• Food Science and Biotechnology
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• 제14권3호
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• pp.344-349
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• 2005

Aldose reductase catalyzes the conversion of glucose into sorbitol. Inhibiting this enzyme in diabetes mellitus can delay or prevent pathogenic process. Aldose reductase inhibitor was screened from Korean fermented soybean pastes (Doen-jang) and purified via sequential processes of ethanol extraction, HP-20 column chromatography, ethyl acetate extraction, silica gel column chromatography, and crystallization. Aldose reductase inhibitor was identified as genistein with molecular weight of 270 Da and molecular formula of $C_{15}H_{10}O_5$ based on UV spectrometry, $^1H$ and $^{13}C\;NMRs$, and mass spectrometry. Genistein inhibited aldose reductase of pig lens with $IC_{50}$ level of $20\;{\mu}M$. Because genistein was effective against aldose reductase of animal source, it may be a potential therapeutic agent for diabetic complications.

• Journal of Ginseng Research
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• 제20권1호
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• pp.106-110
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• 1996

The present study was undertaken to elucidate the effects of ginseng components on rat lens aldose reductase activity. Ginseng total saponin (GTS) exhibited inhibitory activities on rat lens aldose reductase in a dose-dependent manner. Among ginsenosides, Rf and Rgl showed potent inhibitory activities on rat lens aldose reductase. Lipid soluble fraction also inhibited rat lens aldose reductase activities. These data suggest that ginseng components inhibit rat lens aldose reductase activity in vitro.

• Natural Product Sciences
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• 제9권1호
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• pp.4-6
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• 2003

Hyperin from the leaves of Acanthopanax senticosus was tested for its effect on rat lens aldose reductase and demonstrated to exhibit a significant inhibition of rat lens aldose reductase activity with $IC_{50}$ value of $2.63\;{\mu}M$.

• 생약학회지
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• 제24권1호
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• pp.58-62
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• 1993

To search for inhibitory activities for lens aldose reductase, twenty two medicinal plants were tested by the method of bovine lens aldose reductase inhibition test. In this test Rubia akane(68%), Artemisia selengensis(61%), Lespedeza cuneata (58%), Ligustrum lucidum(58%), Viola patrinii(58%) extracts were shown to have aldose reductase inhibitory activity. From the radix of Rubia akane, $2-methyl-1,\;3,\;6-trihydroxy-9,\;10-anthraquinone-3-O-(6'-O-acetyl)-{\alpha}-rhamnosyl-(1{\rightarrow}2)-{\beta}-D-glucoside$ was isolated and the $IC_{50}$ of this compound in the aldose reductase inhibition test was about $1.2{\times}10^{-6}M$.

• Natural Product Sciences
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• 제22권2호
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• pp.102-106
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• 2016

A methanolic extract of Corydalis ternata having aldose reductase inhibitory activity was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. Seven alkaloids, tetrahydrocoptisine (1), corydaline (2), tetrahydropalmatine (3), isocorybulbine (4), corybulbine (5), dehydrocorydaline (6), and N-methyltetrahydroberbinium (7) were isolated from $CHCl_3$ fraction of C. ternata methanol extract. Among them, compounds 1, 5, and 7 exhibited $5.04{\pm}1.97%$, $5.00{\pm}1.26%$, and $1.80{\pm}2.33%$ inhibitions, respectively at $40{\mu}M$. The activities of the single compounds were not comparable to that of the whole extract, suggesting that the whole combination of each single compound was responsible for the activity of the extract as shown in many cases of natural medicines. Even though this is the second report on aldose reductase inhibition activity of C. ternata, recombinant human aldose reductase was employed in this study unlike in the previous report. Furthermore, the aldose reductase inhibitory activities of isocorybulbine, corybulbine, and N-methyltetrahydroberbinium, to the best of our knowledge, were evaluated for the first time in this study. These results suggest a use of the extract of C. ternata for ameliorating diabetic complications.

• 생약학회지
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• 제32권3호통권126호
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• pp.248-252
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• 2001

The present study was undertaken to elucidate the hypoglycemic effect and inhibitory effect of Cudrania tricuspidata root bark on aldose reductase activity. C. tricuspidata MeOH ext. 1,000 mg/kg showed a significant blood glucose lowering effect on alloxan-induced hyperglycemic rats and increasing body weight. C. tricuspidata MeOH ext. showed a potent inhibitory effect on bovine lens aldose reductase.

• 생약학회지
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• 제42권2호
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• pp.187-194
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• 2011

Aldose reductase (AR), the key enzyme in the polyol pathway, plays an important role in the development of the diabetic complications. None of Aldose reductase Inhibitor (ARI) has achieved worldwide use because of limited efficacy or undesirable side effects. Therefore, evaluating natural sources for ARI potential may lead to the development of safer and more effective agents against diabetic complications. Fifty two Chinese herbal medicines have been investigated for inhibitory activities on AR. Among them, twelve herbal medicines, Artemisia anomala (aerial part), Centella asiatica (aerial part), Scutellaria baicalensis (root), Senecio chrysanthermoides (whole plant), Gleditsia japonica (twig), Zizyphus jujube (twig, leaf), Citrus aurantium (fruit), Hydnocarpus anthelmintica (fruit), Potaninia mongolica (aerial part), Tribulus terrestris (fruit), Artemisia apiacea (aerial part) and Eclipta prostrate (aerial part) exhibited a significant inhibitory activity against AR. Particularly, Artemisia anomala, Centella asiatica and Scutellaria baicalensis showed four times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

• Bulletin of the Korean Chemical Society
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• 제25권12호
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• pp.1874-1876
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• 2004

Quantitative structure activity relationship has been probed for spirosuccinimide-fused tetrahydropyrrolo[1,2-a]pyrazine-1,3-dione derivatives acting as aldose reductase inhibitors. While the spirosuccinimide compounds contain a chiral center, the aldose reductase inhibition assay was performed with racemic mixtures in the published work. As the physicochemical descriptors of the QSAR analysis must be evaluated for a definite molecular structure, we devise a new 'racemic' descriptor as the arithmetic mean of the (R)-enantiomer descriptor and the (S)-enantiomer descriptor. The resultant QSAR model derived from the racemic descriptors outperforms the original QSAR models, closely reproducing the observed activity of optically pure enantiomers as well as racemic mixtures.

• 생약학회지
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• 제44권2호
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• pp.168-175
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• 2013

Aldose reductase (AR) plays a central role in the development of the diabetic complications. Eighty one Korean herbal medicines have been investigated for inhibitory activities on AR. Among them, fourteen herbal medicines exhibited a significant inhibitory activity compared with 3,3-tetramethyleneglutaric acid (TMG) as positive control. Particularly, Xanthium strumarium (fruit, whole plant), Ilex cornuta (stem and leaf), Vitex rotundifolia(stem), Sophora flavescens (whole plant), Platycarya stobilacea (flower) showed two times more potent inhibitory activity than 3,3-tetramethyleneglutaric acid (TMG).

• 생약학회지
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• 제45권4호
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• pp.354-358
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• 2014

Aldose reductase (AR) has been demonstrated to play important role in the development of the diabetic complications such as diabetic retinopathy, diabetic neuropathy and diabetic nephropathy. To discover novel treatments for diabetic complications from natural sources, 69 Korean herbal medicines have been investigated for inhibitory activities on AR. Among them, 7 herbal medicines, Eleutherococcus sessiliflorus (stems), Artemisia japonica (whole plants), Wisteria floribunda (leaves), Eurya japonica (stems, twigs and leaves, leaves), Ampelopsis brevipedunculata (stems) exhibited a significant inhibitory activity compared with 3,3-tetramethyleneglutaric acid as positive control.