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인삼으로부터 Acyl-CoA

인삼으로부터 Acyl-CoA
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Studies on Acyl CoA : Cholesterol Acyltransferase Inhibitor isolated from the roots of Panax ginseng (Araliaceae) and It's derivatives
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대학원 약학과
이화여자대학교 대학원
인삼(Panax ginseng C. A. Meyer)은 오갈피나무과(Araliaceae)에 속하는 식물로 뿌리를 주로 약용으로 쓰며 한국, 일본, 중국에 있어서 가장 중요한 동양적 약용식물 중 하나이다. 알려진 용도는 중추신경조정기능, Antistress, 항염효과, 혈당강하작용, 면역적 약리활성, 항암효과, 혈청단백의 생합성 효과, 등의 약리학적 성질이 보고되었다. 인삼의 Polyacetylene 화합물은 항균작용이 있는 것이 많으나, 일반적으로 안정성 때문에 실용성이 적은 것으로 알려져 있으나, 인삼 뿌리의 petroleum ether 분획이 강하게 Cholesteryl Ester Transfer Protein을 저해한다는 보고에 흥미를 갖고 인삼의 Polyacetylene이 Acyl CoA:Cholesterol Acyltransferase 저해제로서 고콜레스테롤혈증과 동맥경화증 예방 및 치료에의 응용을 기대해 볼 수 있기에 인삼의 Polyacetylene물질을 분리하여, ACAT(Acyl CoA:Cholesterol Acyltransferase) 저해활성을 확인하였다. ACAT에 활성을 나타내는 물질을 UV, ^(1)H-NMR, ^(13)C-NMR, IR spectrum으로 분석한 결과 Panaxynol, Panaxydol, Panaxydiol, Panaxydol peroxide로 동정되었고, 이 물질들의 ACAT IC_(50)을 측정한 결과 각각 22.7㎍/㎖, 21.3㎍/㎖, 12.0㎍/㎖, 14.0㎍/㎖를 나타내었다. Panaxydol peroxide는 천연물에서 처음으로 분리되었다. 또한 ACAT 저해활성과 이 성분들의 구조와의 관련성을 알아보기 위해 유도체 9,10-epoxy-1-heptadecene-4,6-diyn-3-one과 Panaxytriol을 합성하였고, ACAT IC_(50)을 측정한 결과 각각 16.7㎍/㎖, 22.6㎍/㎖를 나타내었다.;Acyl-CoA : cholesterol acyltransferase (ACAT) is a key enzyme responsible for cholesterol ester formation in atherogenesis and cholesterol absorption from the intestines. ACAT inhibitors are regarded as potentially useful agents in the treatment of hypercholesterolemia and atherosclerosis. Although a wide variety of synthetic inhibitors of ACAT are now under clinical or preclinical evaluation, there are only a few ACAT inhibitors from microbial origin, for examples, purpactins, AS-183 and pyripyropenes. A large number of synthetic ACAT inhibitors have been reported. However, the inhibitors have not been used clinically because of various side effects including hepatic toxicity. Therefore, new types of ACAT inhibitors are highly demanded to develope as a hypolypidemic as well as antiatherosclerotic agent. In the course of searching ACAT inhibitors from natural sources, polyacetylenes were isolated from the extract of Panax ginseng roots, which were identified as Panaxynol, Panaxydol, Panaxydiol, Panaxydol-peroxide. These compounds inhibited ACAT with an IC_(50) of around 12-22.7μg/ml. In order to investigate the structure-activity relationships, Panaxydol derivatives were synthesized and tested for ACAT inhibitory activity. EHDO and Panaxytriol inhibited ACAT with an IC_(50) of 16.7--22.6 μg/ml These results suggest that Polyacetylenes in Panax ginseng would be used as antiatherosclerotic agents by inhibition of ACAT.
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