Environmental Engineering Reference
In-Depth Information
stems, the highest concentrations of this lignan in
Larrea tridentata
are observed in
leaves (38.3 mg/g) and green stems (32.5 mg/g) [22]. An amount of 10% of leaves
dry weight, approximately, consists of NDGA, representing 80% of all phenolics in
the resin.
Regarding the applications of NDGA in biological systems, several studies on
its pharmacological activities have been conducted and are reported in Table 2. The
earliest and best known property of NDGA is the capacity of inhibiting lipoxyge-
nase [23, 24]. NDGA also inhibits the platelet derived growth factor receptor and
the protein kinase C, both playing an important role in proliferation and survival of
cancers [25]. Lee and co-workers [26] investigated the inhibitory effect of NDGA on
the transforming growth factor-
β
(TGF-
β
) activity in osteoblastic cell lines. TGF-
β
Ta b l e 2
Some of the NDGA pharmacological activities
NDGA pharmacological applications
Mechanisms proposed
References
Cancer chemopreventive activity
Reactivation of methylation-silenced
tumor suppressor gene p161NK4a
Cells arrest at the G1 phase and
induction of cellular senescence in
cancer cells
[103]
Suppression of breast cancer cells
growth
Inhibition of the function or two
receptor tyrosine kinases, IGF-1R
and HER2/neu
[104]
Changes of DNA methylation during
differentiation of human glioma
cells
Inhibition of 5-cytosine DNA
methyltransferase activity
[105]
Protection of DNA oxidation
Phenolic hydrogen atoms donation to
quench hydroxyl radicals
[106]
Apoptosis of lypoxygenase-deficient
FL5.12 cells
Depletion of glutathione and induction
of a decrease in the mitochondrial
membrane potential
[107]
Reduction of lung adenoma
multiplicity of mice
Inhibition of 5-lypoxygenase
[108]
Antimicrobial activity
Inhibition of
Entamoeba histolytica
in
culture
Antiamoebic activity through the
formation of the ortho-quinone form
of NDGA
[109]
Inhibition of
Staphylococcus aureus
,
Bacillus subtilis
and
Streptococcus
faecalis
-
[110]
Fertility and reproductive effects
Suppression of oxytocin-induced
prostaglandin F2alpha
Delay of luteolysis
[111]
Ovulation inhibition, and leukotriene
and prostaglandin reduction
Suppression of ovarian tissue PGE2
and PGF2alpha levels
[112]
Stimulation of pS2 expression
Binding to the estrogen receptor
causing upregulation of the
estrogen-responsive protein pS2
[113]
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