New Tyramine- and Aporphine-Type Alkamides with NO Release Inhibitory Activities from <i>Piper puberulum</i>
Yuan-kun Zheng, Bao-Jun Su, Yaqi Wang, Heng‐Shan Wang, Hai‐Bing Liao, Dong Liang
Abstract
Three new tyramine-type alkamides (1–3), three new natural products (4–6), five new N-acylated/formylated aporphine alkamides with different ratios of rotational isomers (7–11), and 20 known alkamides (12–31) were isolated from an EtOH extract of the stems and leaves of Piper puberulum. The absolute configurations of compounds 7, 8, and 10 were determined by single-crystal X-ray diffraction analysis. In the biological activity assay, compounds 3, 5, and 10–23 displayed inhibitory effects against lipopolysaccharide-induced NO release in BV-2 microglial cells, exhibiting IC50 values of 0.93–45 μM.
Topics & Concepts
TyramineStereochemistryChemistryPiperAlkaloidPiperaceaeIC50Inhibitory postsynaptic potentialPharmacognosyBiological activityIn vitroBiochemistryBiologyBotanyNeurosciencePiperaceae Chemical and Biological StudiesTraditional and Medicinal Uses of AnnonaceaeEssential Oils and Antimicrobial Activity