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1.

Ethnopharmacological relevance

Niranthin is a lignan isolated from Phyllanthus niruri L. This plant has long been used in folk medicine for liver protection and antihepatitis B in many Asian countries. This study was designed to evaluate the anti-hepatitis B virus activity of niranthin using HepG2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models.

Materials and methods

Niranthin was isolated from Phyllanthus niruri L. (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hepatitis B virus activity was evaluated both in vitro and in vivo. The human HBV-transfected liver cell line HepG2.2.15 was used in vitro assay. And the in vivo anti-hepatitis B virus activity was evaluated on the expression of HBV replication, HBsAg, HBeAg, ALT and AST on day 0, 7, 14, 17 after niranthin was dosed intragastricly (i.g.) once a day for 14 days at the dosages of 25, 50 and 100 mg/kg/day in the duck hepatitis B virus (DHBV) infected ducks.

Results

In the human HBV-transfected liver cell line HepG2.2.15, the secretion of HBsAg and HBeAg were significantly decreased after treatment with niranthin for 144 h, with IC50 values for HBsAg of 15.6 µM, IC50 values for HBeAg of 25.1 µM. In DHBV-infected ducklings, niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of niranthin.

Conclusion

The experimental data demonstrated that niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo.  相似文献   

2.

Ethnopharmacological relevance

The aim of this study was to determine the anti-hepatitis B effect of isochlorogenic acid A isolated from Laggera alata (Asteraceae), a traditional Chinese herbal medicine.

Materials and methods

The anti-hepatitis B activity of isochlorogenic acid A was evaluated by the d-galactosamine (D-GalN)-induced HL-7702 hepatocyte damage model and the HBV-transfected HepG2.2.15 cells.

Results

Isochlorogenic acid A significantly improved HL-7702 hepatocyte viability and markedly inhibited the productions of HBsAg and HBeAg. The inhibitory rates of isochlorogenic acid A on the HBsAg and HBeAg expressions were 86.9% and 72.9%, respectively. In addition, isochlorogenic acid A declined markedly the content of hepatitis B virus covalently closed circular DNA (HBV cccDNA) and induced significantly the heme oxygenase-1 (HO-1) expression in HepG2.2.15 cells.

Conclusions

Isochlorogenic acid A was verified to possess the potent anti-hepatitis B activity. The anti-HBV target of isochlorogenic acid A is probably associated with blocking the translation step of the HBV replication. Overexpression of HO-1 may contribute to the anti-HBV activity of isochlorogenic acid A by reducing the stability of the HBV core protein and thus blocking the refill of nuclear HBV cccDNA. Additionally, the hepatoprotective effect of isochlorogenic acid A could be achieved by its antioxidative property and induction of HO-1.  相似文献   

3.

Aim

50% ethanolic extract (ASE) of Amaranthus spinosus (whole plant) was evaluated for in vitro antioxidant and hepatoprotective activity.

Methods

The total phenolics and reducing capacity of ASE was determined using standard curve of gallic acid (0–1.0 mg/ml) and butylated hydroxy anisole. In vitro antioxidant activity was determined by DPPH, superoxide, hydroxyl radicals, hydrogen peroxide and nitric oxide scavenging methods. The hepatoprotective activity of ASE was evaluated at 6, 7, 8, 9 and 10 μg/ml concentration against CCl4 (1%) induced toxicity in freshly isolated rat hepatocytes and HepG2 cells.

Results

ASE was found to contain 336 ± 14.3 mg/g total polyphenolics expressed as gallic acid equivalent while the reducing capacity was 2.26 times of BHA. ASE showed significant antioxidant activity in DPPH assay (IC50 29 μg/ml), scavenges superoxide (IC50 ∼ 66–70 μg/ml), hydrogen peroxide (IC50 ∼120–125 μg/ml), hydroxyl radicals (IC50 ∼140–145 μg/ml) and nitric oxide (IC50 ∼ 135–140 μg/ml). ASE (6, 7, 8, 9 and 10 μg/ml) was able to normalise the levels of biochemical parameters in isolated rat hepatocytes intoxicated with CCl4. A dose dependent increase in percentage viability was observed in CCl4 intoxicated HepG2 cells.

Conclusions

ASE possesses significant hepatoprotective activity which might be due to antioxidant defence factors and phenolics might be the main constituents responsible for activity.  相似文献   

4.
5.
Objective To evaluate the effect of 8-epi-kingiside (8-Epik) derived from the buds of Jasminum officinale var. grandiflorum (JOG) on hepatitis B virus (HBV) replication in HepG2 2.2.15 cell line in vitro and duck hepatitis B virus (DHBV) replication in ducklings in vivo. Methods The concentration of extracellular hepatitis B e antigen and hepatitis B surface antigen (HBsAg) in cell culture medium was determined by ELISA, respectively. The anti-HBV effects of 8-Epik were also demonstrated in the model of DHBV. 8-Epik was ip given (20, 40, and 80 mg/kg, twice daily) to the DHBV-infected ducklings for 10 d. The isotonic saline liquid diet was ip given as negative control and Lamivudine (50 mg/kg, twice daily) was given as positive control. DHBV DNA was measured at days 0 (T0), 5 (T5), 10 (T10), and day 3 after cessation of treatment (P3) by dot blotting. Results 8-Epik effectively blocked HBsAg secretion in HepG2 2.2.15 cells in a dose-dependent manner [IC 50 = (19.4 ± 1.04) μg/mL]. 8-Epik (40 or 80 mg/kg, ip, twice daily) also reduced viremia in DHBV-infected ducks. Conclusion Therefore, 8-Epik is warranted as a potential therapeutic agent for HBV infection.  相似文献   

6.

Aim of the study

Traditional Chinese herb Angong Niuhuang Pill (AGNHP) is a famous preparation for neurological diseases; Qingkailing injection (QKL), an extract of AGNHP has similar clinical applications. This investigation was designed to further elucidate the neuroprotective effect of QKL on intracerebral hemorrhage (ICH).

Materials and methods

ICH was produced in adult Sprague–Dawley rats by injection of collagenase IV. Three incremental doses of QKL injection including low-(0.5 ml/kg), moderate-(1 ml/kg) and high-dosage (2 ml/kg) were administered twice, 3 and 12 h following ICH. TUNEL and caspase-3 activity were measured at 1 d after ICH, and apomorphine-induced rotation was evaluated at 1 d, 7 d, 14 d and 28 d.

Results

Administration of high-dose QKL inhibited TUNEL positive cells (p < 0.05) and caspase-3 activity (p < 0.05) at 1 d following ICH, and reduced apomorphine-induced rotation at 1 d (p < 0.01), 7 d, 14 d and 28 d (p < 0.05), compared with the controls. However, QKL in a low or moderate dose had no such effect.

Conclusion

QKL reduced brain damage of intracerebral hemorrhage through inhibiting apoptosis, which suggested a potential intervention for ICH patients.  相似文献   

7.

Aim of study

Oxidative stress is involved in stroke. In particular, Chinese Herbal Medicine with antioxidant properties is believed to have potential therapeutic effect. In this study, neuroprotective effects of purified Herba Leonuri (pHL) were evaluated in Wistar rats undergone middle cerebral artery occlusion (MCAO).

Materials and methods

The rats were treated with their respective treatments for 2 weeks prior to the MCAO, continually treated for another 7 days after MCAO. During the post-surgery treatment period, neurological deficit score was measured. At the end of treatment, animals were sacrificed and samples were collected for analysis of infarct volume, apoptosis and antioxidant analysis.

Results

Under the treatment of pHL, the infarct volume was reduced significantly from 20.75 ± 0.03% to 15.19 ± 0.02% (p < 0.05). The neurological impairment was alleviated to 1.82 as compared to vehicle (2.43). Plasma antioxidant concentration was increased from 0.31 ± 0.03 mM to 0.42 ± 0.05 mM (p < 0.05). DNA oxidative damage was reduced to 1.19 ± 0.03 in stroke pHL treated group (p < 0.05 as compared to vehicle group, 1.78 ± 0.03). pHL could reduce the level of apoptosis and also the pro-apoptotic proteins, but increase the level of anti-apoptotic proteins.

Conclusion

pHL is believed to have promising therapeutic effect for stroke treatment through antioxidant mechanisms.  相似文献   

8.

Ethnopharmacological relevance

Plectranthus amboinicus (Lour.) Spreng is a medicinal specie often used in Brazil, especially in Northeast Region, for the treatment of several diseases including inflammations and cancer.

Aim of the study

To evaluate the anti-inflammatory and antitumor activities of the hydroalcoholic extract from leaves of P. amboinicus in an attempt to determine whether the medicinal uses are supported by pharmacological effects.

Materials and methods

Anti-inflammatory activity was determined by carrageenan-induced paw edema method. The antitumor effect was evaluated in an in vivo experimental study, using the following tumors: Sarcoma-180 and Erlich ascite carcinoma.

Results

There were statistically significant decreases (p < .05) of edema paw in at the doses of 150, 250 and 350 mg/kg (i.p.) of the hydroalcoholic extract of P. amboinicus. Similarly, the administration of P. amboinicus at the doses of 100, 150, 250 and 350 mg/kg (i.p.) inhibited the growth of sarcoma-180 and Ehrlich ascite carcinoma tumors in mice.

Conclusion

The results suggest that the hydroalcoholic extract of P. amboinicus possesses anti-inflammatory and antitumor activities, supporting the folk use of this medicinal specie.  相似文献   

9.

Aim of the study

Sun-dried rind of the immature fruit of Punica granatum L. (Punicaceae) (Pg) is presently used as a herbal formulation (OMARIA) in Orissa, India, for the therapy and prophylaxis of malaria. The aims of this study were (i) to assess in vitro the antiplasmodial activity of the methanolic extract, of a tannin enriched fraction and of compounds/metabolites of the antimalarial plant, (ii) to estimate the curative efficacy of the Pg extracts and (iii) to explore the mechanism of action of the antiplasmodial compounds. Urolithins, the ellagitannin metabolites, were also investigated for antiplasmodial activity.

Materials and methods

Chloroquine-susceptible (D10) and -resistant (W2) strains of Pf were used for in vitro studies and the rodent malaria model Plasmodium berghei—BALB/c mice was used for in vivo assessments. Recombinant plasmepsins 2 and 4 were used to investigate the interference of Pg compounds with the metabolism of haemoglobin by malaria parasites.

Results

The Pg methanolic extract (Pg-MeOH) inhibited parasite growth in vitro with a IC50 of 4.5 and 2.8 μg/ml, for D10 and W2 strain, respectively. The activity was found to be associated to the fraction enriched with tannins (Pg-FET, IC50 2.9 and 1.5 μg/ml) in which punicalagins (29.1%), punicalins, ellagic acid (13.4%) and its glycoside could be identified. Plasmepsin 2 was inhibited by Pg-MeOH extract and by Pg-FET (IC50 7.3 and 3.0 μg/ml), which could partly explain the antiparasitic effect. On the contrary, urolithins were inactive. Both Pg-MeOH extract and Pg-FET did not show any in vivo efficacy in the murine model.

Conclusions

The in vitro studies support the use of Pg as antimalarial remedy. Possible explanations for the negative in vivo results are discussed.  相似文献   

10.

Aim of the study

To investigate the immunosuppressive effects of HPLC qualitied ethyl acetate extract (EAE) from Urtica dentate Hand on skin allograft rejection in a murine model.

Materials and methods

Allo-skin transplantation model was established by placing skin allograft of C57BL/6 mice in the wound bed which was on the back of Balb/c mice. We used FACS to study the effects of EAE on dendritic cells (DCs) maturation and CD4+CD25+T regulatory cells (Tregs) differentiation. We also studied spleen lymphocyte proliferation and T-bet gene expression in DCs. Concentration of Th1/Th2 cytokines was monitored as markers of Th1/Th2 responses by ELISA.

Results

A significant prolongation of skin allografts survival was observed as a dose-dependent manner in the animals treated with EAE. By FACS, we found that treatment with EAE (200 mg kg−1) resulted in an immature statement of DCs and stimulated the differentiation of CD4+CD25+Tregs. Additionally, the expression of T-bet gene and the proliferation of spleen lymphocytes were efficiently abated in EAE treated mice. Comparing to the model control, EAE-treated recipients showed a significant down-regulation (P < 0.01) of Th1 cytokines (IL-2, IFN-γ) and an obviously increase (P < 0.01) of Th2 cytokine (IL-10) in the serum, which presented in a dose-related way.

Conclusions

The anti-allograft rejection effect of EAE by enhancing CD4+CD25+Tregs differentiation and sustaining DCs immaturation makes EAE to be a possible choice for treating autoimmune diseases in a way of inducing a stable immunological tolerance state.  相似文献   

11.
12.

Aim of the study

The root of Scutellaria baicalensis Georgi (Labiatae), also known as Scutellariae Radix, possesses anticancer, antiviral, and anti-inflammatory properties. And it is one of the most widespread herbal remedies used in Oriental medicine. In the present study, we investigated the effects of Scutellariae Radix water extract (SR) on proinflammatory mediators secreted from lipopolysaccharide (LPS)-induced RAW 264.7 macrophages.

Material and methods

Cell viability was assessed by MTT assay and nitric oxide (NO) concentration in the cultured medium was determined by the Griess reaction. Various Cytokines released from LPS-induced Raw 264.7 cells were measured in the cell culture supernatants using a multiplex bead array assay based on xMAP technology.

Results

We found that SR significantly inhibited the production of NO, interleukin (IL)-3, IL-6, IL-10, IL-12p40, IL-17, interferon-inducible protein (IP)-10, keratinocyte-derived chemokine (KC), and vascular endothelial growth factor (VEGF) in LPS-induced RAW 264.7 cells at the concentrations of 25, 50, 100, 200 μg/ml (p < 0.05).

Conclusions

These results suggest that SR has anti-inflammatory activity related with its inhibition of NO, cytokine, chemokine, and growth factor production in macrophages.  相似文献   

13.

Ethnopharmacological relevance

Solanum torvum (Solanaceae) is a plant used in Cameroon ethnomedicine for the treatment of hypertension.

Aim of the study

The present study was aimed to determine the effect of ethanolic extract of Solanum torvum (100 and 300 mg/kg; p.o. for 6 weeks) on systolic blood pressure (SBP), vascular reactivity, serum glucose, triglycerides, cholesterol, insulin and uric acid in fructose-induced hypertension.

Materials and methods

The effect of ethanolic extract of Solanum torvum (100 and 300 mg/kg; p.o. for 6 weeks) on fructose (10%) induced rise in blood pressure was tested by invasive and non-invasive measurements and the biochemical parameters were studied by using standard kits.

Results

Ethanolic extract of Solanum torvum reduced systolic blood pressure, vascular reactivity changes to catecholamines and reversed the metabolic alterations induced by fructose. The cumulative concentration response curve (CCRC) of Angiotensin II (Ang II) using isolated strip of ascending colon was shifted towards right in rats treated with ethanolic extract of Solanum torvum.

Conclusions

In conclusion, ethanolic extract of Solanum torvum could prevent the development of high blood pressure induced by a diet rich in fructose probably by reversing the metabolic alterations induced by fructose.  相似文献   

14.

Aim of the study

Gynostemma pentaphyllum is a popular folk medicine that has been used for treatment of hepatitis in Asia. Our previous study demonstrates that Gynostemma pentaphyllum n-butanol extract inhibits the onset and improves the recovery of CCl4-induced liver fibrogenesis in rats and inhibits PDGF-induced rat hepatic stellate cells (HSCs) proliferation. In this study, the effect of Gynostemma pentaphyllum extract on cytokines and type I procollagen expression was analyzed.

Materials and methods

Rat HSCs were treated with PDGF, Gynostemma pentaphyllum n-butanol extract, RP-18-Gyp fraction, rapamycin or vehicle. Rat cytokine antibody array chip or ELISA kit was used for cytokines detection. Intracellular protein expression was detected by Western blotting, mRNA expression was analyzed by RT-PCR.

Results

RP-18-Gyp fraction is the more purified gypenosides fraction from Gynostemma pentaphyllum n-butanol extract. In cell proliferation, the inhibitory effect of 200 μg/ml RP-18-Gyp fraction is similar to 500 μg/ml Gynostemma pentaphyllum n-butanol extract. Furthermore, both of them have the ability of decreasing monocyte chemoattractant protein-1 (MCP-1) mRNA expression and protein release and inhibiting type I procollagen protein expression.

Conclusions

Both of Gynostemma pentaphyllum n-butanol extract and its more purified RP-18-Gyp fraction have the biological activities in the inhibition of cell proliferation, MCP-1 release and type I procollagen expression in rat HSCs. These data could provide the evidence to support for the traditional use of Gynostemma pentaphyllum in hepatitis.  相似文献   

15.

Ethnopharmacological relevance

Resistance to current antibacterial drugs and the rise of opportunistic fungal infections are growing global concerns. Traditional medicine is a potential source of new antibacterials and antifungals. Citrullus colocynthis Schrad. (Cucurbitaceae) endemic in Southern Tunisia, is used in folk medicine against dermatological, gynaecological and pulmonary infections.

Aim of study

To assess in vitro antibacterial and anticandidal activity of aqueous and diluted acetone extracts of Citrullus colocynthis Schrad. MIC and MBC/MFC were determined for plant organs at different maturation stages.

Materials and methods

Citrullus colocynthis Schrad. was harvested and its identification was verified. Aqueous and diluted acetone extracts (from the plant's roots, stems, leaves and three maturation stages of its fruit and seeds) were screened for activity against Gram-negative and Gram-positive bacteria (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalis)—and various Candida spp. (Candida glabrata, Candida albicans, Candida parapsilosis and Candida kreusei).

Results

All extracts showed activity against all strains. The highest MICs and MBCs/MFCs were obtained from the fruit aqueous extracts (MIC 0.10 mg/ml against Candida albicans and Candida glabrata, 0.20 mg/ml against Escherichia coli and Pseudomonas aeruginosa), lowest activity from the root extracts.

Conclusions

Citrullus colocynthis Schrad. shows antibacterial and anticandidal properties. The folk medicinal use as a broad-spectrum antimicrobial agent is validated.  相似文献   

16.

Aim of the study

Polyporus umbellatus is a fungus used as a diuretic medicine. The objective of this study was to isolate and elucidate the diuretic constituents of n-hexane, ethyl acetate, n-butanol and water extracts of Polyporus umbellatus and to evaluate their diuretic activity.

Materials and methods

The n-hexane, ethyl acetate, n-butanol and water extracts of Polyporus umbellatus were tested by diuretic experiment of normal rats in metabolic cage. The n-hexane extract and n-butanol extract were prepared separately by the bioassay-guided approach. Three isolated compounds doses (5, 10 and 20 mg/kg BW) were orally administered to normal rats. Water excretion rate, pH and content of Na+, K+ and Cl were measured in the urine of saline-loaded rats.

Results

n-Hexane extract (P < 0.05), n-butanol extract (P < 0.05) and three isolated compounds (ergosta-4,6,8(14),22-tetraen-3-one, ergosterol and d-mannitol) displayed diuretic activity.

Conclusions

The ergosta-4,6,8(14),22-tetraen-3-one was the strongest diuretic constituent in the three compounds. Ergosterol and d-mannitol were found to be also responsible for duiretic effects in Polyporus umbellatus for the first time. Data show that 20 mg/kg dose of the ergosterol for urine out put became significantly higher than in the control rats, but the ratio of Na+/K+ almost unaltered in the three doses. The highest dose of the d-mannitol was significant and increased the cumulative urine output. Regarding the electrolyte excretion, data show that the doses 10 and 20 mg/kg produce significant increase for excretion of Na+ and Cl. The present results provide a quantitative basis explaining application of Polyporus umbellatus as a diuretic medicine. The result proved that its diuretic effects were also due to the contribution of multi-components in clinical application.  相似文献   

17.

Aim of the study

Momordica charantia Linn. Cucurbitaceae (MC), has been used to treat glycemic impairment in humans for centuries. The objective of this study was to determine the acute effect of MC on postprandial glucose levels, energy expenditure/fuel mixture and appetite in overweight men.

Materials and Methods

Five healthy overweight men were supplemented on three randomized conditions where (1) no MC (placebo), (2) 50 mg/kg body weight (MC50) or (3) 100 mg/kg body weight of freeze dried MC were administered orally prior to a 75 g oral glucose tolerance test (OGTT). Plasma glucose and insulin levels were measured before and during the OGTT. Energy expenditure as well as carbohydrate and lipid oxidation rates were measured by indirect calorimetry. Visual analogue scales were used to rate appetite profile.

Results

Plasma glucose and insulin levels significantly increased during the OGTT (p ≤ 0.05) but no significant difference was observed between experimental conditions. Energy expenditure, carbohydrate and lipid oxidation rates as well as appetite profile did not differ between experimental conditions.

Conclusions

These results suggest that from an acute standpoint, a freeze dried MC extraction in its present dose form does not affect plasma glucose/insulin levels, energy expenditure, substrate mixture and appetite scores following an oral glucose load in non-diabetic overweight men.  相似文献   

18.

Ethnopharmacological relevance

Laggera alata, as a traditional Chinese herbal medicine, has been widely used to ameliorate some ailments associated with inflammation including hepatitis in folk.

Aim of the study

Based on anti-inflammatory activity of total phenolics from Laggera alata (TPLA), to further validate the remarkable curative effect Laggera alata in hepatitis, hepatoprotective effect of TPLA was examined.

Materials and methods

TPLA was prepared and its principle components were quantificationally analyzed. The hepatoprotective effects of TPLA were studied using a CCl4-induced injury model in primary cultured neonatal rat hepatocytes, and a CCl4-induced acute and chronic damage model in vivo.

Results

TPLA significantly reduced cellular leakage of hepatocyte aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and improved cell viability in vitro. TPLA markedly decreased the serum AST and ALT levels of the mice, the levels of AST, ALT, total protein, albumin, and sialic acid in rat serum, and the hydroxyproline level in rat liver. Meanwhile, severe hepatic lesions induced by CCl4 in mice/rats were remarkably improved by the administration of TPLA.

Conclusions

This investigation verifies the hepatoprotective effect of TPLA in vitro/in vivo and clarifies its active components dicaffeoylquinic acids responsible for hepatoprotective potential.  相似文献   

19.
20.

Aim of the study

Albizia lebbeck Benth. is used both in Indian traditional system and folk medicine to treat several inflammatory pathologies such as asthma, arthritis and burns. The aim of the present study was to evaluate the scientific basis of anti-inflammatory activity of different organic solvent extracts of Albizia lebbeck.

Materials and methods

The anti-inflammatory activity of Albizia lebbeck was studied using the carrageenan, dextran, cotton pellet and Freund's complete adjuvant induced rat models. The extracts obtained using petroleum ether, chloroform and ethanol were administered at the concentrations of 100, 200 and 400 mg/kg body weight.

Results

The petroleum ether and ethanol extracts at 400 mg/kg, showed maximum inhibition of inflammation induced by carrageenan (petroleum ether—48.6%; ethanol—59.57%), dextran (petroleum ether—45.99%; ethanol—52.93%), cotton pellet (petroleum ether—34.46%; ethanol—53.57%) and Freund's adjuvant (petroleum ether—64.97%; ethanol—68.57%).

Conclusion

The marked inhibitory effect on paw edema shows that Albizia lebbeck possesses remarkable anti-inflammatory activity, supporting the folkloric usage of the plant to treat various inflammatory diseases.  相似文献   

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