Piperlongumine, a potent anticancer phytotherapeutic: Perspectives on contemporary status and future possibilities as an anticancer agent.

Abstract

Piperlongumine, a white to beige biologically active alkaloid/amide phytochemical, has high pharmacological relevance as an anticancer agent. Piperlongumine has several biological activities, including selective cytotoxicity against multiple cancer cells of different origins at a preclinical level. Several preclinical studies have documented the anticancer potential of piperlongumine through its targeting of multiple molecular mechanisms, such as cell cycle arrest, anti-angiogenesis, anti- invasive and anti-metastasis pathways, autophagy pathways, and intrinsic apoptotic pathways in vitro and in vivo. Mechanistically, piperlongumine inhibits cancer growth by resulting in the accumulation of intracellular reactive oxygen species, decreasing glutathione and chromosomal damage, or modulating key regulatory proteins, including PI3K, AKT, mTOR, NF-kβ, STATs, and cyclin D1. Furthermore, combined treatment with piperlongumine potentiates the anticancer activity of conventional chemotherapeutics and overcomes resistance to chemo- and radio- therapy. Nanoformulation of piperlongumine has been associated with increased aqueous solubility and bioavailability and lower toxicity, thus enhancing therapeutic efficacy in both preclinical and clinical settings. The current review highlights anticancer studies on the occurrence, chemical properties, chemopreventive mechanisms, toxicity, bioavailability, and pharmaceutical relevance of piperlongumine in vitro and in vivo.

• Authors: Surya Kant Tripathi, Bijesh Kumar Biswal
• Journal: Pharmacological research (Pharmacol Res) Vol. 156 Pg. 104772 (06 2020) ISSN: 1096-1186 [Electronic] Netherlands
• PMID: 32283222 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
• Copyright: Copyright © 2020 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents, Phytogenic
• Dioxolanes
• piperlonguminine

Topics

• Animals
• Antineoplastic Agents, Phytogenic (adverse effects, pharmacokinetics, therapeutic use)
• Antineoplastic Combined Chemotherapy Protocols (therapeutic use)
• Biological Availability
• Dioxolanes (adverse effects, pharmacokinetics, therapeutic use)
• Drug Compounding
• Drug Resistance, Neoplasm
• Humans
• Neoplasms (drug therapy, metabolism, pathology)
• Signal Transduction
• Treatment Outcome