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1.
IET Nanobiotechnol ; 15(4): 391-401, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34694712

RESUMO

Biogenic silica synthesised from rice husk was used as a controlled release system of an eco-friendly biocide consisting of a Justicia adhatoda extract. Fourier-transform infrared spectroscopy (FTIR) indicated the presence of ester bonds between the silica support and the conjugated Justicia adhatoda extract. Surface area analysis and microscopy confirmed a high level of Justicia adhatoda extract loading in the silica support. The phytochemical investigation of Justicia adhatoda was done by Gas chromatography-mass spectrometry (GC-MS) spectroscopy. Moreover, compared with the naked biogenic silica nanoparticles, a better thermal stability was determined for the conjugated system of the extracted compounds. Trial of kinetic release of silica: Justicia adhatoda ∼29% of loaded Justicia adhatoda was released within 1 h and then the rate of release became slow. Net release of Justicia adhatoda was observed up to 50% within 7 h. The Justicia adhatoda compounds released from silica also showed the improved mortality rate against stored product pest rice weevil (Sitophilus oryzae).


Assuntos
Desinfetantes , Justicia, Planta , Nanopartículas , Extratos Vegetais , Folhas de Planta , Dióxido de Silício
2.
Artigo em Inglês | MEDLINE | ID: mdl-34550061

RESUMO

Endophytic actinobacterial strain 3R004T was isolated from a root of Justicia subcoriacea collected in Thailand. In this report, the taxonomic position of this strain is described using a polyphasic approach. Based on the morphological characteristics and chemical composition of its cells, strain 3R004T was identified as a member of the genus Streptomyces. It produced a long chain of cylindrical spores on aerial mycelia. ll-Diaminopimelic acid was detected in the cell wall peptidoglycan. The menaquinones were MK-9(H4), MK-9(H6) and MK-9(H8). C16 : 0, iso-C16 : 0, anteiso-C15 : 0 and iso-C15 : 0 were detected as the major cellular fatty acids. Polar lipids were diphosphatidylglycerol, phosphatidylethanolamine, phosphatidylglycerol, phosphatidylinositol and one unidentified lipid. Strain 3R004T showed the highest 16S rRNA gene similarity of 99.45 % to Streptomyces cyaneochromogenes MK-45T. The phylogenomic results indicated that strain 3R004T was close to Streptomyces aquilus GGCR-6T and Streptomyces antibioticus DSM 40234T. The DNA-DNA hybridization and average nucleotide identity values among strain 3R004T and closely related Streptomyces species were 35.5-63.1 % and 82.7-94.3 %, respectively. The type strain produced actinomycin D antibiotic as the major secondary metabolite. The maximum productivity of the actinomycin D (378 mg l-1) was observed when the strain was grown in 301 broth at 30 °C, 180 r.p.m. for 12 days. On the basis of phenotypic and genotypic evidence, strain 3R004T represents a novel species of the genus Streptomyces, for which the name Streptomyces justiciae is proposed. The type strain is 3R004T (=LMG 32138T=TBRC 13128T=NBRC 115065T).


Assuntos
Justicia, Planta , Streptomyces , Antibacterianos , Técnicas de Tipagem Bacteriana , Composição de Bases , DNA Bacteriano/genética , Ácidos Graxos/química , Fosfolipídeos , Filogenia , RNA Ribossômico 16S/genética , Análise de Sequência de DNA , Streptomyces/genética , Vitamina K 2
3.
Sci Rep ; 11(1): 17187, 2021 08 25.
Artigo em Inglês | MEDLINE | ID: mdl-34433871

RESUMO

Thrombotic diseases seriously threaten human life. Justicia, as a common Chinese medicine, is usually used for anti-inflammatory treatment, and further studies have found that it has an inhibitory effect on platelet aggregation. Therefore, it can be inferred that Justicia can be used as a therapeutic drug for thrombosis. This work aims to reveal the pharmacological mechanism of the anti-thrombotic effect of Justicia through network pharmacology combined with wet experimental verification. During the analysis, 461 compound targets were predicted from various databases and 881 thrombus-related targets were collected. Then, herb-compound-target network and protein-protein interaction network of disease and prediction targets were constructed and cluster analysis was applied to further explore the connection between the targets. In addition, Gene Ontology (GO) and pathway (KEGG) enrichment were used to further determine the association between target proteins and diseases. Finally, the expression of hub target proteins of the core component and the anti-thrombotic effect of Justicia's core compounds were verified by experiments. In conclusion, the core bioactive components, especially justicidin D, can reduce thrombosis by regulating F2, MMP9, CXCL12, MET, RAC1, PDE5A, and ABCB1. The combination of network pharmacology and the experimental research strategies proposed in this paper provides a comprehensive method for systematically exploring the therapeutic mechanism of multi-component medicine.


Assuntos
Dioxolanos/farmacologia , Fibrinolíticos/farmacologia , Redes Reguladoras de Genes , Lignanas/farmacologia , Mapas de Interação de Proteínas , Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo , Animais , Plaquetas/efeitos dos fármacos , Plaquetas/metabolismo , Células Cultivadas , Quimiocina CXCL12/metabolismo , Nucleotídeo Cíclico Fosfodiesterase do Tipo 5/metabolismo , Dioxolanos/química , Descoberta de Drogas/métodos , Fibrinolíticos/química , Humanos , Justicia, Planta/química , Lignanas/química , Masculino , Metaloproteinase 9 da Matriz/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Proteínas Proto-Oncogênicas c-met/metabolismo , Proteínas rac1 de Ligação ao GTP/metabolismo
4.
J Biosci ; 462021.
Artigo em Inglês | MEDLINE | ID: mdl-33969829

RESUMO

Pigment patterns in corollas are common, and act as nectar guides for pollinators. We discovered multiple floral morphs of Justicia adhatoda L. (Acanthaceae) with variable extents of corolla vein pigmentation in a population in Sariska, Rajasthan. Two floral morphs, one completely white and the other white with dark purple vein pigmentation, were compared in order to investigate any possible differences relating to: (a) corolla surface structure, (b) pollinator visitation, (c) reward for the pollinator, and (d) fitness parameters in the morphs. Both morphs showed similar UV reflectance, had distally located conical cells in petals, indicated similar pollinator visitation and had similar nectar content. Contrastingly, seed germination and seed weight were significantly higher in the purple-veined morph, while fruit set and seed set were higher in the white morph which also showed higher amounts of saturated fatty acids in the seeds. The results about aborted seeds differed inconsistently. Thus, variation in corolla pigmentation in J. adhatoda suggests fitness trade-off between the morphs with higher fruit and seed set, but lower seed germination and seed weight in the white morph compared to the purple-veined. We are led to the possibility of different selective pressures acting on the morphs and resulting in adaptive polymorphism.


Assuntos
Adaptação Fisiológica , Flores/anatomia & histologia , Justicia, Planta/anatomia & histologia , Polinização/fisiologia , Característica Quantitativa Herdável , Cor , Flores/genética , Flores/crescimento & desenvolvimento , Flores/metabolismo , Frutas/genética , Frutas/crescimento & desenvolvimento , Frutas/metabolismo , Aptidão Genética , Justicia, Planta/genética , Justicia, Planta/crescimento & desenvolvimento , Justicia, Planta/metabolismo , Fenótipo , Pigmentação/genética , Néctar de Plantas/fisiologia , Reprodução/genética , Sementes/genética , Sementes/crescimento & desenvolvimento , Sementes/metabolismo
5.
Biophys Chem ; 274: 106607, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33957576

RESUMO

Obesity is a global health problem characterized by excessive fat deposition in adipose tissues and can be managed by targeting pancreatic lipase (PL) activity. In the present study, we investigated the in vitro antioxidant and anti-obesity potentials of methanolic leaf extract of Justicia carnea(MEJC) using lipase inhibition kinetics model. In silico evaluations of MEJC bioactive compounds as potential drug-like agents and inhibitors of PL were also investigated using SwissADME prediction tool, semi-empirical quantum mechanics(SQM), molecular electrostatic potential(MEP) and molecular docking analysis. Gas chromatography-mass spectrometry(GC-MS) revealed presence of campesterol, stigmasterol, beta-amyrin etc. MEJC scavenged reactive species and inhibited PL activity via a mixed inhibition pattern (Ki = 107.69 µg/mL; Kii = 398.00 µg/mL) with IC50 > orlistat's IC50. Molecular docking of GC-MS identified compounds with porcine PL showed compounds 8,10,12 and 14 having high PL-binding affinity and similar binding pose with orlistat. Hydrophobic interactions and van der Waals forces were predominantly involved in the ligands' interactions with some key catalytic site amino acid residues (Ser-153,His-264). Compounds 10,12,13 and 14 indicated high drug-likeness, bioavailability, electronegativity, ELUMO-EHOMO energy gaps and MEP. Our findings show that MEJC is a rich natural source of antioxidant and anti-obesity agents which could be optimized for development of new anti-obesity drugs.


Assuntos
Fármacos Antiobesidade/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/antagonistas & inibidores , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Justicia, Planta/química , Cinética , Lipase/metabolismo , Simulação de Acoplamento Molecular , Obesidade/metabolismo , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Teoria Quântica
6.
Respir Res ; 22(1): 99, 2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-33823870

RESUMO

BACKGROUND: COVID-19 pneumonia has been associated with severe acute hypoxia, sepsis-like states, thrombosis and chronic sequelae including persisting hypoxia and fibrosis. The molecular hypoxia response pathway has been associated with such pathologies and our recent observations on anti-hypoxic and anti-inflammatory effects of whole aqueous extract of Adhatoda Vasica (AV) prompted us to explore its effects on relevant preclinical mouse models. METHODS: In this study, we tested the effect of whole aqueous extract of AV, in murine models of bleomycin induced pulmonary fibrosis, Cecum Ligation and Puncture (CLP) induced sepsis, and siRNA induced hypoxia-thrombosis phenotype. The effect on lung of AV treated naïve mice was also studied at transcriptome level. We also determined if the extract may have any effect on SARS-CoV2 replication. RESULTS: Oral administration AV extract attenuates increased airway inflammation, levels of transforming growth factor-ß1 (TGF-ß1), IL-6, HIF-1α and improves the overall survival rates of mice in the models of pulmonary fibrosis and sepsis and rescues the siRNA induced inflammation and associated blood coagulation phenotypes in mice. We observed downregulation of hypoxia, inflammation, TGF-ß1, and angiogenesis genes and upregulation of adaptive immunity-related genes in the lung transcriptome. AV treatment also reduced the viral load in Vero cells infected with SARS-CoV2. CONCLUSION: Our results provide a scientific rationale for this ayurvedic herbal medicine in ameliorating the hypoxia-hyperinflammation features and highlights the repurposing potential of AV in COVID-19-like conditions.


Assuntos
Anti-Inflamatórios/farmacologia , COVID-19/tratamento farmacológico , Reposicionamento de Medicamentos , Hipóxia/tratamento farmacológico , Justicia, Planta , Pulmão/efeitos dos fármacos , Extratos Vegetais/farmacologia , Pneumonia/prevenção & controle , Fibrose Pulmonar/tratamento farmacológico , Sepse/tratamento farmacológico , Animais , Anti-Inflamatórios/isolamento & purificação , Bleomicina , COVID-19/metabolismo , COVID-19/virologia , Ceco/microbiologia , Ceco/cirurgia , Citocinas/genética , Citocinas/metabolismo , Modelos Animais de Doenças , Hipóxia/genética , Hipóxia/metabolismo , Subunidade alfa do Fator 1 Induzível por Hipóxia/genética , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Prolina Dioxigenases do Fator Induzível por Hipóxia/genética , Prolina Dioxigenases do Fator Induzível por Hipóxia/metabolismo , Mediadores da Inflamação/metabolismo , Justicia, Planta/química , Ligadura , Pulmão/metabolismo , Pulmão/microbiologia , Pulmão/patologia , Masculino , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Extratos Vegetais/isolamento & purificação , Pneumonia/genética , Pneumonia/metabolismo , Pneumonia/microbiologia , Fibrose Pulmonar/induzido quimicamente , Fibrose Pulmonar/genética , Fibrose Pulmonar/metabolismo , Interferência de RNA , RNA Interferente Pequeno/genética , RNA Interferente Pequeno/metabolismo , Sepse/genética , Sepse/metabolismo , Sepse/microbiologia , Transcriptoma
7.
J Org Chem ; 86(8): 5568-5583, 2021 04 16.
Artigo em Inglês | MEDLINE | ID: mdl-33818100

RESUMO

Arylnaphthalene lignans (ANLs) were known to have axial chirality due to the biphenyl skeleton with hindered rotation at the single bond. However, the stable ANL atropisomers have not been isolated from nature until the present study. Phytochemical separation of the methanol extract of the stems and barks of Justicia procumbens led to the isolation of 11 ANL glycosides including four pairs of new atropisomers with stable confirmations at room temperature. Their structures were deduced from elucidation of the extensive spectral data, and their absolute configurations were determined by the circular dichroism, electronic circular dichroism, and X-ray methods as well as the total synthesis of one pair of the atropisomers. The ANL compounds were evaluated for their antiviral potential, and it was found that they displayed great antiviral activity discrepancy between a pair of atropisomers due to the geometric orientation. The 1'P-oriented atropisomers showed much more significant antiviral potency than their corresponding 1'M-oriented counterparts. The biological activity discrepancy caused by the axial chirality will not only inspire synthetic design of novel ANL atropisomers to enrich the structural diversity, but also provide important hints to direct the synthetic approaches toward the antiviral drug development of ANL compounds.


Assuntos
Justicia, Planta , Lignanas , Antivirais , Glicosídeos , Estrutura Molecular
8.
J Ayub Med Coll Abbottabad ; 33(1): 3-8, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33774945

RESUMO

Background: Justicia adhatoda is widely used in traditional medicine for treatment of menorrhagia, piles and bleeding disorders. Oral antiplatelet and anticoagulant drugs are routinely prescribed to patients with cardiovascular diseases. These drugs have one major adverse effect that they can cause spontaneous haemorrhage, which can be fatal. Development of a haemostatic agent can help in effective management of drug-induced haemorrhages. This study was devised to observe the effect of leaf extract of Justicia adhatoda on coagulation profile in mice and to evaluate its effect on in-vitro platelet aggregation. Methods: The study was divided into two parts. First part was designed to evaluate the effect of J. adhatoda leaf extract on coagulation parameters. Three drugs were used to induce coagulopathy viz., warfarin, aspirin and dabigatran. Bleeding time, platelet count, PT and APTT were estimated. Second part of this study was devised to observe the effect of J. adhatoda leaf extract on in vitro platelet aggregation of human. Percent aggregation was recorded by light transmission aggregometer for three minutes. Results: Leaf extract of Justicia adhatoda decreased bleeding time from 6.1±2.36 minutes in normal control to 1.9±1.03 minutes in extract treated mice. There was no effect on the coagulation parameters. Platelet count increased significantly only in the aspirin treated group that received the extract to 540±46.8x103 /µl from 436.9±37.9x103 /µl of aspirin treated group. Platelet aggregation in vitro increased in a dose dependent manner. Conclusion: Justicia adhatoda leaf extract is effective in controlling excessive bleeding in vivo, in mice with acquired platelet defect produced by aspirin. This haemostatic effect is probably due to increased platelet aggregation as indicated by the in vitro results.


Assuntos
Transtornos da Coagulação Sanguínea , Hemostáticos/farmacologia , Justicia, Planta , Extratos Vegetais/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Animais , Transtornos da Coagulação Sanguínea/metabolismo , Transtornos da Coagulação Sanguínea/fisiopatologia , Modelos Animais de Doenças , Humanos , Camundongos , Folhas de Planta/química
9.
Edumecentro ; 13(1): 275-282, ene.-mar. 2021. tab
Artigo em Espanhol | LILACS | ID: biblio-1149245

RESUMO

RESUMEN El presente documento propone un modelo de producción crítica-argumentativa para la formación inicial del área de la salud, centrando el proceso de escritura en la participación de los estudiantes como autores y en la redistribución de roles durante el trayecto de producción. El objetivo es mostrar una aproximación a la escritura argumentativa desde cuatro principios propios del marco de la justicia educativa: deliberación, participación, representación autoral y redistribución de roles.


ABSTRACT This document proposes a critical-argumentative production model for initial training in the health area, focusing the writing process on the participation of students as authors and on the redistribution of roles during the production stage. The objective is to show an approach to argumentative writing from four principles of the framework of educational justice: deliberation, participation, author representation and role redistribution.


Assuntos
Redação , Justicia, Planta
10.
Am J Physiol Lung Cell Mol Physiol ; 320(5): L757-L769, 2021 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-33565386

RESUMO

Severe asthma is a chronic airway disease that exhibits poor response to conventional asthma therapies. Growing evidence suggests that elevated hypoxia increases the severity of asthmatic inflammation among patients and in model systems. In this study, we elucidate the therapeutic effects and mechanistic basis of Adhatoda vasica (AV) aqueous extract on mouse models of acute allergic as well as severe asthma subtypes at physiological, histopathological, and molecular levels. Oral administration of AV extract attenuates the increased airway resistance and inflammation in acute allergic asthmatic mice and alleviates the molecular signatures of steroid (dexamethasone) resistance like IL-17A, KC (murine IL-8 homologue), and HIF-1α (hypoxia-inducible factor-1α) in severe asthmatic mice. AV inhibits HIF-1α levels through restoration of expression of its negative regulator-PHD2 (prolyl hydroxylase domain-2). Alleviation of hypoxic response mediated by AV is further confirmed in the acute and severe asthma model. AV reverses cellular hypoxia-induced mitochondrial dysfunction in human bronchial epithelial cells-evident from bioenergetic profiles and morphological analysis of mitochondria. In silico docking of AV constituents reveal higher negative binding affinity for C and O-glycosides for HIF-1α, IL-6, Janus kinase 1/3, TNF-α, and TGF-ß-key players of hypoxia inflammation. This study for the first time provides a molecular basis of action and effect of AV whole extract that is widely used in Ayurveda practice for diverse respiratory ailments. Further, through its effect on hypoxia-induced mitochondrial dysfunction, the study highlights its potential to treat severe steroid-resistant asthma.


Assuntos
Asma/tratamento farmacológico , Hipóxia/complicações , Justicia, Planta/química , Mitocôndrias/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Pneumonia/prevenção & controle , Animais , Asma/etiologia , Asma/metabolismo , Asma/patologia , Modelos Animais de Doenças , Regulação da Expressão Gênica , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Mitocôndrias/metabolismo , Mitocôndrias/patologia , Pneumonia/etiologia , Pneumonia/metabolismo , Pneumonia/patologia
11.
J Photochem Photobiol B ; 216: 112142, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33592357

RESUMO

In the present study, the effects of elevated UV-B (eUVB; ambient ± 7.2 kJ m-2 day-1) were evaluated on the biochemical and metabolic profile of Adhatoda vasica Nees. (an indigenous medicinal plant) at different growth stages. The results showed reduction in superoxide radical production rate, whereas increase in the content of hydrogen peroxide which was also substantiated by the histochemical localization. Malondialdehyde content, which is a measure of oxidative stress, did not show significant changes at any of the growth stages however photosynthetic rate and chlorophyll content showed reduction at all growth stages under eUV-B exposure. Increased activities of the enzymatic and non-enzymatic antioxidants were noticed except ascorbic acid, which was reduced under eUV-B exposure. The metabolic profile of A. vasica revealed 43 major compounds (assigned under different classes) at different growth stages. Triterpenes, phytosterols, unsaturated fatty acids, diterpenes, tocopherols, and alkaloids showed increment, whereas reduction in saturated fatty acids and sesquiterpenes were observed under eUV-B treatment. Vasicinone and vasicoline, the two important alkaloids of A. vasica, showed significant induction under eUV-B exposure as compared to control. Treatment of eUV-B leads to the synthesis of some new compounds, such as oridonin oxide (diterpene) and α-Bisabolol oxide-B (sesquiterpene), which possess potent anti-inflammatory and anticancerous activities. The study displayed that differential crosstalk between antioxidants and secondary metabolites at different growth stages, were responsible for providing protection to A. vasica against eUV-B induced oxidative stress and enhancing its medicinal properties.


Assuntos
Antioxidantes/metabolismo , Justicia, Planta/metabolismo , Metaboloma/efeitos da radiação , Extratos Vegetais/metabolismo , Plantas Medicinais/metabolismo , Antioxidantes/efeitos da radiação , Ácido Ascórbico/metabolismo , Clorofila/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Peróxido de Hidrogênio/metabolismo , Justicia, Planta/efeitos da radiação , Malondialdeído/metabolismo , Estresse Oxidativo/efeitos da radiação , Fitosteróis/metabolismo , Plantas Medicinais/efeitos da radiação , Metabolismo Secundário/efeitos da radiação , Fatores de Tempo , Tocoferóis/metabolismo , Triterpenos/metabolismo , Raios Ultravioleta
12.
J Ethnopharmacol ; 270: 113771, 2021 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-33388427

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Adhatoda vasica Nees is widely used herb of indigenous system to treat various ailments especially upper respiratory tract infections. Not only, anti-tubercular efficacy of crude extract and phytoconstituents of A. vasica has been documented but its hepatoprotective role against various drugs mediated hepatic alterations in different animal models has also been observed. BACKGROUND AND PURPOSE: Isoniazid, rifampicin and pyrazinamide (H-R-Z) are anti-tubercular drugs normally prescribed by health professionals for the treatment of tuberculosis, however along with their medical effectiveness these drugs also exhibit hepatotoxicity among TB patients. Unexpectedly, substantial toxicological data on the metabolism of anti-TB drugs are available but the mystery behind these xenobiotics is too complex and partly implicit. In this study, we further explored the hepatotoxic effects of these xeno-metabolic products and their amelioration by Adhatoda vasica Nees by elucidating its mechanistic action. METHODS: We generated a hepatotoxic rodent model by oral administration of H, R and Z (30.85, 61.7 and 132.65 mg/kg body weight) drugs for 25 days in Wistar rats. Additionally, to achieve hepatoprotection two different doses of Adhatoda vasica Nees ethanolic leaf extract (200 and 300 mg/kg body weight) were used along with H-R-Z dosage, orally and once daily for 25 days and tried to ascertain their mechanistic action. For this, initially phytoconstituents of the extract were evaluated followed by extract standardization using RP-HPLC and FTIR methods. Furthermore, antioxidant activity of the extract was analyzed by DPPH assay. Finally, different treated groups were analyzed for hepatic oxidative stress markers, antioxidant markers, histopathological changes and gene expression study including CYP2E1, CYP7A1, NAT, NR1I2 and UGT1A1 genes involved in phase I and phase II xeno-metabolism. RESULTS: Estimated content of vasicine in RP-HPLC method and free-radical scavenging activity in DPPH assay was found to be 134.519 ± 0.00269µg/10mg of leaf extract and 47.81 µg/mL respectively. In H-R-Z treated group, a significant increase in the levels of thiobarbituric acid, significant reduction in the levels of GSH, and enzymatic markers and marked changes in hepatic histological architecture were observed. In addition, there was significance up-regulation of CYP7A and NAT genes, down-regulation of CYP2E1 gene and insignificant expression levels of NR1I2 and UGT1A1 genes were observed in H-R-Z group. Conversely, high dose of A. vasica extract effectively diminished these alterations by declining oxidative stress and boosting of antioxidant levels. In addition, it acted as bi-functional inducer of both phase I (CYP2E1) and phase II (NAT and UGT1A1) enzyme systems. CONCLUSION: Hence, we concluded that anti-TB drugs exposure has potential to generate reactive metabolites that eventually cause hepatotoxicity by altering oxidant-antioxidant levels and their own metabolism. This study not only emphasized on xeno-metabolism mediated hepatic alterations but also explore the benefit of A. vasica on these toxic insults.


Assuntos
Antituberculosos/efeitos adversos , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Sequestradores de Radicais Livres/farmacologia , Justicia, Planta/química , Extratos Vegetais/farmacologia , Alcaloides/análise , Animais , Antituberculosos/metabolismo , Arilamina N-Acetiltransferase/genética , Doença Hepática Induzida por Substâncias e Drogas/genética , Doença Hepática Induzida por Substâncias e Drogas/patologia , Colesterol 7-alfa-Hidroxilase/genética , Citocromo P-450 CYP2E1/genética , Modelos Animais de Doenças , Feminino , Sequestradores de Radicais Livres/uso terapêutico , Regulação da Expressão Gênica/efeitos dos fármacos , Glucuronosiltransferase/genética , Isoniazida/efeitos adversos , Isoniazida/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Receptor de Pregnano X/genética , Pirazinamida/efeitos adversos , Pirazinamida/metabolismo , Quinazolinas/análise , Ratos Wistar , Rifampina/efeitos adversos , Rifampina/metabolismo
13.
J Ethnopharmacol ; 266: 113454, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-33065254

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Adhatoda vasica Nees., which existed in a large; number of Tibetan medicine prescriptions for hepatopathy, used as an adjuvant to treat liver diseases. HYPOTHESIS/PURPOSE: Oxidative stress is the key player in the development and progression of liver pathogenesis. In recent years, research is increasingly being focused on exploitation of the active components from medicinal plants to combat the liver oxidative injury. In our study, we aimed to screen the active principles from A. vasica and clarify whether they could relieve oxidative damage induced by tert-Butyl hydroperoxide (t-BHP) and its potential mechanism via activating AMPK/p62/Nrf2 pathway. MATERIALS AND METHODS: Ultra performance liquid chromatography (UPLC) was adopted for analysis of chemical composition in the extracts. Furthermore, the antioxidant activity of the fractions was evaluated using DPPH, ABTS and reducing power assay. Along with this, the compounds in this fraction with highest antioxidant activity were analyzed using UPLC-MS. Based on this, the condition for extracting flavonoids of this subfraction was optimized via response surface method. CCK-8 assay was used to detect cell viability. Detection kits were used to measure the activity changes of AST, ALT, LDH and CAT as well as MDA and GSH levels induced by t-BHP. Detection of reactive oxygen species (ROS) production was used DCFH-DA probe. DAPI staining and flow cytometry was used to detect cell apoptosis. In terms of the mechanistic studies, the expression of proteins involved in AMPK/p62/Nrf2 pathway was measured using western blotting. RESULTS: Eventually, 70% ethanol extract from leaf of A. vasica was chosen due to its highest active components compared with other extracts. Further, ethyl acetate fraction derived from 70% ethanol extract in A. vasica (AVEA) possess highest ability for scavenging DPPH and ABTS free radicals as well as strongest reducing power than other fractions. Chemical composition analysis showed that AVEA contained 17 compounds, including 1 quinazoline alkaloid, 12 flavonoid-C-glycosides and 4 flavonoid-O-glycosides. In addition, the conditions (ratio of solid-liquid 1:14, the concentration of ethanol 73%, and the temperature 65 °C) were selected to enrich the flavonoids in AVEA. Furthermore, AVEA could attenuate t-BHP induced hepatocyte damage via increasing the cell viability, restoring abnormal the activities of AST, ALT, LDH and CAT as well as the levels of MDA and GSH. ROS fluorescence intensity was reduced by AVEA. Meanwhile, it could inhibit the cell apoptosis of BRL 3 A cells, as evidenced by restoration of cell morphology and decreasing the number of apoptotic cells. Further mechanistic studies indicated AVEA could promote p-AMPK expression to further induce autophagy adaptor-p62 protein expression, which could autophagic degradation of Keap1, leading to Nrf2 release and translocation into nucleus to induce antioxidant genes (HO-1, NQO-1, GCLC and GCLM) expression. CONCLUSION: In our study, AVEA was first to screen as the active fraction in A. vasica with alkaloids and abundant flavones. Moreover, the fraction potentiates its beneficial aspect by displaying the protective role on relieving t-BHP induced oxidative stress and activating AMPK/p62/Nrf2 pathway. AVEA helps maintain the redox homeostasis of hepatic cells and could be considered as an effective candidate against oxidative stress related liver disorders.


Assuntos
Justicia, Planta/química , Hepatopatias/prevenção & controle , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Proteínas Quinases Ativadas por AMP/metabolismo , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Células Cultivadas , Fator 2 Relacionado a NF-E2/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Ratos , Ratos Endogâmicos BUF , Espécies Reativas de Oxigênio/metabolismo , terc-Butil Hidroperóxido
14.
Nat Prod Res ; 35(20): 3478-3486, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31928366

RESUMO

Three new compounds (1-3), together with six known compounds (4-9), were isolated from the ethyl acetate fraction of ethanol extract of the aerial parts of Justicia gendarussa Burm.f. All of these known compounds were isolated from the plant for the first time. Their structures including absolute configurations were elucidated on the basis of HR-ESI-MS, NMR spectroscopic analyses, single crystal X-ray diffraction and comparison with the literatures. Compounds 1-9 were tested for their antioxidant and anti-inflammatory activities. Compounds 5 and 8 showed the antioxidant activities with IC50 values of 28.61 ± 1.56 and 22.55 ± 1.38 µM, respectively. Compounds 2 and 3 showed anti-inflammatory activity in LPS-induced RAW 264.7 macrophages with the IC50 values of 20.95 ± 1.11 and 16.50 ± 1.04 µM, respectively.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Justicia, Planta , Componentes Aéreos da Planta/química , Anti-Inflamatórios/química , Antioxidantes/química
15.
Biophys Chem ; 269: 106529, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33360111

RESUMO

The present study investigated the antioxidant and invitro antidiabetic capacities of Justicia carnea aqueous leaf extract (JCAE) using α-amylase inhibition model. α-Amylase binding-interaction with JCAE was also investigated using fluorescence spectroscopy and molecular docking. Phytochemical screening and Gas Chromatography-Mass Spectrometry (GC-MS) analysis indicated presence of bioactive compounds. Phenolic (132 mg GAE/g) and flavonoid contents (31.08 mg CE/g) were high. JCAE exhibited high antioxidant capacity and effectively inhibited α-amylase activity (IC50, 671.43 ± 1.88 µg/mL), though lesser than acarbose effect (IC50, 108.91 ± 0.61 µg/mL). α-Amylase intrinsic fluorescence was quenched in the presence of JCAE. Ultraviolet-visible and FT-IR spectroscopies affirmed mild changes in α-amylase conformation. Synchronous fluorescence analysis indicated alterations in the microenvironments of tryptophan residues near α-amylase active site. Molecular docking affirmed non-polar interactions of compounds 6 and 7 in JCAE with Asp-197 and Trp-58 residues of α-amylase, respectively. Overall, JCAE indicated potential to prevent postprandial hyperglycemia by slowing down carbohydrate hydrolysis.


Assuntos
Justicia, Planta/química , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Compostos Fitoquímicos/metabolismo , Conformação Proteica , Espectroscopia de Infravermelho com Transformada de Fourier , alfa-Amilases/química
16.
J Ethnopharmacol ; 268: 113618, 2021 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-33271244

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Justicia pectoralis Jacq. (Acanthaceae), popularly known as tilo, chambá and anador, is widely used in folk medicine in Latin American countries as a sedative, anti-anxiety, reducing menopause symptoms and in the treatment of pathologies of the respiratory tract. Although J. pectoralis is widely used by the female population, there are no studies on the safety of using this species during pregnancy. AIM OF THIS STUDY: To evaluate the effects of prenatal treatment with dry extract from the aerial parts of J. pectoralis on maternal and developmental toxicity in Wistar rats. MATERIAL AND METHODS: Pregnant Wistar rats (n = 10/group) were treated from gestational day (GD) 0-20 with the vehicle (control group) or with the dry extract of J. pectoralis at doses of 300, 600 or 1200 mg/kg. During pregnancy, clinical signs of toxicity, maternal weight, feed and water intake were evaluated. On GD 21, rats were anesthetized and intracardiac blood was collected to evaluate biochemical parameters. During cesarean section, reproductive performance parameters were recorded. The liver, kidneys, uterus and ovaries were removed for histopathological analysis. Fetuses were examined for possible malformations and/or skeletal and visceral variations. RESULTS: Treatment with dry extract of J. pectoralis did not alter weight gain, feed intake or biochemical and maternal reproductive performance parameters There were also no significant histopathological changes in the maternal organs, as well as external, skeletal and visceral malformations in the fetuses. CONCLUSION: Oral administration of J. pectoralis dry extract during pregnancy did not induce maternal toxicity or embryotoxic and teratogenic effects.


Assuntos
Justicia, Planta , Exposição Materna , Extratos Vegetais/farmacologia , Efeitos Tardios da Exposição Pré-Natal , Acanthaceae , Animais , Biomarcadores Farmacológicos/metabolismo , Relação Dose-Resposta a Droga , Feminino , Exposição Materna/efeitos adversos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Gravidez , Efeitos Tardios da Exposição Pré-Natal/induzido quimicamente , Efeitos Tardios da Exposição Pré-Natal/metabolismo , Ratos , Ratos Wistar
17.
Int J Food Microbiol ; 338: 109019, 2021 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-33310341

RESUMO

In this work, the antibacterial activity of a crude extract of the endophytic fungus Flavodon flavus (JB257), isolated from leaves of Justicia brandegeana, was evaluated against both the vegetative and sporulated forms of Alicyclobacillus acidoterrestris. The microdilution technique was performed in order to determine the antibacterial activity of the crude extract alone as well as in combination with the bacteriocin, nisin. The minimum inhibitory concentration (MIC) of the crude extract and nisin alone against A. acidoterrestris vegetative forms were 250 µg/mL and 31.5 µg/mL, respectively, while the minimum bactericidal concentrations (MBC) were 1000 µg/mL and 62.5 µg/mL,respectively. For A. acidoterrestris spores, treatment with the crude extract at a concentration of 500 µg/mL caused a 47% reduction in growth, while nisin at 62.5 µg/mL could reduce 100% of the growth. The in vitro evaluation of the crude extract combined with nisin against A. acidoterrestris by the Checkerboard method showed a synergistic interaction between the two compounds. In addition, greater selectivity towards bacterial cells over host cells, a human hepatocyte cell line, was achieved when the crude extract was combined with nisin, Using scanning electron microscopy, interferences in the cell membrane of A. acidoterrestris could be observed after treatment with the crude extract. The results presented in this study indicate that the crude extract of the endophyte F. flavus has biotechnological potential in the food industry, especially for the treatment of orange juices through the control of A. acidoterrestris.


Assuntos
Alicyclobacillus/efeitos dos fármacos , Citrus sinensis/microbiologia , Microbiologia de Alimentos/métodos , Sucos de Frutas e Vegetais/microbiologia , Justicia, Planta/química , Justicia, Planta/microbiologia , Polyporales/química , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana , Nisina/farmacologia
18.
Nat Prod Res ; 35(11): 1847-1851, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31282754

RESUMO

Justicia spicigera Schltdl. (Acanthaceae) is used for treatment of gastrointestinal illnesses therapy in traditional medicine. The objective of this study was to give evidence of the antinociceptive and spasmolytic effects of the J. spicigera ethanol extract (JS EtOH) using in in vivo and/or in vitro assays. The JS EtOH exerted regulatory effect on the motility and a partial relaxing response on the intestinal tissue. Furthermore, a significant abdominal antinociceptive response was obtained in mice, which was totally abolished in the presence of 5-HT1A receptor antagonist (WAY100635, 0.1 mg/kg, s.c.) and partially by blocking opioid receptors (NX, 1 mg/kg, i.p.), whereas the inhibition of the NO synthesis (L-NAME, 30 mg/kg, i.p.) facilitated antinociception of this extract. Kaempferitrin was isolated and identified as major secondary metabolite. These results support the analgesic and spasmolytic-like activity of J. spicigera aerial parts involving inhibitory neurotransmission reinforcing the potential of this medicinal plant for alleviating pain.


Assuntos
Trato Gastrointestinal/efeitos dos fármacos , Justicia, Planta/química , Extratos Vegetais/farmacologia , Analgésicos/farmacologia , Animais , Modelos Animais de Doenças , Etanol , Flavonoides/farmacologia , Cobaias , Masculino , Camundongos , Óxido Nítrico/metabolismo , Nociceptividade/efeitos dos fármacos , Dor/tratamento farmacológico , Extratos Vegetais/uso terapêutico
19.
Nat Prod Res ; 35(21): 4032-4040, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32347116

RESUMO

Three novel 14-membered cyclopeptide alkaloids, justicianenes B-D (1-3), were isolated from the EtOH extract of the whole plant of Justicia procumbens L., and their structures were determined on the basis of detailed NMR spectroscopic data and the absolute stereochemistry of the ring-bonded α-amino acids in the cyclopeptide alkaloids were determined by ECD spectra. The isolated compounds were evaluated for their in vitro cytotoxicity against human cancer cell lines, including brest cancer MCF-7, cervix carcinoma HeLa, lung cancer A549 and H460, and diphyllin (14) showed moderate cytotoxicity against the HeLa, A549 and H460 cells with IC50 of 9.13, 23.12, 42.34 µM, respectively, justicianene D showed weak cytotoxicity against the MCF-7 cell with inhibition rate of 50% at the concentration of 90 µM.


Assuntos
Alcaloides , Antineoplásicos Fitogênicos/farmacologia , Justicia, Planta , Peptídeos Cíclicos , Alcaloides/farmacologia , Humanos , Justicia, Planta/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Peptídeos Cíclicos/farmacologia
20.
Rev. ANACEM (Impresa) ; 15(1): 8-12, 2021. tab, graf
Artigo em Espanhol | LILACS | ID: biblio-1248004

RESUMO

Actualmente el cáncer es la segunda causa de muerte en la población chilena; sin embargo, en algunas regiones del país como Arica y Parinacota, Antofagasta, La Serena, Los Lagos y Aysén, en Atacama y La Araucanía ya es la primera (1), inmediatamente apenas por debajo de las afecciones al sistema circulatorio y cardiovascular, y se espera que, al final de la próxima década, llegue a ser la primera causa de muerte en el país (2). Por otra parte, con respecto a los años de vida perdidos en Chile, el cáncer es la primera causa de años de vida perdidos por muerte prematura (175.741 años equivalentes al 22,5% del total de años). Si a lo anterior sumamos los años de vida perdidos por discapacidad, el cáncer es responsable de 221.529 AVISA (Años de vida ajustados por discapacidad), ubicándolo en el séptimo lugar de grupos de causas de carga de enfermedad.(3) Por su incidencia, el cáncer se ha constituido en un problema de salud pública indiscutible e insoslayable, por cuya gravedad demanda al sistema de salud chileno la máxima atención y el mejor de los esfuerzos en las tareas de las pesquisas temprana en toda la población, con el fin de minimizarsusefectos combinados enlasociedad demanera transversal y en cualquier contexto en el que ocurra, debido a la dificultad que significa para el sistema de salud chileno su pesquisa temprana en todos los ciudadanos, sumado a la escasez de recursos tanto humanos como materiales, por lo costos involucrados en su abordaje, es un importante problema social y económico, con repercusión y costos que afectan a laspersonas, sus familiasy comunidades, así como al sistema de salud y al país en su conjunto. (2) A la fecha, en Chile, grandes esfuerzos se han hecho para reducir estas brechas. El mayor de ellos es el programa GES (Garantías explícitas enSalud), mediante el cual los pacientes de acuerdo a su diagnóstico e independientemente de su capacidad de pago o seguro de salud asociado, región geográfica o nivel educacional, son asegurados con una canasta de prestaciones estandarizada, con tiempos de atención antes definidos, asegurando así acceso, oportunidad, protección financiera y calidad delprestador. (4) No obstante luego de 15 años de iniciado elprograma de prestaciones GES, persisten estas diferencias tanto por nivel socioeconómico, y/o educacional, queinfluyen negativamente sobre los estándares de atención de los diferentes prestadores de salud, en razón que diversos estudios se han observado diferencias estadisticamente significativas en las tasas de mortalidad entre el sistema público y privado de 3,12 a 5,8 veces más mortalidad en los pacientes atendidos por FONASA (Fondo nacional de Salud) , respecto a los prestadores privados provenientes de ISAPRES (Instituciones de salud previsional). (5) La ley Nacional del Cáncer recibe el nombre del doctor Claudio Mora a modo de homenaje póstumo, pues él encarnó la dualidad de paciente oncológico y profesional al ser tratado por un cáncer de páncreas, junto al Dr. Jorge Jiménez de la Jara, y la senadora Carolina Goic, quienes fueron grandes impulsores de esta ley, que cuenta con $80 mil millones de pesos anuales ($20 mil millones para infraestructura y $60 mil millones para tratamientos que hoy no son cubiertos por el GES ni por la Ley Ricarte Soto), además de $200 millones anuales por ocho años para la construcción de la Red Nacional Oncológica.(6) La ley nacional del cáncer es un proyecto a largo plazo que requiere de una red oncológica integrada de profesionales y de la coordinación de un equipo interdisciplinario que presenta deficiencias tanto en el número como en la especializaciónde sus equipos médicos. En el presente contexto de la pandemia por coronavirus iniciada en Chile el 1 de marzo de 2020, contrapuesto a lo anterior la disminución de los diagnósticos de cáncer es un hecho, como consecuencia directa de la priorización de camas crítica como camas básicas y de intermedio para atender pacientes infectados por coronavirus, a pesar de lo anterior ha entrado en vigencia la Ley Nacional de Cáncer, es decir, la nueva Ley 21.258, que pretende asegurar que se proporcione un óptimo diagnóstico, tratamiento y seguimiento a los pacientes. (7)


Assuntos
Política Pública , Programas Médicos Regionais , Legislação Médica , Neoplasias/mortalidade , Chile , Justicia, Planta , Equidade , COVID-19 , Oncologia
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