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

  • 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
*Dr. George Pak-Heng Leung, Department of Pharmacology and Pharmacy, The University of Hong
Kong, Hong Kong SAR, PR of China. E-mail address:; 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:; Phone: +852-34008718; Fax:
This is the Pre-Published Version.
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
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
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.,
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
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.,
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
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
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
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
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
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
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
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
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
adverse effects of medicinal herbs shall be enhanced.
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,
Shenzhen. Special thanks go to Ms. Siu-Hung Tsui and Ms. Josephine Hong-Man
Leung for proofreading and providing critical comments on the manuscript.
Abreu, P., Matthew, S., Gonzalez, T., et al. (2006). Anti-inflammatory and antioxidant
activity of a medicinal tincture from Pedilanthus tithymaloides, Life Sci. 78,
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.
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,
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,
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.
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,
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,
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
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,
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,
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,
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,
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
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.
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
Table 1 General compounds and effects of burdock reported in the literature
Classification Compound Molecular
Parts of the
Effect Reference
Leaves, fruits,
seeds, roots
Suppressor of heat shock
Anti-influenza virus
(Ishihara et al., 2006)
(Awale et al., 2006)
(Gao et al., 2002)
Leaves, fruits,
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)
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)
Fruits, roots,
Inhibiting NO production;
(Park et al., 2007)
C15H26O Fruits
Antibacterial, .antiangiogenic (Yayli et al., 2005)
(Tsuneki et al., 2005)
Caffeic acid
Stems, leaves,
the skin of roots
free radical scavenging activity
(Pari and Prasath, 2008)
(Bhat et al., 2007)
Chlorogenic acid
the skin of roots
Neuroprotective ;
Antioxidative ;
anti-anaphylaxis and
anti-HIV ;
(Li et al., 2008)
(Bouayed et al., 2007)
(Chen et al., 2004)
C76H52O46 Roots
haluronidase inhibition
(Miyamoto et al., 1993)
(Bralley et al., 2008)
(C6H10O5)n Roots
Prebiotic effectiveness ;
(Li et al., 2008)
(Rault-Nania et al.,
(Silver and Krantz Jr,
C35H60O6 Roots
mammalian DNA polymerase
λ; anti-diabetes and obesity
(Mizushina et al., 2006)
(Silver and Krantz Jr,
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
Fig. 1. The root of burdock
... Previous studies have shown that inulin-type fructans extracted from Compositae plants can prevent metabolic diseases, boost immunity, and invigorate health effectively (Bode, 2012;Yuan et al., 2021). Burdock (Arctium lappa L.), the Composite family, has been therapeutically applied in Asia, Europe, and North America for hundreds of years (Chan et al., 2011;Zhang, Liu, Lu, Wang, & Chen, 2019). Wang et al. (2016) found that burdock root extracts can protect quail against atherosclerosis by hypolipidemic and anti-oxidant effects. ...
... NF-κB can help to regulate several downstream genes involved in the process of inflammation, cell proliferation, oxidative stress, and apoptosis, which releases of proinflammatory cytokines such as TNF-α and IL-6 (Luedde & Schwabe, 2011;Nafees, Rashid, Ali, Hasan, & Sultana, 2015). These findings may be attributed to the anti-inflammatory effects of BFO (Chan et al., 2011), thereby reducing the risk of early lesions to cardiovascular disease caused by the inflammatory reaction and macrophage recruitment in the hypercholesterolemia patients. ...
Burdock fructooligosaccharide (BFO) is a type of linear inulin extracted from burdock root. In this study, we studied the effect of BFO in hypercholesterolemic mice model and found that BFO could decrease the total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and oxidized LDL (ox-LDL). BFO also reduce the hepatocyte damage, improve the antioxidant enzymes activity and regulate genes related to the cholesterol homeostasis in liver. Besides, we found that BFO protected the blood vessels by significantly balancing inflammatory cytokines and alleviating the up-regulation of TLR4/MyD88/NF-κB pathway in aorta. Furthermore, we established a foam cells model induced by ox-LDL in vitro and found that 500 and 1000 μg/mL BFO could effectively inhibit cell proliferation and reduce the production of intracellular lipids and inflammatory cytokines. Therefore, BFO can reduce the risk of hypercholesterolemia by maintaining cholesterol homeostasis, reducing vascular inflammation and alleviating macrophage foaming to prevent its further development into cardiovascular diseases.
... Arctium lappa L. (family Asteraceae; commonly known as burdock, greater burdock, lappa, thorny burr, beggar's buttons) is a medicinal plant that is native to temperate regions of Europe and Asia, although it has been widely naturalised and is now common globally. Arctium lappa roots have been used for hundreds of years as traditional medicines by multiple European, Asian and North American cultures 9 for a variety of purposes including to improve the immune system and to enhance metabolism, 10 as well as for its anti-inflammatory, [11][12][13][14] anti-cancer, 15,16 and anti-biabetic properties. 17,18 Many of these illnesses are caused by bacterial pathogens and several studies have reported that A. lappa leaf extracts inhibit the growth of Bacillus subtilis, Lactobacillus acidophilus and Pseudomonas aeruginosa. ...
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Introduction: An increase in antibiotic resistance and a corresponding decrease in antimicrobial discovery have directed researchers towards alternative therapies, including plant based medicines. However, synergistic combinations of plant extracts with conventional antibiotics may be a far more effective approach in overcoming resistance and potentiating the activity of antibiotics that are otherwise ineffective against resistant bacterial strains. Materials and Methods: The antibacterial activity of Arctium lappa L. root extracts was investigated by disc diffusion and quantified by liquid dilution and solid phase MIC assays. The extracts were also combined with a range of conventional antibiotics and tested against various microbial triggers of autoimmune diseases. The ΣFIC values obtained from these assays were used to determine the class of combinational effects. Toxicity was evaluated by Artemia nauplii mortality and HDF cytotoxicity assays. Results: Methanolic and ethyl acetate A. lappa root extracts showed good inhibitory activity against several gastrointestinal bacterial pathogens. They were particularly good inhibitors of S. sonneii and B. cereus, with MIC values in the range 150-250μg/mL. The aqueous extract was also a noteworthy inhibitor of B. cereus growth. Of further interest, some combinations of the A. lappa root extracts and conventional antibiotics potentiated bacterial growth inhibition compared to the individual components. Four synergistic and five additive interactions were noted. Notably, no antagonistic interactions were evident, indicating that all combinations could be used without decreasing the antibacterial activity of the components. All extracts were non-toxic in the ALA and HDF assays. Conclusion: Arctium lappa root extracts have potential as inhibitors of bacterial gastrointestinal pathogens. Furthermore, extract components may also potentiate the activity of some antibiotics that are relatively ineffective alone. Isolation and identification of these compounds may be beneficial in drug design against several gastrointestinal bacterial pathogens.
As the global population ages, the treatment of neurodegenerative diseases is becoming more and more important. There is an urgent need to discover novel drugs that are effective in treating neurological diseases. In recent years, natural products and their biological activities have gained widespread attention. Lignans are a class of metabolites extensively present in Chinese herbal medicine and possess good pharmacological effects. Latest studies have demonstrated their neuroprotective pharmacological activity in preventing acute/chronic neurodegenerative diseases and depression. In this review, the pharmacological effects of these disorders, the pharmacokinetics, safety, and clinical trials of lignans were summarized according to the scientific literature. These results proved that lignans mainly exert antioxidant and anti‐inflammatory activities. Anti‐apoptosis, regulation of nervous system functions, and modulation of synaptic signals are also potential effects. Despite the substantial evidence of the neuroprotective potential of lignans, it is not sufficient to support their use in the clinical management. Our study suggests that lignans can be used as prospective agents for the treatment of neurodegenerative diseases and depression, with a view to informing their further development and utilization.
Medicinal plants are a vital input of raw materials for the manufacture of pharmaceuticals to treat various ailments of humans and animals. The excessive demand for natural medicinal therapies has encouraged intensive harvesting of medicinal plants from the wild reserves without proper replenishment. This has put tremendous pressure on many valuable medicinal plant resources, pushing them toward extinction. Therefore, it is urgent to identify alternative production techniques for medicinal plants to fulfill the growing demand while safeguarding their natural stands. The production of therapeutic herbs has evolved from traditional methods to modern techniques including ex vitro and in vitro propagation and biotechnology. In vitro methods are presented as alternative and complementary techniques of propagation providing solutions for the drawbacks associated with conventional propagation techniques. In addition, to in vitro plant propagation, Synseed production, cell suspension cultures, cryopreservation, short-to-medium-term storage, in vitro metabolite production, and root cultures in vitro are some other important aspects of biotechnological interventions for medicinal plant material production. In this context, studying and distributing knowledge on novel involvements of their production are important to promote collaboration and sharing of information among researchers, scientists, and industry professionals leading to more rapid advancements in the field. Therefore, this chapter highlights the recent knowledge based on medicinal plants giving special reference to ex vitro and in vitro production methods emphasizing the most recent advances, limitations, and future prospects.KeywordsEx vitroIn vitroMedicinal plantsNovel technologiesPropagation
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Background: Humans have been consuming medicinal plants (as herbs/ spices) to combat illness for centuries Herbs while ascribing beneficial effects predominantly to the plant/phytochemical constituents, without recognizing Edible microbiome the power of obligatory resident microorganism' communities (MOCs) (live/dead bacteria, fungus, yeast, molds Medicinal microbiome etc.) which remain after industrial microbial reduction methods. Very little is known about the taxonomic Bugs as drugs identity of residual antigenic microbial associated molecular patterns (MAMPs) debris in our botanical over the Immune boosting counter (OTC) products, which if present would be recognized as foreign (non-self) antigenic matter by host pattern recognition receptors (PRRs) provoking a host immune response; this the basis of vaccine adjuvants. As of today, only few research groups have removed the herbal MAMP biomass from herbs, all suggesting that immune activation may not be from the plant but rather its microbial biomass; a hypothesis we corroborate. Purpose: The purpose of this work was to conduct a high through put screening (HTPS) of over 2500 natural plants, OTC botanical supplements and phytochemicals to elucidate those with pro-inflammatory; toll like receptor 4 (TLR4) activating properties in macrophages. Study design: The HTPS was conducted on RAW 264.7 cells vs. lipopolysaccharide (LPS) E. coli 0111:B4, testing iNOS / nitric oxide production (NO2-) as a perimeter endpoint. The data show not a single drug/chemical/ phytochemical and approximately 98 % of botanicals to be immune idle (not effective) with only 65 pro-inflammatory (hits) in a potency range of LPS. Method validation studies eliminated the possibility of false artifact or contamination, and results were cross verified through multiple vendors/ manufacturers/lot numbers by botanical species. Lead botanicals were evaluated for plant concentration of LPS, 1,3:1,6-β-glucan, 1,3:1,4-β-D-glucan and α-glucans; where the former paralleled strength in vitro. LPS was then removed from plants using high-capacity endotoxin poly lysine columns, where bioactivity of LPS null "plant" extracts were lost. The stability of E.Coli 0111:B4 in an acid stomach mimetic model was confirmed. Last, we conducted a reverse culture on aerobic plate counts (APCs) from select hits, with subsequent isolation of gram-negative bacteria (MacConkey agar). Cultures were 1) heat destroyed (retested/ confirming bioactivity) and 2) subject to taxonomical identification by genetic sequencing 18S, ITS1, 5.8 s, ITS2 28S, and 16S. Conclusion: The data show significant gram negative MAMP biomass dominance in A) roots (e.g. echinacea, yucca, burdock, stinging nettle, sarsaparilla, hydrangea, poke, madder, calamus, rhaponticum, pleurisy, aconite etc.) and B) oceanic plants / algae's (e.g. bladderwrack, chlorella, spirulina, kelp, and "OTC Seamoss-blends" (irish moss, bladderwrack, burdock root etc), as well as other random herbs (eg. corn silk, cleavers, watercress, cardamom seed, tribulus, duckweed, puffball, hordeum and pollen). The results show a dominance of gram negative microbes (e.g. Klebsilla aerogenes, Pantoae agglomerans, Cronobacter sakazakii), fungus (Glomeracaea, Ascomycota, Irpex lacteus, Aureobasidium pullulans, Fibroporia albicans, Chlorociboria clavula, Aspergillus_sp JUC-2), with black walnut hull, echinacea and burdock root also containing gram positive microbial strains (Fontibacillus, Paenibacillus, Enterococcus gallinarum, Bromate-reducing bacterium B6 and various strains of Clostridium). Conclusion: This work brings attention to the existence of a functional immune bioactive herbal microbiome, independent from the plant. There is need to further this avenue of research, which should be carried out with consideration as to both positive or negative consequences arising from daily consumption of botanicals highly laden with bioactive MAMPS.
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Objetivo: Analisar a atividade antibacteriana do extrato da semente da espécie A. minus, pelo método de disco difusão frente a bactérias gram-negativas e positivas. Materiais e métodos: A avaliação do extrato bruto realizou-se em concentrações de 10, 50 e 100 mg/mL, utilizando o teste de susceptibilidade antibacteriana, foi realizada através do método de disco difusão. Resultados: As amostras testadas não mostraram atividade bacteriana, ao contrário do que era esperado. Discussão: As plantas medicinais que possuem atividade antibacteriana podem atuar de forma conjunta na redução dos sintomas inflamação, por meio da redução de agentes agressores como as bactérias, isso resultará em diminuição de liberação de mediadores pró-inflamatórios, reduzindo seus efeitos, no entanto isso não pode ser observado nesse estudo. Conclusão: A. minus apresentou resultados negativos para cepas de bactérias gram-negativas e positivas.
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Greater burdock (Arctium lappa L.), a biennial herbaceous plant belonging to the Asteraceae family, is a rich source of some bioactive compounds including chlorogenic acid, arctiin, and inulin which are involved in the treatment of a broad range of disorders. In this study, the phytochemical variability and antioxidant activity of nine Iranian A. lappa populations collected from different geographical regions were investigated. The highest content of chlorogenic acid was recorded in Baft (76.48 mg/g DW), Rudsar (75.5 mg/g DW), and Bijar (74.8 mg/g DW) populations, respectively. The content of chlorogenic acid in A. lappa seeds ranged from 23.4 to 75.1 mg/g DW with the lowest content in the Baft population and the highest content in the Savadkooh population. In addition, the highest content of arctiin was found in the seeds of Savadkooh (78.21 mg/g DW) and Baft (77.7 mg/g DW) populations. The mean total carbohydrate content in A.lappa populations was 31.8 mg/g DW. The maximum antioxidant activity was observed in the roots of Roodsar (IC50 = 78.2 µg/mL) and seeds of Firoozkooh (IC50 = 174.8 µg/mL) populations. In comparison, the antioxidant activity of the roots was the most reliable among the extracts. This information provides a perspective for the plant used in domestication, conservation, and breeding programs and for further commercial exploitation in food industries as a potent natural antioxidant source.
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Utilization of used cooking oil may cause fat accumulation in the body leading to exceeding metabolic capacity of the liver and lipid peroxidation, subsequently triggering oxidative stress that will lead to non-alcoholic fatty liver disease (NAFLD). Burdock root (Arctium lappa) have hypolipidemic, antioxidant, and anti-inflammatory properties. This study aims to determine the effects of Burdock root to reduce steatosis and malondialdehyde (MDA) plasma levels in male Wistar rats fed with used cooking oil. This study used a post-test only control group design. Thirty healthy male Wistar rats were randomized into three groups. All groups were given 0,42 mL of used cooking oil. Fifteen minutes after, the intervention group 0 (P0) was given 1 mL of distilled water 1x/day. The intervention group 1 (P1) was given 100 mg/kg BW of burdock roots ethanolic extract diluted in 1 mL of distilled water 1x/day. The intervention group 2 (P2) was given 200 mg/kg BW of burdock roots ethanolic extract diluted in 1 ml of distilled water 1x/day. After 28 days, histopathological examination of the liver tissue to measure steatosis and peripheral blood taken to measure serum MDA levels and compared between groups. The results showed that the average steatosis in the P0 group was significantly higher than the P1 group (15.51±3.22% vs. 8.92±1.49%, respectively; p = 0.00). Similar results between the P1 group were also significantly higher compared to the P2 group (5.18±1.31%; p = 0.002). The mean serum MDA level revealed a significantly higher results among the P0 group compared to P1 group as well as P1 group compared to P2 group (12.58±1.92 nmol/mL vs. 9.76±0.47 nmol/mL, respectively; p=0.011 and (9.76±0.47 nmol/mL vs. 8.69±0.33 nmol/mL, respectively; p=0.011). The conclusions of this study were that burdock roots could reduce steatosis and serum MDA in male Wistar rats that were given used cooking oil.
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In humans, the immune system serves as a protective barrier against infection; however, when the immune system is out of balance, it can harm the host. Immunomodulators are chemicals or medications that have been employed in the clinic to treat an unbalanced immune response. The majority of immunological medicines in clinical use are cytotoxic. They harm the patient's quality of life by causing various side effects and being associated with higher production costs, longer lead times, and a high failure rate. Furthermore, obtaining single-compound chemicals with low toxicity, high efficacy, and selectivity for specified disorders is difficult for researchers. As a result, techniques based on alternative medicine are gaining attraction in drug development, focusing on innovative natural compounds utilized to treat various disorders. Many plant molecules founded to have biologically beneficial properties. This review aimed to look at the immunomodulatory activity of plant-derived chemicals from widely-used plants.
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.
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.
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.
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.
Treatment of sliced burdock root tissue with copper (II) sulphate stimulated phytoalexin formation. Two were isolated and characterized as (S)-12,1
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.
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.