Astonishing Benefits of Piperine

“Black pepper has been used for many purposes in the past. Native to South India along the Malabar Coast, cultivated through the tropics and found on virtually every restaurant table and in every family kitchen cupboard.”

By: Pallavi Vathiar. Practicing Clinical Nutritionist, Mumbai.

Email: fihealthie@gmail.com

Herbs and spices have the delightful flavor and health benefits of it have made them indispensable in food processing industry. Among the spices, pepper has occupied a supreme and unique position and rightly nicknamed as the King of Spices, being the most extensively consumed spice worldwide (1).

Piperine is well reported in Indian medicine for the treatment of diseases such as rheumatoid arthritis, cancer, asthma, inflammation, anxiety, depression, and infectious diseases.

History of Piperine

Pure Piperine Xtals

The history of black pepper also known as Piper Nigerium can be traced as far back as 1200 BC and in India’s 5,000-year-old system of Ayurveda has been using it as a medicine.

Piperine, as the most abundant alkaloid in pepper, was 1st isolated from the extract of pepper. Piperine was discovered in 1819 by Hans Christian Ørsted, who isolated it from the fruits of Piper nigrum, the source plant of both black and white pepper. 

It was extracted as a yellow crystalline compound with a melting point of 128 to 130 °C. The chemical structure of piperine was later identified as piperoylpiperidine, with the chemical formula of C17H19NO3.

Piperine was found to be a very weak base, which upon acid or alkali hydrolysis decomposes to a volatile basic piperine, known as piperidine (C5H11N), and piperic acid (C12H10O4) (2).

Piperine from Pepper:

Black Pepper and Piperine Powder

Black and white peppers are composed of 2 main components: Volatile (essential) oil and Pungent compounds, these are responsible for their aroma and pungency respectively.

Pepper oil, which is normally extracted by steam distillation of dried pepper corns, does not contain pungent compounds and only represents aromatic and odorous constituents. Because of its aroma, pepper oil is highly valued in the fragrance industry as well as the flavor industries (3).

However, pepper is highly esteemed as a condiment for its pungent and nonvolatile compounds which are found in the oleoresin of pepper. Oleoresin is the solvent‐extractable portion of pepper which constitutes around 6% to 13% of black pepper and possesses odor, flavor, and pungency (4).

Therapeutic Effects

In ancient Chinese and Indian medicine, black pepper was used as a natural medicinal agent for the treatment and alleviation of pain, chills, rheumatism, influenza, muscular pains, chills, and fevers.

In tea form, black pepper was also credited for relieving migraine headaches, strep throat, poor digestion, insomnia and even coma (5).

Anti-oxidant Activity

Piperine has liver‐protective activity due to its antioxidant activity. Experiments have shown that piperine reduces both in vitro and in vivo lipid per-oxidation and prevents the decrease of glutathione (GSH) and total thiols (6).

Orally administered piperine can have a stimulating effect on the digestive enzymes of pancreas and intestines; and it also increases bile acid secretion (7).

Piperine has anticancer and anti-tumor activity. The anti-tumor activity of piperine can be due to its immuno-modulatory properties, including the activation of cellular and humoral immune responses (8).

Anti-inflammatory Activity

Asthma is an inflammatory disease caused by irregular immune responses in the airway mucosa, with symptoms such as inflammation in the airway. Piperine has shown deep inhibitory effects on airway inflammation of asthma due to suppression of Th2 cytokines, immunoglobulin E, eosinophil CCR3 and enhanced TGF‐b gene expression in the lungs. Therefore, it can be considered as a possible immunomodulator (9).

Anti-allergic Activity

Urmila Aswar et al. reported that piperine can be used as an anti-allergic agent. It presents the allergic response through mast cell stabilization through the inhibition of released mediators such as interleukin-6, interleukin-1b, immunoglobulin-E, and histamine. The study on ovalbumin-induced allergic rhinitis, suggests that piperine can be used as a xenobiotic agent for clinical use (10).

Effect of Piperine on Brain Cells

A study by Wattanathorn et al. states that piperine improved memory impairment and protects against the cognitive neuro-degeneration. The mechanism was associated with an increase in the neuronal density and inhibition of acetyl-cholinesterase enzyme in the hippocampus region of the brain on Alzheimer’s disease, neuro-degeneration, and memory impairment individuals (11,12).

A compound named picaridin which is a synthetic analogue of piperine is a highly effective insect repellent and is used as a substitute for DEET (N,N-Di ethyl-meta-toluamide), which can cause both skin irritation and occasional (rare) nerve damage. Picaridin is now widely available in popular insect repellents (13).

Role of Piperine in Traditional Medicine

Long Pepper and Black Pepper

Both black pepper (Piper nigrum) and long pepper (Piper longum), important sources of piperine, is being used in large amounts in traditional pharmacopoeia (Ayurveda, Siddha, Unani, and Tibetan) even today and is used as a bioenhancer in traditional as well as modern medicine.

In Ayurveda, black pepper is used in the treatment of cough, cold, and sore throat. While in other systems of medicines, the peppercorns are used for the treatment of indigestion, plethora, insomnia, and other diseases.

Ayurveda System of Medicine

In Ayurveda, the concept of bioavailability enhancers/biopotentiators is called “yogavahi.”

The role of yogavahi in Ayurveda is described as the agent used to enhance bioavailability, tissue distribution, and efficacy of drugs having poor bioavailability and decreasing adverse effects.

Vladimir Badmaev and Muhammed Majeed et al. reported that “Trikatu” an Ayurvedic formulation containing Black pepper, Long pepper and Ginger is used to enhance the bio-availability of many nutrients including ingredients of vasaka leaves, vasicine, sulfadiazine on human volunteers. The study reveals that piperine an active constituent of black pepper and long pepper, plays a significant role in enhancing the bioavailability of the drug (14).

NameIngredientsMedicinal Use
Curcumin
and
Piperine
Turmeric Powder (395 mg), Natural curcumin extract (400 mg) and piperine (5 mg)Anti-Inflammatory, Powerful anti oxidant, prescribed as a
dietary supplement.
Example

Unani System of Medicine

Filfil siyah (black pepper; piper nigrum), is an integral part of the unani system of medicine, and is used to treat various different ailments.

NameIngredientsMedicinal Use
Habbe Gule AakhZanjabeel Zingiber officinalis, FilfilSiyah Pipernigrum Linn., GuleMadar Calotropis gigantea Linn., Barge Bans Bambusa arundinacea Willd.Backache,
Cervical, Spondylosis,
Anti inflammatory and analgesic activity
Example

Siddha System of Medicine

Classical Siddha preparations that contain black pepper as a medicine are Amukkara Choornam, Nilavembu Kudineer, and Trikaduku Choornam, having pepper species as active constituents (14).

NameIngredientsMedicinal Use
Trikadagu ChoornamChukku (dried ginger), Milagu (pepper) and Thippili (long pepper)Analgesic and Anti inflammatory properties. Digestive, carminative and used in treatment of Indigestion,
gas trouble, constipation, bloating.
Example

Preservation

The piperine in pepper is best preserved when the spice is kept in a cool, dry place, out of direct exposure to sunlight. Whole peppercorns keep their spicy flavour better than ground pepper, which makes pepper grinders valuable in terms of deriving the maximum flavor from this spice. To get the maximum pepper flavor, it is best to grind it right onto food.

Consume it Rightly

Black pepper was listed by FDA (Food and Drug Administration) as a herb, also recognized as safer agents for its use as a spice.

Piperine can be given at a dose of 15-20 mg/person/day in divided dose, which seems to be extremely less than the Lethal Dose (LD50) which is 5 mg/kg of the human dose.

There is no harm including it in your diet, but make sure to consume it in moderation. Do not have more than 1-2 teaspoon of black pepper every day. Having it in excess can have multiple side effects.

Conclusion

Higher dose, poor absorption, low bioavailability and poor patient compliance are the major drawbacks of drugs. As black pepper consists of approximately 5-9% piperine as an active chemical constituent. When combined as piperine with the medication, side effects and toxicity of drugs can be reduced.

Reference:

  1. https://onlinelibrary.wiley.com/doi/full/10.1111/1541-4337.12246
  2. https://onlinelibrary.wiley.com/doi/full/10.1111/1541-4337.12246
  3. Agronomy and Economy of Black Pepper and Cardamom: The” King” and” Queen” of Spices.
  4. https://books.google.co.in/books?id=1pBG99NCLM8C&lpg=PP1&ots=2opTwrXDHs&lr&pg=PP1#v=onepage&q&f=false
  5. https://catbull.com/alamut/Bibliothek/Chemistry_of_Spices.pdf
  6. https://pubmed.ncbi.nlm.nih.gov/8255933/
  7. https://pubmed.ncbi.nlm.nih.gov/19075623/
  8. https://pubmed.ncbi.nlm.nih.gov/15013199/
  9. https://arthritis-research.biomedcentral.com/articles/10.1186/ar2662
  10. https://www.tandfonline.com/doi/full/10.3109/13880209.2014.982299
  11. https://www.sciencedirect.com/science/article/pii/S0278691509005912?via%3Dihub
  12. https://link.springer.com/article/10.1007/s11064-012-0799-9
  13. http://www.medicinehunter.com/marvels-black-pepper
  14. https://www.sciencedirect.com/science/article/abs/pii/0010782482901378

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