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  1. Inhibition of CYP3A by Antimalarial Piperaquine and Its Metabolites in Human Liver Microsomes With IVIV Extrapolation
    Aziz MY, Hoffmann KJ, Ashton M
    J Pharm Sci, 2018 05;107(5):1461-1467.
    PMID: 29352982 DOI: 10.1016/j.xphs.2018.01.009
    The potential of the antimalarial piperaquine and its metabolites to inhibit CYP3A was investigated in pooled human liver microsomes. CYP3A activity was measured by liquid chromatography-tandem mass spectrometry as the rate of 1'-hydroxymidazolam formation. Piperaquine was found to be a reversible, potent inhibitor of CYP3A with the following parameter estimates (%CV): IC50 = 0.76 μM (29), Ki = 0.68 μM (29). In addition, piperaquine acted as a time-dependent inhibitor with IC50 declining to 0.32 μM (28) during 30-min pre-incubation. Time-dependent inhibitor estimates were kinact = 0.024 min-1 (30) and KI = 1.63 μM (17). Metabolite M2 was a highly potent reversible inhibitor with estimated IC50 and Ki values of 0.057 μM (17) and 0.043 μM (3), respectively. M1 and M5 metabolites did not show any inhibitory properties within the limits of assay used. Average (95th percentile) simulated in vivo areas under the curve of midazolam increased 2.2-fold (3.7-fold) on the third which is the last day of piperaquine dosing, whereas for its metabolite M2, areas under the curve of midazolam increased 7.7-fold (13-fold).
    Matched MeSH terms: Quinolines/metabolism; Quinolines/pharmacology*
  2. LC-MS/MS quantitation of antimalarial drug piperaquine and metabolites in human plasma
    Aziz MY, Hoffmann KJ, Ashton M
    J Chromatogr B Analyt Technol Biomed Life Sci, 2017 Sep 15;1063:253-258.
    PMID: 28863865 DOI: 10.1016/j.jchromb.2017.06.035
    PURPOSE: This study aimed to develop a sensitive, quantitative assay for the antimalarial piperaquine (PQ) and its metabolites M1 and M2 in human plasma.

    RESULTS: Analytes were gradiently separated on a C18 column and detected with a Sciex API 4000 MS/MS with an ESI source operated in the positive ion mode with deuterated PQ as internal standard. The response was linear in the range 3.9-2508nM with a runtime of 7.0min per sample. The method was applied to clinical samples from healthy volunteers.

    CONCLUSION: This LC-MS/MS method for the simultaneous quantitation of PQ and two of its metabolites in plasma may prove helpful for assessment of metabolite safety issues in vivo.

    Matched MeSH terms: Quinolines/blood*; Quinolines/metabolism; Quinolines/pharmacokinetics; Quinolines/chemistry
  3. Fulltext Pharmacokinetic evaluation, molecular docking and in vitro biological evaluation of 1, 3, 4-oxadiazole derivatives as potent antioxidants and STAT3 inhibitors
    Khanam R, Hejazi II, Shahabuddin S, Bhat AR, Athar F
    J Pharm Anal, 2019 Apr;9(2):133-141.
    PMID: 31011470 DOI: 10.1016/j.jpha.2018.12.002
    1, 3, 4-Oxadiazole derivatives (4a-5f) were previously synthesized to investigate their anticancer properties. However, studies relating to their antioxidant potential and signal transducer and activator of transcription (STAT) inhibition have not been performed. We investigated previously synthesized 1, 3, 4-oxadiazole derivatives (4a-5f) for various radical scavenging properties using several in vitro antioxidant assays and also for direct inhibition of STAT3 through molecular docking. The data obtained from various antioxidant assays such as 2, 2,-diphenyl-1-picrylhydrazyl radical (DPPH), nitric oxide, hydrogen peroxide, and superoxide anion radical revealed that among all the derivatives, compound 5e displayed high antioxidant activities than the standard antioxidant L-ascorbic acid. Additionally, the total reduction assay and antioxidant capacity assay further confirmed the antioxidant potential of compound 5e. Furthermore, the molecular docking studies performed for all derivatives along with the standard inhibitor STX-0119 showed that binding energy released in direct binding with the SH2 domain of STAT3 was the highest for compound 5e (-9.91kcal/mol). Through virtual screening, compound 5e was found to exhibit optimum competency in inhibiting STAT3 activity. Compound 5e decreased the activation of STAT3 as observed with Western blot. In brief, compound 5e was identified as a potent antioxidant agent and STAT3 inhibitor and effective agent for cancer treatment.
    Matched MeSH terms: Quinolines
  4. Phoebegrandine C, a novel proaporphine-tryptamine dimer, from Phoebe grandis (Nees) Merr
    Mukhtar MR, Hadi AH, Sévenet T, Martin MT, Awang K
    Nat Prod Res, 2004 Apr;18(2):163-7.
    PMID: 14984091
    A novel proaporphine-tryptamine dimer alkaloid, named phoebegrandine C 1, was isolated from the leaves of Phoebe grandis (Nees) Merr. Its structural elucidation was carried out using spectroscopic techniques, notably 2D NMR.
    Matched MeSH terms: Quinolines/isolation & purification*; Quinolines/chemistry*
  5. Fulltext Prediction of Improved Antimalarial Chemoprevention with Weekly Dosing of Dihydroartemisinin-Piperaquine
    Permala J, Tarning J, Nosten F, White NJ, Karlsson MO, Bergstrand M
    Antimicrob Agents Chemother, 2017 May;61(5).
    PMID: 28242661 DOI: 10.1128/AAC.02491-16
    Intermittent preventive treatment (IPT) is used to reduce malaria morbidity and mortality, especially in vulnerable groups such as children and pregnant women. IPT with the fixed dose combination of piperaquine (PQ) and dihydroartemisinin (DHA) is being evaluated as a potential mass treatment to control and eliminate artemisinin-resistant falciparum malaria. This study explored alternative DHA-PQ adult dosing regimens compared to the monthly adult dosing regimen currently being studied in clinical trials. A time-to-event model describing the concentration-effect relationship of preventive DHA-PQ administration was used to explore the potential clinical efficacy of once-weekly adult dosing regimens. Loading dose strategies were evaluated and the advantage of weekly dosing regimen was tested against different degrees of adherence. Assuming perfect adherence, three tablets weekly dosing regimen scenarios maintained malaria incidence of 0.2 to 0.3% per year compared to 2.1 to 2.6% for all monthly dosing regimen scenarios and 52% for the placebo. The three tablets weekly dosing regimen was also more forgiving (i.e., less sensitive to poor adherence), resulting in a predicted ∼4% malaria incidence per year compared to ∼8% for dosing regimen of two tablets weekly and ∼10% for monthly regimens (assuming 60% adherence and 35% interindividual variability). These results suggest that weekly dosing of DHA-PQ for malaria chemoprevention would improve treatment outcomes compared to monthly administration by lowering the incidence of malaria infections, reducing safety concerns about high PQ peak plasma concentrations and being more forgiving. In addition, weekly dosing is expected to reduce the selection pressure for PQ resistance.
    Matched MeSH terms: Quinolines/administration & dosage; Quinolines/pharmacokinetics*; Quinolines/therapeutic use*
  6. Neratinib after trastuzumab-based adjuvant therapy in patients from Asia with early stage HER2-positive breast cancer
    Iwata H, Masuda N, Kim SB, Inoue K, Rai Y, Fujita T, et al.
    Future Oncol, 2019 Jul;15(21):2489-2501.
    PMID: 31140297 DOI: 10.2217/fon-2019-0143
    Aim: To evaluate the efficacy and safety of neratinib as extended adjuvant therapy in patients from Asia based on exploratory analyses of the Phase III ExteNET trial. Patients & methods: A total of 2840 women with early stage HER2-positive breast cancer were randomly assigned to neratinib 240 mg/day or placebo for 1 year after trastuzumab-based adjuvant therapy. Results: A total of 341 patients were from Asia (neratinib, n = 165; placebo, n = 176). 2-year invasive disease-free survival rates were 92.8 and 90.8% with neratinib and placebo, respectively (HR: 0.70; 95% CI: 0.31-1.55), and 5-year rates were 91.9 and 87.2%, respectively (HR: 0.57; 95% CI: 0.27-1.13). Diarrhea was the most common adverse event with neratinib. Conclusion: Extended adjuvant therapy with neratinib reduces disease recurrences in Asian women with HER2-positive breast cancer. Trial registration: Clinicaltrials.gov NCT00878709.
    Matched MeSH terms: Quinolines/administration & dosage; Quinolines/adverse effects; Quinolines/therapeutic use*
  7. Current progress in antimalarial pharmacotherapy and multi-target drug discovery
    Tibon NS, Ng CH, Cheong SL
    Eur J Med Chem, 2020 Feb 15;188:111983.
    PMID: 31911292 DOI: 10.1016/j.ejmech.2019.111983
    Discovery and development of antimalarial drugs have long been dominated by single-target therapy. Continuous effort has been made to explore and identify different targets in malaria parasite crucial for the malaria treatment. The single-target drug therapy was initially successful, but it was later supplanted by combination therapy with multiple drugs to overcome drug resistance. Emergence of resistant strains even against the combination therapy has warranted a review of current antimalarial pharmacotherapy. This has led to the development of the new concept of covalent biotherapy, in which two or more pharmacophores are chemically bound to produce hybrid antimalarial drugs with multi-target functionalities. Herein, the review initially details the current pharmacotherapy for malaria as well as the conventional and novel targets of importance identified in the malaria parasite. Then, the rationale of multi-targeted therapy for malaria, approaches taken to develop the multi-target antimalarial hybrids, and the examples of hybrid molecules are comprehensively enumerated and discussed.
    Matched MeSH terms: Quinolines/pharmacology*; Quinolines/chemistry
  8. Leukotriene receptor antagonism may not be effective in atopic dermatitis treatment after all
    Chin WK
    J Clin Pharm Ther, 2018 Feb;43(1):159-162.
    PMID: 29114905 DOI: 10.1111/jcpt.12648
    WHAT IS KNOWN AND OBJECTIVE: Literature evidence suggests leukotriene involvement in the pathogenesis of atopic dermatitis. This article aimed to discuss whether the off-label use of montelukast, a leukotriene receptor antagonist, is justifiable for the treatment of atopic dermatitis.

    COMMENT: Most non-randomized studies supported the use of montelukast for atopic dermatitis treatment. However, evidence from these studies should be interpreted with caution as it is relatively weak due to the absence of randomization, control groups and blinding processes, subjecting the results to high risk of selection and reporting biases. The inconsistent findings across RCTs may be related to the limited number of patients, nuances in study designs, varying severity of disease and the concomitant use of steroids in some of the studies.

    WHAT IS NEW AND CONCLUSION: Current literature evidence is limited to rationally support the use of montelukast in atopic dermatitis treatment. For now, the conventional treatments should be preferred in the clinical setting.

    Matched MeSH terms: Quinolines/therapeutic use
  9. Fulltext Modified bicinchoninic acid assay for accurate determination of variable length reducing sugars in carbohydrates
    Hussain, H., Ngaini, Z., Chong, N.F-M.
    International Food Research Journal, 2018;25(6):2614-2619.
    MyJurnal
    The accurate determination of reducing ends of malto-oligosaccharides is essential for calculating the enzyme activities of starch debranching enzymes. The suitability of the 3,5-Dinitrosalicylic acid (DNS) method, the Dygert method, and the Bicinchoninic acid (BCA) method for accurate determination of reducing ends from malto-oligosaccharides of different chain lengths is compared. The results showed that BCA assay was much more accurate than the other assays. The results for the BCA assay showed that different malto-oligosaccharides gave observed (measured) values that were significantly similar to the expected (predetermined) values. In contrast, the DNS and Dygert assays underestimated the amount of reducing sugar present for glucose. Furthermore, both DNS and Dygert methods showed increasing degree of overestimation of the amount of reducing sugar present with the increasing length of the malto-oligosaccharide sugar chains. The BCA assay can suitably quantify reducing sugars even in mixtures of oligosaccharides with different chain lengths. Thus, enzyme activities can be measured without bias towards higher values for enzymes that preferentially cleave the longer chain lengths.
    Matched MeSH terms: Quinolines
  10. Cd(2+) Triggered the FRET "ON": A New Molecular Switch for the Ratiometric Detection of Cd(2+) with Live-Cell Imaging and Bound X-ray Structure
    Aich K, Goswami S, Das S, Mukhopadhyay CD, Quah CK, Fun HK
    Inorg Chem, 2015 Aug 3;54(15):7309-15.
    PMID: 26192906 DOI: 10.1021/acs.inorgchem.5b00784
    On the basis of the Förster resonance energy transfer mechanism between rhodamine and quinoline-benzothiazole conjugated dyad, a new colorimetric as well as fluorescence ratiometric probe was synthesized for the selective detection of Cd(2+). The complex formation of the probe with Cd(2+) was confirmed through Cd(2+)-bound single-crystal structure. Capability of the probe as imaging agent to detect the cellular uptake of Cd(2+) was demonstrated here using living RAW cells.
    Matched MeSH terms: Quinolines/chemistry
  11. Fulltext Crystal structure of 2-(1,3-dioxoindan-2-yl)iso-quinoline-1,3,4-trione
    Ghalib RM, Chidan Kumar CS, Hashim R, Sulaiman O, Fun HK
    Acta Crystallogr E Crystallogr Commun, 2015 Jan 1;71(Pt 1):o6-7.
    PMID: 25705509 DOI: 10.1107/S2056989014025997
    In the title iso-quinoline-1,3,4-trione derivative, C18H9NO5, the five-membered ring of the indane fragment adopts an envelope conformation with the nitro-gen-substituted C atom being the flap. The planes of the indane benzene ring and the iso-quinoline-1,3,4-trione ring make a dihedral angle of 82.06 (6)°. In the crystal, mol-ecules are linked into chains extending along the bc plane via C-H⋯O hydrogen-bonding inter-actions, enclosing R 2 (2)(8) and R 2 (2)(10) loops. The chains are further connected by π-π stacking inter-ations, with centroid-to-centroid distances of 3.9050 (7) Å, forming layers parallel to the b axis.
    Matched MeSH terms: Quinolines
  12. Assessment of gas chromatography time-of-flight accurate mass spectrometry for identification of volatile and semi-volatile compounds in honey
    Moniruzzaman M, Rodríguez I, Ramil M, Cela R, Sulaiman SA, Gan SH
    Talanta, 2014 Nov;129:505-15.
    PMID: 25127626 DOI: 10.1016/j.talanta.2014.06.019
    The performance of gas chromatography (GC) combined with a hybrid quadrupole time-of-flight (QTOF) mass spectrometry (MS) system for the determination of volatile and semi-volatile compounds in honey samples is evaluated. After headspace (HS) solid-phase microextraction (SPME) of samples, the accurate mass capabilities of the above system were evaluated for compounds identification. Accurate scan electron impact (EI) MS spectra allowed discriminating compounds displaying the same nominal masses, but having different empirical formulae. Moreover, the use of a mass window with a width of 0.005 Da provided highly specific chromatograms for selected ions, avoiding the contribution of interferences to their peak areas. Additional information derived from positive chemical ionization (PCI) MS spectra and ion product scan MS/MS spectra permitted confirming the identity of novel compounds. The above possibilities are illustrated with examples of honey aroma compounds, belonging to different chemical classes and containing different elements in their molecules. Examples of compounds whose structures could not be described are also provided. Overall, 84 compounds, from a total of 89 species, could be identified in 19 honey samples from 3 different geographic areas in the world. The suitability of responses measured for selected ions, corresponding to above species, for authentication purposes is assessed through principal components analysis.
    Matched MeSH terms: Quinolines/chemistry
  13. Synthesis of novel quinoline-based thiadiazole, evaluation of their antileishmanial potential and molecular docking studies
    Almandil NB, Taha M, Rahim F, Wadood A, Imran S, Alqahtani MA, et al.
    Bioorg Chem, 2019 04;85:109-116.
    PMID: 30605884 DOI: 10.1016/j.bioorg.2018.12.025
    New series of quinoline-based thiadiazole analogs (1-20) were synthesized, characterized by EI-MS, 1H NMR and 13C NMR. All synthesized compounds were subjected to their antileishmanial potential. Sixteen analogs 1-10, 12, 13, 16, 17, 18 and 19 with IC50 values in the range of 0.04 ± 0.01 to 5.60 ± 0.21 µM showed tremendously potent inhibition as compared to the standard pentamidine with IC50 value 7.02 ± 0.09 µM. Analogs 11, 14, 15 and 20 with IC50 8.20 ± 0.35, 9.20 ± 0.40, 7.20 ± 0.20 and 9.60 ± 0.40 µM respectively showed good inhibition when compared with the standard. Structure-activity relationships have been also established for all compounds. Molecular docking studies were performed to determine the binding interaction of the compounds with the active site target.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/metabolism; Quinolines/pharmacology*
  14. Fulltext Montelukast in children with allergic rhinitis amid COVID-19 pandemic
    Kow CS, Hasan SS
    Acta Paediatr, 2020 10;109(10):2151.
    PMID: 32686128 DOI: 10.1111/apa.15491
    Matched MeSH terms: Quinolines
  15. Fulltext Heterocyclic aromatic amines in deep fried lamb meat: The influence of spices marination and sensory quality
    S J, Iqbal SZ, Talib NH, Hasnol ND
    J Food Sci Technol, 2016 Mar;53(3):1411-7.
    PMID: 27570265 DOI: 10.1007/s13197-015-2137-0
    The present study was focused to investigate the effect of selected spices (turmeric, torch ginger, lemongrass and curry leaves) on the formation of heterocyclic amines (HCAs, IQx, MeIQ, MeIQx, DiMeIQx, IQ, harman, norharman, and AαC) in deep fried lamb meat. Meat samples were marinated with optimized levels of turmeric (4 %), 10 % each of torch ginger, lemon grass, curry leaves at medium (70 °C) and well done (80 °C) doneness temperatures. The concentration of HCAs in deep fried meat samples were analysed using LC-MS/MS technique. The results revealed that torch ginger (10 %) has reduced 74.8 % of Me1Qx (1.39 to 0.35 ng/g) at medium doneness, followed by the 64.7 % reduction, using curry leaves and turmeric at medium degree of doneness. Torch ginger has reduced 86.6 % of AαC (2.59 to 0.40 ng/g) at well done doneness. The most prevalence level of HCAs was found in deep fried meat i.e. DiMeIQ (3.69 ng/g) at well done doneness. The sensory evaluation, using a 7 point hedonic test design for colour and texture in deep fried meat samples were resulted in a preferred color of golden brown and slightly tough texture. The use of local spices in marinating of deep fried lamb meat samples will certainly inhibit/reduce the level of these toxic and harmful HCAs.
    Matched MeSH terms: Quinolines
  16. Click chemistry approach: regioselective one-pot synthesis of some new 8-trifluoromethylquinoline based 1,2,3-triazoles as potent antimicrobial agents
    Garudachari B, Isloor AM, Satyanarayana MN, Fun HK, Hegde G
    Eur J Med Chem, 2014 Mar 3;74:324-32.
    PMID: 24486415 DOI: 10.1016/j.ejmech.2014.01.008
    Three series of 8-trifluoromethylquinoline based 1,2,3-triazoles derivatives (5a-c, 6a-d and 7a-c) were synthesized by multi-step reactions by click chemistry approach. Synthesized compounds were characterized by spectral studies and X-ray analysis. The final compounds were screened for their in-vitro antimicrobial activity by well plate method (zone of inhibition). Compounds 5c, 6b, 8b, 11 and 12 were found to be active against tested microbial strains. The results are summarized in Tables 5 and 6.
    Matched MeSH terms: Quinolines/chemistry*
  17. Fulltext A Prospective Study on the Prevalence, Extent of Disease and Outcome of Eosinophilic Gastroenteritis in Patients Presenting with Lower Abdominal Symptoms
    Hui CK, Hui NK
    Gut Liver, 2018 May 15;12(3):288-296.
    PMID: 29212311 DOI: 10.5009/gnl17056
    Background/Aims: The epidemiology of eosinophilic gastroenteritis remains unclear. We aim to determine the prevalence of eosinophilic gastroenteritis in patients with lower abdominal symptoms.

    Methods: In a prospective study, colonoscopy was performed on 2,469 consecutive patients. Biopsies were taken from the terminal ileum and ascending, transverse, descending and sigmoid colon in all patients.

    Results: Sixty-four of the 2,469 patients (2.6%) had eosinophilic gastroenteritis. Only five of the 64 patients (7.8%) with eosinophilic gastroenteritis had endoscopic mucosal abnormalities during colonoscopy. Six of these 64 patients (9.4%) had severe disease at presentation, and seven of these 64 patients (10.9%) required systemic steroid treatment. An elevated absolute peripheral eosinophil count was independently associated with severe disease at presentation (4/6 [66.7%] vs 3/58 [5.2%], p=0.005; odds ratio [OR], 25.320; 95% confidence interval [CI], 2.628 to 243.910), and severe disease at the time of presentation was independently associated with the use of systemic steroid treatment (6/7 [85.7%] vs 0/57 [0%], p=0.008; OR, 18.021; 95% CI, 2.163 to 150.152).

    Conclusions: The prevalence of eosinophilic gastroenteritis is common, and patients usually present normal-appearing mucosa on colonoscopy. Those with severe disease at presentation usually have a raised absolute peripheral eosinophil count and should be commenced on systemic steroids as an initial therapy.

    Matched MeSH terms: Quinolines/administration & dosage
  18. Quality of life assessment in patients with moderate to severe allergic rhinitis treated with montelukast and/or intranasal steroids: a randomised, double-blind, placebo-controlled study
    Goh BS, Ismail MI, Husain S
    J Laryngol Otol, 2014 Mar;128(3):242-8.
    PMID: 24618303 DOI: 10.1017/S002221511400036X
    This study investigated improvements in quality of life associated with eight weeks of montelukast and/or intranasal steroid treatment for moderate to severe allergic rhinitis.
    Matched MeSH terms: Quinolines/therapeutic use*
  19. Fulltext Detection of Quinoline in G. boninense-Infected Plants Using Functionalized Multi-Walled Carbon Nanotubes: A Field Study
    Akanbi FS, Yusof NA, Abdullah J, Sulaiman Y, Hushiarian R
    Sensors (Basel), 2017 Jul 01;17(7).
    PMID: 28671561 DOI: 10.3390/s17071538
    Carbon nanotubes (CNTs) reinforced with gold nanoparticles (AuNPs) and chitosan nanoparticles (CTSNPs) were anchored on a screen-printed electrode to fabricate a multi-walled structure for the detection of quinoline. The surface morphology of the nanocomposites and the modified electrode was examined by an ultra-high resolution field emission scanning electron microscope (FESEM), and Fourier-transform infrared (FT-IR) spectroscopy was used to confirm the presence of specific functional groups on the multi-walled carbon nanotubes MWCNTs. Cyclic voltammetry (CV) and linear sweep voltammetry (LSV) were used to monitor the layer-by-layer assembly of ultra-thin films of nanocomposites on the surface of the electrode and other electrochemical characterizations. Under optimized conditions, the novel sensor displayed outstanding electrochemical reactivity towards the electro-oxidation of quinoline. The linear range was fixed between 0.0004 and 1.0 μM, with a limit of detection (LOD) of 3.75 nM. The fabricated electrode exhibited high stability with excellent sensitivity and selectivity, specifically attributable to the salient characteristics of AuNPs, CTSNPs, and MWCNTs and the synergistic inter-relationship between them. The newly developed electrode was tested in the field. The Ipa increased with an increase in the amount of quinoline solution added, and the peak potential deviated minimally, depicting the real capability of the newly fabricated electrode.
    Matched MeSH terms: Quinolines
  20. Seco-tabersonine alkaloids from Tabernaemontana corymbosa
    Lim KH, Thomas NF, Abdullah Z, Kam TS
    Phytochemistry, 2009 Feb;70(3):424-9.
    PMID: 19217125 DOI: 10.1016/j.phytochem.2009.01.001
    Two seco-tabersonine alkaloids, jerantiphyllines A and B, in addition to a tabersonine hydroxyindolenine, jerantinine H, and a recently reported vincamine alkaloid 7, were isolated from the leaf extract of the Malayan Tabernaemontana corymbosa and the structures were established using NMR and MS analysis. Biomimetic conversion of jerantinines A and E to their respective vincamine and 16-epivincamine derivatives were also carried out.
    Matched MeSH terms: Quinolines/isolation & purification; Quinolines/chemistry*
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