1. New Tyramine- and Aporphine-Type Alkamides with NO Release Inhibitory Activities from Piper puberulum
- Author
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Bao-Jun Su, Hai-Bing Liao, Ya-Qi Wang, Yuan-kun Zheng, Dong Liang, and Heng-Shan Wang
- Subjects
Pharmacology ,010405 organic chemistry ,Stereochemistry ,Organic Chemistry ,Pharmaceutical Science ,Piper puberulum ,Biological activity ,Tyramine ,Inhibitory postsynaptic potential ,01 natural sciences ,0104 chemical sciences ,Analytical Chemistry ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,Complementary and alternative medicine ,chemistry ,Drug Discovery ,Ic50 values ,Molecular Medicine ,Aporphine ,No release - 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.
- Published
- 2021
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