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  3. Overview of piperlongumine analogues and their therapeutic potential

Overview of piperlongumine analogues and their therapeutic potential

  • Eur J Med Chem. 2021 Aug 5:220:113471. doi: 10.1016/j.ejmech.2021.113471.
Peng Zhu 1,  Jianqiang Qian 2,  Zhongyuan Xu 2,  Chi Meng 3,  Weizhong Zhu 2,  Fansheng Ran 3,  Wei Zhang 4,  Yanan Zhang 5,  Yong Ling 6
Affiliations

Affiliations

  • 1 Medical School, Nantong University, Nantong, 226001, China; School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, China; State Key Laboratory of Quality Research in Chinese Medicines, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Macau.
  • 2 Medical School, Nantong University, Nantong, 226001, China; School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, China.
  • 3 School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, China.
  • 4 State Key Laboratory of Quality Research in Chinese Medicines, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Macau. Electronic address: wzhang@must.edu.mo.
  • 5 Medical School, Nantong University, Nantong, 226001, China; School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, China. Electronic address: yznj00@outlook.com.
  • 6 Medical School, Nantong University, Nantong, 226001, China; School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, China. Electronic address: Lyyy111@sina.com.
PMID: 33930801 DOI: 10.1016/j.ejmech.2021.113471
Abstract

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 anti-tumor 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.

Keywords

Biological activities; Derivatives/analogues; Piperlongumine; Reactive oxygen species; Structure and activity relationship.

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