Antileishmanial Activity of Natural Diterpenes from Cistus sp. and Semisynthetic Derivatives Thereof

Nikolas Fokialakis; Eleftherios Kalpoutzakis; Babu Lal Tekwani; Alexios Leandros Skaltsounis; Stephen Oscar Duke

doi:10.1248/bpb.29.1775

Notes

Antileishmanial Activity of Natural Diterpenes from Cistus sp. and Semisynthetic Derivatives Thereof

Nikolas Fokialakis, Eleftherios Kalpoutzakis, Babu Lal Tekwani, Alexios Leandros Skaltsounis, Stephen Oscar Duke

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Keywords: Cistus sp., Leishmania donovani, cis-clerodane, labdane, manoyl oxide, diterpene, antileishmanial activity

JOURNAL FREE ACCESS

2006 Volume 29 Issue 8 Pages 1775-1778

DOI https://doi.org/10.1248/bpb.29.1775

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Abstract

Eleven cis-clerodane diterpenes, seven labdane type diterpenes and one triterpene isolated from Cistus monspeliensis and the resin “Ladano” of Cistus creticus subsp. creticus were evaluated against Leishmania donovani promastigotes, the causative agent for visceral leishmaniasis. In addition, eleven semisynthetic manoyl oxide, seventeen labdane type derivatives and a triterpene were also evaluated for their antileishmanial activity. 18-Acetoxy-cis-clerod-3-en-15-ol, 15,18-diacetoxy-cis-clerod-3-ene and 13-(E)-8a-hydroxylabd-13-en-15-ol 2-chloroethylcarbamate exhibited the most potent and selective leishmanicidal activity with IC₅₀ values of 3.3 μg/ml, 3.4 μg/ml and 3.5 μg/ml, respectively.

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