• 대한본초학회지
• /
• 제32권6호
• /
• pp.1-7
• /
• 2017

Objectives : The heartwood of Sappan Lignum has been used since ancient times as an ingredient in folk medicines against anti-bacterial and anti-anemia purposes. Many bioactive constituents have been derived from this biomass such as chalcones and homoisoflavonoids. In the current investigation, the antioxidant and anti-diabetic properties using DPPH and $ABTS^+$ radicals scavenging, ${\alpha}-glucosidase$, and advanced glycation end products (AGEs) inhibition assays were evaluated by different extraction methods of Sappan Lignum. Methods : In our continuing investigation for bioactive natural ingredients, the antioxidant and ${\alpha}-glucosidase$ inhibitory properties of Sappan Lignum extracts were prepared from different extraction methods and the biological efficacies were investigated in vitro. The antioxidant properties were evaluated employing radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ($ABTS^+$) radicals. In addition, the anti-diabetic effects of Sappan Lignum extracts were tested via ${\alpha}-glucosidase$ and AGEs formation inhibitory assay. The total phenolic contents were determined using a spectrophotometric method. Results : All the tested samples showed dose-dependent radical scavenging and ${\alpha}-glucosidase$ inhibitory activities. Among the tested extracts, the 80% methanolic extract of Sappan Lignum was showed the most potent activity with an $IC_{50}$ value of $82.3{\pm}1.7{\mu}g/m{\ell}$ against DPPH radical scavenging assay. While, $ABTS^+$ radical scavenging activity of 80% methanolic extract was higher than those of other extracts. Also, ${\alpha}-glucosidase$ inhibitory and AGEs formation effects of each extacts and total phenolic contents were evaluated. Conclusions : These results suggested that Sappan Lignum can be considered as a new effective source of natural antioxidant and anti-diabetic materials.

• 한국균학회지
• /
• 제42권3호
• /
• pp.207-212
• /
• 2014

검은비늘버섯을 이용하여 심혈관계 질환과 관련된 기능성 식품 개발을 위한 기초자료를 얻기 위해 검은비늘버섯물 추출물과 유기용매 분획물을 이용하여 심혈관계 질환관련 생리활성을 확인하였다. 물 추출물은 57.57%의 항산화활성을 나타냈지만 혈전용해활성, 트롬빈저해활성, ${\alpha}$-glucosidase 저해효과는 매우 낮게 나타났다. 반면 에틸 아세테이트 분획물은 0.70 plasmin unit의 높은 혈전용해 활성과, 87.36%와 46.44%의 높은 트롬빈 저해활성과 ${\alpha}$-glucosidase 저해활성을 나타냈으며, 물 분획물은 48.27%의 항산화활성을 나타냈다. 혈전용해활성이 높은 에틸 아세테이트 분획물은 섬유소원의 $A{\alpha}$와 $B{\beta}$ chain은 모두 분해시켰지만 ${\gamma}$ chain과는 반응하지 않았으며, $100^{\circ}C$에서 10분간 가열에도 혈전용해 활성에 변화가 없었다. 실험 결과로부터 검은비늘버섯의 에틸아세테이트 분획물은 높은 혈전용해활성과 트롬빈 저해활성과 ${\alpha}$-glucosidase 저해활성을 나타내 심혈관계 질환 관련 치료나 예방을 위한 기능성식품 개발에 이용 가능할 것으로 기대된다.

• 생약학회지
• /
• 제40권2호
• /
• pp.150-154
• /
• 2009

We examined ethanol extracts prepared from the Korean marine algae belonging to the Sargassaceae family for their inhibitory effects on ${\alpha}$-glucosidase activity and free radicals in vitro. Among five marine algae, the extracts of Sargassum yezoense were found to possess strongly ${\alpha}$-glucosidase inhibition and free radicals scavenging activities. Two compounds were isolated via bioactivity guided isolation and tested for their effects on ${\alpha}$-glucosidase, DPPH, $ABTS^{+}$ and $Photochem^{(R)}$ analysis. Their chemical structures were elucidated by spectral analysis and direct comparison with authentic compounds; their structures were identified as sargaquinoic acid (1) and sargahydroquinoic acid (2). The inhibitory effects of compound 1 and 2 ($IC_{50}$ value:14.2 and 12.8 ${\mu}M$, respectively) on ${\alpha}$-glucosidase were more potent that of deoxynojirimycin as a positive control ($IC_{50}$ value:18.0 ${\mu}M$). All compounds displayed antioxidative activity which was measured by DPPH, $ABTS^{+}$ and $Photochem^{(R)}$ apparatus.

• 약학회지
• /
• 제55권6호
• /
• pp.446-450
• /
• 2011

As an effort to find a new scaffold for ${\alpha}$-glucosidase inhibition, we have prepared total 11 phenylalkylated piperazine derivatives and tested their ${\alpha}$-glucosidase inhibitory activities. Compounds 8 ($IC_{50}=2.73{\pm}0.075mM$) possessing two 3-methoxyphenethyl group on 1,4-position of piperazine showed comparable potency to acarbose used as reference. But other compounds were inactive to ${\alpha}$-glucosidase. The result indicated that proper substituents on the piperazine can engender ${\alpha}$-glucosidase inhibitory activities on the piperazine derivatives.

• 한국약용작물학회지
• /
• 제26권5호
• /
• pp.382-390
• /
• 2018

Background: The plant Aster koraiensis has long been used as an ingredient in folk medicine. It has been reported that Aster koraiensis extract (AKE) prevents the progression of diabetes-induced retinopathy and nephropathy. However, although these beneficial effects of AKE on diabetes complications have been identified, the antidiabetic effects of AKE have not yet been completely investigated and quantified. In the present study, the glucose-lowering and antioxidant effects of aqueous and ethanolic AKEs were evaluated. Methods and Results: The glucose-lowering effects of aqueous and ethanolic (30%-, 50%-, and 80%-ethanol) AKEs were investigated via ${\alpha}$-glucosidase inhibitory assays. The mode of inhibition by AKEs on ${\alpha}$-glucosidase was identified through kinetic analysis. The total antioxidant capacity of each of the 4 AKEs was evaluated by assessing their conversion rate of $Cu^{2+}$ to $Cu^+$. The content of chlorogenic acid and 3,5-di-O-caffeoylquinic acid, the bioactive compounds in AKE, in each extract were analyzed by high performance liquid chromatography (HPLC). The AKEs showed potent ${\alpha}$-glucosidase inhibitory activity with mixed inhibition mode, and significant antioxidant capacity. Conclusions: These results of this study suggested that the AKEs tested had ${\alpha}$-glucosidase inhibitory and antioxidant effects. Among the extracts, the 80% ethanol extract showed the most significant ${\alpha}$-glucosidase inhibitory activity, with a half maximal inhibitory concentration ($IC_{50}$ value) of $1.65{\pm}0.36mg/m{\ell}$ and a half maximal effective concentration ($EC_{50}$ value) for its antioxidant activity of $0.42{\pm}0.10mg/m{\ell}$. It can therefore be used as a source of therapeutic agents to treat diabetes patients.

• 미생물학회지
• /
• 제38권2호
• /
• pp.139-143
• /
• 2002

탄수화물분해 효소인 $\alpha$-glucosidase의 활성을 저해하는 물질을 생성하는 미생물을 검색하기 위하여 토양시료로 부터 수종의 미생물을 검색하였다. 토양 시료에서 강력한 $\alpha$-glucosidase 저해제를 생성하는 방선균PM718을 분리하였고 그 저해제의 활성을 기지물질인 acarbose와 비교 측정한 결과 우수한 활성을 나타냄을 확인하였다. 또한 그 활성은 pH 변화에도 안정된 활성을 유지하는 것을 확인하였다.

• 한국약용작물학회지
• /
• 제15권2호
• /
• pp.128-131
• /
• 2007

This study was carried out to investigate inhibitory effect of extracts from Artemisia capillaris Thumb. on maltase, sucrase, ${\alpha}-amylase$, nonspecific ${\alpha}-glucosidase$, and postprandial hyperglycemia. Methanol extract and organic solvent (n-hexane, ethyl acetate, butanol, aqueous) fractions from the medicinal herb were determined for the inhibitory activities against maltase, sucrase and ${\alpha}-amylase$. The methanol extract from A. capillaris strongly inhibited maltase (57%) and ${\alpha}-glucosidase$ (72%) at the concentration of 100 ${\mu}g/m{\ell}$. Among the four fractions (n-hexane, ethyl acetate, butanol, aqueous) examined, the butanol fraction from A. capillaris showed potent inhibitory effects on maltase (73%), sucrase (33%), and ${\alpha}-amylase$ (75%) at the concentration of 100 ${\mu}g/m{\ell}$. The butanol fraction from Artemisia capillaris also exhibited significant reductions (20%) of blood glucose elevation in mice loaded with maltose. These results suggest that the extract from Artemisia capillaris can be used as a new nutraceutical for inhibition on postprandial hyperglycemia

• 한국식품영양과학회지
• /
• 제44권5호
• /
• pp.681-686
• /
• 2015

약용식물 23종 메탄올 추출물의 폴리페놀 함량을 측정한 후 항산화 활성을 측정하고, 항당뇨 활성으로는 ${\alpha}$-amylase 저해 활성, ${\alpha}$-glucosidase 저해 활성을 검정하여 혈당강하 활성을 나타낼 수 있는 약용식물을 선발하고자 한다. 약용식물의 폴리페놀 함량을 분석한 결과 1.50~15.25 mg GAE/g의 다양한 함량 범위로 나타났으며 가장 높은 함량은 주목열매(15.25 mg GAE/g), 화살나무줄기(15.12 mg GAE/g), 두충잎(14.24 mg GAE/g)으로 3종이 나타났다. 60% 이상 DPPH 라디칼 소거능을 본 약용식물로는 두충 줄기수피(80.10%), 구기자나무 뿌리(64.25%), 화살나무 줄기(73.59%), 비수리(78.20%), 주목열매(70.52%), 뽕잎나무 잎줄기(67.81%) 부위 추출물로 6종이 선발되었다. ${\alpha}$-Glucosidase를 80% 이상 저해한 약용소재로는 두충 줄기심재, 두충 줄기수피, 화살나무 줄기, 마, 율무, 녹두 6종이 선발되었다. ${\alpha}$-Amylase를 80% 이상 저해한 약용식물로는 칡뿌리, 두충 줄기수피, 두충잎, 구기자 열매, 화살나무 잎줄기, 화살나무 줄기, 조릿대 지상부, 마, 뽕잎나무 잎줄기 추출물 등 9종이 선발되었다. 항산화 및 항당뇨 활성이 우수했던 약용식물들은 향후 새로운 의약품 개발 및 성인병 예방의 건강기능식품으로 개발하는 데 있어 좋은 기초자료로 활용될 것으로 기대된다.

• Journal of Applied Biological Chemistry
• /
• 제62권1호
• /
• pp.81-86
• /
• 2019

A yellow resin (gamboge) from Garcinia hanburyi has been widely used as folk medicine due to its antibacterial and antitumor activities. We isolated four ${\alpha}$-glucosidase inhibitory compounds from the methanol extract of gamboge. The compounds (1-4) were identified as gambogoic acid (1), moreollic acid (2), gambogic acid (3), and 10-methoxygambogenic acid (4), respectively through spectroscopic data including 2D-NMR and HREIMS. All compounds were examined in the enzyme inhibition assay against ${\alpha}$-glucosidase to identify their inhibitory potencies and kinetic behavior. All compounds (1-4) showed enzyme inhibition against ${\alpha}$-glucosidase, but the activity was significantly affected by the methoxy group on C-10 of ring A and pentenyl pyran moiety of ring D. For example, compound 1 ($IC_{50}=41.4{\mu}M$) bearing pyran ring eight times effective that 4 ($IC_{50}=350.6{\mu}M$) having geranyl group itself. Most active compound was found out to be gambogoic acid (1) which was analyzed most abundant metabolite in gamboge by LC-ESI-MS/MS. In kinetic study, compounds 1 and 2 were proved as noncompetitive inhibitors.

• 원예과학기술지
• /
• 제28권5호
• /
• pp.857-863
• /
• 2010

기생초 꽃의 생리활성을 평가하여 천연물 유래 기능성 소재를 개발하기 위하여 에탄올 추출물 및 용매분획물의 항산화활성, ACE 저해활성, ${\alpha}$-glucosidase 억제능, 항염활성 및 항암활성을 측정하였다. 에탄올 추출물의 DPPH radical 소거 활성($IC_{50}$)과 ABTS radical 소거활성은 각각 $0.100mg{\cdot}mL^{-1}$ 및 3.427 AEAC였으며, 용매분획물 중 ethyl acetate 분획물이 각각 $0.034mg{\cdot}mL^{-1}$ 및 15.785AEAC으로 가장 높았으며, ACE 저해활성 및 ${\alpha}$-glucosidase 억제활성도 각각 40.96% 및 $0.125mg{\cdot}mL^{-1}$로 ethyl acetate 분획물이 우수하였다. 또한 에탄올 추출물, chloroform 및 ethyl acetate 분획물에서 세포독성 없이 효과적으로 NO의 생성을 억제하였고, 대장암 세포주에 대한 에탄올 추출물, n-hexane, chloroform 및 ethyl acetate 분획물의 $IC_{50}$값은 각각 0.208, 0.041, 0.142 및 $0.107mg{\cdot}mL^{-1}$으로 우수한 증식억제효과를 보였다. 이러한 결과를 종합하여 볼 때, 기생초 꽃의 우수한 생리활성을 이용한 기능성 소재로의 활용이 가능 할 것으로 판단된다.