• Title/Summary/Keyword: CA(1-8)-ME(1-12)

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Effects of the Hinge Region of Cecropin A(1-8)-Melittin 2(1-12), a Synthetic Antimicrobial Peptide on Antibacterial, Antitumor, and Vesicle-Disrupting Activity

  • Shin, Song-Yub;Kang, Joo-Hyun;Jang, So-Yun;Kim, KiI-Lyong;Hahm, Kyung-Soo
    • BMB Reports
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    • v.32 no.6
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    • pp.561-566
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    • 1999
  • CA(1-8)-ME(1-12) [CA-ME], composed of cecropin A(1-8) and melittin(1-12), is a synthetic antimicrobial peptide having potent antibacterial and antitumor activities with minimal hemolytic activity. In order to investigate the effects of the flexible hinge sequence, Gly-Ile-Gly, of CA-ME on antibiotic activity, CA-ME and three analogues, CA-ME1, CA-ME2, and CA-ME3, were synthesized. The Gly-Ile-Gly sequence of Ca-ME was deleted in CA-ME1 and replaced with Pro and Gly-Pro-Gly in CA-ME2 and CA-ME3, respectively. CA-ME1 and CA-ME3 showed a significant decrease in antitumor activity and phospholipid vesicle-disrupting ability. However, CA-ME2 showed similar antitumor and vesicle-disrupting activities, as compared with CA-ME. These results suggest that the flexibility or ${\beta}$-turn induced by Gly-Ile-Gly or Pro in the central part of CA-ME may be important in the electrostatic interaction of the N-terminus cationic ${\alpha}$-helical region with the cell membrane surface and the hydrophobic interaction of the C-terminus amphipathic ${\alpha}$-helical region with the hydrophobic acyl chains in the cell membrane. CA-ME3 exhibited lower antitumor and vesicle-disrupting activities than CA-ME and CA-ME2. This result suggests that the excessive ${\beta}$-turn structure caused by the Gly-Pro-Gly sequence in CA-ME3 seems to interrupt ion channel/pore formation in the lipid bilayer. We concluded that the appropriate flexibility or bilayer. We concluded that the appropriate flexibility or ${\beta}$-turn structure provided by the central hinge is responsible for the effective antibiotic activity of the antimicrobial peptides with the helix-hinge-helix structure.

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Antibacterial Activities of Peptides Designed as Hybrids of Antimicrobial Peptides

  • Shin, Song-Yub;Kang, Joo-Hyun;Lee, Myung-Kyu;Hahm, Kyung-Soo
    • BMB Reports
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    • v.29 no.6
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    • pp.545-548
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    • 1996
  • CA(1-8)ME(1-12), the CA-ME hybrid peptide of the amino terminal segments of cecropin A (CA) and melittin (ME), has been reported to have a broad spectrum and improved potency without a hemolytic property. In order to obtain new synthetic peptides with powerful antibacterial activity without hemolytic activity, several hybrid peptides were designed from the sequences of CA, ME, magainin 2, bombinin and lactoferricin. All hybrid peptides were constructed to form an amphipathically basic-flexible-hydrophobic structure and synthesized by the solid phase method. Their hemolytic activities against human red blood cells and antibacterial activities against both Gram-positive and Gram-negative bacteria were detennined. CA(1-8)MA(1-12), CA(1-8)BO(1-12), MA(10-17)ME(1-12) and LF(20-29)ME(1-12) showed comparable activities with broad spectra against both Gram-positive and Gram-negative bacteria relative to CA(1-8)ME(1-12) but without hemolytic properties. These hybrid peptides, therefore, could be useful as model peptides to design a novel peptide with improved antibacterial activity and study on structure-activity relationships of antimicrobial peptides.

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Antifungal Mechanism of Antifungal Peptide Derived from Cecropin A(1-8)- Melittin(1-12) Hybrid against Aspergillus fumigatus

  • Lee, Dong-Gun;Jin, Zhe-Zhu;Maeng, Cheol-Young;Shin, Song-Yub;Seo, Moo-Yeol;Kim, Kil-Lyong;Hahm, Kyung-Soo
    • Journal of Microbiology and Biotechnology
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    • v.9 no.2
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    • pp.168-172
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    • 1999
  • The antifungal mechanism of the antifungal peptide against Aspergillus fumigatus, $K^{18,19}$-CA(l-8)-ME(l-12), derived from cecropin A(l-8)-melittin(l-12) was investigated by confocal laser scanning microscopy, cell wall regeneration, ATPase activity inhibition, and released potassium ion. By confocal laser scanning microscopy, $K^{18,19}$-CA(l-8)-ME(l-12) was detected on the surface of A. fumigatus, while cecropin A used as a negative control peptide was not detected. The protoplast of A. fumigatus treated with$K^{18,19}$-CA(1-8)-ME(1-12) failed to regenerate the fungal cell walls. Compared with cecropin A, the amount of potassium ion released by $K^{18,19}$-CA(l-8)-ME(l-12) was increased. Furthermore, $K^{18,19}$-CA(l-8)-ME(l-12) inhibited the ATPase activity on the plasma membrane. These results suggested that $K^{18,19}$-CA(l-8)-ME(1-12) acts on the plasma membrane of A. fumigatus and its antifungal action is due to the ion channel or pore formation on the plasma membrane.

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Melittin-Hybrid 합성 펩타이드가 Fusarium oxysporum의 성장에 미치는 저해효과

  • Lee, Dong-Gun;Shin, Song-Yub;Lee, Sung-Gu;Lee, Myung-Kyu;Hahm, Kyung-Soo
    • Microbiology and Biotechnology Letters
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    • v.24 no.5
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    • pp.529-533
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    • 1996
  • Melittin (ME) from honeybee venom has a broad range of strong antimicrobial activity, but it has hemolytic activity against eukaryotic cells. In order to design peptides with powerful antifungal activity without cytotoxic property of ME and understand structure-antifungal activity relationships, the hybrid peptides derived from the sequences of ME and cecropin A (CA) or magainin 2 (MA), MA(10-17)ME(1-12) and CA(1-8)ME(1-12). were synthesized by solid phase method. MA(10-17)ME(1-12) showed potent antifungal activity comparable to ME against Fusarium oxysporum with no hemolytic activity against human red blood cells. The hybrid peptides showed strong inhibi- tion of (1, 3)-$\beta$-D-glucan synthase. This result indicates that the antifungal activity of the hybrid peptides against Fusarium oxysporum is attributed to the inhibition of cell wall synthesis. The results therefore showed a successful design of a peptide having antifungal activity without hemolytic property.

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Effect of Nitrogen Rate on the Ionic Balance and the Variance with Leaf Sequance in Mulberry (Morus alba L.) Leaves (시용질소양이 상엽중 이온 균형 및 엽위별 변화에 미치는 영향)

  • 이운주
    • Journal of Sericultural and Entomological Science
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    • v.24 no.2
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    • pp.43-54
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    • 1983
  • In a field trial, the influence was studied by measurement of growth and leaf yields and chemical composition (in organic cations and anions and total nitrogen) with two nitrogen dressings (lower nitrogen treatment 25kg and higher nitrogen treatment 75kg urea/10a as the summer fertilizer) after the summer cutting. The results were as follows; 1. With increasingn nitrogen dressing, branch length and weight were enchanced. The fresh weight of leaves was higher to be 273.6kg/10a in the higher nitrogen treatment than in the lower nitrogen treatment on 20 September. 2. The moisture content of leaves lasted above 73% until on 30 August. Afterward it decreased sharply upto 63% on 20 September. In higher nitrogen treatment it was higher about 0.1∼1.8% than in lower nitrogen treatment. The increasing nitrogen dressings combined with leaf condition led to be soft until on 10 October. 3. Dry matter weight of leaves started decreasing around on 10 September, whereas that of branches increased until around 30 September indicating that the dry matter moved to branch and root from leaves. 4. The increase in Ca$\^$2+/ content was particularly evident, whereas the K$\^$+/ and Mg$\^$2+/ decreased with growth. The Ca$\^$2+/ content was much higher in the high nitrogen treatment than in the low nitrogen treatment. 5. With rapid decrease in total nitrogen and water in the leaves around the end of August, the Ca$\^$2+/ and Cl$\^$-/ which were higher in the lower part moved up to the upper part. Whereas the K$\^$+/, H$_2$PO$_4$$\^$-/ and SO$_4$$\^$2-/ which were higher in the upper part moved down to the lower part. 6. Total nitrogen content decreased sharply 3,200me/kg DM to 2,000me/kg DM at the end of August changing the maxmium content of total nitrogen from upper to lower part in the low nitrogen treatment on 12 September and in the high nitrogen treatment on 22 September, and an apex of branches was died and fallen 10 days after respectively. 7. The sum of cation in leaves (∑C) increased from 1400me/kg DM to 1600me/kg DM with growth, wherease that of anions (∑A) was approximatly the same during the whole growing season. As the result, the ionic balance (C-A) increased from 1000me/kg DM to 1200me/kg DM. 8. ∑C, ∑A and (C-A) were higher in the high nitrogen treatment than in the low nitrogen treatment due to be much higher of Ca$\^$2+/ content and higher of NO$\^$-/$_3$, SO$\^$2-/$_4$ and H$_2$PO$_4$$\^$-/ content.

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Studies on the Mulberry Sapling 1. Soil Characteristics of Nursery Garden Producing Nonsprouting Sapling. (뽕나무 접목묘에 관한 연구 I. 활착불량상묘 발생 묘포지의 토양특성에 관한 연구)

  • Lee, Won-Ju;Jeong, Gwang-Yeong;Kim, Yeong-Taek
    • Journal of Sericultural and Entomological Science
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    • v.27 no.1
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    • pp.12-17
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    • 1985
  • soil survey and chemical analysis on mulberry nursery garden were carried out to study the causes of the non-sprouting phenomenon occured seriously in Buy and Ogchun in 1983 and Sangju in 1984. In addition, 115 nursery garden soils taken from 21 sapling produsers in Chungbuk province were analyzed in 1984. The results were as follows, 1. Symptom of dead saplings was the highest in boron deficiency by 59% and the lowest in rot symptom. The rest of saplings by 34.9% were not detected any symptom. 2. The nursery gardens showen non-sprouting phonomenon were located along the stream. As the result, soil depth was shallow, around 20cm deep and subsoil composed with coarse sand and gravels. 3. Nursery soils were mostly strong acid, low in Ca and Mg content, especially B, whereas available phosphorus and potassium were abundant at some gardens, and deficient at others. 4. Application of red earth or borax to nursery garden, especially to paddy, increased sprouting rate. 5. Paddy nursery garden occupied by 52.8% of 60.8ha of total garden area in Chungbuk province. Ninty point five percent of the nursery garden was lower in pH than 6.5, 87.0% lower in K than 0.5me/100g, 40.8% lower in Ca than 6.5me/100g, 94.8% lower in Mg the 2.00me/100g 99.1% lower in B than 0.3ppm.

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Effect of Split Diets on Laying Performance and Egg Quality in Layers (산란계 사료의 오전, 오후 분리 급여 효과)

  • 이상진;김상호;강보석
    • Korean Journal of Poultry Science
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    • v.25 no.2
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    • pp.71-77
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    • 1998
  • This study was investigated to study split diets on laying performance and eggshell quality with Hy-Line brown layers 43 weeks old for 12 weeks Layers fed a conventional diet and split diets were divided into morning and afternoon diet. The conventional diet contained 3.4 % Ca was given constant nutrients all day. Hens of the split diets fed morning diets contained 0.5 % Ca constantly and afternoon diets contained 5.9, 8.0, and 10.0 % Ca in T1to T3. Split diets were given morning diets from 04:00 to 15:00 and afternoon diets 15:00 to 21 :00 alternately. Egg production, egg weight, and egg mass were not significantly different among diets. Abnormal eggs decreased in T1 and T2, but no significantly differed(P>0.05). Feed intake decreased in all of split diets compared to control diets (P <0.05). So, feed conversion ratio also improved in split diets(P<0.05). ME and CP intake decreased in T2 and T3, and Ca intake increased in proportion to Ca content of diets(P<0.05). ME and CP requirements per kg eggs decreased in the split diets, and that of Ca increased. Although there were not different significantly, egg shell strength and thickness improved slightly in T2 at 12 week. Yolk color, haugh unit and yolk index were not different among diets. Therefore, we concluded that split diet feeding to layer could improve feed and economic efficiency with normal egg production.

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Synthesis of trans-(3R,5S)-Atorvastatin Ca and Curative Effect on Hyperlipidemia Induced by a High-Fat Diet in Rats (trans-(3R,5S)-Atorvastatin Ca의 합성 및 Rat에서 고지방식이로 유도된 고지혈증 치료효과)

  • Choi, Won-Sik;Nam, Seok-Woo;Lee, Gyung-Rak
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.12 no.11
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    • pp.4940-4950
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    • 2011
  • cis-(3R,5R)-Atorvastatin Ca (1) used for hyperlipidemia have four stereomers. However, It is very difficult to prepare stereoselective stereomers. In this paper, the reduction of 3,5-diketo atorvastatin ester (3) was performed using $Me_4NHB(OAc)_3$ in acetic acid as a reductant and showed excellent stereoselectivity in the double reduction of 3,5-diketo atorvastatin ester (3). As a result, reduction of compound 3 by $Me_4NHB(OAc)_3$ was purely obtained with cis-(3R,5R)-atorvastatin ester (4) of 1.5% and trans-(3R,5S)-atorvastatin ester (5) of 98.5%. Also, cis-(3R,5R)-atorvastatin Ca (1) and trans-(3R,5S)-atorvastatin Ca (7) were used to determine efficacy in the treatment of liver damage and hyperlipidemia induced by a high-fat diet in rats and to study the performance of the January 2010 experient was conducted. As a result, total cholesterol (TC), high-density lipoprotein-cholesterol (HDL-c), low-density lipoprotein-cholesterol (LDL-c), and triglyceride (TG) levels of compound 1 and 7 groups were $93.0{\pm}0.5$, $43.5{\pm}0.8$, $40.4{\pm}1.4$, $45.6{\pm}0.9\;mg/d{\ell}$ and $110.0{\pm}0.7$, $33.3{\pm}0.6$, $65.8{\pm}1.9$, $54.8{\pm}1.2\;mg/d{\ell}$, respectively. Atherogenic index (AI) and cardiac risk factor (CRF) in compound 1 and 7 were $1.14{\pm}0.05$, $2.14{\pm}0.05$ and $2.31{\pm}0.06$, $3.31{\pm}0.06$, aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were $51.9{\pm}4.6$, $16.0{\pm}2.1\;IU/{\ell}$ and $75.8{\pm}4.4$, $35.1{\pm}9.7\;IU/{\ell}$. Taken together, while compound 1 treat against high-fat diet-induced hyperlipidemia by attenuating hepatic lipid depots and reducing oxidative stress, compound 7 group had a low curative effect on hyperlipidemia induced by a high-fat diet in rats. These findings suggest that new method about synthesis of stereoselective stereomers and indicate that it may consider using in a clinical trial.

Seasonal Changes in Nutritive Value of Some Grass Species in West Sumatra, Indonesia

  • Evitayani, Evitayani;Warly, L.;Fariani, A.;Ichinohe, T.;Fujihara, T.
    • Asian-Australasian Journal of Animal Sciences
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    • v.17 no.12
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    • pp.1663-1668
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    • 2004
  • This study was carried out to evaluate the potential nutritive value of commonly found grasses collected at native pasture in West Sumatra, Indonesia during dry and rainy seasons. Variables measured included chemical composition, in vitro digestibility, concentration of Ca, P and Mg, gas production and metabolizable energy (ME) content of the grasses. The results showed that species and season had significant effect on chemical composition and mineral concentration. Crude protein content in the dry season ranged from 6.5% (B. decumbens) to 14.4% (P. maximum) and increased slightly from 7.8% (B. decumbens) to 14. 8% (A. compressus) in the rainy season. Data on fiber fraction showed that grass contained more NDF, ADF and ADL in dry season than in rainy season. Data on mineral concentration showed that C. plectostachyus and P. maximum in dry season had higher Ca than those of other species, while in rainy season P. maximum had highest Ca concentration. In dry season, the DMD varied from 50. 4% (P.purpuphoides) to 59.1% (P. purpureum), while in rainy season ranged from 50.3% (A. gayanus) to 61.8% (P. purpureum). The potential and rate of gas production were significantly (p<0.05) affected by species and season. During dry season, potential of gas production ranged from 21.8 ml/200 mg (A. compressus) to 45.1 ml/200 mg (C. plectostachyus), while in rainy season it varied from 35.6 ml/200 mg (A. gayanus) to 47.5 ml/200 mg (P. purpureum). ME content of grasses varied from 6.0 to 8.3 MJ/kg in dry season and increased slightly from 6.4 to 8.6 MJ/kg in rainy season. Both in dry and rainy seasons, the highest ME content was occurred in P. purpureum and C. plectostachyus. In conclusion, nutritive value of the observed grasses in West Sumatra, Indonesia was relatively higher during rainy season compared with dry season. Pennisetum purpureum and Cynodon plectostachyus had the best nutritive value in both dry and rainy seasons.

Studies on the Acid Sulphate Soils - Effect of the Rice Plant Growth by Amounts of Lime Application on No-Percolation and Percolation - (산성(酸性) 유산염(硫酸鹽) 토양(土壤)에 관(關)한 연구(硏究) - 투수(透水)에 의(依)한 석회(石灰) 시용량(施用量)이 수도생육(水稻生育)에 미치는 영향(影響) -)

  • Ha, H.S.
    • Korean Journal of Soil Science and Fertilizer
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    • v.3 no.1
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    • pp.29-34
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    • 1970
  • This experiment was conducted to investigate the influence of amounts of lime dressed on the growth of rice by the treatment of percolation and nonpercolation in the acid sulphate soil. And also analysis of soil chemical components after treatment was carried out. The results obtained were summarized as follows: 1. In the initial stage of growth, number of tillers and plant length showed no distinct differences between the treatments of percolation and nonpercolation, but after August the effect of lime appeared and the percolation treatment was more effective than the nonpercolation. 2. Lime dressing affected good influence on the panicles, grain per panicles and the rate of grain formation, and the treatment of percolation showed better results than nonpercolation. 3. If the yield of rough rice in the control (nonpercolation and lime dressing) was 100, it was 194 in the treatment of nonpercolation 12me/100gr of lime dressed, 268 in the treatment of percolation-4me/100gr of lime and 315 in the 8me/100gr-percolation. 4. Lime dressing affected good influence on the control of Helminthosporium leaf spots. 5. In the case of lime dressing, amounts of available phosphate and soluble silicon dioxide were increased, but ferrous ion ($Fe^{{+}{+}}$) were decreased.

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