• 제목/요약/키워드: structure-bioactivity

검색결과 59건 처리시간 0.024초

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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    • 제20권3호
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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.

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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    • 제22권5호
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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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    • 제24권1호
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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.

갯벌 방선균 유래 Boholamide A의 구조 및 생리활성에 대한 연구 (Structure and Bioactivity of Boholamide A from a Tidal Mudflat Actinomycete)

  • 서정원;문규호
    • 생약학회지
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    • 제52권4호
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    • pp.203-207
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    • 2021
  • LC/MS approach targeting secondary metabolites of bacterial strain resulted in the discovery of boholamide A (1), from the culture of marine actinomycete strain which was isolated from a tidal mudflat in Muan, Republic of Korea. Boholamide A (1), a cyclodepsipeptide with HDMN, APD, glycine, and valine was structurally determined by using 1D/2D NMR spectroscopy, mass spectrometry and UV spectroscopy. Boholamide A (1) showed the inhibitory activity against Bacillus subtilis, with IC50 value of 0.08 mM.

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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ACAT inhibitory effect of Guineensine isolated from Piper longum L.

  • Lee, Seung-Woong;Kim , Koan-Hoi;Kim, Young-Ho;Rho, Mun-Chual;Lee, Hyun-Sun;Kim, Young-Kook
    • 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.201.1-201.1
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    • 2003
  • Study of Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors from medicinal plants, we found strong inhibitory activity of ACAT enzyme from rat liver microsome by the CHC1$_3$ extract of Piper longum. Bioactivity-guided fractionation led to the isolation of Guineensine (1), its structure was elucidated by spectroscopic (IR, UV, MS and NMR) means. It inhibited ACAT activity in a dose-dependent manner with IC$\sub$50/ values of 1.2 $\mu\textrm{g}$/ml on in vitro assay using rat liver microsome.

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Response of Odontoblast to the Bio-Calcium Phosphate Cement

  • Kim, Jin-Woo;Kim, Sung-Won;Kim, Gyoo-Cheon;Kim, Yong-Deok;Kim, Cheol-Hun;Kim, Bok-Joo;Kim, Uk-Kyu
    • Maxillofacial Plastic and Reconstructive Surgery
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    • 제33권4호
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    • pp.301-307
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    • 2011
  • Purpose: If the tooth structure is damaged, then it is impossible to regenerate the tooth. The materials used to restore the tooth structure are not related to the composition of the tooth. The materials used to restore the structure can't replace the natural tooth because they just fill the defective structure. Calcium phosphate cement remineralizes the dentin and almost replaces the natural tooth, but there are some disadvantages. We conducted basic tests with Biomimetic CPC (Bio-CPC) to make sure of the possibility of the biomaterial to remineralize the defective tooth structure. Methods: In this study, the bioactivity and biocompatibility of Bio-CPC were evaluated for its potential value as the bio-material for regeneration of damaged tooth structure by conducting a cell toxicity assay (WST-1 assay), a cytokinesis-block micronucleus assay, a chromosomal aberration test, total RNA extraction and RT-PCR on MDPC-23 mouse odontoblast-like cells. Results: The in vitro cytotoxicity test showed that the Bio-CPC was fairly cytocompatible for the MDPC-23 mouse odontoblast-like cells. Conclusion: Bio-CPC has a possibility to be a new biomaterial and further study of Bio-CPC is needed.

Bioactive Metabolites Produced by Pseudonocardia endophytica VUK-10 from Mangrove Sediments: Isolation, Chemical Structure Determination and Bioactivity

  • Mangamuri, Usha Kiranmayi;Vijayalakshmi, Muvva;Poda, Sudhakar;Manavathi, Bramanandam;Bhujangarao, Ch.;Venkateswarlu, Y.
    • Journal of Microbiology and Biotechnology
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    • 제25권5호
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    • pp.629-636
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    • 2015
  • Chemical investigation of the actinobacterial isolate Pseudonocardia endophytica VUK-10 has led to the segregation of two known bioactive compounds, namely 4-(2-acetamidoethyl) phenyl acetate and 4-((1, 4-dioxooctahydropyrrolo [1, 2-a] pyrazin-3-yl) methyl) phenyl acetate. The strain was isolated from a sediment sample of the Nizampatnam mangrove ecosystem, south coastal Andhra Pradesh, India. The chemical structure of the active compounds was established on the basis of spectroscopic analysis, including 1H NMR and 13C NMR spectroscopies, FTIR, and EIMS. The antimicrobial and cytotoxic activities of the bioactive compounds produced by the strain were tested against opportunistic and pathogenic bacteria and fungi and on MDA-MB-231, OAW, HeLa, and MCF-7 cell lines. The compounds exhibited antimicrobial activities against gram-positive and gram-negative bacteria and fungi and also showed potent cytotoxic activity against MDA-MB-231, OAW, HeLa, and MCF-7 cell lines. This is the first example for this class of bioactive compounds isolated from Pseudonocardia of mangrove origin.

Comparative Molecular Field Analyses (CoMFA) on the Mela-nogenesis Inhibitory Activities of Alkyl-3,4-dihydroxybenzoyl Derivatives.

  • Kim, Sang-Jin;Sung, Nack-Do;Lee, Tack-Hyuck
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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    • pp.225-231
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    • 2003
  • To search and development a new material with superior melanogenesis inhibitory activity, the bioactivities (obs. pl$_{50}$) of alkyl-3,4-dihydroxybenzoyl esters and N-alkyl-3,4-dihydroxybenz-oyl amides as substrate molecules were measured in mouse melanoma cells. And also, we have studied that 3-D QSARs (3 dimensional Quantitative Structure-Activity Relationships) between molecular interaction field of substrates and the bioactivities were analyzed using CoMFA (Comparative Molecular Field Analyses) method. When cross-validation value (q$^2$) is 0.68 at 3 components, the Pearson correlation coefficient ($r^2$) is 0.900. From the basis on the findings, the model was appeared by the contour map such as steric field and electrostatic field relationships between quantitative structure and the bioactivity of the various substrate derivatives. Measured bioactivities (obs. pl$_{50}$) of unknown compounds are very similar to predicted activity (pred. pl$_{50}$) according to the CoMFA model. As the results of prediction, we could conclude that the bioactivities were increased by creation of R$_1$ substitution of 5,5-dime-thylhexoxy, 6,6-dimethylheptyl, 1-amino-6,6-dimethylheptyl group etc and R$_2$ substitution of hydroxy, methyl, methoxy group etc.p etc.

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3D porous ceramic scaffolds prepared by the combination of bone cement reaction and rapid prototyping system

  • 윤희숙;박의균;임지원
    • 한국재료학회:학술대회논문집
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    • 한국재료학회 2012년도 춘계학술발표대회
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    • pp.56.2-56.2
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    • 2012
  • Clinically-favored materials for bone regeneration are mainly based on bioceramics due to their chemical similarity to the mineral phase of bone. A successful scaffold in bone regeneration should have a 3D interconnected pore structure with the proper biodegradability, biocompatibility, bioactivity, and mechanical property. The pore architecture and mechanical properties mainly dependent on the fabrication process. Bioceramics scaffolds are fabricated by polymer sponge method, freeze drying, and melt molding process in general. However, these typical processes have some shortcomings in both the structure and interconnectivity of pores and in controlling the mechanical stability. To overcome this limitation, the rapid prototyping (RP) technique have newly proposed. Researchers have suggested RP system in fabricating bioceramics scaffolds for bone tissue regeneration using selective laser sintering, powder printing with an organic binder to form green bodies prior to sintering. Meanwhile, sintering process in high temperature leads to bad cost performance, unexpected crystallization, unstable mechanical property, and low bio-functional performance. The development of RP process without high thermal treatment is especially important to enhance biofunctional performance of scaffold. The purpose of this study is development of new process to fabricate ceramic scaffold at room temperature. The structural properties of the scaffolds were analyzed by XRD, FE-SEM and TEM studies. The biological performance of the scaffolds was also evaluated by monitoring the cellular activity.

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