• Journal of Microbiology and Biotechnology
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• v.13 no.5
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• pp.778-782
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• 2003

In the course of screening anti-influenza agents from natural products, four neuraminidase inhibitors were isolated from the methanol extract of mushroom Microphorus affinis by purification using solvent partition, silica gel column chromatography, Sephadex LH-20, and semi-preparative HPLC. The chemical structures of these compounds were identified as ${\alpha}-lupeol$, methyl linoleate, methyl palmitate, and methyl oleate by means of spectral data including GC-MS, $^1H-,\;and\;^{13}C-NMR\;with\;IC_{50}$ values of 5.65, 7.07, 7.12, and $7.52\;\mu\textrm{M}$, respectively. They did not inhibit other glycosidases such as glucosidase, mannosidase, and galactosidase, indicating that they were relatively specific inhibitors of neuraminidase. The relationship between the fatty acid structure and inhibitory activity was investigated. The result showed that, in the case of an aliphatic linear hydrocarbon skeleton, at least one carboxyl (presumably any carbonyl) moiety and sixteen carbons were the necessary requirements for potent inhibition, whereas saturated, unsaturated, free, and ester forms did not have any significant effect on the activity.

• Archives of Pharmacal Research
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• v.26 no.5
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• pp.367-374
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• 2003

In the course of screening neuraminidase inhibitors from herbal medicines, Reynoutria elliptica exhibited high inhibitory activity. Four active compounds were isolated from the ethyl acetate soluble fraction by consecutive purification using sillica gel, Sephadex LH-20 chromatography, and recrystallization. The chemical structures of these compounds were identified as 1,3,8-trihydroxy-6-methylanthraquinone (emodin) 1,8-dihydroxy-3-methoxy-6-methylanthraquinone (emodin 3-methyl ether; physcion), 1,3,8-trihydroxy-6-hydoxymethylanthraquinone ($\omega$-hydroxyemodin), and 3,5,4 -trihydroxystilbene (trans-resvertrol) by spectral data including MS, $^1 H-, and ^{13}C-NMR. The IC_{50}$ values of emodin, emodin 3-methyl ether, $\omega$-hydroxyemodin, and trans-resvertrol were 2.81, 74.07, 10.49, and 8.77 $\mu$M, respectively. They did not inhibit other glycosidase such as glucosidase, mannosidase, and galactosidase, indicating that they were relatively specific inhibitors of neuraminidase.

• YAKHAK HOEJI
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• v.58 no.1
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• pp.71-79
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• 2014

Although Korean patients with type 2 diabetes mellitus (T2DM) are generally treated by western medicine, many of them strongly believe in the traditional oriental Sasang constitutional classification and depend on it for food, health supplements, and oriental medicines decision making. Sasang constitutional classification is a part of traditional Korean medicine that divides people into four constitutional types (Tae-Yang: TY, Tae-Eum: TE, So-Yang: SY, and So-Eum: SE), which differ in inherited characteristics such as appearance, personality traits, susceptibility to diseases, and drug responses. It is recommended for T2DM patients to control their blood glucose very well from early stages with drugs and diet. However, many T2DM patients respond differently to their drugs, even though they receive the same medicine. Therefore, the present study investigated whether Sasang constitutional type can explain the therapeutic differences between oral hypoglycemic agents (OHAs) therapy (mono, dual and triple drug therapy). Patients of 618 with T2DM diagnosis and Sasang constitutional type known who received both western and oriental medicine treatment in a hospital between April 2006 and April 2013 retrospectively studied. HbA1c (%) and blood glucose (mg/dl) levels before OHAs therapy and 3 month after were collected for metformin (MET) or sulfonylurea (SU) monotherapy, MET+SU dual therapy, MET+except SU (where was either alpha-glucosidase inhibitor, dipeptidyl peptidase-4 inhibitor, meglitinide or thiazolidinedione) dual therapy, and triple therapy, according to Sasang constitutional type. For statistical analysis, ANOVA was used and paired t-test by SPSS 19.0 where P values less than 0.05 were considered statistically significant. Pattern was similar levels of HbA1c and blood glucose and which was decreased in order of mono, MET+SU dual, MET+except SU dual and triple therapy. In all patients comparison, for the So-yang (SY) constitutional type, either monotherapy was less effective; for Te-eum (TE) type, MET+SU dual therapy was less effective while MET+except SU dual therapy was more effective and the triple therapy was less effective; and for So-eum (SE) type, the triple therapy was more effective. For the management of TE type it is recommended to use drugs except SU when dual therapy is needed, restrict triple therapy and consider dual and insulin therapy; for SY type it is recommended to follow current guidelines; and for SE type it is advisable to skip dual therapy and start the triple therapy early. Finally, the therapeutic response to OHAs is different among Korean T2DM patients with different Sasang constitutional types. Taken together, the choice of effective OHAs therapy for each type is necessary in order to minimize the poor control of blood glucose level, the risk of complications, and the costs from a failure of therapy.

• Journal of Microbiology
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• v.43 no.3
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• pp.313-318
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• 2005

In this study, we demonstrate the use of a PCR-based method for the detection of the specific genes involved in natural-product biosynthesis. This method was applied, using specifically designed PCR primers, to the amplification of a gene segment encoding for sedo-heptulose 7-phosphate cyclase, which appears to be involved in the biosynthetic pathways of $C_7N$ aminoacyclitol or its keto analogue-containing metabolites, in a variety of actinomycetes species. The sequences of DNA fragments (about 540 bp) obtained from three out of 39 actinomycete strains exhibited a high degree of homology with the sedo-heptulose 7-phosphate cyclase gene, which has been implicated in acarbose biosynthesis. The selective cultivation conditions of this experiment induced the expression of these loci, indicating that the range of $C_7N$ aminoacyclitol or its keto analogue-group natural products might be far greater than was previously imagined. Considering that a total of approximately 20 $C_7N$ aminoacyclitol metabolites, or its keto analogue-containing metabolites, have been described to date, it appears likely that some of the unknown loci described herein might constitute new classes of $C_7N$ aminoacyclitol, or of its keto analogue-containing metabolites. As these metabolites, some of which contain valienamine, are among the most potent antidiabetic agents thus far discovered, the molecular detection of specific metabolite-producing actinomycetes may prove a crucial step in current attempts to expand the scope and diversity of natural-product discovery.

• Journal of Microbiology and Biotechnology
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• v.18 no.1
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• pp.110-117
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• 2008

Three kinds of prenylated flavonols, icariside I, icariside II, and icaritin, were isolated from an icariin hydrolysate and their effects on melanogenesis evaluated based on mushroom tyrosinase inhibition and quantifying the melanin contents in melanocytes. Although none of the compounds had an effect on tyrosinase activity, icariside II and icaritin both effectively inhibited the melanin contents with an $IC_{50}$ of 10.53 and $11.13{\mu}M$, respectively. Whereas icariside II was obtained from a reaction with ${\beta}$-glucosidase and cellulase, the icariin was not completely converted into icariside II. Thus, for the high-purity production of icariside II, the reaction was optimized using the response surface methodology, where an enzyme concentration of 5.0mg/ml, pH 7, $37.5^{\circ}C$, and 8 h reaction time were selected as the central conditions for the central composite design (CCD) for the enzymatic hydrolysis of icariin into icariside II using cellulase. Empirical models were developed to describe the relationships between the operating factors and the response (icariside II yield). A statistical analysis indicated that all four factors had a significant effect (p<0.01) on the icariside II production. The coefficient of determination $(R^2)$ was good for the model (0.9853), and the optimum production conditions for icariside II was an enzyme concentration of 7.5mg/ml, pH 5, $50^{\circ}C$, and 12 h reaction time. A good agreement between the predicted and experimental data under the designed optimal conditions confirmed the usefulness of the model. A laboratory pilot scale was also successful.

• Journal of Applied Biological Chemistry
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• v.58 no.4
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• pp.317-323
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• 2015

The extracted phenolic compounds from Cornus kousa fruit for biological activities as functional resources were examined. The phenolic compounds which were extracted with water and 40% ethanol from Cornus kousa fruit were $7.04{\pm}0.27$ and $4.47{\pm}0.18mg/g$, respectively. The 1,1-diphenyl-2-picrylhydrazyl free radical scavenging activity of water and ethanol extracts were 84% and 86% at $50{\mu}g/mL$phenolics, respectively. The 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid radical decolorization activity of water and ethanol extracts were 84 and 95% at $100{\mu}g/mL$ phenolics, respectively. Antioxidant protection factor in water and ethanol extracts at $50{\mu}g/mL$ phenolics were 1.93 and 1.82 PF, respectively. Thiobarbituric acid reactive substance were 69% in water extracts and 89% in ethanol extracts at $150{\mu}g/mL$ phenolics. The inhibition activity on xanthine oxidase in water and ethanol extracts was 34 and 60%, respectively. The inhibition activity on ${\alpha}$-glucosidase was 29% in water extracts and 87% in ethanol extracts. The tyrosinase inhibitory activity was 19% in ethanol extracts. The collagenase inhibition activity of anti-wrinkle effect showed an excellent wrinkle improvement effect as 53% in water extracts and 77% in ethanol extracts at $200{\mu}g/mL$ phenolics. The hyaluronidase inhibition activity as antiinflammation effect of water extracts was confirmed to 34% of inhibition at $200{\mu}g/mL$ phenolic. The results can be expected extracts from Cornus kousa fruit to use as functional resource for antioxidant, antigout, inhibitor of carbohydrate degradation, antiwrinkle activity and antiinflammation activity.

• Korean Journal of Food Science and Technology
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• v.49 no.6
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• pp.668-675
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• 2017

To assess the physiological effects of Aruncus dioicus var. kamtschaticus extract on cytoxicity of a neuronal cell line, antioxidant activity, and neuroprotection against intensive glucose-induced oxidative stress were quantitated. Compared to the other fractions, the ethyl acetate fraction of Aruncus dioicus var. kamtschaticus (EFAD) showed the highest total phenolics and flavonoids. The 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assay and malondialdehyde inhibitory effect test confirmed the superior antioxidant activity of EFAD. Moreover, EFAD also decreased the intracellular ROS level and suppressed neuronal cell death against intensive glucose- or $H_2O_2$-induced oxidative stress. Additionally, assessment of ${\alpha}$-glucosidase and acetylcholinesterase inhibitory activities revealed that EFAD was an effective inhibitor of ${\alpha}$-glucosidase and acetylcholinesterase. Finally, high-performance liquid chromatography analysis identified caffeic acid as the main ingredient of EFAD. Overall, these results suggest that the EFAD is a good natural source of biological compounds that counteract hyperglycemic neuronal defects.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.4
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• pp.452-458
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• 2008

The effect of fermented soybean culture of Bacillus subtilis MORI mixed with mulberry leaves on the lowering the levels of blood glucose and cholesterol was examined using neonatal streptozotocin-induced diabetic (n-STZ) rats. B. subtilis MORI produces 1-deoxynojirimycin (DNJ), an $\alpha$-glucosidase inhibitor. The content of DNJ of soybean fermented culture mixed with mulberry was higher (4.1$\pm$0.0 mg/g dry base) than that (1.5$\pm$0.0 mg/g) of mulberry. The concentration of 50% inhibition (IC50) against rat intestinal $\alpha$-glucosidase of soybean fermented culture mixed with mulberry was $5.6{\pm}0.1{\mu}g$/mL and that of mulberry was $17.0{\pm}0.5{\mu}g$/mL. Experimental groups of diabetic rats were randomly assigned to normal control group (NC group), diabetic control group (DC group) and three diabetic groups fed with DNJ food product. One of the three diabetic groups was M group (60 mg DNJ food product/kg) (DNJ food product containing 30% mulberry) and the other two were MM-60 group (60 mg/kg) and MM-120 group (120 mg/kg) (DNJ-fortified food product containing 30% fermented soybean culture mixed with mulberry leaves). The glucose in serum was significantly decreased in the MM-60 and MM-120 groups fed with DNJ-fortified food product for 4 weeks, compared with DC group. Total cholesterol and triglyceride in serum were also lower in MM-60 and MM-120 groups than the DC group. These results support that the fermented soybean culture of B. subtilis MORI mixed with mulberry leaves improved the metabolism of blood glucose and lipid in the n-STZ rat model.

• Nutrition Research and Practice
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• v.5 no.5
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• pp.435-442
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• 2011

At present, lifestyle-related diseases are one of the most critical health issues worldwide. It has been reported that lipopolysaccharide derived from a Gram-negative bacteria (IP-PA1) symbiotic with wheat exhibited several advantageous biological effects, such as the reduction of plasma glucose levels in NOD mice and low-density lipoprotein (LDL) levels in WHHL rabbits. In this study, the beneficial effects on plasma glucose and lipids of a tea (SI tea) consisting of IP-PA1 and Salacia (which contains an inhibitor of ${\alpha}$-glucosidase) were investigated in the KK-Ay/TaJcl type 2 diabetic model mice and in human subjects with premetabolic syndrome in a double-blind, randomized study. S1 tea significantly decreased plasma glucose levels in KK-Ay/TaJcl mice. A clinical trial of SI tea was performed with 41 subjects between the ages of 40 and 69, who belonged either to a high plasma glucose group (HG: FPG 100-125 mg/dl) or to a hyperlipidemia group (HL: TG ${\geq}$ 150 mg/dl, or LDL ${\geq}$ 120 mg/dl, or HDL <40 mg/dl). These subjects ingested either Salacia without IP-PA1 (the control) or SI tea. Blood samples were collected at 0, 30, and 60 days after initiating SI tea treatment, and were measured for FPG, HbA1c, TG, LDL, and HDL. These results showed that SI tea reduced FPG and HbA1c more rapidly than the control in the HL group, and also significantly improved LDL and HDL levels in the HG group. Thus, SI tea may be helpful in preventing lifestyle-related diseases.

• KSBB Journal
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• v.26 no.6
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• pp.517-522
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• 2011

In our previous study, we isolated and characterized a 1-deoxynojirimycin (DNJ)-producing bacterium, Bacillus subtilis MORI, from chungkookjang, a Korean traditional food. B. subtilis MORI was subjected to ${\gamma}$-irradiation and the resulting bacteria were screened for increased DNJ production. A mutant was identified that produced 7.6 times more DNJ and named B. subtilis MORI 3K-85. In this study, the protein profiles of both strains were compared by one-dimensional and two-dimensional gel electrophoresis (1-DE and 2-DE, respectively) under both native and denaturing conditions. The 1-DE native-PAGE and 1-DE SDS-PAGE analyses identified 5 and 7 bands, respectively, that were found at higher concentrations in B. subtilis MORI 3K-85 than in B. subtilis MORI. Similarly, 2-DE analyses identified 20 protein spots which were found at higher concentrations in B. subtilis MORI 3K-85. The peptide mass profiles of these 20 proteins were analyzed by MALDI-TOF and compared with peptide sequences of B. subtilis and B. amyloliquefaciens in the MASCOT database. This screening suggested that three dehydrogenases, an aldolase, a synthetase, an isomerase, a reductase, and a peroxidase are elevated in B. subtilis MORI 3K-85. Based on this data, one or more of the elevated 8 enzymes might be related to the DNJ biosynthetic pathway.