2007
DOI: 10.1128/aac.00998-06
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Flavonoid Dimers as Bivalent Modulators for Pentamidine and Sodium StiboglucanateResistance in Leishmania

Abstract: Drug resistance by overexpression of ATP-binding cassette (ABC) transporters is an impediment in the treatment of leishmaniasis. Flavonoids are known to reverse multidrug resistance (MDR) in Leishmania and mammalian cancers by inhibiting ABC transporters. Here, we found that synthetic flavonoid dimers with three (compound 9c) or four (compound 9d) ethylene glycol units exhibited a significantly higher reversing activity than other shorter or longer ethylene glycol-ligated dimers, with ϳ3-fold sensitization of … Show more

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Cited by 47 publications
(47 citation statements)
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“…Recent studies have shown that larger flavonoid compounds that contain multiple chemical moieties, for example, dimers of single flavonoid structures or biflavonoids, show enhanced biological activities compared to their monomeric flavonoid counterparts (Zhang et al 2004;Wong et al 2007;Dhawan et al 2002). For example, the flavonoid taiwaniaflavone (Fig.…”
Section: Beneficial Roles Of Naturally Occurring Polyphenolic Compounmentioning
confidence: 99%
“…Recent studies have shown that larger flavonoid compounds that contain multiple chemical moieties, for example, dimers of single flavonoid structures or biflavonoids, show enhanced biological activities compared to their monomeric flavonoid counterparts (Zhang et al 2004;Wong et al 2007;Dhawan et al 2002). For example, the flavonoid taiwaniaflavone (Fig.…”
Section: Beneficial Roles Of Naturally Occurring Polyphenolic Compounmentioning
confidence: 99%
“…have been reported, and some of these compounds showed high efficacy in killing amastigotes and promastigotes of various Leishmania spp. both in vivo and in vitro (103)(104)(105)(106)(107).…”
Section: Treatment: Chemotherapymentioning
confidence: 99%
“…The untreated control group received 0.9% NaCl (n ϭ 5 mice). A total of eight injections, on days 16,20,24,28,32,36,40, and 44, were given. The experiment was completed on day 48.…”
Section: Chemicalsmentioning
confidence: 99%
“…Antipromastigote activity was determined according to procedures described previously (16), with the CellTiter 96 AQueous assay (Promega) employing a tetrazolium compound. Promastigotes were seeded into 96-well flat-bottomed microtiter plates at 1 ϫ 10 5 cells per well, in a final volume of 100 l medium, and were incubated with a series of concentrations of synthetic flavonoid dimers or known antileishmanial agents.…”
Section: Chemicalsmentioning
confidence: 99%
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