Lead compound, Cancer, Gynaecological disorders
Licensing
Ovarian cancer is the fifth
leading cause of death in women with cancer. In
spite of chemotherapy by platinum derivates
and/or taxol after surgery it remains the
leading cause of death from gynaecological
malignancy in many countries.
A novel compound against
ovarian and other cancers has been isolated from
the leaves of an Australian native plant
belonging to the family of Compositae. This
family is known for its natural products,
including sesquiterpene lactones (SLs). To date
great interest is shown for the potential of SLs
as anti‐cancer
agent. Different fractions of the crude plant
extract were tested in vitro against ovarian
cancer cell lines and other cancer cell lines.
Fractions with clear cytotoxic effects were
selected and further analysed. A compound could
be isolated by 1H‐NMR,
13C‐NMR
and ESI mass spectrometry.
This
compound has been further tested against a
variety of ovarian cancer cell lines, other
cancer cell lines and normal cells such as
normal ovarian cells, fibroblasts and
lymphocytes. Apoptosis could be measured after
different concentrations of drug treatment. At 5μg/mL
drug treatment all cancer cells were killed
while normal cells were not affected. A
comparison between this compound with cisplatin
and docetaxol showed that the compound killed
the ovarian cancer cells as did cisplatin.
Furthermore normal cells were killed by both
cisplatin and taxol but not by the compound.
The
structure of the compound is synthesizable,
although all experiments were performed with
purified "natural" compound. In the first pilot
experiment mice were injected with ovarian
cancer cells subcutaneously and the compound was
administered intra peritoneal in different doses
after the ovarian tumours had reached an average
size of 5 mm2. This experiment showed no
regression of tumour although further growth was
inhibited. It was hypothesized that this was
caused by the liphophilic nature of the
compound, so now new invivo studies will be
performed in which nude mice will be injected
with liposome‐encapsulated
compound to improve the activity of the
compound. After this experiment the researchers
would like to collaborate with a commercial
partner to further develop this anti‐cancer
candidate.
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