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Vitro Antimalarial Activity (vitro + antimalarial_activity)
Selected AbstractsDocking Studies of Structurally Diverse Antimalarial Drugs Targeting PfATP6: No Correlation between in,silico Binding Affinity and in,vitro Antimalarial Activity.CHEMMEDCHEM, Issue 9 2009Fatima Bousejra-El Garah Abstract PfATP6, a calcium-dependent ATPase of Plasmodium falciparum, is considered the putative target of the antimalarial drug artemisinin and its derivatives. Herein, the 3D structure of PfATP6 was modeled on the basis of the crystal structure of SERCA,1a, the mammalian homologue. Model validation was achieved using protein structure checking tools. AutoDock4 was used to predict the binding affinities of artemisinin (and analogues) and various other antimalarial agents for PfATP6, for which in,vitro activity is also reported. No correlation was found between the affinity of the compounds for PfATP6 predicted by AutoDock4 and their antimalarial activity. [source] Synthesis and in vitro Antimalarial Activity of Several Simple Analogues of Peroxyplakoric AcidCHINESE JOURNAL OF CHEMISTRY, Issue 11 2005He-Hua Liu Abstract Several simple analogues of peroxyplakoric acid were synthesized by using Kobayashi's method to construct the key 1,2-dioxane core and tested in vitro for antimalarial activity. The scope and limitation of the method was also briefly examined. [source] Antiparasitic, nematicidal and antifouling constituents from Juniperus berriesPHYTOTHERAPY RESEARCH, Issue 12 2008Volodymyr Samoylenko Abstract A bioassay-guided fractionation of Juniperus procera berries yielded antiparasitic, nematicidal and antifouling constituents, including a wide range of known abietane, pimarane and labdane diterpenes. Among these, abieta-7,13-diene (1) demonstrated in vitro antimalarial activity against Plasmodium falciparum D6 and W2 strains (IC50 = 1.9 and 2.0 µg/mL, respectively), while totarol (6), ferruginol (7) and 7, -hydroxyabieta-8,13-diene-11,12-dione (8) inhibited Leishmania donovani promastigotes with IC50 values of 3.5,4.6 µg/mL. In addition, totarol demonstrated nematicidal and antifouling activities against Caenorhabditis elegans and Artemia salina at a concentration of 80 µg/mL and 1 µg/mL, respectively. The resinous exudate of J. virginiana afforded known antibacterial E -communic acid (4) and 4- epi -abietic acid (5), while the volatile oil from its trunk wood revealed large quantities of cedrol (9). Using GC/MS, the two known abietanes totarol (6) and ferruginol (7) were identified from the berries of J. procera, J. excelsa and J. phoenicea. Copyright © 2008 John Wiley & Sons, Ltd. [source] Study of Antimalarial Activity of Chemical Constituents from Diospyros quaesitaCHEMISTRY & BIODIVERSITY, Issue 11 2008Cui-Ying Ma Abstract Bioassay-directed fractionation led to the isolation of seven compounds from a sample of the dried leaves, twigs, and branches of Diospyros quaesitaThw. (Ebenaceae). One of the isolates, betulinic acid 3-caffeate (1), showed in vitro antimalarial activity against Plasmodium falciparum clones D6 (chloroquine-sensitive) and W2 (chloroquine-resistant) with IC50 values of 1.40 and 0.98,,M, respectively. Evaluation of compound 1 in the human oral epidermoid (KB) cancer cell line revealed cytotoxicity at ED50 of 4.0,,M. In an attempt to reduce the cytotoxicity of 1, the acetylated derivative 1a and betulinic acid (1b) were prepared. Of the seven isolates, diospyrosin (2) was determined to be a new neolignan. In addition to 1, other known compounds isolated in this study were pinoresinol, lariciresinol, N -benzoyl- L -phenylalaninol, scopoletin, and poriferast-5-en-3,,7, -diol. The structure of 2 was elucidated based on spectroscopic data analysis including 1D- and 2D-NMR, and HR-ESI-MS. [source] | ||||||||||