• Journal of Life Science
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• v.8 no.4
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• pp.410-415
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• 1998

Procine pepsin hydrolysis of hexapeptide L-S-pNF-Nle-A-OMe in the presence of dipeptide L-L generates a new peak on HPLC analysis of reaction mixtures that is not seen when enzyme is incubated with either peptide alone. The peaks can be detected spectroscopically at either 214 or 254 nm, the latter consistent with a new peptide containing the p-nitro-F residue. The data suggest acyl transpeptidation between E(L-S-pNF) and L-L to form L-S-pNF-L-L. Consistent with this inference are (1) the ability of L-L-NH$_{2}$ and inability of Boc-L-L to undergo a similar transpeptidation reaction, and (2) the data from electrospray mass spectrum. This synthesis requires that Nle-A-L-OMe be released before L-S-pNF, an order opposite to that proposed on the basis of product inhibition kinetics. Consistent with this inference are reciprocal solvent isotope effects ; normal isotope effects of 1.736$\pm$0.121 on the formation of Nle-A-L-OMe and 2.281$\pm$0.184 in the formation of L-S-pNF, coupled to an inverse isotope effects of 0.576$\pm$0.045 on the formation of L-S-pNF-L-L. Because transpeptidation precedes faster in D$_{2}$O, the isotopically-sensitive step must occur after release of Nle-A-L-OMe. Isotopically-enhanced transpeptidation is consistent with the Uni-Bi iso memchanism postulated on the basis of an isotope effects on Vmax but not on Vmax/Km$^{1)}$ and confirmed by isotope effects on the onset of inhibition by pepstatin$^{2)}$.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.44 no.4
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• pp.447-453
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• 2018

Acetyl hexapeptide 8 (AH8) is a synthetic peptide for anti-wrinkle cosmetics ingredient. It was developed as a mimetic of botox, patternd after N -terminal end of the protein synatosomal-associated protein 25 (SNAP25), a substrate of botulinum toxin. While AH8 has good efficacy and safety profiles, the permeation through the skin is poor. Therefore, we tried to enhance the transdermal delivery of AH8 by using of hyaluonic acid (HA), a linear polysaccharide of N-acetyl glucosamine and glucuronic acid. To investigate the effect of HA on AH8 penetration, we analyzed paraffin sections of $Micropig^{(R)}$ skin. Fluorescence labeled AH8 was applied to micropig skin with or without HA. The absorption of AH8 was limited to the stratum corneum (SC) without HA. On the other hand, AH8 penetrated to the dermis with HA. Especially, low molecular weight HA (5 kDa) was most efficient compared to 500 kDa HA and 2000 kDa HA. Experiments using fourier-transform infrared (FTIR) spectroscopy revealed that lower molecular weight HA had a tendency to increase the fluidity of the SC lipids more, which means enhancing the skin penetration. Therefore, HA could be expected to enhance the anti-wrinkle effect of AH8.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.49 no.4
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• pp.365-373
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• 2023

Since the lips are a representative facial part that can express human attraction, aesthetic interest in them has always existed in human history. However, as lips age, they tend to form wrinkles, become thinner, and lose their volume. To counteract this phenomenon, medical procedures such as fillers or fat transplantation have been suggested. In this study, we verified that the one of main effective material complex of L G H&H L IPCERIN^®, combination of cedrol, a sesquiterpene found in cedarwood, and three peptides (acetyl hexapeptide-8, acetyl tetrapeptide-9, and desamidocollagen) could ameliorate the photo-aging and reduce the wrinkles through in vitro experiments. The possibility of improving collagen and elastin expression in skin fibroblasts and reducing MMP expression under photoaging conditions was verified. In addition, it was confirmed that the amount of fat tissue in the lips can be increased by promoting adipose stem cell differentiation and increasing the amount of fat produced in the in vitro adipose stem cell differentiation experiment. Two weeks of human application tests confirmed that a combination of cedrol and peptides can improve the wrinkles, texture, elasticity, and volume of the lips. This study verified that the combination of cedrol and three peptides can be used as effective cosmetic materials to decrease the various signs of aging in the lips.

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

• Journal of Integrative Natural Science
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• v.9 no.4
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• pp.268-274
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• 2016

Filariasis causing nematode Brugia malayi is shown to harbor wolbachia bacteria as symbionts. The sequenced genome of the wolbachia endosymbiont from B.malayi (wBm) offers an unprecedented opportunity to identify new wolbachia drug targets. Hence the enzyme carbonic anhydrase from wolbachia endosymbiont of Brugia malayi (wBm) which is responsible for the reversible interconversion of carbon dioxide and water to bicarbonate and protons (or vice versa) is chosen as the drug target for filariasis. This enzyme is thought to play critical functions in bacteria by involving in various steps of their life cycle which are important for survival, The 3D structure of wBm carbonic anhydrase is predicted by selecting a suitable template using the similarity search tool, BLAST. The BLAST results shows a hexapeptide transferase family protein from Anaplasma phagocytophilum (PDB ID: 3IXC) having 77% similarity and 54% identity with wBm carbonic anhydrase. Hence the above enzyme is chosen as the template and the 3D structure of carbonic anhydrase is predicted by the tool Modeller9v7. Since the three dimensional structure of carbonic anhydrase from wolbachia endosymbiont of Brugia malayi has not yet solved, attempts were made to predict this protein. The predicted structure is validated and also molecular docking studies are carried out with the suitable inhibitors that have been solved experimentally.

• Biotechnology and Bioprocess Engineering:BBE
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• v.5 no.3
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• pp.153-158
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• 2000

Vancomycin belongs to the vancomycin-risocetin family of glycopeptides, and is a subclass of linear sugar containg peptides composed of seven amino acids. Its strochemical configuration forms the basic of a peptidoglycon monomer. The glycosylated hexapeptide chainconsists of chloro-$\beta$-hydroxytyrosines, p-hytidoglycines, N-anthylleucine and aspartic acid forms a rigid molecular frame work and gives the difficulty in the analysis. Voncomycin in the serum samples is usually estimated by liquid chromatography and the bacterial sensitivity was genereally tested by the microbiological assay. The pressent review deals with the qualitative, quantutative, microbioligical and immunological assays and the comparison of the quantitative methods. Clinical implications of vancomycin have also been cited in the review.

• Asian-Australasian Journal of Animal Sciences
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• v.15 no.5
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• pp.757-766
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• 2002

Growth hormone-releasing peptide-2 (GHRP-2, also named KP102) is a new hexapeptide of a series of synthetic growth hormone-releasing peptides (GHRPs) which stimulates the secretion of growth hormone (GH) in vitro and in vivo in several species including calf, sheep and pig. The GH-releasing activity of GHRP-2 is two to three times more effective than that of the original GHRP-6, and GHRP-1 in the rats and humans. To date, GHRP-2 seems to be the most potent member of the family of GHRPs. Since the GHRPs are short peptides (5-7 amino acid residues), they are synthesized easily and are not as readily degraded in plasma as GHreleasing hormone (GHRH). These features ameliorate their potential on domestic animals because of their chemical nature the GHRPs are efficacious when administered i.v. orally or orally. However, studies in cow, pig and sheep do not indicate such a close relationship between GHRH, somatostatin (SS) and GH, calling into question the general applicability of the human and rat models. Perhaps there is an important role for an endogenous GHRP in the regulation of GH secretion in domestic animals. This review provides an overview on the current knowledge of physiological role of GHRP-2 in domestic animals.

• Journal of Microbiology and Biotechnology
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• v.25 no.7
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• pp.1070-1083
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• 2015

A gene (GT-SM3B) encoding a thermostable secreted oligoendopeptidase (GT-SM3B) was cloned from the thermophile Geobacillus thermoleovorans DSM 15325. GT-SM3B is 1,857 bp in length and encodes a single-domain protein of 618 amino acids with a 23-residue signal peptide having a calculated mass of 67.7 kDa after signal cleavage. The deduced amino acid sequence of GT-SM3B contains a conservative zinc metallopeptidase motif (His⁴⁰⁰-Glu⁴⁰¹-X-XHis⁴⁰⁴). The described oligopeptidase belongs to the M3B subfamily of metallopeptidases and displays the highest amino acid sequence identity (40.3%) to the oligopeptidase PepF_Ba from mesophilic Bacillus amyloliquefaciens 23-7A among the characterized oligopeptidases. Secretory production of GT-SM3B was used, exploiting successful oligopeptidase signal peptide recognition by Escherichia coli BL21 (DE3). The recombinant enzyme was purified from the culture fluid. Homodimerization of GT-SM3B was determined by SDS-PAGE. Both the homodimer and monomer were catalytically active within a pH range of 5.0–8.0, at pH 7.3 and 40℃, showing the K_m, V_max, and k_cat values for carbobenzoxy-Gly-Pro-Gly-Gly-Pro-Ala-OH peptidolysis to be 2.17 ± 0.04 × 10^-6 M, 2.65 ± 0.03 × 10^-3 µM/min, and 5.99 ± 0.07 s^-1, respectively. Peptidase remained stable at a broad pH range of 5.0–8.0. GT-SM3B was thermoactive, demonstrating 84% and 64% of maximum activity at 50℃ and 60℃, respectively. The recombinant oligopeptidase is one of the most thermostable M3B peptidase, retaining 71% residual activity after incubation at 60℃ for 1 h. GT-SM3B was shown to hydrolyze a collagenous peptide mixture derived from various types of collagen, but less preferentially than synthetic hexapeptide. This study is the first report on an extracellular thermostable metallo-oligopeptidase.

• Proceedings of the KAIS Fall Conference
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• 2012.05a
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• pp.269-273
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• 2012

본 연구는 알려진 녹차의 다양한 항산화, 항염 효능이 있는 Polyphenol 류 이외의 생물학적 활성을 가지는 펩타이드 및 당단백질 소재에 대한 특성과 분석을 위하여 연구되었다. 녹차에서 수용성 성분을 추출 후 알콜 침전방법을 사용하여 단백질과 펩타이드류를 분리하여 실험에 사용하였다. 전체 추출물 중에는 Glutamic acid가 14073.9ug/g, (39.11%)로 가장 높게 분석되었으며, GPC 분석결과 Mn 886, Mw 25218, Mp 890, Mw/Mn 28.46으로 분석이 되었으며, 전체적으로 3개의 피크로 분석되었다. 함유된 펩타이드를 분석하기 위하여 HPLC를 이용하여 RT 16.148min의 Fraction을 분리하여 펩타이드 분석결과 녹차에서 유래한 TNTLSN이라는 hexapeptide를 동정하였다. 이러한 펩타이드는 친수성이며, 안정도가 높은 특징을 가지고 있고, 분자량이 1000이하로 피부 흡수도가 높을 것으로 기대되며, Biodegradable하며, Renewable 한 자연 친화적인 화장품 소재로서 널리 활용될 수 있을 것으로 판단된다.

• KSBB Journal
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• v.26 no.6
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• pp.483-490
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• 2011

Bioactive peptides (BAP) showed excellent cosmetic activity than bio-materials such as caffeic acid (CA), gallic acid (GA), and nicotinic acid (NA). Caffeoyl tripeptide-1 (CT-1) is a BAP that is stabilized with Gly-His-Lys (GHK) tripeptide and CA by using Fmoc solid phase peptide synthesis. Digalloyl tetrapeptide-19 (DT-19) is stabilized by combining Lys-Glu-Cys-Gly with GA and nicotinoyl tripeptide-1 (NT-1) is synthesized by GHK and NA. According to experiments, CT-1 has an excellent anti-oxidant function even with a very small amount of 10 ppm CT-1. DT-19's tyrosinase inhibition activity has the better effect of about 28.57% in 0.01% and 33.33% in 0.005% of concentration and about 7.89% in 0.001% concentration than vitamin-C. In addition, NT-1 is safer than the NA. Almost BAPs like pal-KTTKS, acetyl hexapeptide, and copper tripeptide-1 have the anti-wrinkle effect while DT-19 and NT-1 are applicable for potential BAPs focused on the whitening effect. The three kinds of BAPs like CT-1, DT-19, and NT-1 consisting of amino acids are safe to the skin, and have more excellent stability than bio-materials which are found to be unstable and cause skin irritation. Due to the high biological activity of BAP in the field of skin care, its utilization will increase constantly.