• Toxicological Research
• /
• v.28 no.1
• /
• pp.51-56
• /
• 2012

A novel synthetic hexapeptide (SFKLRY-$NH_2$) that displays angiogenic activity has been identified by positional scanning of a synthetic peptide combinatorial library (PS-SPCL). This study was carried out to investigate the irritation of the SFKLRY-$NH_2$ on the skin. The tests were performed on the basis of Korea Food and Drug Administration (KFDA) guidelines. In results, cell toxicity is not appeared for SFKLRY-$NH_2$ in HaCaT cells and B16F10 cells. SFKLRY-$NH_2$ induced no skin irritation at low concentration ($10{\mu}m$), mild irritation at high concentration (10mM). We consider that this result is helpful for saying about the safety of SFKLRY-$NH_2$ in clinical use.

• BMB Reports
• /
• v.38 no.3
• /
• pp.334-342
• /
• 2005

Recently, the existence of T cells with dual T cell receptor (TCR) in the immune system is generally accepted, while it has been controversial whether signals through one TCR would affect the functions of the other. In this study T cells expressing two different TCR were obtained from cross-hybrids of LCMV and AND TCR transgenic mice specific for the gp33 and peptide fragment of PCC (fPCC), respectively. Peptide stimulation demonstrated that the dual TCR T cells functioned independently in an antigen-specific manner. To examine whether the tolerance targeted for the one TCR affects the responsiveness of the other, the cross-hybrids were treated with gp33. Although T cells from F1 mice were rendered anergenic to gp33, no functional changes to fPCC were observed in terms of cellular proliferation and IL-2 secretion, suggesting that the dual TCR T cells remained reactive to fPCC. We therefore propose that signaling through the TCR is receptor-specific and 'negative dominance' of one TCR by tolerance induction is not applicable in this dual TCR system.

• Microbiology and Biotechnology Letters
• /
• v.28 no.4
• /
• pp.195-201
• /
• 2000

Glucoamylase of Saccharomyces diastaticus is produced as a large precursor composed of signal peptide (21 amino acid residues), Thr and Ser-rich region and functional glucoamylase. To evaluate the utility of the glucoamylase signal peptide (GSP) for the secretion of foreign proteins, four types of GSP mutants (ml : Pro-18 longrightarrowLeu-18, m2 : Tyr-13 longrightarrowLeu, m3 : Ser-9longrightarrowLeu-9, m4 : Asn-5 longrightarrowPro-5) were constructed and secretion efficiency of each mutant was compared with that of native GSP by the expression and secretion of Bacillus subtilis CMCase under the control of GAP in N-terminal domain and hydrophobic domain. n mutant 4, a polar amino acid was replaced by a helix - breaking Pro residue. CMCase activity assay and Western blot analysis revealed that CMCase secretion by GSP mutants replaced by Leu were increased compared with native GSP. In the case of m2 and m3, the substitution of Leu for Tyr-13 and Ser-9 in the hydrophobic region resulted in a twofold increase in the extracellular CMCase activity.

• Journal of Microbiology and Biotechnology
• /
• v.22 no.10
• /
• pp.1367-1374
• /
• 2012

Pleurocidin, a 25-mer antimicrobial peptide, has been known to exhibit potent antibacterial activity. To investigate the functional roles in N- and C-terminal regions of pleurocidin on the antibacterial activity, we designed four truncated analogs. The antibacterial susceptibility testing showed that pleurocidin and its analogs exerted antibacterial effect against various bacterial strains and further possessed specific activity patterns corresponding with their hydrophobic scale [pleurocidin > Anal 3 (1-22) > Anal 1 (4-25) > Anal 4 (1-19) > Anal 2 (7-25)]. Fluorescence experiments using 1,6-diphenyl-1,3,5-hexatriene (DPH) and 3,3'-dipropylthiadicarbocyanine iodide [$diSC_3(5)$] indicated that the differences in antibacterial activity of the peptides were caused by its membrane-active mechanisms including membrane disruption and depolarization. Blue shift in tryptophan fluorescence demonstrated that the decrease in net hydrophobicity attenuates the binding affinity of pleurocidin to interact with plasma membrane. Therefore, the present study suggests that hydrophobicity in the N- and C-terminal regions of pleurocidin plays a key role in its antibacterial activity.

• Journal of the Korean Applied Science and Technology
• /
• v.28 no.4
• /
• pp.438-448
• /
• 2011

Chitosan is widely used in cosmetics and medical fields. Special emphasis has been put on the chemical modification of chitosan to explore its full potential. We have described the synthesis and biological activity of novel peptide amino acid derivatives. The polyamino acid derivatives were synthesized by introducing alkylamine functional group on chitosan at C-6. The poor aqueous solubility of chitosan derivatives hinder both pharmacological studies and pharmaceutical development. To make amino acid coupled chitosan derivatives with improved biological effect and solubility, some attempts have been taken to consist of amino peptide group like aspartic acid and phenylalanine-aspartic acid derivatives onto chitosan C-6. The resultingly substituted chitosan was characterized by solubility in various solvents. We measured chitosan derivatives with $^1H$-NMR and $^{13}C$-NMR. Also, We were investigated on the physical properties and biological activities of these products.

• Proceedings of the Korean Society of Food Hygiene and Safety Conference
• /
• 2003.11a
• /
• pp.46-46
• /
• 2003

Hypocholesterolemic peptide isolated from glycimin (11S protein) hydrolyzate by trypsin was purified and identified as LPYP and IAVPGEVA. To investigate the effects of phyiscal properties of side chains of the hypocholesterolemic activity, some of mutant peptides were designed and synthesized chemically. The structure related structures of each peptide were simulated and constructed and their conformations were observed by using spectropolarimeter. The hypocholesterolemic activities were monitored by assaying the inhibition of 3-hydroxy-3-methylglutaryl CoA reductase (HMG-CoA reductase) in vitro and by the determination of cholesterol content in mice serum. For LPYP derivatives, Hypocholesterolemic activity was lost when hydrophobic leucine residue at N-terminus was not so critical for maintaining hypocholesterolemic activity. For idealogical design of hypocholesterolemic peptides, the structure of HMG-CoA reductase are shown and inhibition mechanism of some peptides or inhibitors will be presented. For IAVPGEVA derivative inhibition of HMG-CoA reductase has been studied. For detail study of hypocholesterolemic activity, kinetic study of inhibition of peptides on HMG-CoA reductase and structural view of ligand binding should be investigated.

• Bulletin of the Korean Chemical Society
• /
• v.20 no.9
• /
• pp.1073-1077
• /
• 1999

CRAMP, a 37-amino acid cationic antimicrobial peptide was recently deduced from the cDNA cloned from mouse femoral marrow RNA. In order to investigate the structure-activity relationship and functional region of CRAMP, CRAMP and its 18-mer overlapping peptides were synthesized by the solid phase method. CRAMP showed broad spectrum antibacterial activity against both Gram-positive and Gram-negative bacterial strains (MIC: 3.125-6.25 μM) but had no hemolytic activity until 50 μM. CRAMP was found to have a potent anticancer activity (IC50: 12-23 μM) against two human small cell lung cancer cell lines. Furthermore, CRAMP was found to display faster bactericidal rate in B. subtilis rather than E. coli in the kinetics of bacterial killing. Among 18-meric overlapping fragment peptides, only CRAMP (16-33) displayed potent antibacterial activity (MIC: 12.5-50 μM) against several bacteria with no hemolytic activity. Circular dichroism (CD) spectra anal-ysis indicated that CRAMP and its analogues will form the amphipathic α-helical conformation in the cell membranes similar to other antimicrobial peptides, such as cecropins and magainins.

• Bulletin of the Korean Chemical Society
• /
• v.16 no.7
• /
• pp.591-594
• /
• 1995

The influence of protecting groups on the β-sheet-structure-stability of protected peptides was studied in organic solvents. α-amino groups, carboxyl groups and side chain functional groups of model peptides were protected by suitable groups commonly used in peptide synthesis. The difference of the solubilities of model peptides was investigated by the solvent-titration method by using IR absorption spectra. The β-sheet structure of model peptide in CH2Cl2 was easily disrupted by increasing the amounts of DMSO. The β-sheet-structure-stabilizing potentials of each protecting group showed similar behaviors except Npys, Mts and Z2. The result exhibits that the < SPβ > values of protected peptides are almost independent of the kinds of their protecting groups.

• Fisheries and Aquatic Sciences
• /
• v.22 no.5
• /
• pp.10.1-10.14
• /
• 2019

Fish skin waste accounts for part of the solid waste generated from seafood processing. Utilization of fish skin by bioconversion into high-grade products would potentially reduce pollution and economic cost associated with treating fish processing waste. Fish skin is an abundant supply of gelatin and collagen which can be hydrolyzed to produce bioactive peptides of 2-20 amino acid sequences. Bioactivity of peptides purified from fish skin includes a range of activities such as antihypertensive, anti-oxidative, antimicrobial, neuroprotection, antihyperglycemic, and anti-aging. Fish skin acts as a physical barrier and chemical barrier through antimicrobial peptide innate immune action and other functional peptides. Small peptides have been demonstrated to possess biological activities which are based on their amino acid composition and sequence. Fish skin-derived peptides contain a high content of hydrophobic amino acids which contribute to the antioxidant and angiotensin-converting enzyme inhibitory activity. The peptide-specific composition and sequence discussed in this review can be potentially utilized in the development of pharmaceutical and nutraceutical products.

• Journal of Pharmaceutical Investigation
• /
• v.25 no.4
• /
• pp.299-305
• /
• 1995

Cloning the gene encoding a dipeptide transporter is necessary for understanding the absorption mechanism of peptides and peptide-like drugs in the gastrointestinal tract. Functional expression of a dipeptide transporter after microinjection into Xenopus laevis oocytes was performed using the mRNA purified from human intestinal HT-29 cells. Fifty nanoliters of purified mRNA (1 mg/mL) were microinjected into healthy oocytes followed by incubation for 4 days in order to express a dipeptide transporter. Functional expression was determined by a uptake assay using 10 Ci/mL $[^3H]-glycylsarcosine$, a dipeptide substate of the transporter. Seasonal variability and batch-to-batch variability were greater in summer. The usage of beveled micropipettes improves viability of oocytes at 4 days after microinjection. Expression of a dipeptide transporter in oocytes after microinjection of mRNA obtained from HT-29 cells was significantly larger than those after microinjection of water or mRNA obtained from the rabbit intestine.