摘要：The characteristics of absorption, fluorescence, room temperature phosphorescence(RTP) spectra of meso tetrakis(4 N trimethylaminobenzyl)porphin(TAPP) and Palladium porphyrin(Pd TAPP) probe in the presence and absence of ct dna has been studied. Pd TAPP shows a very weak RTP emission in aqueous solution and strong RTP emission in the presence of dna. Maximum RTP was observed at pH=7, with maximum excitation and emission wavelengths at 414 nm and 684 nm, respectively. RTP decay follows a first order exponential equation, RTP lifetime (τ) of probe is (0.72±0.03) ms. The detection limit of ct dna may reach 8.8×10 -7 mol/L. The relative standard deviation(RSD) is less than ±6.6% in the linear range.

摘要：磺胺类药物是重要的化学治疗药物,设计合成新型的磺胺类药物是近年来研究的热点领域之一.以乙酰苯胺为起始原料,经过磺酰化、氨解、N-烷化等多步反应合成了一系列新型磺胺1,2,4-三唑类化合物,其结构经IR、1H NMR、13C NMR、MS和HRMS证实.体外考察了合成的磺胺三唑类化合物的抗细菌和抗真菌活性,结果表明所合成化合物的活性优于磺胺,且化合物普遍给出较好的抗大肠杆菌活性,特别是N-(4-(N-(2-(1H-1,2,4-三唑-1-基)乙基)-N-(3-氟苄基)磺酰氨基)苯基)乙酰胺(7b)显示较优的抗大肠杆菌活性(MIC=16?g/m L).此外,为了初步探讨化合物可能的抗微生物作用机制,利用紫外光谱法初步研究了强活性化合物7b与小牛胸腺dna的相互作用.研究表明化合物7b可能通过嵌入的方式与dna形成复合物进而发挥抗微生物效力.

摘要：由于极短的激发态寿命,钌(II)三联吡啶配合物对脱氧核糖核酸(dna)的光损伤能力低下.设计合成了三个钌(II)三联吡啶配合物[Ru(ttp)(tpy)]2+(1),[Ru(ttp-COOH)(tpy)]2+(2)和[Ru(ttp-COOH)(tpy-pyr)]2+(3),其中tpy为2,2':6',2"-三联吡啶,ttp为4′-(4-甲苯基)-2,2':6',2"-三联吡啶,ttp-COOH为4′-(4-羧基苯基)-2,2':6',2"-三联吡啶,tpy-pyr为4'-(1-芘基)-2,2':6',2"-三联吡啶.比较了TiO2纳米颗粒对它们光损伤小牛胸腺dna的影响.发现TiO2纳米颗粒在空气和氩气条件下均可显著提高配合物3光损伤dna的能力.TiO2纳米颗粒和配合物3间的光诱导电子转移作用及其该作用生成的钌(III)物种可能是促进配合物3对dna光损伤的主要原因.

摘要：设计并合成了天然产物喹叨啉(Quindoline)的两个衍生物:苯并呋喃[3,2-b]喹啉和5-N-甲基苯并呋喃[3,2-b]喹啉,通过MS、1H NMR等手段确认其结构。运用紫外(可见光谱、荧光光谱和圆二色光谱研究了合成的衍生物与小牛胸腺dna结合能力的强弱和结合方式。实验结果表明,5-N季铵化引入的正电荷能提高苯并呋喃喹啉衍生物与小牛胸腺dna的结合能力;圆二色光谱表明合成的衍生物是以嵌插方式与小牛胸腺dna相互作用。

摘要：表柔比星是临床上广泛用于治疗增殖很快肿瘤的药物.应用紫外、荧光、园二色、黏度、循环伏安等方法研究了表柔比星及表柔比星-Fe2+体系与dna的作用.结果发现,在pH=7.4时表柔比星可与Fe2+形成稳定体系,加入dna后表柔比星-Fe2+体系的紫外吸收明显降低.Scatchard图表明,表柔比星-Fe2+体系对溴化乙锭(EB)与dna的结合为竞争性抑制,同时此体系可使dna-EB体系荧光偏振度增大,使dna的热变性温度(tm)上升,黏度增大.循环伏安法表明,dna的加入使得表柔比星及表柔比星-Fe2+体系的式量电位正移.园二色谱法表明,随着表柔比星-Fe2+体系的加入,dna碱基间作用能迅速减弱.综合以上结果得出:表柔比星及表柔比星-Fe2+体系与dna之间均为嵌插作用,而且表柔比星-Fe2+体系具有比单纯表柔比星更好的嵌插效果.这些结果可为合理改善药效、降低抗癌药物毒性和设计新药提供依据.

摘要：碳点(carbon dots,CDs)在材料学及生物医学相关领域的研究已引起科研人员的广泛关注.本文采用一步水热法,制备了三种具有不同元素掺杂的CDs、N-CDs、N,S-CDs,并结合多种光谱法、熔链温度法和黏度法,系统地研究了三种不同元素掺杂的碳点与ctdna结合模式以及结合能力的差异.荧光实验证明三种不同性质的碳点CDs、N-CDs、N,S-CDs与ctdna的相互作用模式为沟槽结合,结合力主要为氢键和范德华力,并伴随着轻微的静电作用力.在强电解质和变性剂的存在下,会减弱碳点与ctdna之间的沟槽结合.圆二色光谱实验和红外光谱实验反映了碳点与ctdna的沟槽结合作用并不会明显改变ctdna的构象.与未掺杂的碳点(CDs)相比,氮硫元素的掺杂可使N,S-CDs与ctdna的沟槽结合能力减弱,但是加大碳点表面电荷,可增强N-CDs与ctdna的结合.这一结论为碳点的设计及其在生物医学领域中的应用提供了理论参考.

摘要：A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS *** the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution *** bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and *** combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive *** addition,the interaction of compound 5l with calf thymus dna demonstrated that this compound could effectively intercalate into dna to form a compound 5l-dna complex that might block dna replication and thereby exert good antimicrobial activity.