• 제목/요약/키워드: Activity-guided isolation

검색결과 213건 처리시간 0.026초

Cytotoxic Quassinoids from Simaba cedron

  • Hitotsuyanagi, Yukio
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.52-55
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    • 1998
  • During a survey of new antitumor substances from higher plants, we have found that the crude extract of Simaba cedron Planchon (Simaroubaceae) showed cytotoxic activity (IC$\sub$50/ 0.7 $\mu\textrm{g}$/mL) against P388 leukemia cells. Activity-guided chromatographic purification using P388 cells led to the isolation of five novel quassinoids, cedronolactones A-E (1-5) and nine known quassinoids, simalikalactone D (6), chaparrinon (7), chaparrin (8), glaucarubolone (9), glaucarubol (10), samaderine Z (11), guanepolide (12), ailanquassin A (13), and polyandrol (14). In this seminar, the structural elucidation of 1-5 and the cytotoxic activity of the isolated compounds are discussed.

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Tyrosinase Inhibitory Prenylated Flavonoids from Sophora flavescens

  • Kim, Soo-Jin;Son, Kun-Ho;Chang, Hyun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • 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.151.2-151.2
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    • 2003
  • For the purpose of the development of a skin-whitening agent, Sophora flavescens was evaluated for tyrosinase inhibitory activity and its active principles were identified followed activity-guided isolation. The ethanol extract and dichloromethane fraction from S. flavescens showed significant inhibition of mushroom tyrosinase. From the dichloromethane fraction, three known prenylated flavonoids, sophoraflavanone G, kuraridin, and kurarinone, were isolated. Compared with kojic acid ($IC_50$=20.5 $\mu$M), these compounds possessed more potent tyrosinase inhibitory activity. (omitted)

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백출 지상부의 항산화 성분 (Anti-oxidative Compounds from The Aerial Parts of Atractylodes macrocephala Koidzumi)

  • 한정훈;김진효;김성건;정성희;김도훈;김기은;황완균
    • 약학회지
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    • 제51권2호
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    • pp.88-95
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    • 2007
  • Atractylodes macrocephala has been used for renal anorexia, gastroenteritis, cold, dyspepsia in Korean folk medicine. Specially aerial parts has been eaten as edible mountain herbs. In order to investigate the efficacy of antioxidant activity the activity guided fractionation and isolation of physiologically active substance were peformed. For the investigation of the active components from Atractylodes macrocephala MeOH extracts of aerial parts of Atractylodes macrocephala Koidzumi L. were suspended with H$_2$O, partitioned by CHCl$_3$. In order to investigate the efficacy of antioxidative activity the activity guided fractionation and isolation of physiologically active substance were peformed. CHCl$_3$, H$_2$O, 30% MeOH, 60% MeOH, MeOH fractions were examined antioxidative activity by DPPH method. It was revealed that 30% MeOH and 60% MeOH fractions have significantly antioxidant activity. From 30% MeOH and 60% MeOH fraction, six flavonoids (7-methoxy-pinocembrin-7-O-${\beta}$-D-glucopyranoside, apige nin-8-C-${\beta}$-D-glucopyranoside, 4'-caffeoyl-luteolin-6-glucopyranoside, luteloin-6-C-${\beta}$-D-glucopyranoside, apigenin-6-C-${\beta}$-D-glucopyranoside, luteolin) and four phenylpropanoids (3-feruloylquinic acid, 4,5-di-O-caffeoylquinic acid, feruloyl acid, 3,5-di-O-caffeoylquinic acid) were isolated. To investigate the antioxidant activities of each compounds, we measured radical scavening activity with DPPH method and anti-lipid peroxidative efficacy on low density lipoprotein (LDL) with TBARS assay. Six compounds (III, IV, V, VI, IX, X) which have antioxidant factor showed significant activities.

Cytotoxic and antimicrobial deterpene from Anisotome Iyallii

  • Choi, Eun-Young;Yang, Hyun-Ok;Choi, Won-Hyung;Lee, Jeong-Ho;Perry-NigelB;Baek, Seung-Hwa
    • 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.392.2-392.2
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    • 2002
  • Cytotoxic activity against the P388 cell line was seen in a crude extract of Anisotome lyallii. A bioactivity guided isolation led to the isolation of a deterpene. which displayed strong Cytotoxic activity against the P388 cell line (IC50 2.3 $\mu$g/ml), as well as antimicrobial activity against Bacillus subtilis. The structure of de terpene 1 was elucidated by spectroscopic methods. (omitted)

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Inhibitory Effect of Trans-N-p-Coumaroyl Tryamine from the Twigs of Celtis chinensis on the Acetylcholinesterase

  • Kim, Dae-Keun;Lee, Kie-Seung
    • Archives of Pharmacal Research
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    • 제26권9호
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    • pp.735-738
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    • 2003
  • The methanolic extract of the twigs of Celtis chinensis was found to show inhibitory activity on acetylcholinesterase (AChE), an enzyme that plays a role in the metabolic hydrolysis of ACh. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of N-p-coumaroyl tyramine. as an inhibitor on AChE. This compound inhibited AChE activity in a dose-dependent manner, and the $IC_50$ value of trans-N-p-coumaroyl tyramine was 34.5 $\mu$g/mL (122 $\mu$M).

Anti-Oxidative compounds from Quercus salieina bark

  • Kim, Ho-Hyun;Lee, Kwang-sup;Ham , In-Hye;Chon, In-Ju;Whang, Wan-Kyunn
    • 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.388.2-388.2
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    • 2002
  • Quercus species have been used for diarrhea. dysentery, dermatitis. haemoptoe, and haemorrhagia in Korean folk medicine. Specially Quercus salicina have been used for diuretic. anti-inflammatory. antiedemic. and litholytic agent. In order to investigate the efficacy of antioxidative activity the activity guided fraction and isolation of physiologically active substance were performed. (omitted)

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Bioassay-Guided Isolation and Identification of Compounds from Arecae Pericarpium with Anti-inflammatory, Anti-oxidative, and Melanogenesis Inhibition Activities

  • Indriana, Amelia;Lee, Kyoung Jin;Kim, Yeong Shik
    • Natural Product Sciences
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    • 제22권3호
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    • pp.193-200
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    • 2016
  • This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.

Catechin-7-O-$\beta$-D-apiofuranoside: An Anti-inflammatory constituent from alnus japonica bark

  • Jeong, Choon-Sik;Kang, Min-Hee;Hyun, Jin-Ee;Lim, Duk-Yun
    • 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.191.3-192
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    • 2003
  • Alnus japonica (Betulaceae) has been traditionally used for purifying blood, and curing feces containing blood, enteritis, diarrhea, alcoholism and cut wounds. In the current work, activity guided isolation of the butanol fraction of the Alnus japonica bark led to the isolation of catechin-7-O-${\beta}$-D-apiofuranoside. Anti-inflammatory activity was determined with carrageenan-induced paw edema in mice as an acute inflammation, complete Freund's adjuvant-induced arthritis as a chronic inflammation. Carrageenan- induced paw edema in mice was significantly inhibited at 0.5, 1, 2, and 3 hr after carrageenan injection by administration of the flavonoid glycoside at the dose of 150mg/kg. (omitted)

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Pyrophen Produced by Endophytic Fungi Aspergillus sp Isolated from Piper crocatum Ruiz & Pav Exhibits Cytotoxic Activity and Induces S Phase Arrest in T47D Breast Cancer Cells

  • Astuti, Puji;Erden, Willy;Wahyono, Wahyono;Wahyuono, Subagus;Hertiani, Triana
    • Asian Pacific Journal of Cancer Prevention
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    • 제17권2호
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    • pp.615-618
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    • 2016
  • Ethyl acetate extracts obtained from culture of endophytic fungi Aspergillus sp isolated from Piper crocatum Ruiz & Pav, have been shown to possess cytotoxic activity against T47D breast cancer cells. Investigations were here conducted to determine bioactive compounds responsible for the activity. Bioassay guided fractionation was employed to obtain active compounds. Structure elucidation was performed based on analysis of LC-MS, $^1H$-NMR, $^{13}C$-NMR, COSY, DEPT, HMQC, HMBC data. Cytotoxity assays were conducted in 96 well plates against T47D and Vero cell lines. Bioassay guided isolation and chemical investigation led to the isolation of pyrophen, a 4-methoxy-6-(1'-acetamido-2'-phenylethyl)-2H-pyran-2-one. Further analysis of its activity against T47D and Vero cells showed an ability to inhibit the growth of T47D cells with IC50 values of $9.2{\mu}g/mL$ but less cytotoxicity to Vero cells with an $IC_{50}$ of $109{\mu}g/mL$. This compound at a concentration of 400 ng/mL induced S-phase arrest in T47D cells.

목단피로부터 멜라닌 생성 억제성분의 분리 (Isolation of Inhibitory Components on Tyrosinase Activity from the Bark of Paeonia moutan)

  • 이승호;박지수;김소영;김진준;정시련
    • 약학회지
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    • 제42권4호
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    • pp.353-358
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    • 1998
  • The MeOH extract of the bark of Paeonia moutan showed potent inhibitory effect on the mushroom tyrosinase activity in vitro. The activity-guided fractionation of t he MeOH extract resulted in the isolation of three active compounds. The chemical structures of these compounds were elucidated by chemical and spectroscopic evidence as catechin, 1,2,3,6-tetra-O-galloyl-${\beta}$-D-glucose and 1,2,3,4,6-penta-0-galloyl-${\beta}$-D-glucose, respectively. Among them, the inhibitory activity by 1,2,3,6-tetra-galloyl-${\beta}$-D-glucose on mushroom tyrosinase was more potent $(IC_{50}=3.5\;{\mu}M)$ than that of kojic acid $(IC_{50}=8.7\;{\mu}M)$ ,but catechin enhanced the mushroom tyrosinase activity 50% in the concentration of 34.5M.

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