• Journal of Nutrition and Health
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• 제31권2호
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• pp.117-125
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• 1998

Mulberry leaves(Mori folium) and silkworm(Bombyx mori) are potnet inhibiters of intestinal $\alpha$-glycosidase, and inhibit the digestion of starch and sucrose in the small intestine. They are able to prevent postprandial hyperglycemia and decrease blood insulin levels. In this study , a high-carbohydrate diet(CHO ; 67.5%, protein ; 20.8%, fat : 11.7%) was received by the control group. In contrast, the experimental groups received a high-carbohydrate diet with extracts of mulberry leaves and silkwork(50mg.100g diet), and acarbose(6.7mg/100g diet). after a 10 week study period , the experimental groups had lower blood glucose and triglyceride levels. The experimental groups tended to have lwer Hb Alc levels. Also, blood insulin levels were lower than the control groups in accordance with blood glucose levels. The activities of intestinal $\alpha$-glucosidase in the middle and distal parts of small intestine were induced by the extracts of mulberry leaves and silkworm in the experimental groups. However, the activities of liver lysosomal glucosidase and the contents of glycogen in the liver were not affected by the mulberry leave and silkworm extracts nor by acarbose. Mulberry leaves and silkworm were able to prevent sudden postprandial peaks in blood glucose as a result of $\alpha$-glycosidase, inhibition, there by decreasing unnecessary insulin secretion.

• The Korean Journal of Physiology and Pharmacology
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• 제3권4호
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• pp.433-438
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• 1999

Two components of the neuroendocrine-hormonal response to long-term treatment of acarbose, adipose tissue-derived leptin and central neuropeptide Y (NPY), were investigated in the ICR mice on a high- carbohydrate diet. Acarbose, administered 5 or 50 mg per 100 g diet for four weeks, dose dependently suppressed body weight gain. The body weight gain was reduced along with the amount of daily food intake in 50 mg acarbose-treated group at $7^{th}\;and\;28^{th}$ day. 5 or 50 mg acarbose treatment administered for four weeks reduced leptin mRNA levels to 62% and 77% of the control group, demonstrating that the amount of leptin mRNA in adipocytes correlates with body weight. As dose of acarbose increased, leptin mRNA level also increased, suggesting that potent inhibition of ${\alpha}-glycosidase$ by a higher dose of acarbose furthers the enzyme activity and leptin gene consequently. On the other hand, central expression level of NPY gene was increased significantly compared with the control group at the same amount of acarbose administered, reflecting that leptin and NPY operate in a negative-feedback circuit to regulate body fat stores.

• 한국식품영양학회지
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• 제25권3호
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• pp.629-636
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• 2012

Ginsenosides, ginseng saponin, are the principal components responsible for the pharmacological and biological activities of ginseng. In order to improve absorption and biological activities, the biotransformation of major ginsenoside to minor ginsenoside, as the more active compound, is required. In this study, we isolated Lactobacillus brevis THK-D57, which has high ${\beta}$-glycosidase activity, from Kimchi. The major ginsenoside Rb1 was converted to the minor ginsenoside 'compound K' during the fermentation of L. brevis THK-D57. The results propose that the biotransformation pathway to produce compound K is as follows: ginsenoside $Rb_1{\rightarrow}ginsenoside$ $Rd{\rightarrow}ginsenoside$ $F_2{\rightarrow}ginsenoside$ compound K.

• 약학회지
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• 제42권6호
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• pp.613-620
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• 1998

Antidiabetic activity of Mori folium ethanol soluble fraction (MFESF) was examined in db/db mice, which is a spontaneously hyperglycemic, hyperinsulinemic and obese animal model . 500 and 1000mg/kg dose for MFFSF (designated by SY 500 and SY 1000, respectively) and 5mg/kg dose for acarbose were administered for 6 weeks. Body weight gain, fasting and non-fasting serum glucose, glycated hemoglobin and triglyceride were all reduced dose dependently when compared between db/db control group and MFESF treated group. At 11th and 13th week after birth, MFESF increased an insulin secretion which may result in lowering serum glucose level. Total activities of sucrase and maltase in SY 500 treated group were decreased when compared to db/db control. On the other hand, those in SY 1000 and acarbose treated groups were increased. This result may suggest that proteins for sucrase and maltase were compensatorily induced due to significant inhibition of glycosidase-catalyzed reaction at doses administered in this study.

• Archives of Pharmacal Research
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• 제21권1호
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• pp.17-23
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• 1998

Flavonoid glycosides were metabolized to phenolic acids via aglycones by human intestinal microflora producing ${\alpha}$-rhamnosidase, exo-${\beta}$-glucosidase, endo- ${\beta}$-glucosidase and/or ${\beta}$-glucuronidase. Rutin, hesperidin, naringin and poncirin were transformed to their aglycones by the bacteria producing ${\alpha}$-rhamnosidase and ${\beta}$-glucosidase or endo- ${\beta}$-glucosidase, and baicatin, puerarin and daidzin were transformed to their aglycones by the bacteria producing ${\beta}$glucuronidase, C-glycosidase and ${\beta}$-glycosidase, respectively. Anti-platelet activity and cytotoxicity of the metabolites of flavonoid glycosides by human intestinal bacteria were more effective than those of the parental compounds. 3,4-Dihydroxyphenylacetic acid and 4-hydroxyl-phenylacetic acid were more effective than rutin and quercetin on anti-platelet aggregation activity. 2,4,6-Trihydroxybenzaidehyde, quercetin and ponciretin were more effective than rutin and ponciretin on the cytotoxicity for tumor cell lines. We insist that these flavonoid glycosides should be natural prodrugs.

• International Journal of Industrial Entomology and Biomaterials
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• 제7권2호
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• pp.161-164
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• 2003

Several polyhydroxylated alkaloids were isolated from the extracts of freeze-dried silkworm powder, and purified by ion exchange chromatographic analysis. Through the HPLC analysis, we could identify 1-deoxynojirimycin (DNJ) and a kind of calystegin $B_2$ (HS-58) as well as a noble compound (HS-74) from the purified polyhydroxylated alkaloids. In order to know the characteristics of these isolated alkaloids as enzyme inhibitors, glycosidase inhibition activities of these identified alkaloids including other two non-purified alkaloids (SWP 3-1 and SWP 3-2) were investigated.

• 약학회지
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• 제43권6호
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• pp.818-826
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• 1999

Antidiabetic activity and mechanism of Sangbackpitang (SBPT) was examined in db/db mice, which is a spontaneously hyperglycemic, hyperinsulinemic and obese animal model. SBPT and acarbose were administered orally for 4 weeks. Fasting and non-fasting serum glucose, glycated hemoglobin and triglyceride were all reduced when compared between db/db control group and SBPT treated group. At 12th week after birth, SBPT increased an insulin secretion although statistic significance was not seen. Total activities of sucrase, maltase and lactase in SBPT treated group were all decreased when compared to db/db control. On the other hand, sucrase and maltase activities in acarbose treated groups were increased. Effect of SBPT on mRNA expression of glucose transporter(GLUT-4) was also examined. Quantitation of glucose transporter was performed by RT-PCR and in vitro transcription with co-amplification of rat-action gene as an internal standard. Muscular GLUT-4 mRNA expression in SBPT treated group was increased significantly. These results may suggest that SBPT lowered blood glucose ascribing to inhibition of glycosidase-catalyzed reaction and upregulation of muscular GLUT-4 mRNA expression.

• 한국약용작물학회지
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• 제20권6호
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• pp.472-478
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• 2012

This study was carried out to investigate solid-state fermentation method using cellulolytic lactic acid bacteria Lactobacillus plantarum TO-2100 in order to increase piperidine alkaloid contents in mulberry leaves. Piperidine alkaloid, one type of which include 1-deoxynojirimycin (1-DNJ), is known to inhibit ${\alpha}$-glycosidase activities. Using this strain, the optimal solid-state fermentation conditions on mulberry leaves powder were found as the following: initial moisture content, temperature and relative humidity were 20%, $30{\sim}35^{\circ}C$ and 60 ~ 70%, respectively, and the fermentation time was 72 hrs. The piperidine alkaloid contents in the fermented mulberry leaves were 2.86% on dry powder, which is 7-fold increase from that of non-fermented mulberry leaves. The 1-deoxynojirimycin contents after applying preparative thin layer chromatography were 2.02% on dry powder, which is 8 times higher than that of non-fermented mulberry leaves. ${\alpha}$-Glycosidase activities was inhibited by 65.7 ~ 84.7% with 3 ~ 5% treatments of hot-water extracts of the fermented mulberry leaves, compared to 16.2 ~ 40.2% with 3 ~ 5% treatments of hot-water extracts of non-fermented mulberry leaves. Therefore, the results suggest that solid-state fermentation method does indeed increase of piperidine alkaloid contents on mulberry leaves.

• 생명과학회지
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• 제19권5호
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• pp.680-683
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• 2009

당가수분해효소 저해제는 2형 당뇨병, 암, 바이러스 감염제 개발의 주요 타켓화합물이 되고 있다. 본 연구에서는 기능성식품 소재로 이용될 수 있는 대나무 잎에서 ${\alpha}$-glucosidase 저해제를 탐색하였다. 대나무 잎을 메탄올 용매로 추출하고, 이들을 핵산, 클로로포름, 부탄올로 용매분획 하였다. 용매 분획된 각 추출물의 ${\alpha}$-glucosidase 저해활성을 검정시험에서 핵산 분획층에서 강한 ${\alpha}$-glucosidase 저해활성(IC50 33.5 ${\mu}$g/ml)을 관찰하였다. 높은 저해활성을 보여준 핵산 분획층의 활성물질은 linoleic acid로 구조동정 되었다. 분리된 linoleic acid는 IC50이 12.4 ${\mu}$M로 높은 ${\alpha}$- glucosidase 저해활성을 나타내었다. 저해활성 메커니즘 연구에서 linoleic acid는 비경쟁적 저해 양상을 나타내었다. 본 연구는 대나무가 ${\alpha}$-glucosidase 저해활성을 나타내는 첫 번째 연구 결과이다.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.70-71
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• 2001

Naturally occurring azasugar and homologous compounds have been the object of numerous synthetic efforts because these classes of compounds have interesting bioloical activities and the flexibility for the synthesis of chiral alkaloid comounds. As part of a program directed toward the preparation of glycosidase inhibitors, we prepared bicyclic perhydrooxazino- and oxazolopyridine from aminoalcohols and epoxyaldehyde as a common synthetic intermediate.