Piperine

Description

General Description:

Piperine is a pungent alkaloid present in Piper nigrum Linn and Piper longum Linn and is thought to be the active ingredient found in black pepper. This discovery has prompted numerous scientific studies into piperine's possible therapeutic effects with the principle effect seeming to be as a bioavailability enhancer. The natural concentration of piperine in black pepper is around 5-9%.

Nutritional Supplements

Suggested Intakes:

The dose of piperine considered to be bioenhancing for absorption of nutrients is calculated as 0.04 to 0.08 mg piperine/kg body weight. This dose is 4,000 to 40,000 times less than the LD(50) dose (dose toxic to 50% animals tested) of piperine.(21) Studies showed therapeutic concentrations of piperine to be between 3mg and 399mg with no adverse effects reported.

Supplemental uses:

Bioavailability

A recent study found that piperine, extracted from black pepper, caused an increase in bioavailability for ions and macromolecules and this might be of pathophysiological importance with respect to food allergy and intolerance. (1)

This study was designed to investigate and understand the absorption dynamics of piperine in the intestine on oral absorption, using human intestinal cells as an experimental model. The results suggested that piperine is absorbed very fast across the intestinal barrier and it may modulate membrane dynamics due to its easy partitioning thus helping efficient permeability across the intestinal wall. (2)

Another study also demonstrated that piperine may have the ability to increase the bioavailability of certain nutrients. This study used coenzyme Q10 as the nutrient and the results showed that piperine did increase plasma levels of coenzyme Q10 and it is thought that this bioenhancing mechanism is non-specific and possibly based on its description in the literature as a thermonutrient. (3)

A recent study was designed to investigate the mode of action regarding piperine's bioenhancing effect. The results showed that piperine may be inducing alterations in membrane dynamics and permeation characteristics, along with induction in the synthesis of proteins associated with cytoskeletal function, resulting in an increase on the small intestine absorptive surface, thus assisting efficient permeation through the epithelial barrier. (4)

The bioenhancing effects of piperine have been demonstrated in several other studies which show that piperine can improve the absorption of many nutrients. These include: Vitamin C, Selenium, Beta-carotene, vitamin A, vitamin B6, Coenzyme Q10. This action is thought to be non-specific which is demonstrated by the range of nutrients which had improved absorption. (6)

Antioxidant:

Piperine was shown to be an effective antioxidant in this recent study. The results suggested that piperine modulates the oxidative changes by inhibiting lipid peroxidation, which may mean that piperine could be an important nutrient for the prevention of atherosclerosis. (7)

Digestive Enzyme Stimulator:

This recent study investigated the effect of piperine on the secretion of digestive enzymes from the pancreas. Other dietary spices were also used including curcumin, ginger and mustard, and most spices, including piperine, were shown to increase the activity of the pancreatic enzymes, amylase and lipase. Piperine was also shown to increase the activity of enzymes released by the small intestine, trypsin and chymotrypsin. (8)

Safety:

Side effects and precautions:

Pregnant and lactating women should consult a qualified health professional before using this product. Piperine is not suitable for use by children. Should not be used in conjunction with any form of medication.

Interactions and Contraindications:

Piperine has been shown to interfere with the metabolism of certain medications which may delay their breakdown and enhance any side-effects. This study was designed to evaluate the effectiveness of piperine on the bioavailability of drugs such as vasicine (brain stimulant) and sparteine (used to induce labour by stimulating the contraction of the womb).

Long pepper was used in the study and blood samples were taken after consumption of both the drug and long pepper. Under the influence of piperine, which is the active ingredient in long pepper, sparteine blood levels increased more than 100%. It is thought that this increase in bioavailability was achieved by promoting rapid absorption from the gastrointestinal tract, or by protecting the drug from being metabolised/oxidised in its first passage through the liver after being absorbed, or by a combination of both. (5)

References:

1) J Nutr 1998 Mar; 128(3):577-81

2) Indian J Exp Biol 1998 Jan; 36(1):46-50

3) Mol Cell Biochem 1998 Dec; 189(1-2):113-8

4) 0955-2863 2003 Feb 1; 11(2): 109-113

5) Phytomedicine 2002 Apr; 9(3): 224-31

6) Nahrung 2000 Feb; 44(1): 42-6

7) J Ethnopharmacol 1981 Sep; 4(2): 229-32

8) www.bioperine.com/Manual/ClinicalStudies1.htm

Further Research:

Influence of Piperine on Curcumin Utilisation
The medicinal properties of curcumin from Curcuma Longa L cannot be utilised because of poor bioavailability due to its rapid metabolism in the liver and intestinal wall. In this study, the effect of combining piperine, a known inhibitor of hepatic and intestinal glucuronidation was evaluated on the bioavailability of curcumin alone, serum levels were either undetectable or very low.

Concomitant administration of piperine 20 mg produces much higher concentrations from 0.25 to 1 h post drug the increase in bioavailability was 2000%. The study shows that in the dosages used, piperine enhances the serum concentration, extent of absorption and bioavailability of curcumin in both rats and humans with no adverse effects.

Plant Med. 1998 May; 64 (4): 353-6.