• Archives of Pharmacal Research
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• v.29 no.10
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• pp.826-833
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• 2006

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

• Journal of the Korean Chemical Society
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• v.40 no.9
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• pp.623-629
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• 1996

In order to identify antibiotic substances in the extract of a lichen, Umbilicaria vellea, the extract was chromatographed and two compounds were isolated. Compound I which showed antifungal and antibacterial activities, melted around 129∼132$^{\circ}C$ and showed UV absorption at 217, 265 and 300 nm. It showed a molecular ion at m/z 196. Its molecular formular was confirmed to be $C_{10}H_{12}O_4$ from elemental analysis. From its IR and NMR data it was identified to be ethyl 2,4-dihydroxy-6-methyl benzoate. Compound II melted around 58∼59$^{\circ}C$ and showed UV absorption at 212, 276 and 282 nm. It showed a molecular ion at m/z 124 and molecular formular was confirmed to be $C_7H_8O_2.$ From the analysis of its IR and NMR spectra it was identified to be 5-methyl-1,3-benzenediol.

• Journal of Life Science
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• v.9 no.1
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• pp.63-68
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• 1999

Many nucleoside compounds such as 5-halogen substituted uridine, 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide, and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate uridine-fatty acid derivatives were chemically synthesized and their antifungal, antibacterial, and antitumor activities were tested. 5-Bromo-2',3'-O-isopropylideneuridine(6) inhibited the growth of Trichophyton rubrum at $0.2{\mu}$g/ml of MIC. 5'-Amino-5'-deoxyuridine-penicillin G(19), 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(20), and 5-iodo-5'-amino-5'-deoxyuridine- penicillin G(22) had antibarterial activity(MIC was $6.25{\mu}$g/ml against S. aureus) and the latter two nucleoside compounds were the most antitumor derivatives(their $IC_{50}$ against L5178Y murine lymphoma cell was $6.5{\mu}$g/ml).

• Bulletin of the Korean Chemical Society
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• v.20 no.9
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• pp.1078-1084
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• 1999

A synthetic cecropin A(1-13)-melittin(1-13) [CA-ME] hybrid peptide was known to be an antimicrobial peptide having strong antibacterial, antifungal and antitumor activity with minimal cytotoxic effect against human erythrocyte. Analogues were synthesized to investigate the influences of the flexible hinge region of CA-ME on the antibiotic activity. Antibiotic activity of the peptides was measured by the growth inhibition against bac-terial, fungal and tumor cells and vesicle-aggregating or disrupting activity. The deletion of Gln-Gly-Ile (P1) or Gly-Gln-Gly-Ile-Gly (P3) from CA-ME brought about a significant decrease on the antibiotic activities. In contrast, Gly-Ile-Gly deletion (P2) from CA-ME or Pro insertion (P5) instead of Gly-Gln-Gly-Ile-Gly of CA-ME retained antibiotic activity. This result indicated that the flexible hinge or β-bend structure provided by Gly-Gln-Gly-Ile-Gly, Gln-Gly, or Pro in the central region of the peptides is requisite for its effective antibiotic activity and may facilitate easily the hydrophobic C-terminal region of the peptide to penetrate the lipid bilayers of the target cell membrane. In contrast, P4 and P6 with Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central region of the peptide caused a drastic reduction on the antibiotic activities. This result suggested that the con-secutive β-bend structure provided by Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central hinge region of the peptide seems to interrupt the ion channel/pore formation on the target cell membranes.

• Journal of the Korean Wood Science and Technology
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• v.28 no.2
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• pp.32-41
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• 2000

Antimicrobial and antioxidative activities on heartwood extractives from Zelkova serrata were investigated to develop a natural fungicide or preservative. The ethanol extract from Z. serrata was fractionated in the order of petroleum ether, diethylether and ethylacetate to determine antimicrobial activity. The highest antimicrobial activity against the tested microorganisms was found in the petroleum ether soluble fraction. An active antimicrobial compound was isolated from petroleum ether soluble fraction, and identified as 7-hydroxy-3-methoxycadalene by $^1H$-, $^{13}C$-NMR and EI-MS spectrometry. This compound showed higher antifungal activity, but lower antibacterial activity than hinokitiol(${\beta}$-thujaplicin), strong antimicrobial compound isolated from Thujopsis dolabrata. Antioxidative activity was also higher than ${\alpha}$-tocopherol and similar to BHT(butylated hydroxytoluene), one of the strongest synthetic antioxidant. As a result, it was concluded that 7-hydroxy-3-methoxycadalene isolated from Z. serrata had strong antifungal and antioxidative activities.

• Journal of the Korean Recycled Construction Resources Institute
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• v.10 no.1
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• pp.117-123
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• 2022

Recently, due to COV ID-19, many people are spending most of their time indoors. So, there is a rising interest on the indoor air quality in the field of building construction. The main sources for the indoor air pollution are human indoors activity, building materials, living supplies and the polluted air from outdoor. The Korean government has designated 17 indoor air pollutants including fine dust, total airborne bacteria, fungi and carbon dioxide, etc.. Most people are always exposed to assorted bacteria and molds in our daily life, because indoor environment for human, moderate temperature are humidity, it is favourable to the growth of most of bacteria and fungi. Pine needles have an antibacterial effect against bacteria and fungi. In this study, the antibacterial activity against bacteria and fungi was tested by cement matrix using pine needle extract. As a result, the cement matrix using pine needle extract showed antibacterial activities against bacteria, but in the case of fungi, it did not show antifungal activity.

• Microbiology and Biotechnology Letters
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• v.37 no.3
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• pp.266-272
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• 2009

The annual productions of yam and its aerial bulbils are estimated to 5,000 and 2,500 ton, respectively. But the majority of bulbils had been discarded without specific use. In this study, methanol extract and its organic solvent fractions were prepared from bulbils of Dioscorea batatas Decne, and their antimicrobial, antithrombin, and antioxidant activities were evaluated, respectively. The methanol extract contained 58.98% of water-soluble materials as like yam's extract. But the bulbils's extract contained 12-folds of total polyphenol and 3.4-folds of total flavonoids compared than yam's extract, respectively. For antimicrobial activity the hexane and ethyl acetate fraction showed strong antibacterial activity at $500{\mu}g/disc$ concentration against gram-negative and gram-positive bacteria. Antifungal activity was not observed in any fractions. Strong antithrombin activity was found in the hexane fractions. At 4.8 mg/mL concentration thrombin time (TT) was over 300 sec, which is 4-folds extended than the TT of yam. In a while, the ethyl acetate fraction showed strong DPPH scavenging activity ($IC_{50}$ of $38.1{\mu}g/mL$), SOD-like activity and reducing power, which are comparable to vitamin C or BHT. Our results suggest that the bulbils of yam as yam tuber have useful bio-activities, such as antibacterial, antithrombosis, and antioxidant activity.

• Korean Journal of Weed Science
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• v.14 no.1
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• pp.16-22
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• 1994

Ninty three species of domestic weeds were collected and screened for antimicrobial, antitumor, antioxidant and herbicidal activities. Among them, few showed antifungal activities. Cuscuta japonica showed inhibitory activity against Alternaria mali, Ambrosia artemisiifolia and Geranium sibiricum against Phytophthora capsici, Aster yomema and Aster pilosus against Phytophthora parasitica. Ambrosia artemisiifolia, Artemisia princeps, Artemisia capillaris, Ludwigia prostrata, Chrysanthemum zawadskii, Bidens frondosa, and Geranium sibiricum showed broad antibacterial activities. Carex chordorhiza, Artemisia capillaris, Persicaria nodosa, Senecio koreanus, Pariicum bisulcatum, Geranium sibiricum showed antiblebbing activity on human chronic leukemia K562 cell, among them, Persicaria nodosa was the strongist. Angelica decursiva, Equisetum arvense, Cimicifuga heracleifolia, Persicaria nodosa, Geranium sibiricum, Oenothera odorata, Cyperus sanguinolentus showed antioxidant activities. Ludwigia prostrata and Peucedanum terebinthaceum showed strong herbicidal activities.

• Food Science and Preservation
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• v.17 no.4
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• pp.541-546
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• 2010

Wild-garlic (Allium victorialis L.) is a perennial plant found in worldwide and has been considered as a favorite vegetable due to its particular smell and taste. However, the study of biological activity of wild-garlic and the development of processed food are in rudimentary. In this study, we evaluated several biological activities, including antioxidant, antimicrobial, and inhibitory activities against human thrombin, $\alpha$-amylase and $\alpha$-glucosidase, of Ulrung wild-garlic. Analysis of the composition showed that Ulrung wild-garlic is nutritive although it is perishable. The color of fresh juice was stably maintained during 10 days-storage at $4^{\circ}C$, but rapidly discolored by heat treatment at $70^{\circ}C$ for 1 h. During heat treatment, the contents of total sugar and total polyphenol were decreased to 75% and 50%, respectively, and acidity was increased from 0.069% to 0.111%. In a while, the brix, reducing sugar, and total flavonoids showed minor changes. The fresh juice showed strong DPPH scavenging activity, reducing power and antibacterial and antifungal activity, but the heat-treated juice lost the antioxidant and antimicrobial activities. The inhibitory activities against human thrombin and $\alpha$-amylase and $\alpha$-glucosidase was negligible in both fresh juice and heat-treated juice. These results suggested that the antioxidant and antimicrobial components in wild-garlic are heat-liable and volatile. Based on our results, we propose non-heat treatment products for processed wild-garlic, for example, fresh juice-added beverage or fermented liquors using wild-garlic.

• Journal of the Korean Chemical Society
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• v.54 no.5
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• pp.515-522
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• 2010

A relation between antimicrobial activities and the formation constants of solid complexes of Cu(II), Ni(II), Co(II), Mn(II) and Fe(III) with tridentate Schiff base ligand, 4-hydroxy-3(1-{2-(benzylideneamino)-phenylimino}-ethyl)-6-methyl-2Hpyran-2-one (HL) derived from o-phenylene diamines, dehydroacetic acid (DHA) and p-chloro benzaldehyde have been studied. The ligand and metal complexes were characterized by elemental analysis, conductivity, magnetic susceptibility, thermal analysis, X-ray diffraction, IR, $^1H$-NMR, UV-vis and mass spectra. From the analytical data, the stiochiometry of the complexes was found to be 1:2 (metal:ligand) with octahedral geometry. The molar conductance values suggest the nonelectrolytic nature of metal complexes. The X-ray diffraction data suggests monoclinic crystal system for Ni(II) and orthorhombic crystal system for Cu(II) and Co(II) complexes. The IR spectral data suggest that the ligand behaves as tridentate ligand with ONN donor atoms sequence towards central metal ion. Thermal behavior (TG/DTA) and kinetic parameters calculated by Coats-Redfern method suggests more ordered activated state in complex formation. The protonation constants of the complexes were determined potentiometrically in THF:water (60:40) medium at $25^{\circ}C$ and ionic strength ${\mu}=0.1\;M$ ($NaClO_4$). Antibacterial activities in vitro were performed against Staphylococcus aureu and Escherichia coli. Antifungal activities were studied against Aspergillus Niger and Trichoderma. The effect of the metal ions and stabilities of complexes on antimicrobial activities are discussed.