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微量量热技术在医药筛选和检验中的应用

张有民, 王保怀   

  1. 北京大学物理化学研究所, 北京 100871
  • 收稿日期:1992-05-06 修回日期:1993-03-14 出版日期:1993-06-15 发布日期:1993-06-15

Application of Microcalorimetric Technique for the Screening and Examination of Medicines

You-Min Zhang, Bao-Huai Wang   

  1. Institute of Physical Chemistry, Beijing University, Beijing 100871
  • Received:1992-05-06 Revised:1993-03-14 Online:1993-06-15 Published:1993-06-15

摘要: 基于物质间相互作用时存在的热能效应, 几年来, 本文用MS-80标准型Calvet 微量量热计进行了一系列药物与人体细胞某些生物大分子相互作用的热动力学实验。这些实验包括: 1.抗癌药物(去甲斑蟊酸钠[ASN], 螺旋藻活性提取[Sp.P][Sp.S])以癌细胞(宫颈癌传代细胞[Hela])、人乳腺癌细胞[Bcap-37][MCF-7]、人胃癌细胞[SGc-7901])以及正常人体细胞(人体胚肺二倍体细胞[2BS])作用的热动力学研究; 2.具有抗单胺氧化酶活性的生物碱类药物(骆驼篷碱[HL]、去氢骆驼篷碱[HM])在水溶液中对小牛胸腺DNA 嵌插结合及其焓变的研究; 3.长效医药(长效避孕药-复方甲基炔诺酮[HQ])和缓释医药(康太克[Contac]-复方盐酸苯丙醇胺)与生理盐水(0.9%的氯化钠水溶液)作用的研究。所有的实验结果都给出了各自的特征热动力学图谱及相互作用的焓变。通过实验结果的分析和总结, 作者提出了将微量量热技术用于筛选和检验医药的新方法。文章中阐述了方法实施的科学依据, 同时简单叙述了实验的过程及操作, 并对实验结果进行了一些必要的讨论, 与其他筛选和检验医药的方法相比, 微量量热法有其明显的特点及优越性。

关键词: 抗癌药, 细胞, DNA, 温度自计曲线, 焓变

Abstract: According to the heating effect caused by interaction between matters, a series of experiments on the interaction between drugs and cells from human bodies, DNA and physiological saline have been carried out with a MS-80 standard Calvet microcalorimeter. The experiments include: (1) Thermokinetic studies of the effect of anticancer drugs [sodium norcantharidate (ASN), the bioactire materials (Sp.P and Sp.S) from algae etc.]on the cancer cells [Hela, human breast carcinoma (Bcap-37), human adenocarcinoma gastric cells (SGc-7901 and MCF-7) etc.] and the normal cells from human bodies [diploid fibroblasts from human fetal lung (2BS) etc.] at 310.15 K:(2) Studies of the in- tercalation binding of some alkaloidal drugs with the bioactivity to inhibit monoamine oxidase (harmalinc and harmine etc.) to call thymus DNA in neutral aqueous solution at 298.15 K:(3) Studies of the interaction between long acting drugs (long acting oral contraceptive-norgestrel etc.) and slowreleasing drug (Contac) and aqueous solution of 0.9% NaCl at 310.15 K. All the experimental results have given their characteristic thermograms and the interaction enthalpy changes. On the analysis of all the results, the authors put forward a method on application of microcalorimetric technique for screening and examination of medicines. The principle of application and the experimental operation of this method have been expounded, and some results of the above experiments have been discussed. As one of the methods for screening and examining medicines, the microcalorimctric method has some distinguished features and advantages over other methods.

Key words: Anticancer drug, Cell, DNA, Thermogram, Enthalpy change

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