• Title/Summary/Keyword: Compound Activity

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Endophytic Diaporthe sp. ED2 Produces a Novel Anti-Candidal Ketone Derivative

  • Yenn, Tong Woei;Ring, Leong Chean;Nee, Tan Wen;Khairuddean, Melati;Zakaria, Latiffah;Ibrahim, Darah
    • Journal of Microbiology and Biotechnology
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    • v.27 no.6
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    • pp.1065-1070
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    • 2017
  • This study aimed to examine the anti-candidal efficacy of a novel ketone derivative isolated from Diaporthe sp. ED2, an endophytic fungus residing in medicinal herb Orthosiphon stamieus Benth. The ethyl acetate extract of the fungal culture was separated by open column and reverse phase high-performance liquid chromatography (HPLC). The eluent at retention time 5.64 min in the HPLC system was the only compound that exhibited anti-candidal activity on Kirby-Bauer assay. The structure of the compound was also elucidated by nuclear magnetic resonance and spectroscopy techniques. The purified anti-candidal compound was obtained as a colorless solid and characterized as 3-hydroxy-5-methoxyhex-5-ene-2,4-dione. On broth microdilution assay, the compound also exhibited fungicidal activity on a clinical strain of Candida albicans at a minimal inhibitory concentration of $3.1{\mu}g/ml$. The killing kinetic analysis also revealed that the compound was fungicidal against C. albicans in a concentration- and time-dependent manner. The compound was heat-stable up to $70^{\circ}C$, but its anti-candidal activity was affected at pH 2.

Insulin secretory activity and mechanism of compound K

  • Choi, Yun-Suk;Han, Gi-Cheol;Sung, Jong-Hwan;Chung, Sung-Hyun
    • Proceedings of the Ginseng society Conference
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    • 2006.05a
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    • pp.69-70
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    • 2006
  • Purpose: Panaxadiols are more potent than panaxatriols as far as insulin secretory activity is concerned. In this study, we examined insulin secretory activity and mechanism of compound K (CK), a major intestinal bacterial metabolite of ginsenosides. Method: Insulin secretory activity of CK was examined using pancreatic beta cells and in Oral Glucose Tolerance Test assay. In addition, insulin secretory mechanism was studied in terms of calcium dependent or independent pathways. Results: In vitro, CK enhanced the insulin secretion concentration-dependently when compared to glucose-stimulated control cells. Insulin secretory mechanism of CK seems to block ATP sensitive K channels, which was confirmed by diazoxide (K channel opener) but, insulin resistance ameliorating activity of CK can't be ruled out. In vivo, CK showed hypoglycemic effect in OGTT.

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Antibacterial Activity and Identification of the Active Compound from Tumeric Extract (울금색소 추출물의 항균성과 물질분리 동정)

  • 한신영;최석철
    • Textile Coloration and Finishing
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    • v.14 no.1
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    • pp.11-17
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    • 2002
  • To identify the antimicrobial activity, of tumeric and its active compound tumeric was fractionated into four groups dichloromethane extract, hexane fraction, methanol soluble fraction and residue's extract. They were tested for antibacterial activity against E. coil and S. aureus and the methanol soluble fraction was found lo be the most active fraction. Compound I, II and III were isolated from TLC and silica gel column chromatography in the methanol soluble fraction. These compounds were analyzed by $^1H-NMR\;and\;^{13}C-NMR$ spectra and identified as curcumin I, II and III. They were also tested for antimicrobial activity against E. coli and S. aureus. Curcumin I was the must active curcuminoids due to the phenolic and methoxyl$(OCH_3)$ moiety in the same molecular structure.

Anti-allergic Activity of Oriental Medicinal Herbs

  • Kim, Young-Mi
    • Korean Journal of Medicinal Crop Science
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    • v.14 no.5
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    • pp.282-288
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    • 2006
  • The effects of extracts from various Oriental medicinal herbs on mast-cell-mediated allergic reactions were investigated in this study. Out of these extracts, the medicinal herb Atractylodis rhizoma alba exhibited the most potent activity in the cells, with $IC_50$ values of $20.5\;{\mu}g/ml$, by DNP-BSA and $33.04\;{\mu}g/ml$, by compound 48/80. Similar to the in vitro activity, Atractylodis rhizoma alba inhibited compound-48/80-induced systemic anaphylaxis by 31.3% at 300 mg/kg in mice. It also suppressed the secretion of $TNF-{\alpha}$, a major pro-inflammatory cytokine in the cells. These results may suggest that Atractylodis rhizoma alba shows anti-allergic activity in compound 48/80-induced anaphylactic mice through the inhibition of mast cells.

Purification of Antimicrobial Substance for the Extract from the Root Bark of Morus alba (상백피 추출물로부터 향균성 물질의 분리정제)

  • 박욱연;김신희;김지회;김용관;장동석
    • Journal of Food Hygiene and Safety
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    • v.10 no.4
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    • pp.225.1-230
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    • 1995
  • The ethanol extract from the root bark of Morus alba showed the strongest antimicrobial activity on the growth of almost all the tested microorganisms which were food-borne pathogens and food-related microorganisms. 1) In order to isolate and purify of antimicrobial substance extracted from the root bark of Morus alba, the antimicrobial substance from the ethanol extract which exhibited a strong antimicrobial activity was purified by solvent fractionation, silica gel column chromatography, TLC and HPLC. Among the fractions fractionated by 4 kind of solvents from the ethanol extract, the antimicrobial activity of ethyl acetate fraction had the strongest antimicrobial activity against B. subtilis. Unknown compound were isolated from the ethyl acetate fraction by silica gel column chromatography, TLC and HPLC and the compounds showed strong absorbance at 207, 217 and 285 nm, therefore, it was supposed to be a kinds of aromatic compound.

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Design and Synthesis of 3-(3-Chloro-4-substituted phenyl)-4-(pyridin-4-yl)-1Hpyrazole- 1-carboxamide Derivatives and Their Antiproliferative Activity Against Melanoma Cell Line

  • El-Gamal, Mohammed I.;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.821-828
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    • 2011
  • Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied.

Pancreatic lipase Inhibitory Compound from Apis mellifera venome

  • Kim, Jun-Ran;Kim, Shin-Duk
    • International Journal of Industrial Entomology and Biomaterials
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    • v.16 no.2
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    • pp.57-59
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    • 2008
  • While searching for pancreatic lipase inhibitors, the active compound was found in a methanol extract of Apis mellifera venome. The active compound was isolated by Diaion HP-20 column chromatography, thin layer chromatography and HPLC. The active compound is stable to the extreme pH and heat. There is no loss of activity both in acidic and alkaline solution in the pH range of 2 to 11 by heating for 15 minutes at $90^{\circ}C$. The rf value of the compound was 0.51 at TLC with butanol : methanol: water (4:1:2) solvent system. The molecular weight of the compound was determined to be 293 by EI-MS.

Antibacterial Activities of Extracts from Chrysanthemum boreale M. (산국 추출물의 항균력)

  • Yang, Min-Suk;Nam, Sang-Hae
    • Applied Biological Chemistry
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    • v.38 no.3
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    • pp.269-272
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    • 1995
  • Antibacterial activity test of solvent fractions, sesquiterpenoid lactones, and Compound I and II extracted from Chrysanthemum boreale M. and Chrysanthemum indium L. were performed against four microorganisms. Among the tested substances, antibacterial activities were appeared against B. subtilis and V. parahaemolyticus at the chloroform fraction, sesquiterpenoid lactones and Compound I extracted from C. boreale. But chloroform fraction and sesquiterpenoid lactones extracted from C. indicum were showed weakly than those of C. boreale. Compound II and all fractions extracted from C. indicum were not appeared against the all tested microorganisms.

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Inhibition of Telomerase Activity in U937 Human Monocytic Leukemia Cells by Compound K, a Ginseng Saponin Metabolite

  • Kang Kyoung-Ah;Lee Kyoung-Hwa;Chae Sung-Wook;Kim Jeong-Ki;Seo Jung-Yeon;Ham Yong-Ho;Lee Kee-Ho;Kim Bum-Joon;Kim Hee-Sun;Kim Dong-Hyun;Hyun Jin Won
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.11 no.1
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    • pp.7-12
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    • 2006
  • Telomerase activation is detected in most cancerous cells; hence, telomerase is a highly selective target for cancer therapy, which plays an important role in the apoptotic process. We have previously reported that the ginseng saponin metabolite, Compound K (20-O-D-glucopyranosyl-20(S)-protopanaxadiol, IH901), inhibits cell proliferation by inducing apoptosis and cell cycle arrest at the $G_1$ phase. The present study investigated the regulation of telomerase activity in Compound K treated U937 cells. Compound K treatment caused a reduction in telomerase activity and down-regulated the human telomerase reverse transcriptase (hTERT) gene, resulting in the decreased expressions of its protein, and of the c-Myc and Spl proteins (transcription factors of hTERT). These results indicate that the anticancer activity of Compound K could be mediated by inhibition of the telomerase activity.

Isolation, Physico-chemical Properties and Biological Activity of Aurodox Group Antibiotics

  • Kim, Si-Kwan;Yeo, Woon-Hyung;Kim, Sang-Seock
    • Journal of Microbiology and Biotechnology
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    • v.6 no.4
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    • pp.265-269
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    • 1996
  • An isolate of Streptomyces rochei synonym was found to produce antibiotics with narrow anti-microbial spectrum against Streptococcus and Xanthomonas sp. Among the antibiotic complex produced by the strain, the main active compound was isolated, and its physico-chemical properties and biological activities were investigated. Molecular weight of the compound was determined to be ${[M+H]}^+$ 797 (FAB-MS). UV, $^1H \;and\;^{13}C$ NMR, and IR spectra suggested that the compound is a kirromycin-like aurodox group antibiotic. However, the anti-microbial spectrum of the main compound was slightly different from that of kirromycin. In addition, it was newly found that kirromycin showed a selective anti-microbial activity against Streptococcus pyogenes and phytopathogenic Xanthomonas sp.

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