Antileishmanial activity of natural diterpenes from Cistus sp. and semisynthetic derivatives thereof.
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.
Fokialakis
Nikolas
N
Natural Products Utilization Research Unit, USDA/ARS, University of Mississippi, USA.
Kalpoutzakis
Eleftherios
E
Tekwani
Babu Lal
BL
Skaltsounis
Alexios Leandros
AL
Duke
Stephen Oscar
SO
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
D000981:Antiprotozoal Agents; D004224:Diterpenes