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1.
J Ethnopharmacol ; 301: 115765, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36195303

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Mesua Assamica (King & prain) Kosterm. (MA) is an evergreen endemic medicinal tree available in Assam in India and other parts of south Asia. The bark of the plant is traditionally used for ant-malarial activity and treating fevers. It was reported to have anti-oxidant, anti-inflammatory, anti-diabetic, anti-cancer and anti-malarial properties, but no research findings have been reported about its protective activity on intestinal inflammatory disorders like ulcerative colitis (UC) yet. AIM OF THE STUDY: The aim of the current study is to evaluate the anti-ulcerative property of ethanolic extract of MA (MAE) in-vitro on GloResponse™ NF-кB-RE-luc2P HEK 293 cells for its anti-oxidant and anti-inflammatory activities and in-vivo chronic restraint stress aggravated dextran sodium sulfate (DSS)-induced UC model. MATERIALS AND METHODS: The chemical constituents of MAE were identified by LC-MS/MS. The in-vitro effects of MAE on GloResponse™ NF-кB-RE-luc2P HEK 293 cells stimulated with TNF-α 30 ng/ml were investigated for its potential therapeutic effects. Parameters such as body weights, behavioural, colonoscopy, colon lengths and spleen weights were measured and recorded in chronic restraint stress aggravated DSS-induced UC model in C57BL/6 mice. Histological, cytokines and immunoblotting analysis in the colon tissues were determined to prove its anti-inflammatory and anti-oxidant activities. RESULTS: MAE poses significant anti-oxidant and anti-inflammatory activity in-vitro in GloResponse™ NF-кB-RE-luc2P HEK 293 cells evidenced by DCFDA and immunoflourescence assay. MAE treatment at 100 mg/kg and 200 mg/kg for 14 consecutive days has reduced Disease activity Index (DAI), splenomegaly and improved the shortened colon length and sucrose preference in mice. MAE treatment has increased the levels of anti-oxidants like GSH and reduced the levels of MDA, MPO and nitrite levels in colon tissues. Moreover, MAE has ameliorated neutrophil accumulation, mucosal and submucosal inflammation and crypt density evidenced by histopathology. Furthermore, MAE treatment significantly reduced the increased pro-inflammatory cytokines like IL-6, IL-1ß and TNF-α. we found from immunoblotting that there is a concomitant decrease in protein expression of NF-κB, STAT3 signalling cascades and phosphorylation of IKBα with an increase in Nrf2, SOD2, HO-1 and SIRT1 in colon tissues. In addition, we have performed molecular docking studies confirming that phytochemicals present in the MAE have a stronger binding ability and druggability to the NF-κB, Nrf2 and SIRT1 proteins. CONCLUSIONS: MAE exhibited significant anti-colitis activity on chronic restraint stress aggravated DSS-induced ulcerative colitis via regulating NF-κB/STAT3 and HO-1/Nrf2/SIRT1 signaling pathways.


Assuntos
Colite Ulcerativa , NF-kappa B , Animais , Humanos , Camundongos , Anti-Inflamatórios , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Cromatografia Líquida , Colite Ulcerativa/induzido quimicamente , Colo , Citocinas/metabolismo , Sulfato de Dextrana , Células HEK293 , Camundongos Endogâmicos C57BL , Simulação de Acoplamento Molecular , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Casca de Planta/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/metabolismo , Transdução de Sinais , Sirtuína 1/metabolismo , Espectrometria de Massas em Tandem , Fator de Necrose Tumoral alfa/metabolismo
2.
Nat Prod Res ; 37(13): 2215-2224, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35129017

RESUMO

Aims of the study were the phytochemical investigation and chemical transformation of isolated compounds of medicinal plant listed in 'Ayurveda' like Dolichandrone atrovirens, endemic to Indian subcontinents. From chloroform extract of D. atrovirens four compounds; Ursolic acid (1), Maslinic acid (2), Lupeol (3), ß-sitosterol (4) and from methanol extract five compounds; ß-sitosterol-3-O-ß-D-glucopyranoside (5), 10-O-trans-p-Methoxycinnamoylcatalpol (6), Kaempferol-3-O-ß-D-glucopyranoside (7), 6-O-[6"(S)-hydroxy-2",6"dimethyl-2"(E)-7"-octadienoyl] catalpol (8) and Ixoside (9) were isolated. Ixoside was used for the semi-synthetic modification via azomethine ylide cycloaddition leading to novel spiro-oxindolo-pyrrolizidine adduct. The structures of novel adducts were elucidated by analysis of IR, MS and 1 D/2D NMR data. Furthermore, to confirm the chemo selection of only one double bond, we performed density functional theory (DFT) calculation, which confirms the chemo selectivity. In addition, in-silico ADME studies and atom-additive approach based on SASA was also examined for the molecules which suggest that they may be potential future candidates for drug discovery.


Assuntos
Compostos Fitoquímicos , Extratos Vegetais , Reação de Cicloadição , Estrutura Molecular
3.
Mol Biol Rep ; 49(3): 2487-2501, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35013861

RESUMO

BACKGROUND: The production of lipid-laden cells in macrophages after significant ingestion of oxidized low-density lipoprotein is considered the most critical phase in the creation of atherosclerotic lesions, which is known as foam cell formation. Targeting foam cell development to find a potential therapeutic strategy for the management of atherosclerosis has yielded numerous promising outcomes. Multiple variables influence foam cell growth, including scavenger receptor expression, cholesterol transporter expression acyl CoA: cholesterol acyltransferase activity, and neutral cholesteryl ester hydrolase activity. Plants used during herbal therapy have been shown to assist with a variety of ailments. RESULT: In this study, we found medicinal plants and their bioactive components suppress foam cell formation in a variety of ways; some inhibit cholesterol transporter and lectin-like oxidized low-density lipoprotein receptor-1 upregulation, while others inhibit the function of acyl CoA: cholesterol acyltransferase activity, and neutral cholesteryl ester hydrolase activity. CONCLUSION: Recent study findings related to the synthesis of the new active component from plant sources by focusing on the typical process involved in the generation of foam cells. We're also looking at using a cellular target-based therapeutic approach to generate novel plant-based medications for the cure of atherosclerosis.


Assuntos
Aterosclerose , Células Espumosas , Aterosclerose/metabolismo , Colesterol/metabolismo , Expressão Gênica , Humanos , Lipoproteínas LDL/metabolismo , Macrófagos/metabolismo
4.
Clin Nutr ESPEN ; 46: 21-32, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34857198

RESUMO

The catastrophic pandemic engendered due to the Novel coronavirus (COVID-19) outbreak which causes severe clinical afflictions on the respiratory system has severely high morbidity and mortality rates. The requirement of novel compounds is at utmost importance due to lack of targeted drug molecule to treat the afflictions and restrict the viral infection and for the usage of prophylactic treatment to avoid the spread of the infection is of utmost importance. Vitamin D is one such naturally available multifunctional molecule, which plays an eminent role in the immune system and instigation of numerous cellular pathways further promoting health benefits and enhancing the human quality of life. This article reviews the current standpoint scenario and future prevalence of vitamin D supplementation in the management of covid-19 patients. Novel findings of Vitamin D suggest that along with regulation of cell growth, neuroprotective and mood-stabilizing effects, it regulates the immune response also modulate cytokine Interleukin-6 (IL-6) by inducing progesterone-induced blocking factor (PIBF), given the IL-6 levels are considerably high in COVID-19 patients which increases the further complications. Vitamin D also have its effect on angiotensin converting enzyme (ACEII) inhibitor through which the COVID-19 virus makes cell entry. Numerous research data elucidate the play of Vitamin D, in complications of COVID-19 including the most common comorbid conditions, neurological manifestations and immunological aspects makes it an ideal molecule for adjuvant therapy. Including Vitamin D as add-on therapy in the management of COVID-19 might aid the arrest of infection and helps fight this arduous epidemic.


Assuntos
COVID-19 , Vitaminas , Humanos , Qualidade de Vida , SARS-CoV-2 , Luz Solar
5.
Health Sci Rev (Oxf) ; 1: 100005, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34977914

RESUMO

With the upsurge in the cases of COVID-19 around the world, plenty of potential COVID-19 complications are becoming more prevalent, including a higher risk of secondary bacterial and fungal infections. Mucormycosis is one such condition which has high prevalence among individuals with diabetes who were infected with COVID-19.The usage of steroids in the treatment further inflates the risk of infection and exacerbation of disease in pre-existent mucormycosis patients. Generally, Corticosteroid-induced diabetes can arise on long-term steroid medication, increasing the likelihood of mucormycosis. In patients with COVID-19, the indications and dose of corticosteroids should be properly regulated, and persons with diabetes who take insulin or oral anti-diabetic medicines should be cautious. To avoid poor outcomes, strategies to improve glycemic management should be emphasized. This narrative review elucidates different disciplines on rampant use of steroids, iron and zinc supplements as well as the methods utilized as primary or adjunctive treatment of this fatal condition. This article may help to pave the way for robust research that needs to be done to tackle the deadly triple burden of the disease.

6.
Curr Drug Deliv ; 14(8): 1053-1059, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-27572089

RESUMO

BACKGROUND: Curcumin is a yellow polyphenolic chemopreventive agent isolated from the rhizomes of Curcuma longa. It is approved as Generally Regarded as Safe by US FDA. Nonetheless, its clinical success is limited due to its poor aqueous solubility, fast metabolism and short biological half-life attributes. OBJECTIVE: Quercetin-decorated liposomes of curcumin (QCunp) are perceived to be able to overcome these biopharmaceutical drawbacks. METHODS: Curcumin liposomes with/without quercetin were prepared by lipid hydration technique. The liposomes were characterized for their particle size, zeta potential, surface morphology, drug loading and release characteristics. The toxicity of the liposomes were evaluated in-vitro and their invivo efficacy were tested against Dalton's ascites lymphoma in mice. RESULTS: Liposomes designed showed particle size of 261.8 ± 2.1 nm with a negative zeta potential of -22.6±1.6 mV. Quercetin decorated liposomes were more effective in increasing the life span and body weight of lymphoma inflicted mice compared to those without quercetin. Similarly, the presence of quercetin also contributed to enhanced cytotoxicity of the liposomal formulation towards HT-29 cells and HCT-15 cells. CONCLUSION: Newer liposomal design exhibited promising potential to emerge as alternative anticancer therapeutics.


Assuntos
Antineoplásicos/química , Curcumina/administração & dosagem , Curcumina/química , Lipossomos/química , Linfoma/tratamento farmacológico , Quercetina/química , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Proliferação de Células/efeitos dos fármacos , Curcumina/farmacologia , Curcumina/uso terapêutico , Ensaios de Seleção de Medicamentos Antitumorais , Células HT29 , Humanos , Lipossomos/administração & dosagem , Lipossomos/síntese química , Linfoma/patologia , Masculino , Camundongos , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/patologia , Tamanho da Partícula , Quercetina/administração & dosagem , Propriedades de Superfície , Células Tumorais Cultivadas
7.
Pharm Biol ; 54(4): 628-36, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26428681

RESUMO

CONTEXT: Hygrophila auriculata (K. Schum) Heine (Acanthaceae) has been traditionally used for the treatment of various ailments such as inflammation, rheumatism, jaundice and malaria. OBJECTIVE: The present study aims to separate terpenoid fraction (TF) from alcohol (70%) extract of the whole plant of Hygrophila auriculata and assess its anti-inflammatory activity. MATERIALS AND METHODS: HPTLC analysis of TF was performed for the estimation of lupeol. Edema was induced in Wistar albino rats by subplanter injection of 0.1 ml of 1% (w/v) carrageenan into the right hind paw after 1 h of TF administration (100 and 200 mg/kg oral). Septic shock was induced by intraperitoneal administration of LPS (100 µg/kg) in rats and interleukins (IL-1ß and IL-6), tumor necrosis factor (TNF-α), superoxide dismutase (SOD), lipid peroxidation (LPO), and nitric oxide (NO) were measured in serum. AutoDock 4.2 was used for molecular docking. RESULTS: Administration of TF significantly (p < 0.005) restored the serum levels of cytokines, LPO (7.77 ± 0.034 versus 4.59 ± 0.059 nmole of TBARS), NO (9.72 ± 0.18 versus 4.15 ± 0.23 µmol nitrite/mg of wet tissue), and SOD (4.89 ± 0.036 versus 7.83 ± 0.033 Unit/mg protein) compared with the LPS-challenged rats. Analysis of in silico results revealed that TNF-α is the most appropriate target in eliciting anti-inflammatory activity. CONCLUSION: The present findings suggest that TF of Hygrophila auriculata possesses great promise as an anti-inflammatory agent which may be due to its antioxidant effect. Molecular docking results could be exploited for lead optimization and development of suitable treatment of inflammatory disorders.


Assuntos
Acanthaceae , Endotoxinas/antagonistas & inibidores , Endotoxinas/toxicidade , Extratos Vegetais/uso terapêutico , Choque Séptico/tratamento farmacológico , Terpenos/uso terapêutico , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Endotoxinas/metabolismo , Feminino , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/metabolismo , Lipopolissacarídeos/toxicidade , Masculino , Camundongos , Simulação de Acoplamento Molecular/métodos , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Choque Séptico/induzido quimicamente , Choque Séptico/metabolismo , Terpenos/isolamento & purificação , Terpenos/farmacologia
8.
Chin J Nat Med ; 12(2): 114-20, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-24636061

RESUMO

AIM: Sargassum wightii Greville is a marine brown alga belonging to the Sargassaceae family which has about 200 species. The ethanolic extract of the whole dry plant powder contained numerous phytoconstituents, including flavonoids. The study was focused on the anticancer activity of Sargassum wightii in mice. METHOD: The ethanolic extract of Sargassum wightii (EESW) at two dose levels was used to examine the anticancer activity in mice using DAL cell lines to induce cancer. The body weight, viable and non-viable tumor cell count, mean survival time, increase in life span, and hematological parameters were observed for anticancer activity of EESW. RESULTS: The intraperitoneal inoculation of DAL cells in mice significantly increased cancer cell count. The decrease in the cancer cell number observed in the EESW-treated group cancer animals indicates that the test drug has a significant inhibitory effect on the tumor cell proliferation. Treatment with EESW also showed a significant decrease in tumor weight, and hence increased the lifespan of DAL-treated mice. In addition, EESW administration significantly restored the hematological parameters in DAL-treated mice. CONCLUSION: The present study results suggest that administration of extract offers enhanced antioxidant potential. Therefore it can be concluded from this study that EESW possesses anticancer activity.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Linfoma/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Sargassum , Animais , Antineoplásicos Fitogênicos/farmacologia , Ascite , Linhagem Celular Tumoral , Proliferação de Células , Hematologia , Humanos , Camundongos , Extratos Vegetais/farmacologia , Taxa de Sobrevida
9.
Asian Pac J Trop Biomed ; 2(4): 269-75, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23569912

RESUMO

OBJECTIVE: To assess anti-psoriatic activity of the methanol extract and the isolated flavonoid quercetin from the rhizome of Smilax china (S. china) Linn. METHODS: Mouse tail test was used for the evaluation of anti-psoriatic activity. Methanol extract (100 and 200 mg/kg b.w.) and isolated flavonoid quercetin (25 and 50 mg/kg b.w.) were tested in Swiss albino mice. Parameters studied in the mouse tail test were changes in epidermal thickness and percentage orthokeratotic values. The anti-inflammatory role of the methanol extract and isolated flavonoid quercetin was evaluated using carrageenan-induced pleurisy in rats. In vitro antiproliferant assay on HaCaT cell lines was also carried out. RESULTS: The isolated flavonoid quercetin from the rhizome of S. china produced significant orthokeratosis (P<0.01) in the mouse tail test. In epidermal thickness, a significant reduction with respect to control was observed in groups treated with retinoic acid and isolated flavonoid quercetin. The methanol extract (200 mg/kg) and isolated flavonoid quercetin (50 mg/kg) showed anti-inflammatory effect in terms of significant inhibition (P<0.001) in leukocyte migration. Maximum antiproliferant activity was shown by isolated flavonoid quercetin (IC50, 62.42±10.20 µg/mL). CONCLUSIONS: From the above data, the flavonoid quercetin shows significant orthokeratosis, anti-inflammatory and maximum antiproliferant activities. To our knowledge, this is the first report on the anti-psoriatic effect of the flavonoid quercetin which is promising for further investigations to prove its anti-psoriatic activity.


Assuntos
Anti-Inflamatórios/farmacologia , Extratos Vegetais/farmacologia , Psoríase/patologia , Quercetina/farmacologia , Smilax/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/toxicidade , Carragenina , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Modelos Animais de Doenças , Humanos , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Pleurisia , Quercetina/química , Quercetina/toxicidade , Ratos , Ratos Wistar , Rizoma/química
10.
Asian Pac J Trop Biomed ; 1(5): 401-5, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23569801

RESUMO

OBJECTIVE: To investigate the anti-anaphylactic, anti-inflammatory and membrane stabilizing properties of plumerianine (compound 1) isolated from the root bark of Plumeria acutifolia Poir. METHODS: The anti-anaphylactic activity of compound 1 (10, 25 and 50 mg/kg) was studied by using models such as passive cutaneous anaphylaxis, passive paw anaphylaxis and its anti-inflammatory activity against carrageenin induced paw edema and cotton pellet granuloma in albino rats was also investigated using ketotifen and indomethacin as reference drugs. RESULTS: A dose-dependent beneficial effect was observed on leakage of evans blue dye in skin challenged with antigen and on paw anaphylaxis induced by antiserum. The compound 1 also exhibited significant (P<0.01) inhibition of rat paw edema and granuloma tissue formation, including significant protection of RBC against the haemolytic effect of hypotonic solution, an indication of membrane-stabilizing activity. CONCLUSIONS: Anti-anaphylactic activity of compound 1 may be possibly due to inhibition of the release of various inflammatory mediators. Anti-inflammatory activity of compound may be related to the inhibition of the early phase and late phase of inflammatory events.


Assuntos
Anafilaxia/tratamento farmacológico , Antialérgicos/farmacologia , Anti-Inflamatórios/farmacologia , Apocynaceae/química , Iridoides/farmacologia , Casca de Planta/química , Extratos Vegetais/farmacologia , Animais , Antialérgicos/química , Antialérgicos/uso terapêutico , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Modelos Animais de Doenças , Membrana Eritrocítica/efeitos dos fármacos , Eritrócitos , Feminino , Iridoides/química , Iridoides/uso terapêutico , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos Wistar
11.
Toxicol Ind Health ; 24(10): 635-42, 2008 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-19141568

RESUMO

D-Galactosamine (GalN)-induced liver injury is associated with reactive oxygen species and oxidative stress. In the present study, we evaluated the effect of alpha lipoic acid (ALA) supplementation on acute GalN-induced oxidative liver injury. Hepatotoxicity induced by single intraperitoneal injection of GalN (500 mg/kg body wt) was evident from increase in lipid peroxidation and serum marker enzymes (asparate transaminase, alanine transaminase, alkaline phosphatase, and lactate dehydrogenase). The decreased activities of enzymic antioxidants (superoxide dismutase, catalase, glutathione peroxidase, and glutathione reductase) as well as glutathione levels were the salient features observed in GalN-induced hepatotoxicity. Pretreatment with ALA (50 mg/kg body weight for 7 days) significantly precluded these changes and prevents the hepatic injury. Hence, this study clearly exemplified that ALA might be a suitable candidate against GalN-induced cellular abnormalities.


Assuntos
Antioxidantes/metabolismo , Doença Hepática Induzida por Substâncias e Drogas , Galactosamina/toxicidade , Fígado/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ácido Tióctico/farmacologia , Análise de Variância , Animais , Biomarcadores/metabolismo , Catalase/metabolismo , Modelos Animais de Doenças , Galactosamina/administração & dosagem , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Injeções Intraperitoneais , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/enzimologia , Hepatopatias/metabolismo , Masculino , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo
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