What Is BioPerine? Uncovering the Benefits of Black Pepper Extract

Authored by Elliot Reimers, M.S.(C), CISSN, CNC

What Is BioPerine?

Odds are you've seen turmeric supplement labels and thought to yourself, "Hmm, what is BioPerine?" In short, BioPerine® is a patented extract of black pepper fruit that contains an industry-leading 95% piperine content. The ingredient is produced by Sabinsa Corporation, a prestigious nutraceutical manufacturer that specializes in natural plant extracts.

Black pepper (Piper nigrum) has been an emphasis of research in recent years due to its promising bioavailability-enhancing properties. However, black pepper has a host of unrelated health benefits, with numerous scientific studies unveiling its role in biological processes that may reduce the risk of disease, enhance weight loss, promote cardiovascular function, and stimulate digestion [1].

The medicinal chemicals in black pepper are predominantly alkaloids, notably the eponymous piperine (1-piperoyl piperidine) and pipernigramides E, F, and G [2]. The characteristic heat, or "kick," that black pepper and long pepper spices add to food is attributable to piperine, which is also the major active therapeutic compound in plants of the Piperaceae family [3].

The black pepper plant is a flowering vine that bears fruits (peppercorns) containing roughly 2-7.4% piperine by mass. In comparison, BioPerine® black pepper fruit extract is standardized to a minimum 95% piperine by mass. Hence, as little as 5 mg BioPerine® provides as much piperine as 250 mg of most black pepper spices. For reference, 1/4 teaspoon of ground black pepper weighs about 500 mg.

With that in mind, let's take a look at the use of black pepper extract supplements like BioPerine® for human health and how piperine works in the body.

Health Benefits of Black Pepper Fruit (Piper nigrum)

Black pepper is arguably the most popular culinary spice across the globe. Its traditional use as a flavor enhancer in food spans back thousands of years. It has also been used in various traditional medicines, preservatives, and health supplements. In fact, the Materia Medica of traditional medicine describes black pepper (Piper nigrum) as one of the three essential herbs of several prescriptions and natural health remedies.

The following subsections provide deeper insights into the health benefits of black pepper and its principle bioactive compound, piperine.

Black Pepper Extract is a Bioavailability Enhancer

The most profound application of black pepper/piperine in medicine is enhancing the bioavailability and absorption of natural compounds and pharmaceutical drugs. When we ingest chemicals and nutrients orally, they are subjected to first-pass metabolism in the liver. Consequently, enzymes of the liver may deactivate the active compounds before they reach the systemic circulation, thereby decreasing absorption and efficacy.

A noteworthy example is that of curcuminoids from turmeric extract supplements, which are notorious for having poor bioavailability due to extensive first-pass metabolism. Piperine has been shown to greatly increase the absorption of bioactive curcuminoids by inhibiting liver and intestinal enzymes that usually deactivate these compounds [4]. Research has found also that piperine bolsters the absorption of several therapeutic drugs and other phytochemicals, such as caffeine and theobromine, by this very mechanism [5, 6].

For the science nerds out there, piperine interferes specifically with CYP3A4-dependent metabolism and glucuronidation by inhibiting UDP-glucuronyltransferase. It also strongly inhibits the aryl hydrocarbon hydroxylase enzyme, P-glycoprotein efflux transporters, and multi-drug resistance proteins (MRPs) in the intestine [7, 8]. The use of black pepper extract supplements may also improve bioavailability and absorption of various nutrients and drugs partly via piperine's modulatory effect on intestinal brush border permeability [9].

Effect of Piperine on Heart Health

Clinical research on BioPerine® has made it clear that black pepper benefits cardiovascular function by increasing the uptake of CoQ10 and iron supplements as much as 30% [10, 11]. Also, piperine-related alkaloids in black pepper have been shown to inhibit inducible nitric oxide synthase (iNOS) [12]. Excess activity of this enzyme can increase the risk of heart disease and atherosclerosis.

In addition, piperine decreases intestinal absorption of dietary cholesterol by internalizing cholesterol transporters, improving blood lipid profiles [13]. In conjunction with the existing body of evidence, this data reveals the specificity of piperine and how black pepper can selectively increase the absorption of some chemicals while doing the opposite for others.

Black Pepper for Weight Loss: Thermogenic Benefits of Piperine

Another intriguing health benefit of black pepper is that it may improve body composition by regulating fat cell differentiation at the genetic level. Recent data indicates that piperine can repress transcription factors that induce adipogenesis — the creation of new fat cells in the body — and increase lipolysis by modifying a subset of histone proteins in the cell nucleus [14].

In simpler terms, piperine alters gene expression in a manner that blunts fat storage and promotes fat breakdown. Intuitively, these are desirable benefits for weight loss and metabolic function.

Black Pepper Extract as a Natural Anti-Diarrheal and Digestive Aid

For certain nutrients and compounds, piperine boasts properties that directly contrast with its bioavailability enhancing properties. In vitro and in vivo data suggests that piperine reduces intestinal cholesterol uptake, delays gastric emptying rate, and blunts chloride secretion in the small intestine [1315, 16]. These mechanisms are likely responsible for the anti-diarrheal and aforementioned cardiovascular benefits of black pepper.

Moreover, piperine has stimulating actions on the production of digestive enzymes and bile acids that break down nutrients in food. Multiple studies demonstrate that a single dose of piperine (5 -20 mg) can elevate trypsin, chymotrypsin, pancreatic lipase, and pancreatic amylase activity by 30-100% more than controls [17, 18].

Piperine May Reduce the Risk of Chronic Disease

The potential role of black pepper as a prophylactic functional food remains a topic of emphasis among researchers. Numerous studies show piperine may protect against chronic diseases of the nervous system, such as Alzheimer's disease, as well as the liver and gastrointestinal tract [19].

Better yet, piperine has demonstrable anti-tumor and anti-cancer properties and has even been investigated in preclinical studies as a natural treatment for breast cancer [20]. 

A fun side note for science lovers: piperine was recently found to neutralize the lethal effects of snake venom in rodents [21]. Pretty neat, eh?

Side Effects of Black Pepper

Interestingly, it was initially thought that black pepper was toxic to the body because piperine has a chemical structure that resembles known carcinogens widely distributed in spices and plant oils, including safrole, methyleugenol, and estragole [22]. Later studies showed that neither black pepper nor piperine causes adverse effects at doses up to 250 times greater than normal human intake [23].

Clinical studies also fail to demonstrate any significant side effects of black pepper extracts such as BioPerine®. However, very large doses of piperine (e.g. ≥0.40 mg/kg body weight per day) may reduce circulating levels of thyroid hormones and testosterone (in men) and complicate blood glucose balance in healthy individuals [24, 25].

As with any dietary supplement, it's wise to consult with a doctor before taking BioPerine® or other black pepper extracts if you have any pre-existing medical conditions or are taking prescriptions.

Where to Find BioPerine Supplements

Now that you're more familiar with black pepper and the science behind its primary chemical constituent (piperine), you might be wondering where to find BioPerine®. Thankfully, you don't have to look too far as BioPerine® is now a ubiquitous ingredient in dietary supplements. Piperine's multifunctional benefits and applications as a bioenhancer make it a versatile complement to many formulas.

Without question, the most common products containing BioPerine® are turmeric supplements, including Transparent Labs Curcumin C3. You can also find BioPerine in PreSeries LEAN Pre-Workout and StrengthSeries Creatine HMB, which are designed for athletes, gym-goers, and bodybuilders striving to cut body fat and perform at peak capacity. The BioPerine® in these formulas helps ensure optimal absorption and duration of action of other active ingredients.

 

 

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