Publication: A Realistic View on -The Essential Medicinal Chemistry of Curcumin-
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Bahadori, FATEMEH
DEMIRAY, Mutlu
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Abstract
The review paper entitled “The Essential Medicinal
Chemistry of Curcumin”, published in the Journal of
Medicinal Chemistry, by Nelson et al.1 is a well-designed paper,
presenting a new (and negative) approach to the well-known
biologically active compound; curcumin. Although some
arguments throughout this paper are completely true, the
approach of the authors is unfortunately far from impartial, and
many of the conclusions the authors draw from some of their
referred papers are especially hard to accept.
On page 1621, line 11, the authors mention that the in vivo
stability of curcumin is T1/2 < 5 min and F < 1% by referring to
the research papers of Wang et al.2 and Yang et al.3 (refs 27 and
28 of the original paper). Interestingly, neither Wang nor Yang
et al. directly report these values as the half-life of curcumin,
which makes this a very biased supposition of the authors. The
paper, published by Wang et al., reports the stability of
curcumin in buffer solvents at laboratory conditions and in rat
blood circulation. Since it is impossible to directly dissolve
curcumin in water, curcumin was dissolved in methanol and
then diluted with a buffer, and the amount of curcumin was
measured in HPLC at different intervals. It is obvious that
curcumin will start precipitating upon dilution with a buffer.
Thus, it is doubtful that the sample injected in HPLC or
administered to rats includes the supposed amount of
curcumin.
Yang et al. also do not report the half-life of curcumin below
5 min. This paper reports the elimination period as 28.1 ± 5.6
and 44.5 ± 7.5 min for 500 mg/kg, p.o. and 10 mg/kg, i.v. of
curcumin, respectively. It is noteworthy that the half-life results
are reported by the studies made in rats, not human studies. A
rat weighing 400 g has a total blood volume of approximately
25.6 mL,4 and the human blood volume is approximately 5.5 L.
The half-life measurements of the compound during blood
circulation were made without considering the insolubility of
curcumin in buffer solutions or the stability measurements in
rat blood circulation and therefore do not accurately illustrate
the fate of curcumin upon circulation within human blood.
More interestingly, the authors acknowledge that the half-life of
curcumin with pH 7.4 and 37 °C in human blood is 360−480
min in Supplemental Table 2 of ref 1. However, they report its
stability as T1/2 < 5 min on page 1621, left column line 11.
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Bahadori F., DEMIRAY M., -A Realistic View on -The Essential Medicinal Chemistry of Curcumin-, ACS MEDICINAL CHEMISTRY LETTERS, cilt.8, ss.893-896, 2017