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11.
Aamer Saeed Gufran Saddique Pervaiz Ali Channar Fayaz Ali Larik Qamar Abbas Mubashir Hassan Hussain Raza Tanzeela Abdul Fattah Sung-Yum Seo 《Bioorganic & medicinal chemistry》2018,26(12):3707-3715
To seek the new medicinal potential of sulfadiazine drug, the free amino group of sulfadiazine was exploited to obtain acyl/aryl thioureas using simple and straightforward protocol. Acyl/aryl thioureas are well recognized bioactive pharmacophore containing moieties. A new series (4a–4j) of sulfadiazine derived acyl/aryl thioureas was synthesized and characterized through spectroscopic and elemental analysis. The synthesized derivatives 4a–4j were subjected to calf intestinal alkaline phosphatase (CIAP) activity. The derivative 4a–4j showed better inhibition potential compared to standard monopotassium phosphate (MKP). The compound 4c exhibited higher potential in the series with IC50 0.251?±?0.012?µM (standard KH2PO4 4.317?±?0.201?µM). Lineweaver-Burk plots revealed that most potent derivative 4c inhibition CIAP via mixed type pathway. Pharmacological investigations showed that synthesized compounds 4a–4j obey Lipinsk’s rule. ADMET parameters evaluation predicted that these molecule show significant lead like properties with minimum possible toxicity and can serve as templates in drug designing. The synthetic compounds show none mutagenic and irritant behavior. Molecular docking analysis showed that compound 4c interacts with Asp273, His317 and Arg166 amino acid residues. 相似文献
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Sandoo A Carroll D Metsios GS Kitas GD Veldhuijzen van Zanten JJ 《Arthritis research & therapy》2011,13(3):R99
Introduction
Patients with rheumatoid arthritis (RA) are at an increased risk for cardiovascular disease (CVD). One of the earliest manifestations of CVD is endothelial dysfunction (ED). ED can occur in both the microcirculation and the macrocirculation, and these manifestations might be relatively independent of each other. Little is known about the association between endothelial function in the microcirculation and the macrocirculation in RA. The objectives of the present study were to examine the relationship between microvascular and macrovascular endothelial function in patients with RA. 相似文献13.
Bacillus thuringiensis is an insecticidal bacterium whose chitinolytic system may be exploited to improve the insecticidal system of Bt-crops. A
nucleotide fragment of 1368 bp from B. thuringiensis serovar konkukian S4, containing the complete coding sequence of the chitin binding protein Cbp50, was cloned and sequenced. Analyses have shown the protein to contain a modular structure consisting of an N-terminal CBM33 domain, two copies of a
fibronectin-like domain and a C-terminal chitin binding domain classified as CBM5. The Cbp50 protein was heterologously expressed
in Escherichia coli, purified and assessed for chitin binding activity. A deletion mutant (CBD-N; containing only the N-terminal CBM33 domain)
of Cbp50 was produced to determine the role of C-terminal domains in the binding activity of the protein. The full-length
Cbp50 was shown to bind β-chitin most efficiently followed by α-chitin, colloidal chitin and cellulose. The polysaccharide
binding activity of CBD-N was drastically decreased. The data demonstrate that both the N-terminal and C-terminal domains
of Cbp50 are essential for the efficient binding of chitin. The purified Cbp50 showed antifungal activity against the phytopathogenic
fungus Fusarium oxysporum and the opportunistic human pathogen Aspergillus niger. This is the first report of a modular chitin binding protein in bacteria. 相似文献
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Hamaad Raza Ahmad Muhammad Fahad Sardar Muhammad Aamer Maqsood Muhammad Zia Ur Rehman Changxiong Zhu 《人类与生态风险评估》2020,26(7):1810-1831
Abstract Potentially toxic elements and particulate matter (PM) in the ecosystem are regarded as extremely hazardous because of their persistence, toxicity and bioaccumulative characteristics. Therefore, present study was conducted to estimate the ecological and human health risks of potentially toxic elements (Cu, Mn, Pb, Cd and Ni) and particle pollution (TSP, PM10 and PM2.5) at 2 and 60 m roadside distance from 15 different sites at dust polluted megacity of Pakistan. The AQI assessments suggested that the majority of sites were found unhealthy for sensitive at 2 and 60 m roadside distance, which reveals that that quality of road pavement and streets are far below than the required standards resulting huge quantity of dust particles suspended in air by natural and anthropogenic activities. The maximum geo-accumulation index (I geo) values (1.47 and 0.52) and pollution index (PI) values (4.18 and 2.15) were observed for Ni at 2 and 60 m distance away from the muddy edge of the roads. Similarly, maximum contamination factor (CF) values (24.5 and 94.5) and ecological risk index (ERI) values (4.11 and 3.15) were found for Cd at 2 and 60 m. The I geo and PI indicated that the road dust at a distance of 2 m was relatively more contaminated as compared to 60 m roadside distance. Highest cancer risk (CR) values (2.33 adult and 10.9 for children) were observed for Pb at 2 m, while highest CR values (1.21 for adult and 5.67 for children) at 60 m distance. No probable health risk was observed as the total hazard index (HIexp) of all potentially toxic elements was <1. However, children were appeared to be more susceptible to potentially toxic elements. Based on the results, we believe that the exponential increase in traffic load and industries have aggravated the pollution level and it is expected to be increased in the future. 相似文献
15.
Samreen Tayyaba Imran Muhammad Zahir Zahir Ahmad Nazir Muhammad Zulqernain Noureen Saima Bashir Safdar Kanwal Sehrish Munir Hassan Maqsood Muhammad Aamer 《Journal of Plant Growth Regulation》2022,41(6):2462-2475
Journal of Plant Growth Regulation - Many agricultural soils fail to supply sufficient boron (B) and phosphorus (P) to growing plants due to their adsorption, precipitation and fixation phenomena.... 相似文献
16.
Irfan Ullah Arshad Javaid Zarfishan Tahir Obaid Ullah Aamer Ali Shah Fariha Hasan Najma Ayub 《PloS one》2016,11(1)
Background
Drug resistant tuberculosis (DR-TB) is a major public health problem in developing countries such as Pakistan.Objective
The current study was conducted to assess the frequency of drug resistant tuberculosis including multi drug resistance (MDR- TB) as well as risk factors for development of DR-TB, in Punjab, Pakistan.Methodology
Drug susceptibility testing (DST) was performed, using proportion method, for 2367 culture positive Mycobacterium tuberculosis (MTB) cases that were enrolled from January 2012 to December 2013 in the province of Punjab, Pakistan, against first-line anti-tuberculosis drugs. The data was analyzed using statistical software; SPSS version 18.Results
Out of 2367 isolates, 273 (11.5%) were resistant to at least one anti-TB drug, while 221 (9.3%) showed MDR- TB. Risk factors for development of MDR-TB were early age (ranges between 10–25 years) and previously treated TB patients.Conclusion
DR-TB is a considerable problem in Pakistan. Major risk factors are previous history of TB treatment and younger age group. It emphasizes the need for effective TB control Program in the country. 相似文献17.
Ziaullah Shah Lee Krumholz Deniz Fulya Aktas Fariha Hasan Mutiullah Khattak Aamer Ali Shah 《Biodegradation》2013,24(6):865-877
A polyurethane (PU) degrading bacterial strain MZA-75 was isolated from soil through enrichment technique. The bacterium was identified through 16S rRNA gene sequencing, the phylogenetic analysis indicated the strain MZA-75 belonged to genus Bacillus having maximum similarity with Bacillus subtilis strain JBE0016. The degradation of PU films by strain MZA-75 in mineral salt medium (MSM) was analyzed by scanning electron microscopy (SEM), fourier transform infra-red spectroscopy (FT-IR) and gel permeation chromatography (GPC). SEM revealed the appearance of widespread cracks on the surface. FTIR spectrum showed decrease in ester functional group. Increase in polydispersity index was observed in GPC, which indicates chain scission as a result of microbial treatment. CO2 evolution and cell growth increased when PU was used as carbon source in MSM in Sturm test. Increase in both cell associated and extracellular esterases was observed in the presence of PU indicated by p-Nitrophenyl acetate (pNPA) hydrolysis assay. Analysis of cell free supernatant by gas chromatography–mass spectrometry (GC–MS) revealed that 1,4-butanediol and adipic acid monomers were produced. Bacillus subtilis strain MZA-75 can degrade the soft segment of polyester polyurethane, unfortunately no information about the fate of hard segment could be obtained. Growth of strain MZA-75 in the presence of these metabolites indicated mineralization of ester hydrolysis products into CO2 and H2O. 相似文献
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Qazi A Pal J Maitah M Fulciniti M Pelluru D Nanjappa P Lee S Batchu RB Prasad M Bryant CS Rajput S Gryaznov S Beer DG Weaver DW Munshi NC Goyal RK Shammas MA 《Translational oncology》2010,3(6):389-399
INTRODUCTION: The incidence of Barrett esophageal adenocarcinoma (BEAC) has been increasing at an alarming rate in western countries. In this study, we have evaluated the therapeutic potential of sulforaphane (SFN), an antioxidant derived from broccoli, in BEAC. METHODS: BEAC cells were treated with SFN, alone or in combination with chemotherapeutic, paclitaxel, or telomerase-inhibiting agents (MST-312, GRN163L), and live cell number determined at various time points. The effect on drug resistance/chemosensitivity was evaluated by rhodamine efflux assay. Apoptosis was detected by annexin V labeling and Western blot analysis of poly(ADP-ribose) polymerase cleavage. Effects on genes implicated in cell cycle and apoptosis were determined by Western blot analyses. To evaluate the efficacy in vivo, BEAC cells were injected subcutaneously in severe combined immunodeficient mice, and after the appearance of palpable tumors, mice were treated with SFN. RESULTS: SFN induced both time- and dose-dependent decline in cell survival, cell cycle arrest, and apoptosis. The treatment with SFN also suppressed the expression of multidrug resistance protein, reduced drug efflux, and increased anticancer activity of other antiproliferative agents including paclitaxel. A significant reduction in tumor volume was also observed by SFN in a subcutaneous tumor model of BEAC. Anticancer activity could be attributed to the induction of caspase 8 and p21 and down-regulation of hsp90, a molecular chaperon required for activity of several proliferation-associated proteins. CONCLUSIONS: These data indicate that a natural product with antioxidant properties from broccoli has great potential to be used in chemoprevention and treatment of BEAC. 相似文献
20.
Santha Kumari Merugu V. B. R. Krishnan K Dr. Ravi Kumar K Dr. Siddique Akber Ansari Dr. Irfan Aamer Ansari Prof. Dr. Hari Babu Bollikolla 《化学与生物多样性》2023,20(8):e202201158
An efficient 1,4-dihydropyridine synthesis under mild conditions has been developed. Numerous substrates were tested, with yields of 1,4-dihydropridines ranging from good to excellent and a wide range of functional group tolerance. A549, HT-29, and HepG2 cancer cells were used to investigate the anticancer efficacy of each of the produced compounds. Additionally, in-silico docking studies were conducted to understand the structure-based features of the anticancer mechanism with the cancer medication target of Adenosine A2A receptor as well as the molecular level interactions of the compounds. 相似文献