There is a great need to be careful about the use and over
reliance upon docking studies to predict in-vivo effect.
Curcumin is thought to exist only in the enol form when dissolved
Thus only the enol variant should be used for docking.
Many targets were selected for myeloma and curcumin was one of
the many drugs selected for docking study. One target being
GADD45B is given as an example in the Myeloma
page although that docking is with the Green Tea phenol EGCG
The docking studies are well and good but the real problem then
arises that if one decides it would be good to get a curcumin
molecule into the bone marrow then how on earth do you do
it. It is a long fraught path from mouth to bone marrow.
Stomach acid and intestine alkalinity along with water are
potential degradation chemicals. Intestinal absorption is a whole
topic and blood transfer complex.
However a starting position for any drug application must be than
the intestinal absortion size must be below 100nm and blood
transport via albumin must be single molecules in solution.
This gives curcumin an immediate problem because the blood levels
for oral consumption of very high doses as shown below are below
4uM and most of the time around 1uM.
This must be considered in the light of the effective doses as
Curcumin solubility in water is approximately 3mg per
litre. Even with maximum intestinal absorption the 5 litres
of blood we have could only hold 15mg dissolved.
By enclosing single molecules of curcumin ( very hydrophobic) in
molecules such as vinylpyrollidone ( very hydrophillic ) we appear
to be able to deliver amorphous curcumin into solution. My most
rapid and concentrated solutions resulted from ( by mass) 1 part
of curcumin and 7 parts of vinylpyrollidone.
For further details search and refer to "Comparative study of curcumin and curcumin formulated in a solid dispersion - Evaluation of their antigenotoxic effects"
Here we are talking about major changes to the delivery of
curcumin. I refer you to Brad Culkin's site.
I find the technique unexplainable , unlikely and of profound
effect. The site may be a little out-of-date in the detail
but the basics seem to provide for a concentrated and protected
delivery of curcumin to the blood.
The above methods are to arrive at curcumin solution in water (or
blood). If this is not thought neccessary then clearly choosing a
solvent which dissolves the molecule is easier. DMSO is