OBJECTIVETo study the chemical constituents from the leaves of Morus multicaulis.

METHODThe compounds were isolated by ion exchange resin, silica gel and Sephadex LH -20 column chromatographies. Their structures were elucidated on the basis of physico-chemical properties and spectral data.

RESULTTwelve compounds were isolated from the leaves of this plant. Their structures were identified as 1-deoxynojirimycin (1), fagomine (2), 2-O-alpha-D-galactopyranosyl-1-deoxynojirimycin (3), quercetin-7-O-beta-D-glucoside (4), kaempferol (5), quercetin (6), scopoletin (7), D-aspartic acid (8), L-proline (9), D-alpha-alanine (10), myo-inositol (11) and dausterol (12).

CONCLUSIONAll compounds were isolated from this plant for the first time.

1-Deoxynojirimycin ; analysis ; chemistry ; isolation & purification ; Imino Pyranoses ; analysis ; chemistry ; isolation & purification ; Kaempferols ; analysis ; chemistry ; isolation & purification ; Morus ; chemistry ; Piperidines ; analysis ; chemistry ; isolation & purification ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Spectrometry, Mass, Electrospray Ionization

The anti-diabetes mechanism of silkworm Bombyx mori L. powder and extracts was found to inhibit the activity of alpha-glycosidase. The major functional component of silkworm powder was 1-deoxynojirimycin (1-DNJ), which exerts a blood glucose-lowering effect. In this study, we aimed to compare the effects of the supplements, including red ginseng extract on the functional components of silkworm. Fifty silkworm larvae were divided into the control group (Con, N=50), group A (A, artificial diet 95% and mulberry leaf powder 5%), group B (B, artificial diet 95% and mulberry powder 5%), group C (C, artificial diet 95% and Rubus coreanus remainders 5%), group D (D, artificial diet 95% and red ginseng extract 5%), and group E (E, artificial diet 95% and yeast powder (Saccharomyces cerevisiae). Body weights and length of silkworm larvae showed significant improvement in group A, D. In particular, the growth rate in group D (artificial diet 95% and red ginseng extract 5%) was larger than that of Con. In addition, the results showed that 1-DNJ concentration was significantly largest in group D. From these results, it is concluded that the addition of red ginseng extract may be effective for larval growth and 1-DNJ accumulation in silkworm rearing with an artificial diet.
1-Deoxynojirimycin ; Body Weight ; Bombyx ; Diet ; Larva ; Morus ; Panax ; Yeasts

OBJECTIVETo study the correlation of 1-deoxynojirimycin (DNJ) between Taxilli Herba parasitized in mulberry and its host-plants.

METHODThe contents of DNJ of Taxilli Herba parasitized in mulberry and non-mulberry were determined by RP-HPLC. DNJ was extracted with 0.05 mol x L(-1) HCl, and then detected by fluorescence detector after derivatized with FMOC-Cl at pH 8.0 with borate buffer. The separation was performed on an Agilent C18 (4.6 mm x 250 mm, 5 microm) column with a mobile phase of acetonitrile-0.1% aqueous acetic acid (51: 49) at a flow rate of 1.0 mL x min(-1). The wavelength of fluorescence detector was operated at lambda(EX) = 254 nm and lambda(EM) = 322 nm.

RESULTThe linear range of DNJ was 3.72-37.2 mg x L(-1) (r = 0.999 9). The average recovery was 96.42%. The contents of DNJ in mulberry and Taxilli Herba parasitized in mulberry were 1.39-10.16 mg x g(-1) and 0.46-2.72 mg x g(-1), respectively. However, the contents of DNJ could not be detected in Taxilli Herba parasitized in non mulberry and its host-plants.

CONCLUSIONAs the characteristic constituent of mulberry, DNJ was accumulated in Taxilli Herba This method can be applied to the quality control of Taxilli Herba from mulberry.

1-Deoxynojirimycin ; analysis ; Chromatography, High Pressure Liquid ; Drug Stability ; Morus ; chemistry ; Reproducibility of Results

OBJECTIVETo develop a high performance liquid chromatographic method for the determination of DNJ in Morus alba leaves with fluorimetric detection after precolumn derivatization with 9-fluorenylmnethyl chlorformate (FMOC-Cl).

METHODDNJ in Morus alba leaves was extracted with 0.05 mol x L(-1) HCl, reacted with FMOC-Cl, and separated on a HiQSiL C18 column at 250 degrees C. Mobile phase consisted of acetonitrile-0.1% aqueous acetic acid (55:45) with a flow rate of 1.0 mL x min. The fluorescence detector was operated at lambdaEX = 254 nm, lambdaEM = 322 nm.

RESULTA satisfactory separation between DNJ and impurity was obtained. The calibration curve was linear over the concentration range from 0.567 microg x mL(-1) to 34 microg mL(-1), r = 0.9998. The average recovery was 97.2%. The contents of DNJ in M. alba collected in different seasons and grown in different environment were determined.

CONCLUSIONThe quantity of DNJ in leaves of M. alba is related to the environment factor, temperature and growing period. The method can be used for qualioy control of the medicinal material.

1-Deoxynojirimycin ; analysis ; Ecosystem ; Morus ; chemistry ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Quality Control ; Seasons ; Temperature

The purpose of this study was to investigate the anti-hyperlipidemic effect of soy bean extract solution fermented by Bacillus subtilis MORI (BTD-1E) in obese db/db mice. Eight-week-old male db/db mice were administered 33.3 mg/kg BTD-1E solution orally once a day for four weeks. The BTD-1E group showed significantly lower body weight compared with the db control group (P<0.05). The BTD-1E group showed significantly lower serum total cholesterol and LDL cholesterol levels compared with the db control group, respectively (P<0.05, P<0.01). The BTD-1E group showed significantly decreased liver weight relative to final body weight compared with the db control group (P<0.01). After four weeks of BTD-1E administration, lipid droplets in the liver were apparently decreased in the BTD-1E group compared to the db control group. In summary, our results suggest that BTD-1E has an anti-hyperlipidemic effect in the obese mouse model.
1-Deoxynojirimycin ; Animals ; Bacillus ; Bacillus subtilis ; Body Weight ; Cholesterol ; Cholesterol, LDL ; Humans ; Liver ; Male ; Mice ; Mice, Obese ; Soybeans

OBJECTIVETo study the chemical constituents of Polygala telephioides.

METHODThe compounds were isolated and purified on macroporous resin, silica gel, Sephadex LH-20, Chromatorex ODS column chromatograph and the structures were determined based on the spectral and chemical evidences.

RESULTFour compounds were obtained and characterized as telephiose G, telephiose D, isomangiferin, quescetin 3-O-beta-D-glucopyranoside, respectively.

CONCLUSIONCompounds 2-4 were obtained from this plant for the first time and the compound 2 (telephiose G) was a new compound.

1-Deoxynojirimycin ; isolation & purification ; Dextrans ; Glucosides ; isolation & purification ; Molecular Structure ; Plant Extracts ; pharmacology ; Polygala ; chemistry ; Silica Gel ; Silicon Dioxide ; isolation & purification ; Spectrometry, Mass, Electrospray Ionization ; Xanthones ; isolation & purification

Here we have investigated how lactosylceramide (LacCer) modulates gene expression of adhesion molecules in TNF-alpha and IFNgamma (CM)-stimulated astrocytes. We have observed that stimulation of astrocytes with CM increased the gene expression of ICAM-1 and VCAM-1. D-Threo-1-phenyl- 2-decanoylamino-3-morpholino-1-propanol (PDMP) and N-butyldeoxynojirimycin (NBDNJ), inhibitors of glucosylceramide synthase (GLS) and LacCer synthase (galactosyltransferase, GalT-2), inhibited the gene expression of ICAM-1 and VCAM-1 and activation of their gene promoter induced by CM, which were reversed by exogenously supplied LacCer. Silencing of GalT-2 gene using its antisense oligonucleotides also attenuated CM-induced ICAM-1 and VCAM-1 expression, which were reversed by LacCer. PDMP treatment and silencing of GalT-2 gene significantly reduced CM-induced luciferase activities in NF-KB, AP-1, GAS, and STAT-3 luciferase vectors-transfected cells. In addition, LacCer reversed the inhibition of NF-KB and STAT-1 luciferase activities by PDMP. Taken together, our results suggest that LacCer may play a crucial role in the expression of ICAM-1 and VCAM-1 via modulating transcription factors, such as NF-KB, AP-1, STAT-1, and STAT-3 in CM-stimulated astrocytes.
1-Deoxynojirimycin ; Antigens, CD ; Astrocytes ; Galactosyltransferases ; Gene Expression ; Glucosyltransferases ; Intercellular Adhesion Molecule-1 ; Lactosylceramides ; Luciferases ; Morpholines ; NF-kappa B ; Oligonucleotides, Antisense ; Transcription Factor AP-1 ; Transcription Factors ; Tumor Necrosis Factor-alpha ; Vascular Cell Adhesion Molecule-1

Fabry disease is an X-linked inborn error of glycosphingolipid catabolism that results from mutations in the gene encoding the alpha-galactosidase A (GLA) enzyme. We have identified 15 distinct mutations in the GLA gene in 13 unrelated patients with classic Fabry disease and 2 unrelated patients with atypical Fabry disease. Two of the identified mutations were novel (i.e., the D231G missense mutation and the L268delfsX1 deletion mutation). This study evaluated the effects of the chemical chaperones 1-deoxygalactonojirimycin (DGJ) on the function of GLA in vitro, in cells containing missense mutations in the GLA gene. Nine missense and a nonsense mutations, including one novel mutation were cloned into mammalian expression vectors. After transient expression in COS-7 cells, GLA enzyme activity and protein expression were analyzed using fluorescence spectrophotometry and Western blot analysis, respectively. DGJ enhanced GLA enzyme activity in the M42V, I91T, R112C and F113L mutants. Interestingly, the I91T and F113L mutations are associated with the atypical form of Fabry disease. However, DGJ treatment did not have any significant effect on the GLA enzyme activity and protein expression of other mutants, including C142W, D231G, D266N, and S297F. Of note, GLA enzyme activity was not detected in the novel mutant (i.e., D231G), although protein expression was similar to the wild type. In the absence of DGJ, the E66Q mutant had wild-type levels of GLA protein expression and approximately 40% GLA activity, indicating that E66Q is either a mild mutation or a functional single nucleotide polymorphism (SNP). Thus, the results of this study suggest that the chemical chaperone DGJ enhances GLA enzyme activity and protein expression in milder mutations associated with the atypical form of Fabry disease.
1-Deoxynojirimycin/*analogs & derivatives/metabolism ; Adolescent ; Adult ; Animals ; Asian Continental Ancestry Group/*genetics ; COS Cells ; Cercopithecus aethiops ; Fabry Disease/*enzymology/genetics ; Gene Expression ; Humans ; Male ; Middle Aged ; Mutation ; Young Adult ; alpha-Galactosidase/*genetics/*metabolism

An HPLC-UV method has been developed for the determination of valibose, miglitol, voglibose and acarbose, the four anti-diabetic drugs. The separation was accomplished successfully by using reversed phase chromatography (Prevail carbohydrate column, 250 mm x 4.6 mm, 5 microm) with a gradient acetonitrile-phosphate buffer solution (pH 8.0) at a wavelength of 210 nm. Furthermore, the method of a high-performance liquid chromatography coupled with ESI-MS in positive ionization mode has been established. These two methods were successfully applied to the assay and qualitative detection of four alpha-glucosidase inhibitors in the potential counterfeit anti-diabetic drugs.
1-Deoxynojirimycin ; analogs & derivatives ; analysis ; Acarbose ; analysis ; Chromatography, High Pressure Liquid ; methods ; Chromatography, Reverse-Phase ; Glycoside Hydrolase Inhibitors ; Hypoglycemic Agents ; chemistry ; Inositol ; analogs & derivatives ; analysis ; Spectrometry, Mass, Electrospray Ionization ; methods ; Spectrophotometry, Ultraviolet ; alpha-Glucosidases ; analysis

The silkworm extract powder contain 1-deoxynojirimycin (DNJ), a potent alpha-glycosidase inhibitor, has therapeutic potency against diabetes mellitus. Therefore, natural products containing DNJ from mulberry leaves and silkworm are consumed as health functional food. The present study was performed to evaluate the safety of the silkworm extract powder, a health food which containing the DNJ. The repeated toxicity studies and gentic toxicity studies of the silkworm extract powder were performed to obtain the data for new functional food approval in MFDS. The safety was evaluated by a single-dose oral toxicity study and a 90 day repeated-dose oral toxicity study in Sprague-Dawley rats. The silkworm extract powder was also evaluated for its mutagenic potential in a battery of genetic toxicity test: in vitro bacterial reverse mutation assay, in vitro chromosomal aberration test, and in vivo mouse bone marrow micronucleus assay. The results of the genetic toxicology assays were negative in all of the assays. The approximate lethal dose in single oral dose toxicity study was considered to be higher than 5000 mg/kg in rats. In the 90 day study, the dose levels were wet at 0, 500, 1000, 2000 mg/kg/day, and 10 animals/sex/dose were treated with oral gavage. The parameters that were monitored were clinical signs, body weights, food and water consumptions, ophthalmic examination, urinalysis, hematology, serum biochemistry, necropsy findings, organ weights, and histopathological examination. No adverse effects were observed after the 90 day administration of the silkworm extract powder. The No-Observed-Adverse-Effect-Level (NOAEL) of silkworm extract powder in the 90 day study was 2000 mg/kg/day in both sexes, and no target organ was identified.
1-Deoxynojirimycin ; Animals ; Biochemistry ; Biological Agents ; Body Weight ; Bombyx* ; Bone Marrow ; Chromosome Aberrations ; Diabetes Mellitus ; Functional Food ; Food, Organic ; Hematology ; Mice ; Micronucleus Tests ; Morus ; Mutagenicity Tests ; Organ Size ; Rats ; Rats, Sprague-Dawley ; Toxicology ; Urinalysis ; Drinking