Τίτλος:
Antileishmanial activity of natural diterpenes from Cistus sp. and semisynthetic derivatives thereof
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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. © 2006 Pharmaceutical Society of Japan.
Συγγραφείς:
Fokialakis, N.
Kalpoutzakis, E.
Tekwani, B.L.
Skaltsounis, A.L.
Duke, S.O.
Περιοδικό:
Biological and Pharmaceutical Bulletin
Λέξεις-κλειδιά:
13 8a hydroxylabd 13 en 15 ol 2 chloroethylcarbamate; 15,18 diacetoxy clerod 3 ene; 18 acetoxy clerod 3 en 15 ol; amphotericin B; antileishmanial agent; Cistus creticus extract; cistus monspeliensis extract; clerodane derivative; diterpene; doxorubicin; herbaceous agent; pentamidine; plant extract; triterpene derivative; unclassified drug, animal cell; antimicrobial activity; article; Cistus; Cistus creticus; cistus monspeliensis; controlled study; cytotoxicity test; drug activity; drug isolation; drug potency; drug purification; drug screening; drug synthesis; IC 50; Leishmania donovani; nonhuman, Animals; Antiprotozoal Agents; Cercopithecus aethiops; Cistus; Diterpenes; Leishmania donovani; Molecular Structure; Species Specificity; Vero Cells