• 제목/요약/키워드: Aldose reductase inhibitory activity

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혈압, 혈당 및 콜레스테롤농도 조절에 영향을 주는 식이 메밀인자의 in vitro 검정 (In vitro Screening of Dietary Factors on Buckwheat(Fagopyrum esculentum Moench) Influencing the Regulation of Blood Pressure, Glucose and Cholesterol Level)

  • 최용순;김복란;김려화;이병훈;심태흠;이상영
    • 한국식품영양과학회지
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    • 제29권2호
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    • pp.280-287
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    • 2000
  • Generally, buckwheat has been regarded as a crop of secondary importance in many countries. In vitro functionalities of buckwheats as a food were evaluated in this study. Five of buckwheat cultivars were extracted with methanol, and the extractant were dried and lyophilized, separately. Or water soluble buckwheat components were digested with the commercial enzymes and the obtained protein hydrolysate was again fractionated by acid precipitation. The antioxidant capacity of the methanol extracts determined using Fe2+-ascorbic acid system was dependent ont the cultivars: The extract of Suwon 4 showed 3.3 times stronger activity than ascorbic acid in terms of IC50. Also, the extracts of buckwheats inhibited efficiently the activities of $\alpha$-amylase and lens aldose reductase. Buckwheat soluble protein or rutin suppressed the in vitro activities of angiotensin-converting enzyme, and the inhibitory degree depended largely on the cultivars. Buckwheat proteins exerted higher hydrophobicity being related to the sterol binding capacity than casein. The results suggested that buckwheat seeds may be desirable and functional food resources in human living in current society.

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한국 자생식물 추출물 23종의 Aldo-keto reductase family 1 B10 (AKR 1 B10) 효소 억제효과 (Inhibitory Effects of 23 Korean Local Plant Extracts on Aldo-keto reductase family 1 B10 (AKR 1 B10))

  • 이주영;송대근;정상훈;김종환;안수용;노주원;판철호
    • 생약학회지
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    • 제40권3호
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    • pp.238-243
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    • 2009
  • We examined ethanol extracts prepared from 23 Korean local plants obtained in Pyeongchang, Gangwon-do for their inhibitory effects on recombinant human AKR 1 B10 (rhAKR1B10) in vitro. To do this, rhAKR1B10 was first expressed in E. coli as a biological active form and purified by using Ni-affinity chromatography followed by gel permeation chromatography. Then, rhAKR1B10 was used for screening out 23 Korean local plant extracts having an inhibitory activity against itself. Among them, six extracts showed more than 50% inhibition of rhAKR1B10 activity at the concentration of $10{\mu}g$/ml. Especially, the extracts of Ligularia fischeri var. spiciformis Nakai and Rhus trichocarpa Miq. were the most potent because their $IC_{50}$ values were 2.94 and $2.00{\mu}g$/ml, respectively.

Inhibitory effects of polyphenols isolated from Rhus verniciflua on Aldo-keto reductase family 1 B10

  • Song, Dae-Geun;Lee, Joo-Young;Lee, Eun-Ha;Jung, Sang-Hoon;Nho, Chu-Won;Cha, Kwang-Hyun;Koo, Song-Yi;Pan, Cheol-Ho
    • BMB Reports
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    • 제43권4호
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    • pp.268-272
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    • 2010
  • Aldo-keto reductase family 1 B10 (AKR1B10) is a member of the NADPH-dependent aldo-keto reductase (AKR) superfamily, and has been considered to be a potential cancer therapeutic target. Total extract from the bark of Rhus verniciflua (Toxicodendron vernicifluum (Stokes)) showed AKR1B10 inhibitory activity. To identify the active compounds from R. verniciflua responsible for AKR1B10 inhibition, nine compounds were isolated via bioactivity-guided isolation and tested for their effects against recombinant human AKR1B10 (rhAKR1B10). Results showed that butein, isolated from the ethyl acetate fraction, was most able to inhibit rhAKR1B10. The inhibitory rate of butein against rhAKR1B10 was 42.86% at $1\;{\mu}M$ with an IC50 value of $1.47\;{\mu}M$, and enzyme kinetic analysis revealed its inhibition mode to be uncompetitive.

한국 자생식물 추출물의 항산화 및 Aldo-keto Reductase Family 1 B10 효소 억제 효과 (Antioxidant and Aldo-keto Reductase Family 1 B10 Inhibition Activities of Korean Local Plant Extracts)

  • 판철호;이주영;송대근;김종환;안수용;배덕성;김영훈;이재권
    • Journal of Applied Biological Chemistry
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    • 제52권4호
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    • pp.216-220
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    • 2009
  • Aldo-keto reductase family 1 B10 (AKR1B10) has been considered as a potential cancer therapeutic target. Ethanol extracts prepared from 82 Korean local plants were examined for their antioxidant activity and inhibitory effects on recombinant human AKR1B10 (rhAKR1B10) in vitro. 21 extracts showed more than 80% of ABTS radical scavenging activity at $100\;{\mu}g/mL$ and 11 extracts inhibited more than 50% of rhAKR1B10 activity at $10\;{\mu}g/mL$. Especially, 9 extracts showed potent inhibition on rhAKR1B10 activity compared with positive control tetramethylene glutaric acid.

고혈당으로 유도된 제브라피쉬 당뇨망막병증 모델에서 약용식물의 효능 평가 (In vivo Screening of Herbal Extracts on High Glucose-induced Changes in Hyaloid-Retinal Vessels of Zebrafish)

  • 이유리;정승현;이익수;김주환;김영숙;김진숙
    • 생약학회지
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    • 제50권1호
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    • pp.25-31
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    • 2019
  • The zebrafish (Danio rerio) is an established model organism for several pathophysiological conditions which are related to human diseases. In this study, we tested the preventive effect of eight herbal extracts, which show the inhibitory effect of advanced glycation end products (AGEs) or aldose reductase (AR) in our previous study, on high glucose (HG)-induced retinal vessel dilation in larval zebrafish and analyzed the change of hyaloid vasculature. HG-induced zebrafish hyaloid vasculatures were significantly increased in the thickness compared to untreated zebrafish (P<0.001, n=6~10). Eight herbal extracts were found to have significant retinal vessel dilation on the inhibitory activity. Particularly, Brandisia hancei (twigs and fruits), Castanopsis orthacantha (leaves and twigs), Litsea japonica (leaves and twigs), Spenceria ramalana (whole plant), and Synedrella nodiflora (leaves and stems) showed potent inhibitory activity against retinal vessel dilation in HG-induced larval zebrafish.

Biological Activities of Licorice F1 Lines and Content Analysis of Phytochemical Constituents

  • Park, Chun-Geon;Lee, Ah Young;Lee, Jeong Hoon;Lee, Jeong Min;Park, Jun Yeon;Lee, Sang-Hoon;Choi, Ae Jin;Park, Chung Berm;Cho, Eun Ju;Lee, Sanghyun
    • Natural Product Sciences
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    • 제20권3호
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    • pp.137-145
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    • 2014
  • The biological activities of licorice F1 (Glycyrrhiza glabra ${\times}$ G. uralensis) lines (G) were investigated, revealing strong radical scavenging activity targeting 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl (${\cdot}OH$) radicals. At a concentration of $100{\mu}g/mL$, most of the licorice F1 lines scavenged DPPH and ${\cdot}OH$ by more than 80%. Gs-1, -2, and -6 can be considered good scavengers of DPPH radical and G-7 have higher antioxidant activity against ${\cdot}OH$ radical. In addition, licorice F1 lines exerted effective anti-microbial activities against Escherichia coli (Gs-12, -17, and -18) and Staphylococcus aureus (Gs-3, -4, -5, -21, and -26). Moreover, Gs-2, - 20, -31, and -32 effectively inhibited the growth of Helicobacter pylori. Among licorice F1 lines, Gs-25 exhibited high anti-inflammatory effects on nitric oxide produced by lipopolysaccharide- and interferon-${\gamma}$-activated RAW 264.7 cells. Furthermore, Gs-1, -12, and -20 inhibited the growth of AGS human gastric adenocarcinoma cells by more than 60% at a concentration of $100{\mu}g/mL$ and Gs-5, -11, -19, and -32 showed inhibitory effects against rat lens aldose reductase ($IC_{50}$ values, 1.69, 6.07, 6.12, and $4.54{\mu}g/mL$, respectively). The total content of glycyrrhizin (1), glycyrrhetinic acid (2), glabridin (3), and isoliquiritigenin (4) in licorice F1 lines was high in Gs-11, -15, and -30. The present study therefore indicated that Gs-2, -26, -31, and -32 of licorice F1 possessing strong anti-oxidative, anti-microbial, anti-inflammatory, anti-cancer, and aldose reductase inhibitory effects may be used as a possible source material for natural health supplements in the future.

산사 추출물의 항산화 및 항당뇨 활성 (Anti-diabetic and Anti-oxidative Activities of Extracts from Crataegus pinnatifida)

  • 남상명;강일준;신미혜
    • 동아시아식생활학회지
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    • 제25권2호
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    • pp.270-277
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    • 2015
  • 장미과에 속한 낙엽교목인 산사나무의 열매인 산사의 항산화 및 항당뇨 관련 활성을 검토하고, 추출 용매에 따른 차이를 비교하기 위하여 총 페놀 함량, DPPH 라디칼 소거능, ABTS 라디칼 소거능, 최종당화산물 억제능, ${\alpha}$-glucosidase 억제능, aldose reductase 억제능을 측정하였다. 수율은 70% 에탄올 추출물이 33.16%로 가장 높았고, 50% 에탄올 추출물이 27.79%로 그 다음 높았으며, 물, 30% 에탄올, 100% 에탄올은 각각 21.71%, 21.88%, 19.03%를 나타내었다. 총 페놀함량은 50% 에탄올 추출물이 $41.83{\pm}0.07mg$ GAE/g으로 가장 높았고, DPPH와 ABTS 라디칼 소거능도 50% 에탄올 추출물이 각각 $80.79{\pm}0.83%$, $34.92{\pm}0.97%$로 가장 높았다. 최종 당화산물 억제능과 ${\alpha}$-glucosidase 억제능도 50% 에탄올 추출물이 $27.09{\pm}2.27%$$58.87{\pm}0.70%$로 가장 높게 나타난 반면에 AR은 물 추출물이 $30.68{\pm}1.41%$로 가장 높게 나타나면서 상이한 경향을 보였다. 이상의 결과를 종합해 보면, 알코올 농도에 따른 산사의 추출물 중 50% 에탄올 추출물이 천연 항산화제로서 가치가 있으며, 당뇨병 예방을 위한 천연물로서의 가능성도 보였으나 당뇨병 합병증 치료에 대한 효과는 미흡한 것으로 나타났다. 향후 좀 더 다양한 fraction에서의 연구와 in vivo 시험 등을 통한 추가적인 연구가 필요할 것으로 사료된다.

Induction of Cyclin D1 Proteasomal Degradation by Branch Extracts from Abeliophyllum distichum Nakai in Human Colorectal Cancer Cells

  • Park, Gwang Hun;Park, Jae Ho;Jeong, Jin Boo
    • 한국자원식물학회지
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    • 제28권6호
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    • pp.682-689
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    • 2015
  • Abeliophyllum distichum Nakai (A. distichum) has been reported to exert the inhibitory effect on angiotensin converting enzyme and aldose reductase. Recently, our group found that branch extracts of A. distichum (EAFAD-B) induce apoptosis through ATF3 activation in human colon cancer cells. However, anti-cancer reagents exert their activity through the regulation of various molecular targets. Therefore, the elucidation of potential mechanisms of EAFAD-B for anti-cancer activity may be necessary. To elucidate the potential mechanism of EAFAD-B for anti-cancer activity, we evaluated the regulation of cyclin D1 in human colon cancer cells. EAFAD-B decreased cellular accumulation of cyclin D1 protein. However, cyclin D1 mRNA was not changed by EAFAD-B. Inhibition of proteasomal degradation by MG132 attenuated EAFAD-B-mediated cyclin D1 downregulation and the half-life of cyclin D1 was decreased in the cells treated with EAFAD-B. In addition, EAFAD-B induced cyclin D1 phosphorylation at threonine-286 and the point mutation of threonine-286 to alanine attenuated EAFAD-B-mediated cyclin D1 proteasomal degradation. Inhibitions of both ERK1/2 by PD98059 and NF-κB by a selective inhibitor, BAY 11-7082 suppressed cyclin D1 downregulation by EAFAD-B. From these results, we suggest that EAFAD-B-mediated cyclin D1 downregulation may result from proteasomal degradation through its threonine-286 phosphorylation via ERK1/2-dependent NF-κB activation. The current study provides new mechanistic link between EAFAD-B and anti-cancer activity in human colon cancer cells.