Abstract：
:Sapphyrins and a series of related porphyrinoid macrocycles have been investigated as potential agents for the treatment of leishmaniasis. The effectiveness of the compounds was evaluated in vitro upon incubation with Leishmania tarentolae or L. panamensis amastigotes and promastigotes. Their effectiveness was also assessed against intracellular L. panamensis. The cytotoxicity of the compounds was evaluated in vitro using the U937 human promonocyte cell line. Effectiveness and cytotoxicity were assessed in the presence and absence of visible light to assess the photodynamic activity of the compounds. Sapphyrin and two related heterosapphyrins were shown to be particularly effective as inhibitors of Leishmania. A photodynamic effect was observed, which may be attributed to the formation of reactive oxygen species. Yields of singlet oxygen ((1)O(2)) produced were determined in ethanol solutions by direct measurement of (1)O(2) phosphorescence. Confocal microscopy demonstrated that sapphyrin and related macrocycles were taken up by the Leishmania cells and that their presence induces the formation of mitochondrial superoxide. Sapphyrins have been widely investigated as anticancer agents and we here show activity against the Leishmania parasites.
journal_name
Photochem Photobioljournal_title
Photochemistry and photobiologyauthors
Hooker JD,Nguyen VH,Taylor VM,Cedeño DL,Lash TD,Jones MA,Robledo SM,Vélez IDdoi
10.1111/j.1751-1097.2011.01034.xsubject
Has Abstractpub_date
2012-01-01 00:00:00pages
194-200issue
1eissn
0031-8655issn
1751-1097journal_volume
88pub_type
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pub_type： 杂志文章,评审
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