• Archives of Pharmacal Research
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• 제25권3호
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• pp.306-312
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• 2002

Aldose reductase, the key enzyme of the polyol pathway, is known to play important roles in the diabetic complication. The inhibitors of aldose reductase, therefore, would be potential agents for the prevention of diabetic complications. To evaluate active principles for the inhibition of aldose reductase from the rhizomes of Belamcanda chinensis, twelve phenolic compounds were isolated and tested for their effects on rat lens aldose reductase. As a result, isoflavones such as tectorigenin, irigenin and their glucosides were found to show a strong aldose reductase inhibition. Tectoridin and tectorigenin, exhibited the highest aldose reductase inhibitory potency, their $IC_{50}$ values, being $1.08{\times}10^{-6}{\;}M{\;}and{\;}1.12{\times}10^{-6}{\;}M$, respectively, for DL-glyceraldehyde as a substrate. Both compounds, when administered orally at 100 mg/kg for 10 consecutive days to streptozotocin-induced diabetic rats, caused a significant inhibition of sorbitol accumulation in the tissues such as lens, sciatic nerves and red blood cells. Tectorigenin showed a stronger inhibitory activity than tectoridin. From these results, it is suggested that tectorigenin is attributed to be a promising compound for the prevention and/or treatment of diabetic complications.

• 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 $1.2{\times}10^{-6}M$.

• Journal of Applied Biological Chemistry
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• 제62권2호
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• pp.203-209
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• 2019

The inhibition of aldose reductase (AR) by the extracts from sixteen noxious and exotic plants was examined. Among them, Aster pilosus showed the highest inhibition of AR ($IC_{50}$ value $0.11{\mu}g/mL$). This study showed that A. pilosus with promising AR-inhibitory activities can be utilized for the development of natural therapies for treating and managing diabetic complications.

• 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.

• Journal of Applied Biological Chemistry
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• 제51권6호
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• pp.302-306
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• 2008

국화과 식물인 민들레, 엉겅퀴, 그리고 고려엉겅퀴를 대상으로 항당뇨 활성 측정 방법 중 하나인 흰쥐 수정체 aldose reductase 저해 활성을 측정하였다. 여러 부위별 추출물 중 민들레 지상부 메탄올 추출물이 $IC_{50}\;8.71\;{\mu}g/mL$로서 뛰어난 저해 활성을 보였다. 국화과 식물에서 분리된 대표적인 화합물인 silymarin과 민들레에서 분리한 luteolin(1)그리고 고려 엉겅퀴에서 분리된 syringin(2)을 대상으로 aldose reductase저해 활성을 측정한 결과 silymarin과 luteolin은 뛰어난 aldose reductase 저해 활성을 보였다.

• Biomolecules & Therapeutics
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• 제10권2호
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• pp.85-88
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• 2002

Systematic fractionation of Angelica gigas roots led to the isolation of linear coumarins such as decursinol angelate, decursin and nodakenin. These compounds were tested for their effects on rat lens aldose reductase. Nodakenin was demonstrated to exhibit significant inhibition of rat lens aldose reductase activity with $IC_{50}$ value of $7.33\Mu\textrm{M}$.

• 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 $2.63\;{\mu}M$.

• Archives of Pharmacal Research
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• 제11권4호
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• pp.312-314
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• 1988

Thirteen monoterpenes were examined for their effects on the bovine lens aldose reductase activity. the monoterpenes tested in this study showed mild inhibitory effects except 3-carene which did not show any significant effect. At the concentration of $10^{-3}$ M(+) Pulegon showed 42% inhibition on lens aldose reductase activity, which is the most otent effect among the tested substance.

• Biomolecules & Therapeutics
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• 제24권2호
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• pp.178-183
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• 2016

Naturally occurring coumarin compounds have received substantial attention due to their pharmaceutical effects. Esculetin is a coumarin derivative and a polyphenol compound that is used in a variety of therapeutic and pharmacological strategies. However, its effect on aldose reductase activity remains poorly understood. In this study, the potential beneficial effects of esculetin on lenticular aldose reductase were investigated in galactose-fed (GAL) rats, an animal model of sugar cataracts. Cataracts were induced in Sprague-Dawley (SD) rats via a 50% galactose diet for 2 weeks, and groups of GAL rats were orally treated with esculetin (10 or 50 mg/kg body weight). In vehicle-treated GAL rats, lens opacification was observed, and swelling and membrane rupture of the lens fiber cells were increased. Additionally, aldose reductase was highly expressed in the lens epithelium and superficial cortical fibers during cataract development in the GAL rats. Esculetin reduced rat lens aldose reductase (RLAR) activity in vitro, and esculetin treatment significantly inhibited lens opacity, as well as morphological alterations, such as swelling, vacuolation and liquefaction of lens fibers, via the inhibition of aldose reductase in the GAL rats. These results indicate that esculetin is a useful treatment for galactose-induced cataracts.

• Natural Product Sciences
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• 제16권4호
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• pp.285-290
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• 2010

The inhibition of rat lens aldose reductase (AR) in vitro using methanol extracts from Korean folk plants was investigated. Among them, the extracts of Saussurea grandifolia and Rumex crispus showed highest inhibition of AR. $IC_{50}$ values of the extracts from S. grandifolia and R. crispus were demonstrated 0.07 and 0.05 mg/ml, respectively. Korean folk plants such as S. grandifolia and R. crispus has a possibility of new natural resources for the inhibition of AR.