2012
DOI: 10.1016/j.exppara.2012.01.015
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Abstract: Polyamine biosynthesis enzymes are promising drug targets for the treatment of leishmaniasis, Chagas' disease and African sleeping sickness. Arginase, which is a metallohydrolase, is the first enzyme involved in polyamine biosynthesis and converts arginine into ornithine and urea. Ornithine is used in the polyamine pathway that is essential for cell proliferation and ROS detoxification by trypanothione. The flavonols quercetin and quercitrin have been described as antitrypanosomal and antileishmanial compounds… Show more

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Cited by 148 publications
(98 citation statements)
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“…Among the 45 compounds that were potent against LmCK1.2, we identified several inhibitors described to have antileishmanial activity, including known CK1 inhibitors, such as anthraquinone (35)(36)(37), or compounds for which we revealed CK1 as a new target, such as gossypol, purpurogallin, and some flavonoids (38)(39)(40)(41)(42)43). These compounds, identified from several libraries, were found at least twice with similar IC 50 s, indicating that our assay is reproducible (data not shown).…”
Section: Resultsmentioning
confidence: 84%
“…Among the 45 compounds that were potent against LmCK1.2, we identified several inhibitors described to have antileishmanial activity, including known CK1 inhibitors, such as anthraquinone (35)(36)(37), or compounds for which we revealed CK1 as a new target, such as gossypol, purpurogallin, and some flavonoids (38)(39)(40)(41)(42)43). These compounds, identified from several libraries, were found at least twice with similar IC 50 s, indicating that our assay is reproducible (data not shown).…”
Section: Resultsmentioning
confidence: 84%
“…Interestingly, this flavonol has demonstrated inhibitory activity on other enzymes from Leishmania spp., such as arginase (da Silva et al, 2012;de Sousa et al, 2014b), ribonucleotide reductase (Sen et al, 2008) and topoisomerase II (Mittra et al, 2000), suggesting that the leishmanicidal action by quercetin is an outcome of the interference in diverse metabolic pathways. The capacity of quercetin in inhibiting several enzymes from Leishmania spp.…”
Section: Discussionmentioning
confidence: 99%
“…Quercetin has also been reported to have multiple targets, including arginase, which is an important enzyme in the polyamine biosynthesis pathway (23), topoisomerase II in kinetoplasts, which induces DNA cleavage leading to apoptosis (25), and iron metal, which is important for growth and replication of the parasite (26). The mechanisms of action and molecular targets of compound 39 remain to be studied.…”
Section: Discussionmentioning
confidence: 99%
“…Infected macrophages were then treated for 3 days at 37°C with either 0.1% dimethyl sulfoxide (DMSO) orpresent in fruits, vegetables, and tea, can provide a good source of compounds for the design of antileishmanial drugs (11,22). Two important members of the flavonoid family, namely, quercetin and luteolin, have been reported to have marked antileishmanial activity (23)(24)(25)(26). Based on monomeric flavonoids, we previously synthesized a library of flavonoid dimers and demonstrated that they represent a new class of potent safe antileishmanial agents against L. donovani promastigotes and amastigotes (19).…”
Section: Discussionmentioning
confidence: 99%