Piperine-A Major Principle of Black Pepper: A Review of Its Bioactivity and Studies

Abstract

Piperine is the main compound present in black pepper, and is the carrier of its specific pungent taste, which is responsible for centuries of human dietary utilization and worldwide popularity as a food ingredient. Along with the application as a food ingredient and food preservative, it is used in traditional medicine for many purposes, which has in most cases been justified by modern scientific studies on its biological effects. It has been confirmed that piperine has many bioactive effects, such as antimicrobial action, as well as many physiological effects that can contribute to general human health, including immunomodulatory, hepatoprotective, antioxidant, antimetastatic, antitumor, and many other activities. Clinical studies demonstrated remarkable antioxidant, antitumor, and drug availability-enhancing characteristics of this compound, together with immunomodulatory potential. All these facts point to the therapeutic potential of piperine and the need to incorporate this compound into general health-enhancing medical formulations, as well as into those that would be used as adjunctive therapy in order to enhance the bioavailability of various (chemo)therapeutic drugs.

Fungal Endophytes as Efficient Sources of Plant-Derived Bioactive Compounds and Their Prospective Applications in Natural Product Drug Discovery: Insights, Avenues, and Challenges

“…Piperine decreases liver marker enzymes activity, inhibits lipopolysaccharide-induced expression of interferon regulatory factor, reduces the activation of STAT1, and inhibits the release of Th-2-mediated cytokines indicating its anti-inflammatory activity. Piperine expresses its anticancer activity through the following mechanisms: activates caspase-3 and caspase-9, cleaves poly(ADP-ribose) polymerase (PARP), decreases Bcl-2 protein expression and increases Bax protein, reduces the expression of phosphorylated STAT3 and nuclear factor kappa B (NF-kB) transcription factors, blocks extracellular signal-regulated kinase (ERK1/2), p38 MAPK, and AKT signaling pathways, and suppresses epidermal growth factor (EGF)-induced matrix metalloproteinase (MMP)-9 expression [ 92 ]. It has bioavailability-enhancing ability for certain drugs and nutrients.…”

Effect of Piperine in Combination with Gamma Radiation on A549 Cells

“…Accumulating literature data on in vitro and in vivo activities of piperine show that piperine has immunomodulatory and antiallergic, anti-inflammatory, enhanced drug bioavailability potential, antimutagenic on healthy cells. 28,29 Cytotoxic effect is selective toward cancer cells. [30][31][32] In the present study, we observe piperine as a new compound for reducing the lung cancer proliferation and reveal a novel radiosensitization method of lung cancer via increased inhibition of cell proliferation after piperine pretreatment prior to the radiation treatment.…”

Piper nigrum based diet had a chemopreventive antineoplastic effect potentiated by Curcuma longa in C57BL/6 mice

“…In addition, piperine sensitize breast (including triple negative), colon and prostate cancer cells to chemotherapy and radiation. While, in murine as well as in human melanoma cells, piperine had antiproliferative activity, trough ROS generation-induced Chk1 activation, causing G1 cell cycle arrest and apoptosis [8,9].…”