Identification of Novel Alkaloids from Portulaca oleracea L. and Characterization of Their Pharmacokinetics and GLP-1 Secretion-Promoting Activity in STC-1 Cells.

Abstract

Six new alkaloids (compounds 1-6) were isolated from Portulaca oleracea L. The compounds were triple pair (1 and 2, 3 and 4, and 5 and 6) enantiomers, with 1, 3, and 5 in the R-configuration and 2, 4, and 6 in the S-configuration, and all could bind to SUR1 according to molecular docking analysis. Treatment of STC-1 cells with each compound led to an influx of intracellular Ca2+, eventually leading to the secretion of glucagon-like peptide-1 (GLP-1), with compound 3 giving the highest secretion, resulting in 24.3 ± 7.03% more GLP-1 than nateglinide-treated cells, suggesting that these alkaloids may be able to reduce blood glucose based on their ability to stimulate the release of GLP-1. Furthermore, compound 3 also exhibited slightly faster absorption than nateglinide, as shown by pharmacokinetic analysis conducted in rats. Therefore, the results showed that some purslane alkaloids (such as compound 3) had good pharmacological activity in vivo and may have preventive and therapeutic effects on diabetes.