DOI QR코드

DOI QR Code

Molecular targets of pepper as bioavailability enhancer

  • Published : 2009.12.31

Abstract

Black pepper (family Piperaceae), is called king of spices because it is one of the oldest spice and alone accounts for about 35% of the world's total spice trade. The pepper is used in Ayurvedic medicine for the treatment of various ailments particularly neurological, broncho-pulmonary and gastrointestinal disorders. Pepper has also been reported to have various pharmacological actions but recently, it is highlighted as a bioavailability enhancer. This results in higher plasma concentration of drugs, nutrients, ions and other xenobiotics, rendering them more bioavailable for physiological as well as pharmacological actions in the body. Numerous scientific studies reported that piperine; a main bioactive compound of pepper, is responsible for its bioavailability enhancing property. It's a well known fact that pepper enhances bioavailability by inhibition of microsomal enzyme system but other mechanisms are also responsible to acts as a bioavailability enhancer. The brief overview of the mechanism of action of pepper as well as its applications as bioavailability enhancer is given in the present article.

References

  1. Amarjit S, Rajesh J. (2000) Pharmaceutical compositions containing at least one NSAID having increased bioavailability. Unitd State Patent No. 6017932
  2. Annamalai AR, Manavalan R. (1990) Effects of 'Trikatu' and its individual components and piperine on gastrointestinal tracts: Trikatu-a bioavailable enhancer. Indian Drugs 27, 595-604
  3. Anonymous. (1989) The Wealth of India, Vol. VIII: Ph-Re, pp. 96-115, Publications & information directorate, CSIR, New Delhi
  4. Atal CK, Dubey RK, Singh J. (1985) Biochemical basis of enhanced drug availability by piperine: Evidence that piperine is a potent inhibitor of drug metabolism. J. Pharmacol. Exp. Ther. 232, 258-262
  5. Atal CK, Zutshi U, Rao PG. (1981) Scientific evidence of the role of Ayurvedic herbals on bioavailability of drugs. J. Ethnopharmacol. 4, 229-233 https://doi.org/10.1016/0378-8741(81)90037-4
  6. Badmaev V, Majeed M, Norkus EP. (1999) Piperine, an alkaloid derived from the black pepper increases serum response of Beta-carotene during 14 days of oral Beta-carotene supplementation. Nutr. Res. 19, 381-388 https://doi.org/10.1016/S0271-5317(99)00007-X
  7. Badmaev V, Majeed M, Prakash L. (2000) Piperine derived from the black pepper increases plasma level of Coenzyme $Q_{10}$ following oral supplementation. J. Nutr. Biochem. 11, 109-113 https://doi.org/10.1016/S0955-2863(99)00074-1
  8. Bajad S, Bedi KL, Singla AK, Johri RK. (2001) Antidiarrheal activity of piperine in mice. Planta Med. 67, 284-287 https://doi.org/10.1055/s-2001-11999
  9. Bano G, Amla V, Raina RK, Zutshi U, Chopra CL. (1978) The effect of piperine on the pharmacokinetics of phenytoin on healthy volunteers. Plannta Med. 53, 568-569 https://doi.org/10.1055/s-2006-962814
  10. Bano G, Raina RK, Zutshi U, Bedi KL, Johri RK, Sharma SC. (1991) Effect of piperine on bioavailability and pharmacokinetics of propranolol and theophylline in healthy volunteers. Eur. J. Clin. Pharmacol. 41, 615-617 https://doi.org/10.1007/BF00314996
  11. Bhardwaj RK, Hartmut G, Laurent B, Ulrich K, Suresh KG, Martin FF. (2002) Piperine, a major constituent of black pepper, inhibits human pglycoprotein and CYP3A4. J. Pharmacol. Exp. Ther. 302, 645-650 https://doi.org/10.1124/jpet.102.034728
  12. Dalvi PR, Dalvi PS. (1991) Differences in the effects of piperine and piperonyl butoxide on hepatic drugmetabolizing system in rats. Drug Chem. Toxicol. 14, 219-229 https://doi.org/10.3109/01480549109017878
  13. Hiwale AR, Dhuley JN, Naik SR. (2002) Effect of coadministration of piperine on pharmacokinetics of beta-lactam antibiotics in rats. Indian J. Exp. Biol. 40, 277-281
  14. Inshad AK, Zahid MM, Ashwani K, Vijeshwar V, Ghulam NQ. (2006) Piperine, a Phytochemical potentiator of Ciprofloxacin against Staphylococcus aureus. Antimicrob. Agents. Ch. 50, 810-812 https://doi.org/10.1128/AAC.50.2.810-812.2006
  15. Johri RK, Thusu N, Khajuria A, Zutshi U. (1992) Piperinemediated changes in the permeability of rat intestinal epithelial cells: The status of gamma-glutamyl transpeptidase activity, uptake of amino acids and lipid peroxidation. Biochem. Pharmacol. 43, 1401-1407 https://doi.org/10.1016/0006-2952(92)90195-O
  16. Johri RK, Zutshi U. (1992) An Ayurvedic formulation 'Trikatu' and its constituents. J. Ethnopharmacol. 37, 85-91 https://doi.org/10.1016/0378-8741(92)90067-2
  17. Karan RS, Bhargava VK, Garg SK. (1998) Effect of Trikatu (piperine) on the pharmacokinetic profile of isoniazid in rabbits. Indian J. Pharmacol. 30, 254-256
  18. Kawada T, Sakabe S, Watanable T, Jamamoto M, Iwai K. (1998) Some pungent principles of species cause the adrenal medulla to secrete catecholamine in anaesthetized rats. Exp. Biol. Med. 188, 229-233
  19. Khajuria A, Thusu N. (2002) Piperine modulates permeability characteristic of intestine by inducing alterations in membrane dynamics: Influence on brush border membrane fluidity, ultrastructure and enzyme kinetics. Phytomedicine 9, 224-231 https://doi.org/10.1078/0944-7113-00114
  20. Khajuria A, Zutshi U, Bedi KL (1998) Permeability characteristics of piperine on oral absorption-an active alkaloid from peppers and a bioavailability enhancer. Indian J. Exp. Biol. 36, 46-50
  21. Lala LG, D'Mello PM, Naik SR. (2004) Pharmacokinetic and phamcodynamic studies on interaction of Trikatu with diclophenac sodium. J. Ethnopharmacol. 91, 277-280 https://doi.org/10.1016/j.jep.2003.12.027
  22. Lambert JD, Hong J, Kim DH, Mishin VM, Yang CS. (2004) Piperine enhances the bioavailability of the tea polyphenol(-)-epigallocatechin-3-gallate in mice. J. Nutr. 134, 1948-1952 https://doi.org/10.1093/jn/134.8.1948
  23. Majeed M, Badmaev V, Rajendran R. (1998) Use of piperine as a bioavailability enhancer. United state patent No. 5,972,382
  24. Majeed M, Badmaev V, Prakash L. (1999) Bioperine: Nature's Own Thermonutrient and Natural Bioavailability Enhancer, pp. 8114-8121, Nutriscience Publication Inc., New Jersey
  25. Majeed M, Prakash L (2000) The medicinal uses of pepper. International Pepper News. XXV, 23-31
  26. Margriet WP, Kristel D, Annemiek J, Sonia BP, Angelo T. (2006) Metabolic effects of spices, teas and caffeine. Physiol. Behav. 89, 85-91 https://doi.org/10.1016/j.physbeh.2006.01.027
  27. Patel K, Srinivasan K. (2000) Influence of digestive spices and their active principles on pancreatic digestive enzymes in albino rats. Nahung. 44, 42-46 https://doi.org/10.1002/(SICI)1521-3803(20000101)44:1<42::AID-FOOD42>3.0.CO;2-D
  28. Raj KPS, Nagarsheth HK. (1978) Pepper. Indian Drugs 16, 199-203
  29. Raffaele C, Angelo A., Francesco B, Alessandra R, Lidia S, Aldo P, Francesco C, Nicola M. (2002) Effect of piperine, the active ingredient of black pepper, on intestinal secretion in mice. Life Sci. 71, 2311-2317 https://doi.org/10.1016/S0024-3205(02)02019-2
  30. Rashmeet KR, Jaswant S. (1991) In vitro and in vivo inhibition of pulmonary cytochrome P450 activities by piperine, a major ingredient of piper species. Indian J. Exp. Biol. 29, 568-573
  31. Russell M. (2003) Piperine multiplies the strength of many supplements and drugs. Delano report
  32. Shobha G, Joy D, Joseph T, Majeed M, Rajendran R, Srivastava N. (1998) Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med. 64, 353-356 https://doi.org/10.1055/s-2006-957450
  33. Singh J, Atal CK, Dubey RK. (1986) Piperine-mediated inhibition of glucuronidation activity in isolated epithelial cells of guinea pig small intestine: evidence that piperine lowers the endogenous UDP-glucuronic acid content. J. Pharmacol. Exp. Ther. 2236, 448-493
  34. Sunila ES, Kuttan G. (2004) Immunodulatory and antitumor activity of Piper longum Linn ad piperine. J. Ethnopharmacol. 90, 339-346 https://doi.org/10.1016/j.jep.2003.10.016
  35. Walker M. (1997) Piperine in Black Pepper: One of newly recognized class of thermonutrients, pp. 31, Health Food Business
  36. Zutshi. (1989) A process for the preparation of pharmaceutical combination with enhanced activity for treatment of tuberculosis and leprosy. Indian Patent No. 1231/Del/89

Cited by

  1. Comparative antioxidant and bioavailability studies of Vitamin C in Phyllanthus emblica Linn. and its combinations with Piper nigrum Linn. and Zingiber officinale Roscoe vol.52, pp.1, 2016, https://doi.org/10.1590/S1984-82502016000100005