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Improvement of Biological Activities of Chitin and Chitosan by Chemical Modification
Reports NRF is supported by Research Projects( Improvement of Biological Activities of Chitin and Chitosan by Chemical Modification | 2004 Year 신청요강 다운로드 PDF다운로드 | 제재영(부경대학교) ) data is submitted to the NRF Project Results
Researcher who has been awarded a research grant by Humanities and Social Studies Support Program of NRF has to submit an end product within 6 months(* depend on the form of business)
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  • Researchers have entered the information directly to the NRF of Korea research support system
Project Number F00006
Year(selected) 2004 Year
the present condition of Project 종료
State of proposition 재단승인
Completion Date 2006년 09월 01일
Year type 결과보고
Year(final report) 2006년
Research Summary
  • Korean
  • 키틴 및 키토산은 다양한 생리활성에도 불구하고 물에 용해되지 않아 그 이용에 제약이 있었다. 본 논문에서는 화학적 수식을 통한 수용성 키틴 키토산 유도체를 만들어 그들의 다양한 생리활성을 연구하였다. 키틴은 게껍질로부터 제조하였고 키틴을 40% 수산화나트륨을 처리하여 탈아세틸화도 다른 키토산을 제조하였다. 제조된 키틴 키토산의 기능성을 높이기 위해서 키틴 키토산의 C-6 위치에 다양한 치환 그룹을 도입하였고 FT-IR, 1H NMR 및 원소분석을 통하여 확인하였다. 수용성 키틴 키토산 유도체의 항균활성은 3종의 그램 양성균 및 그램 음성균에 대하여 측정한 결과, 아미노에틸-키틴 및 다이메틸아미노에틸-키토산의 활성이 다른 유도체보다 우수하였고, 이들의 항균활성은 시험된 박테리아의 종에 따라 다르게 나타났다. 또한 세포 외막과 내막의 투과성을 조사한 결과 빠른 시간에 세포막의 손상시켜 투과성을 높이는 것으로 나타났다. 항산화활성은 DPPH, 하이드록시, 수퍼옥사이드 및 알킬 라디칼을 이용하여 측정한 결과, 아미노에틸-키틴 및 키토산이 우수한 소거능을 나타내었다. 항고혈압 활성에 있어서는 수용성 키틴 키토산 중 아미노에틸기가 도입된 키틴 및 키토산 유도체들만 활성을 보였고 저해양상을 조사한 결과 경쟁적 저해를 하는것으로 나타났다. 고혈압쥐를 이용한 실험에서도 투여 후 3시간째에 가장 우수한 혈압강하 효과를 나타냄을 확인하였다. 알쯔하이머성 치매 질환 유발 인자인 β-secretase의 저해효과를 측정한 결과 키틴 유도체들은 어떠한 저해활성도 나타내지 못하였으나 키토산 유도체들은 저해활성을 나타내었고 그들 중 아미노에틸-키토산의 저해활성이 가장 우수함을 확인하였다. 또한 여러가지 암세포를 이용한 독성실험에서는 다이에틸아미노에틸이 치환된 키토산 유도체가 가장 우수한 세포독성을 나타내었다.
  • English
  • Water-soluble chitin and chitosan derivatives were prepared by chemical modification to overcome solubility problem that limits their utilization. Biological activities of the chemically modified chitin and chitosan were investigated. Chitin was purified from crab shells, and partially (90% or 50%) deacetylated chitins were prepared from chitin by N-deacetylation using 40% NaOH solution under optimum condition. Three different substituting groups were introduced on C-6 position of chitin and chitosan to potentially improve their functional properties, and the chemical structures of the modified derivatives were fully characterized by FT-IR, 1H NMR and elemental analysis.
    Antimicrobial activities of chitin and chitosan derivatives were investigated using three Gram-negative bacteria and three Gram-positive bacteria. AE-chitin, DMAE-chitosan (90%) and DMAE-chitosan (50%) showed lower minimum inhibitory concentration (MIC) values when compared to those of other derivatives. AE-chitin and DMAE-chitosan (90% and 50% deacetylated chitosan derivatives) showed outer and inner membrane permeabilization activity, but their activities were different when tested using chemical probes. Antioxidant activities of derivatives were investigated for 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical, hydroxyl, superoxide, alkyl radical, and hydrogen peroxide using electron spin resonance (ESR) spectroscopy. AE-chitin and AE-chitosan derivatives exhibited the strongest antioxidant activities for reactive oxygen species (ROS) and DPPH radical. Among the derivatives tested, only the derivatives substituted with AE-group exhibited angiotensin I converting enzyme (ACE) inhibitory activity and thus antihypertensive effect. ACE inhibitory patterns appeared to be competitive inhibition, and the inhibition constant (Ki) values of AE-chitin and AE-chitosan (50%) were 60 μg/mL and 6.5 μg/mL, respectively. Antihypertensive effects of these derivatives on spontaneously hypertensive rats (SHR) were observed as these derivatives significantly reduced systolic blood pressure (SBP) after administration. Among these derivatives tested only the chitosan derivatives showed inhibitory effect on β-secretase which is one of the key enzymes involved in Alzheimer disease. AE-chitosan (90%) showed the strongest β-secretase inhibitory activity, and the inhibitory pattern was found to be non-competitive. The determined inhibition constant (Ki) value was 85 μg/mL. In cytotoxic activities of chitosan derivatives, DEAE-chitosan (90%) showed the highest cytotoxic acitivity, and IC50 value was 15.6 μg/mL, 51 μg/mL, and 62.5 μg/mL against HeLa, A549, and HT1080 cell line. The mechanism of cytotoxic activity was related to hydrophobic ineraction between DEAE group and the tumor cell surface.
Research result report
  • Abstract
  • Water-soluble chitin and chitosan derivatives were prepared by chemical modification to overcome solubility problem that limits their utilization. Biological activities of the chemically modified chitin and chitosan were investigated. Chitin was purified from crab shells, and partially (90% or 50%) deacetylated chitins were prepared from chitin by N-deacetylation using 40% NaOH solution under optimum condition. Three different substituting groups were introduced on C-6 position of chitin and chitosan to potentially improve their functional properties, and the chemical structures of the modified derivatives were fully characterized by FT-IR, 1H NMR and elemental analysis.
    Antimicrobial activities of chitin and chitosan derivatives were investigated using three Gram-negative bacteria and three Gram-positive bacteria. AE-chitin, DMAE-chitosan (90%) and DMAE-chitosan (50%) showed lower minimum inhibitory concentration (MIC) values when compared to those of other derivatives. AE-chitin and DMAE-chitosan (90% and 50% deacetylated chitosan derivatives) showed outer and inner membrane permeabilization activity, but their activities were different when tested using chemical probes. Antioxidant activities of derivatives were investigated for 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical, hydroxyl, superoxide, alkyl radical, and hydrogen peroxide using electron spin resonance (ESR) spectroscopy. AE-chitin and AE-chitosan derivatives exhibited the strongest antioxidant activities for reactive oxygen species (ROS) and DPPH radical. Among the derivatives tested, only the derivatives substituted with AE-group exhibited angiotensin I converting enzyme (ACE) inhibitory activity and thus antihypertensive effect. ACE inhibitory patterns appeared to be competitive inhibition, and the inhibition constant (Ki) values of AE-chitin and AE-chitosan (50%) were 60 μg/mL and 6.5 μg/mL, respectively. Antihypertensive effects of these derivatives on spontaneously hypertensive rats (SHR) were observed as these derivatives significantly reduced systolic blood pressure (SBP) after administration. Among these derivatives tested only the chitosan derivatives showed inhibitory effect on β-secretase which is one of the key enzymes involved in Alzheimer disease. AE-chitosan (90%) showed the strongest β-secretase inhibitory activity, and the inhibitory pattern was found to be non-competitive. The determined inhibition constant (Ki) value was 85 μg/mL. In cytotoxic activities of chitosan derivatives, DEAE-chitosan (90%) showed the highest cytotoxic acitivity, and IC50 value was 15.6 μg/mL, 51 μg/mL, and 62.5 μg/mL against HeLa, A549, and HT1080 cell line. The mechanism of cytotoxic activity was related to hydrophobic ineraction between DEAE group and the tumor cell surface.
  • Research result and Utilization method
  • 키틴 및 키토산은 다양한 생리활성에도 불구하고 물에 용해되지 않아 그 이용에 제약이 있었다. 본 논문에서는 화학적 수식을 통한 수용성 키틴 키토산 유도체를 만들어 그들의 다양한 생리활성을 연구하였다. 키틴은 게껍질로부터 제조하였고 키틴을 40% 수산화나트륨을 처리하여 탈아세틸화도 다른 키토산을 제조하였다. 제조된 키틴 키토산의 기능성을 높이기 위해서 키틴 키토산의 C-6 위치에 다양한 치환 그룹을 도입하였고 FT-IR, 1H NMR 및 원소분석을 통하여 확인하였다. 수용성 키틴 키토산 유도체의 항균활성은 3종의 그램 양성균 및 그램 음성균에 대하여 측정한 결과, 아미노에틸-키틴 및 다이메틸아미노에틸-키토산의 활성이 다른 유도체보다 우수하였고, 이들의 항균활성은 시험된 박테리아의 종에 따라 다르게 나타났다. 또한 세포 외막과 내막의 투과성을 조사한 결과 빠른 시간에 세포막의 손상시켜 투과성을 높이는 것으로 나타났다. 항산화활성은 DPPH, 하이드록시, 수퍼옥사이드 및 알킬 라디칼을 이용하여 측정한 결과, 아미노에틸-키틴 및 키토산이 우수한 소거능을 나타내었다. 항고혈압 활성에 있어서는 수용성 키틴 키토산 중 아미노에틸기가 도입된 키틴 및 키토산 유도체들만 활성을 보였고 저해양상을 조사한 결과 경쟁적 저해를 하는것으로 나타났다. 고혈압쥐를 이용한 실험에서도 투여 후 3시간째에 가장 우수한 혈압강하 효과를 나타냄을 확인하였다. 알쯔하이머성 치매 질환 유발 인자인 β-secretase의 저해효과를 측정한 결과 키틴 유도체들은 어떠한 저해활성도 나타내지 못하였으나 키토산 유도체들은 저해활성을 나타내었고 그들 중 아미노에틸-키토산의 저해활성이 가장 우수함을 확인하였다. 또한 여러가지 암세포를 이용한 독성실험에서는 다이에틸아미노에틸이 치환된 키토산 유도체가 가장 우수한 세포독성을 나타내었다. 이상의 결과와 같이 본 연구에서 제조된 수용성 키틴 키토산은 항산화제, 항균제 및 항고혈압 등의 식품 및 의약품 원료로 사용 가능할 것으로 사료된다.
  • Index terms
  • chitin, chitosan, antioxidant, antimicrobial, enzyme inhibitor, cytotoxicity
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