Piperine: Old Spice and New Nutraceutical?

Abstract

Background: Many of the activities associated with pepper fruits have been attributed to piperine, the most active compound present in these spices. Objective: This paper aims to provide an overview of the known properties of piperine, i.e. piperine’s chemistry, its physiological activity, documented interactions as a bioenhancer and reported data concerning its toxicity, antioxidant properties and anticancer activity. Discussion: It is known that piperine possesses several properties. In its interaction with other drugs, it can act as a bioavailability enhancer; this effect is also manifested in combination with other nutraceuticals, e.g. with curcumin, i.e. piperine can modify curcumin’s antioxidant, anti-inflammatory, antimicrobial and anticancer effects. Piperine displays significant immunomodulating, antioxidant, chemopreventive and anticancer activity; these effects have been shown to be dose-dependent and tissue-specific. However, the main limitation associated with piperine seems to be its low bioavailability, a disadvantage that innovative formulations are overcoming. Conclusion: It is predicted that an increasing number of studies will focus on piperine, especially those directed towards unraveling its properties at molecular level. The current knowledge about the action of piperine will form a foundation for ways to improve piperine’s bioavailability e.g. exploitation of different carrier systems. The therapeutical applications of this compound will be clarified, and piperine will be recognized as an important nutraceutical.

Piperine Inhibits TGF-β Signaling Pathways and Disrupts EMT-Related Events in Human Lung Adenocarcinoma Cells

“…Over the last twenty years, numerous studies have shown that many natural products display chemoprotective properties against different types of cancers [1,2]. In this context, piperine (a trans-trans isomer of 1-piperoyl piperidine) (Figure 1), the pungent amide present in Piper spices, such as the widely used black pepper (Piper nigrum L.,) is known to present a broad spectrum of biological activities, including its anti-cancer effect [3][4][5]. Regarding the multidrug resistance (MDR) phenotype, a serious obstacle for the treatment of cancer patients [6], previous studies have demonstrated that piperine inhibits the activity of the main ABC transporters related to MDR phenotype [7,8].…”

Anti-inflammatory effect of piperine ameliorates insulin resistance in monosodium glutamate–treated obese mice

“…Furthermore, we examined the TLR-4, CD11c and IL-1βwith a Western blot analysis. The results showed that piperine (20,40, and 80 µM) inhibited the expression of TLR-4, IL-1β, and CD11c in the RAW264.7 cells after LPS treatment (Fig. 10A-B).…”

“…Piperine is the major alkaloid presented in black pepper (Piper nigrum), long pepper (Piper longum), and many other piper species. Piperine exhibits a wide range of biological properties, such as immunomodulatory, anti-oxidant, anti-lipid metabolism disorder, and anti-inflammatory [18][19][20].…”

Vicinal difluorination as a C=C surrogate: an analog of piperine with enhanced solubility, photostability, and acetylcholinesterase inhibitory activity

“…Piperine (1, Figure 1) is a well-known natural product that is derived from peppercorns [1][2][3]. Many biological studies of 1 have been carried out, and these studies have led to a diverse array of biological activities being claimed for this compound [4][5][6][7][8][9]. For example, 1 is reported to exhibit inhibitory activity towards both acetylcholinesterase (AChE) and β-secretase (BACE-1), which suggests that 1 could hold promise as a dual mechanism-of-action treatment for Alzheimer's disease [4,[10][11][12][13].…”