• Title/Summary/Keyword: Control derivatives

Search Result 409, Processing Time 0.025 seconds

Synthesis of combinatorial library of $\beta$-ketoacetoanilide chlorides and their antifungal activity against main plant pathogens ($\beta$-Ketoacetoanilide 염화물의 조합 라이브러리 합성 및 주요 식물병원균에 대한 항균활성)

  • Hahn, Hoh-Gyu;Nam, Kee-Dal;Bae, Su-Yeal;Yang, Bum-Seung;Lee, Seon-Woo;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
    • /
    • v.8 no.1
    • /
    • pp.8-15
    • /
    • 2004
  • A synthesis of new $\beta$-ketoacetoanilide chloride derivatives and anti fungal activity of these compounds library against 6 typical plant pathogens were described. Reaction of ketene dimer with chlorine followed by treatment of aniline derivatives gave 89 kinds of the corresponding $\beta$-ketoacetoanilide chlorides through combinatorial synthetic technology using Carousel Reaction Stations. Evaluation of antifungal activity (in vivo) of this chemical library against rice blast, rice sheath blight, tomato aray mold, tomato late blight, wheat leaf rust and barley powdery mildew was carried out. In general, $\beta$-ketoacetoanilide chlorides which present a substituent at 4 in phenyl group(para) of the compounds showed selective control activity against tomato late blight caused by Phytophthora infestans.

Effects of the Administration of 5-aryl-2,3-dihydroimidazol [2,1-a] isoquinolines (SDZ-62434) on Kidney

  • Yi, E.Y.;Ma, Y.;Choi, W.J.;Park, J.S.;Cheon, S.H.;Lim, D.K.
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1996.04a
    • /
    • pp.213-213
    • /
    • 1996
  • The effects of the anti-tumor agent, SDZ-y2434, on rat kidney were investigated to predict the toxicities of its derivatives and to develope less toxic derivatives. After adjusted in metabolic cages for 5 days, rats were treated SDZ-62434(acute : 25mg/kg, i.p, once and 50mg/kg, i.p., once; subacute ; 10mg/kg, i.p., daily for 7 days). Kidney weights and urine volume during the treatment were observed. Creatinine concentration, protein concentration and the activities of N-acetyl-${\beta}$-D-glucosaminidase (NAG), alanine aminopeptidase (AAP), ${\gamma}$-glutamyl transpeptidase (GGT) and lactate dehydrogenase(LDH) in 24 hr urine were also determined. The kidney weights after the acute and subacute administration didn't show any difference. Urine volume increased 5 days after the acute administration (50mg/kg) and 3 days after the subacute administration. The excretion of creatinine was increased 5 days after the acute (50mg/kg) and subacute administration. However, the protein excretion didn't show any change. NAG acivity declined 7 days after the subacute administration. AAP and GGT activites increased 3 days after the acute administration (50mg/kg) but, returned to the control value. LDH activity showed continuousely high value after the subacute administration. These results indicates that the acute administration of SDZ-62434 might damage on glomerulus and that the subacute administration might be cytotoxic to kidney cells.

  • PDF

Anti-Angiogenic Activity of Mouse N-/C-terminal deleted Endostatin

  • Cho, Hee-Yeong;Kim, Woo-Jean;Lee, Sae-Won;Kim, Young-Mi;Choi, Eu-Yul;Park, Yong-Suk;Kwon, Young-Guen;Kim, Kyu-Won
    • BMB Reports
    • /
    • v.34 no.3
    • /
    • pp.206-211
    • /
    • 2001
  • Endostatin, a proteolytic fragment of collagen XVIII, is a potent inhibitor of angiogenesis and the growth of several primary tumors. However, the opinions on the activity of endostatin derivatives deleted N- or C- terminal are still controversial. In this regard, we produced mouse endostatin and its derivatives in the prokaryotic system, and studied their anti-tumor activity. The [$^3H$]-thymidine incorporation assay demonstrated that N-terminal deleted mouse endostatin, and a C- and N-terminal deleted mutant, effectively inhibited the proliferation of human umbilical vein endothelial cells (HUVECs). The biological activity of endostatin was also shown by its in vivo anti-angiogenic ability on the chorioallantoic membrane (CAM) of a chick embryo. Treatment of $200\;{\mu}g$ of mouse endostatin, or N-terminal deleted mouse endostatin, inhibited capillary formation of CAM 45 to 71%, which is comparative to a 80% effect of positive control, $1\;{\mu}g$ of retinoic acid. An in vivo mouse tumor growth assay showed that N-terminal deleted mouse endostatin, and the N-/C-terminal deleted mutant, significantly repressed the growth of B16F10 melanoma cells in mice as did the full-length mouse endostatin. According to these results, N-and N-/C-terminal deleted mouse endostatins are the potent inhibitors of tumor growth and angiogenesis.

  • PDF

Antimicrobial Activity of Oleanolic Acid for Foodborne Bacteria (식중독 세균에 대한 Oleanolic Acid의 항균활성)

  • Choi, Kyoung-Hee;Kim, Sejeong;Yoon, Yohan
    • Journal of Food Hygiene and Safety
    • /
    • v.30 no.1
    • /
    • pp.98-102
    • /
    • 2015
  • Oleanolic acid and its derivatives are pentacyclic triterpene acids, which are produced in many plants and herbs. These are considered safe and thus, oleanolic acid is now used for cosmetic and pharmaceutical industry. Oleanolic acid affects peptidoglycan in cell wall of bacteria. Hence, the antimicrobial activity of oleanolic acid is not very obvious to Gram-negative bacteria such as Escherichia coli, Yersinia enterocolitica, Shigella flexneri, and Shigella sonnei because the peptidoglycan is covered with outer membrane. However, oleanolic acid derivatives showed improved antimicrobial activity to Gram-negative bacteria. For Gram-positive bacteria such as Staphylococcus aureus and Listeria monocytogenes, oleanolic acid was very effective on reducing the cell counts of the pathogens. In addition, the cytotoxicity of oleanolic acid for human cell lines was minimal. Therefore, oleanolic acid should be considered as an antimicrobial food additive and a therapeutic agent to control foodborne pathogens.

Impact of Foreign Currency Derivative Usage on Firm Value (외환파생상품사용이 기업가치에 미치는 영향)

  • Jeon, Sang-Won;Kang, Shin-Ae
    • The Journal of the Korea Contents Association
    • /
    • v.12 no.3
    • /
    • pp.285-294
    • /
    • 2012
  • Under conditions of increasing environmental uncertainty, firms' risk management become important. This study examines the impact of foreign currency derivative usage on firm value using 3,004 Korean non-financial firms from 2002 to 2007. The results showed that there was no significant relationship between foreign currency derivative usage and firm value for the whole period and from 2002 to 2004 when exchange rate was relatively less volatile. But form 2005 to 2007 when exchange rate was volatile, foreign currency derivative usage gave significant negative impact on firm value, whereas when contract value was used, the relatinship was significantly positive. These results might be come from the characteristics of contract value and fair value of foreign currency derivatives. increased firm value when contract value was used as foreign currency derivative usage measure. But when fair value was used, there was no significance. For control variables, major shareholders ownership and foreign blockholders ownership was positively related with firm value.

Forced Oscillation Wind Tunnel Test of a 50m Length Airship (50M급 비행선의 강제진동 풍동시험)

  • Chang,Byeong-Hee;Lee,Yung-Gyo;Ok,Ho-Nam
    • Journal of the Korean Society for Aeronautical & Space Sciences
    • /
    • v.31 no.6
    • /
    • pp.17-22
    • /
    • 2003
  • An airship is statically unstable, because it has no wing, relatively small tails and a large hull. Hence, an accurate prediction of dynamic stability is critical. In this study, dynamic stability data of the 50m Length Airship were acquired through forced oscillation wind tunnel tests. The tests were done in Birhle Applied Research Inc's Lange Amplitude Multi-Purpose(BAR LAMP) Facility located in Germany. The tests were composed with 16 static runs and 26 dynamic runs. As results, it is obtained that dynamic characteristics of the airship depend on the sideslip angle, the angular rate and its direction as well as the angle of attack. Generally, three directional moments have damping, but the normal force, the side force, and the cross-derivatives are unstable. The dynamic derivatives are not sensitive to the control surfaces, but nonlinear to the sideslip angle.

EFFECTS OF NOVEL DITHIOL MALONATE DERIVATIVES ON LIVER LIPID PEROXIDATION AND ON MICROSOMAL ELECTRON TRANSPORT SYSTEM

  • Park, Keun-Hee;Lee, Jong-Wook
    • Toxicological Research
    • /
    • v.3 no.2
    • /
    • pp.97-110
    • /
    • 1987
  • The effects of 5 novel hepatotrophic agents, dithiol malonate derivatives (DMDs; DMD1-DMD5), on the liver microsomal lipid peroxidation induced by carbon tetrachloride $(CCl_4)$ and the correlations with the changes of microsomal electron transport system were investigated. All DMDs were found to inhibit the lipid peroxidation induced by $CCl_4$ in mice and rats as well in vitro liver microsomal system. Therefore, each DMD seemed to have direct mode of action on liver microsomes to inhibit the lipid peroxidation. As an ex vivo study, the induced lipid peroxidation by $CCl_4$ and the changes in electron transport system were determined with liver microsomes obtained from rats chronically treated with DMDs for 7 days. The induced lipid peroxide contents in liver microsomal system were lower in DMD1, DMD2 and DMD3 treated group, but higher in DMD4 and DMD5 group when compared to the control group. Cyt. p.450 contents in the microsomes were decreased by the treatment with DMD1, DMD2 and DMD3, but increased significantly by DMD4 with great extent and by DMD5 with less extent. The cyt. p-450 isozymes induced by treatment of DMD4 and DMD5 were identified as 3-methylcholanthrene (MC) type. The NADPH cyt. -C reductase activities of the microsomes treated with DMD1, DMD2, DMD4 and DMD5 were increased in the range of around 20% to 50%, but decreased with DMD3, All DMDs increased dyt. $-b_5$ content and did not alter NAdH-cyt, $-b_5$ reductase activities in the microsomes. In summary, the 5 novel hepatotrophic agents (DMDs) markedly protected against lipid peroxidation induced by $CCl_4$ in vivo and in vitro possibly through the mechanism of direct action on the liver microsomes. The degree of inhibition produced by DMDs on lipid peroxidation induced by $CCl_4$ seemed to coincide rather with cyt. p-450 contents than with other components of liver microsomal electron transport system including NADPH-cyt, -C reductase.

  • PDF

Preparation of Trifluoroacetyl Chitosan Derivatives with Antiviral Activity (항바이러스 활성을 갖는 Trifluoroacetyl Chitosan 유도체의 제조)

  • Kim, Chun-Ho;Shin, Cha-Gyun;Shin, Kye-Sook;Son, Tae-il
    • Applied Chemistry for Engineering
    • /
    • v.10 no.4
    • /
    • pp.599-602
    • /
    • 1999
  • Chitosan was depolymerized by using nitrous acid. In order to synthesize new fluorinated chitosan oligomer(FCO) derivative, free amine groups of resulting low molucular weight chitosan oligomers were reacted with trifluoroacetic anhydride. The structure changes in the samples were conformed by using FT-IR, $^{1}H\;NMR$, $^{13}C\;NMR$ and $^{19}F\{^{1}H\}NMR$. Antiviral activity of FCO was studied by measuring DAN amounts of the replication viruses at 36 hr after the cells were infected with the viral solution containing FCO of various concentrations. The viral replications in the cells infected with the viral solution containing FCO were proportionally decreased with the FCO does, compared to those of the control groups, indicating that FCO efficiently inhibits viral infection. In particular, viral replication was decreased to 40% in the 1% FCO-treated cells.

  • PDF

Control of Drug Release from Polymeric Matrices Coated with Poly(DL-lactide) I. Effect of Coasting Substance on the Drug Release in pH 1.2 Hydrochloride Solution (Poly(DL-lactide)로 피막된 고분자 매트릭스로부터 약물 방출 조절 I. pH 1.2 염산 용액에서 피막물질이 약물방출에 미치는 영향)

  • 나재운;박영훈
    • KSBB Journal
    • /
    • v.14 no.3
    • /
    • pp.297-302
    • /
    • 1999
  • The polymeric matrices coated with poly(DL-lactide) were prepared using chitosan derivatives such as chitosan, chitosan hydrochloride, and sulfonated chitosan for application of drug delivery systems. The drug release study using prednisolone as a model drug was performed in the hydrochloride solution at pH 1.2. The release rate of drug was decreased according to the increased content of matrices. The release rate of prednisolone according to the kinds of polymeric matrices coated were decreased in the order to chitosan, sulfonated chitosan, and chitosan hydrochloride. Drug release rate of polymeric matrices coated with poly(DL-lactide) was not only two times slower than noncoated one, but also the burst effect of initial period of drug release was decreased in comparison with noncoated one. From these results, it was expected that these formulations based on the chitosan derivative matrices coasted with poly(DL-lactide) were acceptable drug delivery devices for a sustained-release dosage form of drug.

  • PDF

Acute Toxicity Assessment of New Algicides of Thiazolidinediones Derivatives, TD53 and TD49, Using Ulva pertusa Kjellman

  • Yim, Eun-Chae;Park, In-Taek;Han, Hyo-Kyung;Kim, Si-Wouk;Cho, Hoon;Kim, Seong-Jun
    • Environmental Analysis Health and Toxicology
    • /
    • v.25 no.4
    • /
    • pp.273-278
    • /
    • 2010
  • Objectives : This study was aimed to examine the acute toxicity assessment of two new algicides, thiazolidinediones derivatives (TD53 and TD49), which were synthesized to selectively control red tide, to the marine ecosystem. Methods : The assessment employed by a new method using Ulva pertusa Kjellman which has been recently accepted as a standard method of ISO. The toxicity was assessed by calculating the $EC_{50}$ (Effective Concentration of 50%), NOEC (No Observed Effect Concentration) and PNEC (Predicted No Effect Concentration) using acute toxicity data obtained from exposure experiments. $EC_{50}$ value of TD49 and TD53 was examined by 96-hrs exposure together with Solutol as a TD49 dispersing agent and DMSO as a TD53 solvent. Results : $EC_{50}$ value of TD53 was $1.65\;{\mu}M$. From the results, values of NOEC and PNEC were calculated to be $0.63\;{\mu}M$ and 1.65 nM, respectively. DMSO under the range of $0{\sim}10\;{\mu}M$, which is same solvent concentration used in examining TD53, showed no toxic effect. $EC_{50}$ value of TD49 was $0.18\;{\mu}M$ and that of Solutol was $1.70\;{\mu}M$. NOEC and PNEC of TD49 were $0.08\;{\mu}M$ and 0.18 nM, respectively and those for Solutol were $1.25\;{\mu}M$ and 1.25 nM, respectively. Conclusions : From the values of NOEC, PNEC of TD53 and TD49, TD49 showed 9 times stronger toxicity than TD53. On the other hand, DMSO showed no toxicity on the Ulva pertusa Kjellman, but Solutol was found to be a considerable toxicity by itself.