초록

간질환예방 및 암치료에 활용될 수 있는 물질을 도출하고자 alcohol dehydrogenase (ADH), S-adenosylhomocysteine hydrolase, Cytochrome 1A1, Cyt.3A4, xanthine oxidase, quinone reductase topoisomerase 등을 중심으로 효능 평가법을 확립함과 동시에 천연물 및 합성화합물을 중심으로 효능 을 실시하고자 하였음.

Abstract ▼

The aim of this study is providing lead compounds for treating or preventing liver diseases and cancer by screening of enzyme inhibitors. Target enzymes such as alcohol dehydrogenase, cytochrome 2E1, and s-adenosyiliomocysteine hydrolase were applied for liver disease, and approximately 15O natural

The aim of this study is providing lead compounds for treating or preventing liver diseases and cancer by screening of enzyme inhibitors. Target enzymes such as alcohol dehydrogenase, cytochrome 2E1, and s-adenosyiliomocysteine hydrolase were applied for liver disease, and approximately 15O natural product extracts derived from herbal medicines were evaluated for the inhibitory potentials. As a result, puerarin, mulberoside A, and rhaponticin were isolated as active lead compounds against ADH. S-adenosyiliomocysteine hydrolase was also considered as a potential target enzyme for hepatitis. In this study/ we developed for the enzyme assay system using HPLC analvsis for detection of S-aadenosyiliomocysteine in the reaction mixture. In addition, topoisomerase Plays an important role in DNA replication, and the enzyme activity 15 higher level in cancer cells compared to normal cells. Therefore, the enzyme inhibitors are considered as good candidates for anticancer agents. Several quinolinedione and naphthoquinone derivatives were synthesized for targeting of topoisomerase inhibitors and tested in cultured human lung and colon cancer cells. Further, based on the cytotoxic potential and relation of chemical structure, the information for the best-fitting molecular formular was provided using comparative molecular field analysis method. Xanthine oxidase and quinone reductase enzyme assays were also applied for the evaluation of natural products extracts and several extracts show potential inhibition as lead extracts.

목차 Contents

• 제1장 연구개발과제의 개요...7
• 제2장 국내외 기술개발 현황...8
• 제3장 연구개발수행 내용 및 결과...9
• 제4장 목표달성도 및 관련분야에의 기여도...24
• 제5장 연구개발결과의 활용계획...35
• 제6장 연구개발과정에서 수집한 해외과학기술정보...36
• 제7장 참고문헌...37