• 생약학회지
• /
• 제41권4호
• /
• pp.289-296
• /
• 2010

Aldose reductase (AR), the principal enzyme of the polyol pathway, has been shown to play an important role in the development of the diabetic complications. Evaluating natural sources for ARI potential may lead to the development of safer and more effective agents against diabetic complications. Sixty four Chinese herbal medicines have been investigated for inhibitory activities on AR. Among them, thirteen herbal medicines, Inula helianthus-aquatilis C. Y. Wu ex Ling. (whole plant), Erigeron breviscapus (Vant.) Hand. Mazz. (whole plant), Lonicera hypoglauca Miq. (leaf, stem), Scutellaria orthocalyx Hang. Mazz. (whole plant), Berchemia floribunda Brongn. (leaf, stem), Michelia alba DC. (flower), Oroxylum indicum (seed), Punica granatum L. (peel), Elsholtzia capituligera (whole plant), Trachelospermum jasminoides (Lindl.) Lem. (whole plant), Elsholtzia strobilifera Benth. (whole plant), Agrimonia pilosa var. nepalensis (D. Don) Nakai (whole plant) and Aster poliothamnus Diels (whole plant) exhibited a significant inhibitory activity against AR. Particularly, Inula helianthus-aquatilis C. Y. Wu ex Ling. showed seven times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

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

• 한국자원식물학회:학술대회논문집
• /
• 한국자원식물학회 2018년도 춘계학술발표회
• /
• pp.62-62
• /
• 2018

Inhibition of aldose reductase (AR) has been shown to prevent the onset and progression of many diabetic complications wherein several AR inhibitors were isolated from plants abundant in polyphenolic compounds. Lespedeza cuneata (Fabaceae), a perennial plant indigenous in East Asian countries, is shown to be abundant in these polyphenolic substances such as flavonoids and tannins. However, there are no studies to date regarding its effects on AR. In this study, the inhibitory activity of the methanol extract and stepwise polarity fractions of Lespedeza cuneata on AR was investigated. The bioactive compounds purified from L. cuneata by repeated column chromatography were also tested for AR inhibition. Results show that the ethyl acetate and n-butanol fractions of L. cuneata exhibited potent inhibition against AR with $IC_{50}$ values of 0.57 and $0.49{\mu}g/mL$, respectively. Further analysis led to the isolation of acacetin (1), afzelin (2), astragalin (3), kaempferol (4), and scutellarein 7-O-glucoside (5). The AR inhibitory effects these five compounds were also determined in which compounds 2, 3, and 5 showed potent AR inhibitory effects with $IC_{50}$ values of 2.20, 1.91, and $12.87{\mu}M$, respectively. Quantitative analysis of astragalin (3) by HPLC-UV was also performed in the leaves and roots of L. cuneata (0.626 and 0.671 mg/g, respectively). This study reports that the flavonoids isolated from L. cuneata show promising AR inhibitory activities which can be further developed as natural therapies for treating and managing diabetic complications.

• Archives of Pharmacal Research
• /
• 제17권5호
• /
• pp.331-336
• /
• 1994

The ether extract from the roots of angelica clahurica was found to inhibit bovine lens aldose reductase (BLAR0 activity in vitro by 100% at 100.mu.g/ml. Systematic fractionation of the ether soluble fraction and subsequent active frctions monitorede by bioassy led to isolation of four furanocoumarins, isoimperatorin (I0, imperatorin (II), ter-O-methyl byakangelicin (III) and byakangelicin (IV), among which compound III and IV were identified as potential AR inhibitors, their $IC_{50}$ values being $2.8{\mu}M{\;}and{\;}6.2{\mu}M$, respectively. Galactosemic cataract formation tors, in rats treated with 40 g/kg/day of galactose was blocked almost completely throughout the exeprimental periods up to 44 days by i.p. administrations of byakangelicin (IV) at 50 mg/kg/day. In coincidence with the inhibitory action on cataract formation, the galactitol accumulation in rats treated with byakangelicin (IV) was found to be markedly prevented by approximately 80.5% compared to those of the contro. These results indicate that byakangelicin (IV), as a main principle of this plant, possesses high potential for a clinically useful drug of the future which prevents and/or improves sugar cataract as well as diabetic complications.

• 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.

• 생명과학회지
• /
• 제18권7호
• /
• pp.1005-1010
• /
• 2008

최근 당뇨병 환자가 급속히 증가하고 있으나, 지속적이고 적절한 치료가 어려워 당뇨병성 합병증의 발생을 증가시키고 있다. 당뇨병 발병 이후의 치료는 완치가 거의 불가능하기 때문에 증상을 개선시키고 급만성 합병증을 막는 이차적 예방에 중점을 두고 있다. 따라서 항당뇨 활성을 가지면서 식용 가능한 천연자원의 개발이 절실히 필요하다. 본 연구에서 약용식물로 알려진 사방오리나무에 대해 아직까지 보고가 없었던 항당뇨 활성에 대해 조사하였다. Pancreatin와 salivary ${\alpha}-amylase$ 에 대해 MeOH 추출물과 HX 분획물이 ${\alpha}-amylase$를 효과적으로 억제하였으며, yeast ${\alpha}-glucosidase$에 대한 억제 활성은 MeOH 추출물과 EA 분획물 그리고 BuOH 분획물의 $IC_{50}$이 각각 $137.36\;{\mu}g/ml$와 $171.52\;{\mu}g/ml$ 그리고 $115.14\;{\mu}g/ml$로 나타남으로써, 현재 혈당강하제로 사용되고 있는 acarbose와 1-deoxynorjirimycin보다 높은 억제 효과를 보였다. 또한 폴리올 대상 이상에 의한 당뇨병성 합병증 유발과 관련하여 Aldose reductase 억제활성을 조사한 결과, $50\;{\mu}g/ml$ 농도에서 EA 분획물과 MeOH 추출물이 각각 84.13%와 58.73%로 녹은 저해활성이 나타났다. 따라서 본 연구를 통하여 국내에 자생하는 사방오리나무 추출물로부터 부작용이 적고 혈당강하효과가 뛰어난 새로운 항당뇨 신물질을 탐색하여 산업화 하고자하며 이를 통하여 바이오 소재산업의 활성화와 바이오 식품 나아가 바이오 의약품 개발 등 다양한 측면에서 부가가치를 창출하고자 한다.

• 생약학회지
• /
• 제25권1호
• /
• pp.41-46
• /
• 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).

• Natural Product Sciences
• /
• 제17권4호
• /
• pp.367-371
• /
• 2011

Effects of the extract and fractions from Parasenecio pseudotaimingasa on rat lens aldose reductase (AR) inhibition have been investigated. Among them, the n-BuOH fraction was exhibited good inhibitory potencies ($IC_{50}$ value 1.42 ${\mu}g/ml$). Phytochemical constituents were isolated from the n-BuOH fraction by open column chromatography. Their structures were elucidated as luteolin-7-O-rutinoside (1) and luteolin-7-Oglucoside (2) on the basis of spectroscopic analysis. Compounds 1 and 2 exhibited strong AR inhibitory activity, with $IC_{50}$ values of 2.37 and 1.05 ${\mu}M$, respectively. This is the first report on the isolation of compounds 1 and 2 from P. pseudotaimingasa. These results suggest that P. pseudotaimingasa could be a useful material in the development of a novel AR inhibitory agent against diabetic complications.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
• /
• pp.184-184
• /
• 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.

• 한국약용작물학회:학술대회논문집
• /
• 한국약용작물학회 2010년도 심포지엄 및 추계학술발표회
• /
• pp.302-303
• /
• 2010