• 생약학회지
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• 제41권3호
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• pp.227-231
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• 2010

Protein tyrosine phosphatase 1B (PTP1B) is predicted to be therapeutic target in treatment of type 2 diabetes and obesity. Thus, in order to search for PTP1B inhibitors, we screened the inhibitory activity of PTP1B in the water extracts of 84 medicinal herbs. Among them, the extracts of Pini Folium, Magnoliae Cortex, Artemisiae asiaticae Herba, Schizonepetae Herba, Menthae Herba, Mume Fructus, Cimicifugae Rhizoma, and Amomi Cardamomi Fructus showed relatively significant (58-68%) inhibitory activity against PTP1B. Especially, the methylene chloride fraction of the methanol extract of Menthae Herba (81% inhibition at 30 ${\mu}g$/ml) showed more potent inhibitory activity against PTP1B than others.

• 생약학회지
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• 제38권2호통권149호
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• pp.108-112
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• 2007

We examined the inhibitory activities against monoamine oxidase (MAO) of Gardenia jasminoides in vitro and in vivo methods. Methanolic extract and ethylacetate fraction of Gardenia jasminoides fruit showed a significant inhibitory activity on MAO-A and MAO-B in vitro. The IC$_{50}$ values of each fraction on MAO-A and MAO-B are as fo11owed; total methanol extracts 1.23 and 1.34 mg/ml, EtOAc fraction 0.72 and 0.77 mg/ml. Water-soluble fraction also showed IC$_{50}$ values of 0.81 mg/ml on MAO-B. MAO-A activity was increased by the oral administration of ethanolic extract of G. jasminoides, while MAO-B activity was decreased. The concentration of serotonin of brain tissue administrated of ethanolic extract of G. jasminoides is slightly increased in rat. This tendency is not different from the activity of deprenyl which is a well known MAO inhibitor was used as a positive control. Consequently, we suggest that G. jasminoides may have the effects on the inhibitory activity against MAO This activity of G. jasminoides is considerable for development of functional materials for treatment and control of depression, dementia, Parkinson' disease, stress and promoting exercise, etc.

• KSBB Journal
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• 제18권1호
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• pp.45-50
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• 2003

송이의 공시균(KFR1432)과 실험실에서 자체 분리한 균(YxT, WxT, $\textrm{NK}_3\textrm{T}$)의 생장속도의 차이와 FE SEM으로 확인한 미세구조의 차이로 공시균과 자체 분리균이 서로 다른 균임을 확인할 수 있었다. Tyrosinase 활성 억제 실험을 위해 각각 균사체의 열수 추출물, 에탄올 추출물, 배양액을 hexane, chloroform, ethyl acetate로 분획하였다. 그 결과 모든 균의 ethyl acetate 분획층과 수층에서 tyrosinase 활성을 억제하는 것으로 나타났으며, KFR1432의 ethyl acetate 분획층과 YxT의 수층에서 억제율이 100%를 넘어 큰 저해 활성을 보였다. 또한 항산화제 처리 결과 ascorbic acid와 glutathion은 생장을 다소 증가시키거나 별 영향을 주지 못한 반면, tocopherol 의 경우 농도가 높아질수록 생장을 억제하는 것으로 나타났다. Tyrosinase 활성 억제에 있어서는 모든 항산화제 처리구에서 무처리구에 비해 높은 억제율을 보였다.

• Natural Product Sciences
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• 제17권3호
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• pp.212-215
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• 2011

In the course of screening anti-adipogenic activity of natural products employing the preadipocyte cell line, 3T3-L1 as an in vitro assay system, the EtOAc fraction of the stem barks of Acer tegmentosum Maxim (Aceraceae) showed significant inhibitory activity on adipocyte differentiation as assessed by measuring fat accumulation using Oil Red O staining. Activity-guided fractionation led to the isolation of active constituent, (+)-catechin. (+)-Catechin showed inhibitory activity on adipocyte differentiation in dose-dependent manner. Further studies with interval treatment demonstrated that (+)-catechin exerted inhibitory activity on adipocyte differentiation via acting on early stage of adipogenesis. Our present study also showed that (+)-catechin significantly inhibited the preadipocyte proliferation. Taken together, these results suggest that (+)-catechin, a constituent of A. tegmentosum might contribute the anti-adipogenic activity of A. tegmentosum.

• Journal of Animal Science and Technology
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• 제47권1호
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• pp.83-90
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• 2005

ACE-inhibitory peptides derived from goat's whey hydrolyzed by various proteolytic enzymes were separated and purified for antihypertension materials. The highest ACE-inhibitory activity of goat's whey hydrolysates was 85.5 % by pepsin for 72 hrs. Also the highest ACE-inhibitory activity of goat's whey hydrolysates was F-4 by pepsin for 72 hrs by Sephadex G-25 gel chromatograms. F-4e and F-4ed from F-4 by RP-HPLC to first and second purification were the highest in ACE-inhibitory activity, respectively. The most abundant amino acid was leucine(I 8.54 %) in F-4ed of ACE-inhibitory peptides after second purification. Amino acid sequence of F-4ed of ACE-inhibitory peptides showed Leu-Lys-Asp-Tyr-Gly-GlyVal- Ser-Leu and Leu-Gly-Asp-Gly-Ala-Gly- Asp-Val-Ala-Phe. $IC_{50}$ calibrated in peptic hydrolysates(72 hrs), F-4, F-4e and F-4ed from goat's whey hydrolysates by pepsin for 72 hrs were 33.93, 28.75, 11.74 and 1.09 mg/ml, respectively. From the results of this experiment, goat's whey hydrolysate by pepsin was shown to have ACE-inhibitory activity.

• 약학회지
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• 제43권1호
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• pp.28-32
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• 1999

Four derivatives of kojic acid were synthesized and their inhibitory activities against tyrosinase were evaluated. The C-2 hydroxymethyl and C-7 hydroxyl of kojic acid were replaced by carboxylate and amine, respectively. These derivatives were coupled to L-phenylalanine, producing two amide compounds. The carboxylate derivative (3), its amide compound (5), and the amine derivative (7) were weak inhibitors. The amide compound (9) where amine derivative (7) coupled to L-phenylalanine showed strong inhibitory activity ($IC_{50}=24.6{\;}{\mu}M$) comparable to kojic acid.

• 대한본초학회지
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• 제26권4호
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• pp.109-113
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• 2011

Objectives : We investigated the antioxidant and Antidiabetic effects of Cnidii Rhizoma Fermentata by Aspergillus oryzae and Aspergillus Kawauchi for 3days. Methods : In this study we compared Cnidii Rhizoma Fermentata with Aspergillus oryzae and Aspergillus Kawauchi that examined using reducing sugar, DPPH radical scavenging activity, ${\alpha}$-amylase and ${\alpha}$-glucosidase inhibitory activity. Also determined changes of pH and sugar content during fermentation for 3days. Results : The values for DPPH radical scavenging activity of Cnidii Rhizoma fermented by Aspergillus oryzae (86.6%) was higher than that of Aspergillus Kawauchi (77.9%). In ${\alpha}$-amylase inhibitory activity, fermented by Aspergillus Kawauchi had the highest inhibitory activity among other groups. But in ${\alpha}$-glucosidase inhibitory activity, fermented by Aspergillus oryzae had the highest inhibitory activity among other groups. While all groups of the sugar content increased During 3days fermentation, the pH was decreased. Conclusions : Based on these results, It was suggested that Cnidii Rhizoma Fermentata can be a useful and cost-effective resource for fuctional food and medicine.

• Journal of Applied Biological Chemistry
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• 제58권1호
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• pp.5-8
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• 2015

This study was to isolate an active component of the chloroform fraction from the methanol extract of Ruta chalepensis leaves and to measure inhibitory effects against ${\alpha}$-glucosidase or ${\alpha}$-amylase. The inhibitory compound of R. chalepensis leaves was isolated using chromatographic methods and identified as quinoline. Quinoline and its structurally related derivatives were tested for their inhibitory activities by evaluating the $IC_{50}$ values against ${\alpha}$-amylase or ${\alpha}$-glucosidase and were compared with that of acarbose. Based on the $IC_{50}$ values, quinazoline exhibited the greatest inhibitory activity ($20.5{\mu}g/mL$), followed by acarbose ($66.5{\mu}g/mL$), and quinoline ($80.3{\mu}g/mL$) against ${\alpha}$-glucosidase. In case of ${\alpha}$-amylase, quinazoline had potent inhibitory activity, followed by quinoline ($179.5{\mu}g/mL$) and acarbose ($180.6{\mu}g/mL$). These results indicate that R. chalepensis extract, quinoline, and quinazoline could be useful for inhibiting ${\alpha}$-glucosidase or ${\alpha}$-amylase.

• KSBB Journal
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• 제28권2호
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• pp.137-145
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• 2013

In order to develop new skin whitening agents, we prepared the $CH_2Cl_2$ layer (NGC) and BuOH layer (NGB) of 75% EtOH extract of the Nelumbinis nucifera Gaertner. We measured their tyrosinase inhibitory activity in vitro and melanin synthesis inhibitory activity in B16-F1 melanoma cells. They did not show inhibitory activity against mushroom tyrosinase but showed melanin synthesis inhibitory activity in a dose-dependent manner. In a melanin synthesis inhibition assay, NGC and NGB suppressed melanin production up to 52% and 46% at a concentration of $100{\mu}g/mL$, respectively. To elucidate the mechanism of the inhibitory effects of NGC and NGB on melanogenesis, we measured the expression of melanogenesis-related proteins by western blot assay. As a result, NGC suppressed the expression of tyrosinase, tyrosinase related protein 1 (TRP-1), tyrosinase related protein 2 (TRP-2), phosphorylated cAMP responsive element binding (p-CREB) protein, and microphthalmia associated transcription factor (MITF). And NGB inhibited the protein expression of tyrosinase and MITF, but had no significant effect on TRP-1, TRP-2, and p-CREB expression. Moreover, NGB increased the expression of phosphorylated extracellular signal-regulated kinase (p-ERK). In addition, we examined the inhibitory effect on the glycosylation of tyrosinase. As a result, NGC and NGB inhibited the activity of ${\alpha}$-glucosidase in vitro and the glycosylation of tyrosinase in B16-F1 melanoma cells. From these results, we concluded that NGC and NGB could be used as active ingredients for skin whitening.

• 한국버섯학회지
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• 제13권3호
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• pp.192-198
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• 2015

잎새버섯으로 준비된 물 추출물과 유기용매 분획물의 혈전용해활성과 트롬빈저해활성, acetylcholinesterase 저해활성, 항산화활성 및 면역활성을 확인하였다. 물 추출물과 물 분획물은 각각 1.55 plasmin unit와 0.85 plasmin unit의 높은 혈전용해활성을 나타내고, 물 분획물과 에틸 아세테이트 분획물은 76.43%와 72.59%의 트롬빈저해활성을 나타냈다. 클로로포름 분획물과 헥산 분획물이 95.14%와 94.74%의 높은 acetylcholinesterase 저해활성을 나타냈으며, 부탄올 분획물과 물 추출물이 94.47%와 91.04%의 항산화활성을 나타냈다. 부탄올 분획물과 물 분획물이 각각 2배 이상의 높은 면역기능활성을 나타냈다. 실험 결과로부터 잎새버섯의 분획물은 높은 혈전용해활성, 트롬빈 저해활성, acetylcholinesterase 저해활성 및 면역 기능활성을 나타내 심혈관계 질환과 치매의 예방 및 면역 기능강화를 위한 기능성식품 개발에 이용할 수 있을 것으로 사료된다.