• Title/Summary/Keyword: Anti-microbial activity

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Synthesis and Biopharmaceutical Studies of Cefazolin Butyrolactone Ester, a Novel Prodrug of Cefazolin (Cefazolin Butyrolactone Ester의 합성 및 생물약제학적 연구)

  • 이진환;조행남;최준식
    • YAKHAK HOEJI
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    • v.47 no.5
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    • pp.331-338
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    • 2003
  • A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.

Flavone Biotransformation by Aspergillus niger and the Characterization of Two Newly Formed Metabolites

  • Mahmoud, Yehia A.-G.;Assawah, Suzan W.;El-Sharkawy, Saleh H.;Abdel-Salam, Amal
    • Mycobiology
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    • v.36 no.2
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    • pp.121-133
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    • 2008
  • Aspergillus niger isolated from Allium sativum was used at large scale fermentation (150 mg flavone/200ml medium) to obtain suitable amounts of the products, efficient for identification. Then spectral analysis (UV, IR, $^1H$-NMR, $^{13}C$-NMR) and mass spectrometry were performed for the two products, which contributed to the identification process. The metabolite (1) was identified as 2'-hydroxydihydrochalcone, and the metabolite (2) was identified as 2'-hydroxyphenylmethylketone, which were more active than flavone itself. Antioxidant activities of the two isolated metabolites were tested compared with ascorbic acid. Antioxidant activity of metabolite (1) was recorded 64.58% which represented 79% of the antioxidant activity of ascorbic acid, and metabolite (2) was recorded 54.16% (67% of ascorbic acid activity). However, the antioxidant activity of flavone was recorded 37.50% which represented 46% of ascorbic acid activity. The transformed products of flavone have anti-microbial activity against Pseudomonas aeruginosa, Aspergillus flavus and Candida albicans, with MIC was recorded $250{\mu}g/ml$ for metabolite (2) against all three organism and 500, 300, and $300{\mu}g/ml$ for metabolite (1) against tested microorganisms (P. aeruginosa, Escherichia coli, Bacillus subtilis, and Klebsiella pneumonia, Fusarium moniliforme, A. flavus, Saccharomyces cerviceae, Kluveromyces lactis and C. albicans) at this order.

Study of Distance Relationships among Domestic Radish (Raphanus sativus L.) by Analyzing its Anti-fungal Protein Gene. (항 곰팡이 단백질 유전자 분석에 의한 국내 무 품종간 유연성에 관한 연구)

  • Hwang, Cher-Won
    • Journal of Life Science
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    • v.17 no.9 s.89
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    • pp.1294-1297
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    • 2007
  • To define diversity of domestic radish, we analysis genetic relationship of anti-fungal protein genes from several domestic radish (Raphanus sativus L.) seeds. We have isolated from domestic radish (Baekwoon) anti-fungal protein named RAP[12]. In this report, we isolate RNAs and raw protein from radish seeds then, RT-PCR analysis was done with another known anti-fungal sequences of radish from Gene Bank/EMBL and anti-fun- gal, anti-yeast activity were done against Bot교tis cenerea, Saccharomyces cerevisiaeι Candida albicans with it's raw proteins. The anti-fungal activity was shown used all seeds but anti-yeast activity was shown only two seeds (Myungsan, Baekwoon). RT-PCR products (about 0.2 Kb) were not shown only two seeds. To identify the sequencing relationship of the domestic radish, we have cloned and sequenced RAP genes of the radish and analysis the sequence relationship with clustalw program. Thus we report the result that there are some different relationship between domestic radish and known other radish's anti- fungal protein[15].

Isolation of Antimicrobial Active Substance from Aristolochia tagala Champ. against Sclerotial Rot (Sclerotinia sclerotiorum) (이엽마두령(Aristolochia tagala Champ.)추출물로부터 균핵병 병원균(Sclerotinia sclerotiorum)에 대한 항균 활성물질 탐색)

  • Kim, Hyun-Sang;Shon, Jinhan;Choi, Yong-Hwa
    • Korean Journal of Organic Agriculture
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    • v.23 no.4
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    • pp.951-962
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    • 2015
  • To develop environment-friendly agricultural products with anti-microbial activity against Sclerotinia sclerotiorum as a pathogen of sclerotium disease, Aristolochia tagala Champ. was extracted by methanol and its extract was fractionated into several solvent fractions. The chloroform fraction, which showed the highest antimicrobial activity, was separated by column chromatography and obtained forty three subfractions. The forty three fractions were searched the anti-fungal activities by bioassay. The most active No. 26 subfraction was analyzed by GC-MS. Each mass spectra, corresponding to each peak of chromatogram, was compared to MS database of Wiley library. As a result, 2,4-di-tetra-butyl-phenol, 2-mono-palmitin, 1-mono-stearin were profiled as maine compounds in No. 26 subfraction. Bioassay using commercial 1-mono-stearin to test for the anti-microbial activity conformed the antimicrobial active compound. In conclusion, 1-mono-stearin identified from Aristolochia tagala Champ. was antimicrobial chemical against Sclerotinia sclerotiorum.

Enzymological Evaluation of Bowel Inflammation Inhibitory Activity and Intestinal Microbial Flora Improvement by Enzymatic Hydrolysate of Schizandrae Fructus (오미자 효소가수분해물에 의한 장내 세균총 개선 및 장관 염증 억제 효과의 효소학적 평가)

  • Ryu, Il-Hwan;Kwon, Tae-Oh;Lee, Kang-Soo;Yun, Yong-Gab
    • Korean Journal of Pharmacognosy
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    • v.38 no.4
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    • pp.363-371
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    • 2007
  • Schizandrae Fruits has been used as a traditional Oriental medicine for treatment of many stress-induced diseases. In the present study, we investigated inhibitory activity of enzymatic hydrolysate of Schizandrae fructus (SC-EX) in growth of tested intestinal microorganism and activity of bowel inflammation related enzyme. SC-EX was added to the proteose peptone-yeast extract-fildes (PYF) media to investigation the effect on the growth of type culture of intestinal microorganism. The growth of lactic acid bacteria such as Bifidobacterium species and Lactobacillus species was accelerated by more than 3% concentration of SC-EX. But, growth of harmfulness bacteria such as E.coli, Clostridium sp. Staphylococcus sp. Streptococcus sp. was inhibited by more than 3% concentration of SC-EX. Also, SC-EX was exhibited a concentration-dependent inhibitory activity of the bowel inflammation related enzymes. The SC-EX was showed 76% and 92% inhibitory activity of 5-lipoxygenase and cyclooygenase at 5% additional concentration respectively. Our results indicated that SC-EX may possess improvement effect on the intestinal flora and Anti-inflammatory effect on the bowel.

Physiological activities of leaf extract of Lonicera morrowii A.Gray, a plant native to Ulleungdo (울릉도 자생식물인 섬괴불나무(Lonicera morrowii A.Gray) 잎 추출물의 생리활성)

  • Lee, Eun-Ho;Park, Hye-Jin;Hong, Eun-Jin;Akhmadjon, Sultanov;Kim, Byung-Oh;Jung, Hee-Young;Kang, In-Kyu;Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • v.63 no.4
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    • pp.443-449
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    • 2020
  • This study was performed to investigate total phenolic contents, anti-oxidant, biological disease-related enzyme inhibitory, and anti-microbial effects of extracts of Lonicera morrowii leaves prepared with water and 40% ethanol. Anti-oxidative activities of the extracts increased in a dose-dependent manner and were very high even at low phenolic concentration. At phenolic concentrations ranging between 50 and 200 ㎍/mL, the water and ethanol extracts inhibited 39.34-76.35 and 47.53-99.83% of xanthine oxidase activity, 30.21-79.06, and 59.40-87.14% of angiotensin converting enzyme activity, and 59.81-80.35 and 36.06-63.58% of α-glucosidase activity, respectively. All inhibitory effect were increased in a dose-dependent manner. In the paper disc agar diffusion assay against seven microbes, L. morrowii extracts had anti-bacteria activities against Helicobacter pylori, Propionibacterium acne but no effect against other bacteria. These results indicate that the extracts from L. morrowii leaves have the possibility to be developed as a physiologically functional source for prevention of adult diseases.

Anti-oxidative Effect of Blueberry Duke Extract in Caenorhabditis elegans (블루베리 듀크 추출물의 예쁜꼬마선충 내의 항산화 효과)

  • Kim, Jun Hyeong;An, Chang Wan;Kim, Yeong Jee;Noh, Yun Jeong;Kim, Su Jin;Jeong, Seong-Yeop;Jeong, Do-Youn;Hwang, In Hyun;Kim, Dae Keun
    • Korean Journal of Pharmacognosy
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    • v.48 no.3
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    • pp.219-225
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    • 2017
  • We investigated the anti-oxidative effect of the blueberry duke (Vaccinium corymbosum L., Ericaceae) ethanol extract in Caenorhabditis elegans model. The ethanol extract of blueberry duke showed relatively significant DPPH radical scavenging and superoxide quenching activities. To prove antioxidant activity of the extract, we checked the activities of superoxide dismutase (SOD), catalase, intracellular ROS, and oxidative stress tolerance in C. elegans. In addition, to verify if the increased stress tolerance of C. elegans by treating with the extract was due to regulation of stress-response genes, we checked SOD-3 expression using a transgenic strain. As a consequence, the blueberry duke ethanol extract increased SOD and catalase activities of C. elegans, and reduced intracellular ROS accumulation in a dose-dependent manner. Besides, blueberry duke ethanol extract-treated CF1553 worms showed higher SOD-3::GFP intensity.

THE ANTIMICROBIAL EFFECT OF HORSERADISH (ARMORACIA RUSTICANA) ROOT EXTRACTS AGAINST OBLIGATE ANAEROBES IN ROOT CANAL (치근관 내 편성 혐기성 세균에 대한 서양산 고추냉이 뿌리 추출물의 항균효과)

  • Lee, Won-Ju;Park, Ho-Won;Shin, Il-Sik;Lee, Ju-Hyun;Seo, Hyun-Woo
    • Journal of the korean academy of Pediatric Dentistry
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    • v.36 no.2
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    • pp.237-244
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    • 2009
  • When the symptom of periapical infection is not released by mechanical instrumentation. anti-microbial agents including antibiosis become necessary in order to remove microorganisms from the root canal. Since anti-microbial agents of natural origins are currently popular, more natural remedies are being sought out. As it turns out, it is well known isothiocyanates (ITCs) in horseradish root extract have anti-microbial activity from many studies. In this research, anti-microbial effects of horseradish root extract and chlorhexidine, a typical anti-microbial agent, were investigated and compared against two kinds of obligate anaerobes. Fusobacterium nucleatum and Prevotella nigrescens, that are often discovered in infected root canal, and Clostridium perfringens, which is resistant to antibiotics and frequently used as a control strain for antibacterial studies 1. The MIC and MBC of horseradish root extract were ranged from 87 to 470 ppm and from 156 to 625 ppm against three kinds of obligate anaerobes, respectively. Horseradish root extract showed the strongest anti-bacterial activity (MBC, 156 ppm) against F. nucleatum and also showed anti-bacterial activity against antibiotic resistant obligate anaerobes. C. perfringens. 2. The MIC and MBC of chlorhexidine were ranged from 3.12 to 6.25 ppm and 10.94 ppm against three kinds of obligate anaerobes, respectively. 3. The MIC with 87-470 ppm of horseradish root exact has the same growth inhibiting effect as the one of 3.12-6.25 ppm of chlorhexidine. Likewise, the MBC with 156-625 ppm of horseradish has the similar bactericidal effect as 10.94 ppm of chlorhexidine.

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Changes of Physiological Activity by Drying Temperature in Leaf of Eriobotrya japonica (건조온도에 따른 비파 잎의 생리활성 변화)

  • Eom, Hyo-Jin;Kim, Sun-Min;Pyo, Byoung-Sik;Lee, Kyoung-In
    • Korean Journal of Pharmacognosy
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    • v.40 no.3
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    • pp.178-183
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    • 2009
  • In DPPH radical and nitric oxide scavenging ability, the extract of lowest temperature condition(40-15H ; 15 hours at $40^{\circ}C$ for drying) exhibited highest activity. The total phenolic and flavonoid contents of each extracts were found to be $120.4{\sim}193.3\;mg$/g and $86.91{\sim}94.55\;mg$/g respectively. It is shown that 40-15H was the highest content in each compound. In antimicrobial activity, a lower drying temperature conditions were found to be more strong activities in disc diffusion assay and each extracts showed MIC of identical level against every tested microbial strains. However 100-2H(2 hours at $100^{\circ}C$ for drying) was exhibited MIC of slightly low level against some strains. And every extract showed fine cell viabilities($101.7{\sim}122.9%$) against RAW 264.7 cell. In anti-proliferation activity against AGS, each extract showed a similar inhibition activity. However in anti-proliferation activity against HeLa, a lower drying temperature conditions showed more strong activities.