• 농업과학연구
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• 제39권2호
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• pp.169-175
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• 2012

To search for the aldose reductase (AR) inhibitors from Korean folk plants, the inhibition of rat lens AR in vitro using the methanol (MeOH) extracts from Korean folk plants was investigated. Among fifty four Korean folk plants tested, the MeOH extract of Cedrela sinensis showed highest inhibition of AR ($IC_{50}$ value, 2.52 ${\mu}g/ml$). The plant C. sinensis has a possibility of new natural resources for the development of AR inhibitor for the prevention of diabetic complications.

• Archives of Pharmacal Research
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• 제29권6호
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• pp.479-483
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• 2006

Eight compounds were isolated from the fruiting bodies of Ganoderma applanatum, and were identified as 2-methoxyfatty acids (1), 5-dihydroergosterol (2), ergosterol peroxide (3) $3{\beta},7{\beta},20,23{\zeta}-tetrahydroxy-11,15-dioxolanosta-8-en-26-oic$ acid (4), $7{\beta},20,23{\zeta}-trihydroxy-3,11,15-trioxolanosta-8-en-26-oic$ acid (5), cerevisterol (6), $7{\beta},23{\zeta}-dihydroxy-3,11,15-trioxolanosta-8,20E(22)-dien-26-oic$ acid (7), and $7{\beta}-hydroxy-3,11,15,23-tetraoxolanosta-8,20E(22)-dien-26-oic$ acid methyl ester (8) by spectral analysis. All compounds were isolated for the first time from this fruiting bodies, and their effect on rat lens aldose reductase (RLAR) activity was tested. Among these eight compounds, ergosterol peroxide (3) was found to exhibit potent RLAR inhibition, its $IC_{50}$ value being $15.4\;{\mu}g/mL$.

• The Korean Journal of Physiology and Pharmacology
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• 제5권3호
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• pp.271-278
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• 2001

Oxidative stress and methylglyoxal (MG), a reactive dicarbonyl metabolites produced by enzymatic and non-enzymatic reaction of normal metabolism, induced aldose reductase (AR) expression in rat aortic smooth muscle cells (SMC). AR expression was induced in a time-dependent manner and reached at a maximum of 4.5-fold in 12 h of MG treatment. This effect of MG was completely abolished by cyclohemide and actinomycin D treatment suggesting AR was synthesized by de novo pathway. Pretreatment of the SMC with N-acetyl-L-cysteine significantly down-regulated the MG-induced AR mRNA. Furthermore, DL-Buthionine-(S,R)-sulfoximine, a reagent which depletes intracellular glutathione levels, increased the levels of MG-induced AR mRNA. These results indicated that MG induces AR mRNA by increasing the intracellular peroxide levels. Aminoguanidine, a scanvenger of dicarbonyl, significantly down-regulated the MG-induced AR mRNA. In addition, the inhibition of AR activities with statil, an AR inhibitor, enhanced the cytotoxic effect of MG on SMC under normal glucose, suggesting a protective role of AR against MG-induced cell damages. These results imply that the induction of AR by MG may contribute to an important cellular detoxification of reactive aldehyde compounds generated under oxidative stress in extrahepatic tissues.

• Journal of Applied Biological Chemistry
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• 제49권1호
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• pp.24-27
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• 2006

Four ursane-type triterpenoids, 2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-4(23),12-dien-28-oic acid (1), 4(R),23-epoxy-2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-12-en-28-oic acid (2), myrianthic acid (3), and tormentic acid (4), and a phenolic compound, ethyl gallate (5), from an EtOAc-soluble extract of the stems of Rumex japonicus, were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) and rat lens aldose reductase (RLAR) inhibitory activity. Compounds 1 and 5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ value of 87 ${\mu}M$ and on RLAR with $IC_{50}$ value of 14.3 ${\mu}M$, respectively. Ethyl gallate (5) was isolated for the first time from this plant.

• Natural Product Sciences
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• 제13권2호
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• pp.160-163
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• 2007

Four glycosides, rosamultin (1), tetracentronside B (2), 4-O-methylellagic acid 3-O-${\alpha}$-$_L$-rhamnopyranoside (3), and vanillic acid 4-O-${\beta}$-$_L$-glucopyranoside (4), isolated from the roots extract of Potentilla discolor, were subjected to in vitro bioassays to evaluate the inhibitory activity on advanced glycation end products (AGEs) formation and rat lens aldose reductase (RLAR). Compound 3 exhibited a significant inhibitory activity against both AGEs formation and RLAR with IC$_{50}$ values of 79.5 and 8.03 ${\mu}$M, respectively. All the compounds (1-4) were isolated for the first time from this plant.

• 한국약용작물학회지
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• 제18권5호
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• pp.305-310
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• 2010

Taxifolin-3-O-$\beta$-D-xylopyranoside and quercetin-3-O-$\alpha$-L-rhamnopyranoside were isolated from an EtOAc-soluble extract of the leaves of Chamaecyparis obtuse. Quercetin-3-O-$\alpha$-L-rhamnopyranoside was found to possess a potent inhibitory activity of human recombinant aldose reductase in vitro, its $IC_{50}$ value being $11.5\;{\mu}M$. Kinetic analysis showed that quercetin-3-O-$\alpha$-L-rhamnopyranoside exhibited uncompetitive inhibition against DL-glyceraldehyde. Also, quercetin-3-O-$\alpha$-L-rhamnopyranoside suppresses sorbitol accumulation in rat lens under high glucose conditions, demonstrating the potential to prevent sorbitol accumulation in vivo. These results suggest that this compound may be a promising agent in the prevention or treatment of diabetic complications.

• Horticulture, Environment, and Biotechnology : HEB
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• 제59권6호
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• pp.899-907
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• 2018

The methanol extracts of flowers obtained from 67 plant species were screened for their inhibitory activity on aldose reductase (AR). Alnus japonica, Aster spathulifolius, Chionanthus retusus, Morus bombycis, Crysanthemum boreale, Persicaria tinctoria, Platycarya strobilacea, and Serratula coronata var. insularis exhibited potent aldose reductase inhibitory (ARI) activity. HPLC-UV analysis of quercetin, an AR inhibitory flavonoid, was performed on extracts showing strong ARI activity. Quercetin was detected in C. retusus, C. boreale, P. tinctoria, and S. coronata var. insularis at concentrations of 1.33, 1.56, 0.82, and $3.37mg\;g^{-1}$ extract, respectively, indicating that quercetin contributed to the ARI activity of these extracts. In the samples in which quercetin was absent, other compounds may be responsible for their potent ARI activity. These results serve as a basis for further studies regarding the bioactive components responsible for the inhibitory effects of various flower extracts on AR activity.

• KSBB Journal
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• 제23권5호
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• pp.419-424
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• 2008

본 연구에서 당뇨병의 예방, 치료제 및 건강기능 식품으로서 산업적 활용가능성을 평가하기 위한 기초연구로서 번행초 추출물을 사용하여 당뇨관련 효소인 $\alpha$-amylase, $\alpha$-glucosidase, $\beta$-glucosidase 그리고 aldose reductase에 대한 저해활성을 조사하였다. 번행초의 HX 분획물은 인간 타액, 돼지 췌장 $\alpha$-amylase에 대해 5 mg/mL 농도에서 각각 62.23%, 88.74%로 높은 저해효과를 나타냈으며, $\alpha$-glucosidase에 대해서도 HX 분획물이 1 mg/mL 농도에서 60.27%로 높은 저해효과를 나타냄으로써 현재 혈당강하제로 사용되고 있는 acarbose와 1-deoxynorjirimycin보다 높은 억제 효과를 보였다. 그리고 만성 합병증에 의한 시력장애, 신경성장애, 신장기능장애, 심장기능 장애 등의 심각한 당뇨병성 합병증 유발과 관련이 있는 aldose reductase에 대한 억제활성을 조사한 결과, 1 mg/mL 농도에서 번행초 DCM 분획과 HX 분획물이 각각 51.95%, 47.22%로 높은 저해활성을 나타냄으로써 당뇨병과 그로 인한 합병증의 예방에도 효과가 있는 것으로 판단된다. 전 세계적으로 당뇨병 환자가 증가추세에 있어 당뇨병 치료제의 시장 규모는 더욱 확대될 가능성이 높은 가운데 지금까지 보고되지 않은 번행초의 항당뇨 효능의 우수성을 검증함으로써 바이오산업육성뿐만 아니라 신소득 작물로 순화재배를 통한 농가소득 향상에도 기여할 것으로 기대된다.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.261.1-261.1
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• 2003

The EtOAc and CH$_2$Cl$_2$ soluble fractions from the fruit body of Ganoderma applanatum showed strong aldose reductase inhibitory activity. Nine compounds were isolated from both fractions. They were identified by spectral data as D-mannitol (1), 2-methoxyfatty acid (2), cerebrosides [(2S,3R,4E,8E)-1-O-${\beta}$-D-glucopyranosyl-3-hydroxy-2-[(R)-2'-hydroxypalmitoyl]amino-9-methyl-4,8-octadecadiene] (3), daucosterol (4), 2,5-dihydroxybenzoic acid (5), protocatechualdehyde (6), 5-dihydroergosterol (7), ergosterol peroxide (8), and cerevisterol (9). (omitted)

• 한국약용작물학회:학술대회논문집
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• 한국약용작물학회 2011년도 추계학술발표회
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• pp.272-273
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• 2011