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Reduction of atherosclerosis in cholesterol-fed rabbits and decrease of expressions of intracellular adhesion molecule-1 and vascular endothelial growth factor in foam cells by a water-soluble fraction of Polygonum multiflorum.

Polygonum multiflorum stilbeneglycoside (PMS) is a water-soluble fraction of Polygonum multiflorum Thunb., one of the most famous tonic traditional Chinese medicines, that has protective effects on the cardiovascular system. The purpose of the present study is to elucidate the effects of PMS on macrophage-derived foam cell functions and the reduction of severity of atherosclerosis in hypercholesterolemic New Zealand White (NZW) rabbits. NZW rabbits were fed for 12 weeks with a normal diet, a high cholesterol diet, or a high cholesterol diet associated with irrigation with different doses of PMS (25, 50, or 100 mg/kg). Treatment of NZW rabbits fed with high cholesterol diet with 100 mg/kg PMS attenuated the increase in plasma cholesterol, low-density lipoprotein cholesterol, very low-density lipoprotein cholesterol, and plasma triglyceride. Treatment with 50 and 100 mg/kg PMS caused 43% and 60% decrease in atherosclerotic lesioned area ratio to total surface area, respectively. In U937 foam cells, PMS could decrease the high expression of intercellular adhesion molecule (ICAM)-1 protein and the vascular endothelial growth factor (VEGF) protein levels in the medium induced by oxidized lipoprotein when analyzed by flow cytometry. The results proved that PMS is a powerful agent against atherosclerosis and that PMS action could possibly be through the inhibition of the expression of ICAM-1 and VEGF in foam cells.

Animals↗

Myocardial protection against ischaemia-reperfusion injury by a Polygonum multiflorum extract supplemented 'Dang-Gui decoction for enriching blood', a compound formulation, ex vivo.

'Dang-Gui Decoction for Enriching the Blood' (BE), a traditional Chinese formulation comprising Angelica sinensis and Astragalus membranaceus, is used for stimulating red blood cell production as well as enhancing cardiovascular function. In the present study, we have demonstrated the myocardial protection afforded by BE pretreatment against ischaemia-reperfusion (IR) injury in isolated-perfused rat hearts. A more complete and potent myocardial protection against IR injury was also shown by a Polygonum multiflorum extract supplemented BE preparation (BEA). The results suggest that the more potent cardioprotective action of BEA may be related to its ability to sustain the myocardial glutathione antioxidant status under conditions of IR-induced oxidative stress, which may possibly in turn result from the synergistic interaction between the BE and Polygonum extract.

Angelica sinensis↗

Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity.

The methanolic extract from the roots of Polygonum (P.) cuspidatum was found to enhance cell proliferation at 30 or 100 microg/mL in MCF-7, an estrogen-sensitive cell line. By bioassay-guided separation from P. cuspidatum with the most potent activity, emodin and emodin 8-O-beta-D-glucopyranoside were isolated as active principles. The methanolic extracts from Polygonum, Cassia, Aloe, and Rheum species, which were known to contain anthraquinones, also showed the MCF-7 proliferation. As a result of the evaluation of various anthraquinones from plant sources and synthetic anthraquinones, aloe-emodin, chrysophanol, chrysophanol 8-O-beta-D-glucopyranoside, and 1,8-dihydroxyanthraquinone showed weak activity. On the other hand, alizalin and 2,6-dihydroxyanthraquinone as well as emodin having the 2- and/or 6-hydroxyl groups showed potent activity. These results show that the unchelated hydroxyl group is essential for strong activity. Emodin and 2,6-dihydroxyanthraquinone also inhibited 17beta-estradiol binding to human estrogen receptors (ERs) with K(i) values of 0.77 and 0.31microM for ERalpha and 1.5 and 0.69 microM for ERbeta. These findings indicate that hydroxyanthraquinones such as emodin are phytoestrogens with an affinity to human estrogen receptors.

Anthraquinones↗

The digestion of bulbils (Polygonum viviparum L.) and berries (Vaccinium myrtillus L. and Empetrum sp.) by captive ptarmigan (Lagopus mutus).

1. The digestion of three foods favoured by ptarmigan (Lagopus mutus) in the wild was studied using captive birds. 2. Bulbils of Polygonum viviparum L. were a good source of metabolizable energy, protein and phosphorus, but were deficient in sodium. Berries of Vaccinium myrtillus L. were the most digestible of the three foods, contained enough protein and P for maintenance, but were probably deficient in Na. A diet of Empetrum sp. berries caused the birds to be in negative nitrogen and P balance, but provided adequate Na. Both species of berries were rich sources of soluble carbohydrate. 3. In the wild, ptarmigan eat a mixed diet, which presumably provides adequate Na, protein and P. 4. The relative proportions of the various end-products of N metabolism varied according to the protein content of the food. With the diet of Vaccinium berries (11 g N/kg dry matter) roughly equal amounts of ammonium salts and urates were excreted. With Polygonum bulbils (29 g N/kg dry matter) the quantities of ammonium salts and urates excreted were similar to those with Vaccinium berries, but some urea was also excreted and about half the N in the birds' droppings was in an unidentified form. 5. When eating Empetrum berries, ptarmigan digested lignin and tannins and excreted ornithurates. The benzoic acid moiety of the ornithuric acid molecule may have been derived partly from the digested lignin and tannins.

Animal Feed↗

Astragalus membranaceus and Polygonum multiflorum protect rat heart mitochondria against lipid peroxidation.

We isolated rat heart mitochondria and induced lipid peroxidation with ADP and FeSO4. Oxygen consumption and MDA formation were measured for quantitating the amount of lipid peroxidation. Using these methods, we screened the water extracts of 14 Chinese medicinal herbs for their effect on lipid peroxidation. It was found that Astragalus membranaceus inhibited 42.1 +/- 3.4% of oxygen consumption and 39.8 +/- 3.2% of MDA production at concentration of 2 mg dried herb/ml mitochondrial suspension. At the same concentration, Polygonum multiflorum inhibited 52.1 +/- 7.3% of oxygen consumption and 50.9 +/- 5.3% of MDA production. Other herbs did not inhibit lipid peroxidation to 50% of control at concentration up to 6 mg dried herb/ml mitochondrial suspension. Purification and identification of the active component(s) in Astragalus membranaceus and Polygonum multiflorum as well as their clinical application await further studies.

Adenosine Diphosphate↗

[Effect of the root of Polygonum multiflorum Thunb. and its processed products on fat accumulation in the liver of mice].

Experiments have shown that the root of Polygonum multiflorum exhibits inhibitory effect on triglyceride (TG) accumulation in the liver of mice induced by CCl4, cortisone acetate and thioacetamide (TAA). Its processed products (I, II) were found to be effective in lowering the accumulated TG induced by cortisone acetate. The root of Polygonum multiflorum and its processed products also reduced the enlargement of liver by CCl4.

Animals↗

[Effect of crystal No 4 of Polygonum cuspidatum on microcirculatory disturbances during burn shock].

A model of burn shock was reproduced in rat. The effects of crystal No 4 of Polygonum cuspidatum (p. c.) on microcirculation of spinotrapezius muscle in rat with burn shock were observed with a special Hitachi TV set with magnification of 4000x. The changes in water content in tissues of lung and burned skin were measured. The survival time of burned animals was recorded. The aggregation of WBC and the degree of tissue damage in lung were examined in pathologic slides. The results showed that during burn shock the number of adhesive WBC in venules was about 8 times more than normal, the amount of open capillaries was reduced by 3/5 of normal. There were apparent aggregation of WBC and tissue damage in the lung. The number of adhesive WBC was decreased by 80%, the amount of open capillary returned to near normal, and the aggregation of WBC and the degree of tissue damage in the lung were alleviated by administration of crystal No 4 of Polygonum cuspidatum. The survival time in p. c.-treated group was prolonged 1.9-fold of that in n.s.-treated group. The results indicated that the decrease of WBC adherence was caused by, on the one hand, the increase of driving force and wall stress after treatment of p.c., and on the other hand, p. c. might affect some humoral factors which promoted WBC adherence.

Animals↗

[Spectral determination of the contents of mineral elements in polygonum cuspidatum].

The present paper reports the determination of mineral elements by FAAS, including K, Ca, Na, Mg, Fe, Zn, Mn and Cu. The best condition for the determination was investigated. The best ionization inhibitor and acidity media were confirmed. The experiment used CsCl to prevent ionization interference, and the concentration of HCl was controlled below 2%. At the same time SrCl prevented interference of P to Ca. So the value of absorbance was stable. The results were obtained by calibration curve method. The analysis method is simple, rapid, accurate and fitting to the determination of mineral elements in plants. The recoveries of the method are 90.5%-108.2%. The relative standard deviations are 0.3%-0.7%. The result show that large amounts of mineral elements are embodied in polygonum cuspidatum. The contents of K and Ca are in conformation with the medical effects of polygonum cuspidatum, and each element is related closely to its growing.

Calcium↗

[Quantitative determination of the (E) - and (Z) -diastereomers of resveratrol and resveratrol glucoside in the roots of Polygonum cuspidatum by HPLC and elementary study on their fluorescence].

AIM: To establish an optimal HPLC method for the determination of the (E)- and (Z)-diastereomers of resveratrol and resveratrol glucoside from the roots of Polygonum cuspidatum. METHODS: The determination was conducted by using reversed-phase high liquid chromatography. Nucleodur 100-5 C18 column (250 mm x 4.6 mm ID, 5 microm), and a mobile phase program of gradient elution with isopropyl alcohol and water at a flow rate of 0.6 mL x min(-1) was employed. The fluorescence detection wavelengths were: lambda(ex) 334 nm, lambda(em) 404 nm. RESULTS: A good linear relationship was obtained under the optimum condition. The average recoveries were 96.7%, 99.1% for the (E)-diastereomers of resveratrol and resveratrol glucoside, 91.1%, 93.7% for the (Z)-diastereomers of resveratrol and resveratrol glucoside, respectively. The RSD of E-resveratrol and its glucoside were 1.34% and 0.72%, respectively. The RSD of Z-resveratrol and its glucoside were 1.27% and 2.08%, respectively. CONCLUSION: This method is accurate and reliable for the quantity analysis of the (E)- and (Z)-diastereomers of resveratrol and resveratrol glucoside in the roots of Polygonum cuspidatum.

Chromatography, High Pressure Liquid↗

Analgesic, antiinflammatory and CNS depressant activities of sesquiterpenes and a flavonoid glycoside from Polygonum viscosum.

Analgesic, antiinflammatory and CNS depressant activities of four sesquiterpenes, viscosumic acid, viscozulenic acid, viscoazucine and viscoazulone, and a flavonoid glycoside, quercetin-3-O-(6''-feruloyl)-beta-D-galactopyranoside isolated form the aerial parts of Polygonum viscosum (Polygonaceae) have been assessed. All test compounds exhibited CNS depressant activity in open field test, all but viscoazulone showed analgesic activity in Eddy's hot plate test, all sesquiterpenes inhibited acetic acid induced abdominal writhing in mice, and all but viscoazucine and the flavonoid glycoside exhibited mild to moderate antiinflammatory effect on carrageenan induced rat paw edema.

Acetic Acid↗

A new stilbene glucoside from the roots of Polygonum multiflorum Thunb.

One new stilbene glucoside (6), along with five known compounds (1-5), were isolated from the roots of Polygonum multiflorum Thumb., and their chemical structures established based on physicochemical and spectroscopic data. Of the compounds, compound 3 showed DNA topoisomerase I and II inhibitory activities.

Antineoplastic Agents, Phytogenic↗

The radical scavenging effects of stilbene glucosides from Polygonum multiflorum.

The extract of the root of Polygonum multiflorum exhibited a significant antioxidant activity assessed by the DPPH radical scavenging activity in vitro. The bioassay-guided fractionation of the extract yielded a stilbene glucoside, (E)-2,3,5,4'-tetrahydroxystilbene-2-O-beta-d-glucopyranoside (1) as an active constituent responsible for the antioxidant property. Compound 1 demonstrated a moderate DPPH radical scavenging activity (IC50, 40 microM), while the corresponding deglucosylated stilbene 2 exhibited a much higher activity (IC50, 0.38 microM).

Free Radical Scavengers↗

Highly potent anti-HIV-1 activity isolated from fermented Polygonum tinctorium Aiton.

A water-soluble extract of fermented Polygonum tinctorium Aiton (Polygonaceae) called Sukumo, exhibited a potent inhibitory activity against HIV type 1 in vitro. The extract potently suppressed acute HIV-1 (IIIB) infection in MT-4 cells with EC50 values of 0.5 microg/ml but exhibited low cytotoxicity to MT-4 cells even at a high concentration (CC50 > 1000 microg/ml). It also inhibited giant cell formation in co-cultures of HIV-infected cells and uninfected Molt-4 cells. Sukumo extract was found to interact with both the viral envelope glycoprotein and cellular receptors, thus blocking virus-cell binding and virus-induced syncytium formation. There was a good correlation between the extract's anti-HIV-1 activity and its inhibitory effects on HIV-1 binding. It also suppressed replication of herpes simplex virus type 1 in Vero cells with an EC 50 of 11.56 microg/ml. On the other hand, there was no appreciable activity against influenza A virus, poliovirus or SARS corona virus when tested at concentrations ranging from 3.2-400 microg/ml as shown by microscopic image analysis for cytopathic effect (CPE). Physico-chemical studies revealed that the anti-HIV activity in the extract was essentially maintained after boiling at 100 degrees C in 1N HCl or 1N NaOH, and after treatment with 100 mM NaIO4. The inhibitory activity of the extract was also not reduced after pronase digestion. The active factor in the extract is likely to be a novel compound(s) having a polyanionic substructure and a molecular weight of 10,000-50,000.

Anti-HIV Agents↗

Preparative isolation and purification of chemical constituents from the root of Polygonum multiflorum by high-speed counter-current chromatography.

High-speed counter-current chromatography methods, combined with solvent partition, were applied to the systematic separation and purification of chemical components from Chinese medicinal herb Polygonum multiflorum extract. The aim of this paper is summing up the rules of solvent system selection for diverse fractions of herbal extract, and establishing the systematic pattern to screen the bioactive constituents rapidly. Nine compounds including emodin, chrysophanol, rhein, 6-OH-emodin, emodin-8-beta-D-glucoside, polygonimitin B, 2,3,5,4'-tetrahydroxystilbene-2-beta-D-glucoside, gallic acid and an unknown glycoside, which differed in quantity and polarity remarkably, were obtained. The purities of them were all above 97% as determined by high-performance liquid chromatography (HPLC), and their structures were identified by 1H NMR and electrospray ionization mass spectrometry (ESI-MS). The results demonstrated that HSCCC is a speedy and efficient technique for systematic isolation of bioactive components from traditional medicinal herbs.

Anthraquinones↗

The estrogenic effects of Polygonum hydropiper root extract induce follicular recruitment and endometrial hyperplasia in female albino rats.

INTRODUCTION: The powdered dry root of Polygonum hydropiper is widely used by a certain ethnic group of women in Assam, India, for the prevention of undesired pregnancy. METHOD: In the present investigation, the estrogenic property of the crude root extract (CRE) of P. hydropiper [compared to estradiol-17beta (E(2)), the reference drug] was tested in ovary-intact and ovariectomized (OVX) rats. The study was carried out by histological observations of ovarian follicles in an ovary-intact model and by histological observations of the endometrial epithelium in both OVX and ovary-intact female albino rats. Serial sections of the ovary and of the uterus were stained with routine hematoxylin-eosin and were observed under a microscope. RESULTS: In the ovary-intact model, CRE induced follicular recruitment, while it promoted follicular atresia at a later stage. Many of the graafian follicles in the treated ovary showed pyknosis of the nuclei of granulosa and theca cells, as well as disparity in granulosa cell organization. In the uterine tissues of both ovary-intact and OVX rats, CRE induced hyperplasia in places of luminal epithelium and degeneration of endometrial glands. In OVX rats, the effect of CRE on uterine endometrium was corroborative with the effect of E(2). CONCLUSIONS: Oral administration of the CRE of P. hydropiper significantly altered the histological structures of both ovary-intact and OVX rats.

Animals↗

beta-Glucosidase inhibitory activities of phenylpropanoid glycosides, vanicoside A and B from Polygonum sachalinense rhizome.

The phenylpropanoid glycosides, vanicoside A and B, isolated from rhizomes of giant knotweed (Polygonum sachalinense) showed beta-glucosidase inhibitory activity, with IC(50) values of 59.8 and 48.3 mug/ml (59.9 and 50.5 muM), respectively. In contrast, p-coumaric acid and ferulic acid, corresponding to phenylpropanoyl moieties of vanicosides, exhibited very little inhibition.

Cinnamates↗

Antioxidant phenolic compounds from rhizomes of Polygonum paleaceum.

Polygonum paleaceum Wall. ex Hook. f. is a small herb in Polygonaceae family. In southwest of China, the rhizomes of this plant were used as folk drug for the treatment of chronic gastritis, duodenal ulcers, dysentery, wound, pain, hemorrhage and irregular menstruation. The crude aqueous acetone extract exhibited high antioxidant activity (SC(50) = 16.72 micro/ml) in 1,1-diphenyl-2-picryldydrazyl (DPPH) radical-scavenging assay. With bioactivity-guided fractionations, 14 antioxidant phenolic compounds 1-14 were obtained from the air-dried rhizomes of this plant. Of them, compound 1, a new phenol named paleaceolactoside, was determined to be 3,5-dihydroxyl hexanoic acid 1,5-lactone 3-(6'-o-galloyl)-o-beta-D-glucopyranoside by detailed spectroscopic analysis. The radical-scavenging activity of all the isolated compounds was also described.

Antioxidants↗