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Whitening effect of novel peptide mixture by regulating melanosome biogenesis, transfer and degradation

  • Lee, Eung-Ji;Kim, Jandi;Jeong, Min Kyeong;Lee, Young Min;Chung, Yong Ji;Kim, Eun Mi
    • The Korean Journal of Physiology and Pharmacology
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    • v.25 no.1
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    • pp.15-26
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    • 2021
  • Peptides are short chain of amino acids linked by peptide bonds. They are widely used as effective and biocompatible active ingredients in cosmetic industry. In this study, we developed novel peptide mixture and identified its anti-pigmentation effect on melanocytes and keratinocytes. Our results revealed that peptide mixture inhibited melanosome biogenesis through the regulation of microphthalmia-associated transcription factor, a key factor of melanogenesis in melanocytes. And we observed that peptide mixture inhibited melanosome uptake through the reduction of protease-activated receptor 2, a phagocytosis-related receptor in keratinocytes. Furthermore, peptide mixture activated autophagy system resulting in degradation of transferred melanosomes in keratinocytes. The anti-pigmentation effect of multi-targeting peptide mixture was assessed in a human skin equivalent model (MelanoDerm). Melanin contents in epidermal layer were significantly decreased by topical treatment of peptide mixture, suggesting that it can be applied as a novel cosmetics material having a whitening function.

Peptide Micelles for Anti-cancer Drug Delivery in an Intracranial Glioblastoma Animal Model

  • Yi, Na;Lee, Minhyung
    • Bulletin of the Korean Chemical Society
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    • v.35 no.10
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    • pp.3030-3034
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    • 2014
  • Bis-chloroethylnitrosourea (BCNU) is currently used as an anti-cancer drug for glioblastoma therapy. In this study, BCNU was loaded into the hydrophobic cores of R3V6 amphiphilic peptide micelles for efficient delivery into brain tumors. The scanning electron microscope (SEM) study showed that the BCNU-loaded R3V6 peptide micelles (R3V6-BCNU) formed spherical micelles. MTT assay showed that R3V6-BCNU more efficiently induced cell death in C6 glioblastoma cells than did BCNU. In the Annexin V assay, R3V6-BCNU more efficiently induced apoptosis than did BCNU alone. Furthermore, the results showed that R3V6 was not toxic to cells. The positive charges of the R3V6 peptide micelles may facilitate the interaction between R3V6-BCNU and the cellular membrane, resulting in an increase in cellular uptake of BCNU. In vivo evaluation with an intracranial glioblastoma rat model showed that R3V6-BCNU more effectively reduced tumor size than BCNU alone. The results suggest that R3V6 peptide micelles may be an efficient carrier of BCNU for glioblastoma therapy.

Clinical Utility and Cross-Reactivity of Insulin and C-Peptide Assays by the Lumipulse G1200 System

  • Oh, Jongwon;Kim, Jae Hyeon;Park, Hyung-Doo
    • Annals of Laboratory Medicine
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    • v.38 no.6
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    • pp.530-537
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    • 2018
  • Background: Measurement of insulin and C-peptide concentrations is important for deciding whether insulin treatment is required in diabetic patients. We aimed to investigate the analytical performance of insulin and C-peptide assays using the Lumipulse G1200 system (Fujirebio Inc., Tokyo, Japan). Methods: We examined the precision, linearity, and cross-reactivity of insulin and C-peptide using five insulin analogues and purified proinsulin. A method comparison was conducted between the Lumipulse G1200 and Roche E170 (Roche Diagnostics, Mannheim, Germany) systems in 200 diabetic patients on insulin treatment. Reference intervals for insulin and C-peptide concentrations were determined in 279 healthy individuals. Results: For insulin and C-peptide assays, within-laboratory precision (% CV) was 3.78-4.14 and 2.89-3.35%, respectively. The linearity of the insulin assay in the range of 0-2,778 pmol/L was $R^2=0.9997$, and that of the C-peptide assay in the range of 0-10 nmol/L was $R^2=0.9996$. The correlation coefficient (r) between the Roche E170 and Lumipulse G1200 results was 0.943 (P <0.001) for insulin and 0.996 (P <0.001) for C-peptide. The mean differences in insulin and C-peptide between Lumipulse G1200 and the Roche E170 were 19.4 pmol/L and 0.2 nmol/L, respectively. None of the insulin analogues or proinsulin showed significant cross-reactivity with the Lumipulse G1200. Reference intervals of insulin and C-peptide were 7.64-70.14 pmol/L and 0.17-0.85 nmol/L, respectively. Conclusions: Insulin and C-peptide tests on the Lumipulse G1200 show adequate analytical performance and are expected to be acceptable for use in clinical areas.

Glucagon-like peptide-1 and glucagon-like peptide-1 receptor agonists in the treatment of type 2 diabetes

  • Lee, Seungah;Lee, Dong Yun
    • Annals of Pediatric Endocrinology and Metabolism
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    • v.22 no.1
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    • pp.15-26
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    • 2017
  • The prevalence of type 2 diabetes (T2D) is increasing worldwide. Patients with T2D suffer from various diabetes-related complications. Since there are many patients with T2D that cannot be controlled by previously developed drugs, it has been necessary to develop new drugs, one of which is a glucagon-like peptide-1 (GLP-1) based therapy. GLP-1 has been shown to ameliorate diabetes-related conditions by augmenting pancreatic ${\beta}-cell$ insulin secretion and having the low risk of causing hypoglycemia. Because of a very short half-life of GLP-1, many researches have been focused on the development of GLP-1 receptor (GLP-1R) agonists with long half-lives such as exenatide and dulaglutide. Now GLP-1R agonists have a variety of dosing-cycle forms to meet the needs of various patients. In this article, we review the physiological features of GLP-1, the effects of GLP-1 on T2D, the features of several GLP-1R agonists, and the therapeutic effect on T2D.

Complement C5a Receptor Signaling in Macrophages Enhances Trained Immunity Through mTOR Pathway Activation

  • Eun-Hyeon Shim;Sae-Hae Kim;Doo-Jin Kim;Yong-Suk Jang
    • IMMUNE NETWORK
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    • v.24 no.4
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    • pp.24.1-24.8
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    • 2024
  • Complement C5a receptor (C5aR) signaling in immune cells has various functions, inducing inflammatory or anti-inflammatory responses based on the type of ligand present. The Co1 peptide (SFHQLPARSRPLP) has been reported to activate C5aR signaling in dendritic cells. We investigated the effect of C5aR signaling via the Co1 peptide on macrophages. In peritoneal macrophages, the interaction between C5aR and the Co1 peptide activated the mTOR pathway, resulting in the production of pro-inflammatory cytokines. Considering the close associations of mTOR signaling with IL-6 and TNF-α in macrophage training, our findings indicate that the Co1 peptide amplifies β-glucan-induced trained immunity. Overall, this research highlights a previously underappreciated aspect of C5aR signaling in trained immunity, and posits that the Co1 peptide is a potentially effective immunomodulator for enhancing trained immunity.

Whitening Efficacy Study of Natural Compounds-Peptide Derivatives via cAMP Signaling Pathway (cAMP 신호전달과정을 통한 신규 천연유래물질 펩타이드 유도체의 미백 효능 연구)

  • Lee, Hye-Suk;Shin, Kyong-Hoon;Ryu, Geun-Seok;Jee, Kyung-Yup;Cho, In-Shik;Kim, Han-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.3
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    • pp.275-282
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    • 2011
  • Novel whitening agents were prepared using peptide-Natural origin compound derivatives. The peptide could be an antagonist of MC1R and Natural origin compound were well-known material as a Tyrosinase inhibitor. We also suggest the new assay method which could evaluate the Antagonistic effectiveness to MC1R using cAMP signaling pathway. 24 candidates were synthesized and 11 peptide derivatives were selected by cAMP assay method. To evaluate cAMP assay, the selected peptide derivatives were assayed to evaluate their melanogensis inhibitory activity. At this work, we could know that the sequences which include -RW- have a melanogensis inhibitory activity, and cAMP assy could use as a evaluating method of MC1R antagonist. But, to evaluate the whitening activity of some material, cross-checking with melanin inhibitory assay method was recommended.

Selection of Skin-Penetrating Peptide Using Phage Display (파지 디스플레이를 이용한 피부 투과 기능성 펩타이드의 개발)

  • Lee, Seol-Hoon;Kang, Nae Gyu;Lee, Sanghwa
    • YAKHAK HOEJI
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    • v.57 no.2
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    • pp.125-131
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    • 2013
  • Biologically active peptides, including growth factors and cytokines, participate in various biological processes in human skin. They could provide a great advantage of maintaining healthy skin. Many peptide growth factors like epidermal growth factor (EGF) and human growth hormone (hGH) have been used in cosmetic formulations. The delivery of peptide growth factors across the Stratum corneum, however, seems not sufficient because of their physical properties such as high molecular weight and hydrophilicity. So increasing the penetration of growth factors of interest into skin would be a major concern for ensuring their maximum biological efficacy. In this study, we have identified several skin penetration-enhancing peptides which facilitate delivery of growth factors, when fused at N-terminus of the target protein, into skin. For efficient and rapid screening, we constructed a skin-penetrating assay system using Franz cell and porcine skin. Next, we carried out phage display screening using M-13 bacteriophage with random 12 -amino acid library on its coat protein P3 on that system. After several selection rounds, peptide sequences facilitate the penetration of phages through the porcine skin were identified from a large population of phages. We found that phages with the most potent peptide (S3-2, NGSLNTHLAPIL) could penetrate the porcine skin eight times more than those with control peptide (12 mino acids scrambled peptide). Furthermore, growth factors conjugated with S3-2 peptide penetrate porcine skin three to five times efficiently than non-conjugated growth factors. In conclusion, our data shows that the skin penetration-enhancing peptide we have characterized could increase the delivery of growth factors and is useful for cosmeceutical application.

Growth hormone-releasing peptide-biotin conjugate stimulates myocytes differentiation through insulin-like growth factor-1 and collagen type I

  • Lim, Chae Jin;Jeon, Jung Eun;Jeong, Se Kyoo;Yoon, Seok Jeong;Kwon, Seon Deok;Lim, Jina;Park, Keedon;Kim, Dae Yong;Ahn, Jeong Keun;Kim, Bong-Woo
    • BMB Reports
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    • v.48 no.9
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    • pp.501-506
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    • 2015
  • Based on the potential beneficial effects of growth hormone releasing peptide (GHRP)-6 on muscle functions, a newly synthesized GHRP-6-biotin conjugate was tested on cultured myoblast cells. Increased expression of myogenic marker proteins was observed in GHRP-6-biotin conjugate-treated cells. Additionally, increased expression levels of insulin-like growth factor-1 and collagen type I were observed. Furthermore, GHRP-6-biotin conjugate-treated cells showed increased metabolic activity, as indicated by increased concentrations of energy metabolites, such as ATP and lactate, and increased enzymatic activity of lactate dehydrogenase and creatine kinase. Finally, binding protein analysis suggested few candidate proteins, including desmin, actin, and zinc finger protein 691 as potential targets for GHRP6-biotin conjugate action. These results suggest that the newly synthesized GHRP-6-biotin conjugate has myogenic stimulating activity through, at least in part, by stimulating collagen type I synthesis and several key proteins. Practical applications of the GHRP-6-biotin conjugate could include improving muscle condition. [BMB Reports 2015; 48(9): 501-506]