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Celebrating 100 Years of Health Sciences
Innovation
Traditional garlic extracts have yielded low amounts
of ajoene as part of a mixture of products. Professors
Roger Hunter and Iqbal Parker and Dr Catherine
Kaschula have developed the first synthetic route
to ajoene analogues, which has been patented by
UCT. The researchers identified the ajoene anti-
cancer “pharmacophore” (the group of atoms in the
molecule of a drug that are actually responsible for
the drug’s action) to be the disulfide, with the vinyl
and sulfoxide groups further enhancing activity. This
facilitates the design and synthesis of more-potent
ajoenes than the natural product. These are currently
undergoing pre-clinical evaluation.
Recently, a fluorescent-tagged ajoene has for the
first time enabled the UCT researchers to track
ajoene’s activity within the cancer cell, as shown in
the photomircographs. It is now thought that ajoene
interferes with protein-folding in the cancer cell,
which induces programmed cell death (apoptosis).
This novel anti-cancer mechanism can be used in
a multi-pronged approach with current anti-cancer
therapeutics to kill cancer cells.
Developing the Potential of Garlic to Fight Cancer
Garlic
(Allium sativum)
has been used in folk medicine for centuries both as a food flavour-enhancer and for its beneficial
health effects. Although the pungent garlic taste is not universally loved, the beneficial medicinal properties are widely
known to fight infections, heart disease and cancer. These medicinal properties are attributed to the organosulfur
compounds found in crushed cloves, of which the compound
E/Z
-ajoene is one of the major constituents (“ajo” comes
from the Spanish for “garlic”).
Fluorescent images of MDA-MB-231 breast cancer
cells treated with a blue fluorescing-ajoene. Breast
cancer cells (B) were stained with a dye which
causes the endoplasmic reticulum (ER) of the cell
to fluoresce red (A) and then treated with the blue-
fluorescing ajoene (C). An overlay of both red and
blue fluorescent signals shows a “pink” signal (D)
indicative of the fluorescing ajoene localising to
the ER (red + blue = pink).
A
B
D
C