Acetylcholinesterase Inhibitors from Angelica polymorpha Stem

Abstract

-Fourteen compounds were isolated from the stem of Angelica polymorpha. On the basis of spectral data, these compounds were identified as isoimperatorin (1), phellopterin (2), bergapten (3), xanthyletin (4), cnidilin (5), geijerine (6), (−)-3'-acetyl hamaudol (7), 7-demethylsuberosine (8), dehydrogeijerin (9), (-)-hamaudol (10), (+)-visamminol (11), divaricatol (12), scopoletin (13), and decursidate (14), respectively. Among them, compounds 4 -6, 8, 9, 13, and 14 were isolated for the first time from A. polymorpha. Dehydrogeijerin (6) and geijerin (9) were isolated for the first time from genus Angelica. All isolates tested for inhibitory activity against acetylcholinesterae. Compounds 1 to 13 showed acetylcholinesterase inhibitory activity with IC 50 values ranging from 1.4 to 37.5 µM.

Interaction studies of Angelica polymorpha and Beilschmiedia pulverulenta phytochemicals with acetylcholinesterase as anti-Alzheimer's disease target

“…The acridone backbone of the compounds conveniently enjoyed hydrophobic interaction with residues Phe330, His440 and Trp84 among the amino acid residues lining the active site. The presence of these interactions possibly explains the high affinity of these compounds to the acetylcholinesterase which is consistent with the report of Kwon and co-workers (Kwon et al, 2017). These residues were earlier found in the interaction between AChE and its previously reported ligands (Harel et al, 1993;Greenblatt et al, 1999;Haviv et al, 2005) indicating that the mechanism of inhibition for the phytoconstituents is compatible with that of reference ligands.…”

“…A total of 20 ligands used in this docking study were selected from the literature Kwon et al, 2017). Out of these compounds, 13 were phytochemicals isolated from A. polymorpha while 5 were phytoconstituents obtained from B. pulverulenta.…”

“…Among the identified plants with cholinesterase inhibitory potential are Angelica polymorpha and Beilschmiedia pulverulenta. These valuable plants have been importantly noted for their uses in folkloric medicine for the management of various diseases including AD Kwon et al, 2017).…”

“…In a recent report, Salleh and co-workers had isolated and characterised the chemical constituents from Beilschmiedia pulverulenta stem bark and evaluated the antiinflammatory and anticholinesterase activities of the constituents in vitro . Likewise, the essential bioactive ingredients in various extracts of A. polymorpha were also recently isolated and structurally characterised (Kwon et al, 2017).…”

Chemical Profiling, Antioxidant, Anticholinesterase, and Antiprotozoal Potentials of Artemisia copa Phil. (Asteraceae)

“…The neuroprotective properties have been associated to the ChE inhibition, as well to the prevention of oxidative damage (Oboh et al, 2013). AChE activity have been reported for 7demethylsuberosin isolated from genus Angelica, suggesting a potential agent for the AD (Kang et al, 2001;Kwon et al, 2017). In addition, Schaftoside isolated from the water layer of Lycopodiella cernua (L.) Pic.Serm.…”