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Sent on Saturday, 2009 Aug 08Search kinetoplastids OR kinetoplastid OR Kinetoplastida OR "trypanosoma brucei" OR leishmania OR brucei OR leishmaniasis OR "African trypanosomiasis"
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| PubMed Results |
- 1: Nat Prod Res. 2009;23(12):1144-50.
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In vitro inhibitory effects of palmatine from Enantia chlorantha on Trypanosoma cruzi and Leishmania infantum.
Faculty of Science, Laboratory of Bio-Organic and Medicinal Chemistry, Department of Organic Chemistry, University of Yaounde I, Box 812 Yaounde, Cameroon.
In an attempt to establish the components responsible for the use of Enantia chlorantha against cutaneous leishmaniasis in local traditional medicine, a well-known palmatine has been isolated in substantial amounts from a methanolic bark extract of this plant species. Palmatine therein obtained exhibited a significant inhibitory activity on growth of both Trypanosoma cruzi (IC(50) 0.068 microM) and Leishmania infantum (IC(50) 0.79 microM).
PMID: 19662580 [PubMed - in process]
- 2: Nat Prod Res. 2009;23(12):1134-43.
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Constituents of Tinospora sinensis and their antileishmanial activity against Leishmania donovani.
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India.
Two new compounds 4-methyl-heptadec-6-enoic acid ethyl ester (2) and 3-hydroxy-2,9,11-trimethoxy-5,6-dihydro isoquino[3,2-a]isoquinolinylium (7) were isolated from an ethanolic extract of the stems of Tinospora sinensis, along with six known compounds (1, 3-6 and 8). The structures of new compounds were established on the basis of detailed spectroscopic studies. Compound 7 exhibited the highest in vitro antileishmanial activity against Leishmania donovani promastigotes and intracellular amastigotes, whereas compounds 2, 4, 5 and 6 demonstrated moderate activity. Other compounds were found to be inactive.
PMID: 19662579 [PubMed - in process]
- 3: Biochem Pharmacol. 2009 Aug 3. [Epub ahead of print]
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Structure-function analysis of the highly conserved charged residues of the membrane protein FT1, the main folic acid transporter of the protozoan parasite Leishmania.
Centre de Recherche en Infectiologie du CHUL, Université Laval, Québec, Canada.
The main plasma membrane folate transporter FT1 of Leishmania belongs to the novel FBT family which is part of the major facilitator superfamily. We have investigated the role of the 10 most conserved charged amino acids of FBTs by site directed mutagenesis. The functions of the mutated proteins were tested for their capacity to transport FA, to sensitize methotrexate resistant cells to methotrexate, for protein production, and for protein localisation. Of the 10 conserved charged amino acids that were mutated to neutral amino acids, all had effects on FT1 transport activities. Only four of the 10 initial mutants (K116L, K133L, R497L, and D529V) retained between 15 and 50% of FT1 activity. The R497 residue was shown to be involved in substrate binding. When the charged conserved residues at position 124, 134, 179, 514, 537 and 565 were changed to neutral amino acids, this led to inactive proteins but the generation of new mutants D124E, R134K, D514E and D537E regained between 20 and 50% of wild-type FT1 activity suggesting that the charge is important for protein function. The mutated protein D179E had, under our standard experimental conditions, no activity, while E565D was completely inactive. The differential activity of the mutated proteins was due either to changes in the apparent Km or Vmax. Mutagenesis experiments have revealed that charged amino acids were essential for FT1 stability or activity and led to a plausible model for the transport of folic acid through FT1.
PMID: 19660435 [PubMed - as supplied by publisher]
- 4: Acta Trop. 2009 Aug 3. [Epub ahead of print]
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Leishmania sp. isolated from human cases of cutaneous leishmaniasis in Brazil characterized as Leishmaniamajor-like.
Departamento de Parasitologia, Instituto de Ciências Biológicas- Universidade Federal de Minas Gerais, CP 486, 30161-970, Belo Horizonte, MG, Brazil.
The identification and characterization of Leishmania are relevant to diagnosis, treatment, eco-epidemiology studies, prophylactic measures and control of the disease. Two strains of Leishmania (MHOM/BR/1971/BH49 and MHOM/BR/1971/BH121), isolated from human cutaneous leishmaniasis, were studied using biological and molecular characteristics, in comparison with WHO reference strains. These studies are important because both strains were incorporated in a vaccine against American Cutaneous Leishmaniasis, and one of these strains has been used to prepare specific and sensitive antigen for serodiagnosis of visceral leishmaniasis in Brazil. Studies were made on the growth rates of promastigotes in Grace's insect medium, infectivity to C57BL/6 and BALB/c mice, electrophoresic mobility patterns of isoenzymes, random amplification of polymorphic DNA (RAPD), simple sequence repeat-anchored PCR amplification (SSR-PCR) and DNA fingerprinting profiles, infectivity to murine macrophages and cellular immune response. Infections of mice and macrophages were significantly different among the strains studied. Attempts to infect mice with culture promastigotes were unsuccessful with BH121, but BH49 infected BALB/c and C57BL/6 mice. Isoenzyme electrophoretic mobility patterns, RAPD and SSR-PCR using DNA amplified by polymerase chain reaction (PCR) with nine arbitrary primers, as well as DNA fingerprinting studies with a biotin-labeled 33.15 fingerprinting probe showed similar profiles to those of the L. major WHO reference strain.
PMID: 19660430 [PubMed - as supplied by publisher]
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