Displaying publications 1 - 20 of 57 in total

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  1. Fulltext Synthesis of 2,3-dioxo-5-(substituted)-arylpyrroles and their 2-oxo-5-aryl-3-hydrazone pyrrolidine derivatives
    Mohammat MF, Shaameri Z, Hamzah AS
    Molecules, 2009;14(1):250-6.
    PMID: 19136912 DOI: 10.3390/molecules14010250
    Some novel 2,3-dioxo-5-(substituted)-arylpyrroles have been synthesized. Among these, pyrrolidine compound 1b was converted to 2,3-dioxo-5-aryl pyrrolidine 2b. Finally a set of hydrazone derivatives was obtained from the reaction of 2b with various hydrazine salts. The structures of all the new synthesized compounds were confirmed by elemental analyses, IR and 1H-NMR spectra.
    Matched MeSH terms: Pyrroles/chemical synthesis*; Pyrroles/chemistry
  2. Synthesis and application of polypyrrole/carrageenan nano-bio composite as a cathode catalyst in microbial fuel cells
    Esmaeili C, Ghasemi M, Heng LY, Hassan SHA, Abdi MM, Daud WRW, et al.
    Carbohydr Polym, 2014 Dec 19;114:253-259.
    PMID: 25263889 DOI: 10.1016/j.carbpol.2014.07.072
    A novel nano-bio composite polypyrrole (PPy)/kappa-carrageenan(KC) was fabricated and characterized for application as a cathode catalyst in a microbial fuel cell (MFC). High resolution SEM and TEM verified the bud-like shape and uniform distribution of the PPy in the KC matrix. X-ray diffraction (XRD) has approved the amorphous structure of the PPy/KC as well. The PPy/KC nano-bio composites were then studied as an electrode material, due to their oxygen reduction reaction (ORR) ability as the cathode catalyst in the MFC and the results were compared with platinum (Pt) as the most common cathode catalyst. The produced power density of the PPy/KC was 72.1 mW/m(2) while it was 46.8 mW/m(2) and 28.8 mW/m(2) for KC and PPy individually. The efficiency of the PPy/KC electrode system is slightly lower than a Pt electrode (79.9 mW/m(2)) but due to the high cost of Pt electrodes, the PPy/KC electrode system has potential to be an alternative electrode system for MFCs.
    Matched MeSH terms: Pyrroles/chemistry*
  3. Simultaneous removal of potent cyanotoxins from water using magnetophoretic nanoparticle of polypyrrole: adsorption kinetic and isotherm study
    Hena S, Rozi R, Tabassum S, Huda A
    Environ Sci Pollut Res Int, 2016 Aug;23(15):14868-80.
    PMID: 27072032 DOI: 10.1007/s11356-016-6540-5
    Cyanotoxins, microcystins and cylindrospermopsin, are potent toxins produced by cyanobacteria in potable water supplies. This study investigated the removal of cyanotoxins from aqueous media by magnetophoretic nanoparticle of polypyrrole adsorbent. The adsorption process was pH dependent with maximum adsorption occurring at pH 7 for microcystin-LA, LR, and YR and at pH 9 for microcystin-RR and cylindrospermopsin (CYN). Kinetic studies and adsorption isotherms reflected better fit for pseudo-second-order rate and Langmuir isotherm model, respectively. Thermodynamic calculations showed that the cyanotoxin adsorption process is endothermic and spontaneous in nature. The regenerated adsorbent can be successfully reused without appreciable loss of its original capacity.
    Matched MeSH terms: Pyrroles/chemistry*
  4. Comprehensive insight into the binding of sunitinib, a multi-targeted anticancer drug to human serum albumin
    Kabir MZ, Tee WV, Mohamad SB, Alias Z, Tayyab S
    Spectrochim Acta A Mol Biomol Spectrosc, 2017 Jun 15;181:254-263.
    PMID: 28376387 DOI: 10.1016/j.saa.2017.03.059
    Binding studies between a multi-targeted anticancer drug, sunitinib (SU) and human serum albumin (HSA) were made using fluorescence, UV-vis absorption, circular dichroism (CD) and molecular docking analysis. Both fluorescence quenching data and UV-vis absorption results suggested formation of SU-HSA complex. Moderate binding affinity between SU and HSA was evident from the value of the binding constant (3.04×104M-1), obtained at 298K. Involvement of hydrophobic interactions and hydrogen bonds as the leading intermolecular forces in the formation of SU-HSA complex was predicted from the thermodynamic data of the binding reaction. These results were in good agreement with the molecular docking analysis. Microenvironmental perturbations around Tyr and Trp residues as well as secondary and tertiary structural changes in HSA upon SU binding were evident from the three-dimensional fluorescence and circular dichroism results. SU binding to HSA also improved the thermal stability of the protein. Competitive displacement results and molecular docking analysis revealed the binding locus of SU to HSA in subdomain IIA (Sudlow's site I). The influence of a few common ions on the binding constant of SU-HSA complex was also noticed.
    Matched MeSH terms: Pyrroles/analysis; Pyrroles/metabolism*; Pyrroles/chemistry
  5. Fulltext A comparative analysis of the influence of human salivary enzymes on odorant concentration in three palm wines
    Lasekan O
    Molecules, 2013 Sep 25;18(10):11809-23.
    PMID: 24071987 DOI: 10.3390/molecules181011809
    The influence of human salivary enzymes on palm wines' odorant concentrations were investigated by the application of aroma extracts dilution analysis (AEDA) and by the calculation of odour activity values (OAVs), respectively. The odorants were quantified by means of stable isotope dilution assays (SIDA), and the degradation profiles of odorants by human saliva were also studied. Results revealed 46 odour-active compounds in the flavour dilution (FD) factor range of 4-256, and all were subsequently identified. Of the 46 odorants, 41 were identified in the Elaeis guineensis wine, 36 in Raphia hookeri wine and 29 in Borassus flabellifer wine. Among the odorants, the highest FD-factors were obtained from acetoin, 2-acetyl-1-pyrroline and 3-isobutyl-2-methoxypyrazine. Among the 13 potent odorants identified, five aroma compounds are reported here as important contributors to palm wine aroma, namely 3-isobutyl-2-methoxy-pyrazine, acetoin, 2-acetyl-1-pyrroline, 3-methylbutylacetate and ethyl hexanoate. Meanwhile, salivary enzymic degradation of odorants was more pronounced among the aldehydes, esters and thiols.
    Matched MeSH terms: Pyrroles/chemistry
  6. Fulltext Characterization of electrosynthesized conjugated polymer-carbon nanotube composite: optical nonlinearity and electrical property
    Bahrami A, Talib ZA, Shahriari E, Yunus WM, Kasim A, Behzad K
    Int J Mol Sci, 2012;13(1):918-28.
    PMID: 22312294 DOI: 10.3390/ijms13010918
    The effects of multi-walled carbon nanotube (MWNT) concentration on the structural, optical and electrical properties of conjugated polymer-carbon nanotube composite are discussed. Multi-walled carbon nanotube-polypyrrole nanocomposites were synthesized by electrochemical polymerization of monomers in the presence of different amounts of MWNTs using sodium dodecylbenzensulfonate (SDBS) as surfactant at room temperature and normal pressure. Field emission scanning electron microscopy (FESEM) indicates that the polymer is wrapped around the nanotubes. Measurement of the nonlinear refractive indices (n(2)) and the nonlinear absorption (β) of the samples with different MWNT concentrations measurements were performed by a single Z-scan method using continuous wave (CW) laser beam excitation wavelength of λ = 532 nm. The results show that both nonlinear optical parameters increased with increasing the concentration of MWNTs. The third order nonlinear susceptibilities were also calculated and found to follow the same trend as n(2) and β. In addition, the conductivity of the composite film was found to increase rapidly with the increase in the MWNT concentration.
    Matched MeSH terms: Pyrroles/chemistry
  7. Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors
    Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Perumal S, et al.
    Bioorg Med Chem, 2013 Apr 1;21(7):1696-707.
    PMID: 23454132 DOI: 10.1016/j.bmc.2013.01.066
    Three-component reaction of a series of 1-acryloyl-3,5-bisbenzylidenepiperidin-4-ones with isatin and L-proline in 1:1:1 and 1:2:2 molar ratios in methanol afforded, respectively the piperidone-grafted novel mono- and bisspiro heterocyclic hybrids comprising functionalized piperidine, pyrrolizine and oxindole ring systems in good yields. The in vitro evaluation of cholinesterase enzymes inhibitory activity of these cycloadducts disclosed that monospiripyrrolizines (8a-k), are more active with IC50 ranging from 3.36 to 20.07 μM than either the dipolarophiles (5a-k) or bisspiropyrrolizines (9a-k). The compounds, 8i and 8e with IC50 values of 3.36 and 3.50 μM, respectively showed the maximum inhibition of acethylcholinesterase (AChE) and butrylylcholinestrase (BuChE). Molecular modeling simulation, disclosed the binding interactions of the most active compounds to the active site residues of their respective enzymes. The docking results were in accordance with the IC50 values obtained from in vitro cholinesterase assay.
    Matched MeSH terms: Pyrroles/chemical synthesis; Pyrroles/pharmacology*; Pyrroles/chemistry*
  8. Elucidation of Pyranonigrin Biosynthetic Pathway Reveals a Mode of Tetramic Acid, Fused γ-Pyrone, and exo-Methylene Formation
    Yamamoto T, Tsunematsu Y, Noguchi H, Hotta K, Watanabe K
    Org. Lett., 2015 Oct 16;17(20):4992-5.
    PMID: 26414728 DOI: 10.1021/acs.orglett.5b02435
    Successful activation of the pyranonigrin biosynthetic gene cluster and gene knockout in Aspergillus niger plus in vivo and in vitro assays led to isolation of six new products, including a spiro cyclobutane-containing dimeric compound, which served as the basis for the proposed comprehensive pyranonigrin biosynthetic pathway. Two redox enzymes are key to forming the characteristic fused γ-pyrone core, and a protease homologue performs the exo-methylene formation.
    Matched MeSH terms: Pyrroles/metabolism*; Pyrroles/pharmacology; Pyrroles/chemistry
  9. Fulltext Effects of γ-rays on electrical conductivity of polyvinyl alcohol-polypyrrole composite polymer films
    Mohd Hamzah Harun, Elias Saion, Noorhana Yahya, Anuar Kassim, Hussain, Muhammad Yousuf, Iskandar Shahrim Mustafa, et al.
    Journal of Nuclear and Related Technologies, 2007;2007(1):1-12.
    MyJurnal
    The composite polymer films of polyvinyl alcohol/polypyrrole/chloral hydrate (PVA-PPy-CH) had been prepared. Effects of γ-rays on the electrical conductivity of the composite polymer films had been investigated by using Inductance Capacitance Resistance meter (LCR) meter at a frequency ranging from 20 Hz to 1 MHz. With the incorporation of chloral hydrate in the polymer sample, the conductivity increased indicates that it is capable to be used as dopant for polymerizing conjugated polymer. The electrical conductivity obtained increased as the dose increased, which is in the order of 10-5 Scm-1 indicates that γ-rays is capable to enhance the electrical conductivity of the composite polymer films. The parameter of s is in the range of 0.31 d s d 0.49 and obeyed simple power law dispersion ωs. The Scanning Electron Microscopy (SEM) micrographs reveal the formation of polypyrrole globules in polyvinyl alcohol matrix which increased as the irradiation dose was increased.
    Matched MeSH terms: Pyrroles
  10. Fulltext Effects of j-rays on electrical conductivity of polyvinyl alcohol-polypyrrole composite polymer films
    Mohd Hamzah Harun, Elias Saion, Noorhana Yahya, Anuar Kassim, Ekramul Mahmud, Muhammad Yousuf Hussain, et al.
    Journal of Nuclear and Related Technologies, 2007;2005(1):1-11.
    MyJurnal
    The composite polymer films of polyvinyl alcohol/polypyrrole/chloral hydrate (PVA-PPy-CH) had been prepared. Effects of J-rays on the electrical conductivity of the composite polymer films had
    been investigated by using Inductance Capacitance Resistance meter (LCR) meter at a frequency
    ranging from 20 Hz to 1 MHz. With the incorporation of chloral hydrate in the polymer sample, the conductivity increased indicates that it is capable to be used as dopant for polymerizing conjugated polymer. The electrical conductivity obtained increased as the dose increased, which is in the order of 10-5Scm-1 indicates that J-rays is capable to enhance the electrical conductivity of the composite polymer films. The parameter of s is in the range of 0.31 d s d 0.49 and obeyed simple power law dispersion Zs. The Scanning Electron Microscopy (SEM) micrographs reveal the formation of polypyrrole globules in polyvinyl alcohol matrix which increased as the irradiation dose was increased.
    Matched MeSH terms: Pyrroles
  11. Fulltext Application of an Effective Statistical Technique for an Accurate and Powerful Mining of Quantitative Trait Loci for Rice Aroma Trait
    Golestan Hashemi FS, Rafii MY, Ismail MR, Mohamed MT, Rahim HA, Latif MA, et al.
    PLoS One, 2015;10(6):e0129069.
    PMID: 26061689 DOI: 10.1371/journal.pone.0129069
    When a phenotype of interest is associated with an external/internal covariate, covariate inclusion in quantitative trait loci (QTL) analyses can diminish residual variation and subsequently enhance the ability of QTL detection. In the in vitro synthesis of 2-acetyl-1-pyrroline (2AP), the main fragrance compound in rice, the thermal processing during the Maillard-type reaction between proline and carbohydrate reduction produces a roasted, popcorn-like aroma. Hence, for the first time, we included the proline amino acid, an important precursor of 2AP, as a covariate in our QTL mapping analyses to precisely explore the genetic factors affecting natural variation for rice scent. Consequently, two QTLs were traced on chromosomes 4 and 8. They explained from 20% to 49% of the total aroma phenotypic variance. Additionally, by saturating the interval harboring the major QTL using gene-based primers, a putative allele of fgr (major genetic determinant of fragrance) was mapped in the QTL on the 8th chromosome in the interval RM223-SCU015RM (1.63 cM). These loci supported previous studies of different accessions. Such QTLs can be widely used by breeders in crop improvement programs and for further fine mapping. Moreover, no previous studies and findings were found on simultaneous assessment of the relationship among 2AP, proline and fragrance QTLs. Therefore, our findings can help further our understanding of the metabolomic and genetic basis of 2AP biosynthesis in aromatic rice.
    Matched MeSH terms: Pyrroles/metabolism*; Pyrroles/chemistry
  12. Fulltext Preliminary Insight of Pyrrolylated-Chalcones as New Anti-Methicillin-Resistant Staphylococcus aureus (Anti-MRSA) Agents
    Gunasekharan M, Choi TI, Rukayadi Y, Mohammad Latif MA, Karunakaran T, Mohd Faudzi SM, et al.
    Molecules, 2021 Sep 01;26(17).
    PMID: 34500755 DOI: 10.3390/molecules26175314
    Bacterial infections are regarded as one of the leading causes of fatal morbidity and death in patients infected with diseases. The ability of microorganisms, particularly methicillin-resistant Staphylococcus aureus (MRSA), to develop resistance to current drugs has evoked the need for a continuous search for new drugs with better efficacies. Hence, a series of non-PAINS associated pyrrolylated-chalcones (1-15) were synthesized and evaluated for their potency against MRSA. The hydroxyl-containing compounds (8, 9, and 10) showed the most significant anti-MRSA efficiency, with the MIC and MBC values ranging from 0.08 to 0.70 mg/mL and 0.16 to 1.88 mg/mL, respectively. The time-kill curve and SEM analyses exhibited bacterial cell death within four hours after exposure to 9, suggesting its bactericidal properties. Furthermore, the docking simulation between 9 and penicillin-binding protein 2a (PBP2a, PDB ID: 6Q9N) suggests a relatively similar bonding interaction to the standard drug with a binding affinity score of -7.0 kcal/mol. Moreover, the zebrafish model showed no toxic effects in the normal embryonic development, blood vessel formation, and apoptosis when exposed to up to 40 µM of compound 9. The overall results suggest that the pyrrolylated-chalcones may be considered as a potential inhibitor in the design of new anti-MRSA agents.
    Matched MeSH terms: Pyrroles/pharmacology*; Pyrroles/chemistry
  13. Fulltext Evaluation of the effect of andrographolide on atherosclerotic rabbits induced by Porphyromonas gingivalis
    Al Batran R, Al-Bayaty F, Al-Obaidi MM, Hussain SF, Mulok TZ
    Biomed Res Int, 2014;2014:724718.
    PMID: 25215291 DOI: 10.1155/2014/724718
    Epidemiologic evidence has demonstrated significant associations between atherosclerosis and Porphyromonas gingivalis (Pg). We had investigated the effect of andrographolide (AND) on atherosclerosis induced by Pg in rabbits. For experimental purpose, we separated thirty male white New Zealand rabbits into 5 groups. Group 1 received standard food pellets; Groups 2-5 were orally challenged with Pg; Group 3 received atorvastatin (AV, 5 mg/kg), and Groups 4-5 received 10 and 20 mg/kg of AND, respectively, over 12 weeks. Groups treated with AND showed significant decrease in TC, TG, and LDL levels (P<0.05) and significant increase in HDL level in the serum of rabbits. Furthermore, the treated groups (G3-G5) exhibited reductions in interleukins (IL-1β and IL-6) and C-reactive protein (CRP) as compared to atherogenicgroup (G2). The histological results showed that the thickening of atherosclerotic plaques were less significant in treated groups (G3-G5) compared with atherogenicgroup (G2). Also, alpha-smooth muscle actin (α-SMA) staining decreased within the plaques of atherogenicgroup (G2), while it was increased in treated groups (G3-G5). Lastly, groups treated with AV and AND (G3-G5) showed significant reduction of CD36 expression (P<0.05) compared to atherogenicgroup (G2). These results substantially proved that AND contain antiatherogenic activity.
    Matched MeSH terms: Pyrroles/administration & dosage; Pyrroles/pharmacology; Pyrroles/toxicity
  14. Fulltext In-situ electrochemically deposited polypyrrole nanoparticles incorporated reduced graphene oxide as an efficient counter electrode for platinum-free dye-sensitized solar cells
    Lim SP, Pandikumar A, Lim YS, Huang NM, Lim HN
    Sci Rep, 2014;4:5305.
    PMID: 24930387 DOI: 10.1038/srep05305
    This paper reports a rapid and in-situ electrochemical polymerization method for the fabrication of polypyrrole nanoparticles incorporated reduced graphene oxide (rGO@PPy) nanocomposites on a ITO conducting glass and its application as a counter electrode for platinum-free dye-sensitized solar cell (DSSC). The scanning electron microscopic images show the uniform distribution of PPy nanoparticles with diameter ranges between 20 and 30 nm on the rGO sheets. The electrochemical studies reveal that the rGO@PPy has smaller charge transfer resistance and similar electrocatalytic activity as that of the standard Pt counter electrode for the I₃(-)/I(-) redox reaction. The overall solar to electrical energy conversion efficiency of the DSSC with the rGO@PPy counter electrode is 2.21%, which is merely equal to the efficiency of DSSC with sputtered Pt counter electrode (2.19%). The excellent photovoltaic performance, rapid and simple fabrication method and low-cost of the rGO@PPy can be potentially exploited as a alternative counter electrode to the expensive Pt in DSSCs.
    Matched MeSH terms: Pyrroles
  15. Fulltext Phase III, randomised, double-blind, multicentre study to evaluate the efficacy and safety of vonoprazan compared with lansoprazole in Asian patients with erosive oesophagitis
    Xiao Y, Zhang S, Dai N, Fei G, Goh KL, Chun HJ, et al.
    Gut, 2020 02;69(2):224-230.
    PMID: 31409606 DOI: 10.1136/gutjnl-2019-318365
    OBJECTIVE: To establish the non-inferior efficacy of vonoprazan versus lansoprazole in the treatment of Asian patients with erosive oesophagitis (EO).

    DESIGN: In this phase III, double-blind, multicentre study, patients with endoscopically confirmed EO were randomised 1:1 to receive vonoprazan 20 mg or lansoprazole 30 mg, once daily for up to 8 weeks. The primary endpoint was EO healing rate at 8 weeks. The secondary endpoints were EO healing rates at 2 and 4 weeks. Safety endpoints included treatment-emergent adverse events (TEAEs).

    RESULTS: In the vonoprazan (n=238) and lansoprazole (n=230) arms, 8-week EO healing rates were 92.4% and 91.3%, respectively (difference 1.1% (95% CI -3.822% to 6.087%)). The respective 2-week EO healing rates were 75.0% and 67.8% (difference 7.2% (95% CI -1.054% to 15.371%)), and the respective 4-week EO healing rates were 85.3% and 83.5% (difference 1.8% (95% CI -4.763% to 8.395%)). In patients with baseline Los Angeles classification grade C/D, 2-week, 4-week and 8-week EO healing rates were higher with vonoprazan versus lansoprazole (2 weeks: 62.2% vs 51.5%, difference 10.6% (95% CI -5.708% to 27.002%); 4 weeks: 73.3% vs 67.2%, difference 6.2% (95% CI -8.884 to 21.223); and 8 weeks: 84.0% vs 80.6%, difference 3.4% (95% CI -9.187% to 15.993%)). Overall, EO healing rates appeared higher with vonoprazan versus lansoprazole. TEAE rates were 38.1% and 36.6% in the vonoprazan and lansoprazole group, respectively.

    CONCLUSION: Our findings demonstrate the non-inferior efficacy of vonoprazan versus lansoprazole in terms of EO healing rate at 8 weeks in this population. Safety outcomes were similar in the two treatment arms.

    TRIAL REGISTRATION NUMBER: NCT02388724.

    Matched MeSH terms: Pyrroles/administration & dosage; Pyrroles/adverse effects; Pyrroles/therapeutic use*
  16. Fulltext Contribution of aroma compounds to the antioxidant properties of roasted white yam (Dioscorea rotundata)
    Lasekan O, Teoh LS
    BMC Chem, 2019 Dec;13(1):133.
    PMID: 31891159 DOI: 10.1186/s13065-019-0650-3
    Background: The aroma chemistry and the contribution of the aroma compounds to the anti-oxidative properties of roasted yam have yet to be characterized. The growing popularity of roasted yam in regions where they are being consumed calls for a concerted effort to elucidate their aroma chemistry as well as their anti-oxidative properties.

    Results: The aroma compounds in roasted white yam (Dioscorea rotundata) were isolated and identified using static headspace-gas chromatography-mass spectrometry (SH-GC-MS) and gas chromatography-olfactometry (GC-O). In addition, the anti-oxidative activities of the most abundant volatile heterocyclic compounds (2 pyrroles, 4 furans and 3 pyrazines) were evaluated on their inhibitory effect towards the oxidation of hexanal for a period of 30 days. Twenty-nine aroma-active compounds with a flavour dilution (FD) factor range of 2-256 and an array of odour notes were obtained. Among them, the highest odour activities (FD ≥ 128) factors were determined for 2-acetyl furan and 2-acetylpyrrole. Other compounds with significant FD factors ≥ 32 were; 2-methylpyrazine, ethyl furfural, and 5-hydroxy methyl furfural.

    Conclusion: Results of the anti-oxidative activity showed that the pyrroles exhibited the greatest antioxidant activity among all the tested heterocyclic compounds. This was followed by the furans and the pyrazines which had the least antioxidant activity.

    Matched MeSH terms: Pyrroles
  17. One-pot microwave assisted stereoselective synthesis of novel dihydro-2'H-spiro[indene-2,1'-pyrrolo-[3,4-c]pyrrole]-tetraones and evaluation of their antimycobacterial activity and inhibition of AChE
    Bharkavi C, Vivek Kumar S, Ashraf Ali M, Osman H, Muthusubramanian S, Perumal S
    Bioorg Med Chem Lett, 2017 Jul 15;27(14):3071-3075.
    PMID: 28552337 DOI: 10.1016/j.bmcl.2017.05.050
    An efficient one-pot microwave assisted stereoselective synthesis of novel dihydro-2'H-spiro[indene-2,1'-pyrrolo[3,4-c]pyrrole]-tetraone derivatives through three-component 1,3-dipolar cycloaddition of azomethine ylides generated in situ from ninhydrin and sarcosine with a series of 1-aryl-1H-pyrrole-2,5-diones is described. The synthesised compounds were screened for their antimycobacterial and AChE inhibition activities. Compound 4b (IC50 1.30µM) has been found to display twelve fold antimycobacterial activity compared to cycloserine and it is thirty seven times more active than pyrimethamine. Compound 4h displays maximum AchE inhibitory activity with IC50 value of 0.78±0.01µmol/L.
    Matched MeSH terms: Pyrroles/chemical synthesis; Pyrroles/pharmacology; Pyrroles/chemistry*
  18. A facile chemo-, regio- and stereoselective synthesis and cholinesterase inhibitory activity of spirooxindole-pyrrolizine-piperidine hybrids
    Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Perumal S, et al.
    Bioorg Med Chem Lett, 2013 May 15;23(10):2979-83.
    PMID: 23570788 DOI: 10.1016/j.bmcl.2013.03.027
    A series of novel hybrid spiro heterocycles comprising pyrrolizine, spiroxindole and piperidine moieties was synthesized chemo-, regio- and stereoselectively in good yields from 1,3-dipolar cycloaddition reaction of a series of 1-acryloyl-3,5-bisarylmethylidenepiperidin-4-ones with azomethine ylides generated in situ from 5-choloroisatin and l-proline in methanol. These cycloadducts displayed significant cholinesterase inhibitory activity. Among the compounds screened, 8g and 8e, showed maximum inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinestrase (BChE) with IC50 values of 3.33 and 3.13μM, respectively.
    Matched MeSH terms: Pyrroles/chemical synthesis; Pyrroles/pharmacology*; Pyrroles/chemistry
  19. Systematic analysis of in vitro photo-cytotoxic activity in extracts from terrestrial plants in Peninsula Malaysia for photodynamic therapy
    Ong CY, Ling SK, Ali RM, Chee CF, Samah ZA, Ho AS, et al.
    J. Photochem. Photobiol. B, Biol., 2009 Sep 4;96(3):216-22.
    PMID: 19647445 DOI: 10.1016/j.jphotobiol.2009.06.009
    One hundred and fifty-five extracts from 93 terrestrial species of plants in Peninsula Malaysia were screened for in vitro photo-cytotoxic activity by means of a cell viability test using a human leukaemia cell-line HL60. These plants which can be classified into 43 plant families are diverse in their type of vegetation and their natural habitat in the wild, and may therefore harbour equally diverse metabolites with potential pharmaceutical properties. Of these, 29 plants, namely three from each of the Clusiaceae, Leguminosae, Rutaceae and Verbenaceae families, two from the Piperaceae family and the remaining 15 are from Acanthaceae, Apocynaceae, Bignoniaceae, Celastraceae, Chrysobalanaceae, Irvingiaceae, Lauraceae, Lythraceae, Malvaceae, Meliaceae, Moraceae, Myristicaceae, Myrsinaceae, Olacaceae and Sapindaceae. Hibiscus cannabinus (Malvaceae), Ficus deltoidea (Moraceae), Maranthes corymbosa (Chrysobalanaceae), Micromelum sp., Micromelum minutum and Citrus hystrix (Rutaceae), Cryptocarya griffithiana (Lauraceae), Litchi chinensis (Sapindaceae), Scorodocarpus bornensis (Olacaceae), Kokoona reflexa (Celastraceae), Irvingia malayana (Irvingiaceae), Knema curtisii (Myristicaceae), Dysoxylum sericeum (Meliaceae), Garcinia atroviridis, Garcinia mangostana and Calophyllum inophyllum (Clusiaceae), Ervatamia hirta (Apocynaceae), Cassia alata, Entada phaseoloides and Leucaena leucocephala (Leguminosae), Oroxylum indicum (Bignoniaceae), Peronema canescens,Vitex pubescens and Premna odorata (Verbenaceae), Piper mucronatum and Piper sp. (Piperaceae), Ardisia crenata (Myrsinaceae), Lawsonia inermis (Lythraceae), Strobilanthes sp. (Acanthaceae) were able to reduce the in vitro cell viability by more than 50% when exposed to 9.6J/cm(2) of a broad spectrum light when tested at a concentration of 20 microg/mL. Six of these active extracts were further fractionated and bio-assayed to yield four photosensitisers, all of which are based on the pheophorbide-a and -b core structures. Our results suggest that the main photosensitisers from terrestrial plants are likely based on the cyclic tetrapyrrole structure and photosensitisers with other structures, if present, are present in minor amounts or are not as active as those with the cyclic tetrapyrrole structure.
    Matched MeSH terms: Pyrroles/chemistry
  20. Fulltext Synergy Effect of Nanocrystalline Cellulose for the Biosensing Detection of Glucose
    Esmaeili C, Abdi MM, Mathew AP, Jonoobi M, Oksman K, Rezayi M
    Sensors (Basel), 2015;15(10):24681-97.
    PMID: 26404269 DOI: 10.3390/s151024681
    Integrating polypyrrole-cellulose nanocrystal-based composites with glucose oxidase (GOx) as a new sensing regime was investigated. Polypyrrole-cellulose nanocrystal (PPy-CNC)-based composite as a novel immobilization membrane with unique physicochemical properties was found to enhance biosensor performance. Field emission scanning electron microscopy (FESEM) images showed that fibers were nanosized and porous, which is appropriate for accommodating enzymes and increasing electron transfer kinetics. The voltammetric results showed that the native structure and biocatalytic activity of GOx immobilized on the PPy-CNC nanocomposite remained and exhibited a high sensitivity (ca. 0.73 μA·mM(-1)), with a high dynamic response ranging from 1.0 to 20 mM glucose. The modified glucose biosensor exhibits a limit of detection (LOD) of (50 ± 10) µM and also excludes interfering species, such as ascorbic acid, uric acid, and cholesterol, which makes this sensor suitable for glucose determination in real samples. This sensor displays an acceptable reproducibility and stability over time. The current response was maintained over 95% of the initial value after 17 days, and the current difference measurement obtained using different electrodes provided a relative standard deviation (RSD) of 4.47%.
    Matched MeSH terms: Pyrroles/chemistry
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