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1.
Molecules ; 26(16)2021 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-34443460

RESUMO

Synthetic heterocyclic compounds have incredible potential against different diseases; pyridines, phenolic compounds and the derivatives of azo moiety have shown excellent antimicrobial, antiviral, antidiabetic, anti-melanogenic, anti-ulcer, anticancer, anti-mycobacterial, anti-inflammatory, DNA binding and chemosensing activities. In the present review, the above-mentioned activities of the nitrogen-containing heterocyclic compounds (pyridines), hydroxyl (phenols) and azo derivatives are discussed with reference to the minimum inhibitory concentration and structure-activity relationship, which clearly indicate that the presence of nitrogen in the phenyl ring; in addition, the hydroxyl substituent and the incorporation of a diazo group is crucial for the improved efficacies of the compounds in probing different diseases. The comparison was made with the reported drugs and new synthetic derivatives that showed recent therapeutic perspectives made in the last five years.


Assuntos
Compostos Azo/uso terapêutico , Fenóis/uso terapêutico , Piridinas/uso terapêutico , Compostos Azo/síntese química , Compostos Azo/química , Imageamento Tridimensional , Fenóis/síntese química , Fenóis/química , Piridinas/síntese química , Piridinas/química
2.
J Enzyme Inhib Med Chem ; 36(1): 1509-1520, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34238110

RESUMO

In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via the diazo-coupling approach between substituted aromatic amines with phenol or naphthol derivatives. The compounds were evaluated for their therapeutic applications against alpha-glucosidase (anti-diabetic) and pathogenic bacterial strains E. coli (gram-negative), S. aureus (gram-positive), S. aureus (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative), P. aeruginosa (gram-negative) drug-resistant strain and P. vulgaris (gram-negative). The IC50 (µg/mL) of TR-1 was found to be most effective (15.70 ± 1.3 µg/mL) compared to the reference drug acarbose (21.59 ± 1.5 µg/mL), hence, it was further selected for the kinetic studies in order to illustrate the mechanism of inhibition. The enzyme inhibitory kinetics and mode of binding for the most active inhibitor (TR-1) was performed which showed that the compound is a non-competitive inhibitor and effectively inhibits the target enzyme by binding to its binuclear active site reversibly.


Assuntos
Antibacterianos/farmacologia , Compostos Azo/farmacologia , Inibidores Enzimáticos/farmacologia , Hipoglicemiantes/farmacologia , Simulação de Acoplamento Molecular , alfa-Glucosidases/metabolismo , Antibacterianos/síntese química , Antibacterianos/química , Compostos Azo/síntese química , Compostos Azo/química , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Escherichia coli/efeitos dos fármacos , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Cinética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Saccharomyces cerevisiae/enzimologia , Staphylococcus aureus/efeitos dos fármacos
3.
Pak J Pharm Sci ; 32(6): 2751-2756, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31969311

RESUMO

Avian influenza or bird flu is a common problem of domestic and wild birds. Some of its strains are able to cross the species barrier and cause infection in various members of class Mammalia. In view of relatively lesser efficacy of vaccines, antiviral therapies remain the only choice for the sustenance of mammals acquiring this highly devastating infection. This study is based on the evaluation of antiviral potential of methanol extracts of eleven selected Cholistani plants. The methanol extracts were prepared by using dried plants material followed by concentrating in a rotary evaporator and finally air dried before dissolving in nanopure water. The suspension was filter sterilized and subjected to in ovo antiviral assays. The allantoic fluids were harvested and haemagglutinin (HA) titers were determined. Among the eleven plants evaluated all methanol extracts were found effective against AIV H9N2 except S. baryosma extract. The medicinal plants O. compressa, N. procumbens, and S. surattense were found to be more effective than others and they retained HA titers at 0 after challenge. The next in order were extracts of O. esculentum, H. salicornicum and S. fruticosa which kept HA titers at 4, 8 and 16 respectively. The extracts of H. recurvum, P. antidotale, S. icolados and A. aspera were found less effective than above mentioned plant extracts and they kept the HA titers at 32, 64, 128 and 256 respectively. These results led us to conclude that the medicinal plants of Cholistan region are a rich source of antiviral agent(s) against AIV H9N2 and could be a source of cost effective alternate therapeutics.


Assuntos
Antivirais/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Antivirais/isolamento & purificação , Galinhas/virologia , Etnobotânica , Testes de Hemaglutinação , Influenza Aviária/tratamento farmacológico , Influenza Aviária/virologia , Paquistão , Extratos Vegetais/isolamento & purificação , Doenças das Aves Domésticas/tratamento farmacológico , Doenças das Aves Domésticas/virologia
4.
Pak J Pharm Sci ; 30(5(Supplementary)): 2025-2029, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29105639

RESUMO

Tuberculosis (TB) is a life threatening infectious disease which is prevalent throughout the world. Mycobacterium bovis based Bacille Calmette-Gue´rin (BCG) is the only vaccine available against TB however, this (single) vaccine is not enough to eradicate it. Furthermore, numbers of researches from different parts of the World have shown its efficacy as variable. Hence other (better) vaccines like DNA vaccines are needed in addition to BCG in order to achieve desired goal of TB eradication. The current study was aimed to develop subunit based DNA vaccines against TB and to check their efficacy. Two constructs Bfrb-pND14 and Mpt32-pND14 were made and used as DNA vaccines. Endotoxin free DNA preparations were made and used in immunization studies. Twenty Balb/c female mice of age eight weeks were used in trial. Two experimental groups each comprising eight animals were used to inoculate Mpt32-pND14 and Bfrb-pND14 vaccines respectively. A group of four animals was used as negative control. Animals were bled through tail periodically and finally through cardiac puncture before euthanization. Antibodies were confirmed through dot blot and Agar Gel Immuno Diffusion test (AGID). All the animals immunized with both vaccines were found positive as tested through dot blot and AGID. The results of this study have indicated that both the M. tb genes have produced strong immune response in mice model through pND14 vector and proved themselves as good subunit based DNA vaccines.


Assuntos
Proteínas de Bactérias/administração & dosagem , Ferritinas/administração & dosagem , Mycobacterium tuberculosis/genética , Vacinas contra a Tuberculose/administração & dosagem , Tuberculose/prevenção & controle , Vacinas de DNA/administração & dosagem , Animais , Anticorpos Antibacterianos/sangue , Proteínas de Bactérias/genética , Proteínas de Bactérias/imunologia , Feminino , Ferritinas/genética , Ferritinas/imunologia , Imunização , Imunogenicidade da Vacina , Camundongos Endogâmicos BALB C , Mycobacterium tuberculosis/imunologia , Tuberculose/imunologia , Tuberculose/microbiologia , Vacinas contra a Tuberculose/imunologia , Vacinas de DNA/imunologia
5.
Parasit Vectors ; 8: 415, 2015 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-26259616

RESUMO

BACKGROUND: Surra, a vector borne disease caused by Trypanosoma (T.) evansi, affects the health, productivity and working capacity of camels. Since clinical signs are not pathognomonic, diagnosis must be confirmed by laboratory methods. This is a first study on the prevalence of surra in Cholistan Desert, Pakistan using a broad variety of diagnostic tests thereby emphasizing it as a risk for the dromedaries of Pakistan. METHODS: In a cross sectional study, 1005 dromedary camels from three districts in the Cholistan Desert were sampled to assess the prevalence of trypanosomosis due to T. evansi by means of parasitological (Giemsa stained thin smear), serological (formol gel test, CATT/T. evansi, ELISA/VSG RoTat 1.2, immune trypanolysis) and molecular tests (TBR1/2 PCR and RoTat 1.2 PCR). Kappa was calculated to assess the degree of agreement between different tests whereas chi-square test along with odds ratios and their 95% confidence intervals were used to study influence of breed, gender, age and locality on disease prevalence. RESULTS: Overall prevalence was 0.7% with Giemsa stained thin smears (GST), 40.1% with formol gel test (FGT), 47.7% with CATT/T. evansi, 44.2% with ELISA/VSG RoTat 1.2, 39.9 % with immune trypanolysis (TL), 31.9 % with TBR1/2 PCR and 30.5% with RoTat1.2 PCR. Based on these results, the Cholistan Desert appears to be a high risk area for surra. According to TL and TBR1/2 PCR, camels at Bahawalpur are approximately two times more likely to be infected than those in Bahawalnagar (OR = 1.8; 95% CI: 1.38-2.42) and Rahim Yar Khan (OR = 1.9; 95% CI: 1.30-2.75). Test agreement of TL was moderate with CATT/T. evansi (k = 0.43; 95% CI: 0.378-0.489) and ELISA/VSG RoTat 1.2 (k = 0.54; 95% CI: 0.489-0.594) and poor with the other tests. Test agreement between TBR1/2 PCR and RoTat1.2 PCR was almost perfect (k = 0.96; 95% CI: 0.950-0.984). We didn't find evidence for the presence of T. evansi type B in the studied population. CONCLUSION: Our study supports using antibody detection tests, rather than parasitological and molecular examination, to assess surra prevalence in camels. It also calls for implementation of measures to control surra in the Cholistan Desert.


Assuntos
Camelus/parasitologia , Trypanosoma/isolamento & purificação , Tripanossomíase/veterinária , Animais , Antígenos de Protozoários/sangue , Camelus/sangue , Estudos Transversais , Clima Desértico , Ensaio de Imunoadsorção Enzimática , Feminino , Masculino , Paquistão/epidemiologia , Reação em Cadeia da Polimerase , Prevalência , Trypanosoma/genética , Trypanosoma/imunologia , Tripanossomíase/sangue , Tripanossomíase/epidemiologia , Tripanossomíase/parasitologia
6.
Clin Vaccine Immunol ; 18(12): 2148-53, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21976221

RESUMO

Two billion people are infected with Mycobacterium tuberculosis, the etiological agent of tuberculosis (TB), worldwide. Ten million to 20 million of the infected individuals develop disease per year. TB is a treatable disease, provided that it is diagnosed in a timely manner. The current TB diagnostic methods are subjective, inefficient, or not cost-effective. Antibody-based blood tests can be used efficiently and cost-effectively for TB diagnosis. A major challenge is that different TB patients generate antibodies against different antigens. Therefore, a multiplex immunoassay approach is needed. We have developed a multiplex panel of 28 M. tuberculosis antigen-coated microbeads. Plasma samples were obtained from over 300 pulmonary TB patients and healthy controls in a country where TB is endemic, Pakistan. Multiplex data were analyzed using computational tools by multivariate statistics, classification algorithms, and cluster analysis. The results of antibody profile-based detection, using 16 selected antigens, closely correlated with those of the sputum-based diagnostic methods (smear microscopy and culture) practiced in countries where TB is endemic. Multiplex microbead immunoassay had a sensitivity and specificity of approximately 90% and 80%, respectively. These antibody profiles could potentially be useful for the diagnosis of nonpulmonary TB, which accounts for approximately 20% of cases of disease. Since an automated, high-throughput version of this multiplex microbead immunoassay could analyze thousands of samples per day, it may be useful for the diagnosis of TB in millions of patients worldwide.


Assuntos
Anticorpos Antibacterianos/sangue , Biomarcadores/sangue , Técnicas de Laboratório Clínico/métodos , Mycobacterium tuberculosis/imunologia , Tuberculose/diagnóstico , Humanos , Imunoensaio/métodos , Microesferas , Paquistão , Plasma/imunologia , Sensibilidade e Especificidade , Escarro/microbiologia
7.
Virol J ; 5: 144, 2008 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-19040734

RESUMO

Our studies were aimed at developing a vaccination strategy that could provide protection against highly pathogenic avian influenza virus (AIV), H7N3 or its variants outbreaks. A purified viral stock of highly pathogenic H7N3 isolate was lysed to isolate viral proteins by electrophresing on 12% sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE), followed by their elution from gel through trituration in phosphate buffered saline (PBS). Overall, five isolated viral polypeptides/proteins upon characterization were used to prepare hyperimmune monovalent serum against respective polypeptides independently and a mixture of all five in poultry birds, and specificity confirmation of each antiserum through dot blot and Western blotting. Antiserum generated from various group birds was pooled and evaluated in 2-week old broiler chicken, for its protection against viral challenge. To evaluate in-vivo protection of each antiserum against viral challenges, six groups of 2-week old broiler chicken were injected with antiserum and a seventh control group received normal saline. Each group was exposed to purified highly pathogenic AIV H7N3 strain at a dose 10(5) embryo lethal dose (ELD(50)). We observed that nucleoprotein (NP) antiserum significantly protected birds from viral infection induced morbidity, mortality and lowered viral shedding compared with antiserum from individual viral proteins or mixed polypeptides/proteins inclusive of NP component. The capability of individual viral polypeptide specific antisera to protect against viral challenges in decreasing order was nucleoprotein (NP) > hemagglutinin (HA) > neuraminidase (NA) > viral proteins mix > viral polymerase (PM) > non-structural proteins (NS). Our data provide proof of concept for potential utilization of passive immunization in protecting poultry industry during infection outbreaks. Furthermore conserved nature of avian NP makes it an ideal candidate to produce antiserum protective against viral infection.


Assuntos
Anticorpos Antivirais/farmacologia , Galinhas/imunologia , Soros Imunes/farmacologia , Imunização Passiva , Vírus da Influenza A/imunologia , Influenza Aviária/prevenção & controle , Peptídeos/imunologia , Animais , Anticorpos Antivirais/imunologia , Embrião de Galinha , Galinhas/virologia , Soros Imunes/imunologia , Influenza Aviária/imunologia , Influenza Aviária/virologia , Nucleoproteínas/imunologia , Proteínas Virais/imunologia
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