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Piperine

  • Enhances the uptake and absorption of dietary supplements

  • Especially effective for supplements metabolized in the liver

  • Inhibits glucuronidation

 

Piperine (or Piperaceae) is the active compound in black pepper. When taken as a dietary supplement, Piperine has the ability to significantly improve the absorption and uptake of many dietary supplements.  Piperine is used for its ability to inhibit phase 2 detoxifying enzymes and to prevent the process of glucuronidation.

 

Piperine may also slow intestinal removal of supplements. These effects allow your body to better absorb many supplements (non-endogenous supplements that are metabolized by the liver). The recommended serving size for Piperine is 20mg. Do not use Piperine if you are taking any medication.

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    • This supplement is the active component extracted from black pepper (piper nigrum)

    • Used as an ‘enhancer’ supplement – it allows your body to better absorb dietary supplements and increases their effects

    • Recommended serving size is 20mg taken with supplements metabolized by the liver

  • DO NOT USE THIS SUPPLEMENT IN COMBINATION WITH MEDICATION

 

Piperine Reviews

 

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Background

 

Black pepper (piper nigrum) is a flowering vine that is commonly used around the world as a spice and seasoning. The fruit of the pepper vine is called a black peppercorn. The peppercorn itself is often used in cooking or is crushed as a seasoning. Black pepper includes the dried, wrinkled skin of the black peppercorn, while white pepper refers to the peppercorn with removed skin. Piperine is the trans-trans isomer of 1-piperoyl piperidine and is known to be the major active component of black pepper. When you take supplements or most forms of medication, a natural process called glucuronidation occurs in your liver. This process involves the addition of a glucuronide molecule to the foreign compound, which signals your body to remove it through urinary excretion. It is one of the body’s key defence mechanisms against toxins.[1]

 

Black pepper is a good source of Piperine – a compound with significant effects on your body’s metabolism of biocompounds and supplements. This compound is used specifically for its ability to downregulate or inhibit phase II detoxification enzymes and prevent the glucuronidation process in the liver.[2] It allows certain supplements (especially water-soluble supplements that are metabolized by your liver) to be better absorbed. This effect has been especially well researched when using this supplement in combination with curcumin or Green Tea Extract. [3]

 

In the past, black pepper extract was used in India for a wide variety of ailments, including constipation, diarrhoea, earache, gangrene, heart disease, hernia, hoarseness, indigestion, insect bites, insomnia, joint pain, liver problems, lung disease, oral abscesses, sunburn, tooth decay and toothaches. Today, the key active component can be purchased online as a dietary supplement to support good health and to improve the uptake and absorption of other supplements.[4]

 

There are several other active components in black pepper extract. However, these have not been found to be nearly as effective as Piperine. As a result, most scientific research into the physiological effects of black pepper extract has focussed on Piperine. Other phytochemical components include:

 

-       Ellitorine

-       Guineensine

-       Pipnoohine

-       Trichostachine

-       Piperonal

 

black-pepper-extract

Piperine Effects / Benefits

 

Piperine, also known as Piperaceae, inhibits detoxifying enzymes in your liver that prevent the accumulation and absorption of water-soluble supplements. This means that this supplement is best taken to potentiate (increase) the effects of supplements that are water-soluble and metabolized in your liver. The absorption of catechins found in Green Tea Extract, for example, is significantly improved when taken with this supplement. The same goes for Curcumin – an active compound found in turmeric, which cannot be absorbed without the action of this compound. [5]

 

A review dated from 2007 found that this most widely used spice possesses great benefits from a supplements perspective. By favourably stimulating the digestive enzymes of the pancreas, this dietary supplement was found to enhance digestive capacity and significantly reduce the gastrointestinal food transit time. Several in vitro studies have indicated that it possesses powerful antioxidant effects and that it may help to support a healthy circulatory system by preventing the formation of ‘bad’ LDL-cholesterol. However, its most important benefit is the ability to inhibit enzymatic biotransforming reactions in the liver, thereby improving absorption and uptake of several forms of supplements and other compounds.[6]

 

Piperine, also referred to simply as black pepper extract, may also improve the absorption of other supplements, including:

 

1. Baicalin:

  • A powerful antioxidant and anti-inflammatory extracted from Blue Skullcap. This supplement is currently being studied for a number of potential health benefits, including the promotion of rest and relaxation, stress reduction, supporting healthy skin, and reducing inflammation.[7] 

  • Studies suggest that Baicalin’s absorption is somewhat inhibited by the process of Baiaclian-glucuronide conjugation, which is prevented when using Piperine. [8]

 

2. Berberine HCl

    • Berberine HCl is one of nature’s most powerful health-promoting compounds. It has been studied for a wide range of benefits, some with potentially clinical efficiency. Berberine is especially useful in promoting a strong circulatory system and supporting a healthy hormone balance. [9]

  • Pharmacokinetics is the scientific term for the movement of foreign compounds in the body. Pharmacokinetics studies of Berberine HCl show that its absorption is hindered by the process of glucuronidation. [10] Taking Piperine blocks this process and may enhance Berberine absorption.

3. Magnolia Bark Extract

    • Magnolia Bark extract contains a number of powerful antioxidants, anti-inflammatory, stress-reducing, and mood-lifting plant compounds. Magnolia bark extract may provide relief from pain and stress while improving mood and helping to support healthy sleep.[11]

  • Studies have indicated that up to around 50% of orally-taken Magnolia Bark extract is excreted in urine as a result of the process of glucuronidation. [12] Taking Piperine with Magnolia Bark extract may help to increase Magnolia Bark uptake.

 

Piperine With Curcumin

 

A lot of research has explored the synergistic relationship between Piperine and curcumin. Curcumin is the active chemical found in turmeric, a common spice used in curries and originating from India. Tumeric has been known to have beneficial effects for a very long time. In Eastern medicine, turmeric is often used as a herbal medicine in tonics or ointments and as an antibiotic, anti-viral, anti-inflammatory, and immune-boosting natural compound. [13]

 

Scientific research correlates with this traditional knowledge and modern research has shown that curcumin has an amazing range of benefits for a wide selection of health factors. In fact, scientists are currently researching curcumin’s potential benefits in counter-acting against various pro-inflammatory diseases, where they have found exciting results and a very safe chemical profile. [14]

 

However, the healing properties of Curcumin often cannot be utilized because of its poor absorption in the liver. This is a direct result of the process of glucuronidation – where enzymes in your liver add a glucuronide molecule to the curcumin to ‘mark’ it for removal and excretion.  Studies have shown a 2000% increase in absorption in humans when using this supplement with curcumin, compared to curcumin alone! [15]


Key Mechanisms of Piperine:

    • This active compound has significant and profound effects on metabolic enzymes in the liver and intestine.

    • It may induce alterations in membrane dynamics and permeation characteristics, along with an increase in absorptive surface area in the small intestine.

    • This supplement affects the P-glycoprotein-mediated efflux system, via modulation of functional activities and gene expression of P-Glycoprotein.

  • Some research has pointed to a dose-dependent increase in gastric acid secretion and a delay in gastrointestinal motility.

This supplement may have a profound and serving-size-dependent effect on the uptake and absorption of many supplements. However, it needs to be used responsibly, and special care should be taken to avoid using this supplement in combination with pharmaceutical agents, unless under the strict supervision of a qualified doctor (because of its potential to increase effects or affect uptake/metabolism).[16]

piperine-for-absorption

Piperine Recommended Usage

 

This compound is unlikely many traditional dietary supplements in the sense that it is not traditionally taken to produce any noticeable effects on the mind or body.

 

This supplement is better used as an ‘enhancer’ supplement – taken in COMBINATION with supplements that are metabolized by the liver. The liver is the organ that is responsible for dealing with foreign compounds and toxins. Almost all supplements that are not found endogenously in your body (not amino acids or neurotransmitters like GABA, choline, melatonin, or 5-HTP) will need to be metabolized in the liver before being taken into your bloodstream.

 

This supplement blocks enzymes in your liver called ‘Phase 2 detoxifying enzymes’ as well as inhibiting the process of glucuronidation. Furthermore, it may also slow the gastric intestinal transit speed, meaning that it will prolong the time your body takes to remove supplements.[17] As a result, this compound has a strong potential to effectively increase the effects of most dietary supplements.

 

When using Piperine to improve the effects of dietary supplements, the recommended serving size is around 20 mg.[18]

 

Piperine Side Effects / Warnings

 

Black pepper is generally regarded as safe and is used around the world in food as a seasoning. This supplement offers a strong extract of the primary active compound from black pepper. There is limited information about the toxicity of Piperine in humans. Studies show a very low toxicity rating at the serving sizes studied to-date.

 

Animal studies show an LD50 value (the dosage at which half the animals are killed) of between 33.5 – 514 mg/kg body weight.[19] For a 75 kg human, this would equate to a lethal serving size of between 2.5 and 38.5 grams – far greater than the recommended size of 20 mg. There is limited research on the safety of black pepper extract for pregnant and nursing women. Please consult with your doctor before using this supplement.

 

Importantly, there may be significant interactions between this supplement and medication. If you are taking any medication, it is very important that you consult with your doctor before using a Piperine supplement. This supplement affects the way that medication is absorbed in the body.

 

DO NOT USE THIS SUPPLEMENT IN COMBINATION WITH ANY MEDICATION.

 

Conclusion

 

In summary, black pepper extract has been used in India and around the world as a herbal remedy for a variety of ailments, for hundreds of years. It was not until fairly recently that the physiological benefits of the key chemical component of black pepper were discovered. When taken as a dietary supplement, this compound helps to improve the absorption and uptake of other dietary supplements – especially those that are metabolised by the liver. It is best used as an ‘enhancer’ supplement, taken to improve the effects of poorly bioavailable supplements.

The recommended serving size for this supplement is a single serving of 20 mg per day, or in combination with your favourite dietary supplement. This supplement has a very low toxicity and is considered to be very safe for use when taken at the suggested serving size. However, it may have considerable interactions with medication. DO NOT USE THIS SUPPLEMENT IF YOU ARE TAKING MEDICATION. There is also limited research into its safety for pregnant and nursing women. It is suggested to consult with your doctor before using this supplement if you have any underlying medical conditions.

 

piperine-chemical-structure

 

Medical Disclaimer: 

Not intended to treat, diagnose, or cure any disease or ailment. Please read and fully understand potential adverse effects before using this product. These statements have not been reviewed by the FDA and are not written by a medical professional. Please consult your doctor before using any supplements, especially if you have any medical conditions.

 

References:



[1]Glucuronidation’, ScienceDirect Topic, available online at http://www.sciencedirect.com/topics/neuroscience/glucuronidation [Accessed October 26, 2017]

[2] Di, X., Wang, X., Di, X., Liu, Y. Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats. J Pharm Biomed Anal. 2015 Nov 10;115:144-9.

[3] Lambert, J.D., et al. Piperine enhances the bioavailability of the tea polyphenol (-)-epigallocatechin-3-gallate in mice. J Nutr. 2004 Aug;134(8):1948-52.

[4] Rao VR, Raju SS, Sarma VU, Sabine F, Babu KH, Babu KS, Rao JM. Simultaneous determination of bioactive compounds in Piper nigrum L. and a species comparison study using HPLC-PDA. Nat Prod Res. 2011 Aug;25(13):1288-94.

[5] Martins, C.A., Leyhausen, G., Volk, J., Geurtsen, W., Curcumin in Combination with Piperine Suppresses Osteoclastogenesis In Vitro. J Endod. 2015 Oct;41(10):1638-45

[6] Srinivasan K. Black pepper and its pungent principle-piperine: a review of diverse physiological effects. Crit Rev Food Sci Nutr. 2007;47(8):735-48.

[7] Scutellaria baicalensis, Examine.com, available online at https://examine.com/supplements/scutellaria-baicalensis/ [Accessed October 26, 2017]

[8] Srinivas, N.R., Baicalin, an emerging multi-therapeutic agent: pharmacodynamics, pharmacokinetics, and considerations from drug development perspectives. Xenobiotica. 2010 May;40(5):357-67

[9] Lan, J., et al., Meta-analysis of the effect and safety of berberine in the treatment of type 2 diabetes mellitus, hyperlipemia and hypertension. J Ethnopharmacol. 2015 Feb 23;161:69-81

[10] Liu, Y., Oxidative demethylation and subsequent glucuronidation are the major metabolic pathways of berberine in rats. J Pharm Sci. 2009 Nov;98(11):4391-401.

[11] Woodbury, A., Yu, S.P., Wei, L., García, P., Neuro-Modulating Effects of Honokiol: A Review. Front Neurol. 2013; 4: 130.

[12] Arora, S., et al., Honokiol: a novel natural agent for cancer prevention and therapy. Curr Mol Med. 2012 Dec; 12(10): 1244–1252.

[13] Chapter 13: Turmeric, the Golden Spice, Herbal Medicine: Biomolecular and Clinical Aspects. 2nd edition. Sahdeo Prasad and Bharat B. Aggarwal., Benzie IFF, Wachtel-Galor S, editors.

Boca Raton (FL): CRC Press/Taylor & Francis; 2011.

[14] Gupta, S.C., Patchva, S., Aggarwa, B.B., Therapeutic Roles of Curcumin: Lessons Learned from Clinical Trials. AAPS J. 2013 Jan; 15(1): 195–218.

[15]  Shoba, G., et al., Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med. 1998 May;64(4):353-6.

[16] Han HK. The effects of black pepper on the intestinal absorption and hepatic metabolism of drugs. Expert Opin Drug Metab Toxicol. 2011 Jun;7(6):721-9.

[17] Bajad, S., et al., Piperine inhibits gastric emptying and gastrointestinal transit in rats and mice. Planta Med. 2001 Mar;67(2):176-9.

[18] Piperine, Examine.com, available online at https://examine.com/supplements/black-pepper/ [Accessed October 26, 2017]

[19] Piyachaturawat, P., Glinsukon, T., Toskulkao, C., Acute and subacute toxicity of piperine in mice, rats and hamsters. Toxicol Lett. 1983 May;16(3-4):351-9.

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