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1.
Nutr Cancer ; 73(11-12): 2363-2375, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32972250

RESUMO

OBJECTIVE: The present study aimed to evaluate the efficacy of methanolic extract of Muntingia calabura L. leaves (MEMC) in ameliorating oxidative stress and inflammation associated with 1,2-dimethyl hydrazine (DMH) induced colon cancer. METHODS: The antioxidant enzymes, oxidative stress markers, liver and renal toxicity markers were evaluated. Histopathological examination of colon tissues was carried out with the aid of alcian blue stain and Hematoxylin and Eosin stain. RESULTS: MEMC supplementation at doses of 100 and 200 mg/kg body weight of rats causes the antioxidant enzymic levels to retain near to its normal range. Meanwhile the oxidative stress markers, which showed an elevation from its normal level upon DMH administration, gets significantly reduced on MEMC treatment. Histopathological observation also revealed that the severity of colorectal cancer was reduced by the supplementation of MEMC. CONCLUSION: The findings from the present study showed that MEMC can exert a potential role to ameliorate the oxidative stress and inflammation associated with colorectal cancer.


Assuntos
Neoplasias do Colo , Metanol , 1,2-Dimetilidrazina/toxicidade , Animais , Antioxidantes/farmacologia , Carcinogênese , Colo , Neoplasias do Colo/induzido quimicamente , Neoplasias do Colo/tratamento farmacológico , Metanol/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar
2.
Drug Dev Ind Pharm ; 47(12): 1998-2003, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35616220

RESUMO

Xanthine oxidase (XO) is accountable for the uric acid synthesis in the body and is considered as a prominent therapeutic target in urate lowering treatment. Eugenol is a natural compound commonly found in clove, cinnamon, etc. and has various biological activities. This study was designed to examine the anti-hyperuricemic effect of eugenol by in vitro and in vivo studies. Potassium oxonate (PO) was used to induce hyperuricemia in Wistar rats. Different doses of eugenol (1.25, 2.5, and 5 mg/kg bwt orally) were used for the treatment and various biological function markers (renal, hepatic, and hematological) were analyzed. The IC50 value obtained for eugenol was 3.51 ± 0.002 µM. The kinetic studies revealed that the eugenol exhibited a mixed type of inhibition. Abnormality in the levels of various biological function markers was observed in the PO treated rats. Upon the eugenol treatment, those biological function markers were retained near to its normal values. The study proved the anti-hyperuricemic potential of eugenol against the PO induced hyperuricemia model.


Assuntos
Hiperuricemia , Animais , Eugenol/farmacologia , Eugenol/uso terapêutico , Hiperuricemia/tratamento farmacológico , Cinética , Ratos , Ratos Wistar , Xantina Oxidase/metabolismo , Xantina Oxidase/uso terapêutico
3.
Pathophysiology ; 26(3-4): 323-330, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31439385

RESUMO

The plant Muntingia calabura L. is a well-known herb which gained attention due to its pharmacological value. The necessity of this plant in human ailments is illustrious in old medical practices. Muntingia calabura L. leaves were therapeutically used for ulcer, fever, headache etc. The study was designed to assess the acute toxicity and anti-inflammatory potential of methanolic extract of Muntingia calabura L. (MEMC) in in vivo models. Two different doses (550, 2000 mg/kg body weight) of MEMC were taken to evaluate the acute toxicity response. The drugs were given orally to wistar rats and were monitored for behavioral changes and mortality for 14 days period. The blood parameter analysis, serum analysis of liver and kidney injury markers and histopathological evaluation of kidney, heart and liver were carried out. The Carrageenan induced paw edema model was performed to inspect the anti-inflammatory response of MEMC. The level of CRP in serum and the histological alterations in the paw tissue were evaluated. There were no evident symptoms of toxicity observed in animals treated with MEMC at the dose of 2000 mg/kg body weight. The Carrageenan induced paw edema model study established the anti-inflammatory potential of MEMC. The MEMC, which is innoxious, can act as a potential anti-inflammatory drug.

4.
Indian J Clin Biochem ; 34(2): 155-163, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31092988

RESUMO

ABSTRACT: The medicinal plant, Terminalia bellirica (Gaertn.) Roxb. is widely used in the traditional Indian system of medicine like Ayurveda for centuries in the treatment of various ailments owing to it's rejuvenating as well as health promoting effects. The present study evaluates protective role of aqueous acetone extract of T. bellirica fruits (AATB) against CCl4 induced liver toxicity in animal model. The liver damage was assessed by liver function markers including ALT, AST, ALP, GGT, LDH, total bilirubin, total protein, albumin, globulin and albumin-globulin ratio. The levels of MDA, ROS, and NO along with the tissue antioxidants were evaluated to assess hepatic oxidative stress and level of lipid peroxidation. Treatment with AATB prior to the exposure of CCl4 significantly reduced the damage when compared to the control rats. The outcome of the present study advocates the traditional use of the plant as ethnic food and health tonic.

5.
Pathophysiology ; 25(4): 381-387, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30032909

RESUMO

The current study aims to the detection of pathogenic potential and virulence factor identification of uropathogenic Escherichia coli BRL-17 isolated from patients urine. The organism was isolated from the patient with chronic pyelonephritis. The identification of organism was done by analyzing gram staining, biochemical, 16S rDNA analysis, Raman microscopy and SEM analysis. The pathogenic potential was identified by multiplex PCR analysis of virulence factor genes like sfa, hly D, pap C. The biofilm forming ability was tested by congo red agar assay and tissue culture plate assay. The result of gram staining and biochemical analysis shows the characteristics of E-coli. The 16S rDNA analysis of the clinically isolated uropathogen showed 100% similarity with uropathogenic Escherichia coli strain. Raman microscopy and SEM confirms the organism as E-coli. The Multiplex PCR study identifies virulence genes like sfa, hly D, pap C in isolated E-coli. The presence of P fimbriae coded pap C gene, S fimbriae coded sfa gene and hemolysin-D coded hly D gene discloses its potential to cause urinary tract infection. Biofilm assay result enhances the organism's role as strong biofilm former. This biofilm forming ability of Escherichia coli strain BRL-17 made the organism to escape from host immune system and helps to colonize in bladder and kidney. This also helps to enhance the resistance to antibiotics. Our study confirms the organism as multidrug resistant, highly virulent, strong biofilm forming E-coli. The strain may be used for the development of animal models of pyelonephritis for the purpose of drug discovery.

6.
Inflammopharmacology ; 2018 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-30003465

RESUMO

Terminalia bellirica (Gaertn.) Roxb. (Family: Combretaceae), known as Bhibhitaki in Sanskrit and locally known as Behera in India, has been used for centuries in Ayurveda, a universal system of medicine in India. The dried fruit of T. bellirica is used for the treatment of several disorders. The present study aims to explore the anti-inflammatory effects of aqueous acetone extracts isolated from T. bellirica (AATB) in RAW 264.7 cell lines. The AATB was prepared from the fruits of T. bellirica. Different concentrations of AATB (6.25-100 µg/ml) were used for MTT assay. The anti-inflammatory effect of AATB was evaluated by using different assays such as total cyclooxygenase (COX), 5-lipoxygenase (5-LOX) activity, nitrate and reactive oxygen species (ROS) production. The mRNA level expression of COX-2, tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) were studied in LPS stimulated RAW 264.7 cells. AATB treatment significantly diminished the elevated levels of inflammatory markers. Moreover, AATB downregulated the mRNA level expression of TNF-α, IL-6 and COX-2 genes. The result of our study suggest the use of AATB and is able to reduce inflammatory conditions associated with various diseases.

7.
Inflammopharmacology ; 26(1): 29-38, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29159716

RESUMO

Rotula aquatica belongs to the family Boraginaceae, and is reported to contain baunerol, steroids and alkaloids. In Ayurveda, R. aquatica has been used for the treatment of various diseases such as diabetes, treatment of piles, venereal disease, and cancer. The current study aims to investigate the anti-inflammatory effect of methanolic extract of R. aquatica (MERA) in RAW 264.7 cells. The cytotoxicity of MERA was analyzed by MTT assay. The total cyclooxygenase (COX) activity, 5-lipoxygenase (5-LOX) activity, myeloperoxidase activity, inducible nitric oxide synthase activity, nitrate level and reactive oxygen species production were studied in LPS-stimulated RAW 264.7 cells. The gene level expression of cyclooxygenase-2 (COX-2), tumor necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6) were also evaluated in this study. The MERA did not show any cytotoxicity at different concentrations (6.25-100 µg/ml). MERA (100 µg/ml) inhibited total COX and 5-LOX activity at 50.53 and 62.03%, respectively, besides significantly (p < 0.05) diminished nitrate and ROS generation, when compared with LPS control. Moreover, MERA down-regulated the mRNA expressions of inflammatory marker genes like TNF-α, IL-6, and COX-2 against LPS stimulation. Our results demonstrate that MERA is able to attenuate inflammatory response, possibly via ROS and NO suppression, inhibiting the production of arachidonic acid metabolites and modulation of proinflammatory mediators and cytokines release.


Assuntos
Anti-Inflamatórios/farmacologia , Boraginaceae/química , Citocinas/metabolismo , Mediadores da Inflamação/metabolismo , Extratos Vegetais/farmacologia , Animais , Araquidonato 5-Lipoxigenase/metabolismo , Linhagem Celular , Inflamação/induzido quimicamente , Inflamação/metabolismo , Interleucina-6/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Peroxidase/metabolismo , Células RAW 264.7 , Espécies Reativas de Oxigênio/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
8.
Microb Pathog ; 113: 102-106, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29066378

RESUMO

We evaluate the role of antioxidant enzyme status and inflammatory cascade in disease progression of cystitis in a rat model. The animals were injected with clinically isolated Uropathogenic Escherichia coli (UPEC) and study the effect of various antioxidant enzymes and inflammatory markers in disease pathology on the 0th day, 12 h and 7th day of infection. The antioxidant status of bladder tissue was decreased during the 7th day of infection. Lipid peroxidation marker MDA was increased on the 7th day of infection in rats. The histopathology of bladder tissue shows severe inflammation and edema. This study reveals the role of decreased antioxidant status during infection play a vital role in upregulation of inflammation and tissue destruction.


Assuntos
Cistite/patologia , Infecções por Escherichia coli/patologia , Glutationa Peroxidase/metabolismo , Glutationa Redutase/metabolismo , Superóxido Dismutase/metabolismo , Infecções Urinárias/patologia , Escherichia coli Uropatogênica/patogenicidade , Animais , Antioxidantes/metabolismo , Catalase/metabolismo , Cistite/microbiologia , Infecções por Escherichia coli/microbiologia , Feminino , Glutationa/metabolismo , Inflamação/microbiologia , Inflamação/patologia , Peroxidação de Lipídeos/fisiologia , Estresse Oxidativo/fisiologia , Ratos , Ratos Wistar , Infecções Urinárias/microbiologia
9.
Microb Pathog ; 109: 189-194, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28578087

RESUMO

Urinary tract infections are the most common bacterial infections affecting millions of people each year worldwide. The animal model provides an excellent and suitable system for studying cystitis and pyelonephritis caused by Escherichia coli and other uropathogens. Using this established model, we evaluate the role of antioxidant defence system, renal injury markers, and blood parameters in the diseases progression during Escherichia coli infection on 0th day, 12h and 7th day. The antioxidant enzymes like SOD, CAT, GSH, GPx, GR levels were evaluated. The blood parameters like AST, ALT, ALP, Total protein, BUN, creatinine level were estimated in infection model. The relative organ weights, anti microbial status of kidney, CRP, WBC count were done for the evaluation of inflammatory response associated with the infection. The oxidative stress marker like MDA was also evaluated. Histopathological analysis of renal tissue provides direct vision to tissue damage. The antioxidant status of renal tissue was decreased during the 7th day of infection. Likewise, renal toxicity markers were significantly increased during bacterial infection. The inflammatory markers like CRP, WBC count and oxidative stress marker like MDA were significantly increased by the infection on 7th day. The histopathology of renal tissue also reveals the inflammation and tissue damage associated with acute pyelonephritis.


Assuntos
Antioxidantes/metabolismo , Biomarcadores/sangue , Progressão da Doença , Pielonefrite/sangue , Pielonefrite/imunologia , Alanina Transaminase/sangue , Fosfatase Alcalina/sangue , Animais , Aspartato Aminotransferases/sangue , Nitrogênio da Ureia Sanguínea , Proteína C-Reativa , Catalase/metabolismo , Modelos Animais de Doenças , Escherichia coli/patogenicidade , Infecções por Escherichia coli/imunologia , Infecções por Escherichia coli/microbiologia , Infecções por Escherichia coli/patologia , Feminino , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Glutationa Redutase/metabolismo , Inflamação/patologia , Rim/lesões , Rim/metabolismo , Rim/microbiologia , Rim/patologia , Peroxidação de Lipídeos , Tamanho do Órgão , Estresse Oxidativo , Pielonefrite/microbiologia , Pielonefrite/patologia , Ratos , Ratos Wistar , Superóxido Dismutase/sangue , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Fatores de Tempo , Infecções Urinárias/sangue , Infecções Urinárias/imunologia , Infecções Urinárias/microbiologia , Infecções Urinárias/patologia
10.
Regul Toxicol Pharmacol ; 86: 349-355, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28389325

RESUMO

Terminalia bellirica (Gaertn.) Roxb. (Family: Combretaceae), known as Bhibhitaki in Sanskrit and locally known as Behera in India is one of the oldest medicinal plants which has widely been used in the traditional system of medicine, especially in Ayurveda for centuries. The dried fruit of Terminalia bellirica is used for treating various ailments. Aqueous acetone extract of Terminalia bellirica (Gaertn.) Roxb fruits (AATB), showed antioxidant potential in our screening study is selected for the present in vivo toxicity evaluation. Acute administration of AATB was done in female Wistar Albino rats as a single dose up to 2000 mg/kg body weight. At the end of the study, Blood was collected for biochemical and hematological analyses, while histological examinations were performed on liver and kidney. There was no alteration in the behavioral pattern, food and water intake in the treated animals. The relative organ weight, biochemical parameters, hematological parameters and histopathological analysis were also found normal. All the parameters of the toxicity evaluation were found to be normal and the data suggests aqueous acetone extract of Terminalia bellirica fruit is safe, to be used as a traditional herbal formulation for its antioxidant potential and other health benefits.


Assuntos
Frutas/química , Extratos Vegetais/toxicidade , Terminalia/química , Acetona , Animais , Feminino , Índia , Rim/efeitos dos fármacos , Rim/patologia , Fígado/efeitos dos fármacos , Fígado/patologia , Tamanho do Órgão/efeitos dos fármacos , Ratos , Ratos Wistar , Testes de Toxicidade
11.
Toxicol Ind Health ; 32(7): 1224-36, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25415873

RESUMO

Hepatic fibrosis, characterized by extracellular matrix accumulation, is the common cause of chronic liver failure and is a leading cause of morbidity and mortality worldwide. The aim of the present study was to evaluate the effect of dried flowers of Woodfordia fruticosa on carbon tetrachloride (CCl4)-induced hepatic fibrosis in rat model. Hepatic fibrosis was induced in male Wistar rats by CCl4 administration (150 µl/100 g rat weight, oral) twice a week for 10 weeks. In preventive model, administration of daily doses of methanolic extract of W. fruticosa (MEWF) at two different doses (100 mg/kg, body weight (b.w.) and 200 mg/kg, b.w.) was started 1 week before the onset of CCl4 administration and continued for 10 weeks. In curative model, MEWF at 100 and 200 mg/kg were given for last 2 weeks after the establishment of fibrosis. MEWF at a dose of 200 mg/kg was able to exert a more pronounced effect as evidenced histologically by significant reduction in fibrotic septa formation in liver tissue, immunohistochemically by abridged expression of collagen III, and also biochemically by serum and tissue antioxidant status, lipid peroxidation, and hydroxyproline level. Liquid chromatography-mass spectrometry analysis revealed the presence of confertin, quercetin methyl ether, ellagic acid, and stigmasterol in MEWF, which could be responsible for its antifibrotic activity. These results indicate the effective protection exerted by MEWF against CCl4-induced hepatic fibrosis in a dose-dependent manner.


Assuntos
Antioxidantes/farmacologia , Flores/química , Cirrose Hepática/tratamento farmacológico , Extratos Vegetais/farmacologia , Woodfordia/química , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Tetracloreto de Carbono/toxicidade , Relação Dose-Resposta a Droga , Imuno-Histoquímica , L-Lactato Desidrogenase/sangue , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Cirrose Hepática/induzido quimicamente , Masculino , Tamanho do Órgão/efeitos dos fármacos , Ratos , Ratos Wistar
12.
Ecotoxicol Environ Saf ; 122: 17-23, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26164724

RESUMO

Population explosion, depletion of water resources and prolonged droughts and floods due to climatic change lead to scarcity of pure and hygienic drinking water in most of the developing countries. Recently nanomaterials attained considerable attention as biosorbent for water purification purpose. However difficulties in removing polymeric surfactants and organic solvents used for nanoproduction and instability of the generated nanoparticles limit the scope of this approach in water cleanup. Here, we describe a novel green method for synthesizing polysaccharide nanoparticles in aqueous medium using honey as the capping agent. The highly stable alginate nanoparticles, characterized by various microscopic and spectroscopic techniques, exhibited a maximum uptake capacity of 333 mg g (-1)of Pb(II) ions from aqueous solution. The effect of various parameters such as initial metal concentration, pH, contact time, temperature and adsorbent dose on sorption process was investigated in batch mode technique. The maximum removal percentage was 94.81 at 45 °C and at pH 4.5 in 60 min contact time. The biosorption followed Freundlich model indicating multilayer adsorption and pseudo second order kinetics. The mechanism involves both surface adsorption and pore diffusion. The positive values of ΔH°, ∆S° and the negative value of ΔG°, confirmed the endothermic nature, randomness and spontaneity of biosorption process.


Assuntos
Alginatos/química , Chumbo/isolamento & purificação , Nanopartículas/química , Poluentes Químicos da Água/isolamento & purificação , Purificação da Água/métodos , Adsorção , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Concentração de Íons de Hidrogênio , Íons , Cinética , Chumbo/química , Soluções , Temperatura , Poluentes Químicos da Água/química
13.
Arch Physiol Biochem ; 128(1): 92-100, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31560224

RESUMO

The current study evaluates the efficacy of methanolic extract of Rotula aquatica Lour. (MERA) against inflammatory changes associated with acute pyelonephritis. The antioxidant enzymes such as SOD, CAT, GPx, GR and oxidative stress markers like GSH content, malondialdehyde (MDA) level, nitrate level, reactive oxygen species (ROS) level and renal toxicity markers were evaluated in this study. The mRNA level expression of Toll-like receptor 4 (TLR-4), nuclear transcription factor kappa B (NF-κB), tumour necrosis factor-alpha (TNF-α), interleukin-6 (IL-6) and Tamm Horsfall protein (THP) were studied by RT-PCR analysis. The oral administration of MERA increases the antioxidant enzyme status in pyelonephritis rat. The elevated levels of oxidative stress markers in pyelonephritic rats were ameliorated by the administration of MERA at 100 mg/kg and 200 mg/kg bwt of the rat. The mRNA level expression of major genes were restored to normal level by MERA.


Assuntos
Boraginaceae/química , Estresse Oxidativo , Extratos Vegetais/farmacologia , Pielonefrite , Animais , Antioxidantes , Inflamação , NF-kappa B/metabolismo , Pielonefrite/tratamento farmacológico , Ratos , Espécies Reativas de Oxigênio
14.
Artigo em Inglês | MEDLINE | ID: mdl-35635500

RESUMO

A series of metal(II) complexes (M=Co (II), Ni(II) and Cu(II)) supported by Schiff base ligand (L=(E)-N'-((6-hydroxybenzo[d]oxazol-5-yl)methylene)isonicotinohydrazide) has been designed and developed from condensation of 6-hydroxybenzo[d]oxazole-5-carbaldehyde and isoniazid. The ligand (H2L) and its metal(II) complexes were structurally characterized utilizing a variety of physicochemical and spectroscopic approaches. The study shows that Schiff bases (H2L) act as monobasic tridentate ONO ligand and conform to octahedral geometry according to the general formula [M(HL)2]. Furthermore, the interaction of these complexes with CT-DNA was investigated at pH = 7.2, utilizing UV-visible absorption, and viscosity measurement. In order to determine the mechanism of binding of the metal(II) complexes to the B-DNA dodecamer, docking studies were conducted using an AutoDock Vina 1.2.0 tool. The photo induced cleavage reveals that the ligand (H2L) and its complexes have UV-visible photo nuclease properties against pUC19 DNA by agarose gel electrophoresis technique. Studies showed that the complexes evaluated firmly bind to CT-DNA via intercalative mode and provides a distinctive pattern of DNA binding.


Assuntos
Complexos de Coordenação , Complexos de Coordenação/química , DNA/química , Isoniazida , Ligantes , Simulação de Acoplamento Molecular , Bases de Schiff/química
15.
Chemosphere ; 298: 134324, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35307393

RESUMO

Nanocellulose fibers are widely acknowledged as a more sustainable alternative to polyimide and polyethylene terephthalate-based plastic films derived from petrochemicals. Cellulose is also utilised in packaging, tissue engineering, electronic, optical, and sensor applications, pharmaceutical applications, cosmetic applications, insulation, water filtration, and hygiene applications, as well as vascular grafts. In the present study to improve the tensile and thermal properties of cellulose nanofibers, polyethylene glycol (PEG 600) with varying concentrations was produced by solvent casting and chemically crosslinked with glutaraldehyde (GA). The effects of various PEG 600 concentrations on nanofibers and the morphology of the resulting nanofibers were investigated. The effects of GA on PEG-nanocellulose morphology, average diameter, tensile strength, elongation, and thermal characteristics were investigated. Strong (GA)-based acetal linkages are used to substitute secondary hydrogen bonds in nanocellulose films. The 1% PEG 600 plasticized nanocellulose scaffolds cross-linked with GA showed a higher tensile modulus (93 MPa) than its GA untreated nanocellulose scaffolds (69 MPa). The Young's modulus of the scaffold is increased up to 83.62 MPa. The crystallinity index values of GA-treated scaffolds were increased, and the mechanical characteristics were greatly improved, according to Fourier transform infrared (FTIR) and XRD analysis on the films. The thermogravimetric analysis (TG/DTG/DSC) of the GA treated plasticized nanocellulose scaffold showed maximum decomposition temperature (Tmax) at 360.01 °C.


Assuntos
Celulose , Polietilenoglicóis , Celulose/química , Glutaral , Raízes de Plantas , Resistência à Tração
16.
Spectrochim Acta A Mol Biomol Spectrosc ; 258: 119843, 2021 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-33933941

RESUMO

Eugenol, a major component in clove has various biological activities. The current study focused to the binding potential of eugenol with Xanthine oxidase (XO) were evaluated using multi spectroscopic techniques and in silico docking studies. Xanthine oxidase, a superoxide generating enzyme, catalyses hypoxanthine and xanthine to uric acid. An excessive uric acid and superoxide anion radical in our body causes many serious clinical complications. The activity and the structural alterations can be a significant method to reduce this kind of risk factors. The results obtained from the fluorescence titration exhibited the interactions initiated by a static quenching mechanism. The ultraviolet (UV), fourier-transform infrared (FTIR), circular dichroism (CD) spectroscopic analysis of eugenol bind with XO indicated the secondary structural alteration in XO. Docking studies showed molecular level interaction of eugenol with the amino acid residues of Thr 1010, Phe 914, Phe 1009, Leu 1014, Phe 1009, Val 1011, Arg 880, Ala 1078, Glu 802, Leu 648and Leu 873 which residing at the catalytic active site of the XO. These results inferred that the eugenol can interact with XO in a remarkable manner and these findings provide a supporting data for the XO inhibition studies to propose a new lead compound.


Assuntos
Eugenol , Xantina Oxidase , Domínio Catalítico , Simulação por Computador , Inibidores Enzimáticos/farmacologia
17.
Int J Biol Macromol ; 154: 888-895, 2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-32209372

RESUMO

Nanosized natural polymers have attained considerable attention in drug delivery applications due to their high encapsulation efficiency, non-toxic nature, sustained and targeted drug delivery. Here we have synthesized Rifampicin loaded alginate nanoparticles by green method. Physicochemical characterization of the nanoparticles was assessed using Transmission electron microscopy, Fourier transform infrared spectroscopy, Dynamic light scattering and X-ray diffraction technique. The swelling and in vitro drug release showed that the framework experiences pH-dependent swelling and release of Rifampicin. Rifampicin has lower release in acid medium and higher release in intestinal condition. Moreover, in view of the drug release results, the release kinetics and transport mechanisms were investigated and discussed. In vitro cytotoxicity assay demonstrated that the nanoparticles were non-toxic in nature. The acute oral toxicity study of the synthesized nanoparticles was done in Wistar albino rats. No systemic toxicity was observed after oral administration of nanoparticles. The present study demonstrated the potential of using alginate nanoparticles synthesized by a green method for drug delivery applications.


Assuntos
Alginatos/química , Portadores de Fármacos/química , Nanopartículas/química , Animais , Linhagem Celular , Liberação Controlada de Fármacos , Feminino , Camundongos , Ratos , Ratos Wistar , Rifampina/administração & dosagem
18.
J Ethnopharmacol ; 261: 113064, 2020 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-32505842

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Muntingia calabura L. is a plant with traditional pharmacological relevance. The various plant parts are used by tribal communities for treating gastric ulcers, prostate gland swellings, headache, cold etc. Hence, an attempt was made to evaluate the anti-colorectal cancer potential of ethyl acetate fraction of M. calabura (EFMC). MATERIALS AND METHODS: HR LC-MS analysis was carried out for the identification of compounds present in EFMC. 1,2 Dimethylhydrazine (DMH) induced animal model was used for the evaluation of anti-CRC potential of EFMC. Antioxidant enzyme status, oxidative stress marker status, hepatic and renal function marker level were determined. Evaluation of mRNA level expression of inflammatory and apoptotic genes, hematological and histopathological examinations were also carried out to figure out the extent of colorectal cancer (CRC) and the beneficial role offered by EFMC. RESULTS: HR LC-MS analysis of EFMC revealed the presence of ten pharmacologically active compounds. EFMC treatment made the altered levels of antioxidant enzymes, oxidative stress markers, liver and renal function markers to retain near to its normal range. The hematological and histopathological evaluations also confirmed the anti-CRC effects exhibited by EFMC. EFMC offered a regulatory control over the inflammatory and apoptotic genes thereby mitigating the damaging effects of CRC. CONCLUSION: The present study depicted the presence of therapeutically active compounds exhibiting strong antioxidant, anti-inflammatory and anticancer potential. The beneficial role offered by these compounds could be responsible for the amelioration of DMH induced CRC. Hence, EFMC can be used as an anti-CRC agent in human subjects.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Proteínas Reguladoras de Apoptose/metabolismo , Apoptose/efeitos dos fármacos , Neoplasias do Colo/tratamento farmacológico , Elaeocarpaceae , Mediadores da Inflamação/metabolismo , 1,2-Dimetilidrazina , Acetatos/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/toxicidade , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/toxicidade , Proteínas Reguladoras de Apoptose/genética , Neoplasias do Colo/induzido quimicamente , Neoplasias do Colo/metabolismo , Neoplasias do Colo/patologia , Modelos Animais de Doenças , Elaeocarpaceae/química , Regulação Neoplásica da Expressão Gênica , Masculino , Estresse Oxidativo/efeitos dos fármacos , Ratos Wistar , Transdução de Sinais , Solventes/química
19.
J Ayurveda Integr Med ; 11(1): 45-52, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-30120055

RESUMO

BACKGROUND: The plant Rotula aquatica Lour. was traditionally well known due to its large number of pharmacological action and medicinal uses. The plant is a necessary component of many Ayurvedic drug preparations since historical times. It is widely used as a crucial ancient drug for kidney and bladder stones. OBJECTIVES: The main objective of the study was to evaluate the acute toxicity and anti inflammatory efficacy of methanolic extract of R.aquatica Lour. in in vivo models. MATERIALS AND METHODS: The qualitative phytochemical analysis and invitro antioxidant activity of the roots of methanolic extract of R.aquatica Lour. (MERA) was evaluated. The acute toxicity effect of MERA was evaluated with two different doses (550, 2000 mg/kg body weight), were administrated orally to Wistar rats. The rats were observed for sign and symptoms of toxicity and mortality for 14 days. The parameters measured including relative organ weight, blood, biochemical and histopathological parameters of hepatic and renal toxicity. The anti-inflammatory effect of MERA was also evaluated in carrageenan and dextran-induced paw edema models. RESULTS: The phytochemical evaluation of MERA shows the presence of secondary metabolites like alkaloids, flavonoids, phenolics and tannins, phytosterols, reducing sugars, proteins and terpenoids. The results of in-vitro antioxidant evaluation of MERA reveal its capability to scavenging free radical at a lower concentration. The MERA did not show any visible signs of toxicity up to the dose of 2000 mg/kg body weight. The results obtained from our carrageenan and dextran-induced paw edema model study also proved the anti-inflammatory effect of MERA in rat model. CONCLUSION: The result shows the potential of MERA as an anti-inflammatory drug to reduce the signs of inflammation devoid of any toxic effect.

20.
Int J Biol Macromol ; 160: 1021-1028, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32504707

RESUMO

In present research, Hevea brasiliensis (Rubber Wood) converted into cellulose by pre-treatment with NaOH (5%) and NaClO2 (5%). In addition, the cellulose was converted to nanocellulose (NC) using ionic liquid, acid hydrolysis and TEMPO oxidation accompanied by ultra-sonication. The prepared nanocellulose characterized by X-ray diffraction (XRD), Scanning Electron Microscopy (SEM), Atomic Force Microscopy (AFM), Fourier transformation infrared spectroscopy (FT-IR). Thermal properties have been studied using thermogravimetric and differential thermal Analysis (TGA/DTA). FT-IR results clearly suggested that the synthetic approaches employed did not alter the principle chemical structure of rubber wood cellulose. SEM and AFM monographs reveal that synthetic approaches affect the morphology/surface topology of prepared nanocellulose. Among the three kinds of NC, NC by TEMPO approach had the largest aspect ratio and superior thermal stability.


Assuntos
Celulose/biossíntese , Celulose/química , Hevea/metabolismo , Celulose/isolamento & purificação , Concentração de Íons de Hidrogênio , Hidrólise , Líquidos Iônicos , Microscopia de Força Atômica , Oxirredução , Espectroscopia de Infravermelho com Transformada de Fourier , Termogravimetria , Difração de Raios X
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