• 제목/요약/키워드: bioassay-guided isolation

검색결과 88건 처리시간 0.036초

참당귀지상부의 플라보노이드 성분 및 생리활성 (Flavonoid Compounds and Biological Activities on the Aaerial Parts of Angelica gigas)

  • 문형인;안규태;이강노;지옥표
    • 약학회지
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    • 제44권2호
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    • pp.119-127
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    • 2000
  • This paper describes isolation and elucidation structure of the components from leaves and evaluate the radical scavenging activity on DPPH radical for antioxidant effect. Bioassay guided fractionation of MeOH extract afforded active EtOAc and BuOH factions. The most active EtOAc fraction was repeatedly chrormatographed over silica and Sephadex LH-20 to afford six flavonoid compounds. Studies on the antioxidant activity of these constituents showed that quercetin was the most active of these compounds. Luteolin and kaempherol are also active, These results suggested that the antioxidant activity of leaves of Angelica gigas may be due to flavonoid components. All the compounds were identified by spectroscopic methods and are the first report from leaves of Angelica gigas.

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Acetylcholinesterase Inhibitors from the Twigs off Vaccinium oldhami Miquel

  • Lee, Jae-Hyeok;Lee, Ki-Taek;Yang, Jae-Heon;Baek, Nam-In;Kim, Dae-Keun
    • Archives of Pharmacal Research
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    • 제27권1호
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    • pp.53-56
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    • 2004
  • In the course of finding Korean natural products with acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the twigs of Vaccinium oldhami significantly inhibited AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two compounds, taraxerol (1) and scopoletin (2), as active constituents. These compounds inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$/ values of compounds 1 and 2 were 33.6 (79 $\muM$) and 10.0 (52 $\muM$) $\mu$g/mL, respectively.

Cytotoxic Constituents from the Roots of Asarum sieboldii in Human Breast Cancer Cells

  • Kim, Eunae;Kim, Hyun Jung;Oh, Ha-Na;Kwak, Ah-Won;Kim, Su-Nam;Kang, Bok Yun;Cho, Seung-Sik;Shim, Jung-Hyun;Yoon, Goo
    • Natural Product Sciences
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    • 제25권1호
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    • pp.72-75
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    • 2019
  • Bioassay-guided fractionation of the roots of Asarum sieboldii led to the isolation of the six compounds methylkakuol (1), sesamin (2), asarinin (3), xanthoxylol (4), and (2E,4E,8Z,10E/Z)-N-(2-methylpropyl) dodeca-2,4,8,10-tetraenamide (5/6). Among the isolates, xanthoxylol (4) exhibited significant cytotoxicity against human breast cancer cells MCF-7 and MDA-MB-231 in vitro with $IC_{50}$ values of 9.15 and $13.95{\mu}M$, respectively.

Preventive Agents against Sepsis and New Phenylpropanoid Glucosides from the Fruits of Illicium verum

  • Lee, Sung-Won;Li, Gao;Lee, Kyong-Sun;Jung, Jun-Sub;Xu, Ming-Lu;Seo, Chang-Seob;Song, Dong-Keun;Son, Jong-Keun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.257.1-257.1
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    • 2003
  • The bioassay-guided fractionation of preventive agents against lethality due to septic shock from the fruits of Illicium verum lead to the isolation of two known racemic mixtures of phenylpropanoids (1 and 2), along with two known phenylpropanoid glucosides (3 and 5) and two new phenylpropanoid glucosides (4 and 6). Their chemical structures were elucidated on the basis of spectroscopic studies. (omitted)

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Protective agents against sepsis from the root bark of Paeonia suffruticosa

  • Li-Gao;Xu , Ming-Lu;Seo, Chang-Seob;Kim, Hyo-Jin;Lee, You-Jeong;Lee, Yeun-Koung;Son, Jong-Keun;Song, Dong-Keun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.199.2-199.2
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    • 2003
  • The bioassay-guided fractionation of protective agents against sepsis-induced lethality from the root bark of Paeonia suffruticosa led to the isolation of ten known compounds: paeonol (1), 2,5-dihydroxy-4-methoxyacetophenone (2) methyl 3-hydroxy-4- methoxybenzoate (3), acetovanillone (4), benzoic acid (5), benzoylpaeoniflorin (6), paeonoside (7), paeoniflorin (8), oxypaeoniflorin (9) and apiopaeonoside (10). Among them, 4 exhibited the highest survival rate in a dose-dependent manner (100% with a dose of 30 mg/kg versus 16.7% for the control experiment) and showed reduction of plasma alanine aminotransferase (ALT) value on the in vivo assay model of sepsis induced by LPS/GalN.

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Inhibitory effects of the stem bark extract of Eucommia ulmoides on the proliferation of human tumor cell lines

  • Choi, Yeon-Hee;Seo, Jee-Hee;Kim, Jung-Sook;Kim, Seong-Kie;Choi, Sang-Un;Kim, Young-Sup;Kim, Young-Kyoon;Ryu, Shi-Yong
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.190.1-190.1
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    • 2003
  • A bioassay-guided fractionation of the stem bark extract of Eucommia ulmoides Oliver (Eucommiaceae) led to the isolation of three iridoid constituents, genipin (1), geniposide (3), geniposidic acid (4) as well as (${\pm}$)-guaiacylglycerol (2) and fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted)

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Melanin Biosynthesis Inhibitors from the Tubers of Gastrodia elata

  • Li Gao;Kim, Jae-Hyon;Xu, Ming-Lu;Seo, Chang-Seob;Kim, Hyo-Jin;Lee, You-Jeong;Lee, Yeun-Koung;Lee, Seung-Ho;Chang, Hyeun-Wook;Son, Jong-Keun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.206.3-207
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    • 2003
  • The bioassay-guided fractionation of the methylene chloride soluble portion of a methanol extract of Gastrodia elata tubers led to the isolation of a new furfural, 5-(4-hydroxy-benzyloxymethyl)-furan-2-carbaldehyde (2), together with four known compounds (1, 3-5), which exhibited potent inhibitory activity at the concentration of 25 $\mu\textrm{g}$/ml on melanin biosynthesis in cultured B-16 mouse melanoma cells.

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Inhibitory effects of the extract of Viscum album on the proliferation of human tumor cell lines

  • Seo, Jee-Hee;Choi, Yeon-Hee;Kim, Jung-Sook;Kim, Seong-Kie;Choi, Sang-Un;Kim, Young-Sup;Ryu, Shi-Yong;Kim, Young-Kyoon
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.202.2-202.2
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    • 2003
  • A bioassay-guided fractionation of the whole extract of Viscum album (a parasitic plant : Loranthaceae) led to the isolation of two triterpenoidal components, oleanolic acid (1), ${\beta}$-amyrin acetate (2), homoflavoyadorinin B (3) as well as large quantity of free fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted)

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신이(辛夷)로부터 멜라닌 생성 억제물질의 분리 (Isolation of Melanin Biosynthesis Inhibitory Compounds from the Flowers of Magnolia denudata)

  • 허광화;김정아;박성희;손애량;장태수;장현욱;정시련;이승호
    • 생약학회지
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    • 제35권2호통권137호
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    • pp.152-156
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    • 2004
  • The bioassay-guided fractionation of the MeOH extract of the flowers of Magnolia denudata led us to the isolation of six compounds identified as fargesin(1), kobusin(2), aschantin(3), magnolin(4), rel-[7s,8s,8's]-3,4,3',4'-tetra- methoxy-9,7'- dihydroxy-8,8',7.O.9'-lignan(5) and oplodiol(6), respectively. Among the isolated compounds, fargesin(1) showed most potent inhibitory effect on the melanin polymer biosynthesis in cultured B-16 mouse melanoma cell lines$(IC_{50},\;45.7\;{\mu}M)$.

자소엽에서 분리된 트리테르페노이드의 베타-아밀로이드 응집 억제 효과 (Anti-Amyloidogenic Effects of Triterpenoids Isolated from Perilla Leaves)

  • 여지윤;이충현;박소영
    • 생약학회지
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    • 제51권4호
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    • pp.238-243
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    • 2020
  • Perilla frutescens Britton var. acuta Kudo, an annual plant primarily cultivated in China, Japan, and Korea, has been used as a traditional medicine to treat inflammatory diseases, depression, and many anxiety-related disorders. Previously, we reported the inhibitory effects of n-hexane layer of P. frutescens var. acuta extract against beta-amyloid (Aβ) aggregation, and the isolation of asarone derivatives as active constituents from n-hexane layer. In this study, dichloromethane layer of P. frutescens var. acuta was applied to bioassay-guided isolation methods accompanied with Thioflavin T (Th T) fluorescence assay to investigate the inhibitory effect on Aβ aggregation and disaggregation. As the results, three triterpenoids including ursolic acid (1), tormentic acid (2) and corosolic acid (3) were isolated. All compounds reduced Aβ aggregation and increased disaggregation of preformed Aβ aggregates in a dose-dependent manner. However, the inhibitory effect of three compounds on Aβ aggregation was not correlated with antioxidant activity, which was measured by DPPH assay. Taken together, these results suggest that the triterpenoid derivatives from P. frutescens have the potential to be developed as good therapeutics or preventatives for AD.