• 한국식품과학회지
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• 제27권2호
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• pp.230-234
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• 1995

식품 유래의 생리활성 peptide를 분리할 목적으로 전통발효식품인 된장으로부터 혈압강하기능을 가지는 ACE(angiotensin converting enzyme)저해활성 peptide를 분획하였다. 시판 된장의 동결건조분말을 냉수로 추출했을 때 총질소의 회수율은 추출시간 30분에 73.3%를 보였다. 용매추출액에서 고분자 polypeptide를 제거하고 저분자 peptide만을 얻기 위해 PM-10 membrane(Amicon)을 이용하여 3시간 동안 한외여과한 결과, 질소성분의 회수율은 80.8%, 염의 회수율은 99.2%에 달했고 투과액의 ACE $IC_{50}$은 $41.8{\mu}g/ml$이었다. 한외여과 투과액을 reverse phase prep-HPLC로 분획하여 7개의 획분을 얻었으며, 그 중 F5분획물의 ACE저해활성이 $IC_{50}=6.8{\mu}g/ml$로 비활성이 가장 높았다. 염은 F1분획물에서 모두 회수되었다. F5분획물을 ion exchange prep-HPLC로 다시 분획하여 얻은 5개의 모든 획분에서 높은 비활성을 보였다($IC_{50}=2.5{\sim}8.3{\mu}g/ml$). 그 중 F53분획물의 비활성이 가장 높았으며($IC_{50}=2.5{\mu}g/ml$), F53의 구성아미노산 분석 결과 histidine의 함량이 특징적으로 높았다.

• 한국식품저장유통학회지
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• 제15권3호
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• pp.456-460
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• 2008

본 연구에서는 백단향의 다양한 추출방법에 따른 항산화활성, 미백 효과 및 세포 독성을 평가 하였다. DPPH 라디칼에 대한 소거능은 n-Hexane 추출물을 제외한 모든 추출물에서 양성대조군인 L-ascorbic acid ($IC_{50}$, $28.7\;{\mu}g/mL$)보다 강하거나 동등한 활성을 나타내었으며, 그중에서도 70% acetone추출물에는 강한 라디칼 소거능($IC_{50}$, $18.6\;{\mu}g/mL$)을 나타내었다. 또한 LDL 산화억제 실험에서도 활성이 인정되었고 총 페놀 함량이 높게 나타난 70% acetone 추출물에 가장 강한 활성($IC_{50}$, $58.3\;{\mu}g/mL$)이 확인되었으며, 다음으로 MeOH, EtOH, Hot water, n-Hexane추출물 순의 활성을 관찰할 수 있었다. Tyrosinase 저해활성을 평가한 결과 양성 대조군인 arbutin ($IC_{50}$, $13.7\;{\mu}g/mL$) 및 kojic acid ($IC_{50}$, $8.3\;{\mu}g/mL$)보다 다소 약한 활성을 나타내었으며 70% Acetone을 이용하여 백단향을 추출할 경우 미백 활성이 가장 강한 결과를 얻었다. 백단향의 열수 추출물은 마우스멜라노마세포(B16F10)에 대해서 1.0 mg/mL의 농도에서 24.7%의 성장억제효과를 나타내었다.

• Food Science and Biotechnology
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• 제16권1호
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• pp.29-36
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• 2007

Five phenolic compounds 1-5 were isolated for the first time from the exudate of geminating peanut (Arachis hypogaea). The structures were fully characterized by analysis of physical and spectral data. All isolated compounds were tested for antioxidant activities using 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and hydroxyl radical. Compounds 2, 3, and 5 exhibited a strong scavenging effect on DPPH (2: $IC_{50}\;=\;10.4\;{\um}M$, 3: $IC_{50}\;=\;45.2\;{\mu}M$, 5: $IC_{50}\;=\;5.0\;{\mu}M$), and ABTS (2: $IC_{50}\;=\;9.6\;{\mu}M$, 3: $IC_{50}\;=\;5.5\;{\mu}M$, 5: $IC_{50}\;=\;3.3\;{\mu}M$) radical activity, whereas these compounds had weak hydroxyl radical scavenging activity ($IC_{50}\;>\;200\;{\mu}M$). The total phenolic contents of the extracts using n-hexane, EtOAc, and n-BuOH were found to be 96.4-964.3 mg gallic acid equivalent per g dry material (GAE/g) and n-BuOH fraction showed the highest total phenolic content (964.3 mg GAE/g). These studies suggest that the exudate of geminating peanut may possess possible health related benefits to humans.

• Archives of Pharmacal Research
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• 제27권4호
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• pp.381-385
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• 2004

Nine phenolic ($1\~9$) and two furan type (10, 11) compounds, were isolated from the methanolic extract of the tuber of Gastrodia elata Blume (Orchidaceae) in the course of continuing search for platelet anit-aggregating plant components. Compound 1 was identified as 4,4'-dihy-droxybenzyl sulfone, a novel compound for the best of our knowledge. Compound 10, 5-hydroxymethyl-2-furancarboxaldehyde, was isolated for the first time from this plant. Compound 1 ($IC_{50};\;83{\mu}M$) was about four times more inhibitory to U46619 induced aggregation than ASA ($IC_{50};\340{\mu}M$). Compound 9, 4,4'-dihydroxy-dibenzylether, ($IC_{50};\;5{\mu}M$, $3{\mu}M\;and\;33{\mu}M$, respectively) was $10\~}80$ fold more potent than ASA ($IC_{50};\;420\;{\mu}M,\;53\;{\mu}M\;and\;340\;{\mu}M$ respectively) to collagen, epinephrine and U46619 induced aggregation, although it is less active than ASA to AA induced aggregation.

• 대한화학회지
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• 제55권5호
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• pp.765-775
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• 2011

Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.

• 한국미생물·생명공학회지
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• 제28권2호
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• pp.87-91
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• 2000

미생물로부터 U937 세포주의 etoposide에 유발된 apoptosis 저해물질을 탐색한 결과 곰팡이 F80834 균주를 선발하였다. 균주 배양액으로부터 저해물질을 분리한 후 UV, EIMS, 1H-NMR, 13C-NMR, DEPT 등의 기기분석을 실시한 결과 terrein으로 동정되었다. 이 물질은 $IC_{50}$ $20\mu\textrm{g}/ml$의 농도로 U937 세포주의 etoposide에 의한 caspase 3 유도를 저해하였다. Etoposide에 의한 세포의 사멸도 IC50 $10\mu\textrm{g}/ml$ 농도로 저해하였으며, 동일한 농도 조건에서 단독 처리시 세포 독성을 나타내지 않았다.

• Journal of Applied Biological Chemistry
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• 제51권6호
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• pp.302-306
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• 2008

국화과 식물인 민들레, 엉겅퀴, 그리고 고려엉겅퀴를 대상으로 항당뇨 활성 측정 방법 중 하나인 흰쥐 수정체 aldose reductase 저해 활성을 측정하였다. 여러 부위별 추출물 중 민들레 지상부 메탄올 추출물이 $IC_{50}\;8.71\;{\mu}g/mL$로서 뛰어난 저해 활성을 보였다. 국화과 식물에서 분리된 대표적인 화합물인 silymarin과 민들레에서 분리한 luteolin(1)그리고 고려 엉겅퀴에서 분리된 syringin(2)을 대상으로 aldose reductase저해 활성을 측정한 결과 silymarin과 luteolin은 뛰어난 aldose reductase 저해 활성을 보였다.

• Journal of Microbiology and Biotechnology
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• 제28권11호
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• pp.1806-1813
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• 2018

A new sesquiterpene lactone dimer [1], together with five known compounds (2-6), was isolated from the flowers of Inula britannica. The structures of these compounds were established by extensive spectroscopic studies and chemical evidence. The inhibitory activities of these isolated compounds (1-6) against human neutrophil elastase (HNE) were also evaluated in vitro; compounds 1 and 6 exhibited significant inhibitory effects against HNE activity, with $IC_{50}$ values of 8.2 and $10.4{\mu}m$, respectively, comparable to that of epigallocatechin gallate (EGCG; $IC_{50}=10.9{\mu}M$). In addition, compounds 3 and 5 exhibited moderate HNE inhibitory effects, with $IC_{50}$ values of 21.9 and $42.5{\mu}M$, respectively. In contrast, compounds 2 and 4 exhibited no such activity ($IC_{50}$ > $100{\mu}M$). The mechanism by which 1 and 3 inhibited HNE was noncompetitive inhibition, with inhibition constant ($K_i$) values of 8.0 and $22.8{\mu}M$, respectively.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.383.3-384
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• 2002

Rosmarinic acid (1) and methyl rosmarinic acid (2), isolated from the ethyl acetate soluble fraction of the methanolic extract of Salvia miltiorrhiza Bunge (Lamiaceae) were found to be the tyrosinase inhibitors and scavengers of 1, 1-diphenyl-2-picrylhydrzyl (DPPH) radical. Compounds 1 and 2 inhibited the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with $IC_{50}$/ of 16.8 $\mu\textrm{M}$ and 21.5 $\mu\textrm{M}$. respectively. It compared well with kojic acid. a well-known tyrosinase inhibitor. with an $IC_{50}$ of 22.4 $\mu\textrm{M}$. The inhibitory kinetics, analyzed by a Lineweaver-Burk plot, found rosmarinic acid and its methyl ester to be competitive inhibitors with $K_{i}$ of $2.35{\times}10^{-5}M$ and $1.52{\times}10^{-5}M$ respectively. In addition, compounds 1 and 2 showed the scavenging activities on DPPH radical, with $IC_{50}$ of 4.27 $\mu\textrm{M}$ and 3.05 $\mu\textrm{M}$. respectively. These scavenging effects were more potent than that of L-ascorbic acid ($IC_{50}$ = 11.75$\mu\textrm{M}$).

• Bulletin of the Korean Chemical Society
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• 제32권9호
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• pp.3459-3464
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• 2011

In order to extend the scaffold of non-peptidic calpain inhibitor, we have designed and synthesized 14 chalcone derivatives categorized into two groups based on their structures. Compounds 7 ($IC_{50}=16.67{\pm}0.42{\mu}M$) and 8 ($IC_{50}=16.92{\pm}0.14{\mu}M$) in group A were most selective ${\mu}$-calpain inhibitor over cathepsins B and L. On the other hand, compound 14 possessing furan ring exhibited inhibitory activities for ${\mu}$-calpain ($IC_{50}=15.39{\pm}1.34{\mu}M$) as well as cathepsin B ($IC_{50}=20.59{\pm}1.35{\mu}M$). The results discovered implicated that chalcone analogues possessing proper size and functional groups can be a potential lead core for selective non-peptidic ${\mu}$-calpain inhibitor. Furthermore, dual inhibitors for ${\mu}$-calpain and cathepsin B can also be developed from chalcones by elaborate structure manipulation.