• Korean Journal of Pharmacognosy
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• v.25 no.1
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• pp.41-46
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• 1994

The ether, ethylacetate and n-butanol soluble fractions from the roots of Scutellaria baicalensis showed a significant inhibition of lens aldose reductase (AR) activity in vitro. During systematic fractionation of the active fractions, 7 flavonoids were isolated and compared their inhibitory activities against rat AR using DL-glyceraldehyde as a substrate, among which baicalin (VII) was found to exhibit the most potent inhibitory activity. Baicalin (VII) and wogonin-7-O-glucuronide (VI), with repeated treatments (30 mg/kg/day, i.p.) throughout the experimental periods caused a significant suppression of cataract formation induced by galactose (40 g/kg/day) as well as the decrease of galactitol accumulation in the rat lens. The flavonoids also exhibited a significant inhibition of sorbitol accumulation in the lenses of diabetic rats induced by streptozotocin (STZ).

• Advances in Traditional Medicine
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• v.9 no.3
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• pp.245-251
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• 2009

Aldose reductase (AR) has been reported to play an important role in sugar-induced cataract. In the present study, the AR inhibitory activity of Enicostemma hyssopifolium (EH), Gymnema sylvestre, Eclipta alba, and Tinospora cordifolia (TC) were studied along with their effect on sugar-induced cataractogenic changes in sheep lenses in vitro. AR inhibitory activity of the aqueous extracts of plants and their anticataract potentials were evaluated in vitro in sheep lenses, considering the activity of normal sheep lenses as 100%. The concentration of the plant extract that showed maximum activity was selected to further study its effect on galactose-induced polyol accumulation in vitro. The $IC_50$ values of EH and TC were calculated to be 102 and 85 ${\mu}g$/ml, respectively. EH showed a significant inhibition (61.3%) in polyol accumulation followed by TC (53.1%). EH and TC possesses a significant anticataract activity in vitro and its anticataract potential could be related with its AR inhibitory effect.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.184-184
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• 1998

Aldose reductase(AR), a rate-limiting enzyme in the polyol pathway, has been demonstrated to cause the intracellular accumulation of sorbitol or galactitol and hence to play key roles not only in the cataract formation in the lens but also in the pathogenesis of diabetic complications such as neuropathy, retinopathy and nephropathy, etc. In a series of investigations to evaluate potential AR inhibitors from medicinal plants, we have shown that some hot water extracts exhibited a significant inhibition of a significant inhibition of bovine lens AR in vitro. Among active plants, the roots of Angelica dahuria (Umbelliferae) were shown to have relatively potent AR inhibitory activity. Systematic fractionation of the ether soluble fraction monitored by bioassay led to isolation of two furanocoumarins, byakangelicin(I) and ter-O-methyl byakangelicin( II), were identified as potential AR inhibitors, their $IC_{50}$ values being 6.2 M and 2.8 M, respectively.

• Archives of Pharmacal Research
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• v.25 no.3
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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.

• Applied Biological Chemistry
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• v.17 no.2
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• pp.93-116
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• 1974

A potent intracellular-lipid-producing yeast, Rhodotorula glutinis var. glutinis SW-17, was screened out from a variety of arable soils, compost heaps, and fodders, and two strains of excellent extracellular-lipid-producing yeasts, Rhodotorula glutinis var. glutinis SW-5 and Rhodotorula graminis SW-54, were screened out from the surface of many species of leaves. And then the intra- and extra-cellular lipid productions by those Rhodotorula yeasts were studied. The results were as follows: 1. During the shaking culture of 8 days at $24^{\circ}C$, both the intra- and extra-cellular lipid accumulation started almost at the stationary phase of growth, when the nitrogen source in the medium was a little more than half used up. The intracellular lipid production by Rhodotorula glutinis var. glutinis SW-17 reached 58.42% (w/w) of dried yeast, and the extracellular lipid production by Rhodotorula graminis SW-54 amounted to 2.62g per liter of the medium. 2. After the carbon and nitrogen sources in the medium were almost consumed, if the yeasts were shake-cultured further in a state of starvation, the yeast cells re-utilized the already produced intra- and extra-cellular lipids and the lipids completely disappeared in the medium in about 90 days. 3. The relative concentration of carbon and nitrogen sources in the media greatly influenced both the intra- and extra-cellular lipid production. When the nitrogen source in the medium was almost used up for the growth of yeast, and excess carbon sources were still available, the lipid production vigorously proceeded. As long as the nitrogen source concentration in the medium was high, the lipid production was greatly suppressed. 4. The optimum pH for both the intra- and extra-cellular lipid production by those yeasts was pH 5.0-6.0. 5. The fatty acid components of the intracellular lipid of Rhodotorula glutinis var. glutinis SW-17 were myristic, palmitic, palmitoleic, stearic, oleic, linoleic, and linolenic acids. The largest components of the fatty acids were palmitic acid equivalent to 30-45% of the whole fatty acids and oleic acid equivalent to 35-50%. 6. The fatty acid components of the extracellular lipid of Rhodotorula glutinis var. glutinis SW-5 and Rhodotorula graminis SW-54 were myristic, palmitic, stearic, oleic, linoleic, linolenic, 3-D-hydroxypalmitic, and 3-D-hydroxystearic acids. The largest components of the fatty acids were 3-D-hydroxypalmitic acid equivalent to 22-25% of the acids and 3-D-hydroxystearic acid equivalent to 13-17%. 7. The polyol component of the intracellular lipids was only glycerol, whereas the polyols of extracellular lipids were glycerol, mannitol, xylitol and arabitol.