Arctium – Burdock Root (Arctii radix)
|Latin name of the genus:||Arctium|
|Latin name of herbal substance:||Arctii radix|
|Botanical name of plant:||Arctium lappa l.|
|English common name of herbal substance:||Burdock root|
Latin name of the genus: Arctium
Latin name of herbal substance: Arctii radix
Botanical name of plant: Arctium lappa L.
English common name of herbal substance: Burdock Root
2.2.Information on traditional/current indications and specified substances/preparations . 10
2.3.Specified strength/posology/route of administration/duration of use for relevant
- 1. Introduction
- 2. Historical data on medicinal use
- 3. Non-Clinical Data
- 3.1. Overview of available pharmacological data regarding the herbal substance(s), herbal preparation(s) and relevant constituents thereof
- 3.2. Overview of available pharmacokinetic data regarding the herbal substance(s), herbal preparation(s) and relevant constituents thereof
- 3.3. Overview of available toxicological data regarding the herbal substance(s)/herbal preparation(s) and constituents thereof
- 3.4. Overall conclusions on non-clinical data
- 4. Clinical Data
- 4.1. Clinical Pharmacology
- 4.1.1. Overview of pharmacodynamic data regarding the herbal substance(s)/preparation(s) including data on relevant constituents
- 4.1.2. Overview of pharmacokinetic data regarding the herbal substance(s)/preparation(s) including data on relevant constituents
- 4.2. Clinical Efficacy
- 4.2.1. Dose response studies
- 4.2.2. Clinical studies (case studies and clinical trials)
- 4.2.3. Clinical studies in special populations (e.g. elderly and children)
- 4.3. Overall conclusions on clinical pharmacology and efficacy
- 5. Clinical Safety/Pharmacovigilance
- 6. Overall conclusions
1.1. Description of the herbal substance(s), herbal preparation(s) or combinations thereof
Arctium lappa L. is known under the synonyms:
Latin: Arctium majus BERNH., Lappa communis var. major COSSON et GERM., Lappa major GAERTN., Lappa officinalis ALL., Lappa vulgaris HILL., Lappa vulgaris var. major NEILR
English: beggars button, burdock,
French: bardane, bouillon noir, choux d’ânes, glouteron, gouteron, grande bardane, grateau, grateron, herbe aux pouilleux, herbe aux teigneux, oreille de géant, pignet, teigneux
German: große Klette, Dollenkraut, gemeine Klette
Italian: bardana, bardana maggiore, farfariaccio, lappa bardana, lappola
Dutch: grote klis, grote klit, dokke, kladden, klevers,
(Blaschek 1998, Delfosse 1998, De Smet 1993, Leclerc 1966, Van Os 1980, Wichtl 1994).
Arctium lappa L. is a biennial member of the Compositae (Asteraceae) that can reach one meter and a half. It has large cordiform leaves. The purple flowers appear from July until September. The spherical flower head, three to four centimeters in diameter, has rough hairs (Delfosse 1998, Lambinon 1998).
Native in Europe, Northern Asia and North America (Wichtl 1994).
The leaves are collected from
The use of fresh leaves is described in literature (Leclerc 1966, Valnet 2001).
–Sesquiterpenes: The dried leaves contain essential oil, arctiol, dehydrofukinone, eremophilene, – eudesmol, fukinanolide, fukinone and petasitolone. The fresh leaves contain onopordopicrin and the ground leaves arctiopicrin.
–Triterpenes: Free terpene alcohols, free sterols, triterpene esters.
From the petrolether extract of dried leaves are isolated: free triterpene alcohols
–Fatty Acids: 94.7% saturated (C14 – C26) and 5.3% unsaturated (C18) fatty acids.
–Phenol Carbonic Acid: Caffeic acid.
The mature fruit is collected in autumn and dried. Thereafter, the dried fruit is purified and dried again in the sun (Blaschek 1998).
The dried, ripe fruit is collected in autumn (Chinese Pharmacopoeia 1995, Körfers 2009).
–Fatty Oils: The seeds contain about 16% fatty oils, namely linoleic acid, oleic acid, octadecatrienic acid, palmitic acid, stearic acid, eicosatrienic acid, arachidonic acid, myristinic acid, linolenic acid, heptadecanic acid, margarinic acid and pentadecanic acid.
–Lignans: The fruit contains a broad spectrum of lignans. Lignans with two phenylpropane units: arctiin, arctigenin, matairesinol. Lignans with three phenylpropane units (“sesquilignans”): lappaol A, lappaol B, lappaol C, lappaol D, lappaol E. Lignans with four phenylpropane units (“dilignans”): lappaol F, lappaol H, neoarctin A, neoarctin B and diarctigenin.
The most recent official definition is included in DAC 2008: dried, total or cut roots of Arctium lappa L. (=A. major Gaertn.), A. minus (Hill) Bernh., A. tomentosum Mill. (Asteraceae) and from related species, hybrids or mixtures thereof. The root is collected in the autumn of the first year or in the spring of the second year.
Similar or identical definitions can be found in Barnes (2007), Blaschek (1998), De Smet (1993), Duke (1988), Uchiyama (2005) and Wichtl (1994).
–Volatile constituents, essential oil: There are only
Blaschek (1998) categorizes them as follows:
Aliphatic hydrocarbons: aplotaxen, dihydroaplotaxen,
Aliphatic and aromatic aldehydes: phenylacetaldehyde, propionaldehyde, benzaldehyde, butyraldehyde, caproicaldehyde, isovaleraldehyde and others
Carbonic acids: carbonic acids from C2 until C13 and also tiglic acid, isovaleric acid among others
H2C O CH2
Figure 1: dehydrocostuslacton
Figure 3: arctinol
–Phenolcarbonic acids and tannins: The fresh root contains 1.9 up to 3.65% polyphenols with chlorogenic acid, isochlorogenic acid and caffeic acid. More recent tests show the presence of derivatives of quinic acid. The root also contains a small amount of tannins.
–Lignans: neoarctin A and the lignanolide arctiin.
Figure 4: arctiin
–Triterpenes: 15.2% triterpenester, 12.8% free sterols (sitosterol, stigmasterol, a.o.), 10.7%, triterpenacetates, 2.9% triterpenacids and 2.4% triterpenalcohols
–Fatty acids: 0.4 until 0.8% fatty acids including linolenic acid, linoleic acid, myristic acid, palmitic- and
–Polysaccharides: The total carbohydrates may represent up to 70% of the dry mass and contain mainly inulin (about 45%).
–Other constituents: The aminoacid fraction contains
Figure 5: baicalin
Figure 6: aplotaxene
Apart from the references cited, market information was included (Barnes 2007, Blaschek 1998, Delfosse 1998, Leclerc 1966, Valnet 2001, Van Hellemont 1985).
Hagers Handbuch der Pharmazeutischen Praxis (Blaschek 1998) mentions different fluid extracts of Radix Bardanae (Extractum Bardanae):
–Extractum Bardanae Portug.
–Extractum Bardanae Brasil.
–Extractum lappae fluidum
–Extractum lappae fluidum Brasil.
–Extractum lappae majoris stabilisatae
No further details could be retrieved for those preparations.
Combinations of herbal substance(s) and/or herbal preparation(s) including a description of vitamin(s) and/or mineral(s) as ingredients of traditional combination herbal medicinal products assessed, where applicable.
‘Essiac’ is described as a formula that consists of four herbal substances: Arctium lappa L., Rheum palmatum L., Rumex acetosella L. and Ulmus rubra L. The preparation is only partially characterised.
Indication: cancer treatments but no convincing clinical evidence is available (Capasso 2003, Ulbricht 2009).
1.2. Information about products on the market in the Member States
Regulatory status overview
MA: Marketing Authorisation TRAD: Traditional Use Registration
Other TRAD: Other national Traditional systems of registration Other: If known, it should be specified or otherwise add ’Not Known’
This regulatory overview is not legally binding and does not necessarily reflect the legal status of the products in the MSs concerned.
In the Czech Republic, a fixed combination (herbal tea) is used. This tea contains Phaseoli fructus sine semine, Myrtilli herba, Salviae officinalis herba, Galegae herba, Polygonii avicularis herba, Taraxaci radix cum herba, Rubi fruticosi folium, Foeniculi fructus, Bardanae radix and Liquiritiae radix.
Indication: adjuvant therapy in diabetes.
An ayurvedic fixed combination is available in Denmark. It contains 40 mg Arctium lappa L. per tablet and 18 other ingredients. No information on details of the preparation is given.
Indication: claudicatio intermittens.
Powdered herbal substance in hard capsules.
A preparation containing powdered herbal substance in capsules is on the market in France since 1980. It contains 350 mg powdered herbal substance per capsule.
Posology: 1 capsule 3 times daily (up to 5 capsules if necessary).
–traditionally used in seborrhoeic skin conditions
–traditionally used to promote urinary and digestive elimination functions.
Extract in hard capsules
A preparation with dry extract made with ethanol 70% V/V (DER
It contains 200 mg dry extract per capsule.
Posology: 1 capsule 2 times daily.
Indications: Traditionally used in seborrhoeic skin conditions.
In Spain powdered or cut herbal substance is on the market as tea since 1973.
A daily dose of 3 g to 6 g can be taken.
Indication: facilitating the elimination of urine.
The herbal substance is also available in combination products.
There is partial information about other products on the Spanish market. The date of commercialising is not specified.
Liquid extract (DER 1:1)
Tincture (1:10) 50 drops 1 to 3 times daily
Dry extract (DER 5:1) 1 g daily
The solvents for all these preparations are not specified.
These preparations are similar to the ones mentioned in the BHP (1983), cited by Barnes (2007) and Blaschek (1998).
Indication: similar uses as presented in registered products.
2. Historical data on medicinal use
2.1. Information on period of medicinal use in the Community
Arctium lappa L. has been widely used in folk medicine (Gentil 2006). Besides, the root and leaves are listed by the Council of Europe as a natural source of food flavouring (category N2) (Barnes 2007).
An herbal tea called ‘Essiac plus’ contains the same four substances as ‘Essiac’ (Arctium lappa L.,
Rheum palmatum L., Rumex acetosella L. and Ulmus rubra L.) plus four additional herbs: Nasturtium officinale L., Cnicus benedictus L., Trifolium pratense L. and Laminaria digitata (Huds.) Lamour. Indication: The tea is used by cancer patients during chemo- and radiation therapy. No further details about concentration and doses are given (Tai and Cheung 2005).
According to Tai and Cheung (2005), a product called
In Spain, powdered or cut root is on the market as tea since 1973. The oral use of preparations with non specified root extract is reported by Leclerc (1966).
In some countries, mainly in Japan, a cultivated form of Arctium lappa L. is used as a vegetable (De Smet 1993).
2.2. Information on traditional/current indications and specified substances/preparations
– Macerate: fresh leaves macerated during one night in salted vinegar (1:125)
Terray, cited by Leclerc (1966), reports good results when using the fresh macerated leaves wrapped around the painful body parts of patients with rheumatism. This can create an urticarial reaction which is considered to be even more beneficial (Leclerc 1966).
– Unknown way of administration and posology:
Tea infusions of leaves are used for stomach ulcer and gastritis. In case of infection of mouth and pharynx, a decoction is used to gargle. Topically it is used to treat skin diseases, insect bites (Bruneton 1999), itching and scratches (Blaschek 1998). Leaves may help to treat bruises, tumours and gouty swellings (Duke 1988).
Kloss, cited by Duke (1988), describes the leaves as ‘excellent for cancer sores, gonorrhea, gout, leprosy, rheumatism, sciatica, scrofula and syphilis’. They have been used to treat bladder stones, eczema, gallstones, gout, and skin afflictions (Duke 1988).
Alcoholic extracts of the leaves are used for treating psoriasis and seborrhoeic eczema. Extracts would also promote hair growth and are used in the production of cosmetics (Blaschek 1998).
The crushed leaves of Arctium lappa L. were also applied on snake bites. Beneficial effects have been attributed to a modification of the main constituents in the venom. The oxidation that happens is thought to be similar to the one of potassium permanganate (Leclerc 1966, Valnet 2001).
As the traditional use is restricted to
The seeds of Arctium lappa are used in Korea for their supposed diuretic,
In Asia, the seeds are used to treat constipation, flatulence, abscesses, dropsy, acne, scarlet fever, flu, snakebite, measles, scrofula and smallpox. Tinctures of the seeds are used for the treatment of kidney diseases, psoriasis, prurigo and acne (Duke 1988).
As only very limited information on the traditional use of the seeds within the Community is available (Blaschek 1998, Valnet 2001), no monograph on A. lappa L., fructus is proposed.
Use of different herbal preparations:
Antibacterial and antimycotic use
No further reference is made to specific preparations. This use dates from 1960 or before that date.
Root preparations have been used for rheumatism (Bradley 1992).
The root of Arctium lappa L. is described as a blood purifier, it is believed to clear toxins from the bloodstream (De Smet 1993).
In folk medicine, root infusions and plasters are often used for its
The root has been used for gout (Valnet 2001).
Choleretic and diuretic use
Burdock root has been considered to have diuretic and diaphoretic actions to stimulate
According to DAC 2008, the root is used in case of gout, rheumatism and to promote urinary
elimination and sweating.
The root can also be used as a diaphoretic and diuretic remedy. Arctium lappa L. promotes sweating, which helps to release toxins through the skin. It also promotes more urine production and gives further elimination of toxins via the kidneys and bladder (De Smet 1993, Duke 1988).
It is also used as a laxative for renal or urinary calculi, jaundice and furunculosis (De Smet 1993).
Treatment against urolithiasis has been mentioned by Valnet (2001).
Root preparations have been used for skin disorders, seborrheic eczema and for stimulation of the hair growth. The hairy character of the plant might explain the belief of its hair growing characteristics (Bradley 1992).
Acording to DAC 2008, the root is externally used in seborrhoe of the skin, other skin diseases, wounds and acne.
It is also used against eczema (De Smet 1993).
Topical application can be used to treat poorly healing wounds, ichtyosis, psoriasis, acne and other skin diseases. The radix can also be added to bathwater. In the past, Oleum Bardanae was used topically for seborrheic eczema. Most of the sources are copying each other, referring to the BHP (1983), which is in fact a compilation of former BHP editions (BHP 1976). This preparation has to be considered as being traditionally used for more than 30 years.
According to DAC (2008), the root is widely used in popular medicine: orally for treatment of
The roasted root can be consumed as a coffee surrogate (Blaschek 1998).
The root decoction alleviates ulcerated, glandular and white tumours (Duke 1988).
2.3.Specified strength/posology/route of administration/duration of use for relevant preparations and indications
(1) Soft stabilised extract of the root:
A stabilised soft extract is described in the Codex Français (1949) and cited by Garnier (1961). R/ Arctium lappa, powdered root 1000 g
Distilled water 8000 g
Macerate of the root in 5000 g distilled water during 12 hours under regular mixing and filter under pressure. Macerate the residue in the remaining part of the water during 12 hours and filter under pressure.
Mix both filtrates and evaporate the water under reduced pressure until 3000 g remain. Let the fluid settle and filter after 24 hours. Evaporate under reduced pressure ‘au
3.1. Overview of available pharmacological data regarding the herbal substance(s), herbal preparation(s) and relevant constituents thereof
Activity of isolated compounds:
In 2008, a study investigated the
A diet containing 0.1, 0.02 or 0.004% arctiin was administered for 18 weeks. Arctiin has been evaluated to exert no definite effects on prostate carcinogenesis in SV 40 T antigen transgenic rats at least in the experiment, although a weak inhibitory tendency was found in high dose groups (Zeng 2005).
Baicalin, a natural compound of Arctium lappa L. and genistin, a baicalin derivative, were found to be potent and selective inhibitors of terminal deoxyribonucleotidyltransferase (TdT), an eukaryotic DNA- polymerase. The IC50 of baicalin and genistin to TdT were respectively 18.6µM and 28.7µM. These inhibitors can be used as tools and molecular probes to distinguish DNA polymerases and to clarify their in vivo biological function (Uchiyama 2005).
Antioxidative effects and
Inhibitors of NO production in macrophages are important targets in the treatment of inflammatory diseases, such as rheumatoid arthritis. The lignans isolappaol C, lappaol C, lappaol D, lappaol F and diarctigenin were isolated from a methanolic extract of the seeds from Arctium lappa L. They were investigated in their inhibitory effects on the NO production in
Kim (2008) describes the
According to Knipping (2008), Arctium lappa L. might be a promising natural component for use in
Arctiin was also able to inhibit acute skin response in mice in vivo.
In 2008, Li studied the prebiotic potential of components of Arctium lappa L. They found that inulin of the root from Arctium lappa L. (1% w/v) promoted the specific growth rate of “beneficial bacteria” in vitro and in vivo. The final bacterial mass in the medium with inulin of Arctium lappa L. was greater
than that in the medium without inulin of Arctium lappa L. By stimulating the growth of these lactobacilli and bifidobacteria in vitro, the resistance to disease is thought to increase because these
Arctiin, a constituent of Fructus Bardanae, delays germination of other plant seeds. The anatomy of the stem is not influenced but in the root abnormal germination (= deformation of the root with root hairs that are shorter and twisted) is induced by Arctium lappa L. Due to short and twisted root hairs the nutrition intake is possibly heavily disturbed. An interaction with DNA is also observed. However, the kind of interaction is not yet clear (Blaschek 1998).
Activity of preparations from the leaves:
Although the root of Arctium lappa L. has been found to cause hypoglycaemia in rats, newer studies have reported that oral administration of leaves to normal mice did not affect glucose homeostasis.
Gentil (2006) examined the antibacterial activity of an ethyl acetate fraction extracted from the leaves of Arctium lappa L., solubilized in propylene glycol (concentration not known).
Antioxidative effects and
Kardašová and Machová (2006) isolated eleven polysaccharides including from the leaves of Arctium lappa L. The polysaccharides were investigated for their ability to inhibit peroxidation of soybean lecithin liposomes by OH radicals. The antioxidant activity value of the polysaccharide from the leaves of Arctium lappa L. (31.3 x
Activity of preparations from the seeds:
Platelet Activating Factor (PAF) antagonism
Platelet Activating Factor (PAF) induces platelet aggregation. In 1992, Iwakami tested the inhibitory effects of the extracts of different plants. Lignans in the seeds of Arctium lappa L. (arctigenin, lappaol A and C) have been found to inhibit the binding of platelet activating factor to rabbit platelets (74% inhibition at 200 μg/ml hot aqueous extract of the seeds) (Blaschek 1998, Iwakami 1992).
In 2008, Xu studied the possible hypoglycaemic effect, effect on glucose tolerance and effect on serum insulin of Fructus Arctii (8.0% w/w) in diabetic and normal animal models. Experimental diabetes was induced in mice with a single injection of alloxan (90 mg/kg body weight), which is similar to diabetes type I.
An ethanolic extract from the fruit of Arctium lappa L. inhibited the growth of Aspergillus parasiticus. Two percent of Arctium lappa L. (part of the plant not specified) was used in an enriched medium, which was inoculated with spores and incubated at 28°C for 9 days. In the presence of Arctium lappa L., no sporulation of Aspergillus parasiticus occurred (Bahk and Marth 1983).
Antioxidative effects and
According to Knott (2008), natural Arctium lappa L. fruit extract (no specifications given) may improve clinical signs of ageing skin. In vitro studies on human dermal fibroblasts and monocyte- derived dendritic cells showed that pure arctiin stimulates collagen synthesis and decreases
Studies in tumor models
A 70% ethanol extract from Fructus Bardanae showed potent antiproliferative activity against B cell hybridoma cells (MH60). The active ingredients were
According to Ishihara (2006), hyperthermia is an effective option for cancer therapy, complementary to chemotherapy or radiotherapy. However, cancer cells may develop thermotolerance. A specific inhibitor of HSP’s (Heat Shock Proteins) in cancer cells would be useful, since it is critical to prevent the induction of thermotolerance, when hypertermia is used to treat cancer. Ishihara used mammalian cells and reported that a methanolic extract from the fruits of Arctium lappa L. (100 µg/ml) suppressed the expression of HSP, which was induced by heat shock. Further investigation identified arctigenin as the active component in the extract (100 µM). Further experiments showed that not only the 100 µg/ml extract and 100 µM arctigenin but also a 50 µg/ml extract and 50 µM arctigenin suppressed the synthesis of HSP70. Arctiin was not found to have an inhibitory effect.
According to Awale (2006), targeting
μg/ml. Arctigenin was identified as the primary compound responsible for such preferential cytotoxicity.
Activity of preparations from the root:
Arctium lappa L. root may contain a desmutagenic factor with a molecular weight >300 000, which might be a
Arctium lappa L. reduced the mutagenicity to Salmonella typhimurium (TA98, TA100) of mutagens (not specified) both requiring and not requiring S9 metabolic activation. A
Antioxidative effects and
Lin (2002) induced liver damage with ethanol and CCl4. When administering Arctium lappa L. extract orally to rats, there was an improvement of the biochemical parameters. A normal saline solution of a dry extract with water of Arctium lappa L. roots was administered to the rats (300 mg/kg). The hepatoprotective mechanism of Arctium lappa L. may be linked to its antioxidant activity, which decreases the oxidative stress of hepatocytes.
Di Mambro (2005) has considered that topical use of antioxidants can protect and possibly correct oxidative skin damage by neutralizing free radicals. The antioxidant effect of an extract of a mixture of Arctium lappa L. root, Glycyrrhiza glabra L. and Symphytum officinale L. (at final concentrations of 0.125, 0.25, 0.50, 1.0, 2.0 and 4.0 µl/ml) was evaluated by Di Mambro (2005) as well as the inhibition of lipid peroxidation, induced by Fe2+. The antioxidant effect was measured by evaluating their
Abdominal angiostrongyliasis in humans is caused by the parasite Angiostrongylus costaricensis. The effect of an aqueous extract of the root of Arctium lappa L. (1:10 m/v) on the evolution of intestinal lesions induced by this parasite was evaluated in mice (500 mg/kg) by Fante (2008). These researchers concluded Arctium lappa L. is not useful for humans affected by abdominal angiostrongyliasis, since the aqueous extract of Arctium lappa L. did not interfere with disease progression and did not protect against the lesions induced by Angiostrongylus costaricensis in mice.
Activity of Arctium lappa in general:
Arctium lappa L. (different parts of the plant) is used for the treatment of various infectious diseases. This antimicrobial activity has been associated with the positive effects of Arctium lappa L. on kidney diseases: nephritis and chronical glomerulonephritis (Blaschek 1998). Its antifurunculous effect may be explained the same way (Barnes 2007).
The antimicrobial activity is attributed to the polyacetylene constituents, although only traces have been found in the dried herb. Furthermore, arctiopicrin shows antibiotic activity against
Activity of Arctium lappa in mixtures:
‘Essiac’2 (see II.3.1.) a formula that consists of four herbal substances ( Arctium lappa L., Rheum palmatum L., Rumex acetosella L. and Ulmus rubra L.) was tested. The preparation is only partially characterised.
Indication: cancer treatments but no convincing clinical evidence is available (Capasso 2003, Ulbricht 2009).
‘Essiac’ has been reported to inhibit cell proliferation and to induce differentiation in human prostate cancer cell lines in vitro. Leonard (2006) has indicated that ‘Essiac’ has potent antioxidant and DNA- protective properties.
The results of their study demonstrate that ‘Essiac’ scavenges OH radicals, O2– radicals and radicals produced by the RAW264.7 cellular reaction with Cr(VI). ‘Essiac’ also inhibited lipid peroxidation in cell membranes caused by exposure to OH radicals and inhibited DNA damage due to OH radicals produced by the Fenton reaction (Leonard 2006).
Kulp (2006) have reported that ‘Essiac’ can stimulate the in vitro growth of human breast cancer cells through estrogen receptor mediated as well as estrogen receptor independent mechanisms of action. No further details about concentration are given. Moreover, Essiac is a mixture.
According to Tai and Cheung (2005),
Bennett (2004), however, showed that
Miscelaneous effects in general:
–Positive effects on nephrosis (fructus Bardanae) (Blaschek 1998).
–Effect against urolithiasis: This effect has been investigated by Grases (1994) using female Wistar rats. They concluded that beneficial effects of a.o. Arctium lappa L. on urolithiasis can be attributed to some disinfectant action.
–Diuretic effect (Blaschek 1998).
The above mentioned effects are described without further specification of the extracts or compounds used.
3.2. Overview of available pharmacokinetic data regarding the herbal substance(s), herbal preparation(s) and relevant constituents thereof
In vitro data:
To investigate the metabolism of arctiin, an experiment with gastric juice (pH
2 Essiac is a common name for complex plant mixtures. By the general us of the name, some confusion about the composition exists and the translation of pharmacological activities into practice remains difficult (Ulbricht 2009).
mainly followed by
In 2003, another in vitro investigation demonstrated that after incubation of arctiin with a human fecal suspension, not only
In vivo data:
200 mg arctiin/kg was administered to rats. One hour after administration, arctigenin was detected in serum. Four hours after administration, arctigenin reached its maximal serum concentration, and four hours later arctigenin was not detectable anymore. Neither arctiin nor
Figure 7: Possible pathway for the transformation of actiin (1) by human intestinal bacteria (Xie 2003).
Pharmacokinetic interactions with other medicinal products
In vitro data:
An ethanolic (55% v/v ethanol:water) extract of Arctium lappa L. root was tested for possible inhibition of CYP3A4, CYP19 and CYP2C19. Chlorogenic acid was used as a marker substance in the extracts.
Finally, the activity of an equivalent of 800 µg herbal substance was tested against 2 ng of ketoconazole.
Among 10 plant extracts tested, the extract from the root of Arctium lappa L. was only a weak inhibitor of CYP3A4 (10th place on 10), CYP19 (9th place on 10) and CYP2C19 (4th place on 4). There were
3.3. Overview of available toxicological data regarding the herbal substance(s)/herbal preparation(s) and constituents thereof
Carcinogenicity data on the roots of Arctium lappa L. come from a study by Hirono (1977). Six male and six female rats were treated with a diet containing 33% of roots of Arctium lappa L. for 120 days. No tumors were detected in any animal (De Smet 1993).
Matsui reported no affection on fertility of female mice when injected twice a day for five days subcutaneously with an extract of Arctium lappa L. This extract was prepared by boiling unspecified plant parts in water (De Smet 1993).
No tests on preparations from A. lappa, root have been performed. Aqueous and methanolic extracts from fruits of Arctium lappa L. were screened for mutagenicity in Salmonella typhimurium strains TA 98 and TA 100 and Bacillus subtilis strains H17 Rec+ and M45
Yamamoto (1982) tested an aqueous or methanolic extract from Arctium fruits in Salmonella typhimurium TA 98 and TA100 in the absence or presence of rat liver
In vivo studies have shown that fresh or boiled plant juice from Arctium lappa L. may cause a significant reduction in
The relevance of those studies for the assessment of preparations of the root is unclear.
3.4. Overall conclusions on
Arctium lappa L. is recommended in various conditions, mostly based on
No safety concerns are originating from the available data on the pharmacological profile.
From in vitro and in vivo experiments in an intestinal environment there is evidence for phase II kinetic activity of actiin. From in vivo experiments (rats) Tmax for arctigenin and excretion parameters could be determined. These data have no relevance for the traditional use of A. lappa, radix. The reported actions on the
Very limited studies did not result in any signs of in vivo carcinogenicity (rats). Because studies did focus on other parts of the plant, the genotoxicity and toxicity on reproduction cannot be fully assessed for the root and
4. Clinical Data
4.1. Clinical Pharmacology
4.1.1. Overview of pharmacodynamic data regarding the herbal substance(s)/preparation(s) including data on relevant constituents
No data available.
4.1.2. Overview of pharmacokinetic data regarding the herbal substance(s)/preparation(s) including data on relevant constituents
No data available.
4.2. Clinical Efficacy
4.2.1. Dose response studies
No data available.
4.2.2. Clinical studies (case studies and clinical trials)
No data available.
‘Essiac’ (see section 1.1 and 1.2) has been used for
‘Essiac’ may contain a lot of preparations, usually insufficiently specified, which provides additional confusion.
4.2.3. Clinical studies in special populations (e.g. elderly and children)
No data available.
4.3. Overall conclusions on clinical pharmacology and efficacy
There is a lack of clinical research assessing the effects of Arctium lappa L. in monopreparations and controlled clinical trials are absent. However, there is a
5. Clinical Safety/Pharmacovigilance
5.1. Overview of toxicological/safety data from clinical trials in humans
No data available.
5.2. Patient exposure
No exact data on patient exposure are available. However, the
5.3. Adverse events and serious adverse events and deaths
The rough hairs of the
Rodriguez (1995) reported three cases of contact dermatitis caused by Arctium lappa L. plasters applied for
parts may be involved. It should be noted that urticaria has been reported after the topical use of the leaves (see 1.1), however this reaction has been attributed as a “beneficial effect” (Leclerc 1966). Allergic reactions are likely to be associated with the presence of
The rough hairs of Arctium lappa L. fruit may hook on clothing. Within the bur and attached to seed pods, Arctium lappa L. has thousands of tiny barbed needles. If these needles imbed in the conjunctiva, it may cause serious ocular reactions. Because they are very small, they are often missed by doctors who are not familiar with the plant. An Arctium lappa L. caused ophthalmic irritation can be recognised by the presence of linear scratch marks running in random directions on the cornea. The needle tip causes direct abrasion every time the eyelid moves, thus causing serious damage. The toxicity of a water soluble noxious agent may also play a role, which is suggested from animal tests. An aqueous extract caused severe reactions, which were not observed following the injection of an oily extract (De Smet 1993).
For dogs (especially
Serious adverse events and deaths
Only one case of serious allergy to Arctium lappa L. is known. A
Some remarks have to be made on this case. Apart from burdock, the patient consumed also carrot and curry with his rice. Skin prick tests revealed an allergic predisposition for burdock but also for carrot (not for curry). Boiled as well as raw plant materials were used for allergy testing (Sasaki 2003).
Atropine like poisoning
De Smet (1993) mentions anticholinergic poisoning, due to adulteration or contamination with belladonna root. This is also reported by Barnes (2007). The patient exhibited symptoms of atropine- like poisoning after ingestion of Arctium lappa L. tea. Atropine is not a constituent of Arctium lappa L., but analysis showed that the tea was contaminated with an herbal source of solanaceous alkaloïds, possibly belladonna root.
Contamination with Atropa belladonna L. is reported in many handbooks. Older roots and roots that show a blue colour after treatment with iodine solutions (indicator for Radix Belladonnae) may not be used for this reason. According to Blaschek (1998), also substitution with Symphytum officinale L. or
Rumex obtusifolius L. may also occur.
5.4. Laboratory findings
No data available.
5.5. Safety in special populations and situations
It has been reported that Arctium lappa L. may cause uterine stimulation and therefore the use of Arctium lappa L. should be avoided during pregnancy and lactation (Barnes 2007). However, no case reports or pharmacological studies that would support this assumption were found.
Intrinsic (including elderly and children) /extrinsic factors
According to Barnes (2007), there are no documented interactions. Nevertheless, the authors warn with respect to the potential interactions with other medicines, particularly those with similar or opposing effects. Apart from this general statement, no clinical evidence is available; consequently, no warning should be included in the monograph.
Arctium lappa L. has also been associated with diuretic effects. Nothing is known about possible additive effects when Arctium lappa L. is taken concomitantly with diuretic drugs. No statement is needed in the monograph.
Tinctures of Arctium lappa L. may contain high concentrations of alcohol and may lead to vomiting if used with disulfiram. This aspect is covered in the monograph by a general warning on ethanol containing preparations.
Use in pregnancy and lactation
In vivo uterine stimulant action has been reported. In view of this and the lack of toxicity data, the use of burdock during pregnancy and lactation is not recommended (Barnes 2007). However, as neither case reports on toxicity nor pharmacological studies demonstrating an effect on the uterus have been found, the standard warning has been included in the monograph; i.e. that the use is not recommended due to insufficient data.
No case of overdose has been reported.
Drug abuse has not been reported.
Withdrawal and rebound
Effects on ability to drive or operate machinery or impairment of mental ability
No studies on the effect on the ability to drive and use machines have been performed.
5.6. Overall conclusions on clinical safety
Under the conditions of use mentioned in the monograph A. lappa, root can be considered as safe. There is evidence for local irritation, due to the barbed needles on the bur of the plant. These are not relevant for the root. Allergic reactions may occur; probably due to
6. Overall conclusions
Some constituents of Arctium lappa L. are well investigated and documented. Many authors have described various pharmacological activities of Arctium lappa L. seed extracts or isolated constituents in animals or in vitro.
Despite their long tradition and their widespread use, there are no data available from controlled clinical studies using herbal preparations containing Arctium lappa L. root. In conclusion, Arctium lappa L. root preparations can only be considered for traditional use. More clinical research is needed to confirm the pharmacological properties.
The monograph on Arctium lappa L. is restricted to the root as there is no documented use of medicinal products from the leaves and there is insufficient evidence on the traditional use of the seeds.
There is no Arctii lappae radix monograph in the European Pharmacopoeia. The most recent official monograph comes from DAC 2008. Contamination with Atropa belladonna root has been mentioned, as well as exchanges with Symphytum officinale L. and Rumex obtusifolius L.
Conclusion: Contamination or adulteration of Arctium lappa root with serious health risks are possible and need to be excluded by adequate quality control in the framework of a registration procedure.
There are very few side effects due to root preparations. The main risks are allergic reactions associated with
Conclusion: Preparations of Arctium lappa root can be considered as safe but no list entry can be prepared.
Therapeutic indications for herbal preparations of Arctium lappa root as given in the monograph are based on more than 30 years traditional use in Europe but not supported by validated clinical experience. Even open clinical observations are missing. The use in seborrhoeic skin conditions (ICD L21, ATC D11AX) in urinary complaints and in stimulation of appetite is plausible on the basis of its
Conclusion: Traditional therapeutic use of Arctium lappa is safe under the conditions addressed in the monograph.