1. No category

Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
Contents lists available at SciVerse ScienceDirect
Journal of Ethnopharmacology
journal homepage: www.elsevier.com/locate/jep
Review
Botany, phytochemistry, pharmacology, and potential application of
Polygonum cuspidatum Sieb.et Zucc.: A review
Wei Peng, Rongxin Qin, Xiaoli Li, Hong Zhou n
Department of Pharmacology, College of Pharmacy, The Third Military Medical University, Chongqing 400038, PR China
art ic l e i nf o
a b s t r a c t
Article history:
Received 31 December 2012
Received in revised form
3 May 2013
Accepted 3 May 2013
Ethnopharmacological relevance: Polygonum cuspidatum Sieb. et Zucc. (Polygonum cuspidatum), also
known as Reynoutria japonica Houtt and Huzhang in China, is a traditional and popular Chinese
medicinal herb. Polygonum cuspidatum with a wide spectrum of pharmacological effects has been used
for treatment of inflammation, favus, jaundice, scald, and hyperlipemia, etc.
Aim of the review: The present paper reviews the traditional applications as well as advances in botany,
phytochemistry, pharmacodynamics, pharmacokinetics and toxicology of this plant. Finally, the tendency
and perspective for future investigation of this plant are discussed, too.
Materials and methods: A systematic review of literature about Polygonum cuspidatum is carried out
using resources including classic books about Chinese herbal medicine, and scientific databases including
Pubmed, SciFinder, Scopus, the Web of Science and others.
Results: Polygonum cuspidatum is widely distributed in the world and has been used as a traditional
medicine for a long history in China. Over 67 compounds including quinones, stilbenes, flavonoids,
counmarins and ligans have been isolated and identified from this plant. The root of this plant is used as
the effective agent in pre-clinical and clinical practice for regulating lipids, anti-endotoxic shock, antiinfection and anti-inflammation, anti-cancer and other diseases in China and Japan.
Conclusion: As an important traditional Chinese medicine, Polygonum cuspidatum has been used for
treatment of hyperlipemia, inflammation, infection and cancer, etc. Because there is no enough systemic
data about the chemical constituents and their pharmacological effects or toxicities, it is important to
investigate the pharmacological effects and molecular mechanisms of this plant based on modern
realization of diseases’ pathophysiology. Drug target-guided and bioactivity-guided isolation and
purification of the chemical constituents from this plant and subsequent evaluation of their pharmacologic effects will promote the development of new drug and make sure which chemical constituent or
multiple ingredients contributes its pharmacological effects. Additionally, chemicals and their pharmacological effects of the other parts such as the aerial part of this plant should be exploited in order to
avoid resource waste and find new chemical constituents.
& 2013 Elsevier Ireland Ltd. All rights reserved.
Keywords:
Polygonum cuspidatum Sieb. et Zucc.
Traditional uses
Botany
Phytochemistry
Pharmacology
Contents
1.
2.
3.
4.
Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
Traditional usages . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
Botany . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
Phytochemistry . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
4.1.
Volatile compounds (essential oils) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
4.2.
Quinones . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
4.3.
Stilbenes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
2
4
4
7
7
7
9
Abbreviations: ACAT, acyl-coenzyme A-cholesterol acyltransferase; CCSP, Clara cell secretory protein; EBV, Epstein–Barr virus; ERs, estrogen receptors; HBV, hepatitis B
virus; HIV, human immunodeficiency virus; HSV, herpes simplex virus; iNOS, inducible nitric oxide synthase; ip, intraperitoneal injection; iv, intravenous injection; IZ,
inhibition zones; LC, liver coefficient; LDLC, low-density lipoprotein cholesterol; LPS, lipopolysaccharide; MAGI, transactivation in multinuclear activation of galactosidase
indicator; MBC, minimal bactericidal concentration; MIC, minimal inhibitory concentration; NAG, N-acetyl-β-glucosaminidase; PCE, ethanol extract of Polygonum
cuspidatum; po, per os; PV, parainfluenza virus; sc, subcutaneous injection; TC, total cholesterol; TC/HDLC, total cholesterol/high-density lipoprotein cholesterol; tid,
ter in die; TNF, tumor necrosis factor; TPA, 12-O-tetradecanoylphorbol-13-acetate; VSV, vesicular stomatitis virus; VV, vaccinia virus.
n
Corresponding author. Tel./fax: +86 23 68771246.
E-mail address: [email protected] (H. Zhou).
0378-8741/$ - see front matter & 2013 Elsevier Ireland Ltd. All rights reserved.
http://dx.doi.org/10.1016/j.jep.2013.05.007
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
2
4.4.
Flavonoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
4.5.
Coumarins and lignans . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
4.6.
Other compounds . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
5. Pharmacodynamics and potential applications . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
5.1.
Lipid regulating effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
5.2.
Anti-shock effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
5.3.
Anti-inflammatory effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
5.4.
Hepatoprotective effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
5.5.
Inhibition of melanogenesis effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
5.6.
Estrogenic effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
5.7.
Antioxidant effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
5.8.
Anticancer effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
5.9.
Antiviral effect . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13
5.10. Antibacterial and antifungal effects . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13
5.11. Other pharmacological effects. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
5.12. Summary of pharmacologic effects. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
6. Pharmacokinetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
7. Toxicology . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
8. Future perspectives and conclusion . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
Acknowledgement. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
1. Introduction
Polygonum cuspidatum Sieb. et Zucc., a traditional, popular
Chinese medicinal herb, is widely distributed in southern China
and Japan. The root of Polygonum cuspidatum has been used in
treatment of inflammation, infection, jaundice, skin burns and
hyperlipemia diseases, in China and Japan.
Since 1977, Polygonum cuspidatum has been listed in the
Pharmacopoeia of the People's Republic of China; the root of this
plant is used as the effective agent. Over 100 prescriptions
containing this plant have been utilized to treat diseases
(Editorial Committee of Chinese Pharmacopoeia, 1977; State
Administration of Traditional Chinese Medicine, 1999; Matsuda
et al., 2001; Shi et al., 2012). Modern investigations demonstrate
that has many pharmacological effects including lipid regulating
effect, anti-shock effect, anti-inflammatory effect, antioxidant
effect, anticancer effect, hepatoprotective effect, antiviral effect,
antibacterial effect, and antifungal effect, etc. (Jiangsu New Medical
College, 1977; Arichi et al., 1980; Kim et al., 2005; Bralley et al.,
2008; Shu et al., 2011).
Now, extensive investigations related to phytochemistry have
been done on the root of this plant. Currently, over 67 compounds
from this plant have been isolated and identified; they are
quinones, stilbenes, flavonoids, counmarins, ligans and others. At
present, emodin and polydatin are used as the indicator compounds to characterize the quality of this plant in the Pharmacopoeia of the People's Republic of China (Editorial Committee of
Chinese Pharmacopoeia, 2010).
Fig. 1. Polygonum cuspidatum Sieb. et Zucc.(A) Whole Polygonum cuspidatum plant, and the arrow represented the stems of Polygonum cuspidatum (B) flowers and leaves
(C) Materia medica of the roots of Polygonum cuspidatum.
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
3
Table 1
The traditional and clinical uses of Polygonum cuspidatum in China.
Preparation name
Appendicitis syrup
Main compositions
Rhizoma Polygoni Cuspidati, Herba Hedyotidis, Herba
Taraxaci Mongolici, Radix et Rhizoma Rhei Palmati
Bai Hu Shi Yin decoction
Rhizoma Polygoni Cuspidati, Rhizoma Imperatae, Herba
Salviae Chinensis, Herba Artemisiae Capillaris
Dang Die Ling
Rhizoma Polygoni Cuspidati, Rhizoma Coptidis, Rhizoma
Coptidis, Radix Glycyrrhizae, Radix Paeoniae Rubra, Folium
Pyrrosiae, Amber, Radix Astragali Mongolici, Rhizoma
Anemarrhenae, Polyporus, Semen Plantaginis, Radix
Angelicae Sinensis, Pheretima Aspergillum
Fu Fang Hu Zhang granule
Rhizoma Polygoni Cuspidati, Cortex Phellodendri Amurensis,
Radix Sophorae Flavescentis
Fu Fang Hu Zhang tablets
Rhizoma Polygoni Cuspidati, Caulis Mahoniae, Folium
Eriobotryae Japonicae
Fu Fang Hu Zhang Zi Cao oil Rhizoma Polygoni Cuspidati, Rhizoma Coptidis, Radix
Sanguisorbae, Radix Lithospermi
Hu Cha tincture
Rhizoma Polygoni Cuspidati, Catechu, Radix Scutellariae
Baicalensis, Borneolum Synthcticum
Hu Yin decoction
Rhizoma Polygoni Cuspidati, Herba Artemisiae Capillaris,
Fructus Jujubae
Hu Zhang Di Yu decoction
Rhizoma Polygoni Cuspidati, Radix Sanguisorbae, Fructus
Crataegi Pinnatifidae, Flos Lonicerae
Hu Zhang Bi Xie decoction
Rhizoma Polygoni Cuspidati, Rhizoma Dioscoreae Collettii,
Semen Plantaginis, Radix et Rhizoma Rhei Palmati, Radix
Cyathulae, Rhzoma Atractylodis Lanceae, Cortex Phellodendri
Amurensis, Cortex Moutan Radicis, Radix Paeoniae Rubra,
Fructus Malvae Vertillatae, Rhizoma Alismatis, Fructus
Gradeniae, Radix et Rhizoma Clematidis Chinensis
Hu Zhang burn gels
Rhizoma Polygoni Cuspidati, Radix Angelicae Sinensis, Galla
Chinensis
Hu Zhang Tang Shang liquid Rhizoma Polygoni Cuspidati, Radix Scutellariae Baicalensis,
Rhizoma Coptidis, Cortex Phellodendri Amurensis, Borneolum
Synthcticum
Hu Zhang Tong Fen granule Rhizoma Polygoni Cuspidati, Rhizoma et Radix Notopterygii,
Radix Angelicae Sinensis, Herba Artemisiae Capillaris, Cortex
Phellodendri Amurensis, Rhzoma Atractylodis Lanceae, Poria,
Radix Cyathulae, Polyporus, Rhizoma Alismatis
Hu Zhang Yu Zhuo decoction Rhizoma Polygoni Cuspidati, Folium Pyrrosiae, Rhizoma
Chanxiong, Radix Angelicae Formosanae, Herba Lycopi Hirti,
Radix Cyathulae
Jia Wei Hu Zhang powders
Rhizoma Polygoni Cuspidati, Olibanum, Herba Lysimachiae,
Cortex Phellodendri Amurensis, Herba Leonuri Japonici, Semen
Vaccariae Segetalis, Radix Salviae Miltiorrhizae, Fructus Lycii,
Herba Ecliptae Prostratae, Fructus Ligustri Lucidui
Jin Dan tablets
Rhizoma Polygoni Cuspidati, Radix Gentianae, Herba
Lysimachiae, pig gal
Qu Feng medical wine
Rhizoma Polygoni Cuspidati, Radix Angelicae Sinensis,
Rhizoma Chanxiong, Himalayan Teasel Root, Radix
Saposhnikoviae, Radix Angelicae Biserratae, Pericarpium Citri
Reticulatae, Rhizoma et Radix Notopterygii, Radix
Aucklandiae, Radix Glycyrrhizae
Re Yan Ning granule
Rhizoma Polygoni Cuspidati, Herba Taraxaci Mongolici, Herba
Patriniae Scabiosaefoliae, Herba Scutellariae Barbatae
Sang Zhi Hu Zhang
Rhizoma Polygoni Cuspidati, Ramulus Mori, Radix Caraganae
decoction
Sinicae, Root of Phoenix Tree, Radix Angelicae Sinensis
Shao Shang Fu Kang liquid
Rhizoma Polygoni Cuspidati, Radix Sanguisorbae, Rhizoma
Bletillae Striatae, Caulis Lonicerae, Rhizoma Coptidis,
Borneolum Synthcticum
Shao Shang Ling tincture
Rhizoma Polygoni Cuspidati, Cortex Phellodendri Amurensis,
Borneolum Synthcticum
Shu Feng Huo Luo pellets
Rhizoma Polygoni Cuspidati, Semen Strychni, Herba Ephedrae
Sinicae, Rhizoma Smilacis Chinae, Rumulus Ginnamomi,
Fructus Chaenomelis Spceiosae, Radix Glycyrrhizae, Radix
Saposhnikoviae, Radix Gentianae Macrophyllae, Herba Taxilli
Chinensis
Su Dan tablets
Rhizoma Polygoni Cuspidati, Radix Aucklandiae, Cortex
Magnoliae Officinalis, Fructus Aurantii Submaturus, Radix
Curcumae Wenyujin, Fructus Gradeniae, Herba Artemisiae
Capillaris, Radix et Rhizoma Rhei Palmati, mirabilite
Wei Xue Ning granule
Rhizoma Polygoni Cuspidati, Radix Paeoniae Alba,Herba
Agrimoniae, Radix Rehmanniae, Caulis Spatholobi, Herba
Ecliptae, Radix Pseudostellariae
Wu Wei Hu Zhang capsule
Rhizoma Polygoni Cuspidati, Fructus Schisandrae Chinensis,
Fructus Gradeniae, Radix Sophorae Flavescentis, Radix
Scutellariae Baicalensis, Spica Prunellae Vulgaris, Fructus
Ligustri Lucidui, Radix Paeoniae Rubra
Traditional and clinical uses
References
Curing appendicitis
Zhou (1985)
Curing acute hepatitis
Zhou (1985)
Curing urinary tract infection
"Zhong Yao Cheng Fang Zhi Ji" , vol. 12n
Curing inflammation, piles,
and proctitis
Curing bronchitis
Zhang et al. (2007a)
Shi et al. (2012)
Curing burn, inflammation and Wang and Liu (2011)
infection
Curing burn and infection
Zhou (1985)
Curing acute hepatitis
Zhou (1985)
Curing acute bacillary
Xu (1985)
dysentery
Curing gout of dampness heat Ding (2012)
accumulation
Curing burn, inflammation,
pain and infection
Curing burn and infection
Feng and Che (2010)
Treating acute gouty arthritis
Zhang et al. (2008)
Treating chronic pelvic pain
syndrome
Chen et al. (2011)
Curing prostatitis
Zhou et al. (2011)
Curing cholecystitis
"Zhong Yao Cheng Fang Zhi Ji" , vol. 16n
Curing arthralgia and myalgia
"Zhong Yao Cheng Fang Zhi Ji" , vol. 2n
Xiao et al. (2001)
Curing inflammations or
"Chinese Pharmacopoeia", vol.1nn
Huang et al. (2003)
bacterial infections
Curing inflammation and pain Zhao et al. (2007)
Curing burn and infection
"Zhong Yao Cheng Fang Zhi Ji" , vol. 17n
Curing burn and infection
"Chinese Pharmacopoeia", vol.1nn
Curing rheumatic arthritis
"Zhong Yao Cheng Fang Zhi Ji" , vol. 5n
Curing cholecystitis
"Zhong Yao Cheng Fang Zhi Ji" , vol. 20n
Curing atherosclerosis
thrombocytopenia
Chen and Zhang (2006);
Hua and Wu (2006)
Curing acute hepatitis
and cirrhosis
Ma (2010)
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
4
Table 1 (continued )
Preparation name
Main compositions
Traditional and clinical uses
References
Yang Yin Jiang Tang tablets
Rhizoma Polygoni Cuspidati, Radix Astragali Mongolici, Radix
Codonopsis, Radix Puerariae Lobatae, Fructus Lycii, Radix
Scrophulariae, Rhizoma Polygonati Odorati, Radix
Rehmanniae, Rhizoma Anemarrhenae, Cortex Moutan Radicis,
Rhizoma Chanxiong, Fructus Schisandrae Chinensis
Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori,
Rhizoma Dryopteridis Crassirhizomatis, Cortex Cinnamomi
Cassiae, Alumen, Pericarpium Punicae Granati, Radix
Angelicae Sinensis, Radix Salviae Miltiorrhizae, Semen
Astragail Complanati, Radix Ginseng, Herba Ephedrae Sinicae
Rhizoma Polygoni Cuspidati, Radix Dactylicapni Scandentis,
Caulis et Folium Clerodendri Bungei, Herba Hedyotidis, Spica
Prunellae Vulgaris, Herba Lobeliae Chinensis, Herba
Houttyniae Cordatae, Radix Gentianae, Radix Rubiae
Cordifoliae, Rhizoma Imperatae
Curing diabetes
"Chinese Pharmacopoeia", vol.1nn
Curing hepatitis B
Jin and Jin (2007)
Curing thanatophidia
bite and hyperlipidemia
"Zhong Yao Cheng Fang Zhi Ji" , vol. 19n
Yi Gan Fu Zheng capsule
Yun Nan She Yao
n
Cited from "Zhong Yao Cheng Fang Zhi Ji".
Cited from "Chinese Pharmacopoeia".
nn
In the present review, the advancements in investigation of
traditional usages, botany, phytochemistry, pharmacology (pharmacodynamics and pharmacokinetics) and toxicology of Polygonum cuspidatum are reviewed, which will be significant for the
exploitation for new drug and full utilization of this plant. The
possible tendency and perspective for future investigation of this
plant are discussed, too.
2. Traditional usages
With a wide spectrum of biological and pharmacological effects,
Polygonum cuspidatum has been used as a traditional medicine for a
long history in China. This plant has been often used for normalizing gallbladders and to cure jaundice in the traditional systems of
medicine (State Administration of Traditional Chinese Medicine,
1999). The root of this plant is used as the effective agent after
commonly processed by insolation, wine or salt (Jiangsu New
Medical College, 1977; State Administration of Traditional Chinese
Medicine, 1999) (Fig. 1C). Dating back over 1800 years according to
traditional Chinese medicine records (State Administration of
Traditional Chinese Medicine, 1999), the medicine application of
this plant was firstly listed in Mingyi Bielu (a famous monograph of
traditional Chinese medicine written in China during the Han
dynasty). In this monograph, this plant was described to be used
to treat abdominal masses since it had good diuretic property
(Tao, 1986; Cui, 1998). In Compendium of Materia Medica (Bencao
Gangmu), another famous monograph of traditional Chinese medicine, this plant was described to be used for treatment of
stranguria, urethritis and postpartum blood stasis (Li, 1979). In
other monographs of materia medica such as Dian-nan Bencao,
Rihuazi Bencao, Sichuan Zhoanyaozhi and others (Lan, 1959; State
Administration of Traditional Chinese Medicine, 1999), this plant
was also described to be used for treatment of suppuration, sore
throat, toothache, ulcer, hemorrhoids, chronic bronchitis and other
ailments.
Currently, in China, this well-known traditional herb is used as
the main composition in the forms of powders, decoctions or
infusions for treatment of inflammatory diseases (including hepatitis and suppurative dermatitis) as well as favus, jaundice, skin
burns, scald and hyperlipemia (Jiangsu New Medical College, 1977;
State Administration of Traditional Chinese Medicine, 1999)
(Table 1). In Japan, this plant is also popular in the traditional
Japanese herbal medicine system; its root is commonly used for
treatment of inflammation (Nonomura et al., 1963; Arichi et al.,
1980).
Polygonum cuspidatum is rich with resveratrol and polydatin
(Yu et al., 2005; Chen et al., 2013; Wu et al., 2013). The average
content of resveratrol is about 1–3 mg/g (Zhang et al., 2006;
Benova et al., 2008; Liang and Zou, 2011). Therefore, this plant
becomes the main resource of resveratrol, replacing grape byproducts (Hao et al., 2012). The average content of polydatin is about
3–8 mg/g. Therefore, this plant becomes the most important
concentrated source of polydatin (Benova et al., 2008; Liang and
Zou, 2011).
Besides its therapeutic applications, Polygonum cuspidatum has
been commonly used in daily food in China and Japan. The tender
stem of this plant is a delicious foodstuff with a little sour taste,
and the juice of roots can be used to dye rice flour (Su, 2010; Kirino
et al., 2012). In India and Southeast Asia, its dry leaves are used as
a kind of tobacco (Kirino et al., 2012).
3. Botany
Polygonum cuspidatum Sieb. et Zucc [synonyms: Reynoutria
japonica Houtt; Huzhang (
in Chinese), Yinyanglian
(
in Chinese), Itadori-kon (in Japanese), Kojo-kon (in
Japanese), Japanese knotweed and Mexican bamboo; Polygonaceae (Fig. 1)] is a large herbaceous perennial plant, and approximately 2 m high. The stems of this plant are numerous, erect,
and hollow with distinct raised nodes, often with red or purple
spots. The leaves are deciduous; the petioles are 1–2 cm
long and papillate. The leaf blades are ovate or broadly elliptic,
5–12 4–9 cm in size, and subleathery. Both leaf surfaces are
glabrous, and the leaves are papillate along the veins, with
broadly cuneate bases, are rounded or truncate in form, and
have entire margins. The apex is acute or shortly acuminate and
is not ciliate. Inflorescences are axillary, paniculate, and
approximately 3–8 cm in length; the bracts are funnel-shaped,
approximately 1–2 mm in length, and oblique. Each inflorescence contains two to four flowers. The pedicels are 3–4 mm in
length, slender, and articulate below the middle. The perianths
are white or greenish and five-parted. The male flowers have
eight stamens, which are longer than the perianth, while the
female flowers have three outer, accresent tepals that are
winged on the abaxial surface, three styles, and fimbriate
stigmas. The fruits are black–brown, shiny, ovoid–ellipsoid, 4–
5 mm achenes with persistent perianths (Arichi et al., 1980;
Editorial Board of Flora of China, 2003).
This plant is native in eastern Asia such as China, Japan and
Korea. It is widely cultivated in many provinces of China including
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
5
Table 2
Chemical compounds isolated from Polygonum cuspidatum.
Classification
nO.
Chemical component
Part of plant
Reference
Quinones
1
2
3
4
5
6
7
8
9
10
11
12
13
14
15
Root
Root
Root
Root
Root, rhizome
Root, rhizome
Root
Root
Root
Root
Root
Root
Root
Root, rhizome
Root
Tsukida and Yoneshige (1954)
Tsukida and Yoneshige (1954)
Kimura et al. (1983)
Kimura et al. (1983)
Murakami et al. (1968)
Murakami et al. (1968)
Tsukida and Yoneshige (1954)
Kimura et al. (1983)
Kimura et al. (1983)
Tsukida and Yoneshige (1954)
Zhang et al. (2012)
Zhang et al. (2012)
Kimura et al. (1983)
Jin and Jin, 2007
Zhu et al. (1985)
16
Physcion
Emodin
Fallacinol
Questin
Anthraglycoside A
Anthraglycoside B
Chrysophanol
Citreorosein
Questinol
Rhein
Polyganin A
Polyganin B
2-Methoxy-6-acetyl-7-methyljuglone
Cuspidatumin A
7-Acetyl-2-methoxy-6-methyl-8-hydroxyl,4-naphthoquinone
Phylloquinone B
Leave
17
Phylloquinone C
Leave
State Administration of Traditional Chinese
Medicine, 1999
State Administration of Traditional Chinese
Medicine, 1999
18
19
20
21
Resveratrol
Polydatin
Resveratrol-4′-O-glucoside
Resveratrol 4-O-D-(2′-galloyl)glucopyranoside
Resveratrol 4-O-D-(6′-galloyl)glucopyranoside
Sodium and potassium trans-resveratrol-3O-β-D-glucopyranoside-6″-sulfate
Sodium and potassium trans-resveratrol-3O-β-D-glucopyranoside-4″-sulfate
Sodium and potassium trans-resveratrol-3O-β-D-glucopyranoside-2″-sulfate
Sodium and potassium trans-resveratrol-3O-β-D-glucopyranoside-4′-sulfate
Sodium and potassium trans-resveratrol-3O-β-D-glucopyranoside-5-sulfate
Sodium and potassium cis-resveratrol-3-O-βD-glucopyranoside-6″-sulfate
Sodium and potassium cis-resveratrol-3-O-βD-glucopyranoside-4″-sulfate
Sodium and potassium cis-resveratrol-3-O-βD-glucopyranoside-3″-sulfate
Sodium and potassium cis-resveratrol-3-O-βD-glucopyranoside-2″-sulfate
Sodium and potassium cis-resveratrol-3-O-βD-glucopyranoside-5-sulfate
Root
Root
Root
Root
Nonomura et al. (1963)
Nonomura et al. (1963)
Gamini et al. (1993)
Hegde et al. (2004)
Root
Hegde et al. (2004)
Root
Xiao et al. (2000)
Root
Xiao et al., (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
Root
Xiao et al. (2000)
33
Rutin
Leave
34
35
36
37
38
39
40
41
Quercetin
Querectin-3-O-arabinoside
Quercitrin
Hyperoside
Isoquercitrin
Luteolin-7-O-glucoside
Apigenin
Reynoutrin
Root
Root
Root
Root
Root
Root
Root
Leave
42
43
(+)-Catechin
(+)-Catechin-5-O-β-D-glucopyranoside
Root
Root
State Administration of Traditional Chinese
Medicine (1999)
Kuznetsova (1979)
Kuznetsova (1979)
Kuznetsova (1979)
Kuznetsova (1979)
Kuznetsova (1979)
Kuznetsova (1979)
Kuznetsova (1979))
State Administration of Traditional Chinese
Medicine (1999)
Jayatilake et al. (1993)
Xiao et al. (2002)
Coumarins and lignans
44
45
46
47
Coumarin
7-Hydroxy-4-methoxy-5-methylcoumarin
Sodium (−)-lyoniresinol-2a-sulfate
Sodium (+)-isolaricireinol-2a-sulfate
Root, rhizome
Root
Root
Root
Jin and Jin, 2007
Kimura et al. (1983)
Xiao et al. (2002)
Xiao et al. (2002)
Other compounds
48
49
50
51
52
53
54
55
56
Protocatechuic acid
2,5-Dimethyl-7-hydroxy chromone
Torachrysone-8-O-d-glucoside
5,7-Dihydroxy-1(3H)-isobenzofuranone
Ambrettolide
β-Sitosterol
Oleanolic acid
Gallic acid
Tryptophan
Root
Root
Root
Root
Root, rhizome
Root, rhizome
Root, rhizome
Root
Root
Kimura et al. (1983)
Kimura et al. (1983)
Kimura et al. (1983)
Liu et al. (2003)
Jin and Jin (2007
Jin and Jin (2007
Jin and Jin (2007
Xiao et al. (2002)
Xiao et al. (2002)
Stilbenes
22
23
24
25
26
27
28
29
30
31
32
Flavonoids
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
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6
Table 2 (continued )
Classification
nO.
Chemical component
Part of plant
Reference
57
58
Root
Root
Xiao et al. (2002)
Xiao et al. (2002)
Root
Root
Xiao et al. (2002)
Xiao et al. (2002)
Root
Xiao et al. (2002)
62
63
2,6-Dihydroxy-bezoic acid
1-(3-O-β-D-Glucopyranosyl-4,5-dihydroxyphenyl)-ethanone
Tachioside
1-(3′,5′-Dihydroxyphenyl)-2-(4″hydroxyphenyl)-ethane-1,2-diol.
Sodium 3,4-dihydroxy-5-methoxybenzoic
acid methyl ester-4-sulfate
Isotachioside
Citric acid
Root
Stem, leave
64
Tartaric acid
Stem, leave
65
Hydroxysuccinic acid
Stem, leave
66
67
Chlorogenic acid
Polyflavanostilbene A
Root
Rhizome
Xiao et al. (2003)
State Administration of Traditional Chinese
Medicine (1999)
State Administration of Traditional Chinese
Medicine (1999)
State Administration of Traditional Chinese
Medicine (1999)
Lin et al., (2010)
Li et al. (2013)
59
60
61
Fig. 2. Chemical structures of quinones.
Anhui, Fujian, Gansu, Guangdong, Guangxi, etc., and other countries such as Japan, Korea, Russia and North America. It is
propagated by seeds and root during March to April, and its root
is harvested in the next spring or autumn and sun dried.
Polygonum cuspidatum flowers from June to September, and sets
fruit from July to October (State Administration of Traditional
Chinese Medicine, 1999).
As widely used as traditional Chinese medicines, there are
some adulterants of this plant, such as roots of Macleaya cordata
(Willd.) R. Br. (Papaveraceae), Sanguisorba offinalis L. (Rosaceae),
Rumex obtusifolius L. (Polygonaceae), Rumex japonicus Houtt.
(Polygonaceae), and Rheum palmatum L. (Polygonaceae), etc. Till
now, several methods have been developed to identify and
distinguish them; these methods are experiential identification,
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
7
Fig. 3. Chemical structures of stilbenes.
indicator compounds to characterize the quality of this plant with a
minimum contents of 0.6% and 0.15%, respectively, in the Pharmacopoeia of the People's Republic of China (Editorial Committee of
Chinese Pharmacopoeia, 2010).
4. Phytochemistry
Since the early 1950s, a lot of chemical compounds have been
isolated from Polygonum cuspidatum in China, Japan, Korean and
other countries. Most investigations just focused on the chemical
constituents of the roots of this plant because the root has
traditionally been used in herbal medicine. In this part, we describe
the main chemical constituents of this plant, their structures and
their isolation parts of this plant (Table 2) (Figs. 2–6).
4.1. Volatile compounds (essential oils)
Fig. 4. Chemical structures of flavonoids.
morphological identification, differential thermal analysis, ultraviolet spectrophotometry, TLC method, HPLC method and the ITS2
sequence of rDNA, etc. (Li et al., 1995; Zhuang et al., 2004; Sun
et al., 2008; Zhang and Peng, 2011; Li et al., 2012). Among these
methods mentioned above, HPLC method is regarded as the most
suitable method to evaluate the quality and authenticity of Polygonum
cuspidatum (Editorial Committee of Chinese Pharmacopoeia, 2010).
Although there are many main constituents including emodin, polydatin, resveratrol, physcion, and anthraglycoside B, etc. (Zhang et al.,
2007b; Zhang and Peng, 2011), emodin and polydatin are used as the
Limited work had been performed on the volatile components
of Polygonum cuspidatum. In one study, the essential oils in the
leaves of Polygonum cuspidatum were isolated by steam distillation
and solvent extraction, and then analyzed by GC/MS, 18 peaks were
identified (Kim et al., 2005). Among these peaks, the major volatile
compounds were 2-hexenal (73.36%), 3-hexen-1-ol (6.97%), n-hexanal
(2.81%), 1-penten-3-ol (2.55%), 2-penten-1-ol (2.21%), and ethy vinyl
ketone (1.13%).
4.2. Quinones
Since the first study of Polygonum cuspidatum in the 1950s,
quinones and their derivatives have been isolated and identified.
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
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Fig. 5. Chemical structures of coumarins and lignans.
Fig. 6. Chemical structures of other compounds.
These structurally unique quinones are classified into anthraquinones, naphthoquinones, and phylloquinones (Tsukida and
Yoneshige, 1954; Nonomura et al., 1963; Murakami et al., 1968;
Kimura et al., 1983; Zhu et al., 1985; Jin and Jin, 2007; Zhang
et al., 2012). Most of them belong to anthraquinones. The
predominant anthraquinone is emodin-type anthraquinone
including physcion (1), emodin (2), fallacinol (3), questin (4),
anthraglycoside A–B (5–6), chrysophanol (7), citreorosein (8),
questinol (9), rhein (10), anthraquinones polyganin A (11) and
B (12) (Fig. 2). Three naphthoquinones, 2-methoxy-6-acetyl7-methyljuglone (13), cuspidatumin A (14) and 7-acetyl-2methoxy-6-methyl-8-hydroxyl-, 4-naphthoquinone (15) were
isolated from Polygonum cuspidatum. What is more, Phylloquinone B (16) and C (17) were also isolated from the leaves of
Polygonum cuspidatum (State Administration of Traditional
Chinese Medicine, 1999).
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
4.3. Stilbenes
Plant stilbenes produced via the general phenylpropanoid
pathway are discovered in only a few higher degrees of plant
species (Chong et al., 2009). Stilbenes are other characteristic
components of this plant. Resveratrol (18) and polydatin (19) were
isolated and identified from this plant in 1963 (Nonomura et al.,
1963). Two stilbenes, identified as resveratrol 4-O-D-(2′-galloyl)glucopyranoside (21) and resveratrol 4-O-D-(6′-galloyl)-glucopyranoside (22), were isolated from a 70% aqueous methanolic extract
of the plant (Hegde et al., 2004). In addition, 10 additional
stilbenoid sulfates were subsequently isolated from an aqueous
acetone extract of the plant (Xiao et al. 2000), including sodium
and
potassium
trans-resveratrol-3-O-β-D-glucopyranoside-6″
-sulfate (23), sodium and potassium trans-resveratrol-3-O-β-Dglucopyranoside-4″-sulfate (24), sodium and potassium transresveratrol-3-O-β-D-glucopyranoside-2″-sulfate (25), sodium and
potassium
trans-resveratrol-3-O-β-D-glucopyranoside-4′-sulfate
(26), sodium and potassium trans-resveratrol-3-O-β-D-glucopyranoside-5-sulfate (27), sodium and potassium cis-resveratrol-3O-β-D-glucopyranoside-6″-sulfate (28), sodium and potassium
cis-resveratrol-3-O-β-D-glucopyranoside-4″-sulfate (29), sodium
and potassium cis-resveratrol-3-O-β-D-glucopyranoside-3″-sulfate
(30), sodium and potassium cis-resveratrol-3-O-β-D-glucopyranoside-2″-sulfate (31), sodium and potassium cis-resveratrol-3-O-βD-glucopyranoside-5-sulfate (32) (Fig. 3).
4.4. Flavonoids
Flavonols existing in numerous plants were detected in the
roots and leaves of Polygonum cuspidatum. These flavonols
included quercetin (34), quercetin derivatives or glycosides
(35–41), catechin (42) and its glycoside (43), and rutin (33)
(Kuznetsova, 1979; Jayatilake et al., 1993; State Administration
of Traditional Chinese Medicine, 1999; Xiao et al., 2002)
(Fig. 4).
4.5. Coumarins and lignans
So far, two coumarins and two lignans were isolated from
Polygonum cuspidatum. In 1983, 7-hydroxy-4-methoxy-5-methylcoumarin (45) was isolated from acetone extracts of Polygonum
cuspidatum (Kimura et al., 1983). Later, another coumarins compound named as coumarin (44) was isolated from this plant (Jin
and Jin, 2007). Additionally, two lignan sulfates were isolated from
an aqueous extract of this plant, including sodium (−)-lyoniresinol-2a-sulfate (46) and sodium (+)-isolaricireinol-2a-sulfate (47)
(Xiao et al., 2002) (Fig. 5).
4.6. Other compounds
An identified compound, 2,5-dimethyl-7-hydroxy chromone
(49), along with two known compounds [protocatechuic acid
(48) and torachrysone-8-O-d-glucoside (50)], were isolated
from this plant (Kimura et al., 1983). Gallic acid (55), tryptophan (56), 2,6-dihydroxy-bezoic acid (57), 1-(3-O-β- D -glucopyranosyl-4,5-dihydroxy-phenyl)-ethanon (58), tachioside
(59), 1-(3′,5′-dihydroxyphenyl)-2-(4″-hydroxyphenyl)-ethane1,2-diol (60), and sodium 3,4-dihydroxy-5-methoxybenzoic
acid methyl ester-4-sulfate (61) were also isolated from an
aqueous extract of this plant (Xiao et al., 2002). 5,7-dihydroxy1(3H)-isobenzofuranon (51) (Liu et al., 2003) and isotachioside
(62) (Xiao et al., 2003) were isolated from this plant. Furthermore, ambrettolide (52), β-sitosterol (53) and oleanolic acid
(54) were isolated (Jin and Jin, 2007). Additionally, citric acid
(63), tartaric acid (64), hydroxysuccinic acid (65) (State
9
Administration of Traditional Chinese Medicine, 1999), and
chlorogenic acid (66) were isolated from the roots, stems and
leaves of this plant (Lin et al., 2010a, 2010b) (Fig. 6). Recently, a
new flavanol-fused stilbene glycoside [polyflavanostilbene A
(67)], possessing a novel rearranged flavanol skeleton fused
stilbene, was isolated from the rhizome of this plant (Li et al.,
2013).
5. Pharmacodynamics and potential applications
5.1. Lipid regulating effect
The lipid regulating effect of stilbene compounds including
resveratrol and polydatin from Polygonum cuspidatum were
investigated in rats and mice models in 1980 (Arichi et al.,
1980). Polydatin (1.71 mmol/L) inhibited the vasoconstriction
induced by norepinephrine in a noncompetitive manner in
rabbits (Luo et al., 1992). If polydatin (100 mg/kg) was intragastricly administered to rats fed with a corn oil–cholesterol–cholic
acid mixture, the triglyceride level was reduced by 40% compared with the control group (Arichi et al., 1980). Additionally,
polydatin prevented platelet deformation and inhibited the
platelet release reaction of rabbits in a dose-dependent manner
(6.7, 26.8, and 107.2 μmol/L) (Liu et al., 1998). Moreover, in a highfat/cholesterol rabbit model (Syrian golden hamster or Japanese
giant ear rabbit), polydatin (25–100 mg/kg/day, po, for 15–21 days)
obviously decreased the serum levels of total cholesterol (TC),
triglyceride and low-density lipoprotein cholesterol (LDLC); the
ratio of total cholesterol/high-density lipoprotein cholesterol (TC/
HDLC) and the liver coefficient (LC) were reduced, too (Du et al.,
2009; Xing et al., 2009).
If resveratrol (50 mg/kg) was intragastricly administered to
mice, lipogenesis from 14C-palmitate in the livers of the mice
was reduced to 47% of control levels (Arichi et al., 1980). In vitro,
the water extract of Polygonum cuspidatum on acyl-coenzyme
A-cholesterol acyltransferase (ACAT) effect were investigated
using isolated rat microsomes as an enzyme source. This result
showed the water extract significantly inhibited ACAT activity in a
dose-dependent manner, and 40 μg/mL of this extract could
significantly inhibit ACAT activity by 50% compared with the
control group. Meanwhile, resveratrol also could decrease ACAT
activity in a dose-dependent manner (10−7–10−3 mol/L) (Park et al.,
2004).
5.2. Anti-shock effect
In vitro, polydatin (0.5%) decreased the levels of tumor necrosis
factor (TNF) and N-acetyl-β-glucosaminidase (NAG) in the supernatant of macrophages stimulated by lipopolysaccharide (LPS/
endotoxin) (Zhang et al., 1995a, 1997; Wu and Huang, 1996). In
vivo, polydatin, at a minimal concentration of 1 mg/kg, was found
to treat endotoxic shock in rats challenged with LPS (Zhang et al.,
1995a, 1995b, 1997; Wu and Huang, 1996; Jin et al., 1997; Shu
et al., 2004). It significantly decreased multiple organ injury of
endotoxic shock rats when administered at a dose of 10 mg/kg/
time (iv, for two times) (Zhang et al., 1995b). After investigation
the effect of polydatin on activity of phospholipase A2 (PLA2) in
the lung of endotoxic shock rats, polydatin (1 mg/kg, ip) was found
to have prophylactic and therapeutic effects on acutely injured
lung (the former was more distinct than the latter), suggesting
polydatin might be a PLA2 inhibitor (Shu et al., 2004). Furthermore, polydatin (1, 5, 10, and 30 mg/kg) dose-dependently inhibited the decrease of Clara cell secretory protein (CCSP) mRNA
and protein expressions in lung of rats challenged with LPS
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(Shu et al., 2011), which might be one of important mechanism of
polydatin to decrease LPS-induced lung injury.
5.3. Anti-inflammatory effect
Pretreatment with extracts of Polygonum cuspidatum could
inhibit LPS-induced iNOS mRNA expression (at doses of 10, 30,
and 60 μg/mL) and NO production (IC50 was 25.2 73.2 μg/mL). The
extracts (20 and 60 μmol/L) in combination with NOS inhibitor
significantly inhibited cyclooxygenase 2 (COX-2) mRNA expression
(Kim et al., 2007).
The inhibitory effect of ethanol extract of Polygonum cuspidatum (PCE) on ear inflammation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) was investigated in mice. The results
showed PCE significantly reduced the ear edema in a dosedependent manner (0.075, 0.15, 0.3, 1.25, and 2.5 mg/ear). 0.15,
0.3, 1.25, or 2.5 mg/ear of PCE was as effective as 0.5 mg/ear of
indomethacin, and 2.5 mg/ear of PCE displayed the outstanding
inhibitory rate of 80%. Additionally, pretreatment of 2.5 mg/kg PCE
could significantly decrease the myeloperoxidase activity in 12-Otetradecanoylphorbol-13-acetate (TPA)-treated mice, suggesting
PCE could inhibit edema and neutrophil infiltration of mice ears
(Bralley et al., 2008).
After treatment with the extract of Polygonum cuspidatum
(containing 20% resveratrol) at a dose of 200 mg/day for 6 weeks,
the mRNA expressions of TNF-α, IL-6, and C-reactive protein and
activation of their regulator NF-κB significant decreased (Ghanim
et al., 2010). In complete adjuvant (FCA)-induced adjuvant arthritis
model, 200 mg/kg of ethyl acetate extract of Polygonum cuspidatum (EAPC) significantly suppressed FCA-induced joint swelling
within 3 days, and EAPC also effectively inhibited positive
responses of C-reactive protein and rheumatoid factor compared
to untreated control (Han et al., 2011).
5.4. Hepatoprotective effect
The results from morphological examination of rats subjected
to liver ischemic injury showed that water extracts of Polygonum
cuspidatum (400 mg/rat/day, po., for 7 days) improved microcirculation of injured liver tissue and inhibited the adhesion of white
blood cells, blood plaque, and liver endothelial cell. Therefore, this
plant was considered to promote hepatocyte regeneration and
restored liver function (Hong et al., 2000). In addition, the water
extract of this plant (400 mg/rat/day, p.o. for 7 days) could protect
liver function in rats suffering from hepatic portal blockage (Gao
et al., 1998). Additionally, polydatin could protect hepatocytes
from oxidative injury induced by H2O2, too (Mo and Shao, 2000).
Recently, polydatin (50, 100 mg/kg/day, p.o. for 5 days) was found
to play the significant hepatoprotective effect on acute liver injury
in mice induced by CCl4, and the mechanisms might be related to
its antioxidant stress and anti-inflammatory effects (Zhang et al.,
2012).
5.5. Inhibition of melanogenesis effect
Tyrosinase is a key enzyme in the metabolism of melanin in
melanocytes. Therefore, inhibitor of the enzyme was important for
hyperpigmentation treatment (Kubo et al., 1995; Li et al., 2004). In
a study in 2008, four anthraqunones (physcion, emodin, citreorosein and anthraglycoside B) and two stilbenes (resveratrol and
polydatin) were isolated from Polygonum cuspidatum, and then the
antityrosinase effects of these compounds were evaluated. An
amount of 10 μmol/L of anthraquinones had the best inhibitory
effect against tyrosinase with physcion (approximately 70%), but
stilbenes did not (Leu et al., 2008). However, another experiment
found polydatin (10, 20, and 50 μg/mL) inhibited tyrosinase
activity and melanin production of melanocytes in a dosedependent manner; the inhibition rates were 20, 60, and 70%,
respectively. To explore the effects of polydatin on melanogenesis,
polydatin (20 and 50 μg/mL) on several key cellular enzymes and
transcriptional factors related to melanogenesis were investigated,
the results suggested polydatin might be used as a safe and new
skin-lightening agent (Jeong et al., 2010).
5.6. Estrogenic effect
Through bioassay-guided separation and analysis of estrogenic activity, emodin and emodin-8-O-β-D-glucopyranoside
were isolated from the methanol extract of Polygonum cuspidatum, and the results showed emodin and emodin-8-O-β-D-glucopyranoside could enhance proliferation of MCF-7 cell, an
estrogen-sensitive cell line; the emodin inhibited 17 β-estradiol
to bind to human estrogen receptors (ERs) with Ki values of 0.77
and 1.5 μM for ERα and ERβ, respectively (Matsuda et al., 2001).
Furthermore, the estrogenic activity of Polygonum cuspidatum
and its fractions were investigated by a recombinant yeast
screening assay; the results showed the ethyl acetate fractions
(Hzs1 and Hzs6) of ethyl acetate extracts of this plant exhibited
strong estrogenic activity (EC50 were 10−4 and 10−3 g/L, respectively). HPLC analysis for the active components suggested that
there was no unknown bioactive compound existed in the
extraction (Zhang et al., 2006).
5.7. Antioxidant effect
Polydatin (3.2, 6.4, 12.8, and 25.6 μmol/L) inhibited the early
stage (1–6 min) of the respiratory burst of polymorphonuclear
leucocytes in a dose-dependent manner. In addition, polydatin had
a strong ability to scavenge oxygen free radicals [IC50 were 14.6,
29.6, and 13.0 μmol/L for superoxide radicals (O2−), hydroxyl
radicals (OH−), and hydrogen peroxide (H2O2), respectively] (Jin
et al., 1993). After rats were treated with polydatin, the water and
malondialdehyde contents of brain decreased; the activities of
superoxide dismutase, catalase and glutathione peroxidase of the
cerebral cortex and hippocampus increased; the optimal dose of
polydatin to reduce free radicals was 12 mg/kg (i.v.) (Leung and
Mo, 1996). In addition, the extract of this plant exhibited good
scavenging activity against DPPH radicals; 100 μg/mL of this
extract possessed the most significantly scavenging activity over
90% (Meng and Hang, 2000; Pan et al., 2007; Lin et al., 2010a).
What is more, 200 mg/day of Polygonum cuspidatum extract
(containing 20% resveratrol) could significantly reduce the reactive
oxygen species generation of mononuclear cells (Ghanim et al.,
2010).
5.8. Anticancer effect
The compounds and extracts of Polygonum cuspidatum also
possessed anticancer/antitumor effect. The main effective substances were thought to be resveratrol and emodin (Zhou et al.,
1989; Tseng et al., 2004; Feng et al., 2006).
The water extracts of this plant (20 g/kg/day, crude herb
medicine equivalent, 10 days) inhibited the growth of Ehrlich's
carcinoma and prolonged the life span of tumor-bearing Kunming
mice (Zhou et al.1989). The ethanol extract of this plant (0.2, 0.4,
0.6, and 0.8 mg/mL) exhibited an antiproliferative effect against
human lung cancer cells of A549 and H1650 cells in a dosedependent manner (Lin et al., 2010a).
Resveratrol (2.5 and 10 mg/kg, ip., for 5 days) significantly
reduced Lewis lung tumor volume (42%) and tumor weight
(44%), and prevented tumor growth and metastasis in lungs
(56%) by inhibiting DNA synthesis of tumor cells, as well as
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
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11
Table 3
Pharmacological effects of Polygonum cuspidatum.
Pharmacological
effects
Detail
Extracts/compounds
Minimal active
concentration/dose
In vitro/in vivo
Reference
Lipid regulating
effect
Inhibits the vasoconstrictive effect
Polydatin
1.71 mmol/L
In vitro
Luo et al. (1992)
Reduce triglyceride level
Reduce lipogenesis of rats
Inhibit the activity of ACAT
Resveratrol
Polydatin
Water extracts/
resveratrol
Polydatin
100 mg/kg, po
50 mg/kg, po
40 μg/ml/10−7 mol/L
In vivo
In vivo
In vitro
Arichi et al., (1980)
Arichi et al., (1980)
Park et al., (2004)
In vivo
Du et al. (2009), Xing et al.
(2009)
Liu et al. (1998)
Anti-shock activity
Antiinflammatory
activity
Hepatoprotective
activity
Inhibition of
melanogenesis
effect
Estrogenic activity
Antioxidant activity
Decreases levels of TC, triglyceride, LDLC, TC/
HDLC, and LC
Prevents platelet deformation, and inhibits the
platelet release reaction
Anti-endotoxic shock
Polydatin
25–100 mg/kg/day, po,
15–21 days,
6.7 μmol/L
Polydatin
1 mg/kg
In vivo
Protect against multiple organ injury
Polydatin
In vivo
Prophylactic and therapeutic effects on acute
lung injure
Decreases levels of TNF and NAG
Polydatin
10 mg/kg/time, iv, for
2 times
1 mg/kg, ip
Zhang et al., (1995a, 1995b),
(1997), Wu and Huang
(1996); Jin et al. (1997); Shu
et al. (2004), (2011)
Zhang et al. (1995b)
In vivo
Shu et al. (2004)
Polydatin
0.5%
In vitro
Inhibits iNOS, NO production, and COX-2
Water extracts
In vitro
Reduced ear edema induced by TPA
Ethanol extracts
10 μg/mL iNOS; IC50 of
NO production was
25.2 73.2 μg/mL;
20 mol/L for COX-2
0.075 mg/ear
Zhang et al. (1995a), Wu and
Huang (1996), Zhang et al.
(1997)
Kim et al. (2007)
In vivo
Bralley et al. (2008)
Reduces myeloperoxidase activity
Reduce TNF-α and IL-6 expression
Ethanol extracts
Extracts (containing
20% resveratrol)
Ethyl-acetate extracts
2.5 mg/ear
In vivo
200 mg/day, for 6weeks In vivo
Bralley et al. (2008)
Ghanim et al. (2010)
200 mg/kg, po
In vivo
Han et al. (2011)
Water extracts
In vivo
Hong et al. (2000)
In vivo
Gao et al. (1998)
Polydatin
400 mg/rat/day, po, for
7 days
400 mg/rat/day, po, for
7 days
0.05 mmol/L
In vitro
Mo and Shao (2000)
Polydatin
50 mg/kg
In vivo
Zhang et al. (2012)
Physcion
10 μmol/L
In vitro
Leu et al. (2008)
10 μmol/L
10 μmol/L
10 μmol/L
20 μg/mL
1 μmol/L
1 μmol/L
In
In
In
In
In
In
Leu et al. (2008)
Leu et al. (2008)
Leu et al. (2008)
Jeong et al. (2010)
Matsuda et al. (2001)
Matsuda et al. (2001)
EC50 ¼ 10−4 g/L and
10−3 g/L
In vitro
Zhang et al., (2006)
3.2 μmol/L
In vitro
Jin et al. (1993)
In vitro
Jin et al. (1993)
Polydatin
IC50 ¼14.6, 29.6, and
13.0 μmol/L for O2−,
OH−, and H2O2.
12 mg/kg, iv
In vivo
Leung and Mo (1996)
Ethanol extracts
0.2 mg/mL
In vitro
Extract (containing
20% resveratrol)
Water extracts
200 mg/day, for 6 weeks In vivo
Meng and Hang (2000), Pan
et al. (2007), Lin et al.
(2010a)
Ghanim et al. (2010)
Inhibit the swelling inflammatory response
induced by serotonin
Protective effect on liver ischemic injury in rats
Protect liver function in rats suffering from
hepatic portal blockage
Protect hepatocytes from oxidative injury
induced by H2O2 in mice
Protective effects against CCl4-induced liver
injury in mice
Inhibit melanogenesis
Emodin,
Citreorosein,
Anthraglycoside B
Polydatin
Enhanced MCF-7 proliferation
Emodin
Emodin-8-O-β-D –
glucopyranoside
Estrogenic activity
Subfractions of ethyl
acetate extracts (Hzs
1 and Hzs 6)
Inhibit the early stage of the respiratory burst of Polydatin
polymorphonuclear leucocytes and scavenges
oxygen free radicals
Scavenging superoxide radicals
Polydatin
Decrease the content of brain water and
malondialdehyde; increase the activities of
superoxide dismutase, catalase, and glutathione
peroxidase in the cerebral cortex and
hippocampus
Scavenging activity against DPPH radicals
Anticancer activity
Water extracts
Reduce reactive oxygen species generation by
mononuclear cells
Inhibit the growth of Ehrlich's carcinoma and
prolong the life span of tumor-bearing mice
Reduce Lewis lung tumor volume and weight in Resveratrol
mice, and prevent tumor growth and metastasis
Aantitumor effects on s.c. gliomas
Resveratrol
In vitro
vitro
vitro
vitro
vitro
vitro
vitro
20 g/kg/day, crude herb In vivo
medicine equivalent, for
10 days
2.5 mg/kg, ip, for 5 days In vivo
Zhou et al. (1989)
40 mg/kg, ip, over a
period of 150 days
Tseng et al. (2004)
In vivo
Kimura and Okuda (2001)
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12
Table 3 (continued )
Pharmacological
effects
Antiviral activity
Detail
Extracts/compounds
Minimal active
concentration/dose
In vitro/in vivo
Reference
Cytotoxic effect against MCF-7 and adriamycinresistant MCF-7 cells
Anti-lung cancer
Anti-uveal melanoma tumors
Resveratrol
In vitro
Feng et al. (2006)
Ethanol extracts
Resveratrol
In vitro
In vivo
Lin et al. (2010a)
van Ginkel et al., (2008)
Anti-human neuroblastomas
Anti-human neuroblastomas
Resveratrol
Resveratrol
In vivo
In vivo
Van Ginkel et al. (2008)
Van Ginkel et al., (2007)
Anti-ovarian cancer
Resveratrol
In vivo
Guo et al. (2010)
Anti-lymph cancer
Anti-atypical teratoid tumors
Anti-hepatic cancer
Resveratrol
Resveratrol
Resveratrol
IC50 ¼58.4 and 56.7 μg/
ml
0.2 mg/mL
20 mg/tumor/times,
peritumor injection,
three times
5 mg/tumor/times,
5 mg/tumor/times,
peritumor injection,
5 times
50 mg/kg/week, ip, once
a week for 4 weeks
100 μmol/L
150 μmol/L
12.5 μmol/L
In vitro
In vitro
In vitro
Anti-glioma cells
Anti-human chronic myelocytic leukemia K562
cells
Anti-human prostate cancer cells
Anti-HIV using AIDS-infected murine model
Emodin
Emodin
100 μmol/L
25 μmol/L
In vitro
In vitro
Yan et al. (2010)
Kao et al. (2009)
Hsu et al. (2010), Liao et al.,
(2010), Siddiqui et al. (2010),
Xu et al. (2010)
Kuo et al. (2009)
Chun-Guang et al. (2010)
Emodin
Water extract
10 μmol/L
50 mg/mouse/day, po,
for 4 weeks
10 μmol/L
In vitro
In vivo
Yu et al. (2008)
Jiang et al. (1998)
In vitro
Zhang et al. (2009)
Attenuate Tat-induced HIV-1 transactivation in
MAGI cells
Anti- HIV-1
Anti- HIV-1
Anti- HIV-1
Anti- HIV-1
Activities against VSV, HSV-1 and 2, PV,
and VV
Anti-HSV-1
Antibacterial and
antifungal
activities
Resveratrol
Resveratrol
5,7Dimethoxyphthalide
Catechin
Emodin-8-O-β-Dglucopyranoside
Hypericin
EC50 ¼ 4.37 7 1.96 μg/mL In vitro
19.97 7 5.09 μg/mL
In vitro
Lin et al., (2010b)
Lin et al., (2010b)
14.4 71.34 μg/mL
11.297 6.26 μg/mL
In vitro
In vitro
Lin et al. (2010b)
Lin et al. (2010b)
1 μg/mL
In vitro
Andersen et al. (1991)
Emodin
4 mg/mL, once a day
applied on the skin, for
7 days
10 μg/mL
13.8 μmol/L
1 g/mL, crude herb
medicine equivalent;
IZ ¼1.122 cm
MIC¼ 312.5 μg/mL
1 g/mL, crude herb
medicine equivalent;
IZ ¼1.113 cm
1 g/mL, crude herb
medicine equivalent;
IZ ¼0.903 cm
1 g/mL, crude herb
medicine equivalent;
IZ ¼0.800 cm
MIC¼ 0.5–4 mg/mL
In vivo
Wang et al. (2003)
In vitro
In vitro
In vitro
Chang et al. (2005)
Yiu et al. (2010)
Wang et al. (2006)
In vitro
In vitro
Shan et al. (2008)
Wang et al. (2006)
In vitro
Wang et al. (2006)
In vitro
Wang et al. (2006)
In vitro
Song et al. (2006), (2007)
MIC¼ 0.25 mg/mL
MIC¼ 0.125 mg/mL
MIC¼ 0.5 mg/mL
MIC¼ 0.5 mg/mL
MIC¼ 1 mg/mL
MIC¼ 0.5 mg/mL
MIC¼ 1 mg/mL
MIC¼ 0.5 mg/mL
10% (v/v)
In
In
In
In
In
In
In
In
In
Ban et al. 2010
Ban et al. (2010)
Ban et al. (2010)
Ban et al. (2010)
Ban et al. (2010)
Ban et al. (2010)
Ban et al. 2010
Ban et al. (2010)
Kim et al. (2005)
MIC¼ 312.5 μg/mL
MIC¼ 312.5 μg/mL
1 g/mL, crude herb
medicine equivalent;
IZ ¼1.112 cm
1 g/mL, crude herb
medicine equivalent;
IZ ¼1.127 cm
1 g/mL, crude herb
medicine equivalent;
IZ ¼0.929 cm
10% (v/v)
In vitro
In vitro
In vitro
Shan et al. (2008)
Shan et al. (2008)
Wang et al. (2006)
In vitro
Wang et al. (2006)
In vitro
Wang et al. 2006
In vitro
Kim et al. (2005)
In vitro
Zhang et al. (2000)
HBV
EBV
Anti-Staphylococcus aureus
Ethanol extracts
Resveratrol
Water extracts
Anti-Staphylococcus albus
Crude extract
Water extracts
Anti-alpha Streptococcus
Water extracts
Anti-beta Streptococcus
Water extracts
Anti-Streptococcus mutans and Streptococcus
sobrinus
Anti-Streptococcus cricetus KCTC 3292
Anti-Streptococcus mutans KCTC 3298
Anti-Streptococcus mutans KCTC 3300
Anti-Streptococcus mutans KCTC 3306
Anti-Streptococcus mutans KCTC 3289
Anti-Streptococcus sobrinus KCTC 3307
Anti-Streptococcus sobrinus KCTC 3308
Anti-Streptococcus sobrinus KCTC 3288
Anti-Bacillus cereus
Methanol extracts
Anti-Listeria monocytogenes
Anti-Pseudomonas aeruginosa
Methanol extract
Methanol extract
Methanol extract
Methanol extract
Methanol extract
Methanol extract
Methanol extract
Methanol extract
Volatile-substances
from leaves
Crude extract
Crude extract
Water extracts
Anti-Escherichia coli
Water extracts
Anti-Bacterium typhosum
Water extracts
Anti-Vibrio parahaemolyticus
Volatile substances
from leaves
Water extracts
vitro
vitro
vitro
vitro
vitro
vitro
vitro
vitro
vitro
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Table 3 (continued )
Pharmacological
effects
Detail
Extracts/compounds
Antifungal activity (Trichophyton rubrum,
Microsporum gypseum, Fonsecaea pedrosoi,
Candida albican)
Others
Resveratrol 4-O –
Inhibitive activities on the bacterial
DNA primase enzyme
D-(2′-galloyl)-
Wound healing activity
glucopyranoside
Resveratrol 4-O –
D-(6′-galloyl)glucopyranoside
Ethanol extract
Protect dopaminergic neurons in rats with
Parkinson's disease
Analgesic effect by using hot plate and
tail-flicking tests
Inhibitory activity against α-glucosidase
Minimal active
concentration/dose
In vitro/in vivo
Reference
MICs were 5, 10, 20,
40 mg/mL, respectively,
crude herb medicine
equivalent
IC50 ¼4 μmol/L
In vitro
Hegde et al. (2004)
IC50 ¼5 μmol/L
In vitro
Hegde et al. (2004)
Ethyl acetate extracts
10% (w/w), applied on
In vivo
the skin, once a day, for
7 days
20 mg/kg/day, po, for 14 In vivo
day
200 mg/kg, po
In vivo
Polyflavano-stilbene A
IC50 ¼17.7 μmol/L
Resveratrol
tumor-induced neovascularization in mice bearing highly metastatic Lewis lung tumors (Kimura and Okuda, 2001). In another
experiment of rats with the s.c or intracerebral gliomas, resveratrol
(40 mg/kg/day, ip, over a period of 150 days) possessed significantly antitumor effects such as slower tumor growth rate, longer
animal survival time and higher animal survival rate. The mechanisms were thought to be related to its cytotoxic effect, increased
apoptosis and inhibited angiogenesis (Tseng et al., 2004). Resveratrol also played its cytotoxic effects against MCF-7 cells and
adriamycin-resistant MCF-7 cells with IC50 values of 58.4 and
56.7 μg/mL, respectively (Feng et al., 2006). Resveratrol also
exhibited anticancer effects against ovarian cancer (Guo et al.,
2010), lymph cancer (Yan et al., 2010), atypical teratoid/rhabdoid
tumors (Kao et al., 2009), hepatic cancer (Hsu et al., 2010; Liao
et al., 2010; Siddiqui et al., 2010; Xu et al., 2010), uveal melanoma
tumors and human neuroblastomas (van Ginkel et al., 2007, 2008),
etc.
Emodin also exhibited cytotoxic effects against glioma cells
(Kuo et al., 2009), human chronic myelocytic leukemia K562 cells
(Chun-Guang et al., 2010) and human prostate cancer cell LNCaP
(Yu et al., 2008).
5.9. Antiviral effect
Several studies demonstrated that the extracts or active compounds isolated from Polygonum cuspidatum were somewhat
beneficial for therapy of human immunodeficiency virus (HIV)
(Jiang et al., 1994, 1998; James, 2006; Zhang et al., 2009; Lin et al.,
2010b). The water extract (50 mg/mouse/day, po, for 4 weeks) had
an antiviral effect in an HIV-infected murine model (Jiang et al.,
1998). Resveratrol pretreatment dose-dependently increased
intracellular NAD+ level and Sirtuins 1 protein expression after
Tat plasmid transfection, and attenuated Tat-induced HIV-1 transactivation in MAGI cells, suggesting resveratrol was considered as
a potential candidate for novel anti-HIV therapeutics (Zhang et al.,
2009). 5,7-dimethoxyphthalide, catechin and emodin 8-O-β-Dglucopyranoside and resveratrol exhibited fairly strong antiviral
effect against HIV-1; EC50 values were 19.977 5.09, 14.4 71.34,
11.29 76.26, and 4.37 71.96 μg/mL, respectively (Lin et al., 2010b).
Additionally, the extract and resveratrol isolated from Polygonum cuspidatum were employed against hepatitis B virus (HBV)
(Chang et al., 2005) and Epstein–Barr virus (EBV) (Yiu et al., 2010).
Less than 1 μg/mL of hypericin and emodin were possible potential
candidates of vesicular stomatitis virus (VSV), types 1 and 2 herpes
In vitro
Wu et al. (2012)
Wang et al. (2011)
Han et al. (2011)
Li et al. (2013)
simplex virus (HSV), parainfluenza virus (PV) and vaccinia virus
(VV) after determined by a direct pre-infection incubation assay
(Andersen et al., 1991; Wang et al., 2003).
5.10. Antibacterial and antifungal effects
Antibacterial effect, an important effect of Polygonum cuspidatum, had been comprehensively investigated. The water extract of
this plant (1 g/mL, crude herb medicine equivalent) possessed a
broad range of antibacterial effect against Staphylococcus aureus,
Staphylococcus albus, Pseudomonas aeruginosa, Escherichia coli,
Bacterium typhosum, alpha Streptococcus and beta Streptococcus;
the inhibition zones were 1.122, 1.113, 1.112, 1.127, 0.903, 0.800, and
0.929 cm, respectively (Wang et al., 2006). The methanol extracts
also possessed antibacterial effects against Streptococcus mutans
and Streptococcus sobrinus [minimal inhibitory concentration
(MIC) was 0.5–4 mg/mL], suggesting methanol extract might be
useful for controlling dental plaque formation and the subsequent
formation of dental caries (Song et al., 2006, 2007). Additionally,
the crude extract of this plant exhibited antibacterial effect against
three of the five common foodborne bacteria including Bacillus
cereus, Listeria monocytogenes, and Staphylococcus aureus (MIC
were 312.5, 156.3, and 312.5 μg/mL, respectively; minimal bactericidal concentration (MBC) were 625, 312.2, and 1250 μg/mL,
respectively), but the MIC and MBC values against Escherichia coli
and Salmonella anatum were more than 2500 μg/mL.
The major antibacterial compounds were identified as stilbenes
(polydatin, resveratroloside and resveratrol) and hydroxyanthraquinones (emodin, emodin-1-O-glucoside, and physcion) by LCESI-MS (Shan et al., 2008). In 2010, the antibacterial effects of the
methanol extract and its subsequent fractions of this plant were
evaluated on the development of dental caries. The results showed
the ethyl acetate fraction, composed of polydatin, resveratrol,
anthraglycoside B and emodin, had a significant antibacterial
effect against Streptococcus cricetus KCTC 3292, Streptococcus
mutans KCTC 3298, Streptococcus mutans KCTC 3300, Streptococcus
mutans KCTC 3306, Streptococcus mutans KCTC 3289, Streptococcus
sobrinus KCTC 3307, Streptococcus sobrinus KCTC 3308 and Streptococcus sobrinus KCTC 3288 (MIC were 0.25, 0.125, 0.5, 0.5, 1, 0.5, 1,
and 0.5 mg/mL, respectively; MBC were 0.5, 2, 1, 2, 2, 2, 4, and
2 mg/mL, respectively). This fraction also exhibited significant
inhibition on glycolytic acid production and glucosyltransferase
effect in Streptococcus mutans and Streptococcus sobrinus (Ban
et al., 2010). The addition of 10% (v/v) of the volatile substances
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extracted from the leaves of this plant could completely inhibit the
growth of Bacillus cereus and Vibrio parahaemolyticus for 72 h (Kim
et al., 2005).
Additionally, the extracts of this plant was also found to exhibit
antifungal effect against four fungus such as Trichophyton rubrum,
Microsporum gypseum, Fonsecaea pedrosoi and Candida albican
(MICs were 5, 10, 20, and 40 mg/mL, respectively, crude herb
medicine equivalent) (Zhang et al., 2000).
What is more, resveratrol 4-O-D-(2′-galloyl)-glucopyranoside
and resveratrol 4-O-D-(6′-galloyl)-glucopyranoside were identified
as two bacterial DNA primase inhibitors (IC50 were 4 and 5 μmol/L,
respectively) (Hegde et al., 2004).
5.11. Other pharmacological effects
The effect of Polygonum cuspidatum extract on wound healing
was investigated on the backs of model rats, the results showed
the extract at a concentration of 10% possessed wound healing
effect; the average times of decrustation and healing time were
7.05 71.23 and 15.10 72.37 days, respectively (Wu et al., 2012).
Additionally, 200 mg/kg of the ethylacetate fraction had a significant analgesic effect determined by hot plate and tail-flicking tests,
suggesting the extract might be used for rheumatoid arthritis (Han
et al., 2011). Importantly, resveratrol (20 mg/kg/day 14 day, p.o.)
could protect dopaminergic neurons in rats with Parkinson's
disease for its radical scavenging ability and antioxidant properties
(Wang et al., 2011). Recently, a flavanol-fused stilbene glycoside
isolated from this plant, named as polyflavanostilbene A, showed
strong inhibition on α-glucosidase (IC50 was 17.7 μmol/L) (Li et al.,
2013).
5.12. Summary of pharmacologic effects
Polygonum cuspidatum has a wide spectrum of pharmacological
effects including lipid regulating effect, anti-shock effect, antiinflammatory effect, antioxidant effect, anticancer effect, hepatoprotective effect, antiviral effect, and antibacterial and antifungal
effects, etc (Table 3). From these pharmacological effects, we can
come to the indication of the extracts and the compounds from
this plant should have a hopeful future for prevention or treatment of diseases (especially hyperlipemia disease, inflammation/
infection, and cancer). However, there is no enough systemic data
of these chemical compounds and their pharmacological effects.
Therefore, it is necessary and important to investigate the pharmacological effects and molecular mechanisms of these chemical
compounds based on modern realization of diseases’ pathophysiology in the future. In addition, isolation and purification of the
chemical constituents from this plant under the guide of target or
bioactivities and subsequent evaluation of their pharmacologic
effects will promote the development of new drug and make sure
which chemical constituent or multiple ingredients contributes its
pharmacological effects.
6. Pharmacokinetics
In one pharmacokinetics experiment of rats accepted Polygonum cuspidatum extract, after the tissues were extracted with
methanol and the urinary and biliary samples were cleaned using
solid-phase extraction, the metabolites were identified by LC/MS/
MS. Resveratrol, one of the main components of Polygonum
cuspidatum, was found to be mainly distributed in the stomach,
duodenum, liver and kidney, along with detectable metabolites
including resveratrol monoglucuronide and resveratrol monosulfate; the majority of the resveratrol was excreted as a metabolite
(Wang et al., 2008). In another pharmacokinetics experiment of
rats, emodin, another active compound of this plant, was investigated using a rapid, sensitive and selective HPLC method. The
results showed emodin could be absorbed rapidly into the bloodstream and distributed quickly into the liver (Peng et al., 2008).
The recent results showed the sulfates/glucuronides of resveratrol
and emodin were the major forms, determined by HPLC method,
in circulation and organs after oral administration of Polygonum
cuspidatum (Lin et al., 2012).
7. Toxicology
Polygonum cuspidatum has been used for hundreds of years as
an important traditional herb in China, but this plant is prohibited
for pregnant women because it is generally considered to induce
abortion according to the theory of traditional Chinese Medicine
(State Administration of Traditional Chinese Medicine, 1999). At
present, the relative systematic toxicity and safety investigation of
this plant were lacking; few evaluations of target-organ toxicity or
side effects had been documented. But it was reported that the
oral administration of anthraquinones (9 g/kg) did not cause death
in mice in a maximal tolerance dose test, and the LD50 of emodin
and polydatin were 249.5 734.3 and 1000 757.3 mg/kg, respectively (Analysis of Chinese medicine research laboratory, Shanghai
institute of pharmaceutical industry, 1976). Under experimental
condition, there were no hemolysis in vitro or agglutination
reaction (0.39 mg/mL), systemic anaphylaxis or passive skin
allergy (5.6 mg/kg) and stimulating effect in rabbit auricular
vessels and muscles (5.6 mg/kg) (Xu et al., 2008). However,
injection of polydatin could dose-dependently induce peritonitis
in a subacute toxicity test (The 173rd unit of PLA, 1973)
8. Future perspectives and conclusion
In traditional Chinese medicine, Polygonum cuspidatum has
long been used for treatment of hyperlipemia, inflammation,
infection and cancer, etc. Quinones and stilbenes are considered
as the major constituents with pharmacologic effects. Many
traditional applications have been studied by modern investigation. However, there is no enough systemic data about the
pharmacokinetics and toxicity of this plant, especially targetorgan toxicity; therefore, more investigations should be done in
the future.
In traditional Chinese medicine, Polygonum cuspidatum is
commonly used in composition with other herbs and not use
alone. Although modern experiments validate this plant alone
exhibits significantly pharmacological effects, it is interesting and
important to investigate pharmacological effects and molecular
mechanisms of Polygonum cuspidatum combined with other herbs
based on modern concepts of diseases’ pathophysiology. Drug
target-guided and bioactivity-guided isolation and purification of
the chemical constituents and subsequent evaluation of the
pharmacologic effects will promote the development of new drug
and make sure which chemical constituent or multiple ingredients
contributes its pharmacological effects.
In traditional Chinese medicine, the root of Polygonum cuspidatum is used as the effective agent. However, the aerial part of
this plant is commonly disposed in landfills without usage
although this part weighs no less than 50% of the total mass of
the plant. At present, there are very few investigations on this part,
it is necessary to investigate the chemical constituents and
pharmacological effects of the aerial part, and then find new
chemical constituents in order to reuse the aerial part as a
value-added product of Polygonum cuspidatum in the future.
Please cite this article as: Peng, W., et al., Botany, phytochemistry, pharmacology, and potential application of Polygonum cuspidatum
Sieb.et Zucc.: A review. Journal of Ethnopharmacology (2013), http://dx.doi.org/10.1016/j.jep.2013.05.007i
W. Peng et al. / Journal of Ethnopharmacology ∎ (∎∎∎∎) ∎∎∎–∎∎∎
With an increasing interest of this plant in recent years, more
and more phytochemical and pharmacological investigations will
renew our knowledge of this plant. Detailed investigations on
toxicity, pharmacodynamics, pharmacokinetics and molecular
mechanism will help to develop its bioactive constituents as
effective drugs.
Acknowledgement
The authors are grateful to the associate professor Cheng-Zi
Yang (Department of pharmacy, Fujian University of Traditional
Chinese Medicine, Fuzhou, China) for the pictures of Polygonum
cuspidatum.
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