• Title/Summary/Keyword: ML-Agents

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Toxicological Analysis of the Entomopathogenic Nematode, Steinernema carpocapsae, and the Symbiotic Bacteria, Xenorhabdus nematophilus on Beneficial Insects and Mammals (유용곤충과 포유류에 대한 곤충병원선충(Steinernema carpocapsae)과 공생세균(Xenorhabdus nematophilus)의 독성)

  • Park, Young-Jin;Kim, Mi-Kyung;Kim, Jin;Yang, Kyung-Hyung;Kim, Yong-Gyun
    • Korean journal of applied entomology
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    • v.40 no.3
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    • pp.259-264
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    • 2001
  • Toxicological studies of two potential biological control agents, the entomopathogenic nematode (Steinernema carpocapsae) and the symbiotic bacteria (Xenorhabdus nematophilus) were conducted against two beneficial insects and one mammal species. Two microbial agents varied in their toxicities between two insect species: an ant, Pristomyrmex pungens, and silkworm, Bombyx mori. In oral toxicity test, the symbiotic bacteria resulted in significant lethal [half lethal concentration of $1.4$\times$10^3$colony-forming units (cfu)/ml] on the ants, while they gave little lethal effect (half lethal concentration of more than $10^{8}$ cfu/ml) on the silkworms. The nematodes, however, gave significant lethal effect [half lethal concentration of 4 infected juveniles (IJs)/ml] on the silkworms, while they did little lethal effect (half lethal concentration of 150,000 IJs/ml) on the ants in topical assays. Both the nematodes and the bacteria did not give lethal effect to the albino rats, Rattus norvegicus, when they were fed orally into the rats. Also, any of these microbial agents were not detected in the internal organs of the treated rats.

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Synthesis and Characterization of Some Quinazoline Derivatives as Potential Antimicrobial Agents under Microwave Irradiation

  • Mehta, Sarika;Swarnkar, Neelam;Vyas, Madhuri;Vardia, Jitendra;Punjabi, Pinki B.;Ameta, Suresh C.
    • Bulletin of the Korean Chemical Society
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    • v.28 no.12
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    • pp.2338-2343
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    • 2007
  • Under the framework of green chemistry, an efficient and extremely fast procedure for the synthesis of 5a-h through four-step procedure starting from 2-arylidenetetralin-1-one 1a-d under microwave irradiation is described. A considerable increase in the reaction rate has been observed with better yield. The structures of the synthesized compounds have been characterized on the basis of their elemental analysis and spectral data. Synthesized compounds 5a-h was evaluated for their antimicrobial activity. Some of the compounds exhibited appreciable activity.

Synthesis of Benzo[c]phenanthridine Derivatives and their in Vitro Antitumor Activities

  • Cho, Won-Jea;Yoo, Su-Jeong;Chung, Byung-Ho;Choi, Bo-Gil;Cheon, Seung-Hoon;Whang, Soon-Ho;Kim, Sin-Kyu;Kang, Boo-Hyon;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.19 no.4
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    • pp.321-325
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    • 1996
  • Aiming at the development of anticancer agents by modification of phenolic benzo[c]phenanthridine alkaloid, additional hydroxyl group was put on C10 position of fagaridine (1) by a biomimetic synthetic procedure to afford 10-hydroxyfagaridine (12). All of the synthetic intermediates were also screened in vitro antitumor activities against five different cell lines as well as 12. Among them the representative cytotoxic results are shown as follows; P-quinone (11) $[ED_50;(A549=0.22; {\mu}g/ml)$, $(HCT;15=0.21 {\mu}g/ml)$, fagaridine (1) $(HCT;15=0.41 {\mu}g/ml)$, olefin (6) $(HCT; 15=0.06 {\mu}g/ml)$, acetal (7) $(SKMEL-2=0.07 {\mu}g/ml)$, dihydrofagaridne (10) $(A549=0.38 {\mu}g/ml)$, 10-hydroxyfagaridine (12) $(A 549=0.45{\mu}g/mi)$. From these observation three main remarks can be drawn; (i) the iminium part of benzo[c]phenanthridine is not essential for showing acitvities, (ii) the additional hydroxyl group did not contribute to enhance the cytotoxicity, (iii) the 3-arylisoquinolin-1(2H)-one derivatives were found to display significant in vitro antitumor activity.

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Effects of Natural Products on the Induction of NAD(P)H: Quinone Reductase in Hepa 1c1c7 Cells for the Development of Cancer Chemopreventive Agents

  • Kim, Young-Mi;Chang, Il-Moo;Mar, Woong-Chon
    • Natural Product Sciences
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    • v.3 no.2
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    • pp.81-88
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    • 1997
  • NAD(P)H:quinone reductase (QR) is one of the protective phase II enzymes against toxicity that accomplishes the capacity of detoxification by modulating the effects of mutagens and carcinogens. The detoxification mechanism is that quinone reductase promotes the 2-electron reduction of quinones to hydroquinones which are less reactive. This study is to search new inducers of quinone reductase from natural products, which can be used as cancer chemopreventive agents. Plant extracts were evaluated by using quinone reductase generating system With Hepa 1c1c7 murine hepatoma cell lines for enzyme inducing properties and crystal violet staining method for the measurement of cytotoxicity provoked. We have tested approximately 106 kinds of natural products after partition into n-hexane, ethyl acetate and aqueous layers from 100% methanol extracts of natural products. The ethyl acetate fractions of Vitex rotundifolia $(fruits,\;2FC:\;12.7\;{\mu}g/ml)$, Cnidium officinale $(aerial\;parts,\;2FC:\;10.5\;{\mu}g/ml)$, Chrysanthemum sinese $(flowers,\;2FC:\;17.4{\mu}g/ml)$ and the hexane fractions of Angelica gigas $(roots,\;2FC:\;13.2\;{\mu}g/ml)$, Smilax china $(roots,\;2FC:\;l1.9\;{\mu}g/ml)$, Sophora flavescens $(roots,\;2FC:\;16.3\;{\mu}g/ml)$ revealed the significant induction of quinone reductase in a murine hepatic Hepa 1c1c7 cell culture system.

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Antiherpetic Activities of Natural Quercetin Alone and in Combinations with Nucleoside Antiherpetic Agents (천연 Quercetin의 항허피스바이러스작용과 Nucleoside계 항허피스바이러스제와의 병용효과)

  • Kim, Young-So;Han, Seong-Sun
    • Korean Journal of Pharmacognosy
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    • v.30 no.2
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    • pp.151-157
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    • 1999
  • In order to find less toxic antiherpetic agents, the effect of natural quercetin on the plaque formation of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) was studied in vitro in cell culture monolayers employing the technique of viral plaque reduction assay. Quercetin caused a concentration-dependent reduction in the plaque formation of herpesviruses. It also exhibited more potent antiherpetic activity on HSV-1 with effective concentration $(EC_{50})$ of $18.7\;{\mu}g/ml$ than on HSV-2 with $EC_{50}$ of $24.5\;{\mu}g/ml$. The combined antiherpetic effects of quercetin with nucleoside antiherpetic agents, acyclovir and vidarabine, were examined on the multiplication of these two strains of herpesviruses in Vero cells by the combination assay. The results of combination assay were evaluated by the combination index (CI) that was calculated by the multiple drug effect analysis. The combinations of quercetin with acyclovir on HSV-1 and HSV-2 showed more potent synergism with CI values of $0.19{\sim}0.89$ for 50%, 70%, 90% effective levels than those with vidarabine with CI values of $0.43{\sim}1.46$.

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Effect of Reducing Agents on Bifidobacterium Fermentation of Saccharified Rice Solution (환원제 첨가가 쌀당화액의 Bifidobacterium발효에 미치는 영향)

  • 이주연;목철균;박종현;장학길
    • Microbiology and Biotechnology Letters
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    • v.27 no.3
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    • pp.230-235
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    • 1999
  • This study was intended to develop a new rice product by the fermentation of saccharified rice solution using Bifidobacterium and to select an appropriate reducing agent to provide the anaerobic condition for the growth of Bifidobacterium during fermentation. The enhancement of the growth of Bifidobacterium in saccharified rice solution was achieved by the treatment of reducing agents such as ascorbic acid and cysteine. The physical and chemical properties of the fermented product were evaluated, and the effect of the reducing agents were compared between ascorbic acid and cysteine. The fermented product with the addition of ascorbic acid shows the lower pH and the higher titratable acidity comparing the product with the addition of cysteine. This indicated that ascorbic acid was more appropriate reducing agent than cysteine for the fermentation of the saccharified rice solution. The number of viable Bifidobacterium in the fermented product with the addition of ascorbic acid(2.2$\times$108~3.4$\times$108CFU/ml) was greater than that with the addition of cysteine (8$\times$107~2.8$\times$108CFU/ml). Ascorbic acid supplement also contributed better sensory properties, such as flavor, taste and overall acceptibility than cysteine supplement did.

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Antifungal Synergy of Theaflavin and Epicatechin Combinations Against Candida albicans

  • Betts, Jonathan W.;Wareham, David W.;Haswell, Stephen J.;Kelly, Stephen M.
    • Journal of Microbiology and Biotechnology
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    • v.23 no.9
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    • pp.1322-1326
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    • 2013
  • New antifungal agents are required to compensate for the increase in resistance to standard antifungal agents of Candida albicans, which is an important opportunistic fungal pathogen that causes minor infections in many individuals but very serious infections in those who are immune-compromised. In this study, combinations of theaflavin and epicatechin are investigated as potential antifungal agents and also to establish whether antifungal synergy exists between these two readily accessible and cost-effective polyphenols isolated from black and green tea. The results of disc diffusion assays showed stronger antibacterial activity of theaflavin:epicatechin combinations against C. albicans NCTC 3255 and NCTC 3179, than that of theaflavin alone. Minimum inhibitory concentrations (MICs) of 1,024 ${\mu}g/ml$ with theaflavin and 128-256 ${\mu}g/ml$ with theaflavin:epicatechin combinations were found. The fractional inhibitory concentration indexes were calculated, and the synergy between theaflavin and epicatechin against both isolates of C. albicans was confirmed. Theaflavin:epicatechin combinations show real potential for future use as a treatment for infections caused by C. albicans.

Antiherpetic Activities of Natural Quercitrin Alone and in Combinations with Nucleoside Antiherpetic Agents (천연 Quercitrin의 항허피스바이러스작용과 Nucleoside계 항허피스바이러스제와의 병용효과)

  • 김영소;어성국;김홍진;이도익;김기호;한성순
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.158-163
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    • 1999
  • In order to find less toxic antiherpetic agents, antiviral activities of quercitrin against two strains of pathogenic viruses such as herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) were determined in Vero cells using plaque reduction assay in vitro. Quercitrin showed a concentration-dependent decrease in plaque formation of HSV-1 and HSV-2. It also exhibited more potent antiherpetic activity on HSV-1 with 50% effective concentration (EC$_{50}$) of 20.4 $\mu$g/ml than on HSV-2 with EC$_{50}$ of 30.4 $\mu$g/ml. The combined antiherpetic effects of quercitrin with nucleoside antiherpetic agents, acyclovir and vidarabine, were examined on the multiplication of these two strains of herpesviruses in Vero cells by the combination assay. The results of combination assay were evaluated by the combination index (CI) that was calculated by the multiple drug effect analysis. The combinations of quercitrin with acyclovir and vidarabine on HSV-1 showed more potent synergism with CI values of 0.27-0.81 for 50%, 70%, 90% effective levels than those on HSV-2 with CI values of 1.03~2.20..20.

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Antibiotic Susceptibility Of Actinobacillus Actinomycetemcomitans From The Patients With Adult Periodontitis (성인형 치주염 환자에서 분린한 Actinobacillus actinomycetemcomitans의 항생재 내성에 관한 연구)

  • Na, Yong-Cheol;You, Hyung-Keun;Sihn, Hyung-Sik
    • Journal of Periodontal and Implant Science
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    • v.26 no.1
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    • pp.202-215
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    • 1996
  • The purpose of this study was to an in estigate the antibiotic susceptibiliity of Actinoobacillus actinomycetemcomitans isolated from the subgingival plaque to adult periodontitis. Seven bacterial strains were tested for their susceptibility to 10 antimicrobial agents under disk diffusion method and broth dilution methold, Seven patients with deep pocket(6mm) were selected for this study. They had not taken antibiotics for 6 months and no history of dental treatment for 6 months and no history of dental treatment for 6 months before this study. The results were as follows : 1. For the antibiotic disk diffusion method, seven A. actinimycetemcomitans were tested with 10 antimicrobial agents which comprised penicillin, gentamycin, clindamycin, lincomycin, ampicillin, erythromycin, tetracycline, amikacin, chloramphenicol, and vancomycin. The sensitive antibiotics were tetracycline, vancomycin, and chloramphenicol and the resistant antibiotics were clindamycin, and lincomycin. The other antimicrobial agents were less active. 2. From the study of determination on the minimal inhibitory concentration(MIC) by broth dilution method, the MIC of tetracycline to seven strains of the A. actinomycetemcomitans was $0.5-1.0{\mu}g/ml$, that of clindamycin was $32{\mu}g/ml$. These data suggest that tetracycline may be valuable drugs in the elimination of A. actinimycetemcomitans from the patients with adult periodontitis

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Isolation and Characterization of Antitumor Agents from Dictamnus albus

  • Kim, Se-Won;Yeo, Woon-Hyung;Ko, Young-Su;Kim, Si-Kwan
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.209-214
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    • 1997
  • This study was carried out to find new antitumor agents from plant resource. Three cytotoxic agents were isolated from the root of Dictamnus albus by hexane extraction, silica gel column chromatography and HPLC. They were identified to be dictamnine $(C_{12}H_9NO_2)$, preskimmianine $(C_{17}H_{21}NO_4)$ and fraxinellone $(C_{14}H_{16}O_3)$ on the basis of spectroscopic evidences. In this study, it was newly found that these compounds possess a cytotoxic activity against lung lymphoma L1210 cell line. Among them. Preskimmianine was the most potent against the lymphoma L1210 with a $IC_{50}$ of $3.125\;{\mu}g/ml\;(10.3\;{\mu}M)$. Toxicity of preskimmianine against normal Iymphocyte was observed at the concentration of $50\;{\mu}g/ml\;(165\;{mu}M)$. These results support the pharmacological role of D. albus, a herb known as Paeksun in Korea and used as an anticancer agent in folk medicine.

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