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Anti-inflammatory, analgesic and diuretic activity of Polygonum lanatum Roxb.

The hexane (PLH), ethyl acetate (PLE) and methanol (PLM) extracts of dried whole plant parts of Polygonum lanatum Roxb. (Family, Polygonaceae) obtained by successive cold extraction, were subjected to evaluate anti-inflammatory, analgesic and diuretic activity in experimental animals. Oral administration of either PLH and PLM at a dose of 300 mg/kg body weight showed statistically significant (p < 0.001) inhibition of rat paw edema by 41.09% and 30.15%, respectively, which was comparable to that of standard drug phenylbutazone (42.15%). Compared to the inhibition of acetic acid-induced writhing by aminopyrine (69.94%, p < 0.001), treatment with either PLH, PLE or PLM elicited significant inhibition of acetic acid-induced writhing reflex by 44.80% (p < 0.001), 33.87% (p < 0.01) and 62.29% (p < 0.001), respectively. In addition, mild to potent diuretic activity was observed after oral administration of these extracts in Swiss albino mice.

Acetates↗

[Effect of polygonum multiflorum thunb on BDNF expression in rat hippocampus induced by amyloid beta-protein (Abeta) 1-40].

OBJECTIVE: To explore the effect of polygonum multiflorum thunb (PMT) on the expression of brain-drived neurtrophic factor (BDNF) in hippocampus CA1 in rats induced by Abeta1-40. METHODS: The rat model was established by injecting Abeta1-40 into the right dorsal hippocampus in rats, and their behavior was observed by Y-maze. The morphological changes of rat hippocampus were examined by the Nissl staining. The expression of BDNF in hippocampus CA1 neurons was also examined by immunohistochemistry and Western blot. RESULTS: After the administration of Abeta1-40, the times of rats learning how to elude electric stimulation were significantly increased, and the expression of BDNF in hippocampus CA1 were obviously reduced. The aggregation of Abeta1-40 in hippocampus and the morphological changes of CA1 hippocampus were found. After the treatment with PMT for 30 days, the times learning how to elude electric stimulation were obviously reduced, while the expression of BDNF in hippocampus CA1 was also increased. CONCLUSION: PMT can reverse the down-regulation of BDNF expression in hippocampus CA1 induced by Abeta1-40.

Amyloid beta-Peptides↗

[Study on purification of 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside from Polygonum multiflori].

OBJECTIVE: To study the conditions and parameters of purifying 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside from Polygonum multiflori. METHOD: Absorption capacity of four resins for 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside was compared. With the adsorption ability as indexes, the process of absorbing and purifying 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside from P. multiflori with S-8 macroporous resin absorbent was selected by orthogonal design. RESULT: The S-8 resin was the best of the four resins. The optimum process condition was 50% ethanol as eluting solvent, the flow rate at 1.5 mL x min(-1), pH at 7-8, and the solution concentration at 0.2 g x mL(-1). The absorption capacity by this process was 36.89 mg x g(-1). CONCLUSION: The process is simple and convenient and the regeneration of resin is easy, so this method of purification is advisable.

Absorption↗

[Effect of prepared Polygonum multiflorum on striatum extracellular acetylcholine and choline in rats of intracerebral perfusion with sodium azide].

OBJECTIVE: To investigate the protection mechanism of prepared Polygonum multiflorum (PPMT) in rat brain with sodium azide (NaN3) perfusion. METHOD: Rats were divided into six groups: control, model, PPMT, Duxil and PPMT + Duxil groups. The intracerebral microdialysis and high performance liquid chromatography-post column Immobilized enzyme reactor-electrochemical detection were used to continuously measure extracellular acetylcholine (ACh) and choline (Ch) levels in striatum of freely moving awake rats. RESULT: The extracellular Ach, Ch levels of striatum stayed stable in the control group during the whole observing period, but the ACh levels in the model group were lower significant than that in the control group. The Ach levels of three drug groups were respectively higher significant than that of model group at some time points. While the extracellular Ch level in striatum of the model group increased singnificantly compared with the control group. The Ch levels of the three drug groups were lower significant than that of the model group respectively at certain time points. The effects of PPMT were similar with that of Duxil. CONCLUSION: The prepared P. multiflorum can improve the impaired cholinergic nerve function to exert the effects of brain protection by elevating extracellular Ach level and improving uptake of extracellular Ch. It may provide the experimental evidence to support the idea that P. multiflorum could be brain protective drug to treat retrogressive disease such as dementia.

Acetylcholine↗

[Medicinal species of genus Polygonum s. lat. distributed in Anhui Province].

OBJECTIVE: To clarify the resource of medicinal plants of genus Polygonum s. lat. distributed in Anhui Province. METHOD: Conducting field investigation and consulting related specimens and data. RESULT AND CONCLUSION: The distribution, growing environment and medicinal use of 32 taxa have been clarified. A scientific basis for further study for these medicinal plants has been provided.

Analgesics, Non-Narcotic↗

Supercritical CO2 extraction of emodin and physcion from Polygonum cuspidatum and subsequent isolation by semipreparative chromatography.

Emodin and physcion are abundant anthraquinone compounds found in the traditional Chinese medicinal herb Polygonum cuspidatum Sied. et Zucc. In this paper, emodin and physcion were successfully extracted with supercritical CO2 plus ethanol modifier after the extraction conditions were optimized with uniform design-sequential optimization. Results showed that the ethanol modifier concentration was the main factor for the effective extraction of the emodin. The optimal extraction condition was obtained: 20 MPa, 30 degrees C, and 95% ethanol, at which the yields of emodin and physcion were 0.616 and 0.178 g/100 g, respectively. The yield obtained by supercritical fluid extraction (SFE) was a little lower than that obtained by sonication extraction (SE). The crude extract obtained by SFE was further isolated and purified by semipreparative chromatography with the mobile phase composed of methanol-water (90:1, v/v). Emodin and physcion were obtained with purity 98.6 and 99.1%, respectively, when determined by HPLC, and identification was performed by retention time and UV spectra of the standards. The result suggested that SFE is an alternative and promising method for extraction of the two compounds from P. cuspidatum owing to its environment-friendly properties and fewer coextracts.

Carbon Dioxide↗

Effects of copper sulfate on black bindweed (Polygonum convolvulus L.).

Seedlings of black bindweed (Polygonum convolvulus L.) were transplanted to soil contaminated with copper sulfate at different dosages. These plants were followed until maturity under greenhouse conditions, and measures of mortality, growth, and reproduction were obtained from harvests 21, 34, and 105 days after the transplant. It was found that application of 125 mg Cu2+ kg-1 resulted in 1.7% lifetime mortality increasing to 100% at 500 mg kg-1. The mortality was dependent on exposure time. No further mortality was observed after 50 days. The population consisted of a relatively tolerant and a sensitive group. This was indicated by differences in lifetime of plants treated with 500 mg kg-1 and by a diversification in biomass of individuals dying from treatment with 315 mg kg-1. The plants surviving treatment had reduced biomass and seed production at dosages above 200 mg kg-1.

Biomass↗

Regulation of cell proliferation, inflammatory cytokine production and calcium mobilization in primary human T lymphocytes by emodin from Polygonum hypoleucum Ohwi.

OBJECTIVE AND DESIGN: This study was designed to elucidate action mechanisms of four anthraquinones identified from Polygonum hypoleucum Ohwi (P. hypoleucum Ohwi) on primary human T lymphocytes. MATERIAL AND METHODS: The cells were isolated from peripheral blood. TREATMENT: T cells were treated with 5 to 60 microM of four anthraquinones with or without phytohemagglutinin (PHA; 5 microg/ml) for 3 days. Effects of 4 anthraquinones on T lymphocyte proliferation, production and gene expression of inflammatory cytokines and intracellular free Ca2+ concentration ([Ca2+]i) were determined. Data were assessed with Student's t-test. RESULTS: On a percentage basis, emodin had the highest suppressing activity on T lymphocyte proliferation with an IC50 of 11.2 +/- 0.6 microM. Emodin decreased cytokine production, IL-2 mRNA expression, and [Ca2+]i in activated T cells. CONCLUSIONS: We hypothesize that the inhibitory mechanisms of emodin on activated T cells proliferation are related to the impairment of cytokine production, IL-2 mRNA level and [Ca2+]i in the cells.

Adult↗

Antibacterial action of tryptanthrin and kaempferol, isolated from the indigo plant (Polygonum tinctorium Lour.), against Helicobacter pylori-infected Mongolian gerbils.

We evaluated the effect of tryptanthrin and kaempferol, both isolated from Polygonum tinctorium Lour., against Helicobacter pylori colony formation in vitro and in H. pylori-infected Mongolian gerbils. H. pylori suspension was mixed with solution of tryptanthrin and/or kaempferol and placed onto agar plates. These plates were incubated at 37 degrees C, under 10% CO2 for 5 days, and the H. pylori colonies were counted. For the in vivo experiment, Mongolian gerbils were inoculated with H. pylori ATCC 43504 orally. After 4 weeks, the infected gerbils were given tryptanthrin and/or kaempferol, administered orally, twice a day for 10 days. The animals were killed and the number of live H. pylori in their stomachs was determined. In vitro both tryptanthrin and kaempferol significantly decreased the numbers of H. pylori colonies a dose-dependent manner. An additive effect on colony formation was observed with the combined use. In the in vivo experiment, oral administration of tryptanthrin and/or kaempferol significantly decreased the numbers of colonies in the gerbils' stomachs. We concluded that tryptanthrin and kaempferol were effective against H. pylori in vivo.

Animals↗

Anti-inflammatory studies on Polygonum glabrum.

Anti-inflammatory studies were conducted on a hot water decoction and on an ethanol extract of the stems of Polygonum glabrum. Effective anti-inflammatory activity was demonstrated against acute carrageenan-induced paw oedema, exudate and granuloma formation in the granuloma pouch test, acute and delayed reactions in formaldehyde arthritis, and acute primary and delayed secondary reactions in adjuvant-induced polyarthritis in albino rats. The acute toxicity in albino mice and 1-month studies on subacute toxicity in rats suggested a good margin of safety. The extract was more effective parenterally than by oral administration.

Animals↗

Ethanol extract of Polygonum cuspidatum inhibits hepatitis B virus in a stable HBV-producing cell line.

Chronic hepatitis B virus (HBV) infection is endemic in Asia and its consequences are among the major public health problems in the world. Unfortunately, the therapeutic efficacies of present strategies are still unsatisfactory with a major concern about viral mutation. In search of effective antiviral agent, we examined the efficacy of extracts of Polygonum cuspidatum Sieb. et Zucc. (P. cuspidatum) against HBV in HepG2 2.2.15 cells by quantitative real time polymerase chain reaction. The expressions of viral antigens, HBeAg and HBsAg, were also determined by enzyme linked immunosorbent assay. The ethanol extract of P. cuspidatum could inhibit dose-dependently the production of HBV (p<0.0001) with an effective minimal dosage of 10 microg/ml. The water extract of P. cuspidatum might also inhibit the production of HBV at a higher dosage. The expression of HBsAg was significantly increased by both ethanol extract and water extract of P. cuspidatum dose-dependently (p<0.0001) and time-dependently (p<0.0001). Higher dose of water extract of P. cuspidatum (30 microg/ml) could inhibit the expression of HBeAg (p<0.05). The extract of P. cuspidatum might contain compounds that would contribute to the control of HBV infection in the future. However, its promoting effect on the expression of HBsAg and its cytotoxicity should be monitored. Further purification of the active compounds, identification and modification of their structures to improve the efficacy and decrease the cytotoxicity are required.

Cell Line↗

In vitro inhibitory effects of Polygonum cuspidatum on bacterial viability and virulence factors of Streptococcus mutans and Streptococcus sobrinus.

OBJECTIVES: Polygonum cuspidatum has been used in Korean folk medicine to improve oral hygiene. This study was performed to evaluate the effects of methanol extract from root of P. cuspidatum (MEP) on bacterial viability and the virulence factors of Streptococcus mutans and Streptococcus sobrinus. METHODS: To test the effects of MEP on bacterial viability, we determined the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) against 20 bacterial strains, including S. mutans and S. sobrinus, using a micro-dilution assay. In case of S. mutans and S. sobrinus, the assays for time-kill and bacterial growth rate at sub-MIC concentrations were also performed. To determine effects of the extract on the virulence factors of S. mutans and S. sobrinus, the assays for sucrose-dependent adherence, water-insoluble glucan formation, glycolytic acid production, and acid tolerance were performed at sub-MIC levels. Phytochemical analysis for constituents of MEP was carried out. RESULTS: MEP showed a broad antibacterial range (MIC 0.5-4 mg/ml). The MBC was two to four times higher than the MIC. The time-kill curves showed S. mutans and S. sobrinus were significantly killed after 1h of incubation. At sub-MIC levels, doubling times of S. mutans and S. sobrinus dose-dependently increased up to 211% and 123%, respectively. At sub-MIC levels, MEP also showed inhibitory effects on the virulence factors of S. mutans and S. sobrinus in a dose-dependent fashion. Phytochemical analysis revealed the presence of alkaloids, sterol/terpenes, tannins, flavonoids, and carbohydrates. CONCLUSION: These data indicate that MEP has inhibitory effects on bacterial viability at higher concentrations (> or =MIC) and the virulence factors of S. mutans and S. sobrinus at sub-MIC concentrations, suggesting that it might be useful for the control of dental plaque formation and subsequent dental caries formation.

Anti-Bacterial Agents↗

Two new bacterial DNA primase inhibitors from the plant Polygonum cuspidatum.

The 70% aqueous methanolic extract of the Peruvian plant Polygonum cuspidatum sp. was found to contain two novel phenolic saccharides 1 and 2, which were identified as inhibitors of the bacterial DNA primase enzyme. Structures of these two compounds were established based on high resolution NMR studies. Compound 1 and 2 inhibited the primase enzyme with an IC(50) of 4 and 5 microM, respectively.

Bacteria↗

Preparative isolation and purification of five compounds from the Chinese medicinal herb Polygonum cuspidatum Sieb. et Zucc by high-speed counter-current chromatography.

High-speed counter-current chromatography (HSCCC) was applied to the separation and purification of five compounds from the Chinese medicinal herb Polygonum cuspidatum Sieb. et Zucc. The crude extracts from P. cuspidatum Sieb. et Zucc were treated with light petroleum-ethyl acetate-methanol-water (2:5:4:6, v/v). Sample 1 was obtained from the lower phase and sample 2 from the upper phase. The sample 1 was separated with light petroleum-ethyl acetate-water (1:5:5, v/v) and yielded 19.3mg of piceid, 17.6 mg of anthraglycoside B from 200mg of sample 1. The sample 2 was separated with light petroleum-ethyl acetate-methanol-water (3:5:4:6, v/v) and light petroleum-ethyl acetate-methanol-water (3:5:7:3, v/v) in a gradient elution and yielded 18.5mg of resveratrol, 35.3mg of emodin and 8.2mg of physcion from 220 mg of sample 2. The purity of each compound is over 95% as determined by HPLC. The chemical structures of these components were identified by (1)H NMR and (13)C NMR.

Anthracenes↗

Inhibitory effects of Polygonum cuspidatum water extract (PCWE) and its component resveratrol [correction of rasveratrol] on acyl-coenzyme A-cholesterol acyltransferase activity for cholesteryl ester synthesis in HepG2 cells.

The pharmacological effects of Polygonum cuspidatum water extract (PCWE) on lipid biosynthesis were investigated in cultured human hepatocyte HepG2 cells. The addition of PCWE (5 and 20 microg/ml), which had no effect on cell proliferation and cellular protein content, caused a marked decrease in the cellular cholesterol content, particularly, the cholesteryl ester content following 24 h of incubation. The incorporation of (14)C-oleate into the cellular cholesteryl ester fraction was also reduced remarkably during incubation for 6 and 24 h. The effect of PCWE on acyl-coenzyme A-cholesterol acyltransferase (ACAT) activity were studied in vitro to explore the mechanism by which PCWE inhibits cholesterol ester formation. The data confirmed that PCWE, in a dose dependent manner, remarkably inhibits ACAT activity. Among the main active chemicals of P. cuspidatum, resveratrol, a kind of flavonoid, decreased ACAT activity in a dose-dependent manner from the level of 10(-3) M. Theses results strongly suggest that PCWE reduces the cholesteryl ester formation in human hepatocytes by inhibiting ACAT.

Animals↗

High-speed counter-current chromatography separation and purification of resveratrol and piceid from Polygonum cuspidatum.

High-speed counter-current chromatography (HSCCC) was applied to the separation and purification of resveratrol and piceid from the dried roots (20.0 g) of Polygonum cuspidatium. The EtOAc extracts were separated with chloroform-methanol-water (4:3:2, v/v). Resveratrol was identified in fraction 5. The water extracts were separated first with EtOAc-EtOH-water (10:1:10, v/v) and then with the same solvent system at the modified volume ratio of 70:1:70. Yields of resveratrol and piceid obtained were 2.18% and 1.07%. Chemical structures of the purified resveratrol and piceid were confirmed by electrospray ionization MS and 1H nuclear magnetic resonance spectroscopy.

Chromatography, High Pressure Liquid↗

Immune reponses in human mesangial cells regulated by emodin from Polygonum hypoleucum Ohwi.

In the hope of identifying agents of therapeutic value in glomerulonephritis from Chinese herbs, we found that methanolic extracts of Polygonum hypoleucum Ohwi (P. hypoleucum Ohwi) inhibit human mesangial cells proliferation activated with interleukin-1beta (IL-1beta) and interleukin-6 (IL-6) previously. This study was designed to identify bioactive components from P. hypoleucum Ohwi and elucidate their action mechanisms. We tested four anthraquinones emodin, emodin 1-O-beta-D-glucoside (49A), physcion (62A), and physcion 1-O-beta-D-glucoside (50A) purified from P. hypoleucum Ohwi for their effects on human mesangial cell proliferation and cytokines production in vitro. On a percentage basis, emodin had the highest suppressing activity on the human mesangial cells proliferation activated by IL-1beta and IL-6. The IC50 of emodin on human mesangial cells proliferation were 17.9+/-1.2 microM. In contrast to 49A, 50A, and 62A, emodin also decreased IL-1beta, IL-6 and tumor necrosis factor-alpha (TNF-alpha) production in human mesangial cells activated with IL-1beta and IL-6. The IC50 of emodin on IL-1beta, IL-6 and TNF-alpha production in activated human mesangial cells were 16.6+/-1.8 microM, 8.2+/-1.3 microM, and 9.5+/-1.6 microM, respectively. Moreover, IL-1beta and TNF-alpha mRNA expression in activated human mesangial cells was impaired by emodin. The intracellular free Ca2+ concentration ([Ca2+]i) in IL-1beta and IL-6 activated human mesangial cells was decreased by emodin. It is unlikely that cytotoxicity was involved because no cell deaths were observable. We hypothesize that the inhibitory mechanisms of emodin on activated human mesangial cells proliferation may be related to the impairments of gene expression and production of cytokines and [Ca2+]i in the cells.

Calcium↗

A tumor cell growth inhibitor from Polygonum hypoleucum Ohwi.

Polygonum hypoleucum Ohwi (P. hypoleucum Ohwi) has been used as a Chinese medicine for a long time. In the present study, four anthraquinones, emodin, emodin 1-O-beta-D-glucoside (49A), physcion (62A), and physcion 1-O-beta-D-glucoside (50A) were identified from P. hypoleucum Ohwi and their inhibitory effects on various tumor cells proliferation were investigated. On a percentage basis, emodin had the highest suppressing activity on the various tumor cells proliferation. At 10 microg/ml, the percentage inhibition on K562 cells proliferation for emodin, 49A, 62A, and 50A were 97+/-3.4%, 18+7.3%, 24+/-3.6%, and 31+/-8.9%, respectively. However, inhibitory activities of 10 microg/ml of emodin, 49A, 62A, or 50A on Raji cells proliferation were 98+/-5.0%, 25+/-5.0%, 22+/-3.2%, and 28+/-4.3%, respectively. It was also found that the both C1 and C3 positions of emodin were important for antitumor action. The IC50s of emodin, 49A, 62A, and 50A on various tumor cells were also calculated. The IC50 of emodin on K562 cells was significantly lower than on Raji, HeLa, Calu-1, Wish, and Vero cells (1.5+/-0.2 vs. 2.8+/-0.4 microg/ml, P < 0.01 ;1.5+/-0.2 vs. 8.4+/-1.6 microg/ml; 1.5+/-0.2 vs. 8.9+/-1.0 microg/ml; 1.5+/-0.2 vs. 8.7+/-0.5 microg/ml; 1.5/-0.2 vs. 3.5+/-0.12 microg/ml; P < 0.001). The results indicated that K562 and Raji cells were more sensitive to emodin treatment. Cell viability test indicated that inhibitory effect of emodin on various tumor cell lines was not through direct cytotoxicity. It suggested P. hypoleucum Ohwi included a tumor cell growth inhibitor.

Anthraquinones↗