Piperine: an emerging biofactor with anticancer efficacy and therapeutic potential

Area of Science:

• Natural product chemistry
• Pharmacology
• Oncology

Background:

• Cancer remains a leading cause of mortality, with current treatments facing challenges like high costs, side effects, and drug resistance.
• Herbaceous plants offer a rich source of natural compounds with novel anticancer mechanisms.
• Piperine, derived from Piper species, is recognized for its potential anticancer properties and ability to enhance drug bioavailability.

Purpose of the Study:

• To provide a comprehensive review of Piperine's anticancer potential, covering its sources, chemistry, and therapeutic applications.
• To explore Piperine's dual role as a direct antitumor agent and a bioenhancer for conventional chemotherapeutics.
• To summarize preclinical and clinical data, mechanisms of action, and safety profile of Piperine in cancer therapy.

Main Methods:

• Literature search on PubMed/MedLine using keywords: "Piperine anticancer," "Piperine derivatives," "Piperine antitumor mechanism," and "Piperine pharmacokinetic and bioavailability."
• Inclusion and exclusion criteria applied to 444 articles, selecting 101 relevant studies published between 2013 and 2023.
• Review of preclinical data, including in vitro studies on various cancer cell lines and in vivo studies on animal models.

Main Results:

• Extensive preclinical research demonstrates Piperine's efficacy in inhibiting proliferation and inducing apoptosis across numerous cancer cell lines (e.g., breast, lung, colon, leukemia).
• In vivo studies in animal models confirm Piperine's antitumor activity.
• Piperine exhibits a novel mechanism of action by modulating apoptosis and autophagy pathways with low toxicity and acts as a bioenhancer, improving absorption and efficacy of other anticancer agents.

Conclusions:

• Piperine shows significant promise as a standalone anticancer agent or as a bioenhancer to improve existing chemotherapy regimens.
• Its unique mechanisms, low toxicity, and ability to overcome drug resistance provide a strong foundation for developing novel cancer therapies.
• Further clinical trials are warranted to fully establish Piperine's role in human cancer treatment.