Genomes and Genes
parasitic sensitivity tests
Summary: Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites.
- Zatra R, Lekana Douki J, Lekoulou F, Bisvigou U, Ngoungou E, Ndouo F. In vitro antimalarial susceptibility and molecular markers of drug resistance in Franceville, Gabon. BMC Infect Dis. 2012;12:307 pubmed publisher..1%, 97.8%, and 0% and 22.2%. These high levels of antimalarial drug resistance in Franceville, Gabon, call for reinforced surveillance of drug efficacy. ..
- Witkowski B, Khim N, Chim P, Kim S, Ke S, Kloeung N, et al. Reduced artemisinin susceptibility of Plasmodium falciparum ring stages in western Cambodia. Antimicrob Agents Chemother. 2013;57:914-23 pubmed publisher..The reduced susceptibility to artemisinin in Pailin appears to be associated with an altered in vitro phenotype of ring stages from Pailin in the RSA. ..
- Leang R, Barrette A, Bouth D, Menard D, Abdur R, Duong S, et al. Efficacy of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum and Plasmodium vivax in Cambodia, 2008 to 2010. Antimicrob Agents Chemother. 2013;57:818-26 pubmed publisher..Although DP appears to be an appropriate new first-line treatment for P. vivax in Cambodia, alternative treatments are urgently needed for P. falciparum-infected patients in western Cambodia. ..
- Rocha T, de Brum Vieira P, Gnoatto S, Tasca T, Gosmann G. Anti-Trichomonas vaginalis activity of saponins from Quillaja, Passiflora, and Ilex species. Parasitol Res. 2012;110:2551-6 pubmed publisher..vaginalis activity (MIC?=?0.025%). In addition, all samples induced erythrocyte lysis and LDH release. As far as we know, this is the first report demonstrating the potential anti-T. vaginalis activity of these saponins...
- Shahinas D, Lau R, Khairnar K, Hancock D, Pillai D. Artesunate misuse and Plasmodium falciparum malaria in traveler returning from Africa. Emerg Infect Dis. 2010;16:1608-10 pubmed publisher..Isolates had an elevated 50% inhibitory concentration to artemisinin, artesunate, and artemether, compared with that of other African isolates. Inappropriate use of artemisinin derivatives can reduce P. falciparum susceptibility. ..
- Rijken M, Boel M, Russell B, Imwong M, Leimanis M, Phyo A, et al. Chloroquine resistant vivax malaria in a pregnant woman on the western border of Thailand. Malar J. 2011;10:113 pubmed publisher..vivax. This is the first clinically and laboratory confirmed case of two high-grade CQ resistant vivax parasite strains from Thailand. ..
- Brand S, Cleghorn L, McElroy S, Robinson D, Smith V, Hallyburton I, et al. Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors. J Med Chem. 2012;55:140-52 pubmed publisher..This compound provides an excellent tool for validation of T. brucei NMT as a drug target for HAT as well as a valuable lead for further optimization. ..
- Wein S, Maynadier M, Tran Van Ba C, Cerdan R, Peyrottes S, Fraisse L, et al. Reliability of antimalarial sensitivity tests depends on drug mechanisms of action. J Clin Microbiol. 2010;48:1651-60 pubmed publisher..Some of them might not detect the antimalarial potential of new classes of compounds with innovative modes of action, which subsequently could become promising new antimalarial drugs. ..
- Kotze A, Lowe A, O Grady J, Kopp S, Behnke J. Dose-response assay templates for in vitro assessment of resistance to benzimidazole and nicotinic acetylcholine receptor agonist drugs in human hookworms. Am J Trop Med Hyg. 2009;81:163-70 pubmed..These assays will have immediate applicability in monitoring for the emergence of drug resistance in human hookworm populations. ..
- Nsobya S, Kiggundu M, Nanyunja S, Joloba M, Greenhouse B, Rosenthal P. In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda. Antimicrob Agents Chemother. 2010;54:1200-6 pubmed publisher..In summary, we demonstrated in parasites from Kampala a range of sensitivities to older drugs; correlation of sensitivities to CQ, MDAQ, and QN; and good activity against nearly all strains for DHA, LM, and PQ...
- Süzgeç Selçuk S, Meriçli A, Güven K, Kaiser M, Casey R, Hingley Wilson S, et al. Evaluation of Turkish seaweeds for antiprotozoal, antimycobacterial and cytotoxic activities. Phytother Res. 2011;25:778-83 pubmed publisher..This is the second study investigating the antiprotozoal activities of Turkish marine algae and identifies Dasya pedicellata, an understudied algal species, as a candidate for further studies. ..
- Nam T, McNamara C, Bopp S, Dharia N, Meister S, Bonamy G, et al. A chemical genomic analysis of decoquinate, a Plasmodium falciparum cytochrome b inhibitor. ACS Chem Biol. 2011;6:1214-22 pubmed publisher..The basis for this difference was revealed by molecular docking studies, in which both of these inhibitors were shown to have distinctly different modes of binding within the ubiquinol-binding site of cytochrome b. ..
- Yuan J, Cheng K, Johnson R, Huang R, Pattaradilokrat S, Liu A, et al. Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. Science. 2011;333:724-9 pubmed publisher..Drugs whose responses mapped to wild-type or mutant pfcrt alleles were tested in combination in vitro and in vivo, which yielded promising new leads for antimalarial treatments. ..
- Phompradit P, Wisedpanichkij R, Muhamad P, Chaijaroenkul W, Na Bangchang K. Molecular analysis of pfatp6 and pfmdr1 polymorphisms and their association with in vitro sensitivity in Plasmodium falciparum isolates from the Thai-Myanmar border. Acta Trop. 2011;120:130-5 pubmed publisher..No association between mutation or amplification of pfatp6 gene and in vitro susceptibility of P. falciparum isolates was found. ..
- López Soto F, Leon Sicairos N, Nazmi K, Bolscher J, de la Garza M. Microbicidal effect of the lactoferrin peptides lactoferricin17-30, lactoferrampin265-284, and lactoferrin chimera on the parasite Entamoeba histolytica. Biometals. 2010;23:563-8 pubmed publisher..The lactoferrin-peptides might be useful as therapeutic agents against amoebiasis and thereby diminish the use of metronidazole, which is extremely toxic for the host. ..
- Jambou R, Martinelli A, Pinto J, Gribaldo S, Legrand E, Niang M, et al. Geographic structuring of the Plasmodium falciparum sarco(endo)plasmic reticulum Ca2+ ATPase (PfSERCA) gene diversity. PLoS ONE. 2010;5:e9424 pubmed publisher..One possible contributor could be the frequency of haemoglobinopathies that are associated with calcium dysregulation in the erythrocyte...
- Jacobs R, Nare B, Wring S, Orr M, Chen D, Sligar J, et al. SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis. PLoS Negl Trop Dis. 2011;5:e1151 pubmed publisher..We have discovered and optimized a novel class of small-molecule boron-containing compounds, benzoxaboroles, to identify SCYX-7158 as an effective, safe and orally active treatment for HAT...
- Peatey C, Skinner Adams T, Dixon M, McCarthy J, Gardiner D, Trenholme K. Effect of antimalarial drugs on Plasmodium falciparum gametocytes. J Infect Dis. 2009;200:1518-21 pubmed publisher..Although a dose-dependent reduction in late-stage gametocyte viability was observed, none of the drugs tested statistically significantly reduced gametocyte numbers. ..
- Urbina J. Ergosterol biosynthesis and drug development for Chagas disease. Mem Inst Oswaldo Cruz. 2009;104 Suppl 1:311-8 pubmed..cruzi infections. ..
- Matsuo A, Silva L, Torrecilhas A, Pascoalino B, Ramos T, Rodrigues E, et al. In vitro and in vivo trypanocidal effects of the cyclopalladated compound 7a, a drug candidate for treatment of Chagas' disease. Antimicrob Agents Chemother. 2010;54:3318-25 pubmed publisher..The 7a cyclopalladate complex exerts an apoptosis-like death in T. cruzi trypomastigote forms and causes mitochondrion disruption seen by electron microscopy. ..
- Lucumi E, Darling C, Jo H, Napper A, Chandramohanadas R, Fisher N, et al. Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay. Antimicrob Agents Chemother. 2010;54:3597-604 pubmed publisher..Ultimately, this study may provide new probes to understand the molecular details of the malaria life cycle and to identify new antimalarials. ..
- Paguio M, Bogle K, Roepe P. Plasmodium falciparum resistance to cytocidal versus cytostatic effects of chloroquine. Mol Biochem Parasitol. 2011;178:1-6 pubmed publisher..falciparum. The results have important implications for development of new antimalarial drugs and for fully defining the genetic loci that confer clinically relevant antimalarial drug resistance phenomena. ..
- Pradines B, Briolant S, Henry M, Oeuvray C, Baret E, Amalvict R, et al. Absence of association between pyronaridine in vitro responses and polymorphisms in genes involved in quinoline resistance in Plasmodium falciparum. Malar J. 2010;9:339 pubmed publisher..These results confirm the interest and the efficacy of the use of a combination of pyronaridine and artesunate in areas in which parasites are resistant to quinolines. ..
- Shahinas D, Liang M, Datti A, Pillai D. A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. J Med Chem. 2010;53:3552-7 pubmed publisher..These data support PfHsp90 as a specific antimalarial target with potential for synergy with known antimalarials. ..
- Kemgne E, Mbacham W, Boyom F, Zollo P, Tsamo E, Rosenthal P. In vitro sensitivity of Plasmodium falciparum field isolates to extracts from Cameroonian Annonaceae plants. Parasitol Res. 2012;110:109-17 pubmed publisher..In summary, acetogenin-rich fractions from Annonaceae species showed high potency against P. falciparum field isolates and safety by oral administration in mice, supporting their detailed investigation for antimalarial drug discovery. ..
- Andriantsoanirina V, Lascombes V, Ratsimbasoa A, Bouchier C, Hoffman J, Tichit M, et al. Rapid detection of point mutations in Plasmodium falciparum genes associated with antimalarial drugs resistance by using High-Resolution Melting analysis. J Microbiol Methods. 2009;78:165-70 pubmed publisher..Results perfectly matched those obtained by DNA sequencing for some important genetic markers of P. falciparum resistance. This technique could be of great value for epidemiological studies, especially in developing countries. ..
- Rottmann M, McNamara C, Yeung B, Lee M, Zou B, Russell B, et al. Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010;329:1175-80 pubmed publisher..The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model. ..
- Mungthin M, Suwandittakul N, Chaijaroenkul W, Rungsrihirunrat K, Harnyuttanakorn P, Seugorn A, et al. The patterns of mutation and amplification of Plasmodium falciparum pfcrt and pfmdr1 genes in Thailand during the year 1988 to 2003. Parasitol Res. 2010;107:539-45 pubmed publisher..The prominent pattern of pfmdr1 at codons 86/184/1034/1042/1246 was NFSND, with prevalence increasing from 40% to 95% during the 10-year period. ..
- Moneriz C, Marín García P, Bautista J, Diez A, Puyet A. Haemoglobin interference and increased sensitivity of fluorimetric assays for quantification of low-parasitaemia Plasmodium infected erythrocytes. Malar J. 2009;8:279 pubmed publisher..5 to 0.1. The use of PG microassays on detergent-free, haemoglobin-depleted samples appears as the best choice both for the detection of Plasmodium in low-density infections and anti-malarial drugs tests. ..
- Pradines B, Pistone T, Ezzedine K, Briolant S, Bertaux L, Receveur M, et al. Quinine-resistant malaria in traveler returning from Senegal, 2007. Emerg Infect Dis. 2010;16:546-8 pubmed publisher..Clinical quinine failure was associated with a 50% inhibitory concentration of 829 nmol/L. Increased vigilance is required during treatment follow-up...
- da Luz R, Vermeersch M, Dujardin J, Cos P, Maes L. In vitro sensitivity testing of Leishmania clinical field isolates: preconditioning of promastigotes enhances infectivity for macrophage host cells. Antimicrob Agents Chemother. 2009;53:5197-203 pubmed publisher..In conclusion, the proposed conditioning protocol further contributes toward a more standardized laboratory model for evaluation of the drug sensitivities of field isolates. ..
- Chevalley S, Coste A, Lopez A, Pipy B, Valentin A. Flow cytometry for the evaluation of anti-plasmodial activity of drugs on Plasmodium falciparum gametocytes. Malar J. 2010;9:49 pubmed publisher..These data form the basis of further studies for developing new methods in drug discovery to decrease malaria transmission. ..
- Brak K, Kerr I, Barrett K, Fuchi N, Debnath M, Ang K, et al. Nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors as promising new leads for Chagas disease chemotherapy. J Med Chem. 2010;53:1763-73 pubmed publisher..These results suggest that nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors have the potential to fulfill the urgent need for improved Chagas disease chemotherapy. ..
- Fall B, Diawara S, Sow K, Baret E, Diatta B, Fall K, et al. Ex vivo susceptibility of Plasmodium falciparum isolates from Dakar, Senegal, to seven standard anti-malarial drugs. Malar J. 2011;10:310 pubmed publisher..Taken together, these data suggest that intensive surveillance of the P. falciparum in vitro susceptibility to anti-malarial drugs in Senegal is required. ..
- Ang K, Ratnam J, Gut J, Legac J, Hansell E, Mackey Z, et al. Mining a cathepsin inhibitor library for new antiparasitic drug leads. PLoS Negl Trop Dis. 2011;5:e1023 pubmed publisher..The end products of this effort include the identification of sub-micromolar cell-active leads as well as the elucidation of structure-activity trends that can guide further optimization efforts. ..
- de Medeiros M, da Silva A, Citó A, Borges A, de Lima S, Lopes J, et al. In vitro antileishmanial activity and cytotoxicity of essential oil from Lippia sidoides Cham. Parasitol Int. 2011;60:237-41 pubmed publisher..The LSEO's activity against both promastigote and the amstigote forms of L. amazonensis, together with its low toxicity to mammalian cells, point to LSEO as a promising agent for the treatment of cutaneous leishmaniasis...
- Boyom F, Ngouana V, Kemgne E, Zollo P, Menut C, Bessiere J, et al. Antiplasmodial volatile extracts from Cleistopholis patens Engler & Diels and Uvariastrum pierreanum Engl. (Engl. & Diels) (Annonaceae) growing in Cameroon. Parasitol Res. 2011;108:1211-7 pubmed publisher..patens and 6.08 and 13.96 ?g/mL, respectively, for those from U. pierreanum. These results indicate that essential oils may offer a promising alternative for the development of new antimalarials. ..
- Jones D, Hallyburton I, Stojanovski L, Read K, Frearson J, Fairlamb A. Identification of a ?-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis. Biochem Pharmacol. 2010;80:1478-86 pubmed publisher..Among the other potent, but less selective screening hits were compound classes with activity against protein kinases, topoisomerases, tubulin, as well as DNA and energy metabolism. ..
- Chaijaroenkul W, Wisedpanichkij R, Na Bangchang K. Monitoring of in vitro susceptibilities and molecular markers of resistance of Plasmodium falciparum isolates from Thai-Myanmar border to chloroquine, quinine, mefloquine and artesunate. Acta Trop. 2010;113:190-4 pubmed publisher..Moreover, the correlation between pfmdr1 gene amplification and susceptibility of the parasite to MQ, QN and AS was observed (decreased susceptibilities to MQ, QN and AS in isolates with increased pfmdr1 copy number). ..
- Suwandittakul N, Chaijaroenkul W, Harnyuttanakorn P, Mungthin M, Na Bangchang K. Drug resistance and in vitro susceptibility of Plasmodium falciparum in Thailand during 1988-2003. Korean J Parasitol. 2009;47:139-44 pubmed publisher..Drug pressure has impact on sensitivity of P. falciparum to MQ. A combination therapy of MQ and ARS is being applied to reduce the parasite resistance, and also increasing the efficacy of the drug. ..
- Andriantsoanirina V, Ratsimbasoa A, Bouchier C, Jahevitra M, Rabearimanana S, Radrianjafy R, et al. Plasmodium falciparum drug resistance in Madagascar: facing the spread of unusual pfdhfr and pfmdr-1 haplotypes and the decrease of dihydroartemisinin susceptibility. Antimicrob Agents Chemother. 2009;53:4588-97 pubmed publisher..In the context of the implementation of the new national policy for the fight against malaria, continued surveillance for the detection of P. falciparum resistance in the future is required. ..
- Tucker M, Mutka T, Sparks K, Patel J, Kyle D. Phenotypic and genotypic analysis of in vitro-selected artemisinin-resistant progeny of Plasmodium falciparum. Antimicrob Agents Chemother. 2012;56:302-14 pubmed publisher..In summary, we define the artemisinin resistance phenotype as a decrease in susceptibility to artemisinins along with the ability to recover from drug-induced dormancy following supraclinical concentrations of the drug. ..
- Teuscher F, Chen N, Kyle D, Gatton M, Cheng Q. Phenotypic changes in artemisinin-resistant Plasmodium falciparum lines in vitro: evidence for decreased sensitivity to dormancy and growth inhibition. Antimicrob Agents Chemother. 2012;56:428-31 pubmed publisher..Our results demonstrate that the AL resistance phenotype has (i) decreased sensitivity of mature-stage parasites, (ii) decreased sensitivity of the ring stage to the induction of dormancy, and (iii) a faster recovery from dormancy. ..
- Pelleau S, Bertaux L, Briolant S, Ferdig M, Sinou V, Pradines B, et al. Differential association of Plasmodium falciparum Na+/H+ exchanger polymorphism and quinine responses in field- and culture-adapted isolates of Plasmodium falciparum. Antimicrob Agents Chemother. 2011;55:5834-41 pubmed publisher..However, we do not exclude the possibility that in particular settings, Pfnhe-1 polymorphism can be used as a molecular marker for surveillance of quinine resistance. ..
- Peatey C, Spicer T, Hodder P, Trenholme K, Gardiner D. A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes. Mol Biochem Parasitol. 2011;180:127-31 pubmed publisher..Here we describe the development of a robust and simple assay that is amenable to a high throughput format for the discovery of new antigametocyte drugs. ..
- Kaiser M, Bray M, Cal M, Bourdin Trunz B, Torreele E, Brun R. Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness. Antimicrob Agents Chemother. 2011;55:5602-8 pubmed publisher..b. gambiense and T. b. rhodesiense forms of human sleeping sickness and both stages of the disease. ..
- Shokri A, Sharifi I, Khamesipour A, Nakhaee N, Fasihi Harandi M, Nosratabadi J, et al. The effect of verapamil on in vitro susceptibility of promastigote and amastigote stages of Leishmania tropica to meglumine antimoniate. Parasitol Res. 2012;110:1113-7 pubmed publisher..tropica to MA. Further works are required to evaluate this synergistic effect on animal model or volunteer human subjects...
- Engel J, Ang K, Chen S, Arkin M, McKerrow J, Doyle P. Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. Antimicrob Agents Chemother. 2010;54:3326-34 pubmed publisher..This high-throughput assay will have an important impact in antiparasitic drug discovery. ..
- Tanaka T, Williamson K. A malaria gametocytocidal assay using oxidoreduction indicator, alamarBlue. Mol Biochem Parasitol. 2011;177:160-3 pubmed publisher..01). Six anti-malarials were also tested and at 10 ?M only primaquine and dihydroartemisinin (DHA) had gametocytocidal activity. This new assay provides an important tool to efficiently screen compounds for gametocytocidal activity. ..