Abstract：
:Leishmaniasis and Chagas' are parasitic protozoan diseases that affect the poorest population in the world, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, novel, safe and more efficacious drugs are essential. In this work, the CH(2)Cl(2) phase from MeOH extract from the leaves of Baccharis retusa DC. (Asteraceae) was fractioned to afford two flavonoids: naringenin (1) and sakuranetin (2). These compounds were in vitro tested against Leishmania spp. promastigotes and amastigotes and Trypanosoma cruzi trypomastigotes and amastigotes. Compound 2 presented activity against Leishmania (L.) amazonensis, Leishmania (V.) braziliensis, Leishmania (L.) major, and Leishmania (L.) chagasi with IC(50) values in the range between 43 and 52 μg/mL and against T. cruzi trypomastigotes (IC(50)=20.17 μg/mL). Despite of the chemical similarity, compound 1 did not show antiparasitic activity. Additionally, compound 2 was subjected to a methylation procedure to give sakuranetin-4'-methyl ether (3), which resulted in an inactive compound against both Leishmania spp. and T. cruzi. The obtained results indicated that the presence of one hydroxyl group at C-4' associated to one methoxyl group at C-7 is important to the antiparasitic activity. Further drug design studies aiming derivatives could be a promising tool for the development of new therapeutic agents for Leishmaniasis and Chagas' disease.
journal_name
Exp Parasitoljournal_title
Experimental parasitologyauthors
Grecco Sdos S,Reimão JQ,Tempone AG,Sartorelli P,Cunha RL,Romoff P,Ferreira MJ,Fávero OA,Lago JHdoi
10.1016/j.exppara.2011.11.002subject
Has Abstractpub_date
2012-02-01 00:00:00pages
141-5issue
2eissn
0014-4894issn
1090-2449pii
S0014-4894(11)00329-8journal_volume
130pub_type
杂志文章abstract：:Ticks are obligate blood-sucking ectoparasites of a wide range of vertebrates. They can transmit a range of pathogens that cause economic losses to livestock production as well as human disease. In the present study, the complete mitochondrial (mt) genome of Dermacentor silvarum was determined. The mt genome is 14,945...
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journal_title：Experimental parasitology
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journal_title：Experimental parasitology
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journal_title：Experimental parasitology
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journal_title：Experimental parasitology
pub_type： 杂志文章
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