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1.
Vet World ; 12(8): 1285-1290, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31641309

RESUMO

Background and Aim: Foot-and-mouth disease (FMD) has been occurring in Algeria since 2014, when an outbreak was announced in Setif, a district in the eastern region of the country. The problem was apparently resolved with the help of vaccination. However, in 2015, 2016, and 2018, FMD recurred. The veterinary authorities and media educated breeders on how to recognize the clinical signs and how to report the disease. This study aimed to evaluate the knowledge and recognition of FMD by farmers and breeders. Moreover, an assessment of the behavior of cattle and sheep owners and herders following FMD cases is examined. Materials and Methods: A cross-sectional survey was conducted from June to October 2018 to evaluate the perception of cattle and sheep owners and breeders regarding FMD in the Northern regions of Algeria, using questionnaires. Results: One hundred questionnaires were distributed; 71 were collected. Data showed that all the responders claimed to know about the disease, while more than half of the owners/herders claimed that they knew the clinical symptoms of FMD and mentioned fever, hypersalivation, lameness, and vesicles. Fewer than half (42%) (30/71) took some measures to prevent the disease, while more than half (58%) (41/71) did not take any measures in 2018. No one claimed to have reported the disease to authorities in 2018, while more than half had done so in 2014. Conclusion: It appears that experienced farmers recognized the clinical signs of FMD, while an academic background was not conclusively necessary for the identification of the clinical signs of the disease. Concerning the assessment of risk-associated behavior in the event of FMD occurrence, the responses of the breeders were not significantly different from those of risk-associated behaviors in the event of an epidemic. Farmers and breeders expressed similarity in terms of communicating the appearance of the disease in their livestock; the majority of them seemed to be aware of the importance of reporting the disease to local authorities, especially in 2014, when the disease first occurred. This behavior is encouraged by refund and technical assistance policies by the veterinary authorities, but in 2018, no disease was reported due to fear of slaughtering and economic loss.

2.
Artif Cells Nanomed Biotechnol ; 46(sup3): S471-S480, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30198334

RESUMO

Utilizing novel approaches for the green synthesis of metal nanoparticles are of great importance. Therefore, we reported biogenic synthesis of silver nanoparticles (AgNPs) using extracts of Leptolyngbya strain JSC-1, and their significant applications against pathogenic bacteria and cancerous HeLa cell line. The biofabricated AgNPs were characterized by UV-visible spectroscopy, FTIR, SEM, TEM, DLS and zeta-potential. The as prepared AgNPs were assessed for inhibition of bacterial growth and induction of apoptosis in HeLa cells by different doses of AgNPs was evaluated. UV-visible spectroscopy and FTIR of AgNPs demonstrated the surface plasmon resonance at 413 nm and interaction among extract and nanoparticles, respectively. Electron microscopy revealed the morphology and DLS demonstrated size distribution of the particles (10-100 nm). Zeta potential values were between -47 and 0 mV, indicating stability of the particles. Proliferation of HeLa cells was significantly inhibited and severe cytotoxicity with higher intracellular uptake were observed after applying high concentration of AgNPs. Efficient inhibition zones (17 ± 2 and 21 ± 2 mm) were produced at maximum concentration (100 µl from 1 mg ml-1 stock of AgNPs) for Staphylococcus aureus and Escherichia coli, respectively. These findings reveal that the biofabricated AgNPs possess strong antibacterial activity and ability to induce apoptosis in cancer cell line (HeLa).


Assuntos
Antibacterianos , Apoptose/efeitos dos fármacos , Misturas Complexas/química , Cianobactérias/química , Escherichia coli/crescimento & desenvolvimento , Nanopartículas Metálicas/química , Prata , Staphylococcus aureus/crescimento & desenvolvimento , Antibacterianos/química , Antibacterianos/farmacologia , Células HeLa , Humanos , Prata/química , Prata/farmacologia
3.
Microb Pathog ; 125: 150-157, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30217515

RESUMO

Low cost and an easy technique for the synthesis of palladium nanoparticles (PdNPs) was developed. Glucosamine was used to stabilize palladium precursor (PdCl2) into palladium nanoparticles. Several analytical techniques were used for the determination of morphology, crystalline structure; size, capping, and composition of synthesize palladium nanoparticles. The UV-visible spectroscopy SPR peak (Surface Plasmon Resonance) at 284 nm revealed synthesis of PdNPs. Energy dispersive X-ray (EDX) and X-ray diffraction (XRD) studies proved the elemental composition and crystalline structure of the synthesized palladium nanoparticles respectively. The average particle sizes (5.5 nm) were obtained by using the 1 M glucosamine solution, with a fixed amount of PdCl2 (4 mM). Moreover, the as synthesized PdNPs was evaluated against Gram negative bacterial E. which shows tremendous antibacterial activity as compare to tobramycin standard antibiotics. It's mechanistically found that PdNPs damage cell membrane and caused imbalance of metabolism system of the cell as a result production of reactive oxygen species (ROS). Thus, these finding revealed that cells become leaky and all organelles come out from cells, finally caused death of the E. coli. Addition, the as prepared PdNPs also showed excellent catalytic activities toward reduction of methylene blue and 4-nitrophenol.Thus, glucosamine mediated PdNPs having dual functions biomedical as well as intoxicating catalyst for industries.


Assuntos
Antibacterianos/metabolismo , Glucosamina/metabolismo , Nanopartículas Metálicas/ultraestrutura , Paládio/metabolismo , Substâncias Redutoras/metabolismo , Membrana Celular/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Excipientes/metabolismo , Redes e Vias Metabólicas/efeitos dos fármacos , Nanopartículas Metálicas/química , Espécies Reativas de Oxigênio/metabolismo , Espectrometria por Raios X , Análise Espectral , Ressonância de Plasmônio de Superfície , Difração de Raios X
4.
J Biotechnol ; 280: 49-54, 2018 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-29885337

RESUMO

Adipic acid (AA) is an important dicarboxylic acid used for the manufacture of nylon and polyurethane plastics. In this study, a novel adipic acid biosynthetic pathway was designed by extending the cis,cis-muconic acid (MA) biosynthesis through biohydrogenation. Enoate reductase from Clostridium acetobutylicum (CaER), an oxygen-sensitive reductase, was demonstrated to have in vivo enzyme activity of converting cis,cis-muconic acid to adipic acid under microaerobic condition. Engineered Escherichia coli strains were constructed to express the whole pathway and accumulated 5.8 ±â€¯0.9 mg/L adipic acid from simple carbon sources. Considering the different oxygen demands between cis,cis-muconic acid biosynthesis and its degradation, a co-culture system was constructed. To improve production, T7 promoter instead of lac promoter was used for higher level expression of the key enzyme CaER and the titer of adipic acid increased to 18.3 ±â€¯0.6 mg/L. To decrease the oxygen supply to downstream strains expressing CaER, Vitreoscilla hemoglobin (VHb) was introduced to upstream strains for its ability on oxygen obtaining. This attempt further improved the production of this novel pathway and 27.6 ±â€¯1.3 mg/L adipic acid was accumulated under microaerobic condition.


Assuntos
Adipatos/metabolismo , Oxirredutases atuantes sobre Doadores de Grupo CH-CH/metabolismo , Oxigênio/farmacologia , Ácido Sórbico/análogos & derivados , Aerobiose , Proteínas de Bactérias/farmacologia , Biocatálise , Vias Biossintéticas , Carbono/farmacologia , Clostridium acetobutylicum/enzimologia , Técnicas de Cocultura , Hidrogenação , Ácido Salicílico/metabolismo , Ácido Sórbico/metabolismo , Hemoglobinas Truncadas/farmacologia
5.
J Anal Methods Chem ; 2018: 7692913, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29888027

RESUMO

Urease enzyme is responsible for gastric cancer, peptic ulcer, hepatic coma, and urinary stones in millions of people across the world. So, there is a strong need to develop new and safe antiurease drugs, particularly from natural sources. In search for new and effective drugs from natural sources bioassay-guided fractionation and isolation of Berberis glaucocarpa Stapf roots bark resulted in the isolation and characterization, on the basis of 1D and 2D NMR data, of two bisbenzylisoquinoline alkaloids, oxyacanthine (1) and tetrandrine (2), followed by urease inhibition studies. Crude extract, all the subfractions and the isolated compounds 1 and 2 displayed excellent urease enzyme inhibition properties in vitro. The antiurease nature and possible mode of action for compounds 1 and 2 were verified and explained through their molecular docking studies against jack-bean urease enzyme. Half-maximum inhibitory concentration (IC50) was calculated for compounds 1 and 2. The IC50 value was found to be 6.35 and 5.51 µg/mL for compounds 1 and 2, respectively. Both compounds 1 and 2 have minimal cytotoxicity against THP-1 monocytic cells.

6.
Pak J Pharm Sci ; 31(3): 821-825, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29716861

RESUMO

A dimeric naphthoquinone namely dihydrodyspyrole R (1) was purified once more from Diospyros lotus. Dihydrodyspyrole R and chloroform fractions were evaluated for their effects on the reversion of multidrug resistance (MDR). The compounds (1) and extract exhibited promising MDR reversing effect in a dose-dependent manner against mouse T-lymphoma cell line. Molecular docking of compound 1 revealed the correlation between in-silico with in-vitro results. The molecular docking results showed that compound 1 is bind closely where co-crystal ligand of P-gp is present. But usually, computational investigation predicts that, if a compound gives lesser score then compound will exhibit good activity. Hence, the docking scores of compound 1 are the near to the Rhodamine. It is conclude that there are certain important structural features of compound 1which are responsible for the inhibiting potency of P-gp from mice. The computational Petra/Osiris/Molinspiration (POM) analysis confirms the possibility of use of compound 1 without side effect or less toxicity risks.


Assuntos
Diospyros , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Lotus , Naftoquinonas/química , Extratos Vegetais/química , Animais , Linhagem Celular Tumoral , Cristalografia por Raios X/métodos , Resistência a Múltiplos Medicamentos/fisiologia , Resistencia a Medicamentos Antineoplásicos/fisiologia , Camundongos , Simulação de Acoplamento Molecular/métodos , Naftoquinonas/isolamento & purificação , Naftoquinonas/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Raízes de Plantas
7.
J Photochem Photobiol B ; 183: 342-348, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29763756

RESUMO

Graphene-based materials have attracted a significant attention in constructing hybrid systems for drug delivery with enhanced antimicrobial activities. In our work, we demonstrated the formation of silver nanoparticles (AgNPs) on graphene oxide (GO) using tobramycin (TOB), an aminoglycoside antibiotic, as reducing and decorating agent. The TOB decorated GO AgNPs (TOB-GO-Ag) composite was used as an antibacterial agent against multi-drug resistant Gram-negative E-coli (BL21 DE3). The reversal of surface potential from -30 mV (GO) to +20 mV confirms the successful reduction of GO by TOB. Atomic force microscopy (AFM) and high-resolution transmission electron microscopic (HRTEM) analyses confirmed the formation of uniformly distributed AgNPs on the reduced GO with an approximate particle size of 5 nm. The as-synthesized nanocomposite displayed significant antibacterial activity as compared to pure AgNPs and TOB. The positively charged TOB-GO-Ag interacts with the negatively charged E. coli membrane and inhibit bacterial growth by the antibacterial actions of the released silver, GO and tobramycin from the TOB-GO-Ag composite. The significant loss of bacterial membrane potential from -52 ±â€¯2 mV (control) to -2 ±â€¯1 mV (treated) indicates a severe cell wall damage caused by TOB-GO-Ag composite. Furthermore, fluorescence study also demonstrated a severe membrane disruption in bacterial cells treated with TOB-GO-Ag composite as compared to pure AgNPs and GO. In conclusion, the development of such hybrid systems would help in enhancing the efficacy of available drugs and eradicating the emerging bacterial resistance.


Assuntos
Antibacterianos/química , Grafite/química , Nanopartículas Metálicas/química , Nanocompostos/química , Prata/química , Tobramicina/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Parede Celular/química , Parede Celular/efeitos dos fármacos , Sinergismo Farmacológico , Escherichia coli/efeitos dos fármacos , Células HEK293 , Humanos , Microscopia de Força Atômica , Microscopia Eletrônica de Transmissão , Nanocompostos/toxicidade , Óxidos/química , Espécies Reativas de Oxigênio/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Tobramicina/farmacologia
8.
Pak J Pharm Sci ; 31(1): 181-186, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29348101

RESUMO

The aim of the present study was to examine the effect of gamma radiation on levofloxacin. Powder form of levofloxacin was subjected to different radiation doses (25, 50, 75, 100 and 125kGy) of Cobalt-60 source in a Gammacell-220 at a rate of 8.5 Gray/hr. The effect of radiation has been investigated with the aid of different spectroscopic techniques (UV-Vis, FT-IR), scanning electron microscopy (SEM), X-ray diffraction (XRD), and by antibacterial activities. UV data did not reveal significant changes in the structure of levofloxacin which is supported by scanning electron microscopy. However, X-rays diffraction shows a change in crystallinity of levofloxacin to an amorphous structure and this has been reflected on the morphology of this compound as indicated by SEM images. The antibacterial activities, on the other hand, reveal resistance of irradiated levofloxacin against bacteria, where some bacteria were highly affected by the irradiated drug. Similarly, FT-IR data show some changes in the functional groups principal absorption bands, in the IR spectrum, at frequencies 3286, 2846, 1716 and 1620 cm-1 for the O-H stretching band of quinolone, C-H stretching band, and C=O stretching band of carboxylic and pyridine. In addition, new peaks appeared which were not seen in the non-irradiated spectrum. In conclusion, some changes occurred in levofloxacin drug with the passage of radiation but the drug was chemically stable.


Assuntos
Antibacterianos/efeitos da radiação , Raios gama , Levofloxacino/efeitos da radiação , Esterilização/métodos , Antibacterianos/química , Bactérias Gram-Negativas/efeitos da radiação , Bactérias Gram-Positivas/efeitos da radiação , Levofloxacino/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pós , Estereoisomerismo , Propriedades de Superfície
9.
Comput Biol Chem ; 71: 10-19, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28957725

RESUMO

Growing resistance in malarial parasites, particularly in Plasmodium falciparum needs a serious search for the discovery of novel drug targets. Inosine monophosphate dehydrogenase (IMPDH) is an important target for antimalarial drug discovery process in P. falciparum for the treatment of malaria. In the absence of x-ray crystal structure of this enzyme, homology modeling proved to be a reasonable alternate to study substrate binding mechanisms of this enzyme. In this study, a 3-D homology model for P. falciparum IMPDH was constructed taking human IMPDH (PDB code 1NF7) as template. Furthermore, an in-silico combinatorial library of ribavirin (RVP) derivatives (1347 molecules) was designed and virtually screened for ligands having selectively greater binding affinity with Plasmodium falciparum IMPDH relative to human IMPDH II. A total of five Ribavirin derivatives were identified as having greater binding affinity (-126 to -108Kcal/mol and -9.4 to -8.6Kcal/mol) with Plasmodium falciparum IMPDH. These five inhibitors should be used as selective and potent for Plasmodium falciparum IMPDH. Such type of study will provide information to synthetic medicinal chemist to enhance the potential of compounds (RVP derivatives) as chemotherapeutic agents to fight against the increasing burden of malarial infections.


Assuntos
Simulação por Computador , IMP Desidrogenase/antagonistas & inibidores , IMP Desidrogenase/química , Simulação de Acoplamento Molecular , Plasmodium falciparum/enzimologia , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , IMP Desidrogenase/metabolismo , Estrutura Molecular , Ribavirina/análogos & derivados , Ribavirina/química , Ribavirina/farmacologia , Relação Estrutura-Atividade
10.
Colloids Surf B Biointerfaces ; 157: 242-253, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-28601753

RESUMO

The study of molecular interactions of drug-protein are extremely important from the biological aspect in all living organisms, and therefore such type of investigation hold a tremendous significance in rational drug design and discovery. In the present study, the molecular interactions between paromomycin (PAR) and human serum albumin (HSA) have been studied by different biophysical techniques and validated by in-silico approaches. The results obtained from Ultraviolet-visible spectroscopy (UV) and Fourier transform infrared spectroscopy (FT-IR) demonstrated a remarkable change upon the complexation of PAR with HSA. Circular Dichroism (CD), Dynamic Light Scattering (DLS) and Resonance Rayleigh scattering (RRS) results revealed a significant secondary structure alteration and reduction of hydrodynamic radii upon the conjugation of PAR with HSA. The fluorescence spectroscopy results also apparently revealed the static quenching mechanism. The number of binding sites, binding constants, and Gibbs free energy values were calculated to illustrate the nature of intermolecular interactions. Similarly, the in-silico docking and molecular dynamics simulation clearly explain the theoretical basis of the binding mechanism of PAR with HSA. The experimental and docking approaches suggested that PAR binds to the hydrophobic cavity site I of HSA. The finding of present investigation will provide binding insight of PAR and associated alterations in the stability and conformation of HSA.


Assuntos
Paromomicina/química , Albumina Sérica Humana/química , Dicroísmo Circular , Estabilidade de Medicamentos , Difusão Dinâmica da Luz , Humanos , Simulação de Acoplamento Molecular , Ligação Proteica , Espectrometria de Fluorescência , Espectroscopia de Infravermelho com Transformada de Fourier , Termodinâmica
11.
Med Chem ; 13(8): 721-726, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28606042

RESUMO

BACKGROUND: Fungi performing a wide range of function in soil by secreting low molecular weight compound known as secondary metabolites. S. rolfsii is a soil borne phytopathogenic fungi was used for the production of bioactive compounds. OBJECTIVE: The present study belongs to evaluate the anticancer potentials of a secondary metabolites isolated from S. rolfsii, their multidrug resistance (MDR), and molecular docking study. METHOD: (1S,3R,4R,5R,E)-3-(3-(3,4-Dihydroxyphenyl)acryloyloxy)-1,4,5 trihydroxycyclohexanecarboxylic acid (1), or best known as chlorogenic acid, was isolated from the ethyl acetate fraction of crude secondary metabolites produced by the soil borne Fungus Screlotium rolfsii. Structure of chlorogenic acid (1) was confirmed by means of FT-IR, 1H NMR, 13C NMR, and mass spectrometry as well as by melting point. RESULTS: Effect of compound 1 on the reversion of multidrug resistant (MDR) mediated by Pglycoprotein (P-gp) against cancer cells was evaluated with a rhodamine-123 exclusion screening test on human mdr1 gene transfected mouse gene transfected L5178 and L5178Y mouse T-cell lymphoma. Compound 1 was also evaluated for Anti-proliferative effect on the L5178 mouse Tcell lymphoma cell line. CONCLUSION: Results from the present investigation revealed that compound 1 exhibits excellent MDR reversing effect in a dose-dependent manner against mouse T-lymphoma cell line. Compound 1 also showed anti-proliferative effect on L5178Y mouse T-lymphoma cell line.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Ácido Clorogênico/farmacologia , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Fungos/química , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ácido Clorogênico/química , Ácido Clorogênico/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Camundongos , Estrutura Molecular , Microbiologia do Solo , Relação Estrutura-Atividade
12.
J Photochem Photobiol B ; 173: 368-375, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28646755

RESUMO

Platinum based drugs are considered as effective agents against various types of carcinoma; however, the severe toxicity associated with the chemically prepared platinum complexes limit their practical applications. Similarly, water pollution caused by various organic moieties is another serious health problem worldwide. Hence, an intense need exists to develop new, effective and biocompatible materials with catalytic and biomedical applications. In the present contribution, we prepared platinum nanoparticles (PtNPs) by a green route using phytochemicals as a source of reducing and stabilizing agents. Well dispersed and crystalline PtNPs of spherical shapes were prepared and characterized. The bio-fabricated PtNPs were used as catalyst and anticancer agents. Catalytic performance of the PtNPs showed that 84% of the methylene blue can be reduced in 32min under visible light irradiation (K=0.078min-1). Similarly the catalytic conversion of 4-nitrophenol to 4-aminophenol was achieved in <20min (K=0.124min-1). The in vitro anticancer study revealed that biogenic PtNPs are the efficient nano-agents possessing strong anticancer activity against the lungs cancer cells line (A549). Interestingly, the as prepared PtNPs were well tolerated by normal human cells, and therefore, could be effective and biocompatible agents in the treatment of different cancer cells.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Neoplasias Pulmonares/patologia , Nanopartículas Metálicas , Platina/química , Platina/farmacologia , Antineoplásicos/metabolismo , Transporte Biológico , Catálise , Linhagem Celular Tumoral , Estabilidade de Medicamentos , Humanos , Nitrofenóis/metabolismo , Oxirredução/efeitos dos fármacos , Tamanho da Partícula , Platina/metabolismo
13.
J Photochem Photobiol B ; 170: 6-15, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28364684

RESUMO

Exogenous drug as an antidote to treat various infections get absorbed in the blood circulatory system of a human can directly contact with transporter proteins such as serum albumin. Therefore, for rational drug discovery, understanding the biomolecular interaction between drugs and protein is highly important. In this contribution, we describe the possible interactions between an antifungal drug Amphotericin B (AmB) and Bovine Serum Albumin (BSA) using multi-spectroscopic techniques and further confirmed through in-silico approaches. Binding effects of AmB on BSA conformation, surface morphology, topology, and stability were determined by Ultraviolet-visible spectroscopy (UV), Fourier transform infrared spectroscopy (FT-IR), Circular Dichroism (CD), Transmission Electron Microscopy (TEM), Dynamic Light Scattering (DLS), Fluorescence Spectroscopy and Molecular dynamic simulations. The Stern-Volmer equation was used to determine the binding site (0.4) and binding constant (8.16×105M-1). The intrinsic intensity of the native BSA was quenched by AmB through static quenching mechanism. The calculated Gibbs free energy value (-8.70kcal/mol) indicated the involvement of hydrogen bonding and hydrophobic contacts in BSA-AmB interaction. The hydrodynamic radii and surface contact area of BSA-AmB molecules are decreasing which can strongly support the stabilizing action of complex particles. Moreover, the finding of this work will provide information for the drug designers to further study the AmB binding mechanism and their pharmacodynamics and pharmacokinetics features in order to achieve better therapeutic efficacy.


Assuntos
Anfotericina B/metabolismo , Soroalbumina Bovina/metabolismo , Anfotericina B/química , Animais , Sítios de Ligação , Bovinos , Dicroísmo Circular , Difusão Dinâmica da Luz , Ligação de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Microscopia Eletrônica de Transmissão , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Soroalbumina Bovina/química , Espectrometria de Fluorescência , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier
14.
Microb Pathog ; 107: 419-424, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28435109

RESUMO

The formation of metal nanoparticles is one of the most vast and intensifying research areas in favor of prospective applications for the advancement of new technologies. It is a well-founded, significant feature of green chemistry that making marvelous interconnection between nano-biotechnology and microbial biotechnology. In the present research, the aqueous extract of medicinally important plant Coptis Chinensis (in Chinese called "gold thread") was applied for the synthesis of gold nanoparticles (Au-NPs). The crystalline structure, size, shape and dispersion of Au-NPs were confirmed by using various characterization techniques i.e. X-ray Diffraction (XRD), High Resolution Transmission Electron Microscope (HRTEM) and Energy Dispersive X-ray (EDX). Well dispersed face centered cubic crystalline structures were obtained in the this contribution. The possible phyto-chemicals involved in the reduction and stabilization of Au-NPs were confirmed by Fourier Transform Infrared Spectroscopy (FT-IR). The prepared NPs were tested against highly drug resistance bacterium Escherichia coli both in light and dark. The results illustrated that the antibacterial efficiency of photo irradiated Au-NPs was several times higher than in dark Au-NPs. The zone of inhibition for irradiated Au-NPs was19 ± 0.5 mm, which was higher than in dark 14 ± 0.4 mm. This high antibacterial activity of photo irradiated Au-NPs are due to the production of reactive oxygen species which is responsible for the inhibition of bacteria.


Assuntos
Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Ouro/efeitos da radiação , Luz , Nanopartículas Metálicas/efeitos da radiação , Espécies Reativas de Oxigênio/metabolismo , Antibacterianos/química , Coptis/química , Farmacorresistência Bacteriana , Ouro/química , Nanopartículas Metálicas/química , Nanopartículas Metálicas/ultraestrutura , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Transmissão , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
15.
Virol J ; 14(1): 86, 2017 04 24.
Artigo em Inglês | MEDLINE | ID: mdl-28438210

RESUMO

BACKGROUND: The BK Polyomavirus (BKPyV) and JC polyomavirus (JCPyV) infections are widespread in human population and have been associated with severe kidney and brain disorders, respectively. The viruses remain latent primarily in reno-urinary tract, reactivating only in case of a compromised immune system. The seroepidemiology and molecular prevalence of BKPyV and JCPyV have been widely studied both in healthy and immunocompromised patients worldwide. However, data regarding the prevalence of these viruses in the immunocompetent or apparently healthy Pakistani population is lacking. Herein, we present the first ever report on quantitative prevalence of BKPyV and JCPyV in the peripheral blood of a randomly selected cohort of healthy Pakistani population. METHODS: A total of 266 whole blood samples were examined. The subjects were divided into three age groups: ≤ 25 years (young), 26-50 years (middle) and ≥ 51 years (elder). Absolute real time PCR assay was designed to quantify the BKPyV and JCPyV viral copy numbers in the range of 106 to 100 copies/mL. RESULTS: Overall, BKPyV was detected in 27.1% (72/266) individuals while JCPyV in 11.6% (31/266) indicating significant difference (p < 0.005) in the distribution of these two viruses. The prevalence of BKPyV significantly decreased from 51% (49/96) in young age group to 8.2% (7/85) in eldest age group. Whereas, JCPyV positivity rate slightly increased from 8.3% (8/96) in young age group to 11.8% (10/85) in elder age group. The median viral load was calculated as 6.2 log and 3.38 log copies/mL of blood for BKPyV and JCPyV, respectively. Notably, no significant difference in viral load of either of the subtypes was found between different age groups. CONCLUSION: The current study provides an important baseline data on the prevalence and viral load of circulating BKPyV and JCPyV in Pakistani population. The prevalence and viral load of BKPyV was comparatively higher than JCPyV. The prevalence of BKPyV significantly decreased with increase in age while JCPyV positivity rate slightly increased with increasing age. Viral load of both BKPyV and JCPyV was not correlated with the individual ages.


Assuntos
Vírus BK/isolamento & purificação , Voluntários Saudáveis , Vírus JC/isolamento & purificação , Infecções por Polyomavirus/epidemiologia , Infecções por Polyomavirus/virologia , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Sangue/virologia , Portador Sadio/epidemiologia , Portador Sadio/virologia , Criança , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Paquistão/epidemiologia , Prevalência , Reação em Cadeia da Polimerase em Tempo Real , Carga Viral , Adulto Jovem
16.
Chem Biodivers ; 14(6)2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28207990

RESUMO

Plant phenolics are known to display many pharmacological activities. In the current study, eight phenolic compounds, e.g., luteolin 5-O-ß-glucoside (1), methyl rosmarinate (2), apigenin (3), vicenin 2 (4), lithospermic acid (5), soyasaponin II (6), rubiadin 3-O-ß-primeveroside (7), and 4-(ß-d-glucopyranosyloxy)benzyl 3,4-dihydroxybenzoate (8), isolated from various plant species were tested at 0.2 mm against carbonic anhydrase-II (CA-II) and urease using microtiter assays. Urease inhibition rate for compounds 1 - 8 ranged between 5.0 - 41.7%, while only compounds 1, 2, and 4 showed a considerable inhibition over 50% against CA-II with the IC50 values of 73.5 ± 1.05, 39.5 ± 1.14, and 104.5 ± 2.50 µm, respectively, where IC50 of the reference (acetazolamide) was 21.0 ± 0.12 µm. In silico experiments were also performed through two docking softwares (Autodock Vina and i-GEMDOCK) in order to find out interactions between the compounds and CA-II. Actually, compounds 6 (30.0%) and 7 (42.0%) possessed a better binding capability toward the active site of CA-II. According to our results obtained in this study, among the phenolic compounds screened, particularly 1, 2, and 4 appear to be the promising inhibitors of CA-II and may be further investigated as possible leads for diuretic, anti-glaucoma, and antiepileptic agents.


Assuntos
Inibidores da Anidrase Carbônica/farmacologia , Fenóis/farmacologia , Urease/antagonistas & inibidores , Domínio Catalítico , Simulação por Computador , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ligação Proteica , Relação Estrutura-Atividade
17.
Biomed Pharmacother ; 87: 678-682, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28088734

RESUMO

Diospyros lotus L. possesses different therapeutic activities such as antioxidant, anti-proliferative, anti-microbial and sedative. However, no studies on the sedative-hypnotic activity of 7-methyljuglone are reported. In the present study, we have evaluated in vivo the anxiolytic-hypnotic like effects of 7-methyljuglone in mice with open field and phenobarbitone-induced sleeping time tests. We have also assessed in silico the involvement of GABAA, GABAB and 5HT1 neurotransmission in its mechanism of action. The intraperitoneal administration of 7-methyljuglone (2.5-10mg/kg) reduce significantly the number of crossed lines in mice open field test and concomitantly it shown a significant activity in term of onset of sleeping time and also in its duration. Moreover, 7-methyljuglone demonstrated in silico an interesting interaction with GABAA but not GABAB and 5HT1binding sites. All of these results, taken together, 7-methyljuglone may be an innovative candidate for designing new pharmaceutical and therapeutic applications.


Assuntos
Diospyros/química , Hipnóticos e Sedativos/farmacologia , Naftoquinonas/farmacologia , Extratos Vegetais/farmacologia , Animais , Antioxidantes/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C
18.
Curr Top Med Chem ; 17(4): 412-417, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-27558680

RESUMO

BACKGROUND: Polyphenols are organic compounds widely found in plants and possess many diverse biological activities. In the current study, eleven polyphenolic compounds [rutin (1), trans-ferulic acid (2), epigallaocatechin gallate (3), fumaric acid (4), chlorogenic acid (5), gallic acid (6), trans-resveratrol (7), propyl gallate (8), (+)-catechin (9), quercetin (10), and kaempferol-3-O-ß-D-galactoside (11)] have been evaluated for their in vitro inhibitory activity against phosphodiesterase- 1 (PDE-1). The active compounds 1, 5, 6, and 7 possessed IC50 values of 173.90 ± 2.58, 36.67 ± 1.60, 325.19 ± 3.62, and 323.81 ± 4.25 µM, respectively. In silico experiments were performed to elucidate the binding patterns of inhibitor molecules with the active sites of the enzymes. RESULT: Molecular docking studies have shown that compounds 1 and 5 have better docking results than standard inhibitor (EDTA) against the PDE-1. In conclusion, chlorogenic acid, rutin, gallic acid, and resveratrol could be promising PDE-1 inhibitors and leads to identify new drug candidates against PDE-1-associated disorders.


Assuntos
Produtos Biológicos/farmacologia , Inibidores Enzimáticos/farmacologia , Inibidores de Fosfodiesterase/farmacologia , Polifenóis/farmacologia , Simulação por Computador , Técnicas In Vitro
19.
Curr Top Med Chem ; 17(4): 383-390, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-27558683

RESUMO

BACKGROUND: The present study was designed to evaluate the anti-hyperalgesic effect of kaempferol-3,7-di-O-α-L-rhamnopyranoside isolated from the ethyl acetate soluble part of Dryopteris cycadina. Pretreatment of the compound at the doses of 2.5, 5, and 10 mg/kg caused a significant reduction in abdominal constrictions in acetic acid-induced writhing test with maximum effect of 63.03% (P < 0.001) at 10 mg/kg i.p. When subjected in formalin test, it evoked a marked antinociceptive effect in both phases in a dose-dependent manner. The maximum (p < 0.01) pain-inhibiting effects were 61.36% and 65.89% in 1st and 2nd phases at 10 mg/kg i.p., respectively. Administration of atropine (non-selective cholinergic receptor antagonist) significantly (p < 0.05) antagonized the antihyperalgesic effect of the compound, while glibenclamide and naloxone did not alter the induced antinociceptive effect and thus, antinociceptive activity of the compound is mediated, at least in part, through cholinergic system antagonism; independent of calcium channel and opioidergic receptor participation. Furthermore, docking studies underlined strong COX-2 inhibitory activity of the compound. RESULT: Our data concluded that overall analgesic activity of the compound seems to involve COX-2 inhibition and activation of cholinergic receptors. However, further detailed studies are required in this direction to confirm the analgesic effect of the compound for its possible clinical utility.


Assuntos
Analgésicos/farmacologia , Dryopteris/química , Quempferóis/farmacologia , Animais , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Simulação de Acoplamento Molecular
20.
J Photochem Photobiol B ; 162: 189-198, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27376463

RESUMO

Water purification is one of the worldwide problem and most of the conventional methods are associated with a number of drawbacks. Therefore it is the need of the day to develop new methods and materials to overcome the problem of water purification. In this research work we present a simple and green approach to synthesize silver decorated titanium dioxide (Ag/TiO2) nanocomposite with an efficient photo catalytic activities. Phytochemicals of the Cestrum nocturnum leaf extract were used to synthesize silver nanoparticles (AgNPs), Titanium dioxide (TiO2) and Ag/TiO2 nanocomposite. To confirm the formation, crystal structure, particle size and shape of green synthesized nanoparticles and nanocomposite, they were characterized by UV-visible spectroscopy (UV-vis), X-ray diffraction spectroscopy (XRD), high resolution transmission electron microscopy (HRTEM), Scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FT-IR). The AgNPs, TiO2 and Ag/TiO2 were evaluated for photo degradation of methylene blue (MB) and photo inhibition of Bacteria. The bio-synthesized Ag/TiO2 nanocomposite was observed to have strong catalytic activities for photo reduction of MB and photo inactivation of bacteria as compared to bare AgNPs and TiO2. In the presence of Ag/TiO2, 90% of MB was degraded only in 40min of irradiation. Alternatively the bare AgNPs and TiO2 degraded less than 30% and 80% respectively of MB even in more than 100min of irradiation. Similarly the Ag/TiO2 has very strong photo inhibition efficiency towards Escherichia coli and Pseudomonas aeruginosa. The zone of inhibition of irradiated Ag/TiO2 nanocomposites against E. coli and P. aeruginosa was 19mm and 17mm respectively which was two times higher than in dark. These promising photocatalytic activities of nanocomposite may be due to the highly decorated AgNPs over the surface of TiO2.


Assuntos
Luz , Azul de Metileno/química , Viabilidade Microbiana/efeitos da radiação , Nanocompostos/química , Fotólise , Prata/química , Titânio/química , Antibacterianos/química , Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/fisiologia , Escherichia coli/efeitos da radiação , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana , Viabilidade Microbiana/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/fisiologia , Pseudomonas aeruginosa/efeitos da radiação , Fatores de Tempo
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