Clinical Studies
Piperine is an alkaloid that is found in black pepper and related plants. Piperine enhances the bioavailability of other nutritional substances such as beta-carotene, curcumin, selenium, pyridoxine (vitamin B6), glucose and amino acids. It may be beneficial as an anti-inflammatory substance, to improve digestion, in pain complaints, asthma, serotonin production (mood enhancing and pain relieving neurotransmitter) and in stomach ulceration.
Published Clinical Studiesclin
Protective action of piperine against experimental gastric ulcer.1
Bai YF, Xu H.
Inner Mongol Institute of Traditional Chinese-Mongol Medicine, Huhehaote 010020, China.
AIM: To study the effects of piperine (Pip) on several experimental gastric ulcers in rats and mice. METHODS: The gastric mucosa damage was induced by stress, indometacin, HCl, and pyloric ligation in rats or mice. The number of gastric ulcers, the volume and acidity of gastric juices, and pepsin A activity were detected. RESULTS: Pip 25, 50, 100 mg/kg ig protected animals from gastric ulceration in a dose-dependent manner. The inhibitory rates were 16.9%, 36.0%, and 48.3% in stress ulcers; 4.4%, 51.1%, and 64.4% in indometacin ulcers; 19.2%, 41.5%, and 59.6% in HCl ulcers; 4.8%, 11.9%, and 26.2% in pyloric ligation ulcers, respectively; Pip inhibited the volume of gastric juice, gastric acidity, and pepsin A activity.
CONCLUSION: Pip has the protective effects against gastric ulceration.
Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers.2
Shoba G, Joy D, Joseph T, Majeed M, Rajendran R, Srinivas PS.
Department of Pharmacology, St. John's Medical College, Bangalore, India.
The medicinal properties of curcumin obtained from Curcuma longa L. cannot be utilised because of poor bioavailability due to its rapid metabolism in the liver and intestinal wall. In this study, the effect of combining piperine, a known inhibitor of hepatic and intestinal glucuronidation, was evaluated on the bioavailability of curcumin in rats and healthy human volunteers. When curcumin was given alone, in the dose 2 g/kg to rats, moderate serum concentrations were achieved over a period of 4 h. Concomitant administration of piperine 20 mg/kg increased the serum concentration of curcumin for a short period of 1-2 h post drug. Time to maximum was significantly increased (P < 0.02) while elimination half life and clearance significantly decreased (P < 0.02), and the bioavailability was increased by 154%. On the other hand in humans after a dose of 2 g curcumin alone, serum levels were either undetectable or very low. Concomitant administration of piperine 20 mg produced much higher concentrations from 0.25 to 1 h post drug (P < 0.01 at 0.25 and 0.5 h; P < 0.001 at 1 h), the increase in bioavailability was 2000%. The study shows that in the dosages used, piperine enhances the serum concentration, extent of absorption and bioavailability of curcumin in both rats and humans with no adverse effects.
Publication Types:
PMID: 9619120 [PubMed - indexed for MEDLINE]
3
Piperine derived from black pepper increases the plasma levels of coenzyme q10 following oral supplementation.
Badmaev V V, Majeed M, Prakash L.
Sabinsa Corporation, Piscataway, NJ, USA
An extract from the fruits of black pepper consisting of a minimum of 98% pure piperine was evaluated in a clinical study using a double-blind design. The relative bioavailability of 90 mg and 120 mg of coenzyme Q10 administered in a single-dose experiment or in separate experiments for 14 and 21 days with placebo or with 5 mg of piperine was determined by comparing measured changes in plasma concentration. The inter-subject variability was minimized by limiting the selection of individuals to healthy adult male volunteers with (presupplementation) fasting coenzyme Q10 values between 0.30 and 0.60 mg/L. The results of the single-dose study and the 14-day study indicate smaller, but not significant, increases in plasma concentrations of coenzyme Q10 in the control group compared with the group receiving coenzyme Q10 with a supplement of piperine. Supplementation of 120 mg coenzyme Q10 with piperine for 21 days produced a statistically significant (p = 0.0348), approximately 30% greater, area under the plasma curve than was observed during supplementation with coenzyme Q10 plus placebo. It is postulated that the bioenhancing mechanism of piperine to increase plasma levels of supplemental coenzyme Q10 is nonspecific and possibly based on its description in the literature as a thermonutrient.
PMID: 10715596 [PubMed - as supplied by publisher]
Antidiarrhoeal activity of piperine in mice.4
Bajad S, Bedi KL, Singla AK, Johri RK.
Peppers are common food ingredients used worldwide. They are also added in traditional antidiarrhoeal formulations of different herbs. Piperine (1) is an alkaloidal constituent of black and long peppers recently established as a bioavailability enhancer of drugs and other substances. As a part of efforts to study its effects on the gastrointestinal tract, the experiments were performed to determine the rationale, if any, for its use in traditional antidiarrhoeal formulations. Antidiarrhoeal activity of 1 against castor oil, MgSO4 and arachidonic acid was studied in mice. It significantly inhibited diarrhoea produced by these cathartics at 8 and 32 mg/kg p.o. dose. Inhibition of castor oil induced enteropooling by 1 suggests its inhibitory effect on prostaglandins. The results validate the rationale for its use in traditional antidiarrhoeal formulations.
Publication Types:
PMID: 11345706 [PubMed - indexed for MEDLINE]
5
Cytoprotective effect of piperine against benzo[a]pyrene induced lung cancer with reference to lipid peroxidation and antioxidant system in Swiss albino mice.
Selvendiran K, Singh JP, Krishnan KB, Sakthisekaran D.
Department of Medical Biochemistry, University of Madras, Taramani Campus, Chennai 600 113, India.
The cytoprotective effect of piperine on benzo[a]pyrene (B[a]P) induced experimental lung cancer was investigated in male Swiss albino mice. Oral administration of piperine (100 mg/kg body wt.) effectively suppressed lung cancer initiated with B[a]P as revealed by the decrease in the extent of lipid peroxidation with concomitant increase in the activities of enzymatic antioxidants (superoxide dismutase, catalase and glutathione peroxidase) and non-enzymatic antioxidant (reduced glutathione, vitamin E and vitamin C) levels when compared to lung cancer bearing animals. Our data suggest that piperine may extend its chemopreventive effect by modulating lipid peroxidation and augmenting antioxidant defense system.
PMID: 12628402 [PubMed - in process]
Effect of piperine on the inhibition of lung metastasis induced B16F-10 melanoma cells in mice.6
Pradeep CR, Kuttan G.
Amala Cancer Research Centre, Thrissur, Kerala, India.
The effect of piperine on the inhibition of lung metastasis induced by B16F-10 melanoma cells was studied in C57BL/6 mice. Simultaneous administration of the compound with tumor induction produced a significant reduction (95.2%) in tumor nodule formation. Increased lung collagen hydroxyproline (22.37 microg/mg protein) in the metastasized lungs of the control animals compared to normal animals (0.95 microg/mg protein) was significantly reduced (2.59 microg/mg protein) in the piperine-treated animals. The high amount of uronic acid (355.83 microg/100 mg tissue) in the metastasized control animals was significantly reduced (65 microg/100 mg tissue) in the animals treated with piperine. Lung hexosamine content was also significantly reduced in the piperine-treated animals (0.98 mg/100 mg lyophilized tissue) compared to the untreated tumor-bearing animals (4.2 mg/100 mg lyophilized tissue). The elevated levels of serum sialic acid and serum gamma glutamyl transpeptidase activity in the untreated control animals was significantly reduced in the animals treated with piperine. The piperine-treated animals even survived the experiment (90 days). Histopathology of the lung tissue also correlated with the lifespan of the drug-treated animals. Our results demonstrate the antimetastatic activity of piperine, an alkaloid present in plants such as Piper nigrum and Piper longum.
PMID: 12553376 [PubMed - indexed for MEDLINE]