PL EN


Preferencje help
Widoczny [Schowaj] Abstrakt
Liczba wyników
Czasopismo
1999 | 44 | 3 |
Tytuł artykułu

Activity of N-lutidinylarylcarboxamides against Leishmania donovani and L.braziliensis

Warianty tytułu
Języki publikacji
EN
Abstrakty
EN
Three arylcarboxamides issued from 2-amino- 4,6-dimethylpyridine, benzamide 1, furan-2-carboxamide 2 and 5-bromofuran-2-carboxamide 3 were evaluated against Leishmania promastigotes, at three doses, 0.5, 5, and 50 µM. Although benzamide 1 exerted but a moderate inhibition against cultured extracellular promastigotes at a concentration of 50 µM, furan-2-carboxamides 2 and 3 had potent activity at the same concentration. The IC₅₀ of 2 against L. donovani and L. braziliensis were 29.9 and 28.3 µM and those of 3 were 25.9 and 36.6 µM, respectively. In a BALB/c mice model of visceral leishmaniosis, an intraperitoneal administration of 10 mg/kg of 2, for 5 days, led to a consistent parasite burden reduction in the spleen smears (75.8 ± 5.7%) and in the microdilution spleen cultures (72.1 ± 0.6%). A very significant correlation (r = 0.96) was found between the two methods of spleen parasite burden quantification. These amides also exhibit potent antiinflammatory activity and it was previously stated that they inhibit arachidonic acid production by interfering in the PLA₂ activation. This suggests fact that they could disrupt Leishmania membrane lipid integrity by protein kinase C inhibition.
Wydawca
-
Czasopismo
Rocznik
Tom
44
Numer
3
Opis fizyczny
p.156-159,fig.
Twórcy
autor
  • Universite de Nantes, 1 rue Gaston Veil, 44035 Nantes, France
autor
autor
autor
autor
Bibliografia
  • Achterberg V., Gercken G. 1987. Cytotoxicity of ester and ether lysophospholipids on Leishmania donovani promastigotes. Molecular and Biochemical Parasitology, 23, 117-122.
  • Aderem A. A., Scott W. A., Cohn Z. A. 1986. Evidence for sequential signals in the induction of arachidonic acid cascade in macrophages. Journal of Experimental Medicine, 163, 139-154.
  • Andrew J. N., King A. N., Sani Ibrahim A., Ukoha I., Ikediobi C. O. 1993. Phospholipase A₂ from Trypanosoma congolense: Characterization and hematological properties. Cellular Biochemistry and Function, 11, 125-130.
  • Berman J. D. 1997. Human leishmaniasis: clinical, diagnostic, and chemotherapeutic developments in the last 10 years. Clinical and Infectious Diseases, 24, 684-703.
  • Buffet P., Sulahian A. A., Garin J. F., Nassar N., Derouin F. 1995. Culture microtitration: a sensitive method for quantifying Leishmania infantum in tissues of infected mice. Antimicrobial Agents and Chemotherapy, 39, 2167-2168.
  • Connelly M. C., Kierszenbaum F. 1984. Modulation of macrophage interaction with Trypanosoma cruzi by phospholipase A₂ - sensitive components of the parasite membrane. Biochemical and Biophysical Research Community, 121, 931-939.
  • Croft S. L. 1988. Recent development in the chemotherapy of leishmaniasis. Trends in Pharmacology Science, 9, 376-381.
  • Croft S. L., Neal R. A., Herrmann D. B. J. 1993. Antileishmania activity of the ether phospholipid ilmofosine. Transactions of the Royal Society of Tropical Medicine and Hygiene, 87, 217-219.
  • Croft S. L., Neal R. A., Pendergast W., Chan H. 1987. The activity of alkyl phosphorylcholines and related derivates against Leishmania donovani. Biochemical Pharmacology, 36, 2633-2636.
  • Davidson R. N., Croft S. L. 1993. Recent advances in the treatment of visceral leishmaniasis. Transactions of the Royal Society of Tropical Medicine and Hygiene, 87, 130-131.
  • Dennis E. A. 1994. Diversity of group types, regulation, and function of phospholipase A₂. Journal of Biological Chemistry, 269, 13057-13060.
  • Hill J. O., North R. J., Collins F. M. 1983. Advantages of measuring changes in the number of viable parasites in murine models of experimental cutaneous leishmaniasis. Infection and Immunity, 39, 1087-1094.
  • Hua Qiu Z., Calvarlho M. S., Leslie C. C. 1993. Regulation of phospholipase A₂ activation by phosphorylation in mouse peritoneal macrophages. Journal of Biological Chemistry, 268, 24506-24513.
  • Lujan H. D., Bronia D. H. 1994. Intermembrane lipid transfer during Trypanosoma cruzi-induced erythrocyte membrane destabilization. Parasitology, 108, 323-334.
  • Mosmann T. 1983. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assay. Journal of Immunological Methods, 65, 55-63.
  • Peter W. 1988. Morphology. In: Parasitology in focus. Facts and trends (Ed. H. Mehlhorn). Springer-Verlag, Berlin, Heidelberg, 161-221.
  • Raffi F., Merrien D., Le Pape P.. Reliquet V. 1995. Use of an itraconazole/allopurinol combination for the treatment of visceral leishmaniasis in a patient with AIDS. Clinical and Infectious Diseases, 21, 1338-1339.
  • Robert-Piessard S., Le Baut G., Courant J., Brion J. D., Sparfel L., Bouhayat S., Petit J. Y., Sanchez R. Y., Juge M., Grimaud N., Welin L. 1990. Non-acidic anti-inflammatory compounds: Activity of N-(4,6-dimethyl-2-pyridinyl) benzamides and derivates. European Journal of Medical Chemistry, 25, 9-19.
  • Van Den Bossche H. 1980. Intracellular phospholipase A. Biochimica et Biophysica Acta, 604, 191-246.
  • Zidovetzki R., Sherman I. W., O'Brien L. 1993. Inhibition of Plasmodium falciparum phospholipase A₂ by chloroquine, quinine, and arteether. Journal of Parasitology, 79, 565-570.
  • Zidane M., Moré M. T., Marjolet M., Le Pape P. 1995. In vitro activity of a glycoprotein of the sponge Pachymastisma johnstonni against Leishmania donovani promastigotes. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy. ICAAC, San Francisco.
Typ dokumentu
Bibliografia
Identyfikatory
Identyfikator YADDA
bwmeta1.element.agro-article-904cdeeb-857e-4495-b86a-278d5d56cf4a
JavaScript jest wyłączony w Twojej przeglądarce internetowej. Włącz go, a następnie odśwież stronę, aby móc w pełni z niej korzystać.