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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2006-5-25
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pubmed:abstractText |
Mycobacterium tuberculosis is an intracellular pathogen that persists within macrophages of the human host. One approach to improving the treatment of tuberculosis (TB) is the targeted delivery of antibiotics to macrophages using ligands to macrophage receptors. The moxifloxacin-conjugated dansylated carboxymethylglucan (M-DCMG) conjugate was prepared by chemically linking dansylcadaverine (D) and moxifloxacin (M) to carboxymethylglucan (CMG), a known ligand of macrophage scavenger receptors. The targeted delivery to macrophages and the antituberculosis activity of the conjugate M-DCMG were studied in vitro and in vivo. Using fluorescence microscopy, fluorimetry, and the J774 macrophage cell line, M-DCMG was shown to accumulate in macrophages through scavenger receptors in a dose-dependent (1 to 50 microg/ml) manner. After intravenous administration of M-DCMG into C57BL/6 mice, the fluorescent conjugate was concentrated in the macrophages of the lungs and spleen. Analyses of the pharmacokinetics of the conjugate demonstrated that M-DCMG was more rapidly accumulated and more persistent in tissues than free moxifloxacin. Importantly, therapeutic studies of mycobacterial growth in C57BL/6 mice showed that the M-DCMG conjugate was significantly more potent than free moxifloxacin.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-10085050,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-10321065,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-12019103,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-12101273,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-12499213,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-14576099,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-14578218,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-14907713,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-15507314,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-15710347,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-2251254,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-2300204,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-2405761,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-731417,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-7979249,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-8018106,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-8888575,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-9069289,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-9525326,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16723555-9869570
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0066-4804
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pubmed:author |
pubmed-author:AgafonovA PAP,
pubmed-author:AlekseevA YAY,
pubmed-author:AzaevM SMS,
pubmed-author:BlinovV MVM,
pubmed-author:DerrickS CSC,
pubmed-author:DushkinM IMI,
pubmed-author:FilimonovP NPN,
pubmed-author:KhoschenkoO MOM,
pubmed-author:KozlovV AVA,
pubmed-author:KrasnovV AVA,
pubmed-author:KurunovYY,
pubmed-author:MelnikovaE VEV,
pubmed-author:MorrisSS,
pubmed-author:PathakAA,
pubmed-author:RassadkinYY,
pubmed-author:ReynoldsR CRC,
pubmed-author:SaraevD VDV,
pubmed-author:SchwartzY SYS,
pubmed-author:ShestapalovA MAM,
pubmed-author:SvistelnikA VAV,
pubmed-author:VavilinV AVA
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pubmed:issnType |
Print
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1982-8
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:16723555-Animals,
pubmed-meshheading:16723555-Antitubercular Agents,
pubmed-meshheading:16723555-Area Under Curve,
pubmed-meshheading:16723555-Aza Compounds,
pubmed-meshheading:16723555-Bronchoalveolar Lavage Fluid,
pubmed-meshheading:16723555-Colony Count, Microbial,
pubmed-meshheading:16723555-Dansyl Compounds,
pubmed-meshheading:16723555-Dose-Response Relationship, Drug,
pubmed-meshheading:16723555-Glucans,
pubmed-meshheading:16723555-Half-Life,
pubmed-meshheading:16723555-Macrophages, Alveolar,
pubmed-meshheading:16723555-Male,
pubmed-meshheading:16723555-Mice,
pubmed-meshheading:16723555-Mice, Inbred C57BL,
pubmed-meshheading:16723555-Mycobacterium tuberculosis,
pubmed-meshheading:16723555-Quinolines
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pubmed:year |
2006
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pubmed:articleTitle |
Novel conjugate of moxifloxacin and carboxymethylated glucan with enhanced activity against Mycobacterium tuberculosis.
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pubmed:affiliation |
Institute of Clinical Immunology SD RAMS, Novosibirsk, Russia.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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