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1.
Chemosphere ; 263: 127922, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32841875

RESUMO

Anaerobic process has been widely applied as a cost-effective method for textile wastewater treatment. However, many bacteria exhibit low metabolic activity in unfavorable conditions due to the entry into a viable but non-culturable (VBNC) state. Thus, in this study, a novel method of using resuscitation-promoting factors (Rpfs), which has been proven to resuscitate and stimulate the growth of VBNC bacteria, is explored to enhance the degradation of the anthraquinone dye reactive blue 19 (RB19) in the anaerobic process. The results show that Rpfs could efficiently prompt RB19 decolorization. Compared to the conventional anaerobic condition, RB19 decolorization efficiency was increased by more than 20% with the Rpf addition. UV-visible spectral and gas chromatograph-mass spectrometry analysis indicate that the aromatic amines structures of RB19 was cleaved. More importantly, the Rpf addition appeared to stimulate and/or enrich some dye-degrading species of the family Peptostreptococcaceae, thus leading to a higher RB19 decolorization efficiency.


Assuntos
Antraquinonas/metabolismo , Biodegradação Ambiental , Anaerobiose , Antraquinonas/química , Bactérias/metabolismo , Corantes/metabolismo , Têxteis
2.
Nat Commun ; 11(1): 5875, 2020 11 18.
Artigo em Inglês | MEDLINE | ID: mdl-33208749

RESUMO

Senna tora is a widely used medicinal plant. Its health benefits have been attributed to the large quantity of anthraquinones, but how they are made in plants remains a mystery. To identify the genes responsible for plant anthraquinone biosynthesis, we reveal the genome sequence of S. tora at the chromosome level with 526 Mb (96%) assembled into 13 chromosomes. Comparison among related plant species shows that a chalcone synthase-like (CHS-L) gene family has lineage-specifically and rapidly expanded in S. tora. Combining genomics, transcriptomics, metabolomics, and biochemistry, we identify a CHS-L gene contributing to the biosynthesis of anthraquinones. The S. tora reference genome will accelerate the discovery of biologically active anthraquinone biosynthesis pathways in medicinal plants.


Assuntos
Antraquinonas/metabolismo , Genoma de Planta , Proteínas de Plantas/genética , Senna (Planta)/metabolismo , Antraquinonas/química , Vias Biossintéticas , Cromossomos de Plantas/genética , Cromossomos de Plantas/metabolismo , Proteínas de Plantas/metabolismo , Senna (Planta)/química , Senna (Planta)/genética
3.
Sci Rep ; 10(1): 17699, 2020 10 19.
Artigo em Inglês | MEDLINE | ID: mdl-33077836

RESUMO

Angiotensin converting enzyme 2 (ACE2) (EC:3.4.17.23) is a transmembrane protein which is considered as a receptor for spike protein binding of novel coronavirus (SARS-CoV2). Since no specific medication is available to treat COVID-19, designing of new drug is important and essential. In this regard, in silico method plays an important role, as it is rapid and cost effective compared to the trial and error methods using experimental studies. Natural products are safe and easily available to treat coronavirus affected patients, in the present alarming situation. In this paper five phytochemicals, which belong to flavonoid and anthraquinone subclass, have been selected as small molecules in molecular docking study of spike protein of SARS-CoV2 with its human receptor ACE2 molecule. Their molecular binding sites on spike protein bound structure with its receptor have been analyzed. From this analysis, hesperidin, emodin and chrysin are selected as competent natural products from both Indian and Chinese medicinal plants, to treat COVID-19. Among them, the phytochemical hesperidin can bind with ACE2 protein and bound structure of ACE2 protein and spike protein of SARS-CoV2 noncompetitively. The binding sites of ACE2 protein for spike protein and hesperidin, are located in different parts of ACE2 protein. Ligand spike protein causes conformational change in three-dimensional structure of protein ACE2, which is confirmed by molecular docking and molecular dynamics studies. This compound modulates the binding energy of bound structure of ACE2 and spike protein. This result indicates that due to presence of hesperidin, the bound structure of ACE2 and spike protein fragment becomes unstable. As a result, this natural product can impart antiviral activity in SARS CoV2 infection. The antiviral activity of these five natural compounds are further experimentally validated with QSAR study.


Assuntos
Betacoronavirus/metabolismo , Peptidil Dipeptidase A/metabolismo , Glicoproteína da Espícula de Coronavírus/metabolismo , Regulação Alostérica , Sequência de Aminoácidos , Antraquinonas/química , Antraquinonas/metabolismo , Betacoronavirus/isolamento & purificação , Sítios de Ligação , Infecções por Coronavirus/patologia , Infecções por Coronavirus/virologia , Emodina/química , Emodina/metabolismo , Humanos , Simulação de Acoplamento Molecular , Pandemias , Peptidil Dipeptidase A/química , Pneumonia Viral/patologia , Pneumonia Viral/virologia , Ligação Proteica , Estrutura Secundária de Proteína , Estrutura Terciária de Proteína , Glicoproteína da Espícula de Coronavírus/química
4.
Chemosphere ; 261: 128201, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33113663

RESUMO

In this work, Ti/SnO2-RuO2 dimensionally stable anode has been successfully fabricated via thermal decomposition method and further used for highly efficient electrocatalytic degradation of alizarin cyanin green (ACG) dye wastewater. The morphology, crystal structure and composition of Ti/SnO2-RuO2 electrode are characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD) and X-ray fluorescence spectroscopy (XRF), respectively. The result of accelerated life test suggests that as-prepared Ti/SnO2-RuO2 anode exhibits excellent electrochemical stability. Some parameters, such as reaction temperature, initial pH, electrode spacing and current density, have been investigated in detail to optimize the degradation condition of ACG. The results show that the decolorization efficiency and chemical oxygen demand removal efficiency of ACG reach up to 80.4% and 51.3% after only 40 min, respectively, under the optimal condition (reaction temperature 25 °C, pH 5, electrode spacing 1.0 cm and current density 3 mA cm-2). Furthermore, the kinetics analysis reveals that the process of electrocatalytic degradation of ACG follows the law of quasi-first-order kinetics. The excellent electrochemical activity demonstrates that the Ti/SnO2-RuO2 electrode presents a favorable application prospect in the electrochemical treatment of anthraquinone dye wastewater.


Assuntos
Antraquinonas/química , Carbocianinas/química , Eletrodos , Eliminação de Resíduos Líquidos/instrumentação , Análise da Demanda Biológica de Oxigênio , Corantes/química , Concentração de Íons de Hidrogênio , Microscopia Eletrônica de Varredura , Oxirredução , Compostos de Rutênio/química , Espectrometria por Raios X , Temperatura , Compostos de Estanho/química , Titânio/química , Eliminação de Resíduos Líquidos/métodos , Águas Residuárias/química , Poluentes Químicos da Água/química , Difração de Raios X
5.
Ecotoxicol Environ Saf ; 201: 110858, 2020 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-32563161

RESUMO

This work presents the research on the treatment of an anthraquinone derivatives of disperse dye Blue SI from aqueous solution using aluminium for the optimization of operational parameters like pH, current density, addition of electrolyte, contact time for the color removal efficiency (CRE) and the results are compared with the performance of copper electrodes in electrocoagulation (EC). The parameters for maximum CRE was found with Al at current density 40 Am-2, time 10 min at pH 7, and for Cu at 60 Am-2 15 min, at pH 6 were optimized. The characterization of the treated water using HPLC, MS studies revealed intermediate compounds. From the XPS analysis of the sludge obtained, the mechanism of EC was deduced. Treated aqueous solution was studied for its phytotoxicity with Vigna radiata and ecotoxicity studies were conducted on Artemia salina to study the toxicity effect of the intermediatory products in the treated dye solution. Blue SI dye aqueous solution treated with aluminium electrodes shows no or lesser toxicity in plants as well as in ecotoxic study compared with copper electrodes.


Assuntos
Alumínio/química , Antraquinonas/análise , Cobre/química , Técnicas Eletroquímicas/métodos , Poluentes Químicos da Água/análise , Purificação da Água/métodos , Animais , Antraquinonas/química , Antraquinonas/toxicidade , Artemia/efeitos dos fármacos , Eletrodos , Floculação , Concentração de Íons de Hidrogênio , Esgotos/química , Vigna/efeitos dos fármacos , Águas Residuárias/química , Poluentes Químicos da Água/química , Poluentes Químicos da Água/toxicidade
6.
Br J Radiol ; 93(1111): 20200034, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32374626

RESUMO

Necrosis plays vital roles in living organisms which is related closely with various diseases. Non-invasively necrotic imaging can be of great values in clinical decision-making, evaluation of individualized treatment responses, and prediction of patient prognosis. This narrative review will demonstrate how the evolution of quinones for necrotic imaging has been promoted by searching for their active centers. In this review, we summarized the recent developments of various quinones with the continuous simplified π-conjugated cores in necrotic imaging and speculated their possible molecular mechanisms might be attributed to their intercalations with exposed DNA in necrotic tissues. We discussed their clinical challenges of necrotic imaging with quinones and their future translation studies deserved to be explored in personalized patient treatment.


Assuntos
Sondas Moleculares , Infarto do Miocárdio/patologia , Necrose/diagnóstico por imagem , Quinonas , Animais , Antraquinonas/química , Células/patologia , DNA/análise , Humanos , Sondas Moleculares/química , Infarto do Miocárdio/diagnóstico por imagem , Naftoquinonas/química , Quinonas/química , Quinonas/classificação , Ratos
7.
J Colloid Interface Sci ; 573: 21-30, 2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32268260

RESUMO

The treatment of organic pigments has gained significant attention worldwide owing to the large amounts of pollutants emitted during the process. The main purpose of this study is to prepare an environmentally friendly, low-cost adsorbent with high efficiency with selective adsorption for water purification. An inorganically modified mesoporous biochar derived from sorghum straw was synthesized in one step, and three typical organic pigments including methyl blue (MB), acid orange 7 (AO7), and alizarin red (AR) were selected as cationic, azo, and anionic pigments, respectively. The characterization results demonstrated that Fe3O4 particles successfully attached to the surface of biochar after modification. Although the enhanced adsorption behaviors of the three pigments on the modified biochar were described effectively by the Langmuir isotherm, the as-prepared materials showed a better selective adsorption effect on the cationic pigments. Moreover, the adsorption processes of all targeted pigments were endothermic and governed by entropy. Smaller molecular dimensions, lighter molecular weight, and the low molecular electrostatic potential of MB are responsible for its selective adsorption; however, the enhanced adsorption affinity is attributed to the hydrogen bond and n-π interaction with the benzene ring of the pigment molecules.


Assuntos
Antraquinonas/química , Compostos Azo/química , Benzenossulfonatos/química , Corantes/química , Compostos Férricos/química , Adsorção , Estrutura Molecular , Tamanho da Partícula , Porosidade , Propriedades de Superfície
8.
Photochem Photobiol Sci ; 19(4): 485-494, 2020 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-32232258

RESUMO

The extensive and repetitive use of antifungal drugs has led to the development of drug-resistant Candida albicans. Antimicrobial photodynamic therapy (aPDT) has received considerable attention as an emerging and promising approach to combat drug-resistant microbes. This study evaluated the photodynamic effects mediated by aloe emodin (AE), a natural compound isolated from Aloe vera and Rheum palmatum, on azole-sensitive and azole-resistant C. albicans in vitro. AE exhibited no significant dark toxicity, but in the presence of light, effectively inactivated C. albicans cells in a concentration-dependent manner. The uptake of AE by fungal cells was investigated by confocal laser scanning microscopy (CLSM), and the results showed that AE possessed stronger ability to enter into C. albicans cells following light irradiation. Transmission electron microscopy analysis suggested that AE-mediated aPDT could induce damage to the cell wall, cytoplasm, and nucleus. Damage to the surface of C. albicans was observed by scanning electron microscopy. These results suggest that AE is a potential PS for use in aPDT of drug-resistant C. albicans strains, and AE-mediated aPDT shows promise as an antifungal treatment.


Assuntos
Antraquinonas/farmacologia , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Farmacorresistência Fúngica/efeitos dos fármacos , Fármacos Fotossensibilizantes/farmacologia , Antraquinonas/química , Antifúngicos/química , Candida albicans/citologia , Luz , Testes de Sensibilidade Microbiana , Estrutura Molecular , Fármacos Fotossensibilizantes/química , Fototerapia
9.
Mater Sci Eng C Mater Biol Appl ; 109: 110621, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32228903

RESUMO

The current study explores the facile fabrication of multilayer self-assembled electrostatic oil-in-water Pickering emulsions (PEs) using quaternized nanocellulose (Q-NC) and diosgenin-conjugate alginate (DGN-ALG) particles as stabilizers to form hydrocolloid nanocarriers. The conditions of formulation such as storage time, pH, temperature and salt effect on the emulsion stability were evaluated. The results deduced showed good emulsion droplet stability over a period of 30 days. Morphological analysis revealed the hydrodynamic sizes of the PE droplets to be spherically shaped with an average diameter of 150 ± 3.51 nm. Creaming index, wettability and critical aggregation concentrations (CAC) as well as chemical characterization of the PEs were examined. In vitro release kinetics of encapsulated quinalizarin as a model drug was investigated with a determined cumulative drug release (CDR) of 89 ± 1.21% in simulated pH blood medium of pH 7.4. In addition, cellular internalization of the PEs was studied via confocal microscopy imaging and showed high cellular uptake. Also, evaluated in vitro cytotoxicity by MTT assay demonstrated excellent anticancer activity in human lung (A549) and breast (MCF-7) cancer cell lines.


Assuntos
Alginatos , Antraquinonas , Neoplasias da Mama/tratamento farmacológico , Celulose , Diosgenina , Sistemas de Liberação de Medicamentos , Neoplasias Pulmonares/tratamento farmacológico , Células A549 , Alginatos/química , Alginatos/farmacocinética , Alginatos/farmacologia , Antraquinonas/química , Antraquinonas/farmacocinética , Antraquinonas/farmacologia , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Celulose/química , Celulose/farmacocinética , Celulose/farmacologia , Diosgenina/química , Diosgenina/farmacocinética , Diosgenina/farmacologia , Feminino , Humanos , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patologia , Células MCF-7
10.
Carbohydr Res ; 490: 107958, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32120022

RESUMO

Rhein is a potential antitumor agent, but the poor water-solubility restricts its clinical applicability. ß-cyclodextrin-drug conjugates provide a possibility to improve the water-solubility of rhein and thereby enhance its bioavailability. A novel ß-cyclodextrin-rhein conjugate (ß-CD-RH) was synthesized by covalently link ß-cyclodextrin with rhein through a 1,8-diamino-3,6-dioxaoctane linker. The structure of ß-CD-RH was characterized by 1H NMR, FT-IR, Maldi-tof MS etc. The inclusion style of ß-CD-RH in water was detected by 2D NMR. The 2D ROESY spectrum provided details of the rhein moiety encapsulated in the ß-CD cavity. The water-solubility of ß-CD-RH is up to 3.24 µmol/mL ß-CD-RH exhibited higher cytotoxicity than rhein and rhein/ß-CD mixture against Hela cells. Our work provides a new way for the preparation of novel ß-CD-drug conjugate.


Assuntos
Antraquinonas/farmacologia , Antineoplásicos/farmacologia , beta-Ciclodextrinas/química , Antraquinonas/química , Antineoplásicos/química , Disponibilidade Biológica , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células HeLa , Humanos , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Água/química
11.
Anal Chim Acta ; 1106: 96-102, 2020 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-32145860

RESUMO

Peroxynitrite (ONOO-) plays a crucial role in the regulation of diverse pathophysiological processes, and high level of ONOO- is profound association with numerous diseases. Herein, we developed an anthraquinone-based fluorescent probe L for ONOO- determination by a new recognition mechanism: amido oxidized nitroso-group by ONOO-. Probe L with amine-based recognition receptor is more selective to ONOO- than other reactive oxygen species, including H2O2 and ClO-. Furthermore, ONOO- could be rapidly detected by probe L with a Limit of Detection of 13 nM. More importantly, L could be used to monitor intracellular ONOO- in SMMC-7721 cells.


Assuntos
Antraquinonas/química , Corantes Fluorescentes/química , Ácido Peroxinitroso/análise , Linhagem Celular Tumoral , Teoria da Densidade Funcional , Humanos , Estrutura Molecular , Imagem Óptica , Tamanho da Partícula , Propriedades de Superfície
12.
Mar Drugs ; 18(2)2020 Feb 18.
Artigo em Inglês | MEDLINE | ID: mdl-32085561

RESUMO

Chemical profiling of the Streptomyces sp. strain SUD119, which was isolated from a marine sediment sample collected from a volcanic island in Korea, led to the discovery of three new metabolites: donghaecyclinones A-C (1-3). The structures of 1-3 were found to be rearranged, multicyclic, angucyclinone-class compounds according to nuclear magnetic resonance (NMR) and mass spectrometry (MS) analyses. The configurations of their stereogenic centers were successfully assigned using a combination of quantum mechanics-based computational methods for calculating the NMR shielding tensor (DP4 and CP3) as well as electronic circular dichroism (ECD) along with a modified version of Mosher's method. Donghaecyclinones A-C (1-3) displayed cytotoxicity against diverse human cancer cell lines (IC50: 6.7-9.6 µM for 3).


Assuntos
Antraquinonas/química , Antraquinonas/farmacologia , Sedimentos Geológicos/microbiologia , Streptomyces/química , Antraquinonas/isolamento & purificação , Antibacterianos , Antifúngicos , Antineoplásicos , Dicroísmo Circular , Humanos , Ilhas , Estrutura Molecular , República da Coreia
13.
Fish Shellfish Immunol ; 99: 331-341, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32084536

RESUMO

The present study was investigated the dietary administration of cassic acid (CA) on growth, innate immunity, transcription profiles of estrogen and follicle-stimulating hormones as well as lysozyme enzyme determined in Clarias gariepinus against Edwardsiella tarda. The weight gain (WG), protein efficacy ratio (PER), and feed conversion ratio (FCR) were significantly improved in infected fish fed dietary administration with CA at 5 and 10 mg kg-1 diets. The survival is higher (96.7% and 98.3%) in the infected groups fed at 5 and 10 mg kg-1 CA diets. The red (RBC) and white (WBC) blood cells, hemoglobin (Hb), and packed cell volume (PCV) was found significantly high in the infected fish feeding at 5 and 10 mg kg-1 CA diets. Total protein and albumin were significantly increased with 5 and 10 mg kg-1 CA diets among weeks 1-4 while the globulin and albumin: globulin ratio increased of these diet only after week 2. The phagocytic and respiratory burst activities were enhanced statistically the infected fish fed at 10 mg kg-1 CA diet group whereas the production of superoxide anion (SOA) and nitric oxide (NO) were significantly increased at 5 and 10 mg kg-1 CA diets. The lymphocyte proliferation and myeloperoxidase (MPO) activity were significantly high the infected fish when fed at 5 and 10 mg kg-1 CA diets after 2nd week whereas the alternate complement activity (ACP), generation of reactive oxygen species (ROS), and lysozyme activity (Lyz) were observed at 5 and 10 mg kg-1 CA diets among weeks 1-4. The accumulative mortality was 10% in infected fish fed at 1 and 5 mg kg-1 CA diets whereas 15% mortality found with 10 mg kg-1 CA diet. The highest levels of estrogen receptor alpha (ERα) mRNA expression found in gonad while the highest levels of follicle stimulating hormone-beta subunit (FSH-ß) mRNA expression found in testis of the infected fish given at 5 and 10 mg kg-1 CA diets. The up-regulation of chick-type lysozyme (c-Lyz) mRNA was observed at 5 and 10 mg kg-1 CA diets after 2nd week while goose-type lysozyme (g-Lyz) mRNA was up-regulation amongst weeks 1-4 of these diets. The present study suggested that E. tarda challenged fish after feeding with 5 and 10 mg kg-1 CA diets did not affect growth and hemato-biochemical parameter, but it enhanced nonspecific immune system and improving ERα, FSH-ß, c-Lyz, and g-Lyz mRNA expression in C. gariepinus against E. tarda.


Assuntos
Antraquinonas/farmacologia , Peixes-Gato , Edwardsiella tarda , Infecções por Enterobacteriaceae/veterinária , Doenças dos Peixes/prevenção & controle , Ração Animal/análise , Fenômenos Fisiológicos da Nutrição Animal , Animais , Antraquinonas/química , Clonagem Molecular , Dieta/veterinária , Suplementos Nutricionais , Infecções por Enterobacteriaceae/microbiologia , Inibidores Enzimáticos , Doenças dos Peixes/imunologia , Doenças dos Peixes/microbiologia , Regulação da Expressão Gênica/efeitos dos fármacos
14.
Chem Commun (Camb) ; 56(22): 3337-3340, 2020 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-32090214

RESUMO

Herein, we report the chemoenzymatic synthesis of a heterodimeric (-)-rugulosin B, homodimeric (-)-rugulosin C, and several rugulin analogues in three to four steps starting from anthraquinones. This work supports dimerization between variously substituted putative monomeric intermediates during the biosynthesis of naturally occurring (+)-rugulosin B and C.


Assuntos
Antraquinonas/síntese química , Naftoquinonas/química , Oxirredutases/metabolismo , Antraquinonas/química , Antraquinonas/metabolismo , Biomimética , Complexos de Coordenação/química , Reação de Cicloadição , Proteínas Fúngicas/genética , Proteínas Fúngicas/metabolismo , Chumbo/química , Naftoquinonas/síntese química , Naftoquinonas/metabolismo , Oxirredução , Oxirredutases/genética , Talaromyces/enzimologia
15.
Dalton Trans ; 49(5): 1613-1619, 2020 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-31942585

RESUMO

We herein designed two new PtIV prodrugs of oxoplatin (cis,cis,cis-[PtCl2(NH3)2(OH)2]), [PtIVCl2(NH3)2(O2C-FA)2] (Pt-2) and [PtIVCl2(NH3)2(O2C-RH)2] (Pt-3), by conjugating with ferulic acid (FA-COOH) and rhein (RH-COOH) which have well-known biological activities. Three other Pt(iv) complexes of [PtIVCl2(NH3)2(O2C-BA)2] (Pt-1), [PtIVCl2(NH3)2(O2C-CA)2] (Pt-4) and [PtIVCl2(NH3)2(O2C-TCA)2] (Pt-5) (where BA-COOH = benzoic acid, CA-COOH = crotonic acid and TCA-COOH = trans-cinnamic acid) were also prepared for the comparative study. Like most PtIV prodrug complexes, the cytotoxicity of Pt-3 containing the biologically active rhein (RH-COOH) ligand against lung carcinoma (A549 and A549/DDP) cells was higher than those of Pt-1, Pt-2, Pt-4, cisplatin and Pt-5. Moreover, the cytotoxicity of Pt-3 in HL-7702 normal cells was lower than those of PtIV derivatives bearing BA-COOH, FA-COOH, TCA-COOH and CA-COOH ligands. The highly efficacious Pt-2 and Pt-3 were found to accumulate strongly in the A549/DDP cells, with the prodrug Pt-3 showing highest levels of penetration into the mitochondria. The prodrug Pt-3 effectively entered the A549/DDP cells and caused mitochondrial damage, significantly greater than Pt-2. In addition, the prodrug Pt-3 exhibited higher antitumor efficacy (inhibition rates (IR) = 67.45%) than Pt-2 (28.12%) and cisplatin (33.05%) in the A549/DDP xenograft mouse model. Thus, the prodrug Pt-3 containing the rhein (RH-COOH) ligand is a promising candidate drug targeting the mitochondria.


Assuntos
Antraquinonas/farmacologia , Antineoplásicos/farmacologia , Cisplatino/análogos & derivados , Ácidos Cumáricos/farmacologia , Compostos Organoplatínicos/farmacologia , Pró-Fármacos/farmacologia , Células A549 , Animais , Antraquinonas/química , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Cisplatino/química , Cisplatino/farmacologia , Ácidos Cumáricos/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Ligantes , Camundongos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Estrutura Molecular , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/metabolismo , Neoplasias Experimentais/patologia , Compostos Organoplatínicos/síntese química , Compostos Organoplatínicos/química , Pró-Fármacos/síntese química , Pró-Fármacos/química , Relação Estrutura-Atividade
16.
Chirality ; 32(3): 299-307, 2020 03.
Artigo em Inglês | MEDLINE | ID: mdl-31975445

RESUMO

(±)-Pratenone A (1), the first representative of natural 3-(1-naphthyl)-2-benzofuran-1(3H)-one polyketides, was isolated from a marine-derived Streptomyces pratensis strain KCB-132 together with three other new analogues (2-4). Its structure was assigned by spectroscopic analysis, and the absolute configurations of the two enantiomers separated by high-performance liquid chromatography were determined by single-crystal X-ray diffraction and electronic circular dichroism calculations. The solvent-induced racemization of 1 and a proposed biogenetic pathway to 1-4 from the co-isolated angucyclinone precursor, as well as their biological activity, are also discussed.


Assuntos
Policetídeos/química , Streptomyces/química , Antraquinonas/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Organismos Aquáticos , Benzofuranos/química , Cromatografia Líquida de Alta Pressão , Dicroísmo Circular , Cristalografia por Raios X , Células HL-60 , Células Hep G2 , Humanos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Policetídeos/isolamento & purificação , Policetídeos/farmacologia , Policetídeos/toxicidade , Staphylococcus aureus/efeitos dos fármacos , Estereoisomerismo , Streptomyces/isolamento & purificação
17.
Biomed Pharmacother ; 123: 109779, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31918211

RESUMO

Staphylococcus xylosus (S. xylosus) is one of the emerging pathogens causing bovine mastitis with high rate of isolation in most of the reported clinical and field cases. To verify the role of glutamine synthetase (GS) in the pathogenesis of S. xylosus, we evaluated the virulence level of the wild-type strain and its glnA mutant strain in biofilm assays in vitro and murine infection model in vivo. From the results, it was observed that the glnA mutant strain was attenuated and could reduce tissue damage. 1-Hydroxyanthraquinone (1-HAQ) is a kind of anthraquinones, it exhibited a significant inhibitory effect on the growth of S. xylosus and biofilm formation in vitro and provided anti-inflammatory effects in vivo. In addition, the rate at which it inhibits the biofilm, inflammatory factors, and CFU of wild-type strains were significantly higher than that of the mutant strains, indicating that 1-hAQ might have pharmacological effects against S. xylosus through the regulation of GS protein. The effect of 1-hAQ on GS was further confirmed by the down-regulation of glnA expression, reduced GS activity, Gln content and the results of molecular docking. Taken together, these findings suggest that 1-hAQ facilitated a significant attenuation of S. xylosus pathogenicity by regulating the GS protein: a vital virulence factor. Therefore, it can be inferred that 1-hAQ may serve as a potential source of organic compound for the development of novel alternative drugs in mitigating the menace of bovine mastitis.


Assuntos
Antraquinonas/farmacologia , Antibacterianos/farmacologia , Glutamato-Amônia Ligase/metabolismo , Staphylococcus/enzimologia , Staphylococcus/patogenicidade , Fatores de Virulência/metabolismo , Animais , Antraquinonas/química , Antraquinonas/uso terapêutico , Antibacterianos/uso terapêutico , Biofilmes/efeitos dos fármacos , Contagem de Colônia Microbiana , Modelos Animais de Doenças , Feminino , Mastite/tratamento farmacológico , Mastite/microbiologia , Mastite/patologia , Camundongos Endogâmicos BALB C , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Staphylococcus/efeitos dos fármacos , Staphylococcus/crescimento & desenvolvimento
18.
Phytother Res ; 34(3): 486-504, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31773816

RESUMO

The present study was designed to review the antidiabetic potential of anthraquinones (AQs) with emphasis on the extent of blood glucose reduction, the half maximal inhibitory concentration values (in vitro studies), the proposed mechanisms of action, and the structure activity relationship studies. We sourced relevant data from the major scientific databases (Pubmed, Science Direct, Medline, and Google Scholar). According to our search, 25 AQs have shown variable antidiabetic potential, whereas one AQ (morindone-6-O-ß-D-primeveroside) showed no blood glucose-lowering ability. Emodin and rhein showed the most promising antidiabetic potential in various models. The proposed mechanisms of antidiabetic action include upregulation of insulin receptor substrates-1, phosphoinositide-3-kinase, and Akt-ser473 expression and elevation of glucagon-like peptide-1 level in diabetic animal models linked to the potent protein tyrosine phosphatase 1B and dipeptidyl peptidase-4 inhibitions. In addition, activation of peroxisome proliferator-activated receptors gamma and inhibition of α-glucosidase activity are other possible targets proposed as the mechanism of AQs antidiabetic action. The position and the number of hydroxyl group showed great influence on the overall antidiabetic potential of AQs. AQs hold promising antidiabetic activity despite scanty information. We hope that the present study will serve as a template to further explore the antidiabetic potential of AQs and subsequent antidiabetic drug development.


Assuntos
Antraquinonas/farmacologia , Diabetes Mellitus/tratamento farmacológico , Emodina/farmacologia , Hipoglicemiantes/farmacologia , Animais , Antraquinonas/química , Glicemia/efeitos dos fármacos , Inibidores da Dipeptidil Peptidase IV/química , Inibidores da Dipeptidil Peptidase IV/farmacologia , Emodina/química , Humanos , Hipoglicemiantes/química , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores
19.
Food Chem ; 311: 126013, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-31855768

RESUMO

Cost effective, simple and accurate two voltammetric methods for determination of boron in hazelnut, peanut, almond, raisin, prune and date samples were described. Metal nanoparticles-carbon nanotube modified glassy carbon electrode (MNP/CNT/GCE, M = Au or Cu) and poly xylenol orange modified pencil graphite electrode (p-XO/PGE) were used as working electrodes. The oxidation of alizarin red s (ARS) in the boron-ARS complex at MNP/CNT/GCE and the oxidation of tiron in the B-tiron complex at p-XO/PGE were monitored as response. The limit of determination values (based on visual evaluation) for CuNP/CNT/GCE, AuNP/CNT/GCE and p-XO/PGE were calculated as 100 µg/L, 125 µg/L and 80 µg/L, respectively. The results were compared with the results obtained by inductively coupled plasma mass spectrometric method and no significant difference between the results was observed. The accuracy experiments of the methods and uncertainty calculations were also performed using a certified reference material (UME CRM 1202 Elements in Hazelnut).


Assuntos
Boro/análise , Frutas/química , Nozes/química , Potenciometria , Antraquinonas/química , Eletrodos , Frutas/metabolismo , Grafite/química , Nanopartículas Metálicas/química , Nanotubos de Carbono/química , Nozes/metabolismo
20.
Carbohydr Polym ; 229: 115473, 2020 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-31826443

RESUMO

The development of solubilizers with high efficiency, high safety and simple technology is one of the important fields in modern pharmaceutical industry. Our previous study found that vinegar baked Radix Bupleurum polysaccharides (VBCP) was a potential candidate. This study aimed to clarify which polysaccharide in VBCP had solubility enhancement effect and its solubilizing mechanism. Here, we reported that a novel acidic branched polysaccharide from VBCP, VBCP-3-A, which was non-toxic and had high solubility to baicalin and rhein. It was much better than that of Tween 80. The solubilization mechanism might be that VBCP-3-A self-assembled to form micelle-like aggregates in water, which can encapsulate water-insoluble constituents through the interaction of both hydrogen bonding and hydrophobic forces. in vivo pharmacokinetic study showed that VBCP-3-A increased Cmax and AUC (0-t) of baicalin and rhein. Those results suggested that VBCP-3-A was a potential solubilizer with high efficiency and high safety.


Assuntos
Bupleurum/química , Portadores de Fármacos/química , Polissacarídeos/química , Animais , Antraquinonas/química , Antraquinonas/farmacocinética , Sequência de Carboidratos , Linhagem Celular , Portadores de Fármacos/toxicidade , Flavonoides/química , Flavonoides/farmacocinética , Humanos , Masculino , Micelas , Raízes de Plantas/química , Polissacarídeos/toxicidade , Ratos Sprague-Dawley , Solubilidade
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