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2种新型ACAT酶抑制剂分析

Analysis of two novel ACAT enzyme inhibitors
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摘要 以药用昆虫斑蝥为材料,通过柱层析和高效液相色谱方法进行有效成分研究,结果从斑蝥中分离得到2种新型ACAT酶抑制剂。分子结构分析表明,化合物1是苯二甲酸(2-乙基庚基)酯,化合物2是邻苯二甲酸二环己酯。2种成分在人体ACAT酶1和人体ACAT酶2的抑制活性试验中表现出很强的抑制活性(1∶IC50=77.3μM,131.2μM和2∶IC50=9.6μM,6.6μM)。 Mylabris phalerate pallas was used for experimental material analysised through column chromatography and HPLC method.Two novel ACAT enzyme inhibitors were isolated from cantharidin.Molecular structure analysis showed that the first inhibitor was Bis(2-ethylheptyl)phthalate and the second inhibitor was Dicyclohexyl phthalate.Compounds 1and 2showed strong inhibitive activities in human ACAT1 and ACAT2inhibitive bioactivity test(1∶IC50=177.3μM,131.2μM and 2∶IC50=9.6μM,6.6μM).
作者 徐明哲
出处 《延边大学农学学报》 2015年第4期326-333,共8页 Agricultural Science Journal of Yanbian University
基金 国家自然科学基金资助项目(51269032)
关键词 斑蝥 ACAT酶抑制剂 邻苯二甲酸(2-乙基庚基)酯 邻苯二甲酸二环己酯 Mylabris phalerate pallas ACAT inhibitor Bis(2-ethylheptyl)phthalate Dicyclohexyl phthalate
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  • 1Chang TY, Chang CC, Cheng D. Acyl-coenzyme A:cholesterol acyltransferase.Annu Rev Biochem 1997, 66:613-638
  • 2Sturley SL. Molecular aspects of intracellular sterol esterification: The acyl coenzyme A:cholesterol acyltransferase reaction. Curt Opin Lipidol 1997, 8:167-173
  • 3Buhman KF, Accad M, Farese RV. Mammalian acyl-CoA:cholesterol acyltransferases. Biochim Biophys Acta 2000, 1529:142-154
  • 4Rudel LL, Lee RG, Cockman TL. Acyl coenzyme A:cholesterol acyltransferase types 1 and 2: Structure and function in atherosclerosis. Curr Opin Lipidol 2001, 12:121-127
  • 5Chang TY, Chang CC, Lin S, Yu C, Li BL, Miyazaki A. Roles of acyl-coenzyme A:cholesterol acyla'ansferase-1 and -2. Curt Opin Lipidol 2001, 12:289-296
  • 6Alegret M, Llaverias G, Silvestre JS. Acyl coenzyme A-cholesterol acyltransferase inhibitors as hypolipidemic and antiatherosclerotic drugs.Methods Find Exp Clin Pharmacol 2004, 26:563-586
  • 7Leon C, Hill JS, Wasan KM. Potential role of acyl-coenzyme A:cholesterol transferase (ACAT) inhibitors as hypolipidemic and antiatherosclerosis drugs.Pharm Res 2005, 22:1578-1588
  • 8Li BL, Chang TY, Chen J, Chang CC, Zhao XN. Human ACAT1 gene expression and its involvement in the development of atherosclerosis. Future Cardiology 2006, 2:93-99
  • 9Chang CC, Huh HY, Cadigan KM, Chang TY. Molecular cloning and functional expression of human acyl-coenzyme A:cholesterol acyltransferase cDNA in mutant Chinese hamster ovary cells. J Biol Chem 1993, 268:20747-20755
  • 10Miyazaki A, Sakashita N, Lee O, Takahashi K, Horiuchi S, Hakamata H,Morganelli PM et al. Expression of ACAT-1 protein in human atherosclerotic lesions and cultured human monocytes-macrophages. Arterioscler Thromb Vasc Biol 1998, 18:1568-1574

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