• Journal of Ginseng Research
• /
• v.20 no.1
• /
• pp.106-110
• /
• 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.

• Biomolecules & Therapeutics
• /
• v.10 no.2
• /
• pp.85-88
• /
• 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 $7.33\Mu\textrm{M}$.

• Archives of Pharmacal Research
• /
• v.11 no.4
• /
• pp.312-314
• /
• 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.

• Natural Product Sciences
• /
• v.22 no.2
• /
• pp.102-106
• /
• 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.

• Biomolecules & Therapeutics
• /
• v.24 no.2
• /
• pp.178-183
• /
• 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
• /
• v.9 no.1
• /
• pp.4-6
• /
• 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 $2.63\;{\mu}M$.

• ALGAE
• /
• v.19 no.4
• /
• pp.349-352
• /
• 2004

We examined MeOH extracts of the marine plants from Korea for their inhibitory activities on rat lens aldose reductase in vitro. Among the MeOH extracts tested, the extracts of Enteromorpha prolifera, Ecklonia cava, Pelvetia siliquosa and Salicornia herbacea exhibited a rat lens aldose reductase inhibition (IC$_{50}$: 3.04, 8.84, 11.42 and 4.99 $\mu$g-ml$^{-1}$, respectively) in vitro.

• Archives of Pharmacal Research
• /
• v.25 no.3
• /
• pp.306-312
• /
• 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.

• YAKHAK HOEJI
• /
• v.48 no.5
• /
• pp.291-296
• /
• 2004

Sparganium stoloniferum Buch.-Ham. (Sparganiaceae) is a perennial herb which has been used as treatments for menstrual disorder, galactagogue and endometriosis in folk remedies. The Sparganii Rhizoma processed, heated with vinegar, used to different purpose compared with origin in medicine. In order to estimate the different effects between processed (PSR) and unprocessed (USR) Sparganii Rhizoma, extraction and systemic fractionation of the rhizomes were archived. Inhibitory effects of the extracts as well as the fractions of PSR and USR on rat lens aldose reductase and on rat platelet aggregation were investigated for the prevention or the treatment of chronic diabetic complications. Their antioxidant effects, measured using lipid peroxidation of liver tissue and radical scavenging activities on 1,1-diphenyl-picrylhydrazyl in vitro, were evaluated. The most of biological activities tested except rat platelet aggregation, fractions from PSR were shown to exhibit stronger activities than those from USR. It seems that caused by changing of the chemical components by heating process in conditioned with acetic acid. Compounds isolated were shown to significant inhibitory activity on rat lens aldose reductase. Inhibitory activity of compounds isolated on rat lens aldose reductase have been tested in vitro. $IC_{50}$/ (6.31 $\mu$M) of cerebroside I (V) was nearly equal to that (6.32 $\mu$M) of a reference compound, tetrametbylene glutaric acid (TMG).

• Bulletin of the Korean Chemical Society
• /
• v.25 no.12
• /
• pp.1874-1876
• /
• 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.