In vitro anti-proliferation/cytotoxic activity of cantharidin (Spanish Fly) and related derivatives
West Indian med. j
;
52(1): 10-13, Mar. 2003.
Article
in English
| LILACS
| ID: lil-410842
ABSTRACT
The anti-cancer therapeutic promise of cantharidin is limited because of its high mammalian toxicity. In order to find new anti-cancer lead compounds with reduced toxicity of the cantharidin prototype, the following seven derivatives were screened against the human SH-SY5Y neuroblastoma and MCF-7 breast cancer cells in vitro 2,3-dimethyl-7-oxabicylo-[2.2.1]heptane-2,3-dicarboxylic anhydride (cantharidin) [1], 1-cyclohexen-1,2-dicarboxylic anhydride [2], cis-4-cyclohexen-1,2-dicarboxylic anhydride [3], cis-1, 2-cyclohexanedicarboxylic anhydride [4], exo-7-oxabicyclo[2.2.1]hept-5-ene-2-3 dicarboxylic anhydride [5], exo-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic anhydride (norcantharidin) [6], and (S)-(-)-O-acetylmalic anhydride [7]. Cantharidin, was found to be the most effective anti-proliferative compound on both cell lines. However, on the human neuroblastoma cells cantharidin was of equal toxicity to compound [6]. Mode of action studies revealed that cantharidin inhibited growth factor-mediated activation of mitogen activated protein kinase (MAPkinase) and attenuated the de-phosphorylation of the extracellular regulated kinases 1 and 2 (erk1 and erk2)
Search on Google
Index:
LILACS (Americas)
Main subject:
Cantharidin
/
Enzyme Inhibitors
/
Anhydrides
Limits:
Humans
Language:
English
Journal:
West Indian med. j
Journal subject:
Medicine
Year:
2003
Type:
Article
Affiliation country:
Germany
Institution/Affiliation country:
University of Hohenheim/DE
Similar
MEDLINE
...
LILACS
LIS