Overview of piperlongumine analogues and their therapeutic potential

Natural products have long been an important source for discovery of new drugs to treat human diseases. Piperlongumine (PL) is an amide alkaloid isolated from Piper longum L. (long piper) and other piper plants and has received widespread attention because of its diverse biological activities. A large number of PL derivatives have been designed, synthesized and assessed in many pharmacological functions, including antiplatelet aggregation, neuroprotective activities, anti-diabetic activities, anti-inflammatory activities, anti-senolytic activities, immune activities, and antitumor activities. Among them, the antitumor effects and application of PL and its derivatives are most extensively studied. We herein summarize the development of PL derivatives, the structure and activity relationships (SARs), and their therapeutic potential on the treatments of various diseases, especially against cancer. We also discussed the challenges and future directions associated with PL and its derivatives in these indications. (C) 2021 Elsevier Masson SAS. All rights reserved.

Automated summary

The study summarizes the diverse biological activities of piperlongumine (PL) and its derivatives, with a focus on their antitumor effects. Researchers discussed the therapeutic potential of PL and its derivatives in treating various diseases, especially cancer, as well as the challenges and future directions for research in this area.