• 동의생리병리학회지
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• 제22권6호
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• pp.1557-1561
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• 2008

Red ginseng possibly has new ingredients converted during steaming and dry process from fresh ginseng. Kujeungkupo method which means 9 repetitive steamings and dryings process was used for the production of red ginseng from 6-year old ginseng roots. Saponin was extracted from each red ginseng produced at the 1st, 3rd, 5th, 7th, and 9th during the steaming and drying treatment, and we analyzed saponin content with TLC. Minor saponins, such as ginsenoside-Rg3, -Rh2, compound K, and F2, increased as the process time of steaming and drying, but major saponins (ginsenoside-Rb1, -Rb2, -Rc, -Rd, -Re, -Rf, -Rg1) were decreased. Major saponins were yet observed almost at the 1st process, then degraded as the increasing time of steaming and drying process. Especially, ginsenoside-Re and -Rg were observed as considerable amount after the 1st treatment, but there were no trace of them after the 9th treatment. Ginsenoside-Rg1, -Rb2, and -Rb1 were also reduced remarkedly by 96.6%, 96%, and 92.3%, respectively. Minor saponins were increased significantly, especially for ginsenoside-Rg3 and ginsenoside-F2. These results suggest that Kujeungkupo method is the very useful method for the production of minor ginsenoside-Rg3 and -Rh2.

• 동의신경정신과학회지
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• 제23권1호
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• pp.145-159
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• 2012

Objectives : This research investigates the effect of the JCT extract regarding Alzheimer's disease. Methods : The effects of the JCT extract on IL-$1{\beta}$, IL-6, TNF-${\alpha}$, COX-2, NOS-II mRNA, APP mRNA, BACE mRNA, Nitric oxide(NO), and ${\beta}A$ protein production in the BV2 microglia cell lines treated with LPS and ${\beta}A$ were investigated. Results : 1. The JCT extract suppressed the expression of IL-$1{\beta}$, IL-6, TNF-${\alpha}$, COX-2, and NOS-II mRNA in BV2 microglial cell line treated with LPS and ${\beta}A$. 2. The JCT extract suppressed the expression of BACE and APP mRNA in BV2 microglial cell line treated with LPS and ${\beta}A$. 3. The JCT extract suppressed the expression of Nitric oxide(NO) in BV2 microglial cell line treated with LPS and ${\beta}A$. 4. The JCT extract suppressed the expression of ${\beta}A$ protein production in BV2 microglial cell line treated with LPS and ${\beta}A$. Conclusions : These results suggest that the JCT group may be effective for the treatment of Alzheimer's disease. Thus, JCT could be considered among the future therapeutic drugs indicated for the treatment of Alzheimer's disease.

• 동의신경정신과학회지
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• 제21권1호
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• pp.71-88
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• 2010

Objectives: This research investigates the effect of the DHJHT extract on Alzheimer's disease. Specifically, the effects of the DHJHT extract on (1) the behavior (2) the infarction area of the hippocampus, and brain tissue injury in AD mice induced with ${\beta}A$ were investigated. Methods: The effects of the DHJHT extract on the proinflammation cytokines mRNA expression and production of BACE, APP and ${\beta}A$ in in BV2 microglial cell line treated by lipopolysacchaide(LPS) plus ${\beta}A$ were investigated. The effects of the DHJHT extract on the behavior of the memory deficit mice induced by scopolamine were investigated. Results: 1. The DHJHT extract suppressed the expression of IL-$1{\beta}$, IL-6, TNF-$\alpha$, COX-2, and NOS-II, BACE and APP mRNA in BV2 microglial cell line treated by LPS plus ${\beta}A$. 2. The DHJHT extract suppressed the expression of ${\beta}A$ production in BV2 microglial cell line treated with LPS plus ${\beta}A$. 3. The DHJHT extract showed significantly inhibitory effect on the scopolamine-induced impairment of memory in the experiment of Morris water maze. 4. The DHJHT group suppressed the expression of IL-$1{\beta}$, TNF-$\alpha$, MDA, and CD68+/CD11b+ in the brain tissue of the mice with AD induced by ${\beta}A$. 5. The DHJHT group reduced the infarction area of hippocampus, and controlled the injury of the brain tissue in the mice with AD induced by ${\beta}A$. 6. The DHJHT group reduced tau protein, and GFAP in the brain tissue of the mice with AD induced by ${\beta}A$. Conclusions: These results suggest that the DHJHT group may be effective for the treatment of AD. Thus, DHJHT could be considered among the future therapeutic drugs indicated for the treatment of AD.

• Journal of Microbiology and Biotechnology
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• 제31권7호
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• pp.1022-1027
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• 2021

Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC₅₀) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC₅₀ of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The K_i value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the K_i values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

• 한국수산과학회지
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• 제53권6호
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• pp.886-893
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• 2020

The seaweed Hizikia fusiformis is rich in protein, carbohydrates, vitamins, and minerals. This study investigated the antioxidant and physiological activities of H. fusiformis extracts prepared with 70% ethanol, 80% methanol, or distilled water. The extraction yields of these various solvent extracts were as follows: ethanol extract, 15.26%; methanol extract, 17.95%; and water extract, 45.62%. The methanol extract showed the highest total polyphenol content (24.06 mg GAE/g), but total flavonoid content was similar in all extracts. ABTS (2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) radical scavenging activity was highest in the ethanol extract (IC50: 0.90 mg/mL), while the methanol extract exhibited the strongest DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity (IC50: 8.09 mg/mL), reducing power (EC50: 0.40 mg/mL), and ferric reducing antioxidant power (0.28 mM). By contrast, tyrosinase and α-glucosidase inhibitory activities were higher in the ethanol extract than in the other extracts. The high BACE1 (β-secretase) inhibitory activity was observed in the ethanol extract (IC50: 1.03 mg/mL). These results indicate that H. fusiformis ethanol extracts may be useful for their antioxidant and functional properties in food and pharmaceutical materials.

• Journal of Applied Biological Chemistry
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• 제66권
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• pp.165-170
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• 2023

Isolation of the culture broth of a marine-derived Acremonium sp. CNQ-049 guided by HPLC-UV yielded compound 1 (3-phenethyl-2-phenylquinazolin-4(3H)-one), and its inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-secretase 1 (BACE1) were evaluated. Compound 1 was an effective selective MAO-B inhibitor with an IC₅₀ value of 9.39 µM and a selectivity index (SI) value of 4.26 versus MAO-A. In addition, compound 1 showed a potent selective butyrylcholinesterase (BChE) inhibition with an IC₅₀ value of 7.99 µM and an SI value of 5.01 versus acetylcholinesterase (AChE). However, compound 1 showed weak inhibitions against MAO-A, AChE, and BACE1. The Ki value of compound 1 for MAO-B was 5.22±1.73 µM with competitive inhibition, and the Ki value of compound 1 for BChE was 3.00±1.81 µM with mixed-type inhibition. Inhibitions of MAO-B and BChE by compound 1 were recovered by dialysis experiments. These results suggest that compound 1 is a dual-functional reversible inhibitor of MAO-B and BChE, that can be used as a treatment agent for neurological disorders.

• 한국식품영양과학회지
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• 제43권2호
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• pp.224-230
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• 2014

항암, 항염증 및 비만억제 등의 생리활성을 지닌 해조류는 최근 건강기능 식품, 기능성 화장품 그리고 의약품 산업 분야에서 미용과 건강식품 소재로 각광받고 있다. 본 연구에서는 10종의 갈조류 메탄올 추출물을 이용하여 1,1-diphenyl-2-picrylhydrazyl(DPPH) 라디칼 소거능과 아밀로이드 베타 단백질($A{\beta}$)의 신경독성에 대한 HT-22 신경세포 보호효과를 조사함으로써 천연물로부터 안전하고 새로운 신경세포 보호소재를 개발해내고자 한다. DPPH 라디칼 소거능의 경우 미역쇠를 포함한 8종의 갈조류에서는 비교적 낮은 활성산소 소거능을 보인 반면, 감태와 패에서 강력한 활성산소 소거능이 나왔다. $A{\beta}$의 신경독성에 대해 10종의 갈조류 추출물이 갖는 HT-22 신경세포 보호효과를 검증하기 위해 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) 분석과 APP, BACE1, iNOS 단백질의 발현양상 및 ERK1/2, p38, JNK1/2 단백질의 활성화 양상을 분석했다. MTT 분석 결과, $A{\beta}$의 신경독성으로부터 미역쇠가 $25{\mu}g/mL$의 농도에서 가장 효과적으로 세포를 보호하고 있는 것으로 나타났고, 알쏭이모자반, 불레기말, 바위수염, 짝잎모자반도 세포 보호효과가 있는 것으로 나타났다. 세포 보호효과가 있는 것으로 밝혀진 5종의 갈조류를 가지고 수행한 단백질 발현분석 결과, 미역쇠는 $A{\beta}$의 신경독성에 의해 HT-22 신경세포에서 발현되는 단백질인 BACE1과 iNOS의 발현을 저해하였다. 이는 미역쇠의 세포보호효과가 $A{\beta}$의 신경독성으로부터 일어난 ERK와 p38의 활성화에 연관된 세포신호전달 경로를 억제하는 것으로 보인다. 그러므로 특히 식용 갈조류인 미역쇠는 $A{\beta}$에 의해 유도된 신경독성에 대해서 신경세포 보호효과를 갖는 건강기능 식품 소재로서의 가치가 충분한 것으로 사료된다.

• 약학회지
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• 제59권4호
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• pp.151-157
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• 2015

The purpose of this study is to demonstrate how lead compounds are best optimized with the application of in silico QSAR and PBPK modeling at the early drug discovery stage. Several predictive QSAR models such as $IC_{50}$ potency model, intrinsic clearance model and brain penetration model were built and applied to a set of virtually synthesized library of the BACE1 inhibitors. Selected candidate compounds were also applied to the PBPK modeling for comparison between the predicted animal pharmacokinetic parameters and the observed ones in vivo. This novel lead optimization strategy using QSAR and PBPK modelings could be helpful to expedite the drug discovery process.

• Mycobiology
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• 제36권3호
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• pp.195-197
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• 2008

To produce a potent antidementia $\beta$-secretase inhibitor from a mushroom, the $\beta$-secretase inhibitory activities of various mushroom extracts were determined. Methanol extracts of Lentinula edodes exhibited the highest inhibitory activity (40.1%). The inhibitor was maximally extracted when a fruiting body of L. edodes was treated with 50% methanol at 40$^{\circ}C$ for 24 h.

• 생태와환경
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• 제38권2호통권112호
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• pp.137-145
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• 2005

전통적인 스크린 방법으로는 자연계에 존재하는 99% 이상의 미생물 자원을 확보하지 못했다. 자연생태계의 핵산을 직접 클로닝하는 전략은 배양 가능한 미생물의 유전적인 정보보다 더 광범위한 유전적인 정보를 전체의 미생물 메타지놈에서 확보하기 위한 계획을 세웠다. 그 결과 유용한 유전자를 탐색하는 한 방법으로 다양한 환경에서 메타지놈 DNA 라이브러리를 구축하는 방법이었다. 본 연구는 국내 중부권에 위치한 대청호로부터 시료를 수집하였고, T-RFLP 방법을 사용하여 미생물 군집의 다양성을 분석하였다. 핵산의 추출은 SDS를 사용한 freeing-thawing 방법을 사용하였으며, 추출한 핵산은 $UltraClean^{TM}kit$ (MoBio, USA)을 사용하여 정제하였다. 메타지놈 라이브러리는 제작은 정제한DNA와 pBACe3.6 vector를 EcoRI, BamHI, 그리고 SacII 등의 제한효소로 partial digestion하였고, 이들을 ligation한 다음 Escherichia coli DH10B에 형질전화 시켜 제작하였다. 메타지놈 라이브러는 14 Mb 정도 확보하였는데, 평균 insert size는 약 13 ${\sim}$ 15 kb이었다. Colony hybridization으로 메타지놈 라이브러리로부터 1, 2-dichloroethane (1, 2-DCE) hydrolytic dehalogenation의 분해에 관련된 유전자를 확인하였다. 1, 2-DCE dehalogenas효소는 기질에 대한 높은 활성을 나타내었다. 1, 2-dichloroethane dehalogenase 유전자의 클론을 만들었고, 염기서열을 분석하였다. 이들 결과로 보아 대청호로부터 제작한 메타지놈에서 dhlA 유전자를 확인한 균주는 1, 2-DCE 분해에 탁월한 능력을 나타내었다.