1. Academic Validation
  2. New Tyramine- and Aporphine-Type Alkamides with NO Release Inhibitory Activities from Piper puberulum

New Tyramine- and Aporphine-Type Alkamides with NO Release Inhibitory Activities from Piper puberulum

  • J Nat Prod. 2021 Apr 23;84(4):1316-1325. doi: 10.1021/acs.jnatprod.1c00055.
Yuan-Kun Zheng 1 Bao-Jun Su 1 Ya-Qi Wang 1 Heng-Shan Wang 1 Hai-Bing Liao 1 Dong Liang 1
Affiliations

Affiliation

  • 1 State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, People's Republic of China.
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.

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