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Papers of the Week


Papers: 10 Jun 2023 - 16 Jun 2023

RESEARCH TYPE:
Basic Science


Animal Studies, Molecular/Cellular, Pharmacology/Drug Development


2023 Jun 06


ACS Omega


37305315


8


22

Argentatin C Analogues with Potential Antinociceptive Activity and Other Triterpenoid Constituents from the Aerial Parts of .

Authors

Xu YM, Wijeratne EMK, Calderon-Rivera A, Loya-López S, Perez-Miller S, Khanna R, Gunatilaka AAL

Abstract

Four new triterpenes, 25-dehydroxy-25-methoxyargentatin C (), 20-hydroxyargentatin C (), 20-hydroxyisoargentatin C (), and 24–argentatin C (), together with 10 known triterpenes (-) were isolated from the aerial parts of . The structures of – were elucidated by detailed analysis of their spectroscopic data, and the known compounds – were identified by comparison of their spectroscopic data with those reported. Since argentatin C () was found to exhibit antinociceptive activity by decreasing the excitability of rat and macaque dorsal root ganglia (DRG) neurons, and its new analogues – were evaluated for their ability to decrease the excitability of rat DRG neurons. Of the argentatin C analogues tested, 25-dehydroxy-25-methoxyargentatin C () and 24–argentatin C () decreased neuronal excitability in a manner comparable to . Preliminary structure-activity relationships for the action potential-reducing effects of argentatin C () and its analogues -, and their predicted binding sites in pain-relevant voltage-gated sodium and calcium channels (VGSCs and VGCCs) in DRG neurons are presented.