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Plant Profiler

Globe artichoke (Cynara scolymus)


Cynara scolymus
Synonyms / Common Names / Related Terms
Alcachofa, alcaucil, artichaut (French), artichiocco, artichoke, artichoke inulin, artichoke juice, Artischocke (German), artiskok, carciofo, cardo, cardo de comer, cardon d'Espagne, cardoon, chlorogenic acid, Cynara®, Cynara cardunculus, Cynara scolymus L., Cynarae folium, cynarin, cynaroside, French artichoke, garden artichoke, Gemuseartischocke (German), golden artichoke, Hekbilin A®, Hepar SL® forte, inulin, kardone, LI220, Listrocol®, luteolin, Raftiline®, scolymoside, tyosen-azami, Valverde Artischoke bei Verdauungsbeschwerden.



Mechanism of Action

Pharmacology:

  • Constituents: Cynarin, luteolin, cynardoside (luteolin-7-O-glycoside), scolymoside, and chlorogenic acid are believed to be artichoke's bioactive constituents. Cynarin is most concentrated in the leaves and is the most studied component of artichoke. Luteolin is reported to be responsible for inhibition of cholesterol synthesis, while cynarin may have no effects.6 Inulin from globe artichokes is reported to be a potent prebiotic and probiotic, and exhibits a long-lasting bifidogenic effect.3,11 Chlorogenic acid, cynarin, luteolin, and cynaroside contained in an organic sub-fraction of artichoke leaf extract have recently been shown to modulate vascular endothelial function through upregulation of nitric oxide production in cultured human umbilical vascular endothelial cells.12
  • Antioxidant effects: In vitro studies have isolated a variety of antioxidant compounds from globe artichoke, and confirmation of the antioxidant activity of artichoke has been noted in multiple pre-clinical studies.13,14,15,5,8,1,16,17,18,19,20 Further studies have confirmed an antioxidant-related hepatoprotective effect in vitro in rat hepatocytes13,14,8,16,1, cultured endothelial cells and monocytes20, and an in vivo rat model21. An additional study demonstrated further antioxidant properties via inhibition of LDL oxidation.5
  • Cardiovascular protection: In vitro and laboratory animal data suggest that artichoke extract may have vasodilatory activity and provide cardioprotection.12,9 An in vitro study suggests that artichoke leaf extract may exhibit cardiovascular protective activities via its effect on the regulation of the endothelial nitric oxide synthase (eNOS) gene. This study investigated the effect of artichoke leaf extract on cultured human umbilical vein endothelial cells demonstrated that treatment with artichoke leaf extract increased activity and expression of the eNOS gene, and increased nitric oxide production.12 Artichoke extracts may offer an additional degree of cardiovascular protection via its overall positive effect on endothelial function.
  • Choleretic effects (stimulation of bile secretion): In vitro studies have demonstrated globe artichoke leaf extract may increase bile secretion in perfused rat liver and liver cell cultures.2,4 It has been suggested that reduction of intrahepatic cholesterol concentration is responsible for globe artichoke extract's ability to treat dyspepsia.2
  • Cholesterol-lowering effects: In vitro and animal studies report that cynarin and artichoke extracts may reduce serum cholesterol and triglyceride levels.10,22,23 Other animal research has noted that artichoke extracts may prevent the development of atherosclerotic plaques.24,25,26 Some of these studies used rats, which are a poor model for human cholesterol metabolism. The antiatherosclerotic action is thought to be the product of two mechanisms of action: an antioxidant effect that reduces LDL oxidation5, and inhibition of cholesterol synthesis 7. Gebhardt reported that globe artichoke extract decreased cholesterol synthesis by inhibiting the action of HMG-CoA reductase, which is required to convert HMG-CoA to mevalonate, the same action as statin drugs.6 In the synthesis of cholesterol, acetyl-CoA is converted to HMG-CoA, then to mevalonate and ultimately to cholesterol. In this study, luteolin was the compound found to be responsible for inhibition of cholesterol synthesis, while cynarin had no effect on cholesterol synthesis. A more recent study involving 28 subjects investigating the effect of supplementing 20mL/daily of frozen artichoke on hyperlipemia, failed to demonstrate a significant reduction in cholesterol relative to the control group. 9 However, the study did note a significant increase in serum triglycerides (5.7%) in the experimental group assigned artichoke juice relative to the control group.
  • Hepatoprotection: In vitro studies report that cynarin and artichoke extracts provide antihepatotoxic and other hepatoprotective properties against a variety of toxins13,14,27,16,1,28,29
  • Prebiotic/probiotic effects: An in vitro study found that inulin extracted from globe artichoke is a potent prebiotic stimulator of beneficial Bifidobacterium bifidum.3 Valerio et al. investigated the ability of artichokes to serve as vehicle for the delivery of probiotic bacterial strains.11 Probiotic bacterial strains were recovered from fecal samples of volunteers fed artichokes inoculated with probiotics. Researchers observed an increase in the presence of probiotic strains in inoculated volunteers, suggesting that not only do artichokes serve as an effective vehicle for delivery of probiotics, but contain substances such as inulin, that favor growth of probiotic strains. Finally, artichokes were shown to protect probiotic bacterial strains during simulated gastric and intestinal digestion.

Pharmacodynamics/Kinetics:

  • The active constituents of artichoke extract have not been detected in human plasma or urine. Several metabolites detected in human plasma have been identified as being derived from mono- and dicaffeoylquininc acids, and flavanoids that are known active phenolic constituents of artichoke leaf extract. The metabolites caffeic acid, ferulic acid, and isoferulic acid achieved peak plasma concentrations within one hour and declined over 24 hours, demonstrating a near bi-phasic profile. The hydrogenated metabolites dihydrocaffeic acid and dihyrdoferulic acid were detected after six to seven hours, suggesting the involvement of more than one pathway in processing caffeoylquinic acids. Peak plasma concentrations of luteolin were reached within 30 minutes, with elimination showing a biphasic profile.30

References
  1. Gebhardt, R. Antioxidative and protective properties of extracts from leaves of the artichoke (Cynara scolymus L.) against hydroperoxide-induced oxidative stress in cultured rat hepatocytes. Toxicol Appl Pharmacol  1997;144(2):279-286. 9194411
  2. Kraft K. Artichoke leaf extract - Recent findings reflecting effects on lipid metabolism, liver and gastrointestinal tracts. Phytomedicine 1997;4(4):369-378.
  3. Lopez-Molina, D., Navarro-Martinez, M. D., Rojas-Melgarejo, F., Hiner, A. N., Chazarra, S., and Rodriguez-Lopez, J. N. Molecular properties and prebiotic effect of inulin obtained from artichoke (Cynara scolymus L.). Phytochemistry 2005;66(12):1476-1484. 15960982
  4. Matuschowski P. Testing of Cynara scolymusin the isolated perfused rat liver. 43rd Ann Congr Soc Med Plant Res 1996;3-7.
  5. Brown, J. E. and Rice-Evans, C. A. Luteolin-rich artichoke extract protects low density lipoprotein from oxidation in vitro. Free Radic Res 1998;29(3):247-255. 9802556
  6. Gebhardt, R. Inhibition of cholesterol biosynthesis in primary cultured rat hepatocytes by artichoke (Cynara scolymus L.) extracts. J Pharmacol Exp Ther  1998;286(3):1122-1128. 9732368
  7. Wegener T. [About the therapeutic activity of the artichoke]. Pflanzliche Gallentherapeutika 1995;16:81.
  8. Fintelmann V. Antidyspeptic and lipid-lowering effects of artichoke leaf extract - results of clinical studies into the efficacy and tolerance of Hepar-SL forte involving 553 patients. J Gen Med 1996;2:3-19.
  9. Lupattelli, G., Marchesi, S., Lombardini, R., Roscini, A. R., Trinca, F., Gemelli, F., Vaudo, G., and Mannarino, E. Artichoke juice improves endothelial function in hyperlipemia. Life Sci 12-31-2004;76(7):775-782. 15581909
  10. Lietti A. Choleretic and cholesterol lowering properties of artichoke extracts. Fitoterapia 1977;48:153-158.
  11. Valerio, F., De Bellis, P., Lonigro, S. L., Morelli, L., Visconti, A., and Lavermicocca, P. In vitro and in vivo survival and transit tolerance of potentially probiotic strains carried by artichokes in the gastrointestinal tract. Appl Environ.Microbiol  2006;72(4):3042-3045. 16598015
  12. Li, H., Xia, N., Brausch, I., Yao, Y., and Forstermann, U. Flavonoids from artichoke (Cynara scolymus L.) up-regulate endothelial-type nitric-oxide synthase gene expression in human endothelial cells. J Pharmacol Exp Ther  2004;310(3):926-932. 15123766
  13. Adzet, T., Camarasa, J., and Laguna, J. C. Hepatoprotective activity of polyphenolic compounds from Cynara scolymus against CCl4 toxicity in isolated rat hepatocytes. J Nat Prod  1987;50(4):612-617. 3430163
  14. Adzet T. Action of an artichoke extract against carbon tetrachloride-induced hepatotoxicity in rats. Acts Pharm Jugosl 1987;37:183-188.
  15. Betancor-Fernandez, A., Perez-Galvez, A., Sies, H., and Stahl, W. Screening pharmaceutical preparations containing extracts of turmeric rhizome, artichoke leaf, devil's claw root and garlic or salmon oil for antioxidant capacity. J Pharm Pharmacol 2003;55(7):981-986. 12906755
  16. Gebhardt R and Fausel M. Antioxidant and hepatoprotective effects of artichoke extracts and constituents in cultured rat hepatocytes. Toxicol in Vitro 1997;11:669-672.
  17. Llorach, R., Espin, J. C., Tomas-Barberan, F. A., and Ferreres, F. Artichoke (Cynara scolymus L.) byproducts as a potential source of health-promoting antioxidant phenolics. J Agric Food Chem  6-5-2002;50(12):3458-3464. 12033811
  18. Visioli, F., Bogani, P., Grande, S., Detopoulou, V., Manios, Y., and Galli, C. Local food and cardioprotection: the role of phytochemicals. Forum Nutr 2006;59:116-129. 16917176
  19. Wang, M., Simon, J. E., Aviles, I. F., He, K., Zheng, Q. Y., and Tadmor, Y. Analysis of antioxidative phenolic compounds in artichoke (Cynara scolymus L.). J Agric Food Chem  1-29-2003;51(3):601-608. 12537429
  20. Zapolska-Downar, D., Zapolski-Downar, A., Naruszewicz, M., Siennicka, A., Krasnodebska, B., and Koldziej, B. Protective properties of artichoke (Cynara scolymus) against oxidative stress induced in cultured endothelial cells and monocytes. Life Sci  11-1-2002;71(24):2897-08. 12377270
  21. Jimenez-Escrig, A., Dragsted, L. O., Daneshvar, B., Pulido, R., and Saura-Calixto, F. In vitro antioxidant activities of edible artichoke (Cynara scolymus L.) and effect on biomarkers of antioxidants in rats. J Agric Food Chem  8-27-2003;51(18):5540-5545. 12926911
  22. Wojcicki, J. Effect of 1,5-dicaffeylquinic acid (cynarine) on cholesterol levels in serum and liver of acute ethanol-treated rats. Drug Alcohol Depend  1978;3(2):143-145. 580239
  23. Wojcicki, J. Effect of 1,5-dicaffeoylquinic acid on ethanol-induced hypertriglyceridemia. Short communication. Arzneimittelforschung 1976;26(11):2047-2048. 1037244
  24. Samochowiec L. Artichoke. Diss Pharm 1959;11:99-112.
  25. Samochowiec L. The effect of artichokes (Cynara scolymus L.) and cardoons (Cynara cardunculus L.) on developed atherosclerotic changes in white rats. Fol Biol 1962;10:75-83.
  26. Samochowiec L. The action of herbs and roots of artichokes (Cynara scolymnus) and cardoon (Cynara cardunculus) on the development of experimental atherosclerosis in white rats. Diss Pharm 1962;14:115.
  27. Camarasa J, Laguna JC, and Gaspar A. Biochemical and histological pattern of cyanarin and caffeic acid treatment in CCl4-induced hepatoxicity. Med Sci Res 1987;15:91-92.
  28. Kiso, Y., Tohkin, M., and Hikino, H. Assay method for antihepatotoxic activity using carbon tetrachloride induced cytotoxicity in primary cultured hepatocytes. Planta Med 1983;49(4):222-225. 6669643
  29. Kiso, Y., Tohkin, M., and Hikino, H. Antihepatotoxic principles of Atractylodes rhizomes. J Nat Prod  1983;46(5):651-654. 6418860
  30. Wittemer, S. M., Ploch, M., Windeck, T., Muller, S. C., Drewelow, B., Derendorf, H., and Veit, M. Bioavailability and pharmacokinetics of caffeoylquinic acids and flavonoids after oral administration of Artichoke leaf extracts in humans. Phytomedicine  2005;12(1-2):28-38. 15693705




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