Piperine

Background

Piperine, the major bio-active component of pepper, also known by its trademarked name as Bioperine, is an alkaloid with a remarkably broad spectrum of therapeutic activities but imparts pungency and biting taste to it. [1]Being a constituent of some nootropic stacks, piperine works to intensify the effects of other smart drugs while also offering independent cognitive enhancement benefits. It is slightly soluble in water but highly soluble in alcohol, chloroform and ether. The Danish chemist Hans Christian Orsted first isolated piperine from black pepper (Piper nigrum) in 1819.

Benefits

Piperine has numerous established health effects and beneficial therapeutic properties and has a long history of use in some types of traditional medicine. The most important benefit of Piperine is known as ‘bio enhancement’ that improves the absorption of nutrients from the intestines and the bioavailability increased 2000% when combining piperine with curcumin.[2]
There are definitely a number of varied nutrients and materials that Piperine may be helpful at improving the absorption of, but it has been studied and shown to help with vitamin C, selenium, beta-carotene, vitamin A, vitamin B-6, and CoQ10 (coenzyme Q 10). Some common health benefits of piperine include –

  • Increase the absorption of nutrients [6]
  • Enhance the bioavailability of key nutrients [7]
  • Improve the levels and activity of the neurotransmitters Serotonin and Dopamine within the brain [8]
  • Enhance cognitive function [9]
  • Increase motivation [10]
  • Boost memory function [11]
  • Improve mood [12]
  • People report it heightens attention and reasoning skills
  • People also report it enhances focus

Piperine may also have immune-suppressing, tumor-inhibiting and antidepressant effects. Scientists came to a conclusion after many years that Piperine or Bioperine can be used by people who have chronic arthritis. It can enhance the body growth and help increase general feelings of well-being

How it works

Piperine has been known for changing metabolism of various drugs and supplements, most notably increasing curcumin bioavailability by 2000%. It influences metabolism by both intestinal absorption as well as down-regulating or inhibiting phase II detoxification enzymes and the glucuronidation process in the liver.  Piperine may also contribute to increase absorption by slowing intestinal transit rate and thus prolonging the time said compounds are exposed to the potential uptake.[3]
Piperine derivatives may be able to modulate the activity of several targets related to neurological disorders, including epilepsy, Parkinson’s disease, depression and pain related disorders. Moreover, the efflux pump inhibitory ability of piperine and its analogues tackles important drug resistance mechanisms and may improve the clinical efficacy of antibiotic and anticancer drugs.[4]
Piperine has been found to modify the rate of glucuronidation by lowering the endogenous UDP-glucuronic acid content and also by inhibiting the transferase activity. Piperine has also been found to inhibit UDP-glucose dehydrogenase (UDP-GDH) activity in both liver and intestine via non-competitive inhibition.[4]

Considerations

As there are very less data regarding the ingredients available in piperine, very few people can be sure about the side effects of the piperine. However, some people reported minor gastrointestinal tract disorder after misusing piperine. Still, you are suggested not to take this supplement at the same time as any prescription medications, certainly not until getting it cleared by a doctor or qualified medical professional.

Recommendations

The usual recommended dosage of piperine is 5-15 mg/day. Though it is absorbed quickly and well from the digestive tract, effects on absorption of other substances begin around 15 minutes after dosing and last for an hour or two. Therefore, the most reliable method for ensuring piperine’s effectiveness is to take a piperine dose about half an hour before taking the coordinated substance whose bioavailability you want to enhance.

Sources