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ABSTRACT: AIM OF THE STUDY: Ginseng (Panax ginseng C. A. Meyer) has been used for diabetes treatment in China for thousands of years. Malonyl ginsenosides (MGR) are natural ginsenosides which exist in both fresh and air-dried ginseng. The objective of this study is to determine the antidiabetic function of MGR on type 2 diabetes. MATERIALS AND METHODS: High fat diet-fed and streptozotocin-induced diabetic rats were treated with 50 and 100mg/kg/d of MGR or vehicle for 3 weeks. The effects of MGR on fasting blood glucose (FBG), intraperitoneal glucose tolerance test (IPGTT), serum insulin (SI), insulin tolerance test (ITT), body weight, total cholesterol (TC), and triglyceride (TG) levels in type 2 diabetic rats were measured. RESULTS: After 3 weeks of treatment, MGR administration showed significantly lower FBG levels compared to the diabetic control group. In glucose tolerance test, IPGTT data showed that both MGR 50 and 100mg/kg groups significantly increased the glucose disposal after glucose load. The ITT also showed improvement of insulin sensitivity during 120min of insulin treatment. In addition, MGR reduced TG and TC contents while showed no effect on body weight in diabetic rats. Histopathologic examination demonstrated that the MGR has protective effects on β-cells in diabetic rats proved by the increase of SI. CONCLUSION: The findings from this study suggest that MGR can alleviate hyperglycemia, hyperlipemia and insulin resistance of type 2 diabetes.
Journal of ethnopharmacology 11/2012; · 2.32 Impact Factor
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ABSTRACT: As one of the main active component of protopanaxdiol type ginsenosides, ginsenoside Rb(3) is rarely reported in the treatment of diabetes. The anti-diabetic activity of ginsenoside Rb(3) was investigated in a model of alloxan-induced diabetic mice in the present study. The physiological parameter such as fasting blood glucose level, oral glucose tolerance, body weight, food intake and water intake were measured. Glucose consumption in C2C12 myotubes was also determined in order to investigate the molecular mechanism of ginsenoside Rb(3) in anti-diabetes. The alloxan-induced diabetic mice were treated with ginsenoside Rb(3) for 2 weeks at doses of 5 mg/kg, 15 mg/kg and 25 mg/kg. After 2 weeks treatment of ginsenoside Rb(3), the fasting blood glucose levels of DG 15 and DG 25 were respectively reduced by 36.70% and 37.50% compared to control group. At a dose of 25 mg/kg, oral glucose tolerance was significantly improved compared to control group (P < 0.05). The AUC decreased by 34.47% (from 2442 ± 291 mmol·min/L to 1600 ± 109 mmol·min/L). Both food intake and water intake were remarkably lowered. The injury of pancreas tissues was repaired, which was observed by using HE staining and optic microscope. In vitro, at concentrations of 100 and 200 µM, ginsenoside Rb(3) increased glucose consumption in C2C12 myotubes by 76.83% and 97.20%, respectively, as compared to the control group. However, the body weight of diabetic mice was not significantly altered. In conclusion, our results showed that ginsenoside Rb(3) reduced fasting blood glucose level, food intake, water intake, improved oral glucose tolerance, and repaired injured pancreas tissues of alloxan-induced diabetic mice. Therefore, it was suggested that ginsenoside possesses the potential of the clinical use in preventing and treating diabetes.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 06/2012; 8(5):934-41. · 1.64 Impact Factor
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ABSTRACT: In the present work, we reported the enzymatic preparation of deapio-platycodin D (dPD) and platycodin D (PD) optimized by response surface methodology (RSM) from Radix Platycodi. During investigation of the hydrolysis of crude platycosides by various glycoside hydrolases, snailase showed a strong ability to transform deapio-platycoside E (dPE) and platycoside E (PE) into dPD and PD with 100% conversion. RSM was used to optimize the effects of the reaction temperature (35-45 °C), enzyme load (5-20%), and reaction time (4-24 h) on the conversion process. Validation of the RSM model was verified by the good agreement between the experimental and the predicted values of dPD and PD conversion yield. The optimum preparation conditions were as follows: temperature, 43 °C; enzyme load, 15%; reaction time, 22 h. The biotransformation pathways were dPE→dPD3→dPD and PE→PD3→PD, respectively. The determined method may be highly applicable for the enzymatic preparation of dPD and PD for medicinal purposes and also for commercial use.
International Journal of Molecular Sciences 01/2012; 13(4):4089-100. · 2.60 Impact Factor
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ABSTRACT: Ginsenoside Rh(2), one of the most important ginsenosides with anticancer properties in red ginseng, has been developed as principal antitumor ingredient for clinical use. However, the cytotoxicity test in human hepatocyte cell line QSG-7701 (IC(50) 37.3μM) indicated that Rh(2) might show strong cytotoxic side-effect on the normal liver cells. For blunting the toxicity, Rh(2) was structurally modified by reacting with octanoyl chloride to give a dioctanoyl ester of Rh(2) (D-Rh(2)) in the present study. MTT assay in QSG-7701 cell line in vitro showed that the cytotoxicity of D-Rh(2) on human hepatocyte cells (IC(50) 80.5μM) was significantly lower than that of Rh(2). While antitumor xenograft assay in mice bearing H22 liver cancer cells in vivo showed that the antitumor activity of D-Rh(2) retained to be strong as that of Rh(2). According to previous pharmacokinetic studies, the fatty acid esterification of Rh(2) might be of detoxification reaction to cells. Additionally, D-Rh(2) showed significant enhancement on increasing thymus index at the dose of 10mg/kg compared with vehicle treated control group. Thus, D-Rh(2) might indirectly affect tumor growth by stimulating lymphocytes to become cytotoxic to tumor cells. Finally, our findings suggested that D-Rh(2), the fatty acid ester of Rh(2), might attenuate the side-effect by detoxification to human normal cell and could be a more potential candidate for developing as an antitumor drug.
Bioorganic & medicinal chemistry letters 12/2011; 22(2):1082-5. · 2.65 Impact Factor
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ABSTRACT: Compound K (CK) is a final intestinal metabolite of protopanaxadiol-type ginsenosides (PDG) from Panax ginseng. Although anti-diabetic activity of CK have been reported with genetic mouse models (db/db mice) in recent years, the therapeutic usefulness of CK and PDG in type 2 diabetes, a more prevalent form of diabetes, remains unclear. In the present investigation, we developed a mouse of non-insulin-dependent diabetes mellitus that closely simulated the metabolic abnormalities of the human disease. For this purpose, type 2 diabetes was induced in male ICR mice by combining of streptozotocin. The male ICR mice fed with HFD for 4 weeks received 100mg/kg of STZ injected intraperitoneally. After 4 weeks, mice with fasting (12h) blood glucose levels (FBG) above 7.8 mmol/L were divided into 3 groups (n=12) and treated with vehicle (diabetes model, DM), 300 mg/kg/day of PDG and 30 mg/kg/day of CK for 4 weeks while continuing on the high-fat diet. Hypoglycemic effects of CK and PDG were consistently demonstrated by FBG levels, and insulin-sensitizing effects were seen during oral glucose tolerance testing (OGTT). Moreover, the mechanism of hypoglycemic effect in type 2 diabetic mice was examined. Gluconeogenic genes, Phosphoenolpyruvate carboxykinase (PEPCK) and Glucose-6-phosphatase (G6Pase), were decreased in two treatment groups with CK showing greater effects. These findings demonstrated the hypoglycemic and insulin-sensitizing capabilities of CK on type 2 diabetes induced by HFD/STZ via down-regulation of PEPCK and G6Pase expression in liver.
Fitoterapia 10/2011; 83(1):192-8. · 1.85 Impact Factor
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ABSTRACT: Radix Saposhnikoviae is one of the most famous Chinese herbal medicines with many pharmacological activities towards inflammatory symptoms and antioxidation. Chromones are considered as one of the effective components. It is important to find a reasonable method to extract the chromones in S. divaricata.
To develop an ultrasonic-assisted extraction (UAE) to extract chromones in Radix Saposhnikoviae and to optimise extraction conditions.
Four chromones (prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside and sec-O-glucosylhamaudol) were extracted by the UAE method combined with response surface methodology (RSM). Box-Behnken design (BBD) was applied to evaluate the effects of three independent variables (ethanol concentration, extraction time and extraction temperature) on the chromones yield of Radix Saposhnikoviae.
Correlation analysis of the mathematical-regression model indicated that a quadratic polynomial model could be employed to optimise the extraction of chromones by UAE method. The optimal conditions to obtain the highest chromones yield of Radix Saposhnikoviae were a solvent of 75% ethanol, an extraction time of 48 min and an extraction temperature of 67°C.
Under these optimal conditions, the experimental values agreed closely with the predicted values. The analysis of variance indicated a high goodness of model fit and the success of RSM method for optimising chromones extraction in Radix Saposhnikoviae.
Phytochemical Analysis 03/2011; 22(4):313-21. · 2.63 Impact Factor
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ABSTRACT: To investigate the protective effects of protopanaxadiol-type ginsenoside (PDG) and its metabolite ginsenoside M1 (G-M1) on carbon tetrachloride (CCl(4))-induced chronic liver injury in ICR mice, we carried out conversion of protopanaxadiol-type ginsenosides to ginsenoside M1 using snailase. The optimum time for the conversion was 24 h at a constant pH of 4.5 and an optimum temperature of 50 °C. The transformation products were identified by high-performance liquid chromatography and electrospray ion-mass spectrometry. Subsequently, most of PDG was decomposed and converted into G-M1 by 24 h post-reaction. During the study on hepatoprotective in a mice model of chronic liver injury, PDG or G-M1 supplement significantly ameliorated the CCl(4)-induced liver lesions, lowered the serum levels of select hepatic enzyme markers (alanine aminotransferase, ALT, and aspartate aminotransferase, AST) and malondialdehyde and increased the activity of superoxide dismutase in liver. Histopathology of the liver tissues showed that PDG and G-M1 attenuated the hepatocellular necrosis and led to reduction of inflammatory cell infiltration. Therefore, the results of this study show that PDG and G-M1 can be proposed to protect the liver against CCl(4)-induced oxidative injury in mice, and the hepatoprotective effect might be attributed to amelioration of oxidative stress.
Molecules 01/2011; 16(12):10093-103. · 2.39 Impact Factor
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ABSTRACT: In the present study, we developed a liquid chromatography-diode array detector-electrospray ionization/mass spectrometric (LC-DAD-ESI/MS) method for analysis of saikosaponins in Bupleurum falcatum. The LC method employed a ZORBAX SB-Aq analytical column (150 x 4.6 mm i.d., 5 μm) at a flow rate of 0.8 mL/min coupled with a diode array detector at 204 nm. A step gradient of acetonitrile-water (v/v) containing 0.5% formic acid from 30 to 70% was applied, leading to a sample analysis time of 30 min. The ESI-MS was carried out in positive and negative modes from 500 to 1,500 m/z. Saikosaponins c, a, and d gave strong sodium adducts at m/z 949.6, 803.5 and 803.6, respectively, in positive mode. The data indicate that the present LC-DAD-ESI/MS assay is an effective method for the determination of saikosaponins c, a and d from the roots of Bupleurum falcatum.
Molecules 01/2011; 16(2):1533-43. · 2.39 Impact Factor
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ABSTRACT: A new saponin, malonylginsenoside Ra3, was isolated from the fresh root of Panax ginseng, along with four known ginsenosides. The new compound was identified as (20S)-protopanaxadiol-3-O-(6-O-malonyl-beta-D-glucopyranosyl(1-->2)-beta-D-glucopyranoside-20-O-beta-D-xylopyranosyl(1-->3)-beta-D-glucopyranosyl(1-->6)-beta-D-glucopyranoside on the basis of extensive 1D and 2D NMR as well as HRESI-MS spectroscopic data analysis.
Molecules 04/2010; 15(4):2319-25. · 2.39 Impact Factor
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ABSTRACT: Glucose uptake assay-guided fractionations of the methanol extract of Schisandra chinensis led to the isolation of the dibenzocyclooctadiene lignans: gomisin J (1), gomisin N (2), wuweizisu B (3), wuweizisu C (4), gomisin C (5), gomisin D (6), (+)-schisandrin A (7), schisandrin C (8), schisandrol A (9), gomisin H (10), angeloylgomisin H (11), gomisin A (12), and schizandrin (13). Among these, 1, 2, 7, and 8 significantly improved basal glucose uptake in HepG2 cells. Their improving effects were concentration-dependent. Compound 2 exhibited a stronger effect than that of rosiglitazone, which has been used as an anti-diabetic drug. The results suggest that these lignans may partially contribute to the anti-diabetic activity of Fructus Schisandrae Chinensis in traditional use by stimulating the glucose uptake into peripheral tissue, which may be responsible for reducing the level of blood glucose in circulation. Thus, these findings show the potential of these lignans for development as hypoglycemic drugs.
Natural product communications 02/2010; 5(2):231-4. · 1.24 Impact Factor
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ABSTRACT: A new oleanane-type triterpenoid saponin, named platycoside N (1), together with six known saponins, was isolated from the roots of Platycodon grandiflorum. On the basis of acid hydrolysis, comprehensive spectroscopic data analyses and comparison with the spectral data of the known compounds, its structure was elucidated as 3-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl-2β,3β,16α,23-tetrahydroxyolean-12-en-28-oic acid 28-O-β-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside. The six known compounds were platycodin D (2), deapioplatycodin D (3), platycodin D3 (4), deapioplatycodin D3 (5), platycoside E (6) and deapioplatycoside E (7).
Molecules 01/2010; 15(12):8702-8. · 2.39 Impact Factor
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ABSTRACT: Protopanaxatriol saponins obtained with AB-8 macroporous resin mainly consisted of ginsenosides Rg(1) and Re. A novel mono-ester of ginsenoside-Rh(1) (ginsenoside-ORh(1)) was synthesized through further enzymatic hydrolysis and octanoyl chloride modifications. A 53% yield was obtained by a facile synthetic method. The structures were identified on the basis of 1D-NMR and 2D-NMR, as well as ESI-TOF-MS mass spectroscopic analyses. The isolated and synthetic compounds were applied in an anti-tumor bioassay, in which ginsenoside ORh(1) showed moderate effects on Murine H22 Hepatoma Cells.
Molecules 01/2010; 15(1):399-406. · 2.39 Impact Factor
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ABSTRACT: An Aspergillus niger strain was isolated from the soil around ginseng fruit. In vitro enzyme assays showed that this strain had the ability to transform total ginsenosides (TGS) into several new products. In a further biochemical study, a beta-glucosidase gene isolated from this strain, bgl1, was expressed in Saccharomyces cerevisiae. His-tagged BGL1 protein (approximately 170 kD) showed the ability to transform ginsenoside Rf into Rh(1).
Molecules 02/2009; 14(6):2043-8. · 2.39 Impact Factor
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ABSTRACT: A new anthraquinone, Rubiacordone A (1) (6-acetoxy-1-hydroxy-2-methylanthraquinone-3-O-alpha-L-rhamnopyranoside), was isolated together with the known anthraquinone, 1-acetoxy-6-hydroxy-2-methylanthraquinone-3-O-[alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside] (2), from the dried roots of Rubia cordifolia. Their structures were elucidated on the basis of extensive 1D and 2D-NMR, as well as HRESI-MS spectroscopic analysis. Metabolites 1 and 2 showed considerable antimicrobial activity against Gram-positive bacteria.
Molecules 01/2009; 14(1):566-72. · 2.39 Impact Factor
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Jiang-Ning Hu,
Xue-Mei Zhu,
Ki-Teak Lee, Yi-Nan Zheng,
Wei Li,
Li-Kun Han,
Zhe-Ming Fang,
Li-Juan Gu,
Bai-Sheng Sun,
Chun-Yan Wang,
Chang-Keun Sung
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ABSTRACT: To optimize ginsenosides hydrolyzing beta-glucosidase production from Aspergillus niger, response surface methodology was carried out in two stages. The Plackett-Burman design was achieved to screen the important variables that influence beta-glucosidase production. Among 10 variables (wheat bran, soybean powder, CaCl(2), ginsenosides, KH(2)PO(4), MgSO(4), polyethylene glycol (PEG), medium volume, inoculum size, and stirring speed), it was found that wheat bran, KH(2)PO(4), and stirring speed had significant effect on beta-glucosidase activity due to very low p-values (p<0.05). Subsequently, wheat bran, KH(2)PO(4), and stirring speed were further optimized using central composite design. The optimal beta-glucosidase production was predicted to be 4650.14 U/ml with the combination of factors (wheat bran, 34.51 g/l; KH(2)PO(4), 1.78 g/l; stirring speed, 161.60 rpm/min). Finally, under optimal fermentation conditions, ginsenoside Rb(1) was converted to Rd and F(2) by A. niger within 10 min. Little compound K was detected at 30 min, and finally F(2) was completely transformed to compound K within 8 h. The putative conversion pathway of Rb(1) by A. niger was Rb(1), Rd, F(2), and compound K.
Biological & Pharmaceutical Bulletin 11/2008; 31(10):1870-4. · 1.66 Impact Factor
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ABSTRACT: We reported that ginger prevented obesity in mice fed a high-fat diet in previous study. In this experiment, we examined the effects of zingerone, the major pungent component of ginger on fat storage in ovariectomized (Ovx) rats. Oral administration of 170 mg/kg zingerone significantly reduced body weight and the final parametrail adipose tissue weight in ovariectomized rats. Blood glucose levels after oral administration of glucose were lower in zingerone-treated Ovx-rats than in the Ovx-rats (control). Basal lipolysis in zingerone-treated Ovx-rats was increased compared with that in the Ovx-rats. Zingerone significantly increased norepinephrine-induced lipolysis associated with the translocation of hormone-sensitive lipase (HSL) from the cytosol to lipid droplets in adipocytes. These results indicate that zingerone may prevent the fat storage through increasing norepinephrine-induced lipolysis in adipocytes.
Yakugaku zasshi journal of the Pharmaceutical Society of Japan 09/2008; 128(8):1195-201. · 0.39 Impact Factor
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ABSTRACT: To investigate the anti-obesity effects of escins extracted from the seeds of Aesculus turbinata BLUME, anti-obesity models in vitro and in vivo were employed. In a preliminary experiment, different solvent fractions of Aesculus turbinata BlUME as well as two isolated compounds were tested for their effects on pancreatic lipase (PL) in vitro. Subsequently, female ICR mice were fed a high fat diet with or without different concentrations of total escins for 11 weeks to examine body weight, parametrial adipose tissue weight, and hepatic triacylglycerol (TG) and total cholesterol (TC) contents. Plasma triacylglycerol levels (TG) after oral administration of lipid emulsions to rats were also investigated. The results showed that total escins (1 mg/ml) as well as two compounds isolated from total escins, namely escin Ib and IIa, showed inhibitory effects on PL activity. In vivo, total escins suppressed the increase in body weight, parametrial adipose tissue weight, TG content, and TC content in mice's liver; TG content in rat plasma was also reduced at 1, 2 and 3 h after oral administration of the lipid emulsion plus different concentrations of escins compared to those in the lipid emulsion groups. Meanwhile, mice fed a high fat diet plus 2% total escins for 3 d had an increased TG level in the feces compared to the HF group. The reason for this may be due to a delay in the intestinal absorption of dietary fat by inhibiting PL activity.
CHEMICAL & PHARMACEUTICAL BULLETIN 02/2008; 56(1):12-6. · 1.59 Impact Factor
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ABSTRACT: A bioassay-guided in vitro screen has revealed that a 70% methanol extract of the leaves of Salix matsudana shows considerable inhibitory activity against cyclooxygenases (COX-1 and COX-2). A subsequent phytochemical study led to the isolation of a new flavonoid, matsudone A (1), together with five known flavonoids--luteolin (2), isoquercitrin (3), 7-methoxyflavone (4), luteolin 7-O-glucoside (5), 4',7-dihydroxyflavone (6)--and two phenolic glycosides, leonuriside A (7) and piceoside (8). Their structures were elucidated on the basis of extensive 1D- and 2D-NMR studies, high resolution ESI mass spectroscopic analyses and comparisons with literature data. The isolated compounds 1-8 were tested for their inhibitory activities against COX-1 and COX-2. Compounds 1, 5 and 6 were found to have potent inhibitory effect on COX-2 and compounds 3-5 exhibited moderate inhibition against COX-1.
Molecules 02/2008; 13(8):1530-7. · 2.39 Impact Factor
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ABSTRACT: To investigate chemical constituents of Portulaca oleracea.
The constituents were isolated by various column chromatography methods, and their structures were elucidated by spectral analysis.
Five compounds were isolated from 70% ethanol extract and their structures were elucidated as oleracein A(1), oleracein B(2), oleracein E(3), hesperidin (4) and caffeic acid (5).
Compound 4 and 5 are isolated from Portulaca oleracea for the first time.
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials 11/2007; 30(10):1248-50.
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ABSTRACT: Four known ginsenosides: ginsenoside-Rb1 (1), Rb3 (2), Rd (3) and Re (4) were isolated from the methanolic extract of the traditional Chinese medicine Panax ginseng C. A. Meyer. Further enzyme reactions and chemical modifications led us to obtain ginsenoside-M1 (5) and synthesize three novel mono-esters of ginsenoside-M1, ginsenoside-DM1 (6), PM1 (7) and SM1 (8) 30 - 50% of yield via a facile and green synthetic strategy. The structures were elucidated on the basis of extensive 1D- and 2DNMR, as well as high resolution ESI-TOF mass spectroscopic analyses. The isolated and synthetic compounds were tested in an anti-tumor bioassay, and compounds 5-8 showed considerable cytotoxicity (SRB) against several human cancer cell lines (breast cancer MCF-7, skin melanoma SK-MEL-2 and human ovarian carcinoma B16), but moderate effects on lung carcinoma COR-L23. The other ginsenosides showed no effects.
Molecules 02/2007; 12(9):2140-50. · 2.39 Impact Factor
