title: Antileishmanial activity of natural diterpenes from Cistus sp. and semisynthetic derivatives thereof.
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 microg/ml, 3.4 microg/ml and 3.5 microg/ml, respectively.
authors.affiliation: Natural Products Utilization Research Unit, USDA/ARS, University of Mississippi, USA.
authors.forename: Nikolas
authors.initials: N
authors.lastname: Fokialakis
authors.forename: Eleftherios
authors.initials: E
authors.lastname: Kalpoutzakis
authors.forename: Babu Lal
authors.initials: BL
authors.lastname: Tekwani
authors.forename: Alexios Leandros
authors.initials: AL
authors.lastname: Skaltsounis
authors.forename: Stephen Oscar
authors.initials: SO
authors.lastname: Duke
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D029758:Cistus / Q000737:chemistry*; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D015394:Molecular Structure; D013045:Species Specificity; D014709:Vero Cells
chemical_list: D000981:Antiprotozoal Agents; D004224:Diterpenes