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1.
Antioxidants (Basel) ; 8(8)2019 Jul 28.
Article in English | MEDLINE | ID: mdl-31357705

ABSTRACT

(1) Background: Graptopetalum paraguayense E. Walther is a traditional Chinese herbal medicine. In our previous study, 50% ethanolic G. paraguayense extracts (GE50) demonstrated good antioxidant activity. (2) Methods: To investigate the hepatoprotective effects of GE50 on ethanol and carbon tetrachloride (CCl4) co-induced hepatic damage in rats, Sprague-Dawley rats were randomly divided into five groups (Control group; GE50 group, 0.25 g/100 g BW; EC group: Ethanol + CCl4, 1.25 mL 50% ethanol and 0.1 mL 20% CCl4/100 g BW; EC + GE50 group: Ethanol + CCl4 + GE50; EC + silymarin group: ethanol + CCl4 + silymarin, 20 mg/100 g BW) for six consecutive weeks. (3) Results: Compared with the control group, EC group significantly elevated the serum aspartate aminotransferase (AST), alanine aminitransferase (ALT), and lactate dehydrogenase (LDH). However, GE50 or silymarin treatment effectively reversed these changes. GE50 had a significant protective effect against ethanol + CCl4 induced lipid peroxidation and increased the levels of glutathione (GSH), vitamin C, E, total antioxidant status (TAS), and the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT), and glutathione S-transferases (GST). Furthermore, in EC focal group, slight fat droplet infiltration was observed in the livers, while in the GE50 or silymarin treatment groups, decreased fat droplet infiltration. HPLC phytochemical profile of GE50 revealed the presence of gallic acid, flavone, genistin, daidzin, and quercetin. (4) Conclusions: The hepatoprotective activity of GE50 is proposed to occur through the synergic effects of its chemical component, namely, gallic acid, flavone, genistin, daidzin, and quercetin. Hence, G. paraguayense can be used as a complementary and alternative therapy in the prevention of alcohol + CCl4-induced liver injury.

2.
Int J Mol Sci ; 20(10)2019 May 27.
Article in English | MEDLINE | ID: mdl-31137784

ABSTRACT

BACKGROUND AND AIMS: Liver fibrosis is the excessive accumulation of extracellular matrix proteins, including collagen, which occurs in most types of chronic liver diseases. Advanced liver fibrosis results in cirrhosis, liver failure, and portal hypertension. Activated hepatic perivascular stellate cells, portal fibroblasts, and myofibroblasts of bone marrow origin have been identified as major collagen-producing cells in the injured liver. These cells are activated by fibrogenic cytokines, such as TGF-ß1. The inhibition of TGF-ß1 function or synthesis is a major target for the development of antifibrotic therapies. Our previous study showed that the water and ethanol extracts of Graptopetalum paraguayense (GP), a Chinese herbal medicine, can prevent dimethylnitrosamine (DMN)-induced hepatic inflammation and fibrosis in rats. METHODS: We used rat hepatic stellate HSC-T6 cells and a diethylnitrosamine (DEN)-induced rat liver injury model to test the potential mechanism of GP extracts and its fraction, HH-F3. RESULTS: We demonstrated that GP extracts and HH-F3 downregulated the expression levels of extracellular matrix (ECM) proteins and inhibited the proliferation and migration via suppression of the TGF-ß1 pathway in rat hepatic stellate HSC-T6 cells. Moreover, the HH-F3 fraction decreased hepatic collagen content and reduced plasma AST, ALT, and γ-GT activities in a DEN-induced rat liver injury model, suggesting that GP/HH-F3 has hepatoprotective effects against DEN-induced liver fibrosis. CONCLUSION: These findings indicate that GP/HH-F3 may be a potential therapeutic agent for the treatment of liver fibrosis. The inhibition of TGF-ß-mediated fibrogenesis may be a central mechanism by which GP/HH-F3 protects the liver from injury.


Subject(s)
Crassulaceae/chemistry , Liver Cirrhosis/drug therapy , Plant Extracts/therapeutic use , Transforming Growth Factor beta/metabolism , Animals , Cell Line , Collagen/genetics , Collagen/metabolism , Extracellular Matrix Proteins/genetics , Extracellular Matrix Proteins/metabolism , Hepatic Stellate Cells/drug effects , Hepatic Stellate Cells/metabolism , Humans , Liver Cirrhosis/metabolism , Plant Extracts/pharmacology , Rats , Rats, Wistar , Signal Transduction , Transforming Growth Factor beta/genetics
3.
J Sci Food Agric ; 96(5): 1772-6, 2016 Mar 30.
Article in English | MEDLINE | ID: mdl-26036956

ABSTRACT

BACKGROUND: Many studies have demonstrated that Graptopetalum paraguayense has good antioxidant ability; however, few studies have examined its anti-inflammatory effect. The study aimed to investigate the anti-inflammatory effects of water extracts of G. paraguayense (WGP, 4 g day(-1)) in subjects with metabolic syndrome (MS). Intervention was administered for 12 weeks. Levels of inflammatory markers [high sensitivity C-reactive protein (CRP), tumour necrosis factor-α (TNF-α), and interleukin-6 (IL-6)] and antioxidant enzymes activities were measured. RESULTS: Forty-two subjects completed the 12 week intervention study (placebo, n = 19; WGP, n = 23). After 12 weeks supplementation, subjects in WGP group had significantly lower levels of inflammatory markers than the baseline (P < 0.05) and the placebo group (CRP, P = 0.07; TNF-α, P = 0.04; IL-6, P = 0.03). The changes in levels of the inflammatory markers were significantly decreased in WGP group (CRP, P = 0.04; TNF-α, P = 0.06; IL-6, P = 0.01) compared to the placebo group. Levels of inflammatory markers were significantly negatively correlated with the antioxidant enzymes activities after supplementation. CONCLUSION: This study demonstrated a significant reduction in inflammatory status in MS after WGP supplementation. WGP may exert an anti-inflammatory effect on MS in addition to its antioxidant ability.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Crassulaceae/chemistry , Dietary Supplements , Metabolic Syndrome/drug therapy , Plant Extracts/pharmacology , Aged , Anti-Inflammatory Agents/chemistry , Antioxidants/metabolism , Biomarkers , Female , Humans , Male , Middle Aged , Plant Extracts/chemistry
4.
Bot Stud ; 56(1): 8, 2015 Dec.
Article in English | MEDLINE | ID: mdl-28510817

ABSTRACT

BACKGROUND: Graptopetalum paraguayense E. Walther is a popular traditional Chinese herb and possesses several health benefits. In earlier studies, we demonstrated that G. paraguayense showed no genotoxicity and showed several biological activities. However, the constituents of G. paraguayense have not been studied yet. In this present study, we isolated and identified the constituents of the leaves of G. paraguayense E. Walther. RESULTS: A total of seven flavonoid compounds were isolated from the methanolic extract of G. paraguayense. The four major compounds isolated were flavonoid glucoside derivatives of quercetin (1, 3) and kampferol (2, 4), each presenting a 3-hydroxyl-3-methylglutaroyl (HMG) substituent; compounds 3 and 4-the 2´´-acetyl derivatives of 1 and 2, respectively-are novel compounds isolated from nature for the first time. High-performance liquid chromatography for the quantitative analyses of the four major HMG-substituted flavonoid glycosides in G. paraguayense E. Walther were accomplished to acquire the high yields of 1-4 in the methanolic extract (4.8, 5.7, 4.3, and 2.5 mg/g, respectively). Furthermore, the antioxidant activities, including radical-scavenging, reducing power and lipid peroxidation inhibitory effects of these isolated flavonoids were also evaluated. All seven of the isolated flavonoid compounds possessed antioxdative activity. CONCLUSIONS: In this study of the constituents of the leaves of G. paraguayense E. Walther, we isolated four major components from its methanolic extract and determined their structures to be (acetylated) HMG-substituted flavonol glycosides, which are rare in nature. All seven of the isolated compounds possessed antioxdative activity, and those flavonoid compounds may be responsible for the functional ingredients in G. paraguayense. Further investigation of their bioactivities or pharmacological activities will be continued.

5.
Food Chem Toxicol ; 62: 492-8, 2013 Dec.
Article in English | MEDLINE | ID: mdl-24036142

ABSTRACT

Hyperglycemia is associated with advanced glycation end products (AGEs). Recently, AGEs were found to cause pancreatic damage, oxidative stress, and hyperglycemia through the AGE receptor. Carboxymethyllysine (CML) is an AGE but whether it induces pancreatic dysfunction remains unclear. Graptopetalum paraguayense, a vegetable consumed in Taiwan, has been used in folk medicine and is an antioxidant that protects against liver damage. We investigated the protective properties of G. paraguayense 95% ethanol extracts (GPEs) against CML-induced pancreatic damage. The results indicated that resveratrol, GPE, and gallic acid (the active compound of GPE) increased insulin synthesis via upregulation of pancreatic peroxisome proliferator activated-receptor-γ (PPARγ) and pancreatic-duodenal homeobox-1 (PDX-1) but inhibited the expression of CML-mediated CCAAT/enhancer binding protein-ß (C/EBPß), a negative regulator of insulin production. Moreover, resveratrol and GPE also strongly activated nuclear factor-erythroid 2-related factor 2 (Nrf2) to attenuate oxidative stress and improve insulin sensitivity in the liver and muscle of CML-injected C57BL/6 mice and resulted in reduced blood glucose levels. Taken together, these findings suggested that GPE and gallic acid could potentially be used as a food supplement to protect against pancreatic damage and the development of diabetes.


Subject(s)
Crassulaceae/chemistry , Hyperglycemia/drug therapy , Lysine/analogs & derivatives , Pancreas/drug effects , Plant Extracts/pharmacology , Stilbenes/pharmacology , Animals , Gallic Acid/analysis , Gallic Acid/pharmacology , Homeodomain Proteins/metabolism , Hyperglycemia/chemically induced , Hyperglycemia/physiopathology , Insulin/blood , Liver/drug effects , Liver/metabolism , Lysine/toxicity , Mice , Mice, Inbred C57BL , NF-E2-Related Factor 2/metabolism , Oxidative Stress/drug effects , PPAR gamma/metabolism , Pancreas/physiopathology , Resveratrol , Taiwan , Trans-Activators/metabolism
6.
Food Chem ; 129(3): 804-9, 2011 Dec 01.
Article in English | MEDLINE | ID: mdl-25212302

ABSTRACT

Accumulation of bioactive compounds, during developmental stages of Graptopetalum paraguayense E. Walther, was investigated between 30 and 90days as a function of physiological maturity. Three distinct phases were defined: immature phase (30days), intermediate developmental phase (30-60days), and maturation phase (60-90days). Gallic acid and quercetin, antioxidative bioactive compounds, were identified as biomarkers for determining the optimum physiological maturity stage in G. paraguayense E. Walther. With regard to the antioxidant activity of G. paraguayense E. Walther at different developmental stages, the results indicated that the leaves of immature G. paraguayense E. Walther had the highest 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonate) (ABTS-), superoxide radical-, and 1,1-diphenyl-2-picrylhydrazyl (DPPH·)-scavenging activities. Fermentation of G. paraguayense E. Walther with Lactobacillus plantarum BCRC 10357 significantly increased the level of flavonoids and total phenolics, including quercetin and gallic acid. Total phenols were the major naturally occurring antioxidant components in lactic acid bacteria-fermented G. paraguayense E. Walther.

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