Biosynthesis of Phytic Acid
Cellular roles proposed for phytic acid including inhibition of protein phosphatases and subsequent
modulation of calcium channel activity, attenua- tion of endocytosis, and inhibition of clathrin
assembly [78,79]. Here, further work is needed to fully confirm these functions.
Although the orientation of the phosphate groups in phytic acid was established, there was
much debate about the conformation adopted [71,80]. 1ax5eq and 5ax1eq Fig. 9 differ signifi-
cantly in overall molecular shape and the orienta- tion of polar groups. Consequently, the two
conformations exhibit significant differences in chelating
ability, including
interaction with
proteins. Therefore, the conformational preference of phytic acid in different environments is critical
to understanding the chemistry and biochemistry of phytic acid. Assignment of conformations for
phytic acid [71] has only recently been fully re- solved.
1
H-NMR spectroscopic methods [80] en- abled Barrientos and Murthy [81] to show that MI
adopts the sterically favorable 1ax5eq conforma- tion one phosphate axial and five equatorial in
pH range 1.0 – 9.0 and the sterically hindered 5ax 1eq conformation above pH 9.5 Fig. 9. Between
pH 9.0 – 9.5 the pKa region of the three least acidic protons both conformations are in dynamic
equilibrium. Dynamic NMR indicates that the activation energy for the conformational inversion
process is 54.8 9 0.8 kJmole compared to that for ring inversion of cyclohexane, about 45 kJ
mole [82]. Inversion to the 5ax1eq form is facili- tated by complexation with metal ions which
reduces electrostatic repulsion and thereby stabi- lizes the sterically hindered, dodeca-anionic form.
Stabilization of the 5ax1eq form is influenced by the size of the counter ion. Alkali metals Na
+
, K
+
, Rb
+
and Cs
+
with hydrated radii less than or equal to 2.76 A
, stabilize the 5ax1eq form whereas Li
+
ion hydrated radii 3.4 A , does not
stabilize that form. In the presence of larger coun- ter ions such as tetramethylammonium and tetra-
butylammonium ions, the presence of the sterically hindered 5ax1eq form is not observed, thus indi-
cating that complexation with counter ions is es- sential for ring inversion of phytic acid [82].
NMR spectroscopy also indicated that the con- formational preferences of individual isomers at
different pH’s are dictated by structural features unique to the isomer such as the number of phos-
phate moieties and the regiochemical and stereo- chemical arrangement of the phosphates [81].
Ins1,2,3,4,6P
5
adopts the 1ax5eq form in the pH range 1.0 – 9.0 and above 9.5 both 1ax5eq and
5ax1eq forms exist in dynamic equilibrium; the exclusive presence of the 5ax1eq form is not
observed. Inositol phosphates containing less than 5 phosphates showed no proclivity to undergo ring
inversion to the sterically hindered form [81].
Molecular modeling studies were carried out using ab initio, semi-empirical and force field
methods MacroModel V6.0 and Gaussian 94, for both the 1ax5eq and 5ax1eq conformations of
phytic acid in the fully protonated and dodeca-an- ionic state [82]. Molecular modeling calculations
were consistent with NMR results in aqueous so- lution. Interestingly, calculations predicted that
the relative stability of the two conformations is the same in vacuum and aqueous solution,
namely, in the fully protonated state the sterically favourable 1ax5eq form of phytic acid is more
stable than the 5ax1eq form and that in the dodeca-anionic state the sterically hindered 5ax
1eq form is more stable than the 1ax5eq form [82].