Displaying publications 1 - 20 of 105 in total

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  1. Ang HH, Chan KL, Mak JW
    Chemotherapy, 1997 Sep-Oct;43(5):311-5.
    PMID: 9309363 DOI: 10.1159/000239583
    Eleven Malaysian Plasmodium falciparum isolates were cultured in vitro and later subjected to antimalarial evaluations in 96-well microtiter plates. After cryopreservation, the IC50 (nM) for ST 195, ST 196, ST 197, ST 244 and ST 245 isolates were, respectively: 180.9, 198.7, 482.0, 580.0 and 690.1 for chloroquine; 3.4, 3.4, 9.2, 4.0 and 5.8 for mefloquine; 21.9, 10.5, 40.7, 40.1 and 48.7 for quinine; 136.7, 58.8, 116.4, 29.4 and 95.4 for cycloguanil, and 48.3, 57.5, 47.4, 61.5 and 37.8 for pyrimethamine. Before cryopreservation they were 172.5, 141.5, 453.2, 636.0 and 651.6 nM for chloroquine; 4.8, 2.6, 9.0, 6.9 and 5.8 nM for mefloquine; 21.3, 8.3, 41.9, 49.6 and 40.1 nM for quinine, 129.9, 47.3, 109.3, 30.6 and 95.4 nM for cycloguanil, and 45.4, 47.4, 40.2, 66.3 and 36.0 nM for pyrimethamine. IC50 (nM) for Gombak A, Gombak C, ST 9, ST 12, ST 85 and ST 148 isolates after 12 months of continuous in vitro culture were, respectively: 477.0, 492.3, 367.1, 809.4, 566.5 and 341.8 for chloroquine; 2.9, 11.1, 8.5, 16.9, 5.3 and 4.2 for mefloquine; 6.2, 58.3, 52.7, 36.7, 31.8 and 26.2 for quinine; 154.5, 57.2, 130.3, 94.2, 81.4 and 102.9 for cycloguanil, 26.9, 24.9, 43.8, 31.0, 14.1 and 56.7 for pyrimethamine. Before the 12-month culture they were 472.3, 452.9, 352.7, 773.7, 702.7 and 322.7 nM for chloroquine; 2.6, 13.2, 8.5, 17.2, 5.0 and 4.0 nM for mefloquine; 6.2, 85.4, 53.9, 38.5, 35.8 and 38.5 nM for quinine; 106.8, 74.3, 112.4, 89.8, 91.8 and 103.3 nM for cycloguanil, and 26.9, 31.4, 47.0, 28.1, 14.9 and 56.7 nM for pyrimethamine. Thus none of these isolates differed in their original susceptibilities after either of these procedures.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  2. Osman CP, Ismail NH, Ahmad R, Ahmat N, Awang K, Jaafar FM
    Molecules, 2010;15(10):7218-26.
    PMID: 20966871 DOI: 10.3390/molecules15107218
    Dichloromethane root extract of Rennellia elliptica Korth. showed strong inhibition of Plasmodium falciparum growth in vitro with an IC₅₀ value of 4.04 µg/mL. A phytochemical study of the dichloromethane root extract has led to the isolation and characterization of a new anthraquinone, 1,2-dimethoxy-6-methyl-9,10-anthraquinone (1), and ten known anthraquinones: 1-hydroxy-2-methoxy-6-methyl-9,10-anthraquinone (2), nordamnacanthal (3), 2-formyl-3-hydroxy-9,10-anthraquinone (4), damnacanthal (5), lucidin-ω-methyl ether (6), 3-hydroxy-2-methyl-9,10-anthraquinone (7), rubiadin (8), 3-hydroxy-2-methoxy-6-methyl-9,10-anthraquinone (9), rubiadin-1-methyl ether (10) and 3-hydroxy-2-hydroxymethyl-9,10-anthraquinone (11). Structural elucidation of all compounds was accomplished by modern spectroscopic methods, notably 1D and 2D NMR, IR, UV and HREIMS. The new anthraquinone 1, 2-formyl-3-hydroxy-9,10-anthraquinone (4) and 3-hydroxy-2-methyl-9,10-anthraquinone (7) possess strong antiplasmodial activity, with IC₅₀ values of 1.10, 0.63 and 0.34 µM, respectively.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  3. Ang HH, Cheang HS
    Chemotherapy, 1999 Nov-Dec;45(6):446-51.
    PMID: 10567775
    Thirty clones were obtained from five Malaysian Plasmodium falciparum isolates using the limiting dilution method. These clones were then subjected to antimalarial testing using the modified in vitro microtechnique. The results showed that ST 85/B3, GC/C10 and ST 85/A2 clones decreased their susceptibilities to 19, 41 and 28% whilst ST 12/F8, ST 85/B3 and ST 85/B3 clones showed increases of 6, 43 and 21%, respectively, against chloroquine, mefloquine and quinine after cryopreservation. Further results also indicated that GC/B4, GC/B7, GC/C10, ST 85/A5, ST 85/D3, ST 148/F8 clones did not show any change (up to 2 decimal places) against chloroquine, ST 12/D5, ST 12/E8, ST 12/F8, ST 148/A5 clones against quinine after cryopreservation. They, however, maintained their original susceptibilities after cryopreservation.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  4. Ang HH, Chan KL, Mak JW
    Folia Parasitol., 1998;45(3):196-8.
    PMID: 9805783
    Five Malaysian isolates of the protozoan Plasmodium falciparum Welch were cultured in vitro following the method of Trager and Jensen (1976, 1977) and subsequently cloned using the limiting dilution method of Rosario (1981). Thirty clones were obtained and were later characterized against schizontocidal drugs, chloroquine, mefloquine and quinine, using the modified in vitro microtechnique. Results showed that these local isolates were heterogeneous and most of the clones exhibited similar pattern of susceptibility as their parent isolate except for ST 168 clone and two ST 195 clones that were sensitive but two ST 165 clones, two ST 168 clones and five ST 195 clones were resistant against quinine, respectively. Results also indicated that they were pure clones compared to their parent isolate because their drug susceptibility studies were significantly different (p < 0.05).
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  5. Gilles HM
    J Infect, 1989 Jan;18(1):11-23.
    PMID: 2644358
    The epidemiology, clinical features, diagnosis, prognosis, management, chemotherapy and chemoprophylaxis of malaria are reviewed.
    Matched MeSH terms: Plasmodium falciparum/drug effects
  6. van Schalkwyk DA, Blasco B, Davina Nuñez R, Liew JWK, Amir A, Lau YL, et al.
    PMID: 30831468 DOI: 10.1016/j.ijpddr.2019.02.004
    New antimalarial agents are identified and developed after extensive testing on Plasmodium falciparum parasites that can be grown in vitro. These susceptibility studies are important to inform lead optimisation and support further drug development. Until recently, little was known about the susceptibility of non-falciparum species as these had not been adapted to in vitro culture. The recent culture adaptation of P. knowlesi has therefore offered an opportunity to routinely define the drug susceptibility of this species, which is phylogenetically closer to all other human malarias than is P. falciparum. We compared the in vitro susceptibility of P. knowlesi and P. falciparum to a range of established and novel antimalarial agents under identical assay conditions. We demonstrated that P. knowlesi is significantly less susceptible than P. falciparum to six of the compounds tested; and notably these include three ATP4 inhibitors currently under development as novel antimalarial agents, and one investigational antimalarial, AN13762, which is 67 fold less effective against P. knowlesi. For the other compounds there was a less than two-fold difference in susceptibility between species. We then compared the susceptibility of a recent P. knowlesi isolate, UM01, to that of the well-established, older A1-H.1 clone. This recent isolate showed similar in vitro drug susceptibility to the A1-H.1 clone, supporting the ongoing use of the better characterised clone to further study drug susceptibility. Lastly, we used isobologram analysis to explore the interaction of a selection of drug combinations and showed similar drug interactions across species. The species differences in drug susceptibility reported by us here and previously, support adding in vitro drug screens against P. knowlesi to those using P. falciparum strains to inform new drug discovery and lead optimisation.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  7. Lundie AR
    J Clin Pathol, 1969 Jul;22(4):509.
    PMID: 4894850
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  8. Clyde DF, Han CM, Huang YS
    Trans R Soc Trop Med Hyg, 1973;67(1):146.
    PMID: 4591211
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  9. Mahoney LE
    Lancet, 1968 Nov 23;2(7578):1139.
    PMID: 4177183
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  10. Ravindar L, Hasbullah SA, Rakesh KP, Raheem S, Ismail N, Ling LY, et al.
    Bioorg Med Chem Lett, 2024 Dec 01;114:129992.
    PMID: 39426430 DOI: 10.1016/j.bmcl.2024.129992
    Malaria continues to pose a significant threat to global health, which is exacerbated by the emergence of drug-resistant strains, necessitating the urgent development of new therapeutic options. Due to their substantial bioactivity in treating malaria, pyridine and pyrimidine have become the focal point of drug research. Hybrids of pyridine and pyrimidine offer a novel and promising avenue for developing effective antimalarial agents. The ability of these hybrids to overcome drug resistance is tinted, offering a potential solution to this critical obstacle in the treatment of malaria. By targeting multiple pathways, these hybrid compounds reduce the likelihood of resistance development, providing a promising strategy for combating drug-resistant strains of malaria. The review focuses on the most recent developments in 2018 in the structural optimization of pyridine and pyrimidine hybrid compounds, highlighting modifications that have been shown to improve antimalarial activity. Structure-activity studies have elucidated the essential characteristics required for potency, selectivity, and pharmacokinetics. Molecular docking and virtual screening expedite the identification of novel compounds with enhanced activity profiles. This analysis could aid in developing the most effective pyridine and pyrimidine hybrids as antimalarial agents.
    Matched MeSH terms: Plasmodium falciparum/drug effects
  11. Naghibi F, Esmaeili S, Abdullah NR, Nateghpour M, Taghvai M, Kamkar S, et al.
    Biomed Res Int, 2013;2013:316185.
    PMID: 24455686 DOI: 10.1155/2013/316185
    Based on the collected ethnobotanical data from the Traditional Medicine and Materia Medica Research Center (TMRC), Iran, Myrtus communis L. (myrtle) was selected for the assessment of in vitro and in vivo antimalarial and cytotoxic activities. Methanolic extract of myrtle was prepared from the aerial parts and assessed for antiplasmodial activity, using the parasite lactate dehydrogenase (pLDH) assay against chloroquine-resistant (K1) and chloroquine-sensitive (3D7) strains of Plasmodium falciparum. The 4-day suppressive test was employed to determine the parasitemia suppression of the myrtle extract against P. berghei in vivo. The IC50 values of myrtle extract were 35.44 µg/ml against K1 and 0.87 µg/ml against 3D7. Myrtle extract showed a significant suppression of parasitaemia (84.8 ± 1.1% at 10 mg/kg/day) in mice infected with P. berghei after 4 days of treatment. Cytotoxic activity was carried out against mammalian cell lines using methyl thiazol tetrazolium (MTT) assay. No cytotoxic effect on mammalian cell lines up to 100 µg/mL was shown. The results support the traditional use of myrtle in malaria. Phytochemical investigation and understanding the mechanism of action would be in our upcoming project.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  12. Parker D, Lerdprom R, Srisatjarak W, Yan G, Sattabongkot J, Wood J, et al.
    Malar J, 2012 Aug 21;11:290.
    PMID: 22908880 DOI: 10.1186/1475-2875-11-290
    BACKGROUND: Drug and multidrug-resistant Plasmodium falciparum malaria has existed in Thailand for several decades. Furthermore, Thailand serves as a sentinel for drug-resistant malaria within the Greater Mekong sub-region. However, the drug resistance situation is highly dynamic, changing quickly over time. Here parasite in vitro drug sensitivity is reported for artemisinin derivatives, mefloquine, chloroquine and quinine, across Thailand.

    METHODS: Blood was drawn from patients infected with P. falciparum in seven sentinel provinces along Thai international borders with Cambodia, Myanmar, Laos, and Malaysia. In vitro parasite sensitivity was tested using the World Health Organization's microtest (mark III) (between 1994 and 2002) and the histidine-rich protein-2 (HRP2)-based enzyme-linked immunosorbent assay (in 2010). Following World Health Organization protocol, at least 30 isolates were collected for each province and year represented in this study. Where possible, t-tests were used to test for significant differences.

    RESULTS: There appears to be little variation across study sites with regard to parasite sensitivity to chloroquine. Quinine resistance appears to have been rising prior to 1997, but has subsequently decreased. Mefloquine sensitivity appears high across the provinces, especially along the north-western border with Myanmar and the eastern border with Cambodia. Finally, the data suggest that parasite sensitivity to artemisinin and its derivatives is significantly higher in provinces along the north-western border with Myanmar.

    CONCLUSIONS: Parasite sensitivity to anti-malarials in Thailand is highly variable over time and largely mirrors official drug use policy. The findings with regard to reduced sensitivity to artemisinin derivatives are supported by recent reports of reduced parasite clearance associated with artemisinin. This trend is alarming since artemisinin is considered the last defence against malaria. Continued surveillance in Thailand, along with increased collaboration and surveillance across the entire Greater Mekong sub-region, is clearly warranted.

    Matched MeSH terms: Plasmodium falciparum/drug effects*
  13. Wong SK, Lim YY, Abdullah NR, Nordin FJ
    PMID: 21232161 DOI: 10.1186/1472-6882-11-3
    Studies have shown that the barks and roots of some Apocynaceae species have anticancer and antimalarial properties. In this study, leaf extracts of five selected species of Apocynaceae used in traditional medicine (Alstonia angustiloba, Calotropis gigantea, Dyera costulata, Kopsia fruticosa and Vallaris glabra) were assessed for antiproliferative (APF) and antiplasmodial (APM) activities, and analysed for total alkaloid content (TAC), total phenolic content (TPC) and radical-scavenging activity (RSA). As V. glabra leaf extracts showed wide spectrum APF and APM activities, they were further screened for saponins, tannins, cardenolides and terpenoids.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  14. Sholikhah EN, Wijayanti MA, Nurani LH, Mustofa
    Med J Malaysia, 2008 Jul;63 Suppl A:98-9.
    PMID: 19025003
    In previous study, in vitro antiplasmodial activity fractions isolated from methanol extract of E. longifolia, Jack. have been evaluated. Among 5 isolates evaluated from the study, isolate 4 showed high in vitro antiplasmodial activity. However, which stage specificity of the isolates on P. falciparum cycles has not been evaluated. This study was intended to evaluate the stage specificity of the isolate on P. falciparum cycles. The study was conducted by observing the percentage of each stages of P. falciparum microscopically after 8, 16, 24, 32, 40, 48, 56, 64, and 72 hours incubation periods with 3 various concentration of isolate 4 compared with control. The result showed that isolate 4 of E. longifolia root methanol soluble fractions most potent at trophozoites stages of P. falciparum.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  15. Min TH, Khairul MF, Low JH, Che Nasriyyah CH, A'shikin AN, Norazmi MN, et al.
    Exp Parasitol, 2007 Apr;115(4):387-92.
    PMID: 17118354
    Chloroquine (CQ) and mefloquine (MQ) are no longer potent antimalarial drugs due to the emergence of resistant Plasmodium falciparum. Combination therapy has become the standard for many regimes in overcoming drug resistance. Roxithromycin (ROM), a known p-glycoprotein inhibitor, is reported to have antimalarial activity and it is hoped it will potentiate the effects of both CQ/MQ and reverse CQ/MQ-resistance. We assayed the effects of CQ and MQ individually and in combination with ROM on synchronized P. falciparum (Dd2 strain) cultures. The IC(50) values of CQ and MQ were 60.0+/-5.0 and 16.0+/-3.0 ng/ml; these were decreased substantially when combined with ROM. Isobolograms indicate that CQ-ROM combinations were relatively more synergistic (mean FICI 0.70) than MQ-ROM (mean FICI 0.85) with their synergistic effect at par with CQ-verapamil (VRP) (mean FICI 0.64) and MQ-VRP (mean FICI 0.60) combinations. We conclude that ROM potentiates the CQ/MQ response on multidrug-resistant P. falciparum.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  16. Ang HH, Cheang HS, Mak JW
    Chemotherapy, 2005 Oct;51(6):377-80.
    PMID: 16227695
    Exposure of Plasmodium falciparum to increasing sublethal drug concentrations followed by drug treatment led to the development of many resistant parasites. Therefore, the susceptibility of these clones to the type II antifolate drugs, cycloguanil and pyrimethamine, before and after subculturing them in vitro for a period of 3 years, was studied.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  17. Rahman NNNA
    Med J Malaysia, 1997 Dec;52(4):390-8.
    PMID: 10968116
    K1 strain of Plasmdoium falciparum is resistant in vitro to chloroquine, pyrimethamine and sulfadoxine. Response of this strain to combinations of antimalarial drugs in the in vitro hypoxanthine incorporation test was coupled with that of a line of strain NF54 relatively sensitive to chloroquine and fully sensitive to other antimalarials. Pyrimethamine and sulfadoxine showed potentiative synergism against NF54 and less marked against K1. Erythromycin and chloroquine showed potentiation, but less marked against NF54. Quinine and clindamycin had an additive effect against NF54 but potentiated against K1. Combinations of chloroquine with quinine or amodiaquine or of amodiaquine with clindamycin or erythromycin showed mild antagonistic or additive effects. In vivo studies in mice, using the 4-day suppressive test, the AS(3CQ) clone of Plasmodium chabaudi was resistant to pyrimethamine and chloroquine but sensitive to sulfadoxine. Similar combinations as above were carried out and their responses were compared between the resistant and sensitive strains. For both strains, the combinations of chloroquine-erythromycin, pyrimethamine-sulfadoxine, quinine-clindamycin showed potentiation; antagonistic effects were observed in chloroquine-amodiaquine combinations whereas when amodiaquine combined with erythromycin the effect was additive. Amodiaquine-clindamycin and chloroquine-quinine combinations have an antagonistic effect against the sensitive strain but additive against the resistant strain.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  18. Yapp DT, Yap SY
    J Ethnopharmacol, 2003 Mar;85(1):145-50.
    PMID: 12576213
    Malaria remains a global problem in the light of chloroquine-resistant strains of Plasmodium falciparum. New compounds are needed for the development of novel antimalarial drugs. Seed, leaf, and fruit skin extracts of Lansium domesticum, a common fruit tree in South-East Asia, are used by indigenous tribes in Sabah, Malaysia for treating malaria. The skin and aqueous leaf extracts of the tree were found to reduce parasite populations of the drug sensitive strain (3D7) and the chloroquine-resistant strain (T9) of P. falciparum equally well. The skin extracts were also found to interrupt the lifecycle of the parasite. The data reported here indicate that extracts of L. domesticum are a potential source for compounds with activity towards chloroquine-resistant strains of P. falciparum.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
  19. Najib Nik A Rahman N, Furuta T, Kojima S, Takane K, Ali Mohd M
    J Ethnopharmacol, 1999 Mar;64(3):249-54.
    PMID: 10363840
    In vitro and in vivo studies revealed that Malaysian medicinal plants, Piper sarmentosum, Andrographis paniculata and Tinospora crispa produced considerable antimalarial effects. Chloroform extract in vitro did show better effect than the methanol extract. The chloroform extract showed complete parasite growth inhibition as low as 0.05 mg/ml drug dose within 24 h incubation period (Andrographis paniculata) as compared to methanol extract of drug dose of 2.5 mg/ml but under incubation time of 48 h of the same plant spesies. In vivo activity of Andrographis paniculata also demonstrated higher antimalarial effect than other two plant species.
    Matched MeSH terms: Plasmodium falciparum/drug effects*
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