Research Update:Artichoke Leaf.

  seminal trace...Artichoke Extract.Artichoke leaf Extract.Cynarin 2%.M.F.C25H24O12.CAS No.4350-09-8.4:1,10:1,20:1.Cynara scolymus.ALE.Artichoke thistle extract...

 


   Phytochemical info of Artichoke Leaf.

 Product Name:
 Synonym:
 Definition:Artichoke Leaf are majorly composed of
 Chemical information disclosed as following table:


   Research Update:Artichoke Leaf.

  Effects of artichoke extract supplementation on gonads of cadmium-treated rats.:Biol Trace Elem Res. 2007 Oct;119(1):51-9.Gurel E, Caner M, Bayraktar L, Yilmazer N, Dogruman H, Demirci C.Department of Biology, Istanbul University, Beyazit, Istanbul 34459, Turkey. egurel@istanbul.edu.tr

 The present study was designed to determine whether artichoke (Cynara scolymus) exerts a protective effect on gonads of cadmium-treated rats and if there is a relationship between artichoke supplementation and nitric oxide (NO) formation in cells. Forty Wistar albino male rats, weighing an average of 90 g each, were equally divided into four groups receiving 1 mg/100 g cadmium chloride by injection (group 1), the same dose CdCl2 plus 3 mg/100 g artichoke extract (group 2), the same dose of artichoke extract (group 3), and male controls (group 4). Four additional groups, labeled 5-8, consisted of identically treated and control female rats. After 4 weeks of treatment, the animals were killed and their gonads were removed for histological examination. As expected, the seminiferous tubules and Leydig cells were damaged by cadmium. Ovarian tissue was not damaged to the same extent as testicular cells. Artichoke extract exerted a clear protective effect against Cd-induced testicular damage and lowered NO production to the same level of that in the control groups.

  Antigenotoxic effect of extract from Cynara cardunculus L.:Phytother Res. 2007 Aug 28;Miadokova E, Nadova S, Vlckova V, Duhova V, Kopaskova M, Cipak L, Rauko P, Mucaji P, Grancai D.Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynska dolina, B©\1, 842 15 Bratislava, Slovakia.

 The extract of artichoke Cynara cardunculus L. (CCE) was investigated for its potential antigenotoxic and antioxidant effects using four experimental model systems. In the Saccharomyces cerevisiae mutagenicity/antimutagenicity assay, CCE significantly reduced the frequency of 4-nitroquinoline-N-oxide-induced revertants at the ilv1 locus and mitotic gene convertants at the trp5 locus in the diploid Saccharomyces cerevisiae tester strain D7. In the simultaneous toxicity and clastogenicity/anticlastogenicity assay, it exerted an anticlastogenic effect against N-nitroso-N'-methylurea-induced clastogenicity in the plant species Vicia sativa L. On the contrary, despite CCE not being mutagenic itself, in the preincubation Ames assay with metabolic activation, it significantly increased the mutagenic effect of 2-aminofluorene in the bacterial strain Salmonella typhimurium TA98. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, CCE exhibited considerable antioxidant activity. The SC(50) value representing 0.0054% CCE corresponds to an antioxidant activity of 216.8 microm ascorbic acid which was used as a reference compound. Although the mechanism of CCE action still remains to be elucidated, different possible mechanisms are probably involved in the CCE antigenotoxic effects. It could be concluded that CCE is of particular interest as a suitable candidate for an effective chemopreventive agent.

  Growth inhibitory effect of ethyl acetate-soluble fraction of Cynara cardunculus L. in leukemia cells involves cell cycle arrest, cytochrome c release and activation of caspases.:Phytother Res. 2007 Aug 17;Nadova S, Miadokova E, Mucaji P, Grancai D, Cipak L.Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynska dolina, B©\1, 842 15 Bratislava, Slovakia.

 An extract of artichoke Cynara cardunculus L. (CCE) has been shown to exhibit antioxidant and antigenotoxic properties. In this study, the ability of CCE to inhibit the growth of L1210 and HL-60 leukemia cells was studied. Treatment of leukemia cells with a variety of concentrations of CCE (500-2500 microg/microL) for 24 h resulted in dose-dependent inhibition of leukemia cell growth. The cell growth inhibition was accompanied by G(0)/G(1) cell cycle arrest and by a loss of cells in S phase. Futhermore, apoptosis detected as a sub-G(0) cell population and apoptotic DNA fragmentation was observed. More detailed analyses of apoptosis induced by CCE in HL-60 cells revealed that apoptosis progressed through the caspase-9/-3 pathway, as release of cytochrome c, caspase-9/-3 activations and specific proteolytic cleavage of poly(ADP-ribose) polymerase. Taken together, the results suggest that CCE exerts an antiproliferative activity on leukemia cells and induces apoptosis of these cells through a mitochondrial/caspase dependent pathway.

  Local food and cardioprotection: the role of phytochemicals.:Forum Nutr. 2006;59:116-29. Review. Visioli F, Bogani P, Grande S, Detopoulou V, Manios Y, Galli C.Department of Pharmacological Sciences, University of Milan, Milan, Italy. francesco.visioli@unimi.it

 For decades, most of the attention of nutritionists and health professionals has focused on the impact of the major dietary components, such as the amounts and types of fats, proteins, carbohydrates and fibers, on human health. However, interest in the role of minor components is rapidly growing. Many constituents of plants are non-nutritional compounds that play key roles in plant physiology and interactions with the environment. Over the past few years, we performed human studies to ascertain the health effects of Mediterranean foods such as extra virgin olive oil and tomatoes. Recently, we became interested in endothelial dysfunction and its implications in aging. To study the effects of local food plants on vascular function, plants were collected in Southern Italy. Extracts were first tested for their antioxidant activity in a variety of assays. The effects on the production of vasorelaxant factors were then investigated in cell culture. Finally, aged rats were fed with a wild artichoke extract and their vasomotion responsiveness was evaluated. In synthesis, the data uniformly demonstrate that phytochemical components of the Mediterranean diet exert cardioprotective effects whose mechanisms are being progressively elucidated.

  Tabletted microspheres containing Cynara scolymus (var. Spinoso sardo) extract for the preparation of controlled release nutraceutical matrices.:J Microencapsul. 2005 Aug;22(5):487-99.Gavini E, Alamanni MC, Cossu M, Giunchedi P.Dipartimento di Scineze del Farmaco, University of Sassari, Italy.

 Controlled release dosage forms based on tabletted microspheres containing fresh artichoke Cynara scolymus extract were performed for the oral administration of a nutritional supplement. Microspheres were prepared using a spray-drying technique; lactose or hypromellose have been chosen as excipients. Microspheres were characterized in terms of encapsulated extract content, size and morphology. Qualitative and quantitative composition of the extract before and after the spray process was determined. Compressed matrices (tablets) were prepared by direct compression of the spray-dried microspheres. In vitro release tests of microparticles and tablets prepared were carried out in both acidic and neutral media. Spray-drying is a good method to prepare microspheres containing the artichoke extract. The microspheres encapsulate an amount of extract close to the theoretical value. Particle size analyses indicate that the microparticles have dvs of approximately 6-7 microm. Electronic microscopy observations reveal that particles based on lactose have spherical shape and particles containing hypromellose are almost collapsed. The hydroalcoholic extract is stable to the microsphere production process: its polyphenolic composition (qualitative and quantitative) did not change after spraying. In vitro release studies show that microparticles characterized by a quick polyphenolic release both in acidic and neutral media due to the high water solubility of the carrier lactose. On the contrary, microspheres based hypromellose release only 20% of the loaded extract at pH 1.2 in 2 h and the total amount of polyphenols is released only after about further 6 h at pH 6.8. Matrices prepared tabletting lactose microspheres and hypromellose microparticles in the weight ratio 1:1 show a slow release rate, that lasts approximately 24 h. This one-a-day sustained release formulation containing Cynara scolymus extract could be proposed as a nutraceutical controlled release dosage form for oral administration.


  Bioavailability and pharmacokinetics of caffeoylquinic acids and flavonoids after oral administration of Artichoke leaf extracts in humans.:Phytomedicine. 2005 Jan;12(1-2):28-38.Wittemer SM, Ploch M, Windeck T, M¨¹ller SC, Drewelow B, Derendorf H, Veit M.Lichtwer Pharma AG, Berlin, Germany.

 Extracts from artichoke leaves are traditionally used in the treatment of dyspeptic and hepatic disorders. Various potential pharmacodynamic effects have been observed in vitro for mono- and dicaffeoylquinic acids (e.g. chlorogenic acid, cynarin), caffeic acid and flavonoids (e.g. luteolin-7-O-glucoside) which are the main phenolic constituents of artichoke leaf extract (ALE). However, in vivo not only the genuine extract constituents but also their metabolites may contribute to efficacy. Therefore, the evaluation of systemic availability of potential bioactive plant constituents is a major prerequisite for the interpretation of in vitro pharmacological testing. In order to get more detailed information about absorption, metabolism and disposition of ALE, two different extracts were administered to 14 healthy volunteers in a crossover study. Each subject received doses of both extracts. Extract A administered dose: caffeoylquinic acids equivalent to 107.0 mg caffeic acid and luteolin glycosides equivalent to 14.4 mg luteolin. Extract B administered dose: caffeoylquinic acids equivalent to 153.8 mg caffeic acid and luteolin glycosides equivalent to 35.2 mg luteolin. Urine and plasma analysis were performed by a validated HPLC method using 12-channel coulometric array detection. In human plasma or urine none of the genuine target extract constituents could be detected. However, caffeic acid (CA), its methylated derivates ferulic acid (FA) and isoferulic acid (IFA) and the hydrogenation products dihydrocaffeic acid (DHCA) and dihydroferulic acid (DHFA) were identified as metabolites derived from caffeoylquinic acids. Except of DHFA all of these compounds were present as sulfates or glucuronides. Peak plasma concentrations of total CA, FA and IFA were reached within 1 h and declined over 24 h showing almost biphasic profiles. In contrast maximum concentrations for total DHCA and DHFA were observed only after 6-7 h, indicating two different metabolic pathways for caffeoylquinic acids. Luteolin administered as glucoside was recovered from plasma and urine only as sulfate or glucuronide but neither in form of genuine glucosides nor as free luteolin. Peak plasma concentrations were reached rapidly within 0.5 h. The elimination showed a biphasic profile.

  Antifungal activity of Cynara scolymus L. extracts.:Fitoterapia. 2005 Jan;76(1):108-11. Zhu XF, Zhang HX, Lo R.Research Center for Eco-Environmental Sciences and Graduate School, Chinese Academy of Sciences, Beijing 100085, China.

 Chloroform, ethanol and ethyl acetate extracts of Cynara scolymus L. leaves, heads and stems were tested for their antifungal activity using the agar-well diffusion assay technique. The leaves extracts and the ethanol fractions were found to be the most effective extract against all the tested organisms.

  Purification of cynarases from artichoke (Cynara scolymus L.): enzymatic properties of cynarase A.:Phytochemistry. 2005 Jan;66(1):41-9.L?wenberg B, De Zeeuw HM.

 A new technique for the culture of T-lymphocytic colonies is reported. The method may be regarded as a human lymphocyte precursor cell assay, as is the myeloid colony culture for granulocyte-macrophage progenitors. The colonies arise under the simultaneous stimulation of phytohemagglutin and a leukocyte feeder. A linear relationship is found between colony numbers and cell numbers plated. The colonies represent aggregates of lymphoblast-like cells, the majority of which are capable of E-rosette formation, are responsive in mixed lymphocyte cultures, and do not exhibit surface immunoglobulins. Their density distribution profile is very similar to that of myeloid colony-forming cells. The finding that most of these colony-forming cells are recovered in the so-called lymphocyte-free stem cell fraction following density fractionation suggests that they originate from a lymphocytic precursor.

  Purification and characterization of a milk-clotting aspartic proteinase from globe artichoke (Cynara scolymus L.).:J Agric Food Chem. 2004 Dec 29;52(26):8182-9.Llorente BE, Brutti CB, Caffini NO.Food Engineering, CULTEV, Department of Basic Sciences, National University of Luj¨¢n, Luj¨¢n, Argentina. llorente@mail.unlu.edu.ar

 The study of proteinase expression in crude extracts from different organs of the globe artichoke (Cynara scolymus L.) disclosed that enzymes with proteolytic and milk-clotting activity are mainly located in mature flowers. Maximum proteolytic activity was recorded at pH 5.0, and inhibition studies showed that only pepstatin, specific for aspartic proteinases, presented a significant inhibitory effect. Such properties, in addition to easy enzyme inactivation by moderate heating, make this crude protease extract potentially useful for cheese production. Adsorption with activated carbon, together with anion exchange and affinity chromatography, led to the isolation of a heterodimeric milk-clotting proteinase consisting of 30- and 15-kDa subunits. MALDI-TOF MS of the 15-kDa chain determined a 15.358-Da mass, and the terminal amino sequence presented 96% homology with the smaller cardosin A subunit. The amino terminal sequence of the 30-kDa chain proved to be identical to the larger cardosin A subunit. Electrophoresis evidenced proteinase self-processing that was confirmed by immunoblots presenting 62-, 30-, and 15-kDa bands.

  Phenolic compounds from the leaf extract of artichoke (Cynara scolymus L.) and their antimicrobial activities.:J Agric Food Chem. 2004 Dec 1;52(24):7272-8.Zhu X, Zhang H, Lo R.Research Center for Eco-Environmental Sciences and Graduate School, Chinese Academy of Sciences, P.O. Box 2871, Beijing 100085, China.

 A preliminary antimicrobial disk assay of chloroform, ethyl acetate, and n-butanol extracts of artichoke (Cynara scolymus L.) leaf extracts showed that the n-butanol fraction exhibited the most significant antimicrobial activities against seven bacteria species, four yeasts, and four molds. Eight phenolic compounds were isolated from the n-butanol soluble fraction of artichoke leaf extracts. On the basis of high-performance liquid chromatography/electrospray ionization mass spectrometry, tandem mass spectrometry, and nuclear magnetic resonance techniques, the structures of the isolated compounds were determined as the four caffeoylquinic acid derivatives, chlorogenic acid (1), cynarin (2), 3,5-di-O-caffeoylquinic acid (3), and 4,5-di-O-caffeoylquinic acid (4), and the four flavonoids, luteolin-7-rutinoside (5), cynaroside (6), apigenin-7-rutinoside (7), and apigenin-7-O-beta-D-glucopyranoside (8), respectively. The isolated compounds were examined for their antimicrobial activities on the above microorganisms, indicating that all eight phenolic compounds showed activity against most of the tested organisms. Among them, chlorogenic acid, cynarin, luteolin-7-rutinoside, and cynaroside exhibited a relatively higher activity than other compounds; in addition, they were more effective against fungi than bacteria. The minimum inhibitory concentrations of these compounds were between 50 and 200 microg/mL.


  Artichoke leaf extract reduces symptoms of irritable bowel syndrome and improves quality of life in otherwise healthy volunteers suffering from concomitant dyspepsia: a subset analysis.:J Altern Complement Med. 2004 Aug;10(4):667-9.Bundy R, Walker AF, Middleton RW, Marakis G, Booth JC.Hugh Sinclair Unit of Human Nutrition, School of Food Biosciences, The University of Reading, Reading, UK. r.bundy@reading.ac.uk

 OBJECTIVES: Does artichoke leaf extract (ALE) ameliorate symptoms of Irritable bowel syndrome (IBS) in otherwise healthy volunteers suffering concomitant dyspepsia? METHODS: A subset analysis of a previous dose-ranging, open, postal study, in adults suffering dyspepsia. Two hundred and eight (208) adults were identified post hoc as suffering with IBS. IBS incidence, self-reported usual bowel pattern, and the Nepean Dyspepsia Index (NDI) were compared before and after a 2-month intervention period. RESULTS: There was a significant fall in IBS incidence of 26.4% (p < 0.001) after treatment. A significant shift in self-reported usual bowel pattern away from "alternating constipation/diarrhea" toward "normal" (p < 0.001) was observed. NDI total symptom score significantly decreased by 41% (p < 0.001) after treatment. Similarly, there was a significant 20% improvement in the NDI total quality-of-life (QOL) score in the subset after treatment. CONCLUSION: This report supports previous findings that ALE ameliorates symptoms of IBS, plus improves health-related QOL.

  Flavonoids from artichoke (Cynara scolymus L.) up-regulate endothelial-type nitric-oxide synthase gene expression in human endothelial cells.:J Pharmacol Exp Ther. 2004 Sep;310(3):926-32. Epub 2004 May 3.Li H, Xia N, Brausch I, Yao Y, F?rstermann U.Department of Pharmacology, Johannes Gutenberg University, Obere Zahlbacher Strasse 67, D-55131 Mainz, Germany. HuigeLi@mail.Uni-Mainz.de

 Nitric oxide (NO) produced by endothelial nitric-oxide synthase (eNOS) represents an antithrombotic and anti-atherosclerotic principle in the vasculature. Hence, an enhanced expression of eNOS in response to pharmacological interventions could provide protection against cardiovascular diseases. In EA.hy 926 cells, a cell line derived from human umbilical vein endothelial cells (HUVECs), an artichoke leaf extract (ALE) increased the activity of the human eNOS promoter (determined by luciferase reporter gene assay). An organic subfraction from ALE was more potent in this respect than the crude extract, whereas an aqueous subfraction of ALE was without effect. ALE and the organic subfraction thereof also increased eNOS mRNA expression (measured by an RNase protection assay) and eNOS protein expression (determined by Western blot) both in EA.hy 926 cells and in native HUVECs. NO production (measured by NO-ozone chemiluminescence) was increased by both extracts. In organ chamber experiments, ex vivo incubation (18 h) of rat aortic rings with the organic subfraction of ALE enhanced the NO-mediated vasodilator response to acetylcholine, indicating that the up-regulated eNOS remained functional. Caffeoylquinic acids and flavonoids are two major groups of constituents of ALE. Interestingly, the flavonoids luteolin and cynaroside increased eNOS promoter activity and eNOS mRNA expression, whereas the caffeoylquinic acids cynarin and chlorogenic acid were without effect. Thus, in addition to the lipid-lowering and antioxidant properties of artichoke, an increase in eNOS gene transcription may also contribute to its beneficial cardiovascular profile. Artichoke flavonoids are likely to represent the active ingredients mediating eNOS up-regulation.

  Effectiveness of artichoke extract in preventing alcohol-induced hangovers: a randomized controlled trial.:CMAJ. 2003 Dec 9;169(12):1269-73.Pittler MH, White AR, Stevinson C, Ernst E.Complementary Medicine, Peninsula Medical School, Universities of Exeter and Plymouth, United Kingdom. m.h.pittler@ex.ac.uk

 BACKGROUND: Extract of globe artichoke (Cynara scolymus) is promoted as a possible preventive or cure for alcohol-induced hangover symptoms. However, few rigorous clinical trials have assessed the effects of artichoke extract, and none has examined the effects in relation to hangovers. We undertook this study to test whether artichoke extract is effective in preventing the signs and symptoms of alcohol-induced hangover. METHODS: We recruited healthy adult volunteers between 18 and 65 years of age to participate in a randomized double-blind crossover trial. Participants received either 3 capsules of commercially available standardized artichoke extract or indistinguishable, inert placebo capsules immediately before and after alcohol exposure. After a 1-week washout period the volunteers received the opposite treatment. Participants predefined the type and amount of alcoholic beverage that would give them a hangover and ate the same meal before commencing alcohol consumption on the 2 study days. The primary outcome measure was the difference in hangover severity scores between the artichoke extract and placebo interventions. Secondary outcome measures were differences between the interventions in scores using a mood profile questionnaire and cognitive performance tests administered 1 hour before and 10 hours after alcohol exposure. RESULTS: Fifteen volunteers participated in the study. The mean number (and standard deviation) of alcohol units (each unit being 7.9 g, or 10 mL, of ethanol) consumed during treatment with artichoke extract and placebo was 10.7 (3.1) and 10.5 (2.4) respectively, equivalent to 1.2 (0.3) and 1.2 (0.2) g of alcohol per kilogram body weight. The volume of nonalcoholic drink consumed and the duration of sleep were similar during the artichoke extract and placebo interventions. None of the outcome measures differed significantly between interventions. Adverse events were rare and were mild and transient. INTERPRETATION: Our results suggest that artichoke extract is not effective in preventing the signs and symptoms of alcohol-induced hangover. Larger studies are required to confirm these findings.

  Efficacy of artichoke leaf extract in the treatment of patients with functional dyspepsia: a six-week placebo-controlled, double-blind, multicentre trial.:Aliment Pharmacol Ther. 2003 Dec;18(11-12):1099-105.Holtmann G, Adam B, Haag S, Collet W, Gr¨¹newald E, Windeck T.Division of Internal Medicine, Department of Gastroenterology, University of Essen, Germany. g.holtmann@uni-essen.de

 BACKGROUND: This study aimed to assess the efficacy of artichoke leaf extract (ALE) in the treatment of patients with functional dyspepsia (FD). METHODS: In a double-blind, randomized controlled trial (RCT), 247 patients with functional dyspepsia were recruited and treated with either a commercial ALE preparation (2 x 320 mg plant extract t.d.s.) or a placebo. The primary efficacy variable was the sum score of the patient's weekly rating of the overall change in dyspeptic symptoms (four-point scale). Secondary variables were the scores of each dyspeptic symptom and the quality of life (QOL) as assessed by the Nepean Dyspepsia Index (NDI). RESULTS: Two hundred and forty-seven patients were enrolled, and data from 244 patients (129 active treatment, 115 placebo) were suitable for inclusion in the statistical analysis (intention-to-treat). The overall symptom improvement over the 6 weeks of treatment was significantly greater with ALE than with the placebo (8.3 +/- 4.6, vs. 6.7 +/- 4.8, P < 0.01). Similarly, patients treated with ALE showed significantly greater improvement in the global quality-of-life scores (NDI) compared with the placebo-treated patients (- 41.1 +/- 47.6 vs. - 24.8 +/- 35.6, P < 0.01). CONCLUSION: The ALE preparation tested was significantly better than the placebo in alleviating symptoms and improving the disease-specific quality of life in patients with functional dyspepsia.

  Validated method for the determination of six metabolites derived from artichoke leaf extract in human plasma by high-performance liquid chromatography-coulometric-array detection.:J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Aug 15;793(2):367-75.Wittemer SM, Veit M.Lichtwer Pharma AG, Wallenroder Strasse 8-10, 13485 Berlin, Germany.

 A validated method was developed for the simultaneous determination of the hydroxycinnamates caffeic (CA), dihydrocaffeic (DHCA), ferulic (FA), dihydroferulic (DHFA), and isoferulic acid (IFA) and the flavonoid luteolin (LUT) in human plasma as metabolites derived from artichoke leaf extract. The method involves sample preparation followed by separation using high-performance liquid chromatography on reversed-phase material with a polar endcapping (Aqua-C(18), 250 x 4.6 mm). Selectivity and sensitivity towards the target compounds were achieved by electrochemical array detection (CoulArray). Calibration curves were constructed in the ranges 2.1-51.7 ng x mL(-1) (CA), 2.0-76.7 ng mL(-1) (DHCA), 2.2-53.7 ng x mL(-1) (FA), 2.1-79.2 ng x mL(-1) (DHFA), 1.1-52.6 ng x mL(-1) (IFA) and 2.1-258.6 ng x mL(-1) (LUT). Linearity could be shown for all target compounds over the entire calibration range. Values for within-day and between-day precision and accuracy were in accordance with the international guidelines for validation of bioanalytical methods. It is concluded that this newly developed method is appropriate for analysing samples from bioavailability and pharmacokinetic studies after oral administration of artichoke leaf extract.


  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 Jul;55(7):981-6.Betancor-Fern¨¢ndez A, P¨¦rez-G¨¢lvez A, Sies H, Stahl W.Institut f¨¹r Biochemie und Molekularbiologie I, Heinrich-Heine-Universit?t D¨¹sseldorf, Postfach 101007, D-40001 D¨¹sseldorf, Germany.

 Pharmaceutical preparations derived from natural sources such as vegetables often contain compounds that contribute to the antioxidant defence system and apparently play a role in the protection against degenerative diseases. In the present study, commercial preparations containing extracts of turmeric, artichoke, devil's claw and garlic or salmon oil were investigated. The products were divided into fractions of different polarity, and their antioxidant activity was determined using the Trolox equivalent antioxidant capacity (TEAC) assay. This test is based on the efficacy of the test material to scavenge 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) derived radicals. Total phenols were determined in all fractions as well as specific carotenoids in the most lipophilic fraction to assess their contribution to the antioxidant activity. For comparison, the radical scavenging effect of selected constituents of the extracts such as curcumin, luteolin, kaempferol, chlorogenic acid, harpagoside, beta-carotene and alpha-tocopherol was investigated and compared with that of Trolox. Curcumin, luteolin, kaempferol, chlorogenic acid and beta-carotene showed an antioxidant activity superior to Trolox in the TEAC assay; harpagoside was barely active. All fractions of the turmeric extract preparation exhibited pronounced antioxidant activity, which was assigned to the presence of curcumin and other polyphenols. The antioxidant activity corresponding to the artichoke leaf extract was higher in the aqueous fractions than in the lipophilic fractions. Similarly, devil's claw extract was particularly rich in water-soluble antioxidants. Harpagoside, a major compound in devil's claw, did not contribute significantly to its antioxidant activity. The antioxidant capacity of the garlic preparation was poor in the TEAC assay. That of salmon oil was mainly attributed to vitamin E, which is added to the product for stabilization. In all test preparations, the antioxidant activity was significantly correlated with the content of total phenolic compounds.

  Occupational rhinitis and bronchial asthma due to artichoke (Cynara scolymus).:Ann Allergy Asthma Immunol. 2003 Jul;91(1):92-5.Miralles JC, Garc¨ªa-Sells J, Bartolom¨¦ B, Negro JM.University General Hospital, Murcia, Spain. jmirallesl@meditex.es

 BACKGROUND: The artichoke is a perennial horticultural plant that belongs to the Compositae family. OBJECTIVE: To present case studies of 2 vegetable warehouse workers who developed occupational rhinitis and bronchial asthma by sensitization to artichoke. METHODS: Skin prick tests with common inhalants and foods were performed. Specific IgE to artichoke, Parietaria judaica pollen, and Olea europaea pollen extracts was measured by a specific IgE enzyme immunosorbent assay kit. Molecular mass of the allergens was studied by the sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) immunoblotting technique. Patients underwent a nasal challenge test, and one patient provided peak expiratory flow rate (PEFR) measurements in her workplace. RESULTS: In both patients, results of skin prick tests to artichoke were positive. Levels of specific IgE for artichoke were 0.68 kU/L in patient 1 and 2.14 kU/L in patient 2. The protein composition of the artichoke extract, studied by SDS-PAGE, showed that most bands ranged from 30 to 14 kDa. The IgE-binding bands with the serum samples of patient 1 showed apparent molecular masses of 56, 48, 38, 31, 27, 25, 16, and 15 kDa; however, the serum samples of patient 2 showed IgE bands of 21 and 19 kDa. Western blotting of artichoke extract showed a complete inhibition of IgE-binding bands when serum samples were preincubated with P. judaica pollen extract. Nasal challenge with artichoke extract triggered a peak nasal inspiratory flow decrease of 81% and 85% in patient 1 and patient 2, respectively. Finally, patient 1 recorded a PEFR decrease of up to 36% after exposure to artichoke in her workplace. CONCLUSIONS: SDS-PAGE immunoblotting inhibition performed for the artichoke extract showed a total disappearance of the specific IgE binding bands when serum samples were previously incubated with P. judaica pollen extract, thus establishing the existence of a serologic cross-reactivity between artichoke and P. judaica pollen.

  Efficacy of different Cynara scolymus preparations on liver complaints.:J Ethnopharmacol. 2003 Jun;86(2-3):203-11.Speroni E, Cervellati R, Govoni P, Guizzardi S, Renzulli C, Guerra MC.Department of Pharmacology, University of Bologna, Via Irnerio 48, Italy. esperoni@biocfarm.unibo.it

 Cynara scolymus leaves extracts have long been used in folk medicine for their choleretic and hepatoprotective activities, that are often related to the cynarin content. These therapeutic properties are also attributed to mono- and di-caffeoylquinic acids and since commercial C. scolymus preparations can differ for their activities, we studied four extracts to evaluate, if present, a relationship between the hepatobiliary properties of the different preparations and their content in phenolics. The antioxidant activity of the commercial preparations examined was also considered in an in vitro system. The results showed that the extract with the highest content in phenolic derivatives (GAE) exerted the major effect on bile flow and liver protection. Also the results of the antioxidant capacity (BR) of the different preparations are in good agreement with the results obtained in vivo. On the contrary, administering rats with doses of chlorogenic acid, equivalent to those present in this extract, we did not observe any choleretic or protective action. An histopathological analysis of liver sections confirmed the biochemical results. Perhaps caffeoyl derivatives have a role in the therapeutic properties of C. scolymus extracts, as reported in literature for "in vitro" studies, but when administered alone, they are not so effective in exerting this action.

  Artichoke leaf extract reduces mild dyspepsia in an open study.:Phytomedicine. 2002 Dec;9(8):694-9.Marakis G, Walker AF, Middleton RW, Booth JC, Wright J, Pike DJ.Hugh Sinclair Unit of Human Nutrition, The University of Reading, UK.

 A recent post-marketing study indicated that high doses of standardised artichoke leaf extract (ALE) may reduce symptoms of dyspepsia. To substantial these findings, this study investigated the efficacy of a low-dose ALE on amelioration of dyspeptic symptoms and improvement of quality of life. The study was an open, dose-ranging postal study. Healthy patients with self-reported dyspepsia were recruited through the media. The Nepean Dyspepsia Index and the State-Trait Anxiety Inventory were completed at baseline and after 2 months of treatment with ALE, which was randomly allocated to volunteers as 320 or 640 mg daily. Of the 516 participants, 454 completed the study. In both dosage groups, compared with baseline, there was a significant reduction of all dyspeptic symptoms, with an average reduction of 40% in global dyspepsia score. However, there were no differences in the primary outcome measures between the two groups, although relief of state anxiety, a secondary outcome, was greater with the higher dosage (P = 0.03). Health-related quality of life was significantly improved in both groups compared with baseline. We conclude that ALE shows promise to ameliorate upper gastro-intestinal symptoms and improve quality of life in otherwise healthy subjects suffering from dyspepsia.

  Choleretic activity and biliary elimination of lipids and bile acids induced by an artichoke leaf extract in rats.:Phytomedicine. 2002 Dec;9(8):687-93.Sa¨¦nz Rodriguez T, Garc¨ªa Gim¨¦nez D, de la Puerta V¨¢zquez R.Pharmacology Department, Faculty of Pharmacy, University of Seville, Seville, Spain.

 The therapeutic properties of artichoke (Cynara scolymus L.) preparations have been known since ancient times. The traditional use of artichoke leaf extract (ALE) in gastroenterology is mainly based upon its strong antidyspeptic actions which are mediated by its choleretic activity. The aim of this study was to investigate the effects of ALE on bile flow and the formation of bile compounds in anaesthetised Wistar rats after acute and repeated (twice a day for 7 consecutive days) oral administration. A significant increase in bile flow was observed after acute treatment with ALE as well as after repeated administration. The choleretic effects of ALE were similar to those of the reference compound dehydrocholic acid (DHCA). Total bile acids, cholesterol and phospholipid were determined by enzymatic assays. There was a strong ALE-induced increase in total bile acid concentration over the entire experiment. With the highest dose (400 mg/kg), a significant increase was obtained after single and repeated administration. The bile acids-increased effects of ALE were much more pronounced than those of reference (DHCA). No significant differences in cholesterol and phospholipid content could be found.


  Anti-hyperlipidemic sesquiterpenes and new sesquiterpene glycosides from the leaves of artichoke (Cynara scolymus L.): structure requirement and mode of action.:Bioorg Med Chem Lett. 2003 Jan 20;13(2):223-8.

 The methanolic extract from the leaves of artichoke (Cynara scolymus L.) was found to suppress serum triglyceride elevation in olive oil-loaded mice. Through bioassay-guided separation, sesquiterpenes (cynaropicrin, aguerin B, and grosheimin) were isolated as the active components together with new sesquiterpene glycosides (cynarascolosides A, B, and C). The oxygen functional groups at the 3- and 8-positions and exo-methylene moiety in alpha-methylene-gamma-butyrolactone ring were found to be essential for the anti-hyperlipidemic activity of guaiane-type sesquiterpene. In addition, inhibition of gastric emptying was shown to be partly involved in anti-hyperlipidemic activity.

  Protective properties of artichoke (Cynara scolymus) against oxidative stress induced in cultured endothelial cells and monocytes.:Life Sci. 2002 Nov 1;71(24):2897-08.Zapolska-Downar D, Zapolski-Downar A, Naruszewicz M, Siennicka A, Krasnodebska B, Ko?dziej B.Chair of Clinical Biochemistry and Laboratory Diagnoastic, Regional Ctr. Atherosclerosis Research, Pomeranian Academy of Medicine, ul. Powsta¨½c¨®w Wlkp. 72, PL-70-111, Szczecin, Poland.

 It is currently believed that oxidative stress and inflammation play a significant role in atherogenesis. Artichoke extract exhibits hypolipemic properties and contains numerous active substances with antioxidant properties in vitro. We have studied the influence of aqueous and ethanolic extracts from artichoke on intracellular oxidative stress stimulated by inflammatory mediators (TNFalpha and LPS) and ox-LDL in endothelial cells and monocytes. Oxidative stress which reflects the intracellular production of reactive oxygen species (ROS) was followed by measuring the oxidation of 2', 7'-dichlorofluorescin (DCFH) to 2', 7'-dichlorofluorescein (DCF). Agueous and ethanolic extracts from artichoke were found to inhibit basal and stimulated ROS production in endothelial cells and monocytes in dose dependent manner. In endothelial cells, the ethanolic extract (50 microg/ml) reduced ox-LDL-induced intracellular ROS production by 60% (p<0,001) while aqueous extract (50 microg/ml) by 43% (p<0,01). The ethanolic extract (50 microg/ml) reduced ox-LDL-induced intracellular ROS production in monocytes by 76% (p<0,01). Effective concentrations (25-100 microg/ml) were well below the cytotoxic levels of the extracts which started at 1 mg/ml as assessed by LDH leakage and trypan blue exclusion. Penetration of some active substances into the cells was necessary for inhibition to take place as juged from the effect of preincubation time. These results demonstrate that artichoke extracts have marked protective properties against oxidative stress induced by inflammatory mediators and ox-LDL in cultured endothelial cells and monocytes.

  Artichoke leaf extract for treating hypercholesterolaemia.:Cochrane Database Syst Rev. 2002;(3):CD003335. Review.Pittler MH, Thompson CO, Ernst E.Department of Complementary Medicine, University of Exeter, 25 Victoria Park Road, Exeter, Devon, UK, EX2 4NT. M.H.Pittler@ex.ac.uk

 BACKGROUND: Hypercholesterolaemia is directly associated with an increased risk for coronary heart disease and other sequelae of atherosclerosis. Artichoke leaf extract (ALE), which is available as an over-the-counter remedy, has been implicated in lowering cholesterol levels. Whether ALE is truly efficacious for this indication, however, is still a matter of debate. OBJECTIVES: To assess the evidence of ALE versus placebo or reference medication for treating hypercholesterolaemia defined as mean total cholesterol levels of at least 5.17 mmol/L (200 mg /dL). SEARCH STRATEGY: We searched MEDLINE, Embase, Amed, Cinahl, CISCOM and the Cochrane Controlled Trial Register. All databases were searched from their respective inception until June 2001. Reference lists of articles were also searched for relevant material. Manufacturers of preparations containing artichoke extract and experts on the subject were contacted and asked to contribute published and unpublished material. SELECTION CRITERIA: Randomized controlled trials of ALE mono-preparations compared with placebo or reference medication for patients with hypercholesterolaemia were included. Trials assessing ALE as one of several active components in a combination preparation or as a part of a combination treatment were excluded. DATA COLLECTION AND ANALYSIS: Data were extracted systematically and methodological quality was evaluated using a standard scoring system. The screening of studies, selection, data extraction and the assessment of methodological quality were performed independently by two reviewers. Disagreements in the evaluation of individual trials were resolved through discussion. MAIN RESULTS: Two randomised trials including 167 participants met all inclusion criteria. In one trial ALE reduced total cholesterol levels from 7.74 mmol/l to 6.31 mmol/l after 42 +/- 3 days of treatment whereas the placebo reduced cholesterol from 7.69 mmol/l to 7.03 mmol/l (p=0.00001). Another trial did state that ALE significantly (p<0.05) reduced blood cholesterol compared with placebo in a sub-group of patients with baseline total cholesterol levels of more than 230 mg/dl. Trial reports and post-marketing surveillance studies indicate mild, transient and infrequent adverse events. REVIEWER'S CONCLUSIONS: Few data from rigorous clinical trials assessing ALE for treating hypercholesterolaemia exist. Beneficial effects are reported, the evidence however is not compelling. The limited data on safety suggest only mild, transient and infrequent adverse events with the short term use of ALE. More rigorous clinical trials assessing larger patient samples over longer intervention periods are needed to establish whether ALE is an effective and safe treatment option for patients with hypercholesterolaemia.

  Inhibition of cholesterol biosynthesis in HepG2 cells by artichoke extracts is reinforced by glucosidase pretreatment.:Phytother Res. 2002 Jun;16(4):368-72.Gebhardt R.Institut f¨¹r Biochemie, Universit?tsklinikum Leipzig, 04103 Leipzig, Germany.

 High-dose aqueous extracts from artichoke leaves were found to inhibit cholesterol biosynthesis from (14)C-acetate rather moderately in HepG2 cells in contrast to primary cultured rat hepatocytes in which the inhibition was stronger. Preincubation of the extracts with several glycohydrolases revealed that pretreatment with beta-glucosidase considerably reinforced the inhibition. A significant reduction of acetate incorporation was found above extract concentrations of 0.01 mg/mL and at 0.2 mg/mL almost 60% inhibition was observed. Cytotoxic effects detected by the MTT-assay were restricted to higher concentrations of the extracts with and without beta-glucosidase pretreatment. Since cynaroside represents a major glucoside in artichoke extracts, both cynaroside and its aglycone luteolin were tested. It could be demonstrated that cynaroside is indeed one of the targets of beta-glucosidase and that the liberated luteolin is responsible for the inhibitory effect. Direct measurements of beta-glucosidase activity in rat hepatocytes and HepG2 cells revealed that endogenous enzyme activity in hepatocytes may be sufficient to convert cynaroside to its aglycone, while in HepG2 cells this may not be the case. These findings emphasize the importance of beta-glucosidase-dependent liberation of luteolin for the ability of artichoke extracts to inhibit hepatic cholesterol biosynthesis.

  Artichoke (Cynara scolymus L.) byproducts as a potential source of health-promoting antioxidant phenolics.:J Agric Food Chem. 2002 Jun 5;50(12):3458-64.Llorach R, Esp¨ªn JC, Tom¨¢s-Barber¨¢n FA, Ferreres F.Department of Food Science and Technology, CEBAS-CSIC, P.O. Box 4195, Murcia 30080, Spain.

 The present study reports a fast, economical, and feasible way to extract antioxidant phenolics from artichoke byproducts: raw artichoke (RA), blanched (thermally treated) artichoke (BA), and artichoke blanching waters (ABW). These byproducts represent a huge amount of discarded material in some industries. Two protocols, with possible industrial applicability, based on both methanol and water extractions were used. Phenolic contents (expressed as caffeic acid derivatives) (grams per 100 g of dry extract) were 15.4 and 9.9 for RA when extracted with methanol and water, respectively; 24.3 and 10.3 for BA when extracted with methanol and water, respectively; and finally, 11.3 g of phenolics/100 mL of ABW. Therefore, methanol extracts yielded more phenolics than water extracts, especially when BA byproducts were used. The higher amount of phenolics in BA could be due to the inactivation of polyphenol oxidase (PPO) at the industrial scale (due to blanching process), avoiding PPO-catalyzed oxidation of these phenolics, a phenomenon that could occur in RA byproducts. Artichoke extracts from industrial byproducts showed a high free radical scavenging activity (versus both DPPH* and ABTS*+ radicals) as well as capacity to inhibit lipid peroxidation (ferric thiocyanate method). According to these results, the use of artichoke extracts from industrial byproducts as possible ingredients to functionalize foodstuffs (to decrease lipid peroxidation and to increase health-promoting properties) is suggested.


  Caffeic acid derivatives in artichoke extract are metabolised to phenolic acids in vivo.:Free Radic Res. 2001 Aug;35(2):195-202. Rechner AR, Pannala AS, Rice-Evans CA.Antioxidant Research Centre, Centre of Age-Related Diseases, GKT School of Biomedical Sciences, King's College London, London SE1 9RT.

 The purpose of this study was to investigate the absorption and metabolism of hydroxycinnamates from artichoke extract by determining the urinary excretion of the conjugates. Ten healthy, non smoking volunteers (5 female, 5 male) were given three capsules containing artichoke extract every 4 h (0, 4, 8 h) following two days of a low-polyphenol diet. One capsule contained 320 mg of artichoke extract equivalent to 34.3 +/- 0.6 mg/g hydroxycinnamates (caffeic acid derivatives) and 5.6 +/- 0.1 mg/g flavonoids. Polyphenols and phenolic acids present in the artichoke extract were not detected in the urine either as conjugates or aglycones. However, ferulic, isoferulic, dihydroferulic and vanillic acid were identified as major metabolites after beta-glucuronidase treatment of urine. The amount excreted as well as the ratio to that of creatinine, a biomarker for the general excretion rate, increased significantly on the study day compared to the pre-supplementation day. Thus, the caffeic acid esters found in the artichoke extract capsule are absorbed, metabolised and excreted as methylated phenolic acids such as ferulic, isoferulic, dihydroferulic and vanillic acid.

  Activity of artichoke leaf extract on reactive oxygen species in human leukocytes.:Free Radic Res. 2000 Nov;33(5):661-5.P¨¦rez-Garc¨ªa F, Adzet T, Ca?igueral S.Untitat de Farmacologia i Farmacogn¨°sia, Facultat de Farm¨¤cia, Universitat de Barcelona, Spain.

 Artichoke leaf extract was studied in human leukocytes for activity against oxidative stress using flow cytometry and dichlorofluorescin diacetate as a fluorescence probe. It produces a concentration-dependent inhibition of oxidative stress when cells are stimulated with agents that generate reactive oxygen species (ROS): hydrogen peroxide, phorbol-12-myristate-13-acetate (PMA), and N-formyl-methionyl-leucyl-phenylalanine (FMLP). Cynarin, caffeic acid, chlorogenic acid, and luteolin, constituents of artichoke leaf extract, also show a concentration-dependent inhibitory activity in the above models, contributing to the antioxidant activity of the extract in human neutrophils.

  Artichoke leaf extract reduces symptoms of irritable bowel syndrome in a post-marketing surveillance study:Phytother Res. 2001 Feb;15(1):58-61.Walker AF, Middleton RW, Petrowicz O.The Hugh Sinclair Unit of Human Nutrition, School of Food BioSciences, The University of Reading, PO Box 226, Whiteknights, Reading RG6 6AP, UK. food@afnovell.reading.ac.uk

 Irritable bowel syndrome (IBS) is a problem reported to affect 22% of the general population. It is characterized by abdominal pain and altered bowel habit, but has so far defied elucidation of its pathogenesis and proved difficult to treat. There is a growing body of evidence which indicates therapeutic properties for artichoke leaf extract (ALE). Dyspepsia is the condition for which the herb is specifically indicated, but the symptom overlap between dyspeptic syndrome and IBS has given rise to the notion that ALE may have potential for treating IBS as well. A sub-group of patients with IBS symptoms was therefore identified from a sample of individuals with dyspeptic syndrome who were being monitored in a post-marketing surveillance study of ALE for 6 weeks. Analysis of the data from the IBS sub-group revealed significant reductions in the severity of symptoms and favourable evaluations of overall effectiveness by both physicians and patients. Furthermore, 96% of patients rated ALE as better than or at least equal to previous therapies administered for their symptoms, and the tolerability of ALE was very good. These results provide support for the notion that ALE has potential value in relieving IBS symptoms and suggest that a controlled trial is justified.

  Influence of ochratoxin A and an extract of artichoke on the vaccinal immunity and health in broiler chicks:Exp Toxicol Pathol. 2000 Mar;52(1):43-55.Stoev SD, Anguelov G, Ivanov I, Pavlov D.Department of Pathomorphology, Faculty of Veterinary Medicine, Thracian University Stara Zagora, Bulgaria. s_stoev@hotmail.com.uzvm.bg

 The combined effect of ochratoxin A (at diet levels of 130, 305 and 790 ppb) and penicillic acid was studied in 100 broiler chicks. Serological investigations revealed significantly lower haemagglutination inhibiting antibody titers in the experimental chicks immunized with vaccine against Newcastle disease. A statistically significant decrease of the body weight and the relative weight of lymphoid organs as well as a significant increase of the relative weight of kidneys and liver were seen. The main degenerative changes were observed in the proximal convoluted tubules in kidneys and slight degenerative changes were found in the hepatocytes. Degenerative changes and depletion of lymphoid cells were observed in the bursa Fabricii, thymus, spleen and Peyer's patches of intestinal mucosa. Serum analyses revealed significant decreases of the total protein and cholesterol, and significant increases of the uric acid and glucose. Haematological analyses showed a slight anaemia, leucocytosis and slightly decompensated metabolic acidosis. A statistically significant protective effect of 5% total water extract of artichoke on humoral immune response (increase of haemaglutination inhibiting antibody titer), relative organ weight as well as on pathomorphological, haematological and biochemical changes induced by ochratoxin A, was established.

  Luteolin-rich artichoke extract protects low density lipoprotein from oxidation in vitro.:Free Radic Res. 1998 Sep;29(3):247-55.Brown JE, Rice-Evans CA.International Antioxidant Research Centre, UMDS-Guy's Hospital, London, UK.

 Flavonoids represent a diverse group of phytochemicals which possess the capacity to act as antioxidants in vitro. This study examined the free radical scavenging properties of a luteolin-rich artichoke extract and some of its pure flavonoid constituents by assessing their ability to prevent Cu2+-mediated LDL oxidation. Artichoke extract retarded LDL oxidation in a dose-dependent manner as measured by a prolongation of the lag phase to conjugated diene formation, a decrease in the rate of propagation and a sparing of endogenous LDL alpha-tocopherol during oxidation. The pure aglycone, luteolin (1 microM), demonstrated an efficacy similar to that of 20 microg/ml artichoke extract in inhibiting lipid peroxidation. Luteolin-7-O-glucoside, one of the glycosylated forms in the diet, also demonstrated a dose-dependent reduction of LDL oxidation that was less effective than that of luteolin. Studies of the copper-chelating properties of luteolin-7-O-glucoside and luteolin suggest a potential role for chelation in the antioxidative effects of artichoke extract. Overall, the results demonstrate that the antioxidant activity of the artichoke extract relates in part to its constituent flavonoids which act as hydrogen donors and metal ion chelators, and the effectiveness is further influenced by their partitioning between aqueous and lipophilic phases.


  Scientific References:

  1.Research Update:Artichoke Leaf.