Abstract
Two labdane type diterpenes, labd-13(E)-ene,-8α,15-diol (1) and labd-13(E)-ene,-8α,15-yl acetate (2) were isolated from the hexane extract of Cistus creticus subsp. eriocephalus (Viv.) Greuter & Burdet leaves, while (+)-19-acetoxy-cis-clerodan-3-en-15-oic acid (3) was isolated from the hexane extract of Cistus monspeliensis L. leaves. The compounds were examined for their in vitro cytostatic and cytotoxic activity against nine human leukemic cell lines, three of which exhibited a multidrug resistant phenotype. They were also evaluated for their anti-inflammatory activity in vivo on the back of hairless mice. The cytostatic and cytotoxic activity of the tested diterpenes followed the order 1>2>3. Topical application of the diterpenes on barrier disrupted skin did not seem to have a significant contribution to the repair rate of the skin barrier.
Abbreviations
GI50:growth inhibition 50
LC50:lethal concentration 50
MED:minimum erythymal dose
MDR:multidrug resistant
MTT:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide
PBS:phosphate buffered saline
RI:retention indices
Rt:retention time
TEWL:transepidermal water loss
TGI:total growth inhibition
Key words
Cistus creticus subsp. eriocephalus, Cistus monspeliensis Cistaceae, labdane diterpenes, clerodane diterpenes, cytostatic/cytotoxic effect, anti-inflammatory activity
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Ass. Prof. Dr. Costas Demetzos
School of Pharmacy
Department of Pharmacognosy
Panepistimiopolis Zografou 15771
Athens
Greece
eMail: demetzos@galenos.pharm.uoa.gr
Fax: +30-1-7274596 and +3022182210
