초록

○ 다양한 곤충 30종의 fibrin plate method 법에 의한 검정에서 딱정벌레목에서 울도하늘소가 가장 혈전 효과가 높았음
○ 흰점박이꽃무지 유충 유래 저분자 화합물 16종(신규화합물 1종) 규명
○ 갈색거저리 유충 유래 저분자 화합물 17종 규명
○ 벼메뚜기 유래 저분자 화합물 5종(신규화합물 2종) 규명
○ 흰점박이꽃무지 등 식용곤충 4종에서 혈전생성과 활성 억제 효과가 있었으며, 피브린 응집, 혈소판 응집 억제 효과가 있었음

(출처 : 보고서 요약서 3p)

Abstract ▼

□ Purpose& Contents
This study aimed to discover small antithrombotic molecules from this edible insect. these compounds inhibited
platelet aggregation. Antithrombotic effects of compounds 1 and 2 were further confirmed in pre-clinical models of pulmonary embolism and arterial thrombosis. Coll

□ Purpose& Contents
This study aimed to discover small antithrombotic molecules from this edible insect. these compounds inhibited
platelet aggregation. Antithrombotic effects of compounds 1 and 2 were further confirmed in pre-clinical models of pulmonary embolism and arterial thrombosis. Collectively, these results demonstrated that compounds could be effective antithrombotic agents and serve as new scaffolds for the development of antithrombotic drug.

□ Results
Protaetia brevitarsis seulensis (Kolbe) has been temporarily registered as a food material by the Ministry of Food and Drug Safety of Korea (MFDS). The current study aimed to discover small antithrombotic molecules from this edible insect. Five indole alkaloids, 5-hydroxyindolin-2-one (1), (1R,3S)-1-methyl-1,2,3,4-tetrahydro-b-carboline-3-carboxylic acid (2), (1S,3S)-1-methyl-1,2,3,4-tetrahydro-b-carboline-3-carboxylic acid (3), (3S)-1,2,3,4-tetrahydro-b-carboline-3-carboxylic acid (4) and L-tryptophan (5), were isolated from the insect. Among them, compounds 1 and 2 prolonged aPTT and PT and impaired thrombin and FXa generation on HUVEC surface. Moreover, these compounds inhibited platelet aggregation. Antithrombotic effects of compounds 1 and 2 were further confirmed in pre-clinical models of pulmonary embolism and arterial thrombosis. Collectively, these results demonstrated that compounds 1 and 2 could be effective antithrombotic agents and serve as new scaffolds for the development of antithrombotic drug. The edible grasshopper Oxya chinensis sinuosa is consumed worldwide for its various medicinal effects. The purpose of this study was to investigate potential bioactive antithrombotic and antiplatelet compounds from O. chinensis sinuosa. Five N-acetyldopamine dimers (1-5) were isolated from O. chinensis sinuosa and compounds 1 and 2 were identified as new chemicals with chiral centers at H-2 and H-3 of the benzo-1,4-dioxane structure. Compounds 1-4 were found to have both FXa and platelet aggregation inhibitory activities. These compounds inhibited the catalytic activity of FXa toward its synthetic substrate, S-2222, by noncompetitive inhibition, and inhibited platelet aggregation induced by ADP and U46619. Furthermore, compounds 1-4 showed enhanced antithrombotic effects, which were assessed using in vivo models of pulmonary embolism and arterial thrombosis. The isolated compounds also showed anticoagulant effects in mice. However, compounds 1-4 did not prolong bleeding time in mice, as shown by tail clipping. N-Acetyldopamine dimers, including two new stereoisomers 1 and 2, are novel antithrombotic compounds showing both FXa inhibition and antiplatelet aggregation activity with a low bleeding risk.

□ Expected Contribution
development of anticoagulants provided their therapeutic effects are established

(출처 : Summary 5p)

목차 Contents

• 표지 ... 1
• 제 출 문 ... 2
• 보고서 요약서 ... 3
• 국 문 요 약 문 ... 4
• Summary ... 5
• 목차 ... 6
• 제 1 장 연구 개발 과제의 개요 ... 7
• 제1절 연구 개발 목적 ... 7
• 제2절 연구 개발의 필요성 ... 7
• 제3절 연구 개발 범위 ... 7
• 제 2 장 국내외 기술개발 현황 ... 8
• 제 3 장 연구 수행 내용 및 결과 ... 9
• 제 4 장 목표달성도 및 관련분야 기여도 ... 79
• 제1절 목표대비 달성도 ... 79
• 제2절 정량적 성과(논문게재, 특허출원, 기타)를 기술 ... 80
• 제 5 장 연구 결과의 활용 계획 ... 80
• 제 6 장 연구 과정에서 수집한 해외 과학 기술 정보 ... 80
• 제 7 장 연구 개발 결과의 보안 등급 ... 80
• 제 8 장 국가과학기술종합정보시스템에 등록한 연구시설·장비 현황 ... 81
• 제 9 장 연구개발과제 수행에 따른 연구실 등의 안전조치 이행실적 ... 81
• 제 10 장 연구개발과제의 대표적 연구실적 ... 82
• 제 11 장 기타사항 ... 83
• 제 12 장 참고문헌 ... 84
• 끝페이지 ... 87