Root Of Polygonum Cuspidatum Research Articles

Polydatin suppresses ultraviolet B-induced cyclooxygenase-2 expressionin vitroandin vivovia reduced production of reactive oxygen species

Funding sources: this work was supported by the grants from the Ministry of Science and Technology (2010CB945400). Conflicts of interest: none declared. Madam, Polydatin (resveratrol‐3‐O‐β‐d‐glucoside; Fig. 1a), a polyphenolic phytoalexin with a strong antioxidative activity, is isolated from the dried roots of Polygonum cuspidatum, which is widely used in traditional Chinese medicine.1, 2 In this study, we demonstrated the underlying mechanisms by which polydatin protects the skin from ultraviolet (UV) B‐induced damage in vitro and in vivo. Polydatin exerted no cell toxicity on HaCaT cells at low concentrations, as cell viability did not decrease when HaCaT cells were treated with various concentrations of polydatin up to 100 μg mL−1 (Fig. 1b). Irradiation with 30 mJ cm−2 of UVB resulted in 42·8 ± 2·7% of cell death compared with the nonirradiated group; polydatin reduced HaCaT cell death induced by UVB‐irradiation in a dose‐dependent manner (Fig. 1c). Furthermore, more cell death was observed after UVB irradiation compared with that seen in the nonirradiated groups. The effect of polydatin in reducing HaCaT cell death is shown in Figure 1d and Figure S1 (see Supporting information).

De novo characterization of the root transcriptome of a traditional Chinese medicinal plant Polygonum cuspidatum

Various active components have been extracted from the root of Polygonum cuspidatum. However, the genetic basis for their activity is virtually unknown. In this study, 25600002 short reads (2.3 Gb) of P. cuspidatum root transcriptome were obtained via Illumina HiSeq 2000 sequencing. A total of 86418 unigenes were assembled de novo and annotated. Twelve, 18, 60 and 54 unigenes were respectively mapped to the mevalonic acid (MVA), methyl-D-erythritol 4-phosphate (MEP), shikimate and resveratrol biosynthesis pathways, suggesting that they are involved in the biosynthesis of pharmaceutically important anthraquinone and resveratrol. Eighteen potential UDP-glycosyltransferase unigenes were identified as the candidates most likely to be involved in the biosynthesis of glycosides of secondary metabolites. Identification of relevant genes could be important in eventually increasing the yields of the medicinally useful constituents of the P. cuspidatum root. From the previously published transcriptome data of 19 non-model plant taxa, 1127 shared orthologs were identified and characterized. This information will be very useful for future functional, phylogenetic and evolutionary studies of these plants.

Resveratrol: Potential as Anticancer Agent

ABSTRACTBackground: Cancer is one of the leading causes of deaths in the world. Current chemotherapeutic agents are associated with serious side effects in patients therefore researchers are trying to find an alternative agent that is effective against cancer as well as less toxic. Resveratrol (3,5,4′-trihydroxystilbene), commonly found in red wine and grape skins, is a phytoalexin agent that was originally extracted from the roots of Polygonum cuspidatum. Resveratrol is believed to work as a chemopreventive agent by producing its effect on cell apoptosis, antiproliferation, and anti-inflammation. Purpose: To determine whether resveratrol is effective as an anticancer agent. Methods: A systematic review was performed by searching various databases for primary, secondary, and tertiary references. Databases included PubMed, EBSCO, Cochrane, AccessPharmacy, and StatRef by using key terms of “resveratrol,” “cancer,” and “anticancer.” Review search looked at both animal and human studies limited within 10 years. Findings: The major mechanisms of actions through which resveratrol works include proapoptotic, antiproliferation, and anti-inflammation. Numerous in vitro and in vivo studies have supported these mechanisms thus warranting further research in human studies for resveratrol's anticancer effects. Pharmacokinetic human studies suggest good tolerability in healthy subjects, although they have low absorptive characteristics. Conclusion: Resveratrol appears to have anticancer effects. Additionally, these studies indicate that resveratrol's chemoprevention effect is dose and duration dependent. It has synergistic effect with anticancer drugs in vitro. Further human studies need to be done.

Resveratrol in cardiovascular disease: what is known from current research?

Resveratrol is a well-known antioxidant that exists in grape skin/seed, red wine, and the root of Polygonum cuspidatum, a traditional Chinese and Japanese medicinal material. Studies have found that resveratrol has many interesting properties, including anti-carcinogenic properties, anti-microbial and antiviral effects, the ability to reverse dyslipidemia and obesity, the ability to attenuate hyperglycemia and hyperinsulinemia, and the ability to protect endothelial function. Heart failure is the final consequence of the majority of cardiovascular diseases, and resveratrol has been shown to directly attenuate heart contraction. The cardiovascular protective capacities of resveratrol are associated with multiple molecular targets and may lead to the development of novel therapeutic strategies for atherosclerosis, ischemia/reperfusion, metabolic syndrome, and heart failure. This article will mainly review recently published basic researches about the protective cardiovascular effects of resveratrol because these results may lead to the development of new clinical therapeutics in patients.

Apoptotic effect of Polygonum Cuspidatum in oral cancer cells through the regulation of specificity protein 1

The aim of this study was to evaluate the growth inhibitory and apoptosis-inducing effects and mechanisms of Polygonum cuspidatum root in oral cancer cells. The testing materials were separated by normal-phase silica gel liquid chromatography. The effect of P. cuspidatum root on apoptotsis and its mechanism were performed using 3-(4,5-dimethylthiazol-20yl)-(3-carboxymethoxyphenyl)-2-(4-sulphophenyl)-2H-tetrazolium) (MTS) assay, western blot analysis, RT-PCR, promoter assay, and (4'-6-Diamidino-2-phenylindole) (DAPI) staining. The methanol extract of P. cuspidatum (MEPC) inhibited the proliferation of oral cancer cells by inducing caspase-dependent apoptosis. Protein and mRNA expression levels and the transactivation of Specificity protein 1 (Sp1) were markedly decreased in KB cells treated with MEPC. Ethyl acetate fraction (EA) from MEPC was more potent than aqueous fraction (AQ) from MEPC to induce apoptosis. F2, F3, and F4 from EA differentially inhibited the growth of KB cells, and it depends on the amount of Emodin in F2, F3, and F4. Moreover, Emodin inhibited oral cancer cell growth and induced caspase-dependent apoptosis by decreasing Sp1. MEPC also decreased an apoptosis-related downstream target of Sp1 protein, survivin. The results from this study strongly suggest that MEPC, its fraction, and Emodin may be potential bioactive materials to cause apoptosis mechanism via the down-regulation of Sp1 in oral cancer cells.

Key compound groups for the neuroprotective effect of roots of Polygonum cuspidatum on transient middle cerebral artery occlusion in Sprague-Dawley rats

Polygonum cuspidatum is a potent anti-oxidant herb that is well known for its various bioactivities. The current study investigates which compound group is most effective, to establish the key compound groups for quality assessment, especially in terms of neuroprotective effects. The roots of P. cuspidatum were extracted with 85% methanol and fractionated with hexane, ethyl acetate, n-butanol and water. Each fraction was applied to an in vitro radical scavenging assay, a lipid peroxidation assay in brain homogenates and an in vivo assay using a transient focal cerebra ischemia model induced by a middle cerebral artery occlusion in a Sprague-Dawley rat. The ethyl acetate fraction was the most effective fraction in both in vitro and in vivo assays, having the highest stilbene and anthraquinone contents. These results suggest that stilbenes and anthraquinones may be key compound groups for the quality assessment of the anti-oxidative and neuroprotective effects of P. cuspidatum.

Abstract 223: Apoptotic activity of Polygonum cuspidatum in KB human oral cancer cells through the downregulation of specificity protein 1

Abstract Polygonum cuspidatum (Polygonaceae) has traditionally been used in folk medicine to improve oral public health. However, there are no reports related to its potential of controlling oral cancer. In this study, we evaluated the anti-tumorigenic effects and mechanisms of methanol extract and its fractions separated from Polygonum cuspidatum root in KB human oral cancer cells. The methanol extract of Polygonum cuspidatum (MEPC) inhibited the proliferation of KB cells in a dose- and time-dependent manner by inducing caspase-dependent apoptosis. Protein and mRNA expression levels and the transactivation of Specificity protein 1 (Sp1) were markedly decreased in KB cells treated with MEPC. Ethyl acetate fraction (EA) from MEPC was more potent than aqueous fraction (AQ) from MEPC to induce apoptosis. F2, F3 and F4 from EA differentially inhibited the growth of KB cells and it depends on the amount of Emodin in F2, F3 and F4. Moreover, Emodin inhibited KB cell growth and induced caspse-dependent apoptosis. Thus, the results from this study strongly suggest that MEPC, its fraction and Emodin may be potential bioactive materials to cause apoptosis mechanism via the down-regulation of Sp1 in KB human oral cancer cells. This paper was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD, Basic Research Promotion Fund, KRF-2008-331-E00260) and Bio R&D program through the Korea Science and Engineering Foundation funded by the Ministry of Education, Science and Technology (M10870050003-08N7005-00311). Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 223.

Anti-HIV Activities of the Compounds Isolated fromPolygonum cuspidatumandPolygonum multiflorum

The 70 % EtOH extract of Polygonum cuspidatum showed inhibitory action against HIV-1-induced syncytium formation at non-cytotoxic concentrations in vitro with a 50 % effective concentration (EC(50)) of 13.94 +/- 3.41 microg/mL. Through bioactivity-guided fractionation, 20 phenolic compounds, including eight stilbenoids, were isolated from the roots of Polygonum cuspidatum, and their anti-HIV-1 activities were evaluated. Results showed that compounds 1, 13, 14, and 16 demonstrated fairly strong antiviral activity against HIV-1-induced cytopathic effects in C8166 lymphocytes at non-cytotoxic concentrations, with EC (50) values of 4.37 +/- 1.96 microg/mL, 19.97 +/- 5.09, 14.4 +/- 1.34 microg/mL, and 11.29 +/- 6.26 microg/mL and therapeutic index (TI) values of 8.12, > 10.02, > 13.89, and > 17.71, respectively. Other compounds showed either weak or no effects. Compound 6 also showed weak inhibition (153.42 +/- 19.25 microg/mL); however, it possesses very good water solubility and showed almost no cytotoxicity (> 2000 microg/mL), therefore achieving a fairly good TI (13.04). The activities of the two compounds (3 and 18) from Polygonum multiflorum were also assayed. The relationship between molecular structures and their bioactivities was also discussed.

Free radical scavenging activity and antiproliferative potential of Polygonum cuspidatum root extracts

Polygonum cuspidatum is widely used as a medicinal herb in Asia. In this study, ethanol and ethyl acetate extracts of P. cuspidatum root were assayed for their 1,1-diphenyl-2-hydrazyl (DPPH) and hydroxyl free radical scavenging activities, total phenolics content, protective effect against DNA damage, and antiproliferative activity on human lung cancer cells. The ethanol and ethyl acetate (lipophilic phase) extracts of P. cuspidatum had significant scavenging effects on DPPH and hydroxyl radicals. Total phenolics content of ethanol and ethyl acetate (lipophilic phase) extracts of P. cuspidatum were 276.78 +/- 39.31 and 231.73 +/- 5.04 mg/ml, respectively; both extracts protected against hydroxyl radical-induced DNA strand scission. Furthermore, the extracts of P. cuspidatum induced apoptosis and inhibited cell growth in A549 and H1650 cell lines, suggesting that P. cuspidatum root extracts exhibit an antiproliferative effect on human lung cancer cells.

Supercritical CO2 and hydrothermal extraction of phytochemical compounds from Polygonum cuspidatum roots

Supercritical CO2 and hydrothermal extraction of phytochemical compounds from Polygonum cuspidatum roots

Effects of a bio-assay guided fraction from Polygonum cuspidatum root on the viability, acid production and glucosyltranferase of mutans streptococci

Polygonum cuspidatum root has been traditionally used for the treatment of dental diseases in Korea. The purpose of this study was to evaluate effects of P. cuspidatum root on the development of dental caries, especially its effects against bacterial viability and caries-inducing factors of Strptococcus mutans and Strptococcus sobrinus. Among methanol extract of P. cuspidatum root and its fraction tested, ethyl acetate fraction, composed of polydatin, resveratrol, anthraglycoside B, and emodin, showed inhibitory effects on glycolytic acid production and glucosyltransferase activity of S. mutans and S. sobrinus in addition to antibacterial activities.

Tissue distribution and excretion of resveratrol in rat after oral administration of Polygonum cuspidatum extract (PCE)

Polygonum cuspidatum extract as a traditional Chinese medicine is extracted from the dried rhizome and root of Polygonum cuspidatum Sieb.et Zucc. Resveratrol is one of its active components. Studies were performed in rats to define the tissue distribution and excretion of resveratrol in urine and bile, and to characterize (if possible) any metabolites of resveratrol observed in tissues after ig 20mg/kg Polygonum cuspidatum extract. For tissue distribution studies, tissues (300 mg) were homogenized and centrifuged with methanol, and metabolites found in selected tissue extract were identified by LC/MS/MS. For urinary and biliary excretion experiments, urine and bile samples were cleaned up by using solid-phase extraction (SPE) with polyamide cartridges. All the concentrations of resveratrol in these biological samples were determined by HPLC with UV detection. After a single oral dose of 20mg/kg PCE in rats, resveratrol was mainly distributed in stomach, duodenum, liver and kidney with detectable metabolites resveratrol monoglucuronide and resveratrol monosulfate. The majority of the resveratrol was excreted as metabolites, only 0.59% and 0.027% of the dosage were excreted in urine and bile respectively as unchanged drug within 24h.

Anthraquinones from Polygonum cuspidatum as tyrosinase inhibitors for dermal use

Four anthraquinones, physcion (1), emodin (2), citreorosein (3) and anthraglycoside B (6), and two stilbenes, resveratrol (4), and piceid (5), were isolated previously from the root of Polygonum cuspidatum. These bioactive compounds were examined for their antityrosinase potency. No antityrosinase activity was detected with treatment using stilbenes. On the other hand, the anthraquinones showed moderate to strong inhibition of tyrosinase. Physcion exhibited the most potent tyrosinase inhibition among the four anthraquinones examined, which was comparable to kojic acid. The ability of anthraquinones to permeate the skin was also examined. Based on the same thermodynamic activity, physcion showed a higher permeation compared with emodin (48-fold), suggesting it as a potent candidate for dermal use. As naturally occurring tyrosinase inhibitors, anthraquinones from P. cuspidatum may be useful as skin-whitening agents to inhibit tyrosinase for dermal use.

Antibacterial properties of Polygonum cuspidatum roots and their major bioactive constituents

Antibacterial activity, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) of crude extract from Polygonum cuspidatum roots were assayed against five common foodborne bacteria ( Bacillus cereus, Listeria monocytogenes, Staphylococcus aureus, Escherichia coli, and Salmonella anatum). The crude extract exhibited potent antibacterial properties. Major bioactive compounds in P. cuspidatum roots were identified as stilbenes (e.g., piceid, resveratroloside, and resveratrol) and hydroxyanthraquinones (e.g., emodin, emodin-1- O-glucoside, and physcion) by LC–ESI-MS. Both stilbenes and hydroxyanthraquinoines greatly contributed to the antibacterial properties. Additionally, scanning electron microscopy was used to observe morphological changes of the bacteria treated with the crude extract and its major antibacterial components. Possible mechanisms of the antibacterial action were also discussed. This study suggests that the roots of P. cuspidatum and its antibacterial components may have potential for use as natural preservatives.

In vitro effects of a fraction separated from Polygonum cuspidatum root on the viability, in suspension and biofilms, and biofilm formation of mutans streptococci

Polygonum cuspidatum (Polygonaceae) has traditionally been used in folk medicine to control oral diseases. Nevertheless, there are no reports related to its possible effect on the diseases, particularly on biofilm-related diseases such as dental caries. In this study, we evaluated in vitro effects of a fraction separated from Polygonum cuspidatum root on the viability, in both suspension and biofilms, and the biofilm formation of mutans streptococci. The separated fraction (F1) showed bacteriostatic and bactericidal activity against mutans streptococci in suspension, with minimum inhibitory concentration (MIC) range of 31.3–250 μg/ml and minimum bactericidal concentration (MBC) range of 0.5–1 mg/ml. At a concentration of 1.5 mg/ml, F1 killed approximately 2 log 10 CFU/ml of Streptococcus mutans and Streptococcus sobrinus after 2 h of exposure. In biofilms, F1 also inhibited the viability of Streptococcus mutans and Streptococcus sobrinus, dependent on the biofilm age, the concentration of F1, and the treatment time. Four hours of exposure to 1.5 mg/ml F1 reduced the viable counts of Streptococcus mutans and Streptococcus sobrinus by greater than 2 log 10 CFU/disc. Furthermore, at sub-MIC levels, F1 inhibited biofilm formation by Streptococcus mutans and Streptococcus sobrinus in a dose-dependent fashion. Based on the preliminary phytochemical analysis, the activity of F1 may be related to the presence of anthraquinones, cardiac glycosides, terpenoids, and phenolics. These results indicate that F1 is probably useful in the control of oral biofilms and subsequent dental caries development.

Antioxidant activity of extract from Polygonum cuspidatum

Numerous diseases are induced by free radicals via lipid peroxidation, protein peroxidation and DNA damage. It has been known that a variety of plant extracts have antioxidant activities to scavenge free radicals. Whether Polygonum cuspidatum Sieb. et Zuce has antioxidant activity is unknown. In this study, dried roots of Polygonum cuspidatum were extracted by ethanol and the extract was lyophilized. Free radical scavenging assays, superoxide radical scavenging assays, lipid peroxidation assays and hydroxyl radical-induced DNA strand scission assays were employed to study antioxidant activities. The results indicate that the IC50 value oí Polygonum cuspidatum extract is 110 microg/ml in free radical scavenging assays, 3.2 microg/ml in superoxide radical scavenging assays, and 8 microg/ml in lipid peroxidation assays, respectively. Furthermore, Polygonum cuspidatum extract has DNA protective effect in hydroxyl radical-induced DNA strand scission assays. The total phenolics and flavonoid content of extract is 641.1 +/- 42.6 mg/g and 62.3 +/- 6.0 mg/g. The results indicate that Polygonum cuspidatum extract clearly has antioxidant effects.

Estimation of trans-Resveratrol in Herbal Extracts and Dosage Forms by High-Performance Thin-Layer Chromatography

A simple, sensitive and precise high-performance thin-layer chromatographic (HPTLC) method of analysis of trans-resveratrol in Polygonum cuspidatum root extracts and in dosage forms was developed and validated. The separation was carried out on a TLC aluminium plates precoated with silica gel 60F-254 as the stationary phase, eluted with chloroform-ethylacetate-formic acid (2.5 : 1 : 0.1) as mobile phase. Densitometric analysis of trans-resveratrol was carried out in the absorbance mode at 313 nm. This system was found to give compact spot for trans-resveratrol (Rf value of 0.40+/-0.03). A good linear regression relationship between peak areas and the concentrations was obtained over the range of 0.5-3.0 microg/spot with correlation coefficient 0.9989. The limit of detection and quantification was found to be 9 and 27 ng/spot. The method was validated for precision and recovery. The spike recoveries were within 99.85 to 100.70%. The RSD values of the precision in the range 0.37-1.84%. The proposed developed HPTLC method can be applied for identification and quantitative determination of trans-resveratrol in herbal extracts and dosage forms.

Constituents from Polygonum cuspidatum.

AbstractFor Abstract see ChemInform Abstract in Full Text.

Dimeric Stilbene Glycosides fromPolygonum cuspidatum

Two dimeric stilbene glycosides were isolated from an aqueous extract of the root of Polygonum cuspidatum. Their structures were established based on chemical evidence and spectroscopic techniques, including extensive 2D NMR methods. One of these glycosides possesses a novel four-membered ring. Both compounds exhibit strong inhibition of lipid peroxidation, but show no cytotoxic, DNA-cleavage activities and no inhibition of protein tyrosine phosphatase 1B (PTP1B).

Constituents from Polygonum cuspidatum.

Two lignan sulfates, a stilbene derivative and a phenol sulfate, together with 10 known compounds, were isolated from an aqueous extract of the root of Polygonum cuspidatum. The new compounds were elucidated based on chemical evidence and spectroscopic techniques including two-dimensional NMR methods. They exhibited no inhibition of lipid peroxidation and no cytotoxic and DNA cleavage activities.