• 생약학회지
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• 제25권1호
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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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• 제9권3호
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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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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• 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.

• Applied Biological Chemistry
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• 제17권2호
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• pp.93-116
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• 1974

토양(土壤), 퇴비(堆肥), 사료(飼料)로부터 세포내지질(細胞內脂質)을 다량생산(多臺生産)하는 효모(酵母)로서 Rhodotorula glutinis var. glutinis SW-17을 선발(選拔)하였고 또 식물엽(植物葉)에서 세포외(細胞外) 지질(脂質)을 다량생산(多量生産)하는 2균주(菌株)의 효모(酵母) Rhodotorula glutinis var. glutinis SW-5 및 Rhodotorula graminis SW-54를 분리동정(分離同定)하여 그들의 세포내외(細胞內外) 지질생산(脂質生産)에 관(關)한 기초적(基礎約)인 연구(硏究)를 한바 다음과 같은 결과(結果)를 얻었다. 1) $24^{\circ}C$에서 8일간(日間) 진탕 배양(培養)할때 균체증식후(菌體增殖後) 질소성분(蜜素成分)이 어느정도(程度) 소모(消耗)되었을 때부터 지방(脂肪)의 생성(生成)이 시작되었으며 이때 Rhodotorula glutinis var. glutinis SW-17은 세포내지질(細胞內脂質)을 효모건체(酵母乾體)에 대하여 최고(最高) 58.42%까지 그리고 Rhodotorula graminis SW-54는 세포외(細胞外) 지질(脂質)을 2.62g/l까지 생산(生産)하였다. 2) 배양액중(培養液中)의 탄소원(炭素源)과 질소원(窒素源)이 $4{\sim}5$일(日)에 전부(全部) 소모(消耗)된 후 기아상태(飢餓狀態)에서 $24^{\circ}C$로 계속 진탕배양하면 효모세포(酵母細胞)는 세포내외(細胞內外) 지질(脂質)을 다시 이용(利用)하여 배양(培養) 90일경(日頃)에는 지질(脂質)이 완전(完全) 소모(消耗)되었다. 3) 세포내외(細胞內外) 지질(脂質)의 생함성(生合成)은 탄소원(炭素源)과 질소원(窒素源)의 상대적(相對約)인 농도(濃度)와 밀접(密接)한 관계(關係)가 있어서 질소(窒素)가 효모증식(酵母增殖)에 전부 이용(利用)되어 질소(窒素) 기아상태(飢餓狀態)에서 과잉(過剩)의 탄소원(炭素源)이 있을때 지질(脂質)이 현저하게 생성(生成)되었다. 반대(反對)로 배양액내(培養液內)의 질소농도(室素濃度)를 증가(增加)시키면 지질생산량(脂質生産量)은 현저하게 저하 되었다. 4) 본분리선정(本分離選定)된 효모균주(酵母菌株)의 배양(培養) 및 지질생성(脂質生成) 최적(最適) pH는 $5.0{\sim}6.0$이었다. 5) 본분리선정(本分離選定)된 효모균주(酵母菌株)의 세포내(細胞內) 지질(脂質)은 myristic, palmitic, palmitoleic, stearic, oleic, linoleic 및 linolenic acid로 구성(構成)되었으며 이중(中) palmitic acid $30{\sim}45%$, oleic acid가 $35{\sim}50%$로 가장 많았다. 6) 본분리(本分離) 선정(選定)된 효모균주(酵母菌株)의 세포회(細胞外) 지질(脂質)의 구성지방산(構成脂肪酸)은 myristic, palmitic, stearic, oleic, linoleic, linolenic, 3-D-hydroxypalmitic 및 3-D-hydroxystearic acid로 구성(構成)되었으며 이중(中) 3-D-hydroxypalmitic acid가 22${\sim}$25%, 3-D-hydroxy-stearic acid가 13${\sim}$17%로 가장 많았다. 7) 본분리선정(本分離選定)된 효모균주(酵母菌株)의 세포내(細胞內) 지질(脂質) 구성(構成) polyol은 glycerol뿐이 었으며 세포외(細胞外) 지질(脂質)의 구성(構成) polyol은 glycerol, mannitol, xylitol 및 arabitol 이었다.