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Leishmanicidal Activity (leishmanicidal + activity)

Distribution by Scientific Domains
Medical Sciences71%
Chemistry28%

Selected Abstracts

Synthesis of 16-Mercaptohexadecylphosphocholine, a Miltefosine Analogue with Leishmanicidal Activity.

CHEMINFORM, Issue 1 2007
Valentin Hornillos
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]

In vitro leishmanicidal activity of some scarce natural products

PHYTOTHERAPY RESEARCH, Issue 7 2004
Marii Takahashi
Abstract Leishmanicidal activity of 46 natural products including several fern and Betula constituents was examined. Several pterosin and atisene compounds from ferns had high activity. Among the triterpenoids the carboxyl group was found to be important for activity. In the diarylheptanoids, the linear-type and the diphenylether-type showed signi,cant activity, and it was found that the carbonyl group at C-11 is necessary for the activity of biphenyl-types. Copyright © 2004 John Wiley & Sons, Ltd. [source]

In vitro Leishmanicidal activity of naturally occurring chalcones

PHYTOTHERAPY RESEARCH, Issue 2 2001
Oliver Kayser
Abstract A variety of chalcones have been shown to exhibit activity against Leishmania parasites. In contrast to synthetic or semisynthetic chalcones, only a few plant-derived compounds have been investigated. To provide a scientific rational for the antiprotozoal potency of plants used in ethnomedicine and containing chalcones, and in the search for new antiprotozoal drugs, we have carried out a primary screening for in vitro leishmanicidal activity of 20 chalcones isolated from plants. The compounds were tested against extracellular promastigotes of Leishmania donovani, L. infantum, L. enrietii and L. major, and against intracellular amastigote L. donovani residing within murine macrophages. Against the extracellular Leishmania (L. donovani), most compounds were active with EC50 values between 0.07 and 2.01,µg/mL. Some of these chalcones, 2,,4,-dihydroxy-4-methoxychalcone, 2,-hydroxy-3,4-dimethoxychalcone and 2-hydroxy-4,4,-dimethoxychalcone also significantly inhibited the intracellular survival of L. donovani parasites with EC50 values between 0.39 and 0.41,µg/mL. When tested against murine bone marrow-derived macrophages as a mammalian host cell control, all compounds with antileishmanial activities also proved to be cytotoxic to varying extents (EC50 0.19,2.06,µg/mL). Correlations between molecular structures and antileishmanial activity are discussed in detail. Specific compounds are illustrated with emphasis on their mode of action and potential for the development of selective antiprotozoal agents. Copyright ­© 2001 John Wiley & Sons, Ltd. [source]

Antileishmanial Physalins from Physalis minima

CHEMISTRY & BIODIVERSITY, Issue 9 2005
Iqbal Choudhary
Three new physalins (1,3) and a new withanolide 7 have been isolated from the whole plant of Physalis minima, along with three known physalins: physalin H (4), isophysalin B (5), and 5,,6, -epoxyphysalin B (6). Their structures were deduced on the basis of in-depth spectroscopic analyses. Compounds 1,6 showed significant in vitro leishmanicidal activities (0.92,19.4,,g/ml) against promastigotes of Leishmania major. [source]

RNA interference reveals a role for TLR2 and TLR3 in the recognition of Leishmania donovani promastigotes by interferon,,-primed macrophages

EUROPEAN JOURNAL OF IMMUNOLOGY, Issue 2 2006
Jean-Frédéric Flandin
Abstract Leishmania donovani promastigotes evade the induction of a proinflammatory response during their invasion of naive macrophages. However, their entry into IFN-,-primed macrophages is accompanied by the secretion of nitric oxide (NO) and proinflammatory cytokines. In the present study, we addressed the hypothesis that priming with IFN-, induces the expression of a receptor that enables mouse macrophages to recognize L. donovani promastigotes. We observed that in IFN-,-primed macrophages, L. donovani promastigotes stimulated Interleukin-1 receptor-associated kinase-1 (IRAK-1) activity. We next showed that Toll-like receptor (TLR)3 is barely detectable in naive macrophages but is expressed in IFN-,-treated macrophages. Silencing of TLR3, TLR2, IRAK-1 and myeloid differentiation factor 88 (MyD88) expression by RNA interference revealed that both TLR are involved in the secretion of NO and TNF-, induced by L. donovani promastigotes. Using L. donovani mutants, we showed that TLR2-mediated responses are dependent on Gal,1,4Man,-PO4 -containing phosphoglycans, whereas TLR3-mediated responses are independent of these glycoconjugates. Furthermore, our data indicate a participation of TLR2 and TLR3 in the phagocytosis of L. donovani promastigotes and a role for TLR3 in the leishmanicidal activity of the IFN-,-primed macrophages. Collectively, our data are consistent with a model where recognition of L. donovani promastigotes depends on the macrophage activation status and requires the expression of TLR3. [source]

In vitro leishmanicidal activity of some scarce natural products

PHYTOTHERAPY RESEARCH, Issue 7 2004
Marii Takahashi
Abstract Leishmanicidal activity of 46 natural products including several fern and Betula constituents was examined. Several pterosin and atisene compounds from ferns had high activity. Among the triterpenoids the carboxyl group was found to be important for activity. In the diarylheptanoids, the linear-type and the diphenylether-type showed signi,cant activity, and it was found that the carbonyl group at C-11 is necessary for the activity of biphenyl-types. Copyright © 2004 John Wiley & Sons, Ltd. [source]

In vitro Leishmanicidal activity of naturally occurring chalcones

PHYTOTHERAPY RESEARCH, Issue 2 2001
Oliver Kayser
Abstract A variety of chalcones have been shown to exhibit activity against Leishmania parasites. In contrast to synthetic or semisynthetic chalcones, only a few plant-derived compounds have been investigated. To provide a scientific rational for the antiprotozoal potency of plants used in ethnomedicine and containing chalcones, and in the search for new antiprotozoal drugs, we have carried out a primary screening for in vitro leishmanicidal activity of 20 chalcones isolated from plants. The compounds were tested against extracellular promastigotes of Leishmania donovani, L. infantum, L. enrietii and L. major, and against intracellular amastigote L. donovani residing within murine macrophages. Against the extracellular Leishmania (L. donovani), most compounds were active with EC50 values between 0.07 and 2.01,µg/mL. Some of these chalcones, 2,,4,-dihydroxy-4-methoxychalcone, 2,-hydroxy-3,4-dimethoxychalcone and 2-hydroxy-4,4,-dimethoxychalcone also significantly inhibited the intracellular survival of L. donovani parasites with EC50 values between 0.39 and 0.41,µg/mL. When tested against murine bone marrow-derived macrophages as a mammalian host cell control, all compounds with antileishmanial activities also proved to be cytotoxic to varying extents (EC50 0.19,2.06,µg/mL). Correlations between molecular structures and antileishmanial activity are discussed in detail. Specific compounds are illustrated with emphasis on their mode of action and potential for the development of selective antiprotozoal agents. Copyright ­© 2001 John Wiley & Sons, Ltd. [source]