• 제목/요약/키워드: antidiabetic activities

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Ginsenoside Rg3의 함량증가를 위한 변환 기술 (Transformation Techniques for the Large Scale Production of Ginsenoside Rg3)

  • 남기열;최재을;박종대
    • 한국약용작물학회지
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    • 제21권5호
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    • pp.401-414
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    • 2013
  • Ginsenoside Rg3 (G-Rg3) contained only in red ginseng has been found to show various pharmacological effects such as an anticancer, antiangiogenetic, antimetastastic, liver protective, neuroprotective immunomodulating, vasorelaxative, antidiabetic, insulin secretion promoting and antioxidant activities. It is well known that G-Rg3 could be divided into 20(R)-Rg3 and 20(S)-Rg3 according to the hydroxyl group attached to C-20 of aglycone, whose structural characteristics show different pharmacological activities. It has been reported that G-Rg3 is metabolized to G-Rh2 and protopanaxadiol by the conditions of the gastric acid or intestinal bacteria, thereby these metabolites could be absorbed, suggesting its absolute bioavailability (2.63%) to be very low. Therefore, we reviewed the chemical, physical and biological transformation methods for the production on a large scale of G-Rg3 with various pharmacological effects. We also examined the influence of acid and heat treatment-induced potentials on for the preparation method of higher G-Rg3 content in ginseng and ginseng products. Futhermore, the microbial and enzymatic bio-conversion technologies could be more efficient in terms of high selectivity, efficiency and productivity. The present review discusses the available technologies for G-Rg3 production on a large scale using chemical and biological transformation.

Pharmacological actions of morusinol on modulation of platelet functions via integrin αIIb/β3 signaling

  • Hyuk-Woo Kwon
    • Journal of Applied Biological Chemistry
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    • 제66권
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    • pp.171-178
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    • 2023
  • Morus alba, a popular medicinal plant belonging to the family Moraceae, has long been used commonly in traditional medicine and has various physiological activities, including antidiabetic, anti-microbial, diuretic, anti-oxidant, and anti-cancer activities. Morusinol was isolated from the root bark of M. alba; however, its biological effects have not yet been reported. Therefore, we examined the inhibitory effects of morusinol on human platelet aggregation, Ca2+ mobilization, and αIIb/β3 activity. Our data showed that collagen-induced human platelet aggregation was inhibited by morusinol without cytotoxicity. In this study, we examined whether morusinol inhibits platelet aggregation through the regulation of integrin αIIb/β3 and its associated signaling molecules. We observed that morusinol inhibited αIIb/β3 activation by regulating vasodilator-stimulated phosphoprotein, phosphatidylinositol-3 kinase, Akt (protein kinase B), and glycogen synthase kinase-3α/β. These results show that morusinol inhibited fibronectin adhesion, fibrinogen binding, and clot retraction. Taken together, morusinol shows strong antiplatelet and anti-clot retraction effects and is a potential therapeutic drug candidate to prevent platelet-related thrombosis and cardiovascular disease.

Effects of Extraction Methods on In Vitro Biological Capacities and Rheological Properties of Polysaccharides from Red Pepper Stems

  • Yoo, Sang-Hun;Chang, Yoon Hyuk
    • Preventive Nutrition and Food Science
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    • 제22권3호
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    • pp.223-230
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    • 2017
  • The purposes of this study were to produce polysaccharides from red pepper stems using different extraction methods and evaluate their chemical composition, in vitro biological capacities, and rheological properties. Two polysaccharides were extracted from red pepper stems using an autoclave and alkali treatments, and the extracts were named PAU and PAL, respectively. The contents of total phenolics and flavonoids were significantly higher in PAU than those in PAL. PAU exhibited greater scavenging activities on 2,2-diphenyl-1-picrylhydrazyl radicals, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radicals, superoxide radicals, and nitrite compared to PAL, suggesting that PAU served as better antioxidants. Similarly, in vitro inhibitory abilities against carbohydrate hydrolyzing enzymes of PAU were higher than those of PAL. Steady shear rheological analysis demonstrated that PAU showed higher psuedoplastic shear-thinning behavior compared to PAL. Based on the results from dynamic shear rheological properties, it was found that both samples had predominantly viscous behavior rather than elastic behavior.

Vanadium Yeast의 독성저감 효과 (Toxic Reduction Effect of Vanadium Yeast)

  • 박승희;정규혁
    • 한국환경성돌연변이발암원학회지
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    • 제21권2호
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    • pp.156-163
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    • 2001
  • Vanadium has been known as environmental polluants resulted from the burning of fossil fuels in nature. It led to toxic responses by prooxidant activity, inducing free radicals and the accumulation in the tissues. Recently, there has been growing interest in an essential nutritional requirement of vandium and especially the treatment of diabetes. But because of its strong toxicity, thease chemicals have narrow safety margin. In order to reduce metal toxicity, and increase absorption and biological activities, metal ions such as selenium and chromium were uptaken in yeast cells. In this study, Vanadium yeast was prepared by uptaking vanadate in yeast cells. Vanadate induced hematological and biochemical changes in the experimental rat blood were inhibited by the treatments of vanadium yeast. Lipid peroxidation and catalase activity were significantly increased in kidney and liver after a single intraperitoneal injection of vanadate to rats. However, these observations were apparently reduced in the vanadium yeast treated group. Vanadium amount in blood, kidney and liver after a single intraperitoneal injection of vanadium yeast was significantly reduced than that of vanadate treated group. In conclusion, vanadium yeast uptaken vanadate in yeast cells could reduce toxic effects of vanadate.

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Metabolism of Ginsenosides to Bioactive Compounds by Intestinal Microflora and Its Industrial Application

  • Kim, Dong-Hyun
    • Journal of Ginseng Research
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    • 제33권3호
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    • pp.165-176
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    • 2009
  • Korean ginseng, which contains ginsenosides and polysaccharides as its main constituents, is orally administered to humans. Ginsenosides and polysaccharides are not easily absorbed by the body through the intestines due to their hydrophilicity. Therefore, these constituents which include ginsenosides Rb1, Rb2, and Rc, inevitably come into contact with intestinal microflora in the alimentary tract and can be metabolized by intestinal microflora. Since most of the metabolites such as compound K and protopanaxatriol are nonpolar compared to the parental components, these metabolites are easily absorbed from the gastrointestinal tract. The absorbed metabolites may express pharmacological actions, such as antitumor, antidiabetic, anti-inflammatory, anti-allergic, and neuroprotective effects. However, the activities that metabolize these constituents to bioactive compounds differ significantly between individuals because all individuals possess characteristic indigenous strains of intestinal bacteria. Recently, ginseng has been fermented with enzymes or microbes to develop ginsengs that contain these metabolites. However, before using these enzymes and probiotics, their safety and biotransforming activity should be assessed. Intestinal microflora play an important role in the pharmacological action of orally administered ginseng.

Supplementation of a Novel Microbial Biopolymer, PGB1, from New Enterobacter sp. BL-2 Delays the Deterioration of Type 2 Diabetic Mice

  • Yeo, Ji-Young;Lee, Yong-Hyun;Jeon, Seon-Min;Jung, Un-Ju;Lee, Mi-Kyung;Jung, Young-Mi;Choi, Myung-Sook
    • Journal of Microbiology and Biotechnology
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    • 제17권12호
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    • pp.1983-1990
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    • 2007
  • Antidiabetic effects of a novel microbial biopolymer (PGB) 1 excreted from new Enterobacter sp. BL-2 were tested in the db/db mice. The animals were divided into normal control, rosiglitazone (0.005%, wt/wt), low PGB1 (0.1%, wt/wt), and high PGB1 (0.25%, wt/wt) groups. After 5 weeks, the blood glucose levels of high PGB1 and rosiglitazone supplemented groups were significantly lower than those of the control group. In hepatic glucose metabolic enzyme activities, the glucokinase activities of PGB1 supplemented groups were significantly higher than the control group, whereas the PEPCK activities were significantly lower. The plasma insulin and hepatic glycogen levels of the low and high PGB1 supplemented groups were significantly higher compared with the control group. Specifically, the insulin and glycogen increases were dose-responsive to PGB1 supplement. PGB1 supplement did not affect the IPGTT and IPITT compared with the control group; however, rosiglitazone significantly improved IPITT. High PGB1 and rosiglitazone supplementation preserved the appearance of islets and insulin-positive cells in immunohistochemical photographs of the pancreas compared with the control group. These results demonstrated that high PGB1 (0.25% in the diet) supplementation seemingly contributes to preventing the onset and progression of type 2 diabetes by stimulating insulin secretion and enhancing the hepatic glucose metabolic enzyme activities.

Six new dammarane-type triterpene saponins from Panax ginseng flower buds and their cytotoxicity

  • Li, Ke-Ke;Li, Sha-Sha;Xu, Fei;Gong, Xiao-Jie
    • Journal of Ginseng Research
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    • 제44권2호
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    • pp.215-221
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    • 2020
  • Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F1 (1), 3β-acetoxyl ginsenoside F1 (2), ginsenoside Rh24 (6), ginsenoside Rh25 (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh26 (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

Multiple Low Dose Streptozotocin으로 유도된 당뇨 흰쥐에서 투여 시기에 따른 인삼의 항당뇨 활성 비교 (Comparisons of Antidiabetic Effect of Panax Ginseng on MLD STZ-induced Diabetic rats in Terms of Time of Administration)

  • 박경수;이동억;성종환;정성현
    • Journal of Ginseng Research
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    • 제26권4호
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    • pp.191-195
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    • 2002
  • MLD STZ로 당뇨를 유발시킨 SD rat에서 투여 시기에 따른 백삼의 항당뇨 활성을 비교한 결과를 요약하면 다음과 같다. 1. 동시 투여군은 실험 시작 초반에 체중이 감소하는 듯 하였다가 당뇨 대조군에 비하여 현저히 체중이 증가하였고 후 투여군 역시 백삼의 투여에 의하여 체중이 증가하였다. 2. 동시 투여군에서 STZ 투여 후 초반 7일간 혈당이 상승 하였으나 곧 탁월한 혈당 강하 활성을 나타내었으며 또한 계속적:인 당뇨병의 진행을 막아주었다. 후 투여군에서는 즉각적으로 혈당 강하 활성이 나타났고 이는 투여 종료 시점까지 유지되었다. 3. 동시 투여군과 후 투여군 모두 식이량과 음용수 섭취량을 개선시켜 주었다. 4. 동시 투여군과 후 투여군은 모두 체중 대비 신장 무게의 비를 낮추어 줌으로써 고혈당으로 인해 야기되는 신장비대를 개선시켜 주었다. 5. STZ로 유도된 당뇨 흰쥐에서 백삼이 혈당 강하 활성을 나타내는 것은 췌장 베타세포의 보호 활성과 insulin의 분비 촉진과 관련이 있을 것으로 추측된다. 6. 각 투여군에서 투여 종료시점의 혈당이 당뇨 대조군에 비하여 각각 64%, 67%수준을 나타내어 백삼이 당뇨병이 발생되기 전이나 혹은 당뇨병이 발생된 후에 투여되더라도 우수한 혈당강하 효과를 나타낼 수 있음을 알 수 있었다. 따라서 인삼은 impaired glucose tolerance(IGT)를 나타내는 사람에서 당뇨병의 발병을 예방할 목적으로 투여할수 있을 뿐만 아니라 이미 당뇨병이 발병된 사람에서도 우수한 혈당 강하 활성을 나타내어 치료제로서의 가능성도 보여주었다.

커피 볶음 정도에 따른 생화학적 성분 및 생리활성의 변화 (Changes of biochemical components and physiological activities of coffee beans according to different roasting conditions)

  • 남상해;강수지
    • 한국식품저장유통학회지
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    • 제22권2호
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    • pp.182-189
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    • 2015
  • 4종류의 커피 원두(CS, Colombia superimo; EY, Ethiopia yirgacheffee; IM, Indonesia mandheling; IMM, India monsooned malabar AA)를 생두(raw coffee bean)와 각각 다른 온도(200, $250^{\circ}C$)와 시간(10, 15, 20 min)으로 로스팅하였으며, 최적의 로스팅 조건을 찾기 위하여 로스팅 중에 변화되는 pyrazine을 비롯한 몇 가지 성분과 항산화, 항당뇨 효과를 조사하였다. Caffeine 함량은 로스팅 정도에 따라 크게 차이를 보이지 않았으나, 5-caffeoylquinic acid와 total phenolic compounds는 대체로 로스팅이 강해질수록 크게 감소하였다. Pyrazine 화합물은 IMM에서 가장 많이 생성되었으며, $250^{\circ}C$에서는 시간이 경과할수록 급격히 줄어들었다. DPPH 라디칼 소거활성은 같은 처리농도에서의 BHT와 ${\alpha}$-tocopherol의 활성에 비하여 대부분 80% 이상의 효과를 나타내었다. 한편 FRAP assay에서는 로스팅 정도가 강해질수록 활성이 약간 감소하였다. ${\alpha}$-Glucosidase 저해활성은 유의할 만한 수준이었으나, $250^{\circ}C$에서 20분 roasting할 경우에는 활성이 80% 이상 줄어들었으며, ${\alpha}$-amylase 저해활성도 유사한 경향이었다. 이러한 결과로 로스팅 정도에 따른 생리활성과 커피의 고소한 향과 초콜릿 향을 내는 pyrazine 화합물의 생성을 종합적으로 보았을 때, $200^{\circ}C$에서 15분정도 로스팅하는 것이 가장 최적의 조건인 것으로 판단하였다. 따라서 이러한 결과는 커피산업에서 로스팅 조건을 달리한 원두커피의 향과 생리활성이 높은 커피를 생산하는데 활용될 수 있을 것이라 기대된다.

Rats Lens Aldose Reductase Inhibitor Activities of Leguminous Seed Extracts

  • Kim, Byung-Su;Kim, Min-Jeong;Kim, Hye-Young;Ahn, Young-Joon;Lee, Hoi-Seon
    • Preventive Nutrition and Food Science
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    • 제6권1호
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    • pp.38-42
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    • 2001
  • The methanol extracts of 25 leguminous seeds in vitro were evaluated for inhibitory activities against lens aldose reductase of Sprague Dawley male rats. The responses varied with both leguminous seed and concentration used. At the concentration of 0.1 mg/mL, the methanol extracts from Amphicaraea edgeworthii, Canavalia lineata, Gylcine max var. solitae, Glycine max var. yagkong, Glycine max var. hooktae, Glycine max var. bangkong, Glycine max var. geumdu, Glycine max var. chungtae, Glycine max var. mejukong, Glycine soja, Phaseolus radiatus var. geodu, Vicia tetrasperma, Vigna angulasis, and Vigna sinensis inhibited enzyme activity by greatertha 60%. In following study, at the concentration of 0.01 mg/mL, the extracts of C. lineata and V. tetraspermahad relatively strong inhibitory activity against aldose reductase. Because of their potent inhibitory activities, the activity of each solvent fraction from C. lineata and V. tetrasperma was determined, and the potent activity was showed from chloroform and hexane fractions, respectively. {TEX}$IC_{50}${/TEX} values of C. lineata and V. tetrasperma were 0.004 and 0.006 mg/mL, respectively. As a naturally occurring therapeutic agent, leguminous seeds described could be useful for developing new agents of antidiabetic complications.

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