Piperine by Ray Sahelian, M.D. Piperine health benefit

Dried, ground pepper is one of the most common spices in European cuisine and its descendants, having been known and prized since antiquity for both its flavor and its use as a medicine. The spiciness of black pepper is due to the chemical piperine. Bioperine is a standardized extract of piperine. Piperine may have antioxidant, anti-inflammatory, anti-tumor potential.

Source Naturals Bioperine 10 mg
Black Pepper fruit extract with 95 percent piperine

Bioperine is a pure form of piperine, derived from the fruits of black pepper.

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Piperine and toxins
In mice, a significant suppression in the micronuclei formation induced by benzo(a)pyrene and cyclophosphamide was reduced following oral administration of piperine.

Piperine for mood support
Antidepressant like effects of piperine in chronic mild stress treated mice and its possible mechanisms.
Life Sci. 2007 Mar 20;80(15):1373-81. Laboratory for Brain and Mind, Institute of Neuroinformatics, Dalian University of Technology, Dalian, 116023,China.
In this study, we investigated the antidepressant effect of piperine in mice exposed to chronic mild stress procedure. Repeated administration of piperine for 14 days at the doses of 2.5, 5 and 10 mg/kg reversed the stress -induced changes in sucrose consumption, plasma corticosterone level and open field activity. Furthermore, the decreased proliferation of hippocampal progenitor cells was ameliorated and the level of brain-derived neurotrophic factor in hippocampus of CMS stressed mice was up-regulated by piperine treatment in the same time course. In summary, up-regulation of the progenitor cell proliferation of hippocampus and cytoprotective activity might be mechanisms involved in the antidepressant like effect of piperine.

Piperine as antioxidant
Efficacy of piperine, an alkaloidal constituent from Piper nigrum on erythrocyte antioxidant status in high fat diet and antithyroid drug induced hyperlipidemic rats.
Cell Biochem Funct. 2006 Nov-Dec;24(6):491-8. Department of Biochemistry, Annamalai University, Annamalainagar-608 002, Tamilnadu, India.
The main aim of this study was to investigate the effect of piperine on erythrocyte antioxidant status in high fat diet (HFD) and antithyroid drug induced hyperlipidemic rats. Male Wistar rats were divided into eight groups. The first four groups were fed a control diet and in addition were given respectively 1% carboxymethyl cellulose (CMC); 10 mg/kg body weight carbimazole (CM); 10 mg CM + 40 mg/kg body weight piperine and 10 mg CM + 2 mg/kg body weight atorvastatin. A similar pattern was followed for the next four groups except that they were all fed HFD instead of the control diet. Erythrocyte osmotic fragility, total cholesterol, phospholipids, lipid peroxidation products, enzymic and non-enzymic antioxidant status were studied in all experimental groups. Significantly increased osmotic fragility, total cholesterol/phospholipid ratio, thiobarbituric acid reactive substances and lipid hydroperoxides were observed in the plasma and erythrocytes of HFD fed and CM treated rats compared to the control. Superoxide dismutase, catalase, glutathione peroxidase, vitamin E and reduced glutathione in erythrocytes and vitamin C in the plasma were also significantly lowered in HFD fed, antithyroid drug treated rats compared to control animals. Concurrent piperine supplementation along with HFD and antithyroid drug administration normalized erythrocyte osmotic fragility, reduced lipid peroxidation, and improved the enzymic and non-enzymic antioxidant status compared to those rats that did not receive piperine. Thus, our results indicate that piperine supplementation markedly protects erythrocytes from oxidative stress by improving the antioxidant status in HFD fed antithyroid drug treated rats.

Piperine and Drug Interactions
Piperine from black (Piper nigrum Linn) and long (P. longum Linn) peppers increased the AUC of phenytoin, propranolol and theophylline in healthy volunteers and plasma concentrations of rifamipicin (rifampin) in patients with pulmonary tuberculosis.

Piperine side effects
Not enough human studies have been done to determine the side effects of chronic supplementation with piperine. For the time being, it is a good idea to take 2 days off a week, and one full week off each month from the use of a piperine supplement. It is quite likely that the small amounts of piperine could provide health benefits while larger amounts could be toxic or damaging to the liver or other organs.

Piperine Research

Studies on the chemical constituents from herb of Rhodobryum roseum
Zhongguo Zhong Yao Za Zhi. 2005 Jun;30(12):895-7.
To study the chemical constituents from herb of Rhodobryum roseum. The compounds were isolated by column chromatography, and identified by IR, NMR data. Eight compounds were isolated and identified. They are piperine, caffeic acid methyl ester, uracil glucoside, ursolic acid, 5alpha, 8alpha-epidioxy-methylcholesta-6, 22-dien-3beta-ol, 5alpha, 8alpha-epidioxy-methylcholesta-6,9, 22-trien-3beta-ol, beta-sitosterol and daucosterol.

Piperine: researchers discover new flavor in an ancient spice.
Trends Pharmacol Sci. 2005 Sep;26(9):437-9.
Studies with animals that are deficient in the vanilloid (capsaicin) receptor TRPV1 have confirmed the pivotal role that TRPV1 has in the development of post-inflammatory hyperalgesia, and enhanced TRPV1 expression has been described in various human disorders. Natural products have provided several lead structures for the development of vanilloid ligands. A recent study shows that piperine, the irritant principle in black pepper, is more efficient than capsaicin in the desensitization of human TRPV1, which suggests that this pharmacological aspect of vanilloids can be dissociated from its potency. This finding raises the intriguing possibility that piperine can be used as a chemical template for the design of improved TRPV1 agonists.

Immunomodulatory and antitumor activity of Piper longum Linn. and piperine.
J Ethnopharmacol. 2004 Feb;90(2-3):339-46.
Alcoholic extract of the fruits of the plant Piper longum and its component piperine was studied for their immunomodulatory and antitumor activity. Alcoholic extract of the fruits was 100% toxic at a concentration of 500 microg/ml to Dalton's lymphoma ascites (DLA) cells and 250 microg/ml to Ehrlich ascites carcinoma (EAC) cells. Piperine was found to be cytotoxic towards DLA and EAC cells at a concentration of 250 microg/ml. Alcoholic extract and piperine was also found to produce cytotoxicity towards L929 cells in culture at a concentration of 100 and 50 microg/ml, respectively. Administration of alcoholic extract of Piper longum (10 mg/dose/animal) as well as piperine (1.14 mg/dose/animal) could inhibit the solid tumor development in mice induced with DLA cells and increase the life span of mice bearing Ehrlich ascites carcinoma tumor to 37.3 and 58.8%, respectively. Administration of Piper longum extract and piperine increased the total WBC count to 142.8 and 138.9%, respectively, in Balb/c mice. The number of plaque forming cells also enhanced significantly by the administration of the extract (100.3%) and piperine (71.4%) on 5th day after immunization. Bone marrow cellularity and alpha-esterase positive cells were also increased by the administration of Piper longum extract and piperine.

Piperine Questions

Q. Is piperine necessary for absorption of chrysin?
   A. We have not come across any research that says piperine is necessary for this purpose.

Q. I am a private practice veterinarian performing a research trial utilizing curcumin in horses for various inflammatory conditions. It is my understanding, that based on prior research, that curcumin bioavailability is compromised and in turn the absorption and therapeutic blood levels are low. I also understand that various research trials are demonstrating the concurrent use of piperine, which enhances the absorption and bioavailability. I am curious if your research supports this as well and if there is any further information that you might have to support this fact.
   A. We have not seen convincing research that indicates piperine is needed for curcumin absorption or bioavailability. Almost all studies with curcumin have not used any piperine, therefore we tend to understand that curcumin works well by itself.

Q. I heard of the benefits in guinea pig skin pigmentation with topical piperine. I'm a researcher in Italy really interested in new experiences for treating this disease, I would like to know if you have experience with piperine also in vitiligo?
   A. I have not studied the role of piperine in vitiligo.