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Lycopene

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Description

What is it?

Lycopene is a non-provitamin A carotenoid that is responsible for the red and pink coloration of certain fruits, such as tomatoes, pink grapefruit, watermelon, papaya, and guava. Lycopene derived from tomato (Solanum lycopersicum) sources has been most widely studied and accounts for significant portions of its dietary intake. (23) Lycopene is most commonly recognized as an antioxidant with roles in preventing oxidative stress across a wide variety of conditions. (6)(34)

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Main uses

Anti-oxidant applications
Cardiometabolic disorders
Infertility and prostatic disorders

Formulations

Form
Bioavailability
Lactolycopene (e.g., Ateronon ® - contains 6% lycopene as Lyc-o-mato ® within whey protein matrix) (24)
Equal increase in bioavailability to tomato paste (24)
Lyc-o-mato® (e.g., Lycored - contains lycopene (6%), β-carotene (0.15%), phytoene and phytofluene (1%) and vitamin E (2%), phospholipids (15%), and phytosterol (0.6%) in oleoresin oil (22)
Equal increase in bioavailability to synthetic lycopene (Lycovit ®) (12)
Equal increase in plasma lycopene between tomato oleoresin, synthetic beadlets, and tomato juice, (21) but higher than raw tomato (2)
Lycovit® (10% water-soluble, synthetic beadlets) (12)(30)
Equal bioavailability of synthetic lycopene to tomato-based lycopene (Lyc-o-mato®) (12)
Redivivo® (10% w/w water soluble beadlet. Composed of synthetic crystalline lycopene (all-trans)) (8)
Doses of 6.5 mg, 15 mg & 30 mg were more bioavailable compared to baseline after 2 months of supplementation (8)

Dosing & administration

Adverse effects

The observed level of safety for lycopene has been described at 75mg per day, though higher concentrations have been ingested without adverse effects. (27) Doses of lycopene as high as 120 mg per day have been ingested without adverse effects in healthy subjects, (9) and have been shown to be safe at this dose after a year of consumption. (7) Rare instances of allergic skin reactions have been reported. (8)

Pharmacokinetics

Absorption

  • Approximately 10-30% of lycopene is absorbed after oral intake. (6)
  • Absorption occurs via passive diffusion in the intestine and by the scavenger receptor class B type I (SR-BI) cholesterol membrane transporter. (17)(31)
  • Uptake is saturable, with less than 6 mg typically absorbed regardless of doses ranging from 10-120mg. (9)

Distribution

  • The SR-BI cholesterol membrane transporter is also located in the liver, adrenals, ovaries, placenta, kidneys, prostate, and brain. (33)
  • Highest concentrations are distributed to the testes, and then sequentially to the adrenals, liver, prostate, breast, pancreas, skin, colon, ovaries, lungs, stomach, kidney, adipose tissues, and cervix, thereafter. (6)

Metabolism

  • Lycopene appears to be metabolized by β-carotene 9′,10′-oxygenase (BCO2). (33)
  • Lycopene may also be metabolized to CO2 via B-oxidation. (25)

Excretion

  • Apo-10′-lycopenoic acid or the reduced to apo-10′-lycopene metabolites are excreted in the urine. (25)
  • Lycopene has a half-life of two to three days. (29)

References

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Böhm, V., & Bitsch, R. (1999). Intestinal absorption of lycopene from different matrices and interactions to other carotenoids, the lipid status, and the antioxidant capacity of human plasma. European Journal of Nutrition, 38(3), 118-125.
Briviba, K., Kulling, S. E., Moseneder, J., Watzl, B., Rechkemmer, G., & Bub, A. (2004). Effects of supplementing a low-carotenoid diet with a tomato extract for 2 weeks on endogenous levels of DNA single strand breaks and immune functions in healthy non-smokers and smokers. Carcinogenesis, 25(12), 2373-2378.
Brown, M. J., Ferruzzi, M. G., Nguyen, M. L., Cooper, D. A., Eldridge, A. L., Schwartz, S. J., & White, W. S. (2004). Carotenoid bioavailability is higher from salads ingested with full-fat than with fat-reduced salad dressings as measured with electrochemical detection. The American Journal of Clinical Nutrition, 80(2), 396-403.
Burton-Freeman, B. M., & Sesso, H. D. (2014). Whole food versus supplement: comparing the clinical evidence of tomato intake and lycopene supplementation on cardiovascular risk factors. Advances in Nutrition, 5(5), 457-485.
Chauhan, K., Sharma, S., Agarwal, N., & Chauhan, B. (2011). Lycopene of tomato fame: Its role in health and disease..International Journal of Pharmaceutical Sciences Review and Research, 10(1), 99-115.
Clark, P. E., Hall, M. C., Borden, L. S., Miller, A. A., Hu, J. J., Lee, W. R., . . . Torti, F. M. (2006). Phase I-II prospective dose-escalating trial of lycopene in patients with biochemical relapse of prostate cancer after definitive local therapy. Urology, 67(6), 1257-1261.
Devaraj, S., Mathur, S., Basu, A., Aung, H. H., Vasu, V. T., Meyers, S., & Jialal, I. (2008). A dose-response study on the effects of purified lycopene supplementation on biomarkers of oxidative stress. Journal of the American College of Nutrition, 27(2), 267-273.
Diwadkar-Navsariwala, V., Novotny, J. A., Gustin, D. M., Sosman, J. A., Rodvold, K. A., Crowell, J. A., . . . Bowen, P. E. (2003). A physiological pharmacokinetic model describing the disposition of lycopene in healthy men. Journal of Lipid Research, 44(10), 1927-1939.
Gajendragadkar, P. R., Hubsch, A., Mäki-Petäjä, K. M., Serg, M., Wilkinson, I. B., & Cheriyan, J. (2014). Effects of oral lycopene supplementation on vascular function in patients with cardiovascular disease and healthy volunteers: A randomised controlled trial. PLoS ONE, 9(6), e99070.
Gärtner, C., Stahl, W., & Sies, H. (1997). Lycopene is more bioavailable from tomato paste than from fresh tomatoes. The American Journal of Clinical Nutrition,66(1), 116-122.
Hoppe, P. P., Krämer, K., Berg, H. V., Steenge, G., & Vliet, T. V. (2003). Synthetic and tomato-based lycopene have identical bioavailability in humans. European Journal of Nutrition, 42(5), 272-278.
Karemore, T., & Motwani, M. (2012). Evaluation of the effect of newer antioxidant lycopene in the treatment of oral submucous fibrosis. Indian Journal of Dental Research, 23(4), 524-528.
Kim, J. Y., Paik, J. K., Kim, O. Y., Park, H. W., Lee, J. H., Jang, Y., & Lee, J. H. (2011). Effects of lycopene supplementation on oxidative stress and markers of endothelial function in healthy men. Atherosclerosis, 215(1), 189-195.
Kumar, A., Bagewadi, A., Keluskar, V., & Singh, M. (2007). Efficacy of lycopene in the management of oral submucous fibrosis. Oral Surgery, Oral Medicine, Oral Pathology, Oral Radiology, and Endodontology, 103(2), 207-213.
Mackinnon, E. S., Rao, A. V., Josse, R. G., & Rao, L. G. (2010). Supplementation with the antioxidant lycopene significantly decreases oxidative stress parameters and the bone resorption marker N-telopeptide of type I collagen in postmenopausal women. Osteoporosis International, 22(4), 1091-1101.
Moussa, M., Landrier, J., Reboul, E., Ghiringhelli, O., Coméra, C., Collet, X., . . . Borel, P. (2008). Lycopene absorption in human intestinal cells and in mice involves scavenger receptor class B type I but not niemann-pick C1-like 1. The Journal of Nutrition, 138(8), 1432-1436.
Neuman, I., Nahum, H., & Ben-Amotz, A. (2000). Reduction of exercise-induced asthma oxidative stress by lycopene, a natural antioxidant. Allergy, 55(12), 1184-1189.
Neyestani, T. R., Shariatzadeh, N., Gharavi, A., Kalayi, A., & Khalaji, N. (2007). Physiological dose of lycopene suppressed oxidative stress and enhanced serum levels of immunoglobulin M in patients with Type 2 diabetes mellitus: A possible role in the prevention of long-term complications. Journal of Endocrinological Investigation, 30(10), 833-838.
Oborna, I., Malickova, K., Fingerova, H., Brezinova, J., Horka, P., Novotny, J., . . . Svobodova, M. (2011). A randomized controlled trial of lycopene treatment on soluble receptor for advanced glycation end products in seminal and blood plasma of normospermic Men. American Journal of Reproductive Immunology, 66(3), 179-184.
Paetau, I., Rao, D., Wiley, E. R., Brown, E. D., & Clevidence, B. A. (1999). Carotenoids in human buccal mucosa cells after 4 wk of supplementation with tomato juice or lycopene supplements. The American Journal of Clinical Nutrition, 70(4), 490-494.
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Richelle, M., Bortlik, K., Liardet, S., Hager, C., Lambelet, P., Baur, M., . . . Offord, E. A. (2002). A food-based formulation provides lycopene with the same bioavailability to humans as that from tomato paste. The Journal of Nutrition, 132(3), 404-408.
Ross, A. B., Vuong, L. T., Ruckle, J., Synal, H. A., Schulze-König, T., Wertz, K., . . . Williamson, G. (2011). Lycopene bioavailability and metabolism in humans: An accelerator mass spectrometry study. The American Journal of Clinical Nutrition, 93(6), 1263-1273.
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Shao, A., & Hathcock, J. N. (2006). Risk assessment for the carotenoids lutein and lycopene. Regulatory Toxicology and Pharmacology, 45(3), 289-298.
Singh, M., Krishanappa, R., Bagewadi, A., & Keluskar, V. (2004). Efficacy of oral lycopene in the treatment of oral leukoplakia. Oral Oncology, 40(6), 591-596.
Stahl, W., & Sies, H. (1992). Uptake of lycopene and its geometrical isomers is greater from heat-processed than from unprocessed tomato juice in humans. The Journal of Nutrition, 122(11), 2161-2166.
Stice, C. P., Liu, C., Aizawa, K., Greenberg, A. S., Ausman, L. M., & Wang, X. (2015). Dietary tomato powder inhibits alcohol-induced hepatic injury by suppressing cytochrome p450 2E1 induction in rodent models. Archives of Biochemistry and Biophysics, 572, 81-88.
Story, E. N., Kopec, R. E., Schwartz, S. J., & Harris, G. K. (2010). An update on the health effects of tomato lycopene. Annual Review of Food Science and Technology, 1(1), 189-210.
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Wang, X. (2012). Lycopene metabolism and its biological significance. The American Journal of Clinical Nutrition, 96(5), 1214S–1222S.
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Zhao, X., Aldini, G., Johnson, E. J., Rasmussen, H., Kraemer, K., Woolf, H., . . . Yeum, K. (2006). Modification of lymphocyte DNA damage by carotenoid supplementation in postmenopausal women. The American Journal of Clinical Nutrition, 83(1), 163-169.