Pharm Biol. 2014 Mar;52(3):398-401. doi: 10.3109/13880209.2013.837077. Epub 2013 Oct 23.
Leishmanicidal activity of a daucane sesquiterpene isolated from Eryngium foetidum.
Abstract
CONTEXT:
Eryngium
foetidum L. (Apiaceae) is a traditional herb that has been used for
numerous medicinal applications, including as a treatment for parasitic
infections, especially in the Neotropics from where it originates.
OBJECTIVE:
This
study evaluates the in vitro leishmanicidal and cytotoxicity activities
of isolated compounds based on a bioassay-guided fractionation
approach.
MATERIALS AND METHODS:
Defatted
aerial parts of E. foetidum were subjected to extraction with methanol
followed by partitioning with n-hexane, ethyl acetate and 50% methanol.
Then, the first two fractions were subsequently fractionated by column
chromatography and HPLC. Compound identity was confirmed by mass
spectrometry and NMR spectroscopy. Leishmania tarentolae (promastigotes)
and L. donovani (amastigotes) were used as testing parasites. L6 rat
myoblasts were used for cytotoxicity. All extracts and fractions were
tested at 20 μg/mL.
RESULTS:
The
initial methanol extract showed 20% growth inhibition of L. tarentolae.
Then, the n-hexane and ethyl acetate fractions were also active showing
approximately 40% growth inhibition. From these two fractions, the
following compounds were isolated: lasidiol p-methoxybenzoate (1), a
daucane sesquiterpene; and
4-hydroxy-1,1,5-trimethyl-2-formyl-cyclohexadien-(2,5)-[α-acetoxymethyl-cis-crotonate]
(2), a terpene aldehyde ester derivative. Compound 1 inhibited the
growth of both L. tarentolae and L. donovani with IC₅₀ values of 14.33
and 7.84 μM, respectively; and showed no cytotoxicity (IC₅₀ > 50 μM).
Compound 2 was inactive in the L. tarentolae assay (IC₅₀ > 50 μM).
DISCUSSION AND CONCLUSION:
This
study presented the bioassay-guided fractionation with the
leishmanicidal and cytotoxicity activities of two compounds isolated for
the first time from an Eryngium species.
