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  1. Synthesis, in vitro antiurease, in vivo antinematodal activity of quinoline analogs and their in-silico study
    Zaman K, Rahim F, Taha M, Sajid M, Hayat S, Nawaz M, et al.
    Bioorg Chem, 2021 10;115:105199.
    PMID: 34329995 DOI: 10.1016/j.bioorg.2021.105199
    Synthesis of quinoline analogs and their urease inhibitory activities with reference to the standard drug, thiourea (IC50 = 21.86 ± 0.40 µM) are presented in this study. The inhibitory activity range is (IC50 = 0.60 ± 0.01 to 24.10 ± 0.70 µM) which displayed that it is most potent class of urease inhibitor. Analog 1-9, and 11-13 emerged with many times greater antiurease potential than thiourea, in which analog 1, 2, 3, 4, 8, 9, and 11 (IC50 = 3.50 ± 0.10, 7.20 ± 0.20, 1.30 ± 0.10, 2.30 ± 0.10, 0.60 ± 0.01, 1.05 ± 0.10 and 2.60 ± 0.10 µM respectively) were appeared the most potent ones among the series. In this context, most potent analogs such as 1, 3, 4, 8, and 9 were further subjected for their in vitro antinematodal study against C. elegans to examine its cytotoxicity under positive control of standard drug, Levamisole. Consequently, the cytotoxicity profile displayed that analogs 3, 8, and 9 were found with minimum cytotoxic outline at higher concentration (500 µg/mL). All analogs were characterized through 1H NMR, 13C NMR and HR-EIMS. The protein-ligand binding interaction for most potent analogs was confirmed via molecular docking study.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/pharmacology*; Quinolines/chemistry
  2. Fulltext Zinc/Aluminium⁻Quinclorac Layered Nanocomposite Modified Multi-Walled Carbon Nanotube Paste Electrode for Electrochemical Determination of Bisphenol A
    Zainul R, Abd Azis N, Md Isa I, Hashim N, Ahmad MS, Saidin MI, et al.
    Sensors (Basel), 2019 Feb 22;19(4).
    PMID: 30813385 DOI: 10.3390/s19040941
    This paper presents the application of zinc/aluminium-layered double hydroxide-quinclorac (Zn/Al-LDH-QC) as a modifier of multiwalled carbon nanotubes (MWCNT) paste electrode for the determination of bisphenol A (BPA). The Zn/Al-LDH-QC/MWCNT morphology was examined by a transmission electron microscope and a scanning electron microscope. Electrochemical impedance spectroscopy was utilized to investigate the electrode interfacial properties. The electrochemical responses of the modified electrode towards BPA were thoroughly evaluated by using square-wave voltammetry technique. The electrode demonstrated three linear plots of BPA concentrations from 3.0 × 10-8⁻7.0 × 10-7 M (R² = 0.9876), 1.0 × 10-6⁻1.0 × 10-5 M (R² = 0.9836) and 3.0 × 10-5⁻3.0 × 10-4 M (R² = 0.9827) with a limit of detection of 4.4 × 10-9 M. The electrode also demonstrated good reproducibility and stability up to one month. The presence of several metal ions and organic did not affect the electrochemical response of BPA. The electrode is also applicable for BPA determination in baby bottle and mineral water samples with a range of recovery between 98.22% and 101.02%.
    Matched MeSH terms: Quinolines
  3. Fulltext Montelukast sodium-induced hypomania
    Zainal, N.Z., Tan, T.Y
    Malaysian Journal of Psychiatry, 2015;24(1):96-98.
    MyJurnal
    Objective: A rare case of induced hypomania was reported. Method: Patient was a 78-year-old Indian female with squamous cell carcinoma of the nasal septum, childhood bronchial asthma and underlying bipolar disorder. Her bipolar disorder is currently in remission. She developed hypomanic symptoms after one week of initiation of montelukast sodium for treatment of acute exacerbation of bronchial asthma. Result: Her hypomanic symptoms improved after stopping usage of montelukast sodium. Conclusion: Montelukast sodium likely had induced hypomania in this patient.
    Matched MeSH terms: Quinolines
  4. Fulltext Moxifloxacin-warfarin interaction
    Yew KL, Lee WC
    Med J Malaysia, 2012 Aug;67(4):420-1.
    PMID: 23082454 MyJurnal
    Matched MeSH terms: Quinolines/adverse effects*
  5. Development of LC-MS/MS method and application to bioequivalence study of a light sensitive drug montelukast
    Wong EYL, Loh GOK, Tan YTF, Peh KK
    Drug Dev Ind Pharm, 2021 Feb;47(2):197-206.
    PMID: 33300818 DOI: 10.1080/03639045.2020.1862177
    OBJECTIVE: The aim of the study was to develop a simple, highthroughput and sensitive LC-MS/MS method and apply to a bioequivalence study of montelukast, a light sensitive drug.

    METHOD: The effects of organic modifiers in mobile phase, protein precipitation agent to plasma sample ratio, and light on montelukast stability in unprocessed and processed human plasma, were evaluated. Validation was conducted in accordance with European Medicines Agency Guideline on bioanalytical method validation.

    RESULTS: No interference peak was observed when acetonitrile was used as an organic modifier. Acetonitrile to plasma ratio of 4:1 produced clean plasma sample. Approximately 3 % of cis isomer was detected in unprocessed plasma samples while 21 % of cis isomer was detected in processed plasma samples after exposing to fluorescent light for 24h. The standard calibration curve was linear over 3.00-1200.00 ng/mL. All method validation parameters were within the acceptance criteria.

    CONCLUSION: The validated method was successfully applied to a bioequivalence study of two montelukast formulations involving 24 healthy Malaysian volunteers. The light stability of a light sensitive drug in unprocessed and processed human plasma samples should be studied prior to pharmacokinetic/bioequivalence studies. Measures could then be taken to protect the analyte in human plasma from light degradation.

    Matched MeSH terms: Quinolines/pharmacology*; Quinolines/chemistry
  6. 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
  7. Inhibitory effect of the extract from Sonchus olearleu on the formation of carcinogenic heterocyclic aromatic amines during the pork cooking
    Teng H, Chen Y, Lin X, Lv Q, Chai TT, Wong FC, et al.
    Food Chem Toxicol, 2019 Jul;129:138-143.
    PMID: 31034934 DOI: 10.1016/j.fct.2019.04.043
    The aim of this study was to assess the inhibitory effects of Sonchus olearleu extract on the generation of heterocyclic amines in roasted pork patties cooked by pan-frying. All samples were cooked for two different durations (45 min and 105 min) under 200 °C and 230 °C. 2-amino-3-methylimidazo[4,5-f]quinoline (IQ), 2-ami- no-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx), 2-amino-3,4,8-trimethylimidazo[4,5-f]quinox-aline (4,8-DiMeIQx), harman, and norharman were detected and quantified. In patties cooked at 230 °C for 105 min, S. olearleu extract (0.5%) significantly inhibited the formation of IQ, harman, and norharman by 39%, 67%, and 63%, respectively. In contrast to IQ, the levels of harman and norharman were significantly reduced by the extracts tested. However, no such effects were observed for MeIQx and 4, 8-DiMeIQx. Notably, the inhibitory effect on heterocyclic amines is significantly correlated with the antioxidant potential and total phenolic content of S. olearleu extract.
    Matched MeSH terms: Quinolines
  8. Synthesis of quinoline derivatives as diabetic II inhibitors and molecular docking studies
    Taha M, Sultan S, Imran S, Rahim F, Zaman K, Wadood A, et al.
    Bioorg Med Chem, 2019 09 15;27(18):4081-4088.
    PMID: 31378594 DOI: 10.1016/j.bmc.2019.07.035
    In searchof the potenttherapeutic agent as an α-glucosidase inhibitor, we have synthesized twenty-five analogs (1-25) of quinoline-based Schiff bases as an inhibitoragainst α-glucosidase enzyme under positive control acarbose (IC50 = 38.45 ± 0.80 µM). From the activity profile it was foundthat analogs 1, 2, 3, 4, 11, 12 and 20with IC50values 12.40 ± 0.40, 9.40 ± 0.30, 14.10 ± 0.40, 6.20 ± 0.30, 14.40 ± 0.40, 7.40 ± 0.20 and 13.20 ± 0.40 µMrespectively showed most potent inhibition among the series even than standard drug acarbose (IC50 = 38.45 ± 0.80 µM). Here in the present study analog 4 (IC50 = 6.20 ± 0.30 µM) was found with many folds better α-glucosidase inhibitory activity than the reference drug. Eight analogs like 5, 7, 8, 16, 17, 22, 24 and 25 among the whole series displayed less than 50% inhibition. The substituents effects on phenyl ring thereby superficially established through SAR study. Binding interactions of analogs and the active site of ligands proteins were confirmed through molecular docking study. Spectroscopic techniques like 1H NMR, 13C NMR and ESIMS were used for characterization.
    Matched MeSH terms: Quinolines/chemical synthesis*
  9. Molecular hybridization conceded exceptionally potent quinolinyl-oxadiazole hybrids through phenyl linked thiosemicarbazide antileishmanial scaffolds: In silico validation and SAR studies
    Taha M, Ismail NH, Ali M, Rashid U, Imran S, Uddin N, et al.
    Bioorg Chem, 2017 04;71:192-200.
    PMID: 28228228 DOI: 10.1016/j.bioorg.2017.02.005
    The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover a novel series of compounds 6-23 based on the concept of molecular hybridization. Most of the synthesized analogues exhibited potent leishmanicidal potential. The most potent compound (23, IC50=0.10±0.001μM) among the series was found ∼70 times more lethal than the standard drug. The current series 6-23 conceded in the development of fourteen (14) extraordinarily active compounds against leishmaniasis. In silico analysis were also performed to probe the mode of action while all the compounds structure were established by NMR and Mass spectral analysis.
    Matched MeSH terms: Quinolines/pharmacology; Quinolines/chemistry
  10. Synthesis and study of the α-amylase inhibitory potential of thiadiazole quinoline derivatives
    Taha M, Tariq Javid M, Imran S, Selvaraj M, Chigurupati S, Ullah H, et al.
    Bioorg Chem, 2017 10;74:179-186.
    PMID: 28826047 DOI: 10.1016/j.bioorg.2017.08.003
    α-Amylase is a target for type-2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized thiadiazole quinoline analogs (1-30), characterized by different spectroscopic techniques such as 1HNMR and EI-MS and screened for α-amylase inhibitory potential. Thirteen analogs 1, 2, 3, 4, 5, 6, 22, 23, 25, 26, 27, 28 and 30 showed outstanding α-amylase inhibitory potential with IC50 values ranges between 0.002±0.60 and 42.31±0.17μM which is many folds better than standard acarbose having IC50 value 53.02±0.12μM. Eleven analogs 7, 9, 10, 11, 12, 14, 15, 17, 18, 19 and 24 showed good to moderate inhibitory potential while seven analogs 8, 13, 16, 20, 21 and 29 were found inactive. Our study identifies novel series of potent α-amylase inhibitors for further investigation. Structure activity relationship has been established.
    Matched MeSH terms: Quinolines/chemical synthesis; Quinolines/pharmacology*; Quinolines/chemistry
  11. Fulltext Sustainable Syntheses of (-)-Jerantinines A & E and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site
    Smedley CJ, Stanley PA, Qazzaz ME, Prota AE, Olieric N, Collins H, et al.
    Sci Rep, 2018 Jul 13;8(1):10617.
    PMID: 30006510 DOI: 10.1038/s41598-018-28880-2
    The jerantinine family of Aspidosperma indole alkaloids from Tabernaemontana corymbosa are potent microtubule-targeting agents with broad spectrum anticancer activity. The natural supply of these precious metabolites has been significantly disrupted due to the inclusion of T. corymbosa on the endangered list of threatened species by the International Union for Conservation of Nature. This report describes the asymmetric syntheses of (-)-jerantinines A and E from sustainably sourced (-)-tabersonine, using a straight-forward and robust biomimetic approach. Biological investigations of synthetic (-)-jerantinine A, along with molecular modelling and X-ray crystallography studies of the tubulin-(-)-jerantinine B acetate complex, advocate an anticancer mode of action of the jerantinines operating via microtubule disruption resulting from binding at the colchicine site. This work lays the foundation for accessing useful quantities of enantiomerically pure jerantinine alkaloids for future development.
    Matched MeSH terms: Quinolines/isolation & purification; Quinolines/chemistry
  12. Fulltext Characterisation of Silver Nanoparticles using a Standardised Catharanthus Roseus Aqueous extract
    Siti Zulaikha Ghozali, Mohd Nazri Ismail, Nor Hazwani Ahmad
    Malaysian Journal of Medicine and Health Sciences, 2018;14(102):1-6.
    MyJurnal
    The biosynthesis of nanoparticles has been proposed as a cost-effective and environmental friendly alternative to chemical and physical methods. The present study was aimed to characterise Catharanthus roseus (C. roseus)-silver nanoparticles (AgNPs) using a standardised C. roseus aqueous extract. Methods: The standardisation was performed by using Liquid Chromatography/Time-of-Flight ion trap Mass Spectrometry. An optimised C. roseus-AgNPs have been previously synthesised. Further characterisation of C. roseus-AgNPs was evaluated by zeta potential analysis and fourier transform infrared spectroscopy (FTIR). Results: The chromatography analysis has revealed presence of thirteen possible indole alkaloids in C. roseus extract which were lochrovicine, lochnerine, vinleurosine, vindolinine, tabersonine, catharanthine, serpentine, catharosine, vincristine, catharine, ajmalicine, vinleurosine, and vindolicine. Zeta potential analysis exhibited the value at -16.6 mV. FTIR spectrum of C. roseus aqueous extract showed the absorption band at 3210.83 cm-1 (C-H stretch), 2934.11 (C-H bond), 1578.15 (N=O stretch), 1388.76 and 1314.89 (N=O bend), 1119.29 (C-O bond) and 729.94 (C-Cl bond). In comparison, FTIR spectrum of C. roseus-AgNP s showed the absorption band at 2925.01 and 2924.97 (C-H bond), 1622.93 (C-C=C symmetric stretch), 1383.19 and 1384.13 (N-O bend), 1037.92/1038.76/1238.3/1117.2 (C-O bond), 3169.4 (O-H bond), 774.59 and 691.53 (C-Cl bond). Conclusion: The present findings have shown that the C. roseus aqueous extract contains alkaloids that may responsible as reducing and stabilising agents in the synthesis of AgNPs.
    Matched MeSH terms: Quinolines
  13. Fulltext Mathematical modelling of the growth of Klebsiella pneumoniae on 2-methylquinoline
    Shukor, M.S., Shukor, M.Y.
    Bioremediation Science and Technology Research, 2015;3(1):16-19.
    MyJurnal
    Quinolines compounds are toxic pollutants. Their biodegradation by microbes represents a tool
    for bioremediation. The growth of Klebsiella penumoniae on 2-methylquinoline shows typical
    sigmoidal bacterial growth curves. Since there exists a variety of models for describing the
    growth profile of microorganism such as logistic, Gompertz, Richards, Schnute, Baranyi-
    Roberts, Von Bertalanffy, Buchanan three-phase and more recently Huang models, the growth
    curves exhibit under such conditions would be an excellent study for finding the best model.
    The Huang model was chosen as the best model based on statistical tests such as root-meansquare
    error (RMSE), adjusted coefficient of determination (R2), bias factor (BF), accuracy
    factor (AF) and corrected AICc (Akaike Information Criterion). Novel constants obtained from
    the modelling exercise would be used for further secondary modelling.
    Matched MeSH terms: Quinolines
  14. 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
  15. 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*
  16. [Diagnosis and Treatment of the First Imported Case of Plasmodium knowlesi Infection in China]
    Pan B, Pei FQ, Ruan CW, Lin RX, Cen YZ, Liu MR, et al.
    Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi, 2016 12;34(6):513-6.
    PMID: 30141606
    Objective: To diagnose and treat the first imported active case of Plasmodium knowlesi infection in China.

    Methods: The clinical information of the patient was collected. Microscopy of blood smear was conducted after Giemsa staining. Genomic DNA was extracted from blood, and PCR was conducted to amplify rDNA. The PCR products were sequenced and analyzed with BLAST

    Results: The patient returned from a one-week tour in a tropical rain forest in Malaysia. The first disease attack occurred in Guangzhou on Oct. 16, 2014, with fever, shivering and sweating. The patient was initially diagnosed as malaria and hospitalized on Oct. 26, 2014. Microscopic observation revealed typical forms of P. knowlesi in blood smear. The red blood cells became enlarged, with big trophozoites appearing as a ring with dual cores and dark brown malaria pigment. The trophozoites were slightly bigger and thicker than P. falciparum. The schizont had 6-8 merozoites, with obvious brown malaria pigment. PCR resulted in a specific band of 1 099 bp. BLAST analysis showed that the sequence of the PCR product was 99% homologous to P. knowlesi (acession No. AM910985.1, L07560.1 and AY580317.1). The patient was diagnosed as P. knowlesi infection, and was then given an 8-day treatment with chloroquine and primaquine, together with dihydroartemisinin piperaquine phosphate tablet. The patient was discharged after recovery on Oct. 28, 2014.

    Conclusion: According to the clinical symptoms, epidemiological history and laboratory test, the patient has been confirmed as P. knowlesi infection. It may also be the first active case of knowlesi malaria reported in China.

    Matched MeSH terms: Quinolines
  17. Fulltext In-vitro activity of quinupristin/dalfopristin, levofloxacin and moxifloxacin against fusidic acid and rifampicin-resistant strains of methicillin-resistant Staphylococcus aureus (MRSA) from Malaysian hospitals
    Norazah A, Lim VKE, Rohani MY, Kamel AGM
    Med J Malaysia, 2005 Oct;60(4):411-5.
    PMID: 16570701
    The in-vitro susceptibility of quinupristin/dalfopristin, levofloxacin and moxifloxacin against methicillin-resistant Staphylococcus aureus (MRSA) strains, which are also resistant to fusidic acid and rifampicin were carried out to determine whether these antibiotics can be used as an alternative treatment for multiply resistant MRSA strains. The minimum inhibitory concentrations (MIC) of these antibiotics were determined by E-test. Quinupristin/dalfopristin had good activity (MIC90 = 1 mg/L) against these strains while most of the strains showed intermediate resistance to moxifloxacin with MIC90 = 2 mg/L). However, more than 90% of these strains were resistant to levofloxacin with the MICs that ranged from 8 mg/L to 16 mg/L with the majority inhibited at 8 mg/L.
    Matched MeSH terms: Quinolines/pharmacology*
  18. Efficacy and safety of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum malaria in endemic countries: meta-analysis of randomised controlled studies
    Naing C, Mak JW, Aung K, Wong JY
    Trans R Soc Trop Med Hyg, 2013 Feb;107(2):65-73.
    PMID: 23222952 DOI: 10.1093/trstmh/trs019
    The present review aimed to synthesise available evidence on the efficacy of dihydroartemisinin-piperaquine (DP) in treating uncomplicated Plasmodium falciparum malaria in people living in malaria-endemic countries by performing a meta-analysis of relevant studies. We searched relevant studies in electronic data bases up to December 2011. Published results from randomised controlled trials (RCTs) comparing efficacy of DP with other artemisinin-based combination therapies (ACTs), or non-ACTs, or placebo were selected. The primary endpoint was 28-day and 42-day treatment failure. We identified 26 RCTs. Many of the studies included in the present review were of high quality. Overall, DP, artesunate-mefloquine (MAS3) and artemether-lumefentrine (AL) were equally effective for reducing the risk of recurrent parasitaemia. The PCR confirmed efficacy of DP (99.5%) and MAS3 (97.7%) at day 28 exceeded 90%; both are efficacious. Comparable efficacy was also found for DP (95.6%) and AL (94.3%). The present review has documented that DP is comparable to other currently used ACTs such as MAS3 and AL in treating uncomplicated falciparum malaria. The better safety profile of DP and once-daily dosage improves adherence and its fixed co-formulation ensures that both drugs are taken together. Our conclusion is that DP has the potential to become a first-line antimalarial drug.
    Matched MeSH terms: Quinolines/adverse effects; Quinolines/therapeutic use*
  19. Fulltext Influence of the pfmdr1 Gene on In Vitro Sensitivities of Piperaquine in Thai Isolates of Plasmodium falciparum
    Mungthin M, Watanatanasup E, Sitthichot N, Suwandittakul N, Khositnithikul R, Ward SA
    Am J Trop Med Hyg, 2017 03;96(3):624-629.
    PMID: 28044042 DOI: 10.4269/ajtmh.16-0668
    Piperaquine combined with dihydroartemisinin is one of the artemisinin derivative combination therapies, which can replace artesunate-mefloquine in treating uncomplicated falciparum malaria in Thailand. The aim of this study was to determine the in vitro sensitivity of Thai Plasmodium falciparum isolates against piperaquine and the influence of the pfmdr1 gene on in vitro response. One hundred and thirty-seven standard laboratory and adapted Thai isolates of P. falciparum were assessed for in vitro piperaquine sensitivity. Polymorphisms of the pfmdr1 gene were determined by polymerase chain reaction methods. The mean and standard deviation of the piperaquine IC50 in Thai isolates of P. falciparum were 16.7 ± 6.3 nM. The parasites exhibiting chloroquine IC50 of ≥ 100 nM were significantly less sensitive to piperaquine compared with the parasite with chloroquine IC50 of < 100 nM. No significant association between the pfmdr1 copy number and piperaquine IC50 values was found. In contrast, the parasites containing the pfmdr1 86Y allele exhibited significantly reduced piperaquine sensitivity. Before nationwide implementation of dihydroartemisinin-piperaquine as the first-line treatment in Thailand, in vitro and in vivo evaluations of this combination should be performed especially in areas where parasites containing the pfmdr1 86Y allele are predominant such as the Thai-Malaysian border.
    Matched MeSH terms: Quinolines/pharmacology*
  20. 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*
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