高等学校化学学报
高等學校化學學報
고등학교화학학보
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES
2014年
4期
831-838
,共8页
蒋建宏%李旭%肖圣雄%谷惠文%李传华%杨平%魏得良%何笃贵%李爱桃%李霞%姚飞虹%李强国
蔣建宏%李旭%肖聖雄%穀惠文%李傳華%楊平%魏得良%何篤貴%李愛桃%李霞%姚飛虹%李彊國
장건굉%리욱%초골웅%곡혜문%리전화%양평%위득량%하독귀%리애도%리하%요비홍%리강국
邻香草醛%甲氧苄氨嘧啶%热动力学参数%牛血清白蛋白%粟酒裂殖酵母细胞
鄰香草醛%甲氧芐氨嘧啶%熱動力學參數%牛血清白蛋白%粟酒裂殖酵母細胞
린향초철%갑양변안밀정%열동역학삼수%우혈청백단백%속주렬식효모세포
o-Vanillin%Trimethoprim%Thermokinetic property%Bovine serum albumin%S. pombe cell
用等摩尔的邻香草醛( C8 H8 O3)与甲氧苄胺嘧啶( C14 H18 N4 O3)反应,合成了一种新的化合物2-{[4-氨基-5-(3,4,5-三甲氧基-苄基)-嘧啶-2-亚胺基]-甲基}-6-甲氧基-苯酚(APYP).通过元素分析、核磁共振、摩尔电导、红外光谱和紫外光谱等手段对其进行了表征,其化学式为C22 H24 N4 O5.采用微量热法测定了APYP在301.15 K时对粟酒裂殖酵母细胞的生长代谢的产热曲线,计算得到了粟酒裂殖酵母细胞生长速率常数k,抑制率I 以及半抑制浓度IC50等热动力学参数.实验结果表明,随着APYP浓度的增加,粟酒裂殖酵母细胞的生长代谢速率常数k减小,抑制率I增加,半抑制浓度IC50为123.2 mg/L(或2.96×10-4 mol/L),即APYP对粟酒裂殖酵母细胞有抑制作用.同时利用荧光光谱和紫外光谱等方法研究了 APYP 与牛血清白蛋白( BSA)在接近生理条件下的相互作用,探讨了荧光猝灭机理,计算了反应的结合常数、结合位点、结合距离及热力学参数,研究了APYP与BSA之间的能量转移情况；并通过同步荧光光谱考察了APYP对BSA二级结构的影响.
用等摩爾的鄰香草醛( C8 H8 O3)與甲氧芐胺嘧啶( C14 H18 N4 O3)反應,閤成瞭一種新的化閤物2-{[4-氨基-5-(3,4,5-三甲氧基-芐基)-嘧啶-2-亞胺基]-甲基}-6-甲氧基-苯酚(APYP).通過元素分析、覈磁共振、摩爾電導、紅外光譜和紫外光譜等手段對其進行瞭錶徵,其化學式為C22 H24 N4 O5.採用微量熱法測定瞭APYP在301.15 K時對粟酒裂殖酵母細胞的生長代謝的產熱麯線,計算得到瞭粟酒裂殖酵母細胞生長速率常數k,抑製率I 以及半抑製濃度IC50等熱動力學參數.實驗結果錶明,隨著APYP濃度的增加,粟酒裂殖酵母細胞的生長代謝速率常數k減小,抑製率I增加,半抑製濃度IC50為123.2 mg/L(或2.96×10-4 mol/L),即APYP對粟酒裂殖酵母細胞有抑製作用.同時利用熒光光譜和紫外光譜等方法研究瞭 APYP 與牛血清白蛋白( BSA)在接近生理條件下的相互作用,探討瞭熒光猝滅機理,計算瞭反應的結閤常數、結閤位點、結閤距離及熱力學參數,研究瞭APYP與BSA之間的能量轉移情況；併通過同步熒光光譜攷察瞭APYP對BSA二級結構的影響.
용등마이적린향초철( C8 H8 O3)여갑양변알밀정( C14 H18 N4 O3)반응,합성료일충신적화합물2-{[4-안기-5-(3,4,5-삼갑양기-변기)-밀정-2-아알기]-갑기}-6-갑양기-분분(APYP).통과원소분석、핵자공진、마이전도、홍외광보화자외광보등수단대기진행료표정,기화학식위C22 H24 N4 O5.채용미량열법측정료APYP재301.15 K시대속주렬식효모세포적생장대사적산열곡선,계산득도료속주렬식효모세포생장속솔상수k,억제솔I 이급반억제농도IC50등열동역학삼수.실험결과표명,수착APYP농도적증가,속주렬식효모세포적생장대사속솔상수k감소,억제솔I증가,반억제농도IC50위123.2 mg/L(혹2.96×10-4 mol/L),즉APYP대속주렬식효모세포유억제작용.동시이용형광광보화자외광보등방법연구료 APYP 여우혈청백단백( BSA)재접근생리조건하적상호작용,탐토료형광졸멸궤리,계산료반응적결합상수、결합위점、결합거리급열역학삼수,연구료APYP여BSA지간적능량전이정황；병통과동보형광광보고찰료APYP대BSA이급결구적영향.
A new compound 2-{[4-amino-5-(3,4,5-trimethoxy-benzyl)-pyrimidin-2-ylimino]-methyl}-6-me-thoxy-phenol ( APYP ) was synthesized using equivalent moles of o-vanillin ( C8 H8 O3 ) and trimethoprim ( C14 H18 N4 O3 ) . Elemental analysis, molar conductivity, UV-Visual, IR and NMR spectroscopy were em-ployed to characterize the composition and structure of APYP. The analytical results showed that the molecular formula of the compound is C22 H24 N4 O5 . The thermokinetic properties of the action of APYP on growth meta-bolism of S. pombe were studied by a TAM air isothermal calorimeter at 301.15 K. The microbial growth rate constant( k) , inhibition ratio( I) and half inhibition concentration( IC50 ) were obtained. Experimental results show that the k values of S. pombe decreased and I values of S. pombe increased with the increase in the con-centrations of APYP and the IC50 value of APYP was found to be 123.20 mg/L. The APYP has good inhibition activity on the growth of S. pombe. Besides, fluorescence spectroscopy and UV-Vis absorption spectroscopy were employed to investigate the interactions of APYP with bovine serum albumin( BSA) under the approxima-tively physiological conditions. The binding constants, binding sites, binding distance, and the thermodynam-ic parameters were calculated. The energy transfer between the donor( BSA) and acceptor( APYP) was inves-tigated. Furthermore, synchronous fluorescence spectroscopy was used to investigate the structural change of BSA molecules with additions of APYP.
