The preparation and antihyperlipidaemic assay of piperlonguminine in vivo

The natural product piperlonguminine (GBN) which is extracted from Piper longum Linn., has high antihyperlipidaemic activity and low toxicity. However, the content of natural GBN in P. longum (0.20–0.25%) is low, and it is not easy to prepare enough sample of natural GBN for further studies, such as large-scale animal experiments. Therefore, in the present study, we tested and confirmed the antihyperlipidaemic activity of chemically synthesised GBN in rats for the first time. The results of the antihyperlipidaemic assay in vivo showed that synthetic GBN had significant lipid-lowering activities. Synthetic GBN not only inhibited body weight gain (66.3 ± 22.50 g vs. 83.9 ± 19.95 g) but also significantly decreased total cholesterol (TC, 9.67 ± 3.32 mmol/L vs. 22.26 ± 5.84 mmol/L), total glycerol (TG, 1.47 ± 0.08 mmol/L vs. 2.86 ± 0.75 mmol/L), and low-density lipoprotein cholesterol (LDL-C, 3.57 ± 1.15 mmol/L vs. 5.44 ± 1.42 mmol/L) while increasing high-density lipoprotein cholesterol (HDL-C, 1.31 ± 0.56 mmol/L vs. 0.68 ± 0.20 mmol/L) in the serum of rats fed a high-fat diet.