Document Detail


Defibrotide interferes with several steps of the coagulation-inflammation cycle and exhibits therapeutic potential to treat severe malaria.
MedLine Citation:
PMID:  22116094     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
OBJECTIVE: The coagulation-inflammation cycle has been implicated as a critical component in malaria pathogenesis. Defibrotide (DF), a mixture of DNA aptamers, displays anticoagulant, anti-inflammatory, and endothelial cell (EC)-protective activities and has been successfully used to treat comatose children with veno-occlusive disease. DF was investigated here as a drug to treat cerebral malaria.
METHODS AND RESULTS: DF blocks tissue factor expression by ECs incubated with parasitized red blood cells and attenuates prothrombinase activity, platelet aggregation, and complement activation. In contrast, it does not affect nitric oxide bioavailability. We also demonstrated that Plasmodium falciparum glycosylphosphatidylinositol (Pf-GPI) induces tissue factor expression in ECs and cytokine production by dendritic cells. Notably, dendritic cells, known to modulate coagulation and inflammation systemically, were identified as a novel target for DF. Accordingly, DF inhibits Toll-like receptor ligand-dependent dendritic cells activation by a mechanism that is blocked by adenosine receptor antagonist (8-p-sulfophenyltheophylline) but not reproduced by synthetic poly-A, -C, -T, and -G. These results imply that aptameric sequences and adenosine receptor mediate dendritic cells responses to the drug. DF also prevents rosetting formation, red blood cells invasion by P. falciparum and abolishes oocysts development in Anopheles gambiae. In a murine model of cerebral malaria, DF affected parasitemia, decreased IFN-γ levels, and ameliorated clinical score (day 5) with a trend for increased survival.
CONCLUSION: Therapeutic use of DF in malaria is proposed.
Authors:
Ivo M B Francischetti; Carlo J Oliveira; Graciela R Ostera; Stephanie B Yager; Françoise Debierre-Grockiego; Vanessa Carregaro; Giovanna Jaramillo-Gutierrez; Jen C C Hume; Lubin Jiang; Samuel E Moretz; Christina K Lin; José M C Ribeiro; Carole A Long; Brandi K Vickers; Ralph T Schwarz; Karl B Seydel; Massimo Iacobelli; Hans C Ackerman; Prakash Srinivasan; Regis B Gomes; Xunde Wang; Robson Q Monteiro; Michail Kotsyfakis; Anderson Sá-Nunes; Michael Waisberg
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Intramural; Research Support, Non-U.S. Gov't     Date:  2011-11-23
Journal Detail:
Title:  Arteriosclerosis, thrombosis, and vascular biology     Volume:  32     ISSN:  1524-4636     ISO Abbreviation:  Arterioscler. Thromb. Vasc. Biol.     Publication Date:  2012 Mar 
Date Detail:
Created Date:  2012-02-20     Completed Date:  2012-04-13     Revised Date:  2013-04-15    
Medline Journal Info:
Nlm Unique ID:  9505803     Medline TA:  Arterioscler Thromb Vasc Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  786-98     Citation Subset:  IM    
Affiliation:
Section of Vector Biology, Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD 20892, USA. ifrancischetti@niaid.nih.gov
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Inflammatory Agents / pharmacology*
Anticoagulants / pharmacology*
Antimalarials / pharmacology*
Blood Coagulation / drug effects*
Cells, Cultured
Complement Activation / drug effects
Cytokines / blood
Dendritic Cells / drug effects,  immunology,  parasitology
Disease Models, Animal
Dose-Response Relationship, Drug
Endothelial Cells / drug effects*,  immunology,  metabolism,  parasitology
Female
Glycosylphosphatidylinositols / metabolism
Hemoglobins / metabolism
Humans
Inflammation Mediators / blood
Malaria, Cerebral / blood,  drug therapy*,  immunology,  parasitology
Mice
Mice, Inbred BALB C
Mice, Inbred C57BL
Nitric Oxide / metabolism
Plasmodium berghei / drug effects*,  pathogenicity
Plasmodium falciparum / drug effects*,  growth & development,  metabolism,  pathogenicity
Platelet Aggregation / drug effects
Polydeoxyribonucleotides / pharmacology*
Receptors, Purinergic P1 / drug effects,  metabolism
Severity of Illness Index
Thromboplastin / metabolism
Time Factors
Grant Support
ID/Acronym/Agency:
Z01 AI000810-11/AI/NIAID NIH HHS
Chemical
Reg. No./Substance:
0/Anti-Inflammatory Agents; 0/Anticoagulants; 0/Antimalarials; 0/Cytokines; 0/Glycosylphosphatidylinositols; 0/Hemoglobins; 0/Inflammation Mediators; 0/Polydeoxyribonucleotides; 0/Receptors, Purinergic P1; 10102-43-9/Nitric Oxide; 83712-60-1/defibrotide; 9035-58-9/Thromboplastin
Comments/Corrections
Comment In:
Arterioscler Thromb Vasc Biol. 2012 Mar;32(3):541-4   [PMID:  22345588 ]

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