Nemzeti Kutatási Fejlesztési és Innovációs Hivatal(NKFIH-4300- 1/2017-NKP_17)
OTKA(K-134221)
OTKA(K-135712)
TKP2020(IKA-05)
Stipendium Hungaricum Scholarship(Stipendium) Támogató: Tempus
Arctigenin is a bioactive dibenzylbutyrolactone-type lignan exhibiting various pharmacological
activities. The neuroprotective effects of arctigenin were demonstrated to be mediated
via inhibition of AMPA and KA type glutamate receptors in the somatosensory cortex
of the rat brain. The aim of this study was to compare the effects of arctigenin with
matairesinol and trachelogenin on synaptic activity in ex vivo rat brain slices. Arctigenin,
matairesinol and trachelogenin were isolated from Arctium lappa, Centaurea scabiosa
and Cirsium arvense, respectively, and applied on brain slices via perfusion medium
at the concentration range of 0.5-40 µM. The effects of the lignans were examined
in the CA1 hippocampus and the somatosensory cortex by recording electrically evoked
field potentials. Arctigenin and trachelogenin caused a significant dose-dependent
decrease in the amplitude of hippocampal population spikes (POPS) and the slope of
excitatory postsynaptic potentials (EPSPs), whereas matairesinol (1 µM and 10 µM)
decreased EPSP slope but had no effect on POPS amplitude. Trachelogenin effect (0.5
µM, 10 µM, 20 µM) was comparable to arctigenin (1 µM, 20 µM, 40 µM) (p ˃ 0.05). In
the neocortex, arctigenin (10 µM, 20 µM) and trachelogenin (10 µM) significantly decreased
the amplitude of evoked potential early component, while matairesinol (1 µM and 10
µM) had no significant effect (p>0.05). The results suggest that trachelogenin and
arctigenin act via inhibition of AMPA and KA receptors in the brain and trachelogenin
has a higher potency than arctigenin. Thus, trachelogenin and arctigenin could serve
as lead compounds in the development of neuroprotective drugs.
