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Planta Med 2001; 67(7): 614-618
DOI: 10.1055/s-2001-17362
Original Paper
Pharmacology...
© Georg Thieme Verlag Stuttgart · New York

Cytotoxic and Anti-Inflammatory Activity of Labdane and cis-Clerodane Type Diterpenes

Costas Demetzos1*, Kostas Dimas2 , Sophia Hatziantoniou3 , Thalia Anastasaki1 , Dimitra Angelopoulou1
  • 1 School of Pharmacy, Department of Pharmacognosy, University of Athens, Athens, Greece
  • 2 International Institute of Anticancer Research, Attiki, Greece
  • 3 Department of Pharmaceutical Technology University of Athens, Athens, Greece
Further Information

Publication History

September 22, 2000

January 6, 2001

Publication Date:
24 September 2001 (online)

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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

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