCLUSION: Variceal bleeding during pregnancy coincided with unfavourable outcomes. Although endoscopic obliteration of varices is a safe and effective method for antenatal management of varices in women, prenatal obliteration results in less morbidity. On rare occasions, obliterated varices can bleed in subsequent pregnancies. Therefore, preconception evaluation of the state of varices prior to each pregnancy and their ligation are important aspects of counselling. A successful foetomaternal outcome is achievable with multidisciplinary backup in a tertiary care centre.


Assuntos
Hepatopatia Veno-Oclusiva/complicações , Hipertensão Portal/complicações , Veia Porta , Complicações na Gravidez/epidemiologia , Adulto , Endoscopia Gastrointestinal , Feminino , Hepatopatia Veno-Oclusiva/epidemiologia , Hepatopatia Veno-Oclusiva/terapia , Humanos , Hipertensão Portal/epidemiologia , Hipertensão Portal/terapia , Fígado/irrigação sanguínea , Gravidez , Complicações na Gravidez/terapia , Resultado da Gravidez , Estudos Retrospectivos , Adulto Jovem
18.
Asian Pac J Trop Med ; 4(8): 619-23, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21914539

RESUMO

OBJECTIVE: To investigate hepatoprotective activity of ethanol extract of Melothria heterophylla Lour Cogn. (EEMH) against CCl(4)-induced hepatic damage in rats. METHODS: ß-sitosterol was isolated by column chromatography and characterized spectroscopically. Two different doses (200 and 400 mg/kg bw) of EEMH were administered orally in alternate days. The hepatoprotective activity was studied in liver by measuring biochemical parameters such as serum aspartate amino transferase (AST), alanine amino transferase (ALT), alkaline phosphatase (ALP), total protein and total bilirubin. Lipid peroxidation product and different antioxidant enzyme activities were assessed in liver homogenate. RESULTS: EEMH reduced all biochemical parameters and lipid peroxidation, as well as it increased the antioxidant enzyme activities in comparison with silymarin. The protective effect of the extract on CCl(4) induced damage was confirmed by histopathological examination of the liver. CONCLUSIONS: This result strongly supports the protective effect of EEMH against acute liver injury, and may be attributed to its antioxidative activity.


Assuntos
Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Cucurbitaceae/química , Fígado/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Sitosteroides , Alanina Transaminase/sangue , Fosfatase Alcalina/sangue , Animais , Antioxidantes/química , Aspartato Aminotransferases/sangue , Tetracloreto de Carbono/efeitos adversos , Doença Hepática Induzida por Substâncias e Drogas/sangue , Doença Hepática Induzida por Substâncias e Drogas/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Extratos Vegetais/química , Substâncias Protetoras/química , Ratos , Ratos Wistar , Silimarina/farmacologia , Sitosteroides/química , Sitosteroides/farmacologia
19.
Biol Pharm Bull ; 29(11): 2202-5, 2006 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-17077515

RESUMO

The potential role of the methanolic extract of Heliotropium zeylanicum (BURM.F) LAMK (MEHZ) in the treatment of diabetes along with its antioxidant and antihyperlipidemic effects was studied in streptozotocin-induced diabetic rats. Oral administration of (MEHZ) 150 and 300 mg/kg/d for 14 d significantly decreased the blood glucose level and considerably increased the body weight, food intake, and liquid intake of diabetic-induced rats. MEHZ significantly decreased thiobarbituric acid reactive substances and significantly increased reduced glutathione, superoxide dismutase and catalase in streptozotocin-induced diabetic rats at the end of 14 d of treatment. The study also investigated the antihyperlipidemic potential of MEHZ. The results show that the active fraction of MEHZ is promising for development of a standardized phytomedicine for the treatment of diabetes mellitus.


Assuntos
Antioxidantes/uso terapêutico , Diabetes Mellitus Experimental/prevenção & controle , Heliotropium/química , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Administração Oral , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Glicemia/análise , Peso Corporal/efeitos dos fármacos , Catalase/metabolismo , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/metabolismo , Ingestão de Líquidos/efeitos dos fármacos , Ingestão de Alimentos/efeitos dos fármacos , Glutationa/metabolismo , Hipercolesterolemia/induzido quimicamente , Hipercolesterolemia/metabolismo , Hipercolesterolemia/prevenção & controle , Hipertrigliceridemia/induzido quimicamente , Hipertrigliceridemia/metabolismo , Hipertrigliceridemia/prevenção & controle , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/isolamento & purificação , Hipolipemiantes/administração & dosagem , Hipolipemiantes/isolamento & purificação , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Fitoterapia/métodos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Ratos Wistar , Estreptozocina , Superóxido Dismutase/metabolismo , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Tolbutamida/farmacologia
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