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@ARTICLE{Daaboul:128678,
author = {H. E. Daaboul and C. F. Daher and R. I. Taleb and J. Boulos
and K. Bodman-Smith and P. Boukamp$^*$ and W. N. Shebaby and
C. Dagher and M. El-Sibai and M. A. Mroueh},
title = {β-2-himachalen-6-ol protects against skin cancer
development in vitro and in vivo.},
journal = {Journal of pharmacy and pharmacology},
volume = {69},
number = {11},
issn = {0022-3573},
address = {Wallingford, Oxon},
publisher = {Pharmaceutical Press64910},
reportid = {DKFZ-2017-04693},
pages = {1552 - 1564},
year = {2017},
abstract = {Previous studies in our laboratory showed that Daucus
carota oil extract (DCOE) possesses remarkable in-vitro
anticancer activity and antitumour promoting effect against
DMBA/TPA skin carcinogenesis in mice. Chemical analysis of
DCOE led to the isolation of the β-2-himachalen-6-ol (HC),
major sesquiterpene with a potent anticancer activity
against various colon, breast, brain and skin cancer cells.
This study investigated the anticancer activity of HC
against invasive epidermal squamous cell carcinoma cells and
evaluated its effect in a DMBA/TPA skin carcinogenesis
Balb/c murine model.HaCaT-ras II-4 epidermal squamous cells
were treated with HC (1, 5, 10, 25 and 50 μg/ml), and cell
viability was evaluated with WST 1 assay kit. Cell cycle
analysis was carried out by flow cytometry, and
pro/anti-apoptotic proteins were measured using Western
blot. The effect of topical and intraperitoneal (IP)
treatment with HC in mice was assessed using the
DMBA/TPA skin carcinogenesis model. Cisplatin (2.5 mg/kg;
IP) was used as a positive control. Papilloma incidence,
yield and volume were monitored, and isolated papillomas
were assessed for their pro/anti-apoptotic proteins and
morphology.β-2-himachalen-6-ol showed a dose-dependent
decrease in cell survival with an IC50 and IC90 of 8 and
30 μg/ml, respectively. Flow cytometry analysis revealed
that treatment with 10 μg/ml HC significantly increased
the number of cells undergoing late apoptosis $(28\%),$
while 25 μg/ml caused a larger cell shift towards late
apoptosis $(46.6\%)$ and necrosis $(39\%).$ A significant
decrease in protein levels of p53 and Bcl-2 and a
significant increase in p21 and Bax were observed. Also,
there was a significant decrease in p-Erk and p-Akt protein
levels. The treatment of mice (IP and topical) with HC
caused a significant decrease in papilloma yield, incidence
and volume. Similar effects were observed with cisplatin
treatment, but HC-treated groups exhibited twofold to
threefold increase in survival rates. Similar patterns in
the pro- and anti-apoptotic proteins were observed in mice
treated with HC, except for a significant increase in p53
protein.In conclusion, HC treatment induced cell cycle
arrest (low dose) and promoted apoptosis partly via
inhibition of the MAPK/ERK and PI3K/AKT pathways with no
significant toxicity to laboratory mice.},
cin = {A110},
ddc = {610},
cid = {I:(DE-He78)A110-20160331},
pnm = {311 - Signalling pathways, cell and tumor biology
(POF3-311)},
pid = {G:(DE-HGF)POF3-311},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:28872682},
doi = {10.1111/jphp.12796},
url = {https://inrepo02.dkfz.de/record/128678},
}