医学研究与教育
醫學研究與教育
의학연구여교육
MEDICAL RESEARCH AND EDUCATION
2013年
2期
8-11
,共4页
张仕国%马正月%申蕊%王伟华%杨更亮
張仕國%馬正月%申蕊%王偉華%楊更亮
장사국%마정월%신예%왕위화%양경량
硫色满酮%乙酰胆碱酯酶抑制剂%Mannich碱%阿尔茨海默症%动力学
硫色滿酮%乙酰膽堿酯酶抑製劑%Mannich堿%阿爾茨海默癥%動力學
류색만동%을선담감지매억제제%Mannich감%아이자해묵증%동역학
thiochromanones%acetylcholinesterase inhibitors%Mannich bases%Alzheimer’s disease%kinetics
目的研究6-氟硫色满酮Mannich碱对乙酰胆碱酯酶的抑制活性及作用类型.方法在体外采用Ellman方法对6-氟硫色满酮Mannich碱进行乙酰胆碱酯酶抑制实验和动力学实验.结果该化合物浓度为10-6mol/L时对乙酰胆碱酯酶的抑制率是51%,活性优于对照组利伐司替明,动力学实验初步证明是混合型竞争抑制.结论6-氟硫色满酮Mannich碱作为乙酰胆碱酯酶抑制剂具有进一步研究价值.
目的研究6-氟硫色滿酮Mannich堿對乙酰膽堿酯酶的抑製活性及作用類型.方法在體外採用Ellman方法對6-氟硫色滿酮Mannich堿進行乙酰膽堿酯酶抑製實驗和動力學實驗.結果該化閤物濃度為10-6mol/L時對乙酰膽堿酯酶的抑製率是51%,活性優于對照組利伐司替明,動力學實驗初步證明是混閤型競爭抑製.結論6-氟硫色滿酮Mannich堿作為乙酰膽堿酯酶抑製劑具有進一步研究價值.
목적연구6-불류색만동Mannich감대을선담감지매적억제활성급작용류형.방법재체외채용Ellman방법대6-불류색만동Mannich감진행을선담감지매억제실험화동역학실험.결과해화합물농도위10-6mol/L시대을선담감지매적억제솔시51%,활성우우대조조리벌사체명,동역학실험초보증명시혼합형경쟁억제.결론6-불류색만동Mannich감작위을선담감지매억제제구유진일보연구개치.
@@@@Objective To study the inhibition activity and kinetics style of 6-fluorothiochromanone Mannich bases to acetylcholinesterase. Methods The inhibition and kinetics tests of 6-fluorothiochromanone Mannich bases to acetylcholinesterase were carried out by Ellman methods in vitro. Results The inhibition ratio of acetylcholinesterase was 51% when the concentration of this compound was 10-6mol/L, its inhibitive activity was better than Rivastigmine and primary kinetics experiments proved to be a mixed type of inhibition. conclusion 6-fluorothiochromanones Mannich bases are worthy for further research in acetylcholinesterase inhibitors.