Abstract：
:Crude CH2Cl2 extract from leaves of Piper laevicarpu (Piperaceae) displayed antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi (Y strain) and antimicrobial potential against Cryptococcus gattii (strain-type WM 178). Bioactivity-guided fractionation of crude extract afforded one new natural bioactive lactam derivative, named laevicarpin. The structure of isolated compound, which displayed a very rare ring system, was elucidated based on NMR, IR and MS spectral analysis. Using MTT assay, the trypomastigotes of T. cruzi demonstrated susceptibility to laevicarpin displaying IC50 value of 14.7μg/mL (49.6μM), about 10-fold more potent than the standard drug benznidazole. The mammalian cytotoxicity of laevicarpin was verified against murine fibroblasts (NCTC cells) and demonstrated a CC50 value of 100.3μg/mL (337.7μM-SI=7). When tested against Cryptococcus gattii, laevicarpin showed an IC50 value of 2.3μg/mL (7.9μM) and a MIC value of 7.4μg/mL (25μM). Based in the obtained results, laevicarpin could be used as a scaffold for future drug design studies against the Chagas disease and anti-cryptococosis agents.
journal_name
Fitoterapiajournal_title
Fitoterapiaauthors
da Silva A Maciel D,Freitas VP,Conserva GA,Alexandre TR,Purisco SU,Tempone AG,Melhem MS,Kato MJ,Guimarães EF,Lago JHdoi
10.1016/j.fitote.2016.04.005subject
Has Abstractpub_date
2016-06-01 00:00:00pages
24-8eissn
0367-326Xissn
1873-6971pii
S0367-326X(16)30077-6journal_volume
111pub_type
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