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Artichoke

Scientific Name(s): Cynara cardunculus L., Cynara scolymus L.
Common Name(s): Alcachofra, Extractum Cynarae aq. Siccum, Garden artichoke, Globe artichoke

Clinical Overview

Use

Artichoke has been used for its antioxidant and GI soothing effects. It may also have moderately hypoglycemic and hypolipidemic properties; however, clinical information for any use is lacking.

Dosing

A range of divided doses from 600 to 3,200 mg/day have been used in clinical trials.

Contraindications

Allergy to Asteraceae family plants (eg, daisy, chrysanthemum, marigold, Echinacea, ragweed); bile duct obstruction.

Pregnancy/Lactation

Artichoke heads are generally recognized as safe (GRAS) when used as food. Information is lacking for artichoke leaf extract; caution is warranted.

Interactions

None well documented.

Adverse Reactions

Mild, transient, and infrequent adverse reactions generally limited to GI complaints. Allergic reactions and a case of hepatotoxicity have been reported.

Toxicology

Specific toxicological studies are limited. No toxicity was observed in vitro in a study of artichoke leaf extract on human umbilical endothelial cells and hamster ovary cells. Some genotoxicity was demonstrated in vitro on bone marrow cells at the highest dose administered.

Botany

The artichoke is a member of the daisy family. It is a perennial herb, widely cultivated in Mediterranean regions and adjoining parts of central Europe. This well-known plant grows to a height of approximately 2 m. It has a strong, erect stem, and its large, thistle-like leaves are lobed and gray-green. The edible flower bud is purple-green and enclosed by scales or bracts, and blooms from July to August. The plant should not be confused with the Jerusalem artichoke (Helianthus tuberosus).1, 2, 3, 4

History

The artichoke has been cultivated for thousands of years, with the Greek physician Dioscorides (circa AD 40-90) recommending the application of mashed roots on the body to sweeten offensive odors. The artichoke was used as food and medicine by ancient Egyptians, Greeks, and Romans (although the exact plant used has been disputed), and appeared in Europe in the 15th century. The botanical name is derived in part from the tradition of fertilizing the plant with ashes, and partly from the Greek skolymos, meaning "thistle" from the spines found on the bracts that enclose the flower heads forming the edible portion of the plant. The French have used artichoke juice as a liver tonic. The herb's abilities to break down fat and improve bile flow have been recognized. Artichoke has been used traditionally to treat a variety of conditions, including hepatic diseases, jaundice, dyspepsia, and chronic albuminuria. It has also been used as a diuretic and to manage postoperative anemia.1, 2, 3, 4

Chemistry

Nutritionally, the artichoke head contains fat, carbohydrates, and protein. It also contains fiber (inulin), calcium, phosphorus, potassium, folic acid, vitamin C, niacin, thiamine, trace minerals, and carotenoids. Artichoke is an ideal source for essential polyunsaturated fatty acids, containing stearic, palmitic, oleic, and linoleic (50%) acids. Artichoke seed oil composition has been described. Color and anthocyanin pigments in artichoke have been evaluated, and the identity of numerous enzymes, including oxidases, peroxidases, cynarase, and ascorbinase, have been reported.

Caffeic acid and its derivatives in artichoke have been widely studied. Hydroxymethylacrylic acid also has been isolated from artichoke.

Bitter sesquiterpene principles, such as grosheimin, cynaratriol, and cynaropicrin, have been reported from the plant, along with dehydrocynaropicrin, grosulfeimin and related guaianolides, and cynarolide. Flavonoids (0.1% to 1%), including flavone glycosides and rutin, are present in artichoke. Flavonoid glycosides apigenin, luteolin, cynaroside, scolimoside, cosmoside, quercetin, isorhamnetin, maritimein, and others also have been reported. Volatile oils of artichoke include beta-selinene and caryophyllene as major sesquiterpenes, eugenol, phenylacetaldehyde, and decanal.

Much of the pharmacologic activity of the leaves has been attributed to the presence of caffeoylquinic acid derivatives, mono- and di-caffeoylquinic acids, including chlorogenic, neochlorogenic, and cryptochlorogenic acids, luteolin, and cynarin.

High-performance liquid chromatography and other analytic methods have been described. The relative proportion of these compounds varies with the strain, age, and generation of the plant. For example, germinating seeds of the artichoke have higher cynarin content than the leaves, while cynaropicrin content is highest in young leaves, but not in the root of mature fruits and flowers.2, 5, 6, 7, 8, 9, 10, 11, 12, 13

Uses and Pharmacology

Antioxidant activity

Animal data

Antioxidant activity of artichoke leaf extract has been demonstrated in animal studies using both histology and oxidative stress biomarkers.14, 15, 16, 17, 18, 19 Protective effects have also been demonstrated against carbon tetrachloride-, lead-, and cadmium-induced toxicity.15, 20, 21

Clinical data

A small clinical study conducted among athletes found that pretreatment with artichoke leaf extract over 5 weeks increased their total antioxidant capacity over untreated participants following intensive exercise. Effects on performance were not reported.22

Cancer

Animal data

Artichoke leaf extract protected hamster ovary cells against induced DNA lesions.19 Flavonoids and the polyphenol fractions possess chemopreventive effects as well, as seen with mouse skin cancers and human breast cancer and heptatoma cell lines.23, 24, 25

Clinical data

Research reveals no clinical trials using artichoke for the prevention or treatment of cancer.

Cholesterol-lowering effects

Animal data

Artichoke has been found to possess cholesterol-lowering effects in rodent studies. Leaf extracts were found to inhibit cholesterol biosynthesis. An increased excretion of fecal bile acids was also reported. Constituents cynaroside and aglycone luteolin were suggested to be mainly responsible for this effect, while chlorogenic, caffeic dicaffeoylquinic acids, and cynarin demonstrated little or no inhibitory effects.26, 27, 28

Clinical data

A Cochrane systematic review of clinical trials evaluating hypolipidemic effects of artichoke leaf extract has been published covering studies to mid-2012.29 Only 3 studies met inclusion criteria, and one of these was only available as an abstract. A modest positive effect on the lipid profile was shown with decreased total cholesterol. Two studies published since the review have reported reductions in total cholesterol, one demonstrating improved measures of endothelial function and the other reporting increased high-density lipoprotein (HDL) and decreased low-density lipoprotein (LDL). Participant numbers in these studies are small, with 18 in one and 92 in the other.30, 31 A small clinical study conducted among athletes designed to measure antioxidant effects found that pretreatment with artichoke leaf extract over 5 weeks decreased total cholesterol, but had no effect on HDL, LDL, or triglycerides.22 Similarly, a clinical study evaluating the hypotensive effects of artichoke leaf juice found no effect on the lipid profile, despite reducing systolic and diastolic pressure in patients with mild hypertension.32

Diabetes

Animal data

Limited studies in rats show a moderate hypoglycemic effect of artichoke flowering head extract.33, 34, 35

Clinical data

Limited clinical trials among overweight people have shown reduction in glycosylated hemoglobin and glycemia, with artichoke extracts alone and in combination with Phaseolus vulgaris (common bean).36, 37 A small clinical study conducted among athletes designed to measure antioxidant effects found that pretreatment with artichoke leaf extract over 5 weeks had no effect on serum glucose.22

As a component of medical nutrition therapy for patients with type 2 diabetes, the American Diabetes Association Standards of Care (2014) recommends higher quality dietary fat intake, as an alternative to decreased fat intake, by replacing saturated and/or trans fats with mono- and poly-unsaturated fatty acids in the diet. This Mediterranean-style approach to eating may improve glycemic control and cardiovascular disease risk factors (moderate quality evidence).57

GI effects

Animal data

Experiments in rodents with induced gastric-ulcers have shown dose-dependent increases in mucus production and reductions in gastric ulceration with both artichoke leaf and flower bud/head extract.38, 39

Clinical data

Very long chain inulin derived from artichoke root given to healthy adults (N = 32) increased the fecal bacterial count, acting as a probiotic.40 Probiotic-enriched artichokes have also been used as an enriched fiber-rich vegetable in constipation and to deliver probiotics.41, 42, 43 Post hoc analysis of an open-label study suggests artichoke leaf extract provided symptomatic relief in irritable bowel syndrome.44

Other uses

Alcohol hangover

A randomized trial evaluating artichoke as a cure for hangover found no significant difference compared with placebo among the 15 participants.45

Antimicrobial

Probiotic-enriched artichoke heads antagonized Escherichia coli and Clostridium spp. in an experiment.46 An extract from the fruit of artichoke inhibited Campylobacter species in vitro, while the leaf extracts showed antifungal activity.47 A small clinical study among patients with chronic hepatitis C found no effect on viral load or liver enzymes, despite being well tolerated.48

Antispasmodic

Guinea pig and rat ileum have demonstrated both contractile and relaxing effects from hydrophilic and lipophilic leaf extracts.49, 50

Dermatological

Cynaropicrin extracted from artichoke leaves suppressed nuclear factor kappa-B and prevented photoaging processes in a mouse skin model.51

Dosing

Divided doses from 600 to 3,200 mg/day have been used in clinical trials.22, 29, 30, 31

Peak plasma levels of hydroxycinnamic acids at 0.5 hours have been reported, with a biphasic elimination profile. Bioavailability after cooking has also been demonstrated.4, 12

Pregnancy / Lactation

Artichoke heads are GRAS when used as food. Avoid dosages above those found in food because safety and efficacy are unproven. Information is lacking for artichoke leaf extracts; caution is warranted.52

Interactions

Case reports are lacking. Artichoke leaf extract chelated lead in the gonads of rats20; however, no literature on chelation of other elements (eg, iron) is available.

Adverse Reactions

Most clinical studies with artichoke leaf extract report mild, transient, and infrequent adverse reactions generally limited to GI complaints, including bloating.29, 39, 48

A case report of hepatotoxicity associated with consumption of a French commercial artichoke product has been published; the manufacturers of the product acknowledge 2 other cases.53

Contact with artichoke and other Asteraceae family plants (daisy, chrysanthemum, marigold, Echinacea, and ragweed) has caused allergic reactions in sensitive individuals, with cynaropicrin and other sesquiterpene lactones possibly being the responsible chemical constituents. Dermatitis, rhinitis, asthma, and edema of the tongue have been reported rarely. Anaphylaxis to the inulin content has been reported,54 as well as nonallergic irritant contact dermatitis.55

The Expanded Commission E Monographs warn against the use of artichoke preparations in any bile duct pathology because of its choleretic properties.3

Toxicology

Specific toxicological studies are limited. No toxicity was observed in vitro in a study of artichoke leaf extract on human umbilical endothelial cells and hamster ovary cells.18, 19, 56 Median lethal doses in rats of 265 mg/kg (intraperitoneal) and 2,000 mg/kg (oral) have been estimated based on caffeoylquinic acid content.2 Some genotoxicity was demonstrated in vitro on bone marrow cells at the highest dose tested (2,000 mg/kg oral) and may be due to the flavonoid content of the leaf extract.52

References

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26. Küskü-Kiraz Z, Mehmetçik G, Dogru-Abbasoglu S, Uysal M. Artichoke leaf extract reduces oxidative stress and lipoprotein dyshomeostasis in rats fed on high cholesterol diet. Phytother Res. 2010;24(4):565-570.19777605
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