• Title/Summary/Keyword: Bioactivity-guided fractionation

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The Synergistic Antibacterial Activity of 1-Acetyl-$\beta$-Carboline and $\beta$-Lactams Against Methicillin-Resistant Staphylococcus aureus (MRSA)

  • Shin, Hee-Jae;Lee, Hyi-Seung;Lee, Dae-Sung
    • Journal of Microbiology and Biotechnology
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    • v.20 no.3
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    • pp.501-505
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    • 2010
  • 1-Acetyl-$\beta$-carboline was isolated as an anti-MRSA agent from the fermentation broth of a marine actinomycete isolated from marine sediment. The producing strain was identified to be Streptomyces sp. by phylogenetic analysis of the 16S rRNA gene sequence. The anti-MRSA agent was isolated by bioactivity-guided fractionation of the culture extract by solvent partitioning, ODS open flash chromatography, and purification with a reversed-phase HPLC. Its structure was elucidated by extensive 2D NMR and mass spectral analyses. Combination of 1-acetyl-$\beta$-carboline with ampicillin exhibited synergistic antibacterial activity against MRSA.

Cholinesterase Inhibitors Isolated from the Fruits Extract of Evodia officinalis (오수유의 Cholinesterase 저해활성 성분)

  • Lee, Ji-Young;Cha, Mi-Ran;Choi, Chun-Whan;Kim, Young-Sup;Lee, Bong-Ho;Ryu, Shi-Yong
    • Korean Journal of Pharmacognosy
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    • v.43 no.2
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    • pp.122-126
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    • 2012
  • The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

HIV Integrase Inhibitory Activity of Agastache regosa

  • Kim, Hye-Kyung;Lee, Hyeong-Kyu;Shin, Cha-Gyun;Huh, Hoon
    • Archives of Pharmacal Research
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    • v.22 no.5
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    • pp.520-523
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    • 1999
  • We have been screening anti-HIV integrase compounds from Korean medicinal plants by using an in vitro assay system which is mainly composed of recombinant human immunodeficency virus type 1 integrase and radiolabeled oligonucleotides. From the above screening, the aqueous methanolic extract of the roots of Agastache rugosa exhibited a significant activity. Bioactivity-guided chromatographic fractionation of the methanolic extract resulted in the isolation of rosmarinic acid. The structure of the compound was determined by spectroscopic data and by the comparison with the reported values. The $IC_{50}$ of the rosmarinic acid was approximately $10{\mu}g/ml$ against HIV integrase.

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Characterization of an Antibiotic Produced by Bacillus subtilis JW-1 that Suppresses Ralstonia solanacearum

  • Kwon, Jae Won;Kim, Shin Duk
    • Journal of Microbiology and Biotechnology
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    • v.24 no.1
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    • pp.13-18
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    • 2014
  • Bacillus subtilis JW-1 was isolated from rhizosphere soil as a potential biocontrol agent of bacterial wilt caused by Ralstonia solanacearum. Seed treatment followed by a soil drench application with this strain resulted in >80% reduction in bacterial wilt disease compared with that in the untreated control under greenhouse conditions. The antibacterial compound produced by strain JW-1 was purified by bioactivity-guided fractionation. Based on mass spectroscopy and nuclear magnetic resonance spectral data ($^1H$, $^{13}C$, $^1H-^1H$ correlation spectroscopies, rotating frame nuclear Overhauser effect spectroscopy, and heteronuclear multiple-bond correlation spectroscopy), the structure of this compound was elucidated as a cyclic lipopeptide composed of a heptapeptide (Gln-Leu-Leu-Val-Asp-Leu-Leu) bonded to a ${\beta}$-hydroxy-iso-hexadecanoic acid arranged in a lactone ring system.

The Inhibition of Diacylglycerol Acyltransferase by Terpenoids from Youngia koidzumiana

  • Dat Nguyen Tien;Cai Xing Fu;Rho Mun-Chual;Lee Hyun Sun;Bae KiHwan;Kim Young Ho
    • Archives of Pharmacal Research
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    • v.28 no.2
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    • pp.164-168
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    • 2005
  • The EtOAc extract of Youngia koidzumiana significantly inhibited the diacylglycerol acyltransferase (DGAT) from rat liver microsomes. Bioactivity-guided fractionation led to the isolation of nine compounds, the structures of which were established using physicochemical and spectral data. Of the isolated compounds, oleanolic acid (2), methyl ursolate (7) and corosolic aicd (8) inhibited DGAT, with $IC_{50}$ values of 31.7, 26.4, and $44.3{\mu}M$, respectively. However, sesquit-erpenoids showed only weak inhibitory effects toward DGAT.

New Phenylpropanoids from Sasa quelpaertensis Nakai with Tyrosinase Inhibition Activities

  • Sultana, Nasim;Lee, Nam-Ho
    • Bulletin of the Korean Chemical Society
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    • v.30 no.8
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    • pp.1729-1732
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    • 2009
  • Bioactivity-guided fractionation led to the isolation of two new phenylpropanoids, 3-O-p-coumaroyl-1-(4-hydroxy- 3,5-dimethoxyphenyl)-1-propanone (1) and 3-O-p-coumaroyl-1-(4-hydroxy-3,5-dimethoxyphenyl)-1-O-$\beta$-gulcopyranosylpropanol (2), together with three known compounds, N-p-coumaroylserotonin (3), N-feruloylserotonin (4) and p-coumaric acid (5) from the leaves of Sasa quelpaertensis Nakai. Their structures were elucidated by spectroscopic methods including 1D and 2D-NMR. Compared to arbutin (I$C_{50}$ 0.048 mM) as a control, compounds 3 and 4 exhibited stronger tyrosinase inhibition activities with an I$C_{50}$ values of 0.027 mM and 0.026 mM, respectively. Compounds 1 (I$C_{50}$ 0.055 mM) and 2 (I$C_{50}$ 0.053 mM) also showed strong activities.

Chemical Constituents from Buddleja officinalis and Their Inhibitory Effects on Nitric Oxide Production

  • Park, Tae Wook;Lee, Chul;Lee, Jin Woo;Jang, Hari;Jin, Qinghao;Lee, Mi Kyeong;Hwang, Bang Yeon
    • Natural Product Sciences
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    • v.22 no.2
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    • pp.129-133
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    • 2016
  • Bioactivity-guided fractionation of a methanolic extract of Buddleja officinalis led to the isolation of two monoterpenes, crocusatin M (1), crocusatin C (2), a flavonoid, acacetin (3), three lignans, lariciresinol (4), pinoresinol (5), and syringaresinol (6), and two triterpenoidal saponins, mimengoside B (7) and songarosaponin A (8). The structures of isolates were identified based on 1D-, 2D-NMR, and MS data analysis. All isolates were tested for their inhibition on LPS-induced NO production in RAW 264.7 cells. As a result, mimengoside B (7) and songarosaponin A (8) showed a mild inhibitory activity of NO production.

Apocarotenoids from an Association of Two Marine Sponges

  • Shinde, Pramod B.;Kim, Mi-Ae;Son, Byeng-Wha;Lee, Chong-O.;Jung, Jee-H.
    • Natural Product Sciences
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    • v.13 no.4
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    • pp.365-368
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    • 2007
  • Bioactivity-guided fractionation of MeOH extract of an association of two sponges, Jaspis sp. and Poecillastra sp. resulted in isolation of four apocarotenoids (1 - 4). Their structures were determined on the basis of MS and NMR spectroscopic analyses and by direct comparison with those of reported. This is the first report on isolation of these compounds from any sponge. Isolated metabolites were evaluated for cytotoxicity against a small panel of solid human tumor cell lines.

Chemical Constituents from the Apical Bud of Gardenia sootepensis and Their Bioactivity (Gardenia sootepensis의 끝눈으로부터 생리활성 성분)

  • Youn, Ui Joung;Chang, Leng Chee
    • Korean Journal of Pharmacognosy
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    • v.48 no.2
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    • pp.113-118
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    • 2017
  • Bioassay guided fractionation and isolation of the $CH_2Cl_2$ extract from the apical bud of Gardenia sootepensis (Rubiaceae) led to the isolation of five known flavonoids (1-5). The structures of the compounds were determined by 1D and 2D NMR, and MS experiments, as well as by comparison of their data with published values. Compounds 1-5 were isolated for the first time from this plant source. The isolated compounds were evaluated for their cancer chemopreventive potential based on their ability to inhibit nitric oxide (NO) production. Among the isolates, compound 4 exhibited considerable NO inhibitory activity with an $IC_{50}$ value of $13.8{\mu}M$.

Aromatase Inhibitors from Isodon excisus var. coreanus

  • Jeong, Hyeh-Jean;Chang, Leng-Chee;Kim, Ho-Kyoung;Kim, Il-Hyuk;A.Douglas Kinghorn;John M.Pezzuto
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.243-245
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    • 2000
  • The diethyl ether extract of isodon excisus var. coreanus exhibited significant inhibitory activity in aromatase assay. Bioactivity-guided fractionation of the extract led to the isolation of three active compounds: inflexin(ent-1${\alpha}$-hydroxy-3${\beta}$,6a-diacetoxykau r-16-en-11,15-dione) (1), ursolic acid (2), and ursolic acid 3-O-acetate (3).

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