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Sent on Thursday, 2012 April 05Search: kinetoplastids OR kinetoplastid OR Kinetoplastida OR "trypanosoma brucei" OR leishmania OR brucei OR leishmaniasis OR "African trypanosomiasis"
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PubMed Results |
1. | Phytother Res. 2012 Apr 4. doi: 10.1002/ptr.4692. [Epub ahead of print]Antitrypanosomal Properties of Panax ginseng C. A. Meyer: New Possibilities for a Remarkable Traditional Drug.Herrmann F, Sporer F, Tahrani A, Wink M.SourceInstitute of Pharmacy and Molecular Biotechnology, Heidelberg University, Germany. Florian.Herrmann@t-online.de. AbstractAfrican trypanosomiasis is still a major health problem in many sub-Saharan countries in Africa. We investigated the effects of three preparations of Panax ginseng, Panax notoginseng, isolated ginsenosides, and the polyacetylene panaxynol on Trypanosoma brucei brucei and the human cancer cell line HeLa. Hexane extracts and the pure panaxynol were toxic and at the same time highly selective against T. b. brucei, whereas methanol extracts and 12 isolated ginsenosides were significantly less toxic and showed only weak selectivity. Panaxynol was cytotoxic against T. b. brucei at the concentration of 0.01 µg/mL with a selectivity index of 858, superior even to established antitrypanosomal drugs. We suggest that the inhibition of trypanothione reductase, which is only found in trypanosomes, might explain the observed selectivity. The high selectivity together with a cytotoxic concentration in the range of the bioavailability makes panaxynol and other polyacetylenes in general very promising lead compounds for the treatment of African trypanosomiasis. Copyright © 2012 John Wiley & Sons, Ltd. Copyright © 2012 John Wiley & Sons, Ltd. |
PMID: 22473703 [PubMed - as supplied by publisher] | |
2. | Eur J Med Chem. 2012 Mar 16. [Epub ahead of print]Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives.Audisio D, Messaoudi S, Cojean S, Peyrat JF, Brion JD, Bories C, Huteau F, Loiseau PM, Alami M.SourceUniv Paris-Sud, CNRS, BioCIS-UMR 8076, Laboratoire de Chimie Thérapeutique, LabEx LERMIT, Faculté de Pharmacie, 5 rue J.-B. Clément, Châtenay-Malabry, F-92296, France. AbstractA new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC(50) values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation. Copyright © 2012 Elsevier Masson SAS. All rights reserved. |
PMID: 22472166 [PubMed - as supplied by publisher] | |
3. | Mol Microbiol. 2011 Dec;82(6):1433-43. doi: 10.1111/j.1365-2958.2011.07900.x. Epub 2011 Nov 10.Replication of the ERES:Golgi junction in bloodstream-form African trypanosomes.Bangs JD.SourceDepartment of Medical Microbiology & Immunology, University of Wisconsin School of Medicine and Public Health, Madison, WI 53706, USA. jdbangs@wisc.edu AbstractThe biogenesis of the ER Exit Site/Golgi Junction (EGJ) in bloodstream-form African trypanosomes is investigated using tagged markers for ER Exit Sites, the Golgi and the bilobe structure. The typical pattern is two EGJ in G1 phase (1 kinetoplast/1 nucleus, 1K1N) through S-phase (2K1N), duplication to four EGJ in post-mitotic cells (2K2N) and segregation of two EGJ to each daughter. Lesser cell percentages have elevated EGJ copy numbers in all stages, and blocking cell cycle progression results in even higher copy numbers. EGJs are closely aligned with the flagellar attachment zone (FAZ) indicating nucleation on the FAZ-associated ER (FAZ:ER). Only the most posterior EGJ in each cell is in proximity to the bilobe, which is located at the base of the FAZ filament near the mouth of the flagellar pocket. These results indicate that EGJ replication in bloodstream trypanosomes is not tightly coupled to the cell cycle. Furthermore, segregation of EGJ is not obligately mediated by the bilobe, rather assembly of the EGJ on the FAZ:ER, which is coupled to the flagellar cytoskeleton, apparently ensures segregation with fidelity during cytokinesis. These findings differ markedly from procyclic-form trypanosomes, and models highlighting these stage-specific differences in EGJ biogenesis are proposed. © 2011 Blackwell Publishing Ltd. |
PMID: 22026408 [PubMed - indexed for MEDLINE] | |
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