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1.
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
2.
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
3.
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
4.
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
5.
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
6.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-865426

RESUMO

Objective: To evaluate the anti-bacterial and anti-biofilm activity of ethyl acetate fraction of Rotula aquatica Lour. (EFRA) against clinically isolated uropathogenic Escherichia coli. Methods: In vitro antibacterial and anti-biofilm studies were employed. The antimicrobial activity of EFRA was assayed by the well diffusion method. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the active fraction were determined by Resazurin method. The time-kill kinetic assay, acridine orange-ethidium bromide staining, propidium iodide uptake assay, and scanning electron microscopic (SEM) analysis were done to evaluate the efficacy of EFRA in killing uropathogenic Escherichia coli. The anti-biofilm activity was determined by 3-[4,5-dimethyl-2-thiazolyl]-2, 5-diphenyl-2H-tetrazolium-bromide (MTT) assay and specific biofilm formation assay. Results: The well diffusion assay of EFRA showed a very clear zone of inhibition against Escherichia coli BRL-17. The MIC and MBC of EFRA were 2.5 mg/mL and 5 mg/mL, respectively. The time-kill kinetic assay, fluorescence microscopic analysis, propidium iodide uptake assay, and SEM analysis displayed the effect of EFRA in killing the bacteria. The MTT assay and specific biofilm formation assay showed that EFRA prevented the formation of biofilms. Conclusions: The results of the present study confirm that EFRA could prevent bacterial growth and inhibit its biofilm formation.

7.
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.

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