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A review of the pharmacological effects of Arctium lappa (burdock)

Authors:
  • State Key Laboratory of Chinese Medicine and Molecular Pharmacology,Shenzhen,China

Abstract and Figures

Arctium lappa, commonly known as burdock, is being promoted/recommended as a healthy and nutritive food in Chinese societies. Burdock has been used therapeutically in Europe, North America and Asia for hundreds of years. The roots, seeds and leaves of burdock have been investigated in view of its popular uses in traditional Chinese medicine (TCM). In this review, the reported therapeutic effects of the active compounds present in the different botanical parts of burdock are summarized. In the root, the active ingredients have been found to "detoxify" blood in terms of TCM and promote blood circulation to the skin surface, improving the skin quality/texture and curing skin diseases like eczema. Antioxidants and antidiabetic compounds have also been found in the root. In the seeds, some active compounds possess anti-inflammatory effects and potent inhibitory effects on the growth of tumors such as pancreatic carcinoma. In the leaf extract, the active compounds isolated can inhibit the growth of micro-organisms in the oral cavity. The medicinal uses of burdock in treating chronic diseases such as cancers, diabetes and AIDS have been reported. However, it is also essential to be aware of the side effects of burdock including contact dermatitis and other allergic/inflammatory responses that might be evoked by burdock.
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A review of the pharmacological effects of Arctium Lappa (burdock)
Yuk-Shing Chana, Long-Ni Chenga, Jian-Hong Wua, Enoch Chana, Yiu-Wa Kwanb, Simon Ming-Yuen
Leec, George Pak-Heng Leungd, Peter Hoi-Fu Yua, Shun-Wan Chana
a State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Department of Applied
Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong
b Institute of Vascular Medicine, School of Biomedical Sciences, Faculty of Medicine, The Chinese
University of Hong Kong, Hong Kong
c Institute of Chinese Medical Sciences, University of Macau, Av. Padre Tomas Pereira S.J., Taipa,
Macau, PR China
d Department of Pharmacology and Pharmacy, The University of Hong Kong, Hong Kong
Correspondence
*Dr. George Pak-Heng Leung, Department of Pharmacology and Pharmacy, The University of Hong
Kong, Hong Kong SAR, PR of China. E-mail address: gphleung@hkucc.hku.hk; Phone:
+852-28192861; Fax: +852-28170859
*Dr. Shun-Wan Chan, State Key Laboratory of Chinese Medicine and Molecular Pharmacology,
Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University,
Hong Kong SAR, PR of China. E-mail address: bcswchan@polyu.edu.hk; Phone: +852-34008718; Fax:
+852-23649932
This is the Pre-Published Version.
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Abstract. Arctium lappa, commonly known as burdock, is being
promoted/recommended as a healthy and nutritive food in Chinese societies. Burdock
has been used therapeutically in Europe, North America and Asia for hundreds of
years. The roots, seeds and leaves of burdock have been investigated in view of its
popular uses in Traditional Chinese Medicine (TCM). In this review, the reported
therapeutic effects of the active compounds present in the different botanical parts of
burdock are summarized. In the root, the active ingredients have been found to
“detoxify” blood in TCM term and promote blood circulation to the skin surface,
improving the skin quality/texture and curing skin diseases like eczema. Antioxidants
and anti-diabetic compounds have also been found in the root. In the seeds, some
active compounds possess anti-inflammatory effects, and potent inhibitory effects on
the growth of tumors such as the pancreatic carcinoma. In the leaf extract, the active
compounds isolated can inhibit the growth of micro-organisms in the oral cavity. The
medicinal uses of burdock in treating chronic diseases like cancers, diabetes and
AIDS have been reported. However, it is also essential to be aware of the side-effects
of burdock including contact dermatitis and other allergic/inflammatory responses
that might be evoked by burdock.
Key Words: Arctium lappa (burdock); Traditional Chinese Medicine;
Anti-inflammatory; Pharmacology
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Introduction
Starting from the end of twentieth century, the majority of people in developed
countries are becoming wealthier and more health conscious. They tend to spend extra
money on different functional foods or nutraceuticals in order to pursue healthy aging.
Natural products have been used in the treatment of various chronic human
pathological conditions because they are rich in antioxidants (Guo et al., 2008). In
traditional Chinese medicine (TCM), it is believed that food and medicine stem from
the same origin but with different uses and applications (Chan et al., 2010). Therefore,
it is common for Chinese people to incorporate different medicinal herbs into their
diet to produce various “healthy” food recipes in order to achieve better taste, more
attractive appearance and improved texture of the food and most importantly to
improve health.
Burdock, a perennial herb in the family of Compositae, stores most of its
nutrients during the first year. These nutrients are then used for the flower-blooming
process afterwards. The plant, which can be found worldwide, has been cultivated as a
vegetable for a period of long time in Asia (Morita et al., 1993). Burdock, called
“Niubang” in Chinese, has been used in China and some Western countries for over
3000 years and its therapeutic uses were documented in The Compendium of Materia
Medica (Bencao gangmu in Chinese) written by Li Shizhen, the most
famous/important figure in the history and development of TCM, during the Ming
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dynasty (Yu et al., 2003).
Burdock is traditionally used to treat diseases such as sore throat and infections
such as rashes, boils and various skin problems. In TCM understanding, these
pathological events are mainly due to the accumulation of toxin in the body. The dried
root of one-year old burdock (Figure 1) is the major part used for different therapeutic
purposes although burdock leaves and fruit/seeds are also used. It is suggested that the
root of this herb is particularly effective and invaluable in eliminating heavy metals
from our body. Therefore it appears to have the function of draining toxins in terms of
TCM theory (Yu et al., 2003).
In contrast to some famous and expensive medicinal herbs such as Ganoderma
lucidum (Lingzhi) and Panax ginseng (Ginseng) that have been used for a long period
of time with their rich and highly acclaimed nutritional values, burdock possesses
various therapeutic values but is still sold at a low price. Moreover, it can be easily
cultivated. In light of the aforementioned properties of this herb, the aim of this
review is to summarize the currently available scientific information on burdock so as
to provide a comprehensive overview of this herb.
Active ingredients found in burdock
With the advancement of different state-of-the-art analytical techniques, more
active ingredients of burdock have been identified over the last decade (Park et al.,
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2007). The major active ingredients isolated from this herb are: tannin, arctigenin,
arctin, beta-eudesmol, caffeic acid, chlorogenic acid, inulin, trachelogenin 4,
sitosterol-beta-D-glucopyranoside, lappaol and diarctigenin (Table 1). Apart from
these compounds, burdock also contains various common nutrients (Table 2).
Pharmacological effects
The extracts from different parts of burdock have long been considered good for
health. They help enhance the body’s immune system and improve metabolic
functions (Lin et al., 2002). Biological activities and pharmacological functions
reported for the Arctium species include anti-inflammatory, anti-cancer, anti-diabetic,
anti-microbial and antiviral activities.
Anti-inflammatory effects
Inhibition of inducible nitric oxide synthase (iNOS) expression and nitric oxide
(NO) production, suppression of pro-inflammatory cytokine expression, inhibition of
the nuclear factor-kappa B (NF-κB) pathway, activation of antioxidant enzymes and
scavenging of free radicals are the essential mechanisms of burdock’s
anti-inflammatory action.
The extract of burdock has been shown to exhibit anti-inflammatory response by
inhibiting degranulation and release of cysteinyl leukotrienes (Cys-LTs) by peripheral
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blood mononuclear cells (PBMCs). Cys-LTs are synthesized inflammatory mediators
as histamine and prostaglandins. The blockade of Cys-LT is regarded as inhibition of
inflammatory response. Also, the extract of burdock significantly inhibited acute
mouse ear edema due to induced allergic response. Therefore, there has been evidence
suggesting that burdock has significant anti-inflammatory effect (Knipping et al.,
2008).
Lappaol F, diarctignin and arctigenin, found in the seeds or leaves of burdock,
are lignans that can inhibit NO production. The excessive production of NO by iNOS
(EC1.14.13.39) is involved in various inflammatory diseases such as rheumatoid
arthritis, autoimmune disease, chronic inflammation and atherosclerosis. Therefore,
inhibition of NO production by iNOS in macrophages are potential treatments for
certain inflammatory diseases (Wang et al., 2007). Lappol F and diarctignin strongly
inhibited NO production in lipopolysccachride (LPS)-stimulated murine macrophage
RAW264.7 cells with IC50 values of 9.5 and 9.6 µM, respectively (Park et al., 2007).
Further study elucidated that diarctigenin could directly target NF-κB-activating
signaling cascade by direct inhibition of the DNA binding ability of NF-κB and
inhibition of NF-κB-regulated iNOS expression (Kim et al., 2008).
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, potently inhibited
iNOS expression and NO production through suppression of NF-κB activation and
inhibition of I-κBα phosphorylation and p65 nuclear translocation in LPS-activated
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macrophages (Cho et al., 2002). In addition, arctigenin strongly inhibited the
expression of pro-inflammatory cytokines tumor necrosis factor-α (TNF-α) and IL-6,
in LPS-stimulated RAW264.7 cells, THP-1 human monocyte-macrophage and
differentiated human macrophage U937 (Cho et al., 2002; Zhao et al., 2009). Further
study showed that arctigenin-induced inhibition of TNF-α production might be
mediated by arctigenin’s potent inactivation of mitogen-activated protein (MAP)
kinases including ERK1/2, p38 kinase and JNK through the inhibition of MAP kinase
kinase (MKK) activity, leading to inactivation of activator protein-1 (AP-1) (Cho et
al., 2004; Zhao et al., 2009).
On the other hand, expression of inflammation-associated cyclooxygenase 2
(COX-2) and formation of prostaglandin E2 (PGE2) are the results of increased NO
production. Inhibitor of COX-2 causes a potent inflammatory effect, since the
prostaglandin family is associated with the onset of inflammation. The methanolic
extract of burdock has been proven to be effective in inhibiting the expression level of
COX-2 mRNA. Therefore the anti-inflammatory effect of Burdock is attributed to the
lowered PGE2 release (Wang et al., 2007).
In view of the inflammatory processes, inflammation has usually been
investigated together with the pathway of free radicals. There have been a lot of
studies on the association between free radicals, oxidative stress and inflammation
(Weber et al., 2005; Abreu et al., 2006; Pontiki et al., 2006). Instead of just looking at
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the action of drugs/herbs on pro-inflammatory cytokines or/and other inflammatory
mediators, their free radical scavenging capacities should also be considered. There
are increasing studies focusing on both the effects of pro-inflammatory signaling and
free-radical scavenging capacity of individual drug/herb, which may contribute to the
resultant anti-inflammatory effect of them (Lee et al., 2007). Recent studies have
demonstrated that burdock’s anti-inflammatory characteristics on
carrageenan-induced rat paw edema and carbon tetrachloride (CCl4)-induced
hepatotoxicity. The carrageenan-induced rat paw edema assay is a widely used model
for acute inflammatory testing. Burdock has shown to have significant inhibition on
the growth of rat paw edema in a dose-related manner, thus suggesting some
significant anti-inflammatory activities of burdock (Lin et al., 1996). Lin et al (1996)
demonstrated the antioxidant power of burdock extract by detecting the signal
intensities of 5,5-dimethyl-1- pyrroline-N-oxide (DMPO)-OOH in relation to
superoxide dismutase (SOD) concentration. For hepatoprotective effect, burdock was
shown to suppress the CCl4 or acetaminophen-intoxicated mice as well as the ethanol
plus CCl4-induced rat liver damage. The underlying hepatoprotective ability of
burdock could be related to the decrease of oxidative stress on hepatocytes by
increasing glutathione (GSH), cytochrome P-450 content and NADPH-cytochrome c
reductase activity and by decreasing malondialdehyde (MDA) content, hence
alleviating the severity of liver damage based on histopathological observations (Lin
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et al., 2000; Lin et al., 2002). In summary, the anti-inflammatory action of burdock is
attributed to its high free radical scavenging capacities and antioxidant activity.
Anti-cancer activities
During the development of tumors, very large amounts of nutrients (oxygen and
nutrients) are required in order to sustain the rapid proliferation of the tumor cells.
However, tumor cells can still survive under extreme conditions like low oxygen and
low carbohydrate availability due to their relatively high tolerance to hostile
environment. Arctigenin, an active compound found in the seeds of burdock, has the
ability to eradicate nutrient-deprived cancer cells (Awale et al., 2006). In addition to
its board spectrum of activities on different cancer cell lines, e.g. PANC-1 and AsPC-1,
arctigenin seems to exhibit a highly preferential cytotoxicity to cancer cells that are
bathed in glucose-deprived conditions (Awale et al., 2006). This is because arctigenin
has a potent inhibitory effect on the phosphorylation of Akt (Guo et al., 2008), which
is stimulated under glucose-deprived conditions. Hence, the rate of glucose formation
in cancer cells is decreased, which in turn leads to cell death due to a lack of nutrients
(Awale et al., 2006).
Protection of cells from harmful substances can greatly reduce the chance of
tumor formation and thus suppresses cancer cell proliferation. Flavoniod-type
anti-oxidants and some other active polyphenol antioxidants found in the root of
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burdock may account for the suppressive effects on cancer metastasis (Tamayo et al.,
2000). It has been shown that extracts of the root protect cells from toxic substances
and lower the mutations of cells (Miyamoto et al., 1993)
Tannin, a phenolic compound, is one of the most common active compounds
found in the root of burdock. It induces macrophage responses, inhibits tumor growth,
and possesses immuno-modulatory properties (Miyamoto et al., 1993). However,
tannin is potentially toxic in nature. It may cause stomach upset and at high
concentrations it has some dangerous side effects such as nephrotoxicity and hepatic
necrosis (Miyamoto et al., 1993). Therefore, the use of tannin should be carefully
monitored.
Anti-diabetic activity
Burdock has been used to treat diabetes by TCM practitioners. Several studies
have suggested that the root or/and fruit are possible parts with hypoglycemic effect.
Sitosterol-beta-D-glucopyranoside is considered to be the most potent and efficacious
substance among the large profile of active compounds found in the root of burdock.
It has demonstrated potent inhibitory effects on alpha glucosidase activities. Alpha
glucosidases are involved in the processing of glycoprotein and glycogenolysis.
Inhibitors of glycosidase are potential therapeutic agents in treating diabetes mellitus
and obesity (Mitsuo et al., 2005). In addition, gamma-glucoside-fructose ester, also
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known as inulin, can help to regulate blood glucose levels. Inulin, a natural
carbohydrate present in the root of burdock, can act on cell surface receptors to keep
the blood glucose level constant, therefore improving the tolerance to high glucose
level. Also, the production of short chain fatty acids is also increased (Silver and
Krantz Jr, 1931). The anti-diabetic activity of total lignan from the fruit of burdock
has been studied in a model of alloxan-induced diabetes in mice and rats. It has been
proven that total lignan from burdock is a safe anti-diabetic agent and may help
prevent diabetic complications (Xu et al., 2008).
Anti-microbial and antiviral activity
It has been reported that the lyophilized extract of the leaves of burdock exhibits
anti-microbial activity against oral micro-organisms and is the most effective against
bacteria related to endodontic pathogens such as: Bacillus subtilis, Candida albicans,
Lactobacillus acidophilus and Psedomonas aeruginosa (Pereira et al., 2005).
Chlorogenic acid isolated from the leaves also have shown restraining effects on
Escherihchia coli, Staphylococcus aureus, and Micrococcus luteus (Lin et al., 2004).
Therefore, the leaves of Burdock may be useful in treating tooth/gum diseases that are
related to micro-organisms in the oral cavity. It is also a potential topical remedy for
skin problems such as eczema, acne, and psoriasis. In addition, the polyacetylene
ingredients extracted from the root of burdock also possess potent anti-bacterial and
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anti-fungal activities (Takasugi et al., 1987).
Constituents of burdock have also demonstrated antiviral activity. Phenolic
constituents like caffeic acid and chlorogenic acid possess strong inhibitory effect on
herpesvirus (HSV-1, HSV-2) and adenovirus (ADV-3, ADV-11) (Chiang et al., 2002).
Arctigenin, one of the lignanoid ingredients, has demonstrated activities against
human immunodeficiency virus type-1 (HIV-1) both in vivo and in vitro (Schroder et
al., 1990; Eich et al., 1996). These suggest potential uses of these promising natural
compounds isolated from burdock to treat infection by these viruses, especially HIV.
Other activities
Lignans isolated from burdock have been shown to be potent platelet-activating
factor (PAF) receptor antagonists, calcium antagonists and hypotensive agent
(Ichikawa et al., 1986; Iwakami et al., 1992). Arctiin, a lignin isolated from burdock
seeds, has protective effect against 2-amino-1-methyl-6-phenylimidazo [4,5-b]
pyridine (PhIP)-induced carcinogenesis (Hirose et al., 2000). Besides arctiin,
polyphenolics in burdock, especially caffeic acid and chlorogenic acid, also have
significant anti-mutagenic activity, and the anti-mutagenic capacity of the extract of
burdock has a positive correlation with polyphenolic content (Liu and Tang, 1997).
The anti-decrepitude effect of burdock has also been noted. Li et al. (2004) have
eluciated that the main mechanism of burdock’s anti-decrepitude effect involves
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improvement of SOD activity and reduction of MDA and lipofuscin content.
Furthermore, burdock has been used as an adjunctive therapy or alternative medicine
for the treatment of gout, hypertension, arteriosclerosis and other inflammatory
disorders (Li et al., 2004).
However, burdock has also been reported to have side-effects. The most
commonly reported side-effect of burdock is the induction of contact dermatitis.
Patients suffered from contact dermatitis after extended topical use of the root oil of
burdock. Another reported case was a massage liniment containing burdock extracts
had caused contact dermatitis (Paulsen, 2002). There was also case of development of
anaphylaxis due to burdock consumption. A Japanese man had developed urticaria 10
times after consuming boiled burdock as food, with redness occurring over his entire
body. In addition, he experienced difficulties in breathing an hour after consuming
boiled burdock. It was found that this patient had a low blood pressure of 64/29
mmHg. He was diagnosed to be in anaphylactic shock (Sasaki et al., 2003). Therefore,
it seems to be a misconception that herbs that are of natural sources have less
side-effect comparing to drugs. It was suggested that adverse clinical effects for
herbal drugs range from allergic skin reactions, the Stevens-Johnson syndrome and
photosensitization to toxic dermatosis. Since most herbs are readily accessible by the
general public, increasing number of cases of herb-induced adverse effects is expected
(Niggemann and Gruber, 2003). Therefore, public awareness about the possibility of
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adverse effects of medicinal herbs shall be enhanced.
Conclusions
Burdock contains many active ingredients (isolated from different parts of the plant)
that have been shown to possess many therapeutic effects for the treatment of various
diseases. Multiple reports in the literature have demonstrated a wide range of possible
clinical uses of this herb because of its anti-inflammatory, anti-tumor/cancer,
anti-diabetic, anti-microbial and antiviral effects. In conclusion, the medicinal use of
burdock in treating chronic diseases like cancers, diabetes and AIDS is promising.
However, it is also essential to be aware of the side-effects of burdock including
contact dermatitis and other allergic/inflammatory responses that might be evoked by
burdock. It is expected that further investigations will lead to a better understanding of
some other roles that Arctium lappa plays in preventing and treating of human
diseases, as well as the potential adverse effects and toxicity of the herb. That could
provide us with more information on the beneficial effect and the potential risk of
consuming burdock as a functional food.
Acknowledgments. This research was financially supported by the Department of
Applied Biology and Chemical Technology, The Hong Kong Polytechnic University
and State Key Laboratory of Chinese Medicine and Molecular Pharmacology,
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Shenzhen. Special thanks go to Ms. Siu-Hung Tsui and Ms. Josephine Hong-Man
Leung for proofreading and providing critical comments on the manuscript.
References
Abreu, P., Matthew, S., Gonzalez, T., et al. (2006). Anti-inflammatory and antioxidant
activity of a medicinal tincture from Pedilanthus tithymaloides, Life Sci. 78,
1578-1585.
Awale, S., Lu, J., Kalauni, S. K., et al. (2006). Identification of arctigenin as an
antitumor agent having the ability to eliminate the tolerance of cancer cells to
nutrient starvation, Cancer Res. 66, 1751-1757.
Bhat, S. H., Azmi, A. S., and Hadi, S. M. (2007). Prooxidant DNA breakage induced
by caffeic acid in human peripheral lymphocytes: Involvement of endogenous
copper and a putative mechanism for anticancer properties, Toxicol. Appl.
Pharm. 218, 249-255.
Bouayed, J., Rammal, H., Dicko, A., et al. (2007). Chlorogenic acid, a polyphenol
from Prunus domestica (Mirabelle), with coupled anxiolytic and antioxidant
effects, J. Neurol. Sci. 262, 77-84.
Bralley, E., Greenspan, P., Hargrove, J. L., et al. (2008). Inhibition of hyaluronidase
activity by select sorghum brans, J. Med. Food. 11, 307-312.
Chan, E., Wong, C. Y. K., Wan, C. W., et al. (2010). Evaluation of Anti-Oxidant
Capacity of Root of Scutellaria baicalensis Georgi, in Comparison with Roots
of Polygonum multiflorum Thunb and Panax ginseng CA Meyer, Am J
Chinese Med. 38, 815-827.
Chen, F. A., Wu, A. B., and Chen, C. Y. (2004). The influence of different treatments
on the free radical scavenging activity of burdock and variations of its active
components, Food Chem. 86, 479-484.
Chiang, L. C., Chiang, W., Chang, M. Y., et al. (2002). Antiviral activity of Plantago
major extracts and related compounds in vitro, Antivir. Res. 55, 53-62.
Cho, M. K., Jang, Y. P., Kim, Y. C., et al. (2004). Arctigenin, a phenylpropanoid
dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via
potent MKK inhibition: the role in TNF-alpha inhibition, Int.
Immunopharmacol. 4, 1419-1429.
Cho, M. K., Park, J. W., Jang, Y. P., et al. (2002). Potent inhibition of
lipopolysaccharide-inducible nitric oxide synthase expression by
dibenzylbutyrolactone lignans through inhibition of I-kappa B alpha
phosphorylation and of p65 nuclear translocation in macrophages, Int.
16
Immunopharmacol. 2, 105-116.
Eich, E., Pertz, H., Kaloga, M., et al. (1996). (-)-Arctigenin as a lead structure for
inhibitors of human immunodeficiency virus type-1 integrase, J. Med. Chem.
39, 86-95.
Gao, Y., Dong, X., Kang, T. G., et al. (2002). Activity of in vitro anti-influenza virus
of arctigenin. 33, 724-726.
Guo, J. F., Zhou, J. M., Zhang, Y., et al. (2008). Rhabdastrellic acid-A inhibited
PI3K/Akt pathway and induced apoptosis in human leukemia HL-60 cells,
Cell Biol. Int. 32, 48-54.
Hirose, M., Yamaguchi, T., Lin, C., et al. (2000). Effects of arctiin on PhIP-induced
mammary, colon and pancreatic carcinogenesis in female Sprague-Dawley rats
and MeIQx-induced hepatocarcinogenesis in male F344 rats, Cancer Lett. 155,
79-88.
Ichikawa, K., Kinoshita, T., Nishibe, S., et al. (1986). The Ca-2+ Antagonist Activity
of Lignans, Chem. Pharm. Bull. 34, 3514-3517.
Ishihara, K., Yamagishi, N., Saito, Y., et al. (2006). Arctigenin from Fructus Arctii is a
novel suppressor of heat shock response in mammalian cells, Cell Stress
Chaperon. 11, 154-161.
Iwakami, S., Wu, J. B., Ebizuka, Y., et al. (1992). Platelet Activating Factor(Paf)
Antagonists Contained in Medicinal-Plants - Lignans and Sesquiterpenes,
Chem. Pharm. Bull. 40, 1196-1198.
Kim, B. H., Hong, S. S., Kwon, S. W., et al. (2008). Diarctigenin, a Lignan
Constituent from Arctium lappa, Down-Regulated Zymosan-Induced
Transcription of Inflammatory Genes through Suppression of DNA Binding
Ability of Nuclear Factor-kappa B in Macrophages, J. Pharmacol. Exp. Ther.
327, 393-401.
Knipping, K., van Esch, E., Wijering, S. C., et al. (2008). In Vitro and In Vivo
Anti-Allergic Effects of Arctium lappa L, Exp. Biol. Med. (Maywood). 233,
1469.
Lee, C. P., Shih, P. H., Hsu, C. L., et al. (2007). Hepatoprotection of tea seed oil
(Camellia oleifera Abel.) against CCl4-induced oxidative damage in rats, Food
Chem. Toxicol. 45, 888-895.
Li, Y. J., Liu, S. M., Li, S. L., et al. (2004). The Experimental Study of the Effect of
Anti-decrepitude of Arctium lappa L. 15, 545-546.
Li, Y. J., Shi, W., Li, Y. D., et al. (2008). Neuroprotective effects of chlorogenic acid
against apoptosis of PC12 cells induced by methylmercury, Environ. Toxicol.
Phar. 26, 13-21.
Lin, C. C., Lin, J. M., Yang, J. J., et al. (1996). Anti-inflammatory and radical
scavenge effects of Arctium lappa, Am. J. Chin. Med. 24, 127-137.
17
Lin, S. C., Chung, T. C., Lin, C. C., et al. (2000). Hepatoprotective effects of Arctium
lappa on carbon tetrachloride- and acetaminophen-induced liver damage, Am J
Chin Med. 28, 163-173.
Lin, S. C., Lin, C. H., Lin, C. C., et al. (2002). Hepatoprotective effects of Arctium
lappa Linne on liver injuries induced by chronic ethanol consumption and
potentiated by carbon tetrachloride, J. Biomed. Sci. 9, 401-409.
Lin, X. C., Liu, C. Y., Chen, K. S., et al. (2004). Extraction and content comparison of
chlorogenic acid in Arctium lappa L. leaves collected from different terrain
and its restraning bacteria test, Nat. Prod. Res. & Dev. 16, 328-330.
Liu, L., and Tang, L. (1997). Studies on antimutagenicity of Burdock, Acta
Academiae Medicine Nanjing. 4, 343-345.
Matsumoto, T., Hosono-Nishiyama, K., and Yamada, H. (2006). Antiproliferative and
apoptotic effects of butyrolactone lignans from Arctium lappa on leukemic
cells, Planta Med. 72, 276-278.
Mitsuo, M., Nobuo, Y., and Katsuya, T. (2005). Inhibitory compounds of alpha
glucosidase activity from Arctium lappa L, J. Oleo Sci. 54, 589-594.
Miyamoto, K., Nomura, M., Sasakura, M., et al. (1993). Antitumor-Activity of
Oenothein-B, a Unique Macrocyclic Ellagitannin, Jpn. J. Cancer Res. 84,
99-103.
Mizushina, Y., Nakanishi, R., Kuriyama, I., et al. (2006).
beta-sitosterol-3-O-beta-D-glucopyranoside: A eukaryotic DNA polymerase
lambda inhibitor, J. Steroid Biochem. 99, 100-107.
Morita, T., Ebihara, K., and Kiriyama, S. (1993). Dietary Fiber and Fat-Derivatives
Prevent Mineral-Oil Toxicity in Rats by the Same Mechanism, J. Nutr. 123,
1575-1585.
Niggemann, B., and Gruber, C. (2003). Side-effects of complementary and alternative
medicine, Allergy. 58, 707-716.
Pari, L., and Prasath, A. (2008). Efficacy of caffeic acid in preventing nickel induced
oxidative damage in liver of rats, Chem-Biol. Interact. 173, 77-83.
Park, S. Y., Hong, S. S., Han, X. H., et al. (2007). Lignans from Arctium lappa and
their inhibition of LPS-induced nitric oxide production, Chem. Pharm. Bull.
55, 150-152.
Paulsen, E. (2002). Contact sensitization from Compositae-containing herbal
remedies and cosmetics, Contact Dermatitis. 47, 189-198.
Pereira, J. V., Bergamo, D. C., Pereira, J. O., et al. (2005). Antimicrobial activity of
Arctium lappa constituents against microorganisms commonly found in
endodontic infections, Braz. Dent. J. 16, 192-196.
Pontiki, E., Hadjipavlou-Litina, D., Chaviara, A. T., et al. (2006). Evaluation of
anti-inflammatory and antioxidant activities of mixed-ligand Cu(II) complexes
18
of then and its Schiff dibases with heterocyclic aldehydes and
2-amino-2-thiazoline, Bioorg. Med. Chem. Lett. 16, 2234-2237.
Rault-Nania, M. H., Demougeot, C., Gueux, E., et al. (2008). Inulin supplementation
prevents high fructose diet-induced hypertension in rats, Clin. Nutr. 27,
276-282.
Sasaki, Y., Kimura, Y., Tsunoda, T., et al. (2003). Anaphylaxis due to burdock, Int. J.
Dermatol. 42, 472-473.
Schroder, H. C., Merz, H., Steffen, R., et al. (1990). Differential in vitro anti-HIV
activity of natural lignans, Z Naturforsch C. 45, 1215-1221.
Silver, A. A., and Krantz Jr, J. C. (1931). The effect of the ingestion of burdock root
on normal and diabetic individuals a preliminary report, Ann. Intern. Med. 5,
274.
Takasaki, M., Konoshima, T., Komatsu, K., et al. (2000). Anti-tumor-promoting
activity of lignans from the aerial part of Saussurea medusa, Cancer Lett. 158,
53-59.
Takasugi, M., Kawashima, S., Katsui, N., et al. (1987). Studies on Stress
Metabolites .5. 2 Polyacetylenic Phytoalexins from Arctium-Lappa,
Phytochemistry. 26, 2957-2958.
Tamayo, C., Richardson, M. A., Diamond, S., et al. (2000). The chemistry and
biological activity of herbs used in Flor-Essence (TM) herbal tonic and Essiac
(TM), Phytother. Res. 14, 1-14.
Tsuneki, H., Ma, E. L., Kobayashi, S., et al. (2005). Antiangiogenic activity of
beta-eudesmol in vitro and in vivo, Eur. J. Pharmacol. 512, 105-115.
Wang, B. S., Yen, G. C., Chang, L. W., et al. (2007). Protective effects of burdock
(Arctium lappa Linne) on oxidation of low-density lipoprotein and oxidative
stress in RAW 264.7 macrophages, Food Chem. 101, 729-738.
Weber, V., Rubat, C., Duroux, E., et al. (2005). New 3-and 4-hydroxyfuranones as
anti-oxidants and anti-inflammatory agents, Bioorgan. Med. Chem. 13,
4552-4564.
Xia, Z. Q., Costa, M. A., Pelissier, H. C., et al. (2001). Secoisolariciresinol
dehydrogenase purification, cloning, and functional expression - Implications
for human health protection, J. Biol. Chem. 276, 12614-12623.
Xu, Z. H., Wang, X. Y., Zhou, M. M., et al. (2008). The antidiabetic activity of total
lignan from fructus arctii against alloxan-induced diabetes in mice and rats,
Phytother. Res. 22, 97-101.
Yayli, N., Yasar, A., Gulec, C., et al. (2005). Composition and antimicrobial activity
of essential oils from Centaurea sessilis and Centaurea armena,
Phytochemistry. 66, 1741-1745.
Yu, B. S., Yan, X. P., Xiong, J. Y., et al. (2003). Simultaneous determination of
19
chlorogenic acid, forsythin and arctiin in Chinese traditional medicines
preparation by reversed phase-HPLC, Chem. Pharm. Bull. 51, 421-424.
Zhao, F., Wang, L., and Liu, K. (2009). In vitro anti-inflammatory effects of
arctigenin, a lignan from Arctium lappa L., through inhibition on iNOS
pathway, J. Ethnopharmacol. 122, 457-462.
20
Caption:
Table 1 General compounds and effects of burdock reported in the literature
Table 2 Major nutritional ingredients contained in the burdock roots
Fig. 1 The root of burdock
21
Table 1 General compounds and effects of burdock reported in the literature
Classification Compound Molecular
Formula
Parts of the
plant
Effect Reference
Lignans
Arctigenin
C12H24O7
Leaves, fruits,
seeds, roots
Suppressor of heat shock
antitumor;
Anti-influenza virus
(Ishihara et al., 2006)
(Awale et al., 2006)
(Gao et al., 2002)
Arctiin
C27H34O11
Leaves, fruits,
roots
Anti-tumor-promoting activity;
chemopreventive activity;
antiproliferative activity against
B cell hybridoma cell, MH60
(Takasaki et al., 2000)
(Hirose et al., 2000)
(Matsumoto et al., 2006)
22
Trachelogenin
C21H24O7 Fruits
Ca2+ antagonist activity ;
Anti-HIV properties
(Ichikawa et al., 1986)
(Xia et al., 2001)
Lappaol F
C40H42O12 Fruits, seeds
Inhibiting NO production (Park et al., 2007)
Diarctigenin
C42H46O12
Fruits, roots,
seeds
Inhibiting NO production;
(Park et al., 2007)
23
Terpenoids
Beta-eudesmol
C15H26O Fruits
Antibacterial, .antiangiogenic (Yayli et al., 2005)
(Tsuneki et al., 2005)
Polyphenols
Caffeic acid
C9H8O4
Stems, leaves,
the skin of roots
Antioxidative;
free radical scavenging activity
(Pari and Prasath, 2008)
(Bhat et al., 2007)
Chlorogenic acid
C16H18O9
Leaves;
the skin of roots
Neuroprotective ;
Antioxidative ;
anti-anaphylaxis and
anti-HIV ;
(Li et al., 2008)
(Bouayed et al., 2007)
(Chen et al., 2004)
24
Tannin
C76H52O46 Roots
Anti-tumor;
immuno-modulator;
haluronidase inhibition
(Miyamoto et al., 1993)
(Bralley et al., 2008)
Fructose
Inulin
(C6H10O5)n Roots
Prebiotic effectiveness ;
antihypertension;
anti-diabetes
(Li et al., 2008)
(Rault-Nania et al.,
2008)
(Silver and Krantz Jr,
1931)
Sterols
Sitosterol-beta-D-
glucopyranoside
C35H60O6 Roots
mammalian DNA polymerase
λ; anti-diabetes and obesity
(Mizushina et al., 2006)
(Silver and Krantz Jr,
1931)
25
Table 2 Major nutritional ingredients contained in the burdock roots
Types Nutrient ingredients
Amino Acid Essential amino acids Aspartic acid (25-28%) Arginine (18-20%)
Metal elements Potassium Calcium Iron Magnesium Manganese Sodium Zinc Copper
Vitamins B1 B2 C A
Others Crude fiber Phosphorus Carotene
26
Fig. 1. The root of burdock
... Chlorogenic acid obtained from its root extract has shown antibacterial activity against Klebsiella pneumoniae and has also been found to possess anti-β-lactamase activity (Rajasekharan et al. 2017). Besides it also inhibits the formation of biofilm by Escherichia coli and candida (Chan et al. 2011). ...
... These actions might be due to the occurrence of phenolic compounds in the plant. Chan and colleagues reported that the antioxidant and anti-inflammatory potential of these compounds assist in detoxifying and mediate healing action of the plant (Chan et al. 2011). Burdock is used as an ingredient in various commercial cosmetic products because of the presence of various hydroxycinnamic acid derivatives which contribute in antimicrobial, anti-inflammatory, anti-collagenase, and anti-tyrosinase activities as well protection against ultraviolet radiations ). ...
Chapter
More than half of the population in developing nations depends on natural medication for treatment of different sicknesses and problems. Among them, Achillea millefolium from Asteraceae family is one restoratively significant plant called as “yarrow” and revealed as being utilized in folklore medication for sicknesses, for example, skin irritations, convulsive, hepatobiliary, and gastrointestinal issues. Monoterpenes are the most delegate metabolites, establishing 90% of the fundamental oils comparable to the sesquiterpenes, and a wide scope of chemical compounds have likewise been found. Distinctive pharmacological examinations in numerous in vitro and in vivo models have demonstrated the capability of A. millefolium with anti-inflammatory, antiulcer, anticancer activities, and so forth loaning help to the reasoning behind various of its conventional uses. Because of the essential pharmacological activities, A. millefolium will be a superior alternative for new medication discovery. Our chapter extensively gathers late phytochemical and pharmacological activities of A. millefolium, and should, accordingly, act as an appropriate reference for future investigation into the plant’s phytochemical profiling and by and large pharmacological assessment.
... of its high nutritional value [9] also the volatile oil from the root is known to boost skin and hair quality [5]. Traditionally, a mixture of the root extract with honey and oil is applied on the chest for treatment of common cold [10]. ...
Conference Paper
Full-text available
This study was undertaken to determine the changes that occur in volatile oil composition of cultivated burdock root as influenced by mineral fertilizer application in the Wine Land Region of the Western Cape province of South Africa. Harvested dry roots from different treatments was used for oil extraction by hydro distillation and the composition of the oil from the different treatments was determined by GC/MS. In total, T 7 recorded the highest number of compounds (20) with 7 of the compounds of peak% over 5. While T 3 had 19 compounds with 6 of the compounds of peak% over 5. However, T 4 , T 5 , T 6 and T 8 , recoded 14 compounds. Nevertheless, T 1 and T 2 had the least number of compounds with 5 compounds of peak % over 5 for T 1 and 4 compounds for T 2. Overall, the two treatments T 3 and T 7 with the highest number of compounds were treatments with less supplementary phosphorous.
... The enzymes involved in glycopeptide and glycogenolysis are alpha glucosidases. The inhibition of glycosidase is a potential treatment for DM and obesity (Chan et al., 2010). Also known as inulin, gamma-lucoside-fructose ester, assists in the regulation of blood glucose levels. ...
Article
Full-text available
Diabetes mellitus (DM) type 2 is amongst the most common chronic diseases, being responsible for various problems in humans and contributing to increased mortality rates worldwide. Fructooligosaccharide, which can be produced from the roots of burdock (Arctium lappa L.), has been shown to have a wide range of pharmacological proprieties, including antiviral, anti-inflammatory, hypolipidemic, and antidiabetic effects. Moreover, burdock also contains chlorogenic acid, which has been used in traditional medicine as an antioxidant. Considering its natural origin and minimal toxicity, burdock fructooligosaccharides (BFO) has gained considerable attention from researchers owing its wide, efficient, and beneficial action against DM. Although the effectiveness of fructooligosaccharide and chlorogenic acid has been extensively discussed, limited information is available on the application of burdock for DM treatment. In this review, we discuss the beneficial contributions, and the recent in vitro and in vivo analytical findings on A. lappa extract as DM therapy.
Article
Background: Arctigenin (ATG) is the active ingredient of the Chinese herbal medicine Arctium lappa, with anti-inflammatory and antioxidant effects. Excessive inflammation and cell apoptosis are important causes of intervertebral disc degeneration (IDD). Hence, this study probed into the possible role of ATG in IDD. Methods: Interleukin (IL)-1β (10 ng/ml) was adopted to induce human nucleus pulposus cells (HNPCs) as a cell model for IDD. The effects of different concentrations of ATG (0, 2, 5, 10, 20, 50 μmol/L) on the viability of HNPCs and effects of ATG (10, 50 μmol/L) on the viability of IL-1β-induced HNPCs were detected by cell counting kit-8 (CCK-8). After IL-1β-induced HNPCs were transfected with miR-483-3p inhibitor and/or treated with ATG, cell viability and apoptosis were determined by CCK-8 and flow cytometry; the expressions of miR-483-3p, extracellular matrix (ECM)-related genes, and inflammation-related genes were measured by quantitative real time polymerase chain reaction (qRT-PCR), and expressions of ECM/apoptosis/NF-κB pathway-related proteins were quantified by Western blot. Results: ATG had no significant effect on the viability of HNPCs but could promote the viability of IL-1β-induced HNPCs. ATG inhibited apoptosis, ECM degradation, inflammation, and activation of NF-κB pathway in HNPCs induced by IL-1β, but promoted the expression of miR-483-3p. MiR-483-3p inhibitor reversed the above-mentioned regulatory effects of ATG. Conclusion: Arctigenin suppresses apoptosis, ECM degradation, inflammation, and NF-κB pathway activation in HNPCs by up-regulating miR-483-3p.
Article
Sequencing results, annotation, and analysis of the mitochondrial genome of Aphis fabae mordvilkoi are demonstrated in this work. It was shown that mtDNA of Aphis fabae mordvilkoi has a structure and size typical of aphids and does not carry any rearrangements identified in other known mitochondrial genomes of aphids of the genus Aphis L.
Article
This study was aimed to investigate the effects of dietary arctiin (ARC) supplementation (100, 200 and 400 mg/kg) on the growth performance and immune response of broilers after a Salmonella pullorum (S. pullorum) challenge, and we conducted in vitro anti-bacterial test to explore the bacteriostatic mechanism of ARC. The in vivo trial was randomly assigned to 6 groups: non-infected control group (NC) and positive control group (PC) received a basal diet; TET group, received a basal diet supplemented with 100 mg/kg chlortetracycline; ARC100, ARC200 and ARC400 groups received a basal diet containing 100, 200, 400 mg/kg ARC, respectively. From d 14 to d 16, all birds (except NC group) were infected with 1 mL (1×10 8 CFU/mL) fresh S. pullorum culture by oral gavage per day. In vivo results showed that dietary supplementation of 200 mg/kg ARC significantly increased average daily gain (P<0.05) and decreased feed-to-gain ratio of broilers versus the PC group during d 15-28 after challenged with S. pullorum (P<0.05). The jejunal crypt depth (CD) were decreased by supplementing 100 or 200 mg/kg ARC in diets compared with PC birds at d 19 (P<0.05). The jejunal villi height (VH) were increased by supplementing 100, 200 or 400 mg/kg ARC in diets compared with PC birds at d 28 (P<0.05). Besides, dietary supplementation of 200 mg/kg ARC increased the jejunal VH to CD ratio (VH:CD) than PC group both at d 19 and d 28 (P<0.05). Notably, the broilers had lower serum lipopolysaccharide (LPS) and diamine oxidase (DAO) levels in the ARC100 and ARC200 groups at d 28 than those in the PC group (P<0.05). Furthermore, in comparison to PC birds, the birds in ARC groups (100, 200, 400 mg/kg) had higher serum contents of IgM and IL-10, and the birds in ARC200 group had higher serum contents of IgA at d 19 (P<0.05). At d 28, the birds in ARC groups (100, 200, 400 mg/kg) had lower serum contents of IL-8, and the birds in ARC200 group had lower serum contents of IFN-γ compared to the PC birds (P<0.05). The in vitro experiment showed that ARC significantly inhibited the biofilm formation and adhesion of S. pullorum (P<0.05). Metabonomics analysis revealed that ARC can restrain the formation of the biofilm by affecting a variety of metabolic pathways of S. pullorum. Therefore, dietary supplementation of 200 mg/kg ARC might be a potentially way to substitute antibiotics to control S. pullorum infection in broilers.
Article
They studied the effect of the herbal medicine "Burdock root oil" on oxidative damage to liver, kidney and blood tissues. The experiment was performed on 50 non-linear white male rats weighing 180-220 g, divided into 5 groups. The first group - control; animals of groups II and III were subjected to fractional gamma irradiation for five days (0.6 G/day; dose rate 1 Gr/min (60Co)). The total dose was 3 Gr. Animals of the fourth and fifth groups were exposed to a combination of gradiation (as in groups I and III) and potassium dichromate (Cr+6). Potassium dichromate was administered intraperitoneally daily at a dose of 2.8 mg/kg of body weight (0.1LD50) for 5 days (0.5LD50). Rats of groups 3 and 5 received Burdock root oil at a dose of 2.5 ml/kg of body weight intragastrically for 14 days prior to the experimental exposure. Fractional exposure, combined exposure g-radiation, gamma radiation and Cr+6 led to an increase in malondialdehyde and diene conjugates in blood plasma, liver and kidney tissues. Under g-irradiation, the activity of superoxide dismutase enzymes (SOD) and catalase (CAT) in red blood cells compensation increased significantly against the background of a decrease in the level of SH-groups in blood plasma. In liver and kidney tissues, all studied enzymes and reduced glutathione (GSH) levels decreased. Under the conditions of combined exposure g-radiation and potassium dichromate - all the studied indicators of antioxidant protection decreased. The introduction of Burdock root oil before isolated and combined exposure provided significant antioxidant protection in the studied tissues. Conclusion: it can be assumed, that the "Burdock root oil" it is a potential drug that can be used as a radiation protector, in conditions of combined influence of a physical and chemical agent-a detoxifier. In our opinion, the antioxidant potential of the herbal medicine justifies the continuation of further research in clinical practice.
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Immune thrombocytopenia (ITP) is a bleeding disorder characterized by a decreased number of platelets. It is an immune system-mediated condition, with formation of antibodies against a structural platelet antigen. Although the pathogenesis remains elusive, primary disease is idiopathic and comprises 80% of cases. However, quite a few secondary causes have been established including Helicobacter pylori, varicella-zoster virus and cytomegalovirus. A few cases with an incidental association with herbal medications have been reported, but this causality has not been studied in detail. Here we present the case of 38-year-old African-American woman who presented with symptomatic thrombocytopenia, with a platelet count of 5 K/µl 1 week after she had consumed herbal tea containing Rumex crispus (yellow dock) and Arctium lappa (burdock). The association between unstudied herbs and ITP needs further research, given the widespread use of these substances and ongoing public uncertainty about their benefits.
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Full-text available
Arctium lappa L., also known as burdock, is a popular medicinal plant in traditional Chinese medicine due to its potential therapeutic properties. Saccharides from Arctium lappa L. root (ALR-S) have been extensively studied for their anti-inflammatory and anti-diabetes effects. Platelets play a pivotal role in thrombosis. The present study describes the effects of ALR-S on platelet activation and thrombosis using a laser injury thrombosis in vivo model. The study also measured the effects of ALR-S on platelet activation by analysing aggregation, ATP release, platelet spreading, adhesion and clot retraction in vitro. Specifically, the effects were ALR-S concentration-dependent inhibition of platelet aggregation and ATP release. Activated platelets pretreated with ALR-S showed diminished CD62P expression levels and fibrinogen binding, as measured by flow cytometry. ALR-S inhibited platelet spreading on fibrinogen and adhesion on collagen under shear. ALR-S attenuated platelet activation by decreasing oxidative stress and thrombus formation. These results demonstrated the antiplatelet effects of ALR-S, suggesting the antithrombotic and cardiovascular protective activities of ALR-S as a functional food.
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Arctium lappa (A. lappa) is one of the most significant edible medicinal plants with high antibacterial effects, in which it could be supposed to grow with more beneficial effects under administration by salicylic acid and chitosan based biofertilizers. Accordingly, the effects of salicylic acid, chitosan, and 50% moisture discharge were investigated in this work to see the antimicrobial treatments of some foodborne pathogens effects by A. lappa. To this aim, plants were cultivated based on different concentrations of salicylic acid and chitosan with/without drought stress, in which their extracted essential oils were examined for showing the antimicrobial effect against different bacterial agents. The results indicated that the salicylic acid and chitosan administrated A. lappa could work with improved inhibitory functions. Comparing with referenced antibiotics showed even higher antimicrobial effects of A. lappa against the targeted bacterial agents, in which the species with 14 mmol of salicylic acid and 2 g/l of chitosan was a distinguished one for approaching the purpose. Consequently, the achievements of this work could be further investigated for producing novel antibiotic drug agents.
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The herbal mixtures, Essiac™ and Flor‐Essence™, are sold as nutritional supplements and used by patients to treat chronic conditions, particularly cancer. Evidence of anticancer activity for the herbal teas is limited to anecdotal reports recorded for some 40 years in Canada. Individual case reports suggest that the tea improves quality of life, alleviates pain, and in some cases, impacts cancer progression among cancer patients. Experimental studies with individual herbs have shown evidence of biological activity including antioxidant, antioestrogenic, immunostimulant, antitumour, and antiocholeretic actions. However, research that demonstrates these positive effects in the experimental setting has not been translated to the clinical arena. Currently, no clinical studies of Essiac™ or Flor‐essence™ are published, but a clinical study is being planned at the British Columbia Cancer Agency by the University of Texas‐Center for Alternative Medicine (UT‐CAM) and Tzu‐Chi Institute for Complementary and Alternative Medicine. Copyright © 2000 John Wiley & Sons, Ltd.
Article
The methanolic extract from the seeds of Arctium lappa was found to inhibit the LPS-induced nitric oxide (NO) production in murine macrophage RAW264.7 cells. Bioassay-guided fractionation of a methylene chloride soluble fraction led to the isolation of three lignan compounds, arctiin (1), arctigenin (2), and lappaol B (3). Their structures were elucidated by UV, IR, MS, and NMR data, as well as by comparison with those of the literatures. Arctigenin (2) and lappaol B (3) had an iNOS inhibitory activity with IC50 values of 12.5 and 25.9 μM, respectively.
Article
Methanol extract from Arctium lappa L. showed an inhibitory activity of α-glucosidase. The methanol extract was re-extracted with ethyl acetate and water. The ethyl acetate extract showed inhibitory activity. The inhibitory compound was isolated from the ethyl acetate extract and identified as sitosterol-β -D-glucopyranoside (1) by EI-MS, FAB-MS, IR, 1H and 13C NMR spectroscopy. Compound 1 inhibited 97.3% of α-glucosidase activity at a concentration of 200.0 μ mol/mL, and the ID50 (50% inhibition dose) value was 30 μ mol/mL. In addition, the inhibitory compounds from the ethyl acetate extract were also identified as methyl palmitate (2), methyl linoleate (3) and methyl linoleneate (4) by GC-MS analysis. Compound 2-4 inhibited 73.4%, 66.5% and 68.5% of α-glucosidase activity at a concentration of 200 μ mol/mL, and the ID50 values were 52.8, 47.5 and 46.7 μ mol/mL. To research the structure-activity relationship, methyl steareate (5), methyl oleate (6), palmitic acid (7), linoleic acid (8), linolenic acid (9), stearic acid (10) and oleic acid (11) were also assayed.
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The root of Arctium lappa Linne (A. lappa) (Compositae), a perennial herb, has been cultivated for a long time as a popular vegetable. In order to investigate the hepatoprotective effects of A. lappa, male ICR mice were injected with carbon tetrachloride (CCl4, 32 μl/kg, i.p.) or acetaminophen (600 mg/kg. i.p.). A. lappa suppressed the SGOT and SGPT elevations induced by CCl4 or acetaminophen in a dose-dependent manner and alleviated the severity of liver damage based on histopathological observations. In an attempt to elucidate the possible mechanism(s) of this hepatoprotective effect, glutathione (GSH), cytochrome P-450 (P-450) and malondialdehyde (MDA) contents were studied. A. lappa reversed the decrease in GSH and P-450 induced by CCl4 and acetaminophen. It was also found that A. lappa decreased the malondialdehyde (MDA) content in CCl4 or acetaminophen-intoxicated mice. From these results, it was suggested that A. lappa could protect the liver cells from CCl4 or acetaminophen-induced liver damages, perhaps by its antioxidative effect on hepatocytes, hence eliminating the deleterious effects of toxic metabolites from CCl4 or acetaminophen.
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Treatment of sliced burdock root tissue with copper (II) sulphate stimulated phytoalexin formation. Two were isolated and characterized as (S)-12,1
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The root of burdock (Arctium lappa L.) has long been cultivated as a popular vegetable in Taiwan and Japan for dietary use and folk medicine. The present study investigated the influence of the different treatments of peeling and heat treatment on (1) the free radical scavenging activity of burdock, using a 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and on (2) variations of its active components, chlorogenic acid and caffeic acid, by a HPLC method. Treatments were divided into four groups: group I, root of burdock without heat treatment; group II, peeled root of burdock without heat treatment; group III, root of burdock with heat treatment; and group IV, peeled root of burdock with heat treatment. Freeze-dried powders from both the root and peeled root of burdock, after heat treatment, had poor physical properties due to the apparent coagulation according to visual observations. The active phenolic components, chlorogenic acid and caffeic acid, existed mainly in the skin of burdock root, and the content of chlorogenic acid was much higher than that of caffeic acid. Burdock possessed significant free radical scavenging activity, which was mainly attributed to chlorogenic acid, whose free radical scavenging activity was similar to that of caffeic acid and higher than that of vitamin E. Peeling of the root greatly decreased the free radical scavenging activity and the concentrations of these two active components, due to elimination of the components in the discarded skin. Heat treatment slightly decreased the free radical scavenging activity, which was partially due to the degradation of chlorogenic acid.
Article
The protective effects of burdock (Arctium lappa Linne) on oxidation of low-density lipoprotein (LDL) and nitric oxide production were investigated. The results showed that methanolic extracts of burdock (MEB) and their major components, chlorogenic acid (CHA) and caffeic acid (CA), showed marked antioxidant activity against oxidative damage of liposome (p < 0.05), deoxyribose (p < 0.05) and protein (p < 0.05). In addition, at a concentration of 500 μg/ml, the inhibitory effect of MEB on LDL oxidation was 66.9% compared to the control (p < 0.05). MEB, at 200 μg/ml, not only enhanced GSH levels, but also increased activity of GSH reductase, GSH peroxidase, GSH transferase and catalase, which were 3.82-, 24.9-, 4.35- and 3.02-fold compared to the control (p < 0.05), respectively. MEB directly scavenged nitric oxide in a concentration-dependent fashion (p < 0.05). Moreover, MEB showed a reducing effect on nitric oxide production of lipopolysaccharide (LPS)-induced RAW 264.7 cells. The expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) in activated RAW 264.7 cells were inhibited by MEB. Reverse transcription-polymerase chain reaction (RT-PCR) analysis revealed that the expression of iNOS and COX-2 mRNA in activated macrophages were suppressed by a high concentration (500 μg/ml) of MEB. Furthermore, a downregulated degradation of IκB-α by MEB was found, indicating that MEB reduced iNOS enzyme expression as a result of preventing NF-κB activation. These results suggest that MEB displays an inhibitory action on biomolecules and has a bioactive action for attenuating excessive NO generation at inflammatory site as well as in cardiovascular disease.