• Archives of Pharmacal Research
• /
• 제16권4호
• /
• pp.327-330
• /
• 1993

A series of 2-chloro and 2-bromo-3-(substituted)-1, 4-naphthalenedione derivatives (1-25) were tested for antifungal and antibacterial activities in vitro against Candida albicans 10231 aand Local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Fusarium oxysporium KTCC 6501, Bacillus subtilis ATCC 6633, Pseudomonas arruginosa NCTC 10490, Staphylococcus aureus ATCC 6358p, Escherichia coli NIHJ and Acinetobacter baumanii Local. The MiC values were determined by twofold afar diution/streak method. Among thee derivatives, 1, 9, 20, 21, 23 and 25 showed more potent antifungal activities than fluconazole. 20 and 23 completely inhibited the gorwth of fungi, such as Candida albicans, Aspegillus niger, Ticophyton mentagrophytes and fusarium oxysporium, at $3.2\;\mu{g/ml}$. Also some derivatives had the antibacterial activities against Gram-positive bacteria.

• 대한한방부인과학회지
• /
• 제25권3호
• /
• pp.27-39
• /
• 2012

Objectives: Recently Ciprofloxacin, used in the treatment of mastitis, showed many serious side effects. The object of this study was to recognize whether TNS and KWT can be used in the treatment of mastitis by observing the in vitro antibacterial effects of TNS and KWT aqueous herbal extracts against S. aureus. Methods: Antibacterial activities of TNS and KWT aqueous extracts against S. aureus ATCC 25923 were detected using standard agar microdilution methods. In addition, the effects on the bacterial growth curve were monitored at MIC and $MIC{\times}2$ levels. The effects on the intracellular killing and bacterial invasion of individual test materials were also observed using Raw 264.6 and MCF-7. The results were compared with Ciprofloxacin, a second generation of quinolone antibiotics in the present study. Results: MIC of aqueous extracts of TNS and KWT against S. aureus were detected as ($0.313{\pm}0.107$) and ($0.137{\pm}0.053$) mg/ml, respectively. MIC of Ciprofloxacin was detected as ($0.469{\pm}0.297$) ${\mu}g/ml$ at same conditions. In addition, TNS, KWT aqueous herbal extracts and Ciprofloxacin were also showed marked dosage-dependent inhibition of bacterial growth, and dramatical inhibitions on the both intracellular killing assays and bacterial invasion using Raw 264.6 and MCF-7 cells were detected. Conclusions: The results obtained in this study suggest that TNS and KWT aqueous herbal extracts showed antibacterial effects against S. aureus, and they also showed dosage-dependent inhibitory effects on the bacterial growth. And they showed the significant intracellular killing and bacterial invasion effects. It means, KWT and TNS may show more potent anti-infectious effects against S. aureus in vivo.

• Journal of Microbiology and Biotechnology
• /
• 제12권6호
• /
• pp.1006-1009
• /
• 2002

The biological activities of farnesoic acid derivatives against pathogenic fungi and bacteria were investigated. Farnesoic acid and its derivatives showed growth inhibitory activities against various bacteria. Among the compounds tested, geranylgeranoic acid (3) had potent antibacterial activity against Salmonella typhimurium, Proteus vulgaris, and Bacillus subtilis with minimum inhibitory concentration (MIC) in the range of $6.25-12.5{\mu}g/ml$. On the other hand, amide derivatives of farnesoic acid showed some antifungal activities. In particular, 3,7,11-trimethyl-dodeca-2,6,10-trienoic acid amide (5a) had a potent antifungal activity against Aspergillus niger, Candida albicans, and Trichophyton sp. with MIC in the range of $6.25-12.5{\mu}g/ml$.

• Journal of Microbiology and Biotechnology
• /
• 제20권8호
• /
• pp.1204-1209
• /
• 2010

We evaluated the antibacterial activities of selected edible Korean plant seeds against the food-borne pathogens Staphylococcus aureus KCTC1927, Escherichia coli KCTC2593, Salmonella typhimurium KCTC2054, and Bacillus cereus KCTC1014. While screening for antibacterial agents, we discovered that wheat germ extract contains 2,6-dimethoxy-1,4-benzoquinone (DMBQ) and is highly inhibitory to S. aureus and B. cereus. This is the first report of the antibacterial activity of wheat germ extract. We also investigated the antibacterial activities of the 1,4-benzoquinone standards 1,4-benzoquinone (BQ), hydroquinone (HQ), methoxybenzoquinone (MBQ), and 2,6-dimethoxy-1,4-benzoquinone (DMBQ). DMBQ and BQ were the most highly inhibitory to S. aureus and S. typhimurium, followed by MBQ and HQ. MICs for DMBQ and BQ ranged between 8 and 64 ${\mu}g/ml$ against the four foodborne pathogens tested. DMBQ and BQ showed significant antibacterial activity; the most sensitive organism was S. aureus with an MIC of 8 ${\mu}g/ml$. BQ exhibited good activity against S. typhimurium (32 ${\mu}g/ml$) and B. cereus (32 ${\mu}g/ml$). The results suggest that wheat germ extract has potential for the development of natural antimicrobials and food preservatives for controlling foodborne pathogens.

• Bulletin of the Korean Chemical Society
• /
• 제32권1호
• /
• pp.229-238
• /
• 2011

A series of novel glucose derived benzyl and alkyl 1,2,3-triazoles and their hydrochlorides have been synthesized via Cu(I)-catalyzed 1,3-dipolar cycloaddition. All the new compounds were characterized by MS, IR and NMR spectra. The DEPT, APT, $^1H$-$^1H$ and $^1H-^{13}C$ 2D NMR spectra for some compounds were also recorded. These compounds were evaluated for their in vitro antibacterial activities against Staphylococcus aureus ATCC 29213, Bacillus subtilis, Bacillus proteus, Pseudomonas aeruginosa, Escherichia coli ATCC 25922, and antifungal activities against Candida albicans and Aspergillus fumigatus. The bioactive data revealed that (3R,4S,5S,6S)-2-(hydroxymethyl)-6-methoxy-4,5-bis((1-octyl-1H-1,2,3-triazol-4-yl)methoxy)-tetrahydro-2H-pyran-3-ol 8a exhibited excellent antifungal activity against A. fumigatus with an MIC value of 0.055 mM compared to Fluconazole. It also showed broad inhibitory efficacy against tested bacterial strains with MIC values ranging from 0.049 mM to 0.39 mM.

• Fisheries and Aquatic Sciences
• /
• 제22권6호
• /
• pp.13.1-13.9
• /
• 2019

Background: Marine invertebrates are well known as pivotal bioresources with bioactive substances such as anti-inflammatory sterols, antitumor terpenes, and antimicrobial peptides. However, there are few scientific reports on chemical compositions and bioactivities of marine invertebrates from the East Sea of South Korea. Methods: In this study, chemical compositions and biological activities were evaluated on both 70% EtOH and hot water extracts of 5 species of marine invertebrates (Crossaster papposus japonicus, Actinostola carlgreni, Stomphia coccinea, Actinostola sp., and Heliometra glacialis) collected from the East Sea of South Korea. The antioxidant activities were measured by ABTS radical scavenging assay. The cytotoxicity and anti-inflammatory activity were evaluated using MTT and Griess reagents. Moreover, the antibacterial effect was evaluated using paper disc assay and minimum inhibitory concentration (MIC) assay. Results: In the results of antioxidant activities, 70% EtOH extract of A. carlgreni showed the highest activity ($IC_{50}\;0.19{\pm}0.03mg/ml$) compared to other extracts. Moreover, 70% EtOH extract of A. carlgreni could significantly suppress the nitric oxide (NO) production in lipopolysaccharide-induced RAW 264.7. All extracts treated under $400{\mu}g/ml$ have no cytotoxic effects on RAW 264.7 macrophages. In the antibacterial test, both 70% EtOH extracts of C. papposus japonicus and H. glacialis showed a significant antibacterial effect on Staphylococcus aureus. The MIC values were evaluated at 256 and $512{\mu}g/ml$, respectively. Conclusions: These results suggested the bioactive potentials of marine invertebrates from the East Sea of South Korea in pharmaceutical and nutraceutical applications.

• 약학회지
• /
• 제41권2호
• /
• pp.225-232
• /
• 1997

The in vitro antibacterial activity of DWP20367 (1-Cyclopropyl-6-fluoro-8-chloro-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a new broad-spectrum fluoroquinolone, was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20367 was showed antibacterial activity much higher than CPFX, SPFX and OFLK against gram-positive bacteria, while it was slightly more superior to quinolones against gram-negative bacteria. DWP20367 was particularly effective against MRSA, and its $MlC_{90}$ against clinical isolates of methicillin-susceptible S. aureus, low methicillin-resistant S. aureus and high methicillin-resistant S. aureus were 0.098, 0.781 and 1.563 micro g/ml, respectively. Against S. pneumoniae, MIC90 of DWP20367 was 2- to 8-fold higher than those of CPFX. With a view of MIC90, DWP20367 showed slightly more potent activity against P. aeruginosa and E. coli isolates than the control quinolones. DWP20367 activity was not affected by inoculum size and medium pH. But addition of $Mg^{2+}, \;Ca^{2+} $Mg2+, Ca2+ or horse serum (25%) decreased its antibacterial activity. DWP20367 was showed rapidly bactericidal activity within 2 to 4 h, and regrowth was not observed even after 24 h incubation at concentrations near the 4-fold of MIC.

• 약학회지
• /
• 제41권1호
• /
• pp.132-138
• /
• 1997

The antimicrobial activity of Manuka oil, a steam distillate from Leptospermum scoparium, was investigated, and it's MIC against ten kinds of microorganisms was determin ed. MICs against bacteria and fungi were measured by means of both two-fold dliution method and agar plate two-fold dilution method, respectively. MICs of Manuka oil against Staphylococcus aureus KCTC 1916 and Micrococcus luteus KCTC 1915, gram-positive microrganisms, were identical as 3.05 ${\mu}$g/ml, while it's antibacterial activity against gram-negative microrganisms such as Pseudomonas aeruginosa KCTC 2513, Escherichia coli KCFC 1682, Klebsiella pneunioniae KCTC 2001 or Proteus vulgaris KCTC 2433 was negligible(MIC: ${\geq}$ 1000 ${\mu}$g/ml), suggesting a high susceptibility of gram-positive bacteria to Manuka oil. In addition, MIC against Aspergillus niger KCTC 6077 was 24 ${\mu}$g/ml. and that against the other fungi, Tricophyton mentagrophytes KCTC 1374 and Candida albicans KCTC 1940 was ${\geq}$ 1000 ${\mu}$g/ml. When Manuka oil ointment was used in combination with other drugs. i.e.. gentamycin sulfate, chlotrimazol and hydrocortisone acetate, and diphenhydramine HCl and hydrocortisone acetate. it's antibacterial activity against Staphylococcus aureus KCTC 1916 was higher than Manuka oil ointment or other drugs alone. In conclusion, Manuka oil possesses a selective antibacterial activity against Staphylococcus aureus KCTC 1916, and can be used as a potent antibacterial agent against it.

• Bulletin of the Korean Chemical Society
• /
• 제31권7호
• /
• pp.2003-2010
• /
• 2010

A new class of halobenzyloxy or alkoxy 1,2,4-triazoles and their hydrochlorides were synthesized through cyclization starting from commercially available phenylhydrazine. The structures were characterized by MS, IR and $^1H$ NMR spectra as well as elemental analyses. All the synthesized compounds were screened for their antibacterial activities in vitro against Staphylococcus aureus (ATCC29213), methicillin-resistant Staphylococcus aureus (N315), Bacillus subtilis, Escherichia coli (ATCC25922), Pseudomonas aeruginosa, Shigella dysenteriae, Eberthella typhosa, and antifungal activities against Candida albicans (ATCC76615), Aspergillus fumigatus by broth microdilution assay method. The results of preliminary bioassay indicated that 3-(2,4-difluorobenzyloxy)-1-phenyl-1H-1,2,4-triazole hydrochloride exhibited the best inhibitory activity with an MIC value of 56.25 ${\mu}M$ against P. aeruginosa superior to Chloramphenicol, and showed comparable activity with Chloramphenicol against E. coli (ATCC25922).

• Bulletin of the Korean Chemical Society
• /
• 제31권12호
• /
• pp.3684-3692
• /
• 2010

A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to $25\;{\mu}g/mL$, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: $25\;{\mu}g/mL$, $50\;{\mu}g/mL$ and $100\;{\mu}g/mL$ in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.