Hepatoprotective effect of total flavonoids from Glycyrrhiza uralensis Fisch in liver injury mice.

This work aimed to investigate the hepatoprotective effect of total flavonoids from Glycyrrhiza uralensis. The main compounds in licorice total flavonoids (LTF) were isolated from Glycyrrhiza uralensis and their total content in LTF were more than 60%. Hepatoprotective effects of LTF were investigated in three kinds of hepatic injury mice model induced by high-fat emulsion, Chinese liquor and tetrachloromethane. Serum ALT, AST and ALP levels and hepatic MDA, TG, cholesterol, and hydroxyproline of hepatic injury mice were reduced by LTF. Simultaneously, hepatic SOD and glutathione were increased by LTF. These results suggested that LTF can repair liver tissue and reduce hepatic injury via alleviating inflammation, improving antioxidant enzyme activity and reducing oxidative stress in liver tissue and it may be a valuable natural source of hepatoprotective activity.

Spectrum-effect relationship between HPLC fingerprints and bioactive components of Radix Hedysari on increasing the peak bone mass of rat.

The traditional Chinese medicine of Radix Hedysari plays an important role in invigorating gas for ascending, benefiting blood for promoting production of fluid, and promoting circulation for removing obstruction in collaterals, which is consistent with the principle of treatment for osteoporosis. This study is designed to investigate the bioactive components on increasing peak bone mass (PBM) by exploring the spectrum-effect relationship between chromatography fingerprints and effect. Multiple indicators are selected to evaluate the pharmacological activity. In fingerprints, 21 common peaks are obtained, five of which are identified. Furthermore, gray relational analysis (GRA) is a quantitative method of gray system theory and is used to describe the correlation degree of common peaks and pharmacological activities with relational value. 21 components are then divided into three different regions, of which ononin and calycosin play an extremely significant role in increasing PBM. In addition, factor analysis and hierarchical cluster analysis (HCA) are used to screen the optimal producing area for Radix Hedysari. This provides a comprehensive and efficient method to improve the quality evaluation of Radix Hedysari, confirming the bioactive components for PBM-enhancement and further develop its medicinal value.

Anti-atherosclerotic effect of Fermentum Rubrum and Gynostemma pentaphyllum mixture in high-fat emulsion- and vitamin D3-induced atherosclerotic rats.

BACKGROUND: The mixture of Hongqu and gypenosides (HG) is composed of Fermentum Rubrum (Hongqu, in Chinese) and total saponins of Gynostemma pentaphyllum (Thunb.) Makino (Jiaogulan, in Chinese) in a 3.6:1 weight ratio. Both Hongqu and Jiaogulan are considered valuable traditional Chinese medicines (TCMs); they have been commonly used in China for the treatment of hyperlipidemia and related diseases for centuries. The aim of the current study was assess the anti-atherosclerotic effect of HG. METHODS: Sixty-four Wistar rats were randomly divided into eight groups: normal, model, positive control (simvastatin, 1 mg/kg), Hongqu-treated (72 mg/kg), gypenoside (total saponin)-treated (20 mg/kg), and three doses HG-treated (50, 100, and 200 mg/kg). All of the rats were fed a basal diet. Additionally, the model group rats were intragastrically administered a high-fat emulsion and intraperitoneally injected with vitamin D3. The serum lipid profiles, oxidative stress, inflammatory cytokine, and hepatic antioxidant levels were then determined. Furthermore, the liver histopathology and arterial tissue were analyzed, and the expression of hyperlipidemia- and atherosclerosis (AS)-related genes was measured using reverse transcription-polymerase chain reaction. RESULTS: The AS rat model was established after 80 days. Compared to the model group, the HG-treated groups showed an obvious improvement in the serum lipid profiles, oxidative stress, and inflammatory cytokine levels, and showed markedly increased hepatic total antioxidant capacity. Moreover, the expression of genes related to lipid synthesis and inflammation reduced and that of the genes related to lipid oxidation increased in the liver and arterial tissue, which also reflected an improved health condition. CONCLUSION: the anti-atherosclerotic effects of HG were superior to those of simvastatin, Hongqu, and the gypenosides. Therefore, HG may be a useful anti-atherosclerotic TCM preparation.

Lipid-lowering, hepatoprotective, and atheroprotective effects of the mixture Hong-Qu and gypenosides in hyperlipidemia with NAFLD rats.

BACKGROUND: Hyperlipidemia and its complications are among the most harmful of diseases with a worldwide impact, which creates an urgent imperative to find safe and effective drugs for treatment. HG is mainly composed of two kinds of traditional Chinese medicines (TCM), Hong-Qu and gypenosides. Previously, the ingredients of the mixture mainly composed by Hong-Qu and gypenosides (HG) were widely used for purposes of lipid-lowering, antiatherosclerosis effects, and maintaining cardiovascular health in China. The purpose of this study was to determine whether HG provides any benefit to patients with hyperlipidemia. METHODS: Forty-eight adult male Sprague-Dawley rats with fatty liver disease were randomly divided into six groups: normal, model, two positive controls, and two doses of HG-treated groups. The normal rats were fed a basal diet, and the other rats were fed a high-fat diet. Thereafter, the serum lipid profiles, hepatic steatosis, cytokines, enzymes, and relevant mRNA of rats were analyzed in serum, aorta tissue or hepatic tissues, respectively. RESULTS: After 65 days of feeding the high-fat diet to rats, there were significantly disordered serum lipid profiles, elevated oxidative stress biomarkers, and decreased antiinflammatory cytokines in the serum levels. Additionally, aortic foam cell formation was increased. The gene expression levels including hydroxymethylglutaryl-CoA reductase (HMGR), peroxisome proliferator-activated receptor alpha (PPAR-α), sterol response element-binding protein-1c (SREBP-1c), fatty acid synthase (FAS), acetyl-CoA carboxylase-1 (ACC-1) and carnitine palmitoyl transferase-1(CPT-1) in hepatic tissue were also altered by a high-fat diet fed to Sprague-Dawley rats, and HG treatment significantly resolved and normalized these alterations. Moreover, HG not only caused a significant decrease in the lipid drops on the hepatic tissues, but also restored the antioxidant components. CONCLUSION: HG is beneficial for regulating the stability of blood lipids, has atheroprotective characteristics and may prevent nonalcoholic fatty liver disease (NAFLD), providing more than just a theoretical basis for drug research of cardiovascular disease (CVD) treatment.

[Advances of tumor targeting peptides drug delivery system with pH-sensitive activities].

The pH-sensitive peptides drug delivery systems, which target to acidic extracellular environment of tumor tissue, have many advantages in drug delivery. They exhibit a high specificity to tumor and low cytotoxicity, which significantly increase the efficacy of traditional anti-cancer drugs. In recent years the systems have received a great attention. The pH-sensitive peptides drug delivery systems can be divided into five types according to the difference in pH-responsive mechanism,type of peptides and carrier materials. This paper summarizes the recent progresses in the field with a focus on the five types of pH-sensitive peptides in drug delivery systems. This may provide a guideline to design and application of tumor targeting drugs.

Quantification and bio-assay of α-glucosidase inhibitors from the roots of Glycyrrhiza uralensis Fisch.

This work aimed to investigate the α-glucosidase inhibitor from the roots of Glycyrrhiza uralensis Fisch. Seven flavonoids were isolated, and the total content of compounds 1-7 were more than 50% in Glycyrrhiza total flavones (GTF), and the content of compound 1 and 2 was abundant in GTF. The results of the α-glucosidase inhibitory activities indicated that compounds 1-6 and GTF respectively with the IC50 values of 31.303, 30.263, 23.363, 19.528, 10.854, 26.454 and 21.641 µg/mL exhibited the more potent activity than acarbose with the IC50 values of 38.995 µg/mL. These result suggested that Glycyrrhiza flavonoids may become a valid alternative of potential basis for new hypoglycaemic and antidiabetic agents.