• 대한약학회:학술대회논문집
• /
• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
• /
• pp.209.3-210
• /
• 2000

• 농업과학연구
• /
• 제39권1호
• /
• pp.69-73
• /
• 2012

The purpose of this study was to evaluate the potential of naturally occurring aldose reductase (AR) inhibitors from white-color natural products (Aruncus dioicus var. kamtschaticus, Chionanthus retusa, Cosmos bipinnatus, Hibiscus syriacus, Hydrangea paniculata, Magnolia denudata, Prunus padus, Robinia pseudo-accacia, Rhododendron mucronulatum for. albiflorum, Spiraea blumei, and Spiraea prunifolia var. simpliciflora). The MeOH extract of white-color natural products were tested on rat lens AR inhibition in vitro. Among them, the MeOH extract of R. mucronulatum for. albiflorum showed highest inhibition on AR ($IC_{50}$ value, 1.07 ${\mu}g/ml$). These results suggested that R. mucronulatum for. albiflorum, a white-color natural product, could be a useful resource in the development of a novel AR inhibitory agent against diabetic complications.

• Journal of Applied Biological Chemistry
• /
• 제60권1호
• /
• pp.29-33
• /
• 2017

The methanol extract of Rhododendron mucronulatum for. albiflorum (RMFA) stems inhibited aldose reductase (AR) activity. The RMFA fractions obtained by stepwise extraction with solvents of different polarity were tested for AR inhibition in vitro using the lens of a rat. Among them, the ethyl acetate (EtOAc) fraction inhibited AR more than the other fractions. Quercetin (1) from the EtOAc fraction showed a high AR inhibition with $IC_{50}$ of $2.11{\mu}M$. The stems of RMFA contained the highest amount (5.12 mg/g extract) of quercetin. Our results suggest that RMFA, which contained quercetin, could be a useful material for the development of supplementary functional foods.

• 농업과학연구
• /
• 제40권1호
• /
• pp.47-51
• /
• 2013

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 in Chungcheong Province was investigated. Among Korean folk plants tested, the MeOH extract of Persicaria longiseta showed highest inhibition of AR ($IC_{50}$ value, $5.14{\mu}g/ml$). Consequently, P. longiseta has a possibility of new natural resources for the development of AR inhibitor for the prevention of diabetic complications.

• Archives of Pharmacal Research
• /
• 제18권2호
• /
• pp.65-68
• /
• 1995

The methanol extract from the whole parts of the flowers of Chrysanthemum boreals was found to exhibit a significant inhibition of a rat lens aldose reductase (RLAR) activity in vitro. Bioassay guided systematic fractionation of the methanol extract led to the isolation of four flavonoids which were identified as acacetin (1), apigenin (II), luteolin (III) and linarin (IV). Compounds I-III were demonstrated to exhibit a significant inhibition of RLAR. Luteolin (II) was found to be the most potent AR inhibitor with $IC_{50}$ value of $5{\times}10^{-7}M$.

• Journal of Applied Biological Chemistry
• /
• 제51권1호
• /
• pp.13-16
• /
• 2008

Five anthraquinones, emodin (1), ${\omega}$-hydroxyemodin (2), chrysophanol-8-O-${\beta}$-D-glucoside (3), emodin-8-O-${\beta}$-D-glucoside (4), and physcion-8-O-${\beta}$-D-glucoside (5), and five flavonoids, kaempferol-3-O-${\beta}$-D-glucoside (6), quercetin (7), quercitrin (8), isoquercitrin (9), and (+)-catechin (10), were isolated from the EtOAc-soluble extract of the fruits of Rumex japonicus. The structures of 1-10 were identified by spectroscopic methods including NMR studies. This is the first report on the isolation of compounds 3-5 from this plant. The isolates were subjected to in vitro bioassays to evaluate their inhibitory activities on the rat lens aldose reductase (RLAR), among which two anthraquinones (1 and 4), and five flavonols (5-9) showed significant activities on RLAR.

• Natural Product Sciences
• /
• 제12권4호
• /
• pp.210-213
• /
• 2006

A 4,5-dioxoaporphine type alkaloid, cepharadione B (1), a phenolic acid, protocatechuic acid (2), and flavonols, quercetin (3), afzelin (4), and quercitrin (5), were isolated from the EtOAc-soluble extract of the whole plants of Houttuynia cordata. All the isolates (1-5) were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) formation and rat lens aldose reductase (RLAR) inhibitory activity. The three flavonols 3-5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ values of 66.9, 58.9, and $32.3{\mu}M$, respectively. While the two flavonol rhamnosides 4 and 5 showed a remarkable inhibitory activity against RLAR with $IC_{50}$ values of 0.81 and $0.16{\mu}M$, respectively.

• 농업과학연구
• /
• 제39권2호
• /
• pp.169-175
• /
• 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
• /
• 제29권6호
• /
• pp.479-483
• /
• 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 $15.4\;{\mu}g/mL$.

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