ABSTRACT
Hexane extracts of Heracleum verticillatum, H. sibiricum, H. angustisectum, and H. ternatum were studied for their furanocoumarin content antioxidant potential and acetylcholinesterase and α-amylase inhibitory activities. Quantification of the furanocoumarins was performed by 1 H-NMR. Pimpinellin was found to be the main component in the roots of all studied species. Bergapten and imperatorin were the major compounds in the fruits of H. sibiricum and H. verticillatum, respectively, while byakangelicol dominated in H. angustisectum and H. ternatum fruits. The leaf and fruit extracts of H. angustisectum demonstrated the highest DPPH radical scavenging activity and TEAC (IC50 0.58â mg/mL and 1.83â mm, respectively). The root extracts of H. verticillatum and H. angustisectum were found to be the most effective against acetylcholinesterase (IC50 0.30 and 0.34â mg/mL, respectively). The studied extracts were not active or demonstrated a weak inhibitory effect (%Inh. up to 29.7) towards α-amylase.
Subject(s)
Antioxidants/pharmacology , Biphenyl Compounds/antagonists & inhibitors , Enzyme Inhibitors/pharmacology , Furocoumarins/pharmacology , Heracleum/chemistry , Hypoglycemic Agents/pharmacology , Picrates/antagonists & inhibitors , Acetylcholinesterase/metabolism , Alzheimer Disease/drug therapy , Alzheimer Disease/metabolism , Animals , Antioxidants/chemical synthesis , Antioxidants/chemistry , Diabetes Mellitus, Type 2/drug therapy , Electrophorus , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Furocoumarins/chemical synthesis , Furocoumarins/chemistry , Humans , Hypoglycemic Agents/chemical synthesis , Hypoglycemic Agents/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Swine , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolismABSTRACT
The cytoprotective activity of F16BP has been documented in severe conditions such as convulsions, reperfusion injury, septic shock, diabetic complications, hypothermia-induced injury, UV-provoked skin damage and in other processes including apoptosis and excitotoxicity. F16BP shows very efficient cytoprotective activity in astroglial cells exposed to H(2)O(2)-provoked oxidative stress and during neuronal injury caused by hypoxic conditions. As most of the aforementioned processes involve iron activity-related conditions, we investigated the ferric and ferrous iron binding properties of F16BP under physiological conditions using (31)P NMR and EPR spectroscopy. Our results indicate that cytoprotective F16BP activity is predominantly based on ferrous iron sequestration. (31)P NMR spectroscopy of F16BP employing paramagnetic properties of iron clearly showed that F16BP forms stabile complexes with Fe(2+) which was verified by EPR of another divalent cation-Mn(2+). On the other hand, F16BP does not sequester ferric iron nor does it increase its redox activity as shown by (31)P NMR and EPR spin-trapping. Therefore, F16BP may be beneficial in neurodegenerative and other conditions that are characterised by ferric iron stores and deposits.