Effect of the monascus pigment threonine derivative on regulation of the cholesterol level in mice

Different amino acid derivatives were synthesized during cultivation of a Monascus species. Derivatives exhibiting an inhibitory activity against HMG-CoA reductase were screened by in vitro tests. The threonine derivative had a high inhibitory activity of 38% while four other derivatives showed a greater than 23% activity. The orange monascus pigment showed a high activity of 36%. In vivo tests using female C57BL/6 mice were performed with the threonine derivative and orange pigment. Changes in the cholesterol and lipid levels in mice due to addition of the pigments were investigated. The total cholesterol (TC) level of mouse serum was reduced by 8–9% with the threonine derivative and by 16% with orange pigment. Supplementation with the threonine derivative and orange pigment decreased the LDL cholesterol level by 18–26% and increased the HDL cholesterol level by 1–9%. The atherogenic index (AI) value was reduced by 23–27% with pigment supplementation. The anti-atherosclerosis effect of monascus pigments can be induced by control of the lipid content in the serum rather than in the liver of mice.     

Stoichiometric and nonstoichiometric polyelectrolyte complex of chitosan and polyethyleneglycol‐monosuccinate: Preparation and characterization

Stoichiometric and nonstoichiometric polyelectrolyte complex (PEC) was prepared with polyethylene glycol‐monosuccinate (PEGMS), and chitosan (CS). A series of PEGMS were synthesized by a 1 : 1 mol ratio between PEG and succinic anhydride. Then, the novel PEC was prepared by a various mole reaction of the above synthesized PEGMS and CS. The physicochemical properties of the synthesized PEC was characterized by using elemental analysis, FTIR, ¹H, and ¹³C nuclear magnetic resonance, dissolution behavior, and phase transition phenomenon. Furthermore, some properties of the PEC obtained were analyzed by UV‐Visible spectrometry, wide‐angle X‐ray diffraction, differential scanning calorimeter, scanning electron microscope, and estimated solubility, and cell viability assay, respectively. It was found that the observed FTIR, ¹H, and ¹³C‐NMR data was in good agreement with the chemical structure of the prepared PEGMS and PEC. The dissolution behaviors of nonstoichiometric PEC were found to depend on the pH of the solution as well as on the PEGMS/CS composition. The study of MTT assay suggested that the viability of HepG2 human hepatoblastoma cell on PEC were increased significantly in accordance with mole ratio of CS. As the results, the obtained several product is a useful intermediate, which permits further chemical modification for the amino group of CS and may have potential applications in biocompatible or cosmetic systems. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci 2007     

Soybean (Glycine max L. Merr.) hexane extracts inhibit cellular fatty acid uptake by reducing the expression of fatty acid transporters

Intake of saturated and trans-fatty acids is a strong risk factor for coronary heart disease. We investigated the inhibitory effects of 2 hexane extracts from white (WBE) and black soybeans (BBE) on cellular fatty acid uptake in vitro. Transcellular uptake of elaidic acid (t18:1), a major trans-fatty acid present in processed foods, in Caco-2 monolayers was significantly reduced by 28.3 and 16.7% 60 min after WBE and BBE treatment, respectively. Results of flow cytometry (FACS) analysis showed significant reductions in boron-dipyrromethene (BODIPY) fluorescence-labeled fatty acid uptake by 35.4 and 40.2% with WBE and BBE treatment, respectively. BBE treatment significantly reduced the expression of fatty acid transport protein-4 and CD36 in Caco-2 cells, as determined by quantitative real time-polymerase chain reaction (qRT-PCR). Similar trends were found in WBE treatment, although to a lesser degree. These observations suggest that soybean extract may reduce fatty acid uptake and cellular fat accumulation by altering fatty acid transporter expression.     

Toxicological evaluation of the isoflavone puerarin and its glycosides

Puerarin, an isoflavone derived from kudzu roots, has strong biological activities. However, its bioavailability in vivo is often limited by its insolubility. A novel transglycosylase increases the solubility of puerarin >100-fold, by converting it to puerarin glycosides. Since over-consumption of an isoflavone might have toxic effects, therefore, we investigated the potential antimutagenic activity, bone marrow micronucleus test, and a 28-day oral repeated administration test with puerarin and its glycosides. In Ames tests, neither puerarin nor its glycosides exhibited mutagenic effects up to 200 μg/plate. Puerarin and its glycoside, glucosyl-α-(1,6)-puerarin, significantly reduced the mutagenic effect of 4-nitroquinoline-1-oxide by up to 41%. In bone marrow micronucleus tests using ICR mice, neither puerarin nor glucosyl-α-(1,6)-puerarin interfered with erythrocyte production in the bone marrow. Both compounds decreased the prevalence of polychromatic erythrocytes. Sprague–Dawley rats were orally dosed with puerarin and its glycosides daily for 28 days. Neither puerarin nor its glycosides caused significant alterations in histology, and biochemical and hematologic parameters. These results suggest that puerarin and its glycosides do not have significant toxic effects, at least in rodents, either in vitro or in vivo at doses of up to 250 mg/kg per day.