Nazar Ul Islam | Sarhad University of Science & Information Technology (original) (raw)

Papers by Nazar Ul Islam

Gold and silver nanoparticles (Au-and Ag-NPs) were biosynthesized using the gum extract of Prunus... more Gold and silver nanoparticles (Au-and Ag-NPs) were biosynthesized using the gum extract of Prunus armeniaca. These were characterized with UV–Vis spectroscopy, FTIR, SEM, EDX, XRD and atomic absorption (AA). The effect of gum and metal ions concentration, reaction temperature and time on the synthetic stability of nanoparticles was studied along with their post-synthetic stability against varying pH and salt concentrations, long term storage and extreme of temperature. Au-and Ag-NPs were also tested for antibacterial, antinociceptive and anti-inflammatory activities. Formation of Au-and Ag-NPs was confirmed from the surface plasmon resonance centered at 555 and 450 nm respectively and was further corroborated from the results of FTIR, EDX, XRD and AA. SEM analysis showed that Au-and Ag-NPs were mostly spherical and in the size range of 5–40 nm. It was observed that 0.5% w/v gum, 3 mM Au/Ag ions solution, reaction temperature of 80 °C and reaction time of 4 h were suitable for the efficient synthesis of Au-and Ag-NPs. The results of post-synthetic stability revealed that Au-and Ag-NPs were stable in different concentrations of NaCl (1–3 M), neutral to acidic pH (7–2) and without any long term storage (eight months) or thermal (100 °C) induced degradable changes. The TGA spectrum further confirmed their thermal stability, where three successive weight losses were observed in the temperature range of 50–800 °C. Au-and Ag-NPs possessed mild to moderate antibacterial activity as observed from their zone of inhibition against Staphylococcus aureus (10 ± 0.3 mm, 18 ± 0.5 mm), Escherichia coli (9 ± 0.5 mm, 10.2 ± 0.8 mm) and Pseudomonas aeruginosa (7.9 ± 0.3 mm, 11.2 ± 0.3 mm). Au-NPs significantly alleviated the acetic acid induced writhes

Pakistan Journal of Biological Sciences, 2007

Hydro-ethanolic crude extract of Hypericum perforatum Linn. family hypericaceae (St. John&#39... more Hydro-ethanolic crude extract of Hypericum perforatum Linn. family hypericaceae (St. John's Wort) aerial parts (Hp. Cr) was studied for its possible antinociceptive effect against acetic acid-induced abdominal constriction assay in mice. Hp. Cr (10-20 mg kg(-1)), opium (10-30 mg kg(-1)), morphine (0.75-3.0 mg kg(-1)) and aspirin (50-100 mg kg(-1)) showed dose-dependent antinociceptive effect. In animals treated with naloxone (0.5 mg kg(-1)), the antinociceptive effect of Hp. Cr was significantly reduced similar to that of opium, while effect of aspirin remained unchanged. These results suggest that the antinociceptive effect of Hypericum perforatum may be mediated through activation of opioid receptors.

The carboxylic acid group (–COOH) present in classical NSAIDs is partly responsible for the gastr... more The carboxylic acid group (–COOH) present in classical NSAIDs is partly responsible for the gastric toxicity associated with the administration of these drugs. This concept has been extensively proven using NSAID prodrugs. However, the screening of NSAIDs with no carboxylic
acid at all has been neglected. The goal of this work was to determine if new NSAID derivatives devoid of acidic moieties would retain the anti-inflammatory activity of the parent compound, without causing gastric toxicity. To test this concept, we replaced the carboxylic acid group in ibuprofen, flurbiprofen, and naproxen with three ammonium moieties. We tested the resulting water-soluble NSAID derivatives for anti-inflammatory and ulcerogenic activity in vitro and
in vivo. In this regard, we observed that all non-acidic NSAIDs exerted a potent anti-inflammatory activity, suggesting that the acid group in commercial 2-phenylpropionic acid NSAIDs not be an essential requirement for anti-inflammatory activity. These data provide complementary evidence supporting the discontinuation of ulcerogenic acidic NSAIDs.

Archives of Pharmacal Research, 2013

The aim of the current study was to explore in vivo any relative gastroulcerogenic prospective pr... more The aim of the current study was to explore in vivo any relative gastroulcerogenic prospective propensity of newly synthesized nitrogen containing derivatives of salicyl alcohol; compound (I) [1-(2-hydroxybenzyl) piperidinium chloride], compound (II) [4-carbamoyl-1-(2hydroxybenzyl)piperidinium chloride] and aspirin in albino rats. The experimental groups received the following oral treatments daily for 6 days: group I saline control; group II, standard (aspirin) treatment group [150 mg/kg of body weight]; group III, test (compound I) treatment group [100, 150 mg/kg]; group IV, test (compound II) treatment group [100, 150 mg/kg]. The results showed that in the case of the aspirin treated group and compound (I) [150 mg/kg], there was a significant increase in gastric volume, free acidity, total acidity, ulcer score and a decrease in gastric pH.

Background: Conjugated and drug loaded silver nanoparticles are getting an increased attention fo... more Background: Conjugated and drug loaded silver nanoparticles are getting an increased attention for various biomedical applications. Nanoconjugates showed significant enhancement in biological activity in comparison to free drug molecules. In this perspective, we report the synthesis of bioactive silver capped with 5-Amino-β-resorcylic acid hydrochloride dihydrate (AR). The in vitro antimicrobial (antibacterial, antifungal), enzyme inhibition (xanthine oxidase, urease, carbonic anhydrase, α-chymotrypsin, cholinesterase) and antioxidant activities of the developed nanostructures was investigated before and after conjugation to silver metal. Results: The conjugation of AR to silver was confirmed through FTIR, UV-vis and TEM techniques. The amount of AR conjugated with silver was characterized through UV-vis spectroscopy and found to be 9% by weight. The stability of synthesized nanoconjugates against temperature, high salt concentration and pH was found to be good. Nanoconjugates, showed significant synergic enzyme inhibition effect against xanthine and urease enzymes in comparison to standard drugs, pure ligand and silver. Conclusions: Our synthesized nanoconjugate was found be to efficient selective xanthine and urease inhibitors in comparison to Ag and AR. On a per weight basis, our nanoconjugates required less amount of AR (about 11 times) for inhibition of these enzymes.

Naunyn-Schmiedeberg's Archives of Pharmacology, 2014

The present study was conducted to synthesize nitrogen containing derivatives of salicyl alcohol ... more The present study was conducted to synthesize nitrogen containing derivatives of salicyl alcohol and to investigate in vivo their ulcerogenic potential in comparison with aspirin in rats. The compounds [4-(2-hydroxybenzyl) morpholin-4-iumchloride (I)] and [1,4-bis(2-hydroxybenzyl) piperazine-1,4-diium chloride (II)] were synthesized and their chemical structures were characterized using spectral data. In our previous study (Ali et al., Afr J Pharm Pharmacol 7:585-596, 2013), both compounds showed anti-inflammatory, antinociceptive, and antipyretic properties in standard animal models and a greater binding affinity for cyclooxygenase-2 versus cyclooxygenase-1 in molecular docking and dynamics analysis. For in vivo studies, animals were randomly divided into four groups. The synthetic compounds (both at 100 or 150 mg/kg), aspirin (150 mg/kg), or saline vehicle was administered orally, once daily for 6 days and then tested for ulcerogenic activity. At the end of the procedure, gastric juice and tissues were collected and subjected to biochemical and histological analyses. The results of the study revealed that in the case of the aspirin-treated group, there was a significant increase in gastric juice volume, free acidity, total acidity, and ulcer score and a decrease in gastric pH. Moreover, histological examination of the gastric mucosa of the aspirin-treated group indicated morphological changes while neither of the synthetic compounds showed any significant ulcerogenic or cytotoxic properties. The results of the present study suggest that both compounds are free from ulcerogenic side effects and may represent a better alternative to aspirin.

In the present study, gold nanoparticles (GNPs) were prepared at boiling temperature (90-95oC) b... more In the present study, gold nanoparticles (GNPs) were prepared at boiling temperature (90-95oC) by treating gold ions with Citrus fruit extracts. The effect of mixing ratios of the reactants and concentration of gold hydrochloride was studied. In the standardization process, 10-3 M solution
of HAuCl4.3H2O was reacted with fruit extracts for half an hour at 90-95o C in different ratios. GNPs were characterized by UV-Vis spectroscopy (UV-Vis) and atomic force microscopy (AFM). Their stability was evaluated against varying pH solutions and volumes of sodium chloride along with metals and antibiotics sensing ability. The gold nanoparticles were tested for antibacterial and antifungal activities against various pathogenic strains. The UV-Vis spectra of gold nanoparticles gave surface plasmon resonance at about 540 nm while the AFM images revealed the particle size within the range of 70-100 nm. GNPs showed remarkable stability in varying pH solutions and salt volumes as well as high detection ability towards cobalt, copper, ceftriaxone and penicillin. Moreover, the GNPs possessed moderate antibacterial and good antifungal activity. These results
concluded that the Citrus fruit extracts can be utilized for large scale synthesis of cost-effective nanoparticles which may have compatibility for biomedical and pharmaceutical applications.

Background: Nanotechnology has potential future for enhancing therapeutic efficacy and reducing t... more Background: Nanotechnology has potential future for enhancing therapeutic efficacy and reducing the unwanted
effects of herbal drugs. The biological research on Euphorbia species has been supported by the use of some plants in traditional medicines. Many species of Euphorbia have been reported as having strong sedative and analgesic effects. In the present research work gold nanoparticles of Euphorbia milii methanolic extract (Au-EM) were synthesized, characterized and tested for antinociceptive, muscle relaxant and sedative activities.
Methods: Au-EM was prepared by stirring 1 mM warm trihydrated tetrachloroaurate solution with E. milii methanolic
extract without using any external reducing agents. The gold nanoparticles were characterized by UV-Visible spectroscopy
infrared spectrophotometery, atomic force microscopy and scanning electron microscopy while their stability was
evaluated against varying pH and different volumes of sodium chloride (NaCl). The metal sensing capacity of
Au-EM was tested towards cobalt, copper, lead, mercury and nickel. Au-EM was evaluated in BALB/c mice at a dose of 10 and 20 mg/kg for antinociceptive, muscle relaxant and sedative activities in comparison with the crude E. milii methanolic extract.
Results: Au-EM showed remarkable stability in different NaCl and pH solutions. Au-EM produced significant (P < 0.01) antinociceptive effect at doses of 10 and 20 mg/kg as compared to the crude E. milii methanolic extract
In the rotarod test, Au-EM showed significant muscle relaxant effect at 10 mg/kg (P <0.05)and20mg/kg(P <0.01) after 30, 60 and 90 min. In an open field test significant sedative effect (P < 0.05) of Au-EM was observed at 10 and 20 mg/kg. Moreover significant detection sensitivity was demonstrated towards all the tested heavy metals.
Conclusions: These results concluded that the gold nanoparticles improved the potency of E. milii methanolic extract
and exhibited significant analgesic, muscle relaxant and sedative properties. The significant metals sensing ability and
enhanced stability in different NaCl and pH solutions may enable us to explore different formulations of E. milii gold
nanoparticles for potentially effective and safe nano-herbal therapy.

This paper reports a rapid, facile and one-pot synthesis of environmentally safe gold nanopartic... more This paper reports a rapid, facile and one-pot synthesis of environmentally safe gold nanoparticles capped and stabilized with galls extract of Pistacia integerrima. The aqueous gold ions when exposed to P. integerrima galls extract were rapidly reduced as evident from abrupt color
change to ruby red, suggesting the biosynthesis of gold nanoparticles (Au-NPs) which were further characterized by UV–Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR) and Scanning electron microscopy (SEM). Their stability was evaluated against varying pH and different volumes of sodium chloride (NaCl) as well as at a range of temperature (20–80 C). Au-NPs were tested for enzyme inhibition, antibacterial, antifungal, antinociceptive, muscle relaxant and
sedative activities. The UV–Vis spectra of the gold nanoparticles gave surface plasmon resonance at 540 nm while the SEManalysis revealed the particle size in the range of 20–200 nm. FTIR spectra conﬁrmed the involvement of amines, amide groups and alcohols in capping and reduction of gold nanoparticles. Au-NPs showed remarkable stability in different NaCl and pH solutions as well as at elevated temperature. Au-NPs have good antifungal activity and possessed antinociceptive and muscle relaxant properties as observed from their zone of inhibition and signiﬁcant attenuation of acetic acid induced writhing and reduction of time spent on the rota rod respectively. These results concluded that the gall extract of P. integerrima is a very good bioreductant for the synthesis of gold nanoparticles that have potential for various biomedical and harmaceutical applications.

Abstract This study reports a facile and reproducible green extracellular synthetic route of high... more Abstract This study reports a facile and reproducible green extracellular synthetic route of highly stable gold nanoparticles. The aqueous gold ions when exposed to Salix alba L. leaves extract were bioreduced and resulted in the biosynthesis of gold nanoparticles (Au-WAs). The anoparticles
were characterized by UV–Visible spectroscopy (UV–Vis), Fourier transform infrared spectroscopy (FTIR), atomic force microscopy (AFM) and scanning electron microscopy (SEM). Their stability was evaluated against varying volumes of pH and sodium chloride as well as at elevated temperature along with enzymes inhibition, antibacterial, antifungal, anti-nociceptive, muscle relaxant and sedative activities. The UV–Vis spectra of the gold nanoparticles gave surface
plasmon resonance at 540 nm while the AFM and SEM nanoparticles analyses revealed the particle size of 63 nm and 50–80 nm respectively. FTIR spectra conﬁrmed the involvement of amines, amide and aromatic groups
in capping and reduction of the gold nanoparticles. Au-WAs showed remarkable stability in different volumes of salt and various pH solutions however, Au-WAs were relatively unstable at elevated temperature. Au-WAs possessed good antifungal activity and showed signiﬁcant antinociceptive and muscle relaxant properties. These results revealed that the leaves extract of S. alba is a very good bio-reductant for the synthesis of gold nanoparticles that have potential for various biomedical and pharmaceutical applications.

Bioisosterism has unique relevance in the field of pharmaceutical sciences and is conducted to cu... more Bioisosterism has unique relevance in the field of pharmaceutical sciences and is conducted to curtail side effects or to alter the biological activity of a lead molecule. In the biomedical field, the aim of exchanging one bioisostere for another is to boost the preferred pharmacological, biological or physical qualities of a substance without making substantial changes in the chemical skeleton. A vital feature of medicinal chemistry has been to ascertain a correlation between chemical skeleton of drugs and their physicochemical properties and in turn such properties modify the pharmacological properties and consequently the therapeutic response of drugs. Drugs with analogous structures often are liable to have comparable pharmacological properties. The present review highlights the vital role of bioisosterism as a special approach of structural modification and optimization process in drug design programme with clear 2D and 3D structural drawings.

Journal of Chemical Crystallography, 2009

Abstract The reaction of Cu(OOCCH3)2·H2O with (2,4-diamino-5-(3′,4′,5′-trimethoxybenzyl) pyrimidi... more Abstract The reaction of Cu(OOCCH3)2·H2O with (2,4-diamino-5-(3′,4′,5′-trimethoxybenzyl) pyrimidine (trimethoprim) in ethanolic solution at 80 °C affords the title complex which has been characterized by elemental, IR, and NMR (1H and 13C).The crystal structure has been determined by single crystal X-ray diffraction. Compound 1 (C36H48Cu2N8O14) is triclinic, space group P-1 with a = 7.2676(4) Å, b = 11.6721(7) Å, c = 12.8279(8) Å, α = 95.839(1)°, β = 93.456(1)°, γ = 105.541(1)°, Z = 1. Two copper atoms are coordinated directly to each other as well as are held together by four bridging aceto groups. Each copper atom is also bonded opposite the Cu–Cu vector to a trimethoprim molecule through the N(1) atom of the pyrimidine ring. Trimethoprim acts as a monodentate ligand through the pyrimidine nitrogen N(1) atom. The complex was screened for the activity against several bacteria, showing more activity against bacteria as compared to trimethoprim. Graphical Abstract To enhance the activity of trimethoprim, its derivative was prepared and there bacterial activity against several bacteria was analyzed.

) piperazine-1,4-diium chloride (II)]. The synthetic compound I, II and standard (aspirin) were e... more ) piperazine-1,4-diium chloride (II)]. The synthetic compound I, II and standard (aspirin) were evaluated in the laboratory animal model at three different dose levels for each activity. These compounds were examined for, anti-inflammatory activity in carrageenan induced paw edema model [50, 100 and 150 mg/kg intraperitoneally (i.p)], antinociceptive properties in acetic acid induced writhing model (15, 30 and 45 mg/kg i.p), hot plate test model (30 and 45 mg/kg i.p) and antipyretic activity in Brewer's yeast induced pyrexia model (50,100 and 150 mg/kg i.p), using Swiss albino mice.

Multinuclear NMR and M6ssbauer spectroscopy have been carried out for di-and triorganotin carboxy... more Multinuclear NMR and M6ssbauer spectroscopy have been carried out for di-and triorganotin carboxylates derived from 3-(-2-furanyl)-2-propenoic acid. Their spectroscopic characterization showed that triorganotin carboxylates are either 4-coordinate monomers or 5-coordinate polymers with bridging carboxylate groups. Although a polymeric structure is favoured for most compounds in the solid state, the solution studies indicated that they exist as monomeric 4-coordinate species in non-coordinating solvents. Diorganotin carboxylates of the general formula R2Sn(OOCCHCHC4H30) 2 and dimeric [(R2SnOOCCHCH-C4H30)20]2 are penta-coordinate in noncoordinating solvents while in the solid phase intra-or intermolecular interactions are possible. Moreover, we report the fluxional behaviour of carboxylate anions in dimeric distannoxanes. The biological activity of these organotin carboxylates proved them to be powerful biocides.

Purple acid phosphatases (PAPs) are binuclear metallohydrolases that have a multitude of biologic... more Purple acid phosphatases (PAPs) are binuclear metallohydrolases that have a multitude of biological functions and are found in fungi, bacteria, plants and animals. In mammals, PAP activity is linked with bone resorption and over-expression can lead to bone disorders such as osteoporosis. PAP is therefore an attractive target for the development of drugs to treat this disease. A series of penicillin conjugates, in which 6-aminopenicillanic acid was acylated with aromatic acid chlorides, has been prepared and assayed against pig PAP. The binding mode of most of these conjugates is purely competitive, and some members of this class have potencies comparable to the best PAP inhibitors yet reported. The structurally related penicillin G was shown to be neither an inhibitor nor a substrate for pig PAP. Molecular modelling has been used to examine the binding modes of these compounds in the active site of the enzyme and to rationalise their activities.

The production of metallo-β-lactamases is the most important strategy by which pathogenic bacteri... more The production of metallo-β-lactamases is the most important strategy by which pathogenic bacteria become resistant to currently known β-lactam antibiotics. The emergence of these enzymes is particularly concerning for the future treatment of bacterial infections. There are no clinically available drugs capable of inhibiting any of the metallo-β-lactamases, so there is an urgent need to find such inhibitors. In this review, an up-to-date status of the inhibitors investigated for the inhibition of metallo-β-lactamases has been given so that this rich source of structural information of presently known metallo-β-lactamases could be helpful in generating a broad-spectrum potent inhibitor of metallo-β-lactamases.

This communication reports facile one pot synthesis of amoxicillin and sodium salt of amoxicillin... more This communication reports facile one pot synthesis of amoxicillin and sodium salt of amoxicillin stabilized gold nanoparticles (Au-NPs). Primarily the cyclic thioether linkage i.e. the thiozolidine ring of amoxicillin is utilized for sequestering Au(III). Fluorescence quenching of these clusters makes it an efficient protocol for sensing Cu 2+ at nano scale levels.

Pakistan Journal of Biological Sciences, 2007

Archives of Pharmacal Research, 2013

Naunyn-Schmiedeberg's Archives of Pharmacology, 2014

Journal of Chemical Crystallography, 2009