Abstract：
:Parasitic diseases continue to be a major worldwide health problem, and there is an urgent need for development of therapeutic drugs. This paper describes synthesis of dehydrodiferulic acid dilactone 1 and dehydrodisinapic acid dilactone 2 furofuran lignans by oxidative coupling of ferulic and sinapic acids, respectively. Their schistosomicidal, trypanocidal, and leishmanicidal activities were evaluated in vitro against Schistosoma mansoni adult worms, trypomastigote and amastigotes forms of Trypanosoma cruzi, and promastigote forms of Leishmania amazonensis. Compound 1 did not display significant schistosomicidal activity, but it presented potent trypanocidal activity, since it induced death of trypomastigotes and amastigotes with IC50/24h of 9.3μM and 7.3μM, respectively. Compound 2 had slight trypanocidal and schistosomicidal activities. None of the compounds were active against L. amazonensis. These results demonstrated that furofuran lignans are potentially useful for anti-parasitic drugs development and should be further investigated.
journal_name
Phytochemistryjournal_title
Phytochemistryauthors
Pereira AC,Esperandim VR,Ferreira da Silva D,Magalhães LG,Lima TC,Nanayakkara DN,Cunha WR,Bastos JK,Andrade e Silva MLdoi
10.1016/j.phytochem.2014.08.010subject
Has Abstractpub_date
2014-11-01 00:00:00pages
119-25eissn
0031-9422issn
1873-3700pii
S0031-9422(14)00325-2journal_volume
107pub_type
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