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%.
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.
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.
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
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.
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)
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)
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)
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
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.