• 대한화장품학회지
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• 제46권1호
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• pp.81-88
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• 2020

Diesel particulate matter (DPM)은 피부각질세포에서 염증을 일으킨다. 또 aryl hydrocarbon receptor (AhR)을 통한 xenobiotic response element (XRE) promoter activity에 영향을 주어 cytochromeP (CYP) family의 발현을 촉진시킨다. 이 연구에서는 LG-HMC의 미세먼지 유발 피부 염증완화 및 XRE 발현 조절기능에 대하여 연구를 진행하였다. 먼저, HaCaT에서 DPM이 XRE promoter를 과활성화 시켜주는 것을 확인하였고, 이를 LG-HMC가 완화 시켜주는 것을 확인하였으며 이들 원료 중, 상백피추출물, 황금추출물이 XRE promoter의 과활성화 억제에 관여하는 것을 확인하였다. 이어, HaCaT에서 DPM에 의해 발현이 증가하는 염증성 사이토카인에 대해 LG-HMC 및 상백피추출물, 황금추출물이 염증성 사이토카인의 발현을 줄여주는 것을 확인하였다. 추가적으로 상백피추출물과 황금추출물이 DPPH 라디컬을 효과적으로 줄여줌으로써 미세먼지에 의한 라디컬 손상도 효과적으로 방어할 수 있는 소재임을 확인하였다. 결과적으로 LG-HMC가 미세먼지에 의한 피부염증완화와 피부방어효과를 갖는 것을 확인하였고, LG-HMC를 구성하는 상백피추출물과 황금추출물이 미세먼지에 의한 손상방어에 중요한 역할을 하는 것을 확인하였다.

• Bulletin of the Korean Chemical Society
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• 제32권8호
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• pp.2577-2583
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• 2011

We have designed a 20-residue hybrid peptide CA(1-8)-MA(1-12) (CAMA) incorporating residues 1-8 of cecropin A (CA) and residues 1-12 of magainin 2 (MA) with high bacterial cell selectivity. CAMA-P2 is an ${\alpha}$-helical antimicrobial peptide designed from a CAMA hybrid peptide and substitution of Gly-Ile-Gly hinge sequence of CAMA to Pro influences the flexibility at central part of CAMA. Based on structure-activity relationships of CAMA peptides, to investigate the effects of the total positive charges on antimicrobial activity of CAMA-P2, the $Ser^{14}{\rightarrow}$Lys analogue (CAMA-syn1) was synthesized. The role of tryptophan at C-terminal ${\alpha}$-helix on its antimicrobial activity as well as synergistic activity was also investigated using $Ser^{14}{\rightarrow}$Lys/$Phe^{18}{\rightarrow}$Trp analogue (CAMA-syn2). Also, we designed CAMA-syn3 by substitution of $Lys^{16}$ located opposite side of substituted $Lys^{14}$ of CAMA-syn1 with Leu residue, resulting in increase of hydrophobicity and amphipathicity of the peptide. All of CAMA-syn analogues showed good antimicrobial activities similar to those of CAMA and CAMA-P2. The CAMA-syn1 and CAMA-syn2 showed low hemolytic activity and cytotoxicity against human keratinocyte Haca-T cells while CAMA-syn3 showed hemolytic activity and cytotoxicity at its MIC value. We then investigated their abilities to act synergistically in combination with the antimicrobial flavonoids and synthetic compounds screened in our laboratory. The results showed that all peptides exhibited synergistic effects with dihydrobinetin, while only CAMA-syn2 exhibited synergistic effects with YKAs3001 against both S. aureus and MRSA, suggesting that Trp residue at C-terminus of CAMA-syn2 may facilitate the polar antibiotic flavonoids and synthetic compounds to permeabilize the membrane. This study will be useful for the development of new antibiotic peptides with potent antimicrobial and synergistic activity but without cytotoxicity.